Purchasability


Ligand source activities (1 row/activity)

Select all ChEMBL ID Receptor Species Purchasable p-value
(-log)		 Activity
Type		 Activity
Relation		 Activity
Value		 Unit Assay Type Assay Description Mol
weight		 Rot
Bonds		 H don H acc LogP Smiles
CHEMBL18661 hrh3_human Human Yes 10.4 EC50 = 0.0 nM Funct
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
165 2 2 2 1.0 N1CCC(CC1)Cc1[nH]cnc1
CHEMBL19010 hrh3_human Human Yes 10.3 EC50 = 0.1 nM Funct
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
342 6 1 2 3.2 Ic1ccc(cc1)COCCCc1cnc[nH]1
CHEMBL19439 hrh3_human Human Yes 10.2 EC50 = 0.1 nM Funct
Agonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assayAgonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assay
170 3 3 3 0.6 NC(=N)SCCc1cnc[nH]1
CHEMBL19439 hrh3_human Human Yes 10.1 EC50 = 0.1 nM Funct
Agonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assayAgonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assay
170 3 3 3 0.6 NC(=N)SCCc1cnc[nH]1
CHEMBL4159570 hrh3_human Human No 10.0 EC50 = 0.1 nM Funct
Agonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assayAgonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assay
500 7 1 5 5.0 COc1cc(N2C(=O)/C(=C\c3ccccc3)C2(C(=O)NC(C)(C)C)c2ccccc2)cc(OC)c1OC
CHEMBL4170869 hrh3_human Human No 10.0 EC50 = 0.1 nM Funct
Agonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assayAgonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assay
520 6 1 3 5.9 COc1ccc(N2C(=O)/C(=C\c3ccccc3)C2(C(=O)NC2CCCCC2)c2cc(F)c(F)c(F)c2)cc1
CHEMBL4441731 hrh3_mouse Mouse Yes 10.0 EC50 = 0.1 nM Funct
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
207 4 2 5 0.2 CCCNC1CN(c2ccnc(N)n2)C1
CHEMBL4596734 hrh3_mouse Mouse Yes 10.0 EC50 = 0.1 nM Funct
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
207 4 2 5 0.2 CCCNC1CN(c2ccnc(N)n2)C1
CHEMBL4159570 hrh3_human Human No 9.9 EC50 = 0.1 nM Funct
Agonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assayAgonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assay
500 7 1 5 5.0 COc1cc(N2C(=O)/C(=C\c3ccccc3)C2(C(=O)NC(C)(C)C)c2ccccc2)cc(OC)c1OC
CHEMBL322988 hrh3_human Human Yes 9.9 EC50 = 0.1 nM Funct
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
125 2 2 2 0.5 CC(CN)c1cnc[nH]1
CHEMBL19439 hrh3_human Human Yes 9.9 EC50 = 0.1 nM Funct
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
170 3 3 3 0.6 NC(=N)SCCc1cnc[nH]1
CHEMBL18661 hrh3_human Human Yes 9.9 EC50 = 0.1 nM Funct
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
165 2 2 2 1.0 N1CCC(CC1)Cc1[nH]cnc1
CHEMBL4170869 hrh3_human Human No 9.9 EC50 = 0.1 nM Funct
Agonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assayAgonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assay
520 6 1 3 5.9 COc1ccc(N2C(=O)/C(=C\c3ccccc3)C2(C(=O)NC2CCCCC2)c2cc(F)c(F)c(F)c2)cc1
CHEMBL18661 hrh3_human Human Yes 9.9 EC50 = 0.1 nM Bind
Inhibition of the cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H3 receptorInhibition of the cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H3 receptor
165 2 2 2 1.0 N1CCC(CC1)Cc1[nH]cnc1
CHEMBL18661 hrh3_human Human Yes 9.9 EC50 = 0.1 nM Bind
Inhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H3 receptorInhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H3 receptor
165 2 2 2 1.0 N1CCC(CC1)Cc1[nH]cnc1
CHEMBL82298 hrh3_human Human Yes 9.8 EC50 = 0.2 nM Funct
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
159 2 1 2 1.4 n1ccc(cc1)Cc1c[nH]cn1
CHEMBL82298 hrh3_human Human Yes 9.7 EC50 = 0.2 nM Bind
Inhibition of the cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H3 receptorInhibition of the cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H3 receptor
159 2 1 2 1.4 n1ccc(cc1)Cc1c[nH]cn1
CHEMBL82298 hrh3_human Human Yes 9.7 EC50 = 0.2 nM Funct
Agonist activity at human histamine H3 receptor assessed as beta galactosidase activityAgonist activity at human histamine H3 receptor assessed as beta galactosidase activity
159 2 1 2 1.4 n1ccc(cc1)Cc1c[nH]cn1
CHEMBL425994 hrh3_human Human No 9.7 EC50 = 0.2 nM Funct
Inverse agonist activity at human histamine H3 receptor by GTP gammaS assayInverse agonist activity at human histamine H3 receptor by GTP gammaS assay
419 9 1 6 4.7 CN(C)Cc1cc(OCCCN2CCCCC2)ccc1Nc1ncnc2ccccc12
CHEMBL1172579 hrh3_human Human No 9.7 EC50 = 0.2 nM Funct
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
309 3 1 2 3.9 FC(F)(F)c1cccc(N2CCC(Cc3c[nH]cn3)CC2)c1
CHEMBL112084 hrh3_rat Rat No 9.7 EC50 = 0.2 nM Bind
In vitro intrinsic activity against histamine H3 receptor from synaptosomes of rat cerebral cortexIn vitro intrinsic activity against histamine H3 receptor from synaptosomes of rat cerebral cortex
196 7 1 2 2.4 CC(C)CCOCCCc1c[nH]cn1
CHEMBL2145444 hrh3_rat Rat No 9.7 EC50 = 0.2 nM Bind
In vitro intrinsic activity against histamine H3 receptor from synaptosomes of rat cerebral cortexIn vitro intrinsic activity against histamine H3 receptor from synaptosomes of rat cerebral cortex
196 7 1 2 2.4 CC(C)CCOCCCc1c[nH]cn1
CHEMBL1185581 hrh3_rat Rat No 9.6 EC50 = 0.3 nM Bind
In vitro intrinsic activity against histamine H3 receptor from synaptosomes of rat cerebral cortexIn vitro intrinsic activity against histamine H3 receptor from synaptosomes of rat cerebral cortex
210 8 1 2 2.8 CC(C)CCCOCCCc1c[nH]cn1
CHEMBL2145442 hrh3_rat Rat No 9.6 EC50 = 0.3 nM Bind
In vitro intrinsic activity against histamine H3 receptor from synaptosomes of rat cerebral cortexIn vitro intrinsic activity against histamine H3 receptor from synaptosomes of rat cerebral cortex
210 8 1 2 2.8 CC(C)CCCOCCCc1c[nH]cn1
CHEMBL4159472 hrh3_human Human No 9.6 EC50 = 0.3 nM Funct
Agonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assayAgonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assay
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
CHEMBL4177416 hrh3_human Human No 9.6 EC50 = 0.3 nM Funct
Agonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assayAgonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assay
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
CHEMBL4159472 hrh3_human Human No 9.5 EC50 = 0.3 nM Funct
Agonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assayAgonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assay
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
CHEMBL4177416 hrh3_human Human No 9.5 EC50 = 0.3 nM Funct
Agonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assayAgonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assay
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
CHEMBL4441731 hrh3_human Human Yes 9.5 EC50 = 0.3 nM Funct
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
207 4 2 5 0.2 CCCNC1CN(c2ccnc(N)n2)C1
CHEMBL4596734 hrh3_human Human Yes 9.5 EC50 = 0.3 nM Funct
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
207 4 2 5 0.2 CCCNC1CN(c2ccnc(N)n2)C1
CHEMBL175782 hrh3_human Human Yes 9.5 EC50 = 0.3 nM Funct
Agonist activity at human histamine H3 receptor assessed as beta galactosidase activityAgonist activity at human histamine H3 receptor assessed as beta galactosidase activity
179 2 1 2 1.3 CN1CCC(CC1)Cc1[nH]cnc1
CHEMBL268229 hrh3_human Human Yes 9.5 EC50 = 0.3 nM Funct
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
125 2 2 2 0.3 C[C@H](Cc1cnc[nH]1)N
CHEMBL175782 hrh3_human Human Yes 9.5 EC50 = 0.3 nM Funct
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
179 2 1 2 1.3 CN1CCC(CC1)Cc1[nH]cnc1
CHEMBL175782 hrh3_human Human Yes 9.5 EC50 = 0.3 nM Funct
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
179 2 1 2 1.3 CN1CCC(CC1)Cc1[nH]cnc1
CHEMBL153051 hrh3_human Human Yes 9.4 EC50 = 0.4 nM Bind
Inhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H3 receptorInhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H3 receptor
151 2 2 2 0.6 c1nc(C[C@@H]2CCNC2)c[nH]1
CHEMBL268490 hrh3_human Human Yes 9.4 EC50 = 0.4 nM Funct
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
125 3 2 2 0.2 CNCCc1cnc[nH]1
CHEMBL1632409 hrh3_human Human No 9.4 EC50 = 0.4 nM Funct
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
322 7 3 3 3.8 N=C(NCc1ccc(Cl)cc1)SCCCCc1c[nH]cn1
CHEMBL3121095 hrh3_human Human No 9.4 EC50 = 0.4 nM Funct
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
339 4 1 4 2.6 O=C1NN=C(c2ccc(OC3CCN(C4CCC4)CC3)cc2)[C@H]2C[C@@H]12
CHEMBL3121096 hrh3_human Human No 9.3 EC50 = 0.5 nM Funct
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
339 4 1 4 2.6 O=C1NN=C(c2ccc(OC3CCN(C4CCC4)CC3)cc2)[C@@H]2C[C@H]12
CHEMBL281576 hrh3_human Human Yes 9.3 EC50 = 0.5 nM Funct
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
184 4 3 3 1.0 NC(=N)SCCCc1cnc[nH]1
CHEMBL110098 hrh3_rat Rat No 9.3 EC50 = 0.6 nM Bind
In vitro intrinsic activity against histamine H3 receptor from synaptosomes of rat cerebral cortexIn vitro intrinsic activity against histamine H3 receptor from synaptosomes of rat cerebral cortex
210 6 1 2 2.8 CC(C)(C)CCOCCCc1c[nH]cn1
CHEMBL2145443 hrh3_rat Rat No 9.3 EC50 = 0.6 nM Bind
In vitro intrinsic activity against histamine H3 receptor from synaptosomes of rat cerebral cortexIn vitro intrinsic activity against histamine H3 receptor from synaptosomes of rat cerebral cortex
210 6 1 2 2.8 CC(C)(C)CCOCCCc1c[nH]cn1
CHEMBL237394 hrh3_human Human No 9.2 EC50 = 0.6 nM Funct
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
442 7 0 7 4.6 CCOc1ccc(-n2ncc(-c3ccc4cc(CCN5CCC[C@H]5C)ccc4n3)c2C)nn1
CHEMBL237394 hrh3_human Human No 9.2 EC50 = 0.6 nM Funct
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
442 7 0 7 4.6 CCOc1ccc(-n2ncc(-c3ccc4cc(CCN5CCC[C@H]5C)ccc4n3)c2C)nn1
CHEMBL3417586 hrh3_human Human No 9.2 EC50 = 0.6 nM Funct
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
327 6 1 4 2.4 C[C@@H]1CCCN1CCCOc1ccc(C2=NNC(=O)[C@H]3C[C@@H]23)cc1
CHEMBL4535316 hrh3_human Human No 9.2 EC50 = 0.6 nM Funct
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
193 3 2 5 -0.1 CCNC1CN(c2ccnc(N)n2)C1
CHEMBL4598409 hrh3_human Human No 9.2 EC50 = 0.6 nM Funct
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
193 3 2 5 -0.1 CCNC1CN(c2ccnc(N)n2)C1
CHEMBL90019 hrh3_human Human Yes 9.2 EC50 = 0.6 nM Funct
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
139 4 2 2 0.7 NCCCCc1cnc[nH]1
CHEMBL3220120 hrh3_human Human No 9.2 EC50 = 0.6 nM Funct
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
328 4 0 4 3.6 CC1(C)COC(c2ccc(O[C@H]3C[C@H](N4CCCCC4)C3)cc2)=N1
CHEMBL18661 hrh3_human Human Yes 9.2 EC50 = 0.7 nM Funct
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
165 2 2 2 1.0 N1CCC(CC1)Cc1[nH]cnc1
CHEMBL18661 hrh3_human Human Yes 9.2 EC50 = 0.7 nM Funct
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
165 2 2 2 1.0 N1CCC(CC1)Cc1[nH]cnc1
CHEMBL268229 hrh3_human Human Yes 9.2 EC50 = 0.7 nM Bind
Inhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H3 receptorInhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H3 receptor
125 2 2 2 0.3 C[C@H](Cc1cnc[nH]1)N
CHEMBL1923729 hrh3_human Human No 9.2 EC50 = 0.7 nM Funct
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
326 6 0 4 3.3 C[C@@H]1CCCN1CCCOc1ccc(-c2ccc(=O)n(C)c2)cc1
CHEMBL3417585 hrh3_human Human No 9.2 EC50 = 0.7 nM Funct
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
327 6 1 4 2.4 C[C@@H]1CCCN1CCCOc1ccc(C2=NNC(=O)[C@@H]3C[C@H]23)cc1
CHEMBL3087669 hrh3_human Human No 9.2 EC50 = 0.7 nM Funct
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
382 4 1 5 3.9 Cc1cc(N2CC[C@H](N3CCC[C@@H]3C)C2)ccc1NC(=O)c1c(C)noc1C
CHEMBL1935100 hrh3_human Human No 9.2 EC50 = 0.7 nM Funct
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
315 6 1 4 2.6 C[C@@H]1CCCN1CCCOc1ccc(C2=NNC(=O)CC2)cc1
CHEMBL1935114 hrh3_human Human No 9.1 EC50 = 0.7 nM Funct
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
343 6 1 4 3.2 C[C@@H]1CCCN1CCCOc1ccc(C2=NNC(=O)C(C)(C)C2)cc1
CHEMBL237394 hrh3_rat Rat No 9.1 EC50 = 0.7 nM Funct
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
442 7 0 7 4.6 CCOc1ccc(-n2ncc(-c3ccc4cc(CCN5CCC[C@H]5C)ccc4n3)c2C)nn1
CHEMBL237394 hrh3_rat Rat No 9.1 EC50 = 0.7 nM Funct
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
442 7 0 7 4.6 CCOc1ccc(-n2ncc(-c3ccc4cc(CCN5CCC[C@H]5C)ccc4n3)c2C)nn1
CHEMBL1098230 hrh3_human Human No 9.1 EC50 = 0.8 nM Funct
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
260 4 1 2 4.0 CC(C)(C)c1ccc(SCCc2c[nH]cn2)cc1
CHEMBL1098230 hrh3_human Human No 9.1 EC50 = 0.8 nM Funct
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
260 4 1 2 4.0 CC(C)(C)c1ccc(SCCc2c[nH]cn2)cc1
CHEMBL1098230 hrh3_human Human No 9.1 EC50 = 0.8 nM Funct
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
260 4 1 2 4.0 CC(C)(C)c1ccc(SCCc2c[nH]cn2)cc1
CHEMBL237191 hrh3_human Human No 9.1 EC50 = 0.8 nM Funct
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
401 5 0 5 4.6 Cc1nc(N2CCCC2)ncc1-c1ccc2cc(CCN3CCC[C@H]3C)ccc2n1
CHEMBL237191 hrh3_human Human No 9.1 EC50 = 0.8 nM Funct
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
401 5 0 5 4.6 Cc1nc(N2CCCC2)ncc1-c1ccc2cc(CCN3CCC[C@H]3C)ccc2n1
CHEMBL4560428 hrh3_human Human No 9.1 EC50 = 0.8 nM Funct
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
221 5 2 5 0.6 CCCCNC1CN(c2ccnc(N)n2)C1
CHEMBL4594866 hrh3_human Human No 9.1 EC50 = 0.8 nM Funct
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
221 5 2 5 0.6 CCCCNC1CN(c2ccnc(N)n2)C1
CHEMBL1835782 hrh3_human Human No 9.1 EC50 = 0.8 nM Funct
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
367 6 0 5 3.2 C[C@@H]1CCCN1CCCOc1ccc(-c2nn(C)c(=O)c3c2CCC3)cc1
CHEMBL1835783 hrh3_human Human No 9.1 EC50 = 0.8 nM Funct
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
367 6 0 5 3.2 Cn1nc(-c2ccc(OCCCN3CCCCC3)cc2)c2c(c1=O)CCC2
CHEMBL1950743 hrh3_human Human No 9.1 EC50 = 0.8 nM Funct
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
355 4 1 4 3.3 CC1(C)CC(c2ccc(OC3CCN(C4CCC4)CC3)cc2)=NNC1=O
CHEMBL2441636 hrh3_human Human No 9.1 EC50 = 0.9 nM Funct
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
371 4 1 4 3.4 Cc1cc(N2CC[C@H](N3CCC[C@@H]3C)C2)ccc1NC(=O)C1CCOCC1
CHEMBL2036653 hrh3_human Human No 9.1 EC50 = 0.9 nM Funct
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
403 8 0 6 2.5 COC(=O)N1CCN(CC(=O)c2ccc(OCCCN3CCC[C@H]3C)cc2)CC1
CHEMBL19439 hrh3_rat Rat Yes 9.0 EC50 = 1 nM Bind
In vitro intrinsic activity against histamine H3 receptor from synaptosomes of rat cerebral cortexIn vitro intrinsic activity against histamine H3 receptor from synaptosomes of rat cerebral cortex
170 3 3 3 0.6 NC(=N)SCCc1cnc[nH]1
CHEMBL1813057 hrh3_human Human No 9.0 EC50 = 1 nM Funct
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
327 6 0 5 2.7 C[C@@H]1CCCN1CCCOc1ccc(-c2ccc(=O)n(C)n2)cc1
CHEMBL2036635 hrh3_human Human No 9.0 EC50 = 1 nM Funct
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
449 9 0 5 3.6 C[C@@H]1CCCN1CCCOc1ccc(C(=O)CN2CCN(C(=O)c3ccccc3)CC2)cc1
CHEMBL496616 hrh3_human Human No 9.0 EC50 = 1 nM Bind
Inverse agonist activity at human histamine H3 receptor expressed in CHO cells by GTPgamma[35S] binding assayInverse agonist activity at human histamine H3 receptor expressed in CHO cells by GTPgamma[35S] binding assay
371 4 2 4 2.6 CC(C)N1CCC(Oc2ccc3[nH]c(C(=O)N4CCC(O)C4)cc3c2)CC1
CHEMBL19439 hrh3_rat Rat Yes 9.0 EC50 = 1 nM Funct
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
170 3 3 3 0.6 NC(=N)SCCc1cnc[nH]1
CHEMBL4162793 hrh3_human Human No 9.0 EC50 = 1.1 nM Funct
Agonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assayAgonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assay
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
CHEMBL82298 hrh3_human Human Yes 9.0 EC50 = 1.1 nM Funct
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
159 2 1 2 1.4 n1ccc(cc1)Cc1c[nH]cn1
CHEMBL1172754 hrh3_human Human No 9.0 EC50 = 1.1 nM Funct
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
309 3 1 2 3.9 FC(F)(F)c1ccc(N2CCC(Cc3c[nH]cn3)CC2)cc1
CHEMBL1173809 hrh3_human Human No 9.0 EC50 = 1.1 nM Funct
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
259 3 1 2 3.0 Fc1ccc(N2CCC(Cc3c[nH]cn3)CC2)cc1
CHEMBL1945845 hrh3_human Human No 9.0 EC50 = 1.1 nM Funct
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
339 4 1 4 3.1 Cc1n[nH]c(=O)cc1-c1ccc(OC2CCN(C3CCC3)CC2)cc1
CHEMBL1813065 hrh3_human Human No 9.0 EC50 = 1.1 nM Funct
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
313 6 1 4 2.7 C[C@@H]1CCCN1CCCOc1ccc(-c2cn[nH]c(=O)c2)cc1
CHEMBL1829335 hrh3_human Human Yes 9.0 EC50 = 1.1 nM Funct
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
313 6 1 4 2.7 C[C@@H]1CCCN1CCCOc1ccc(-c2ccc(=O)[nH]n2)cc1
CHEMBL1950643 hrh3_human Human No 9.0 EC50 = 1.1 nM Funct
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
325 4 1 4 2.8 O=c1ccc(-c2ccc(OC3CCN(C4CCC4)CC3)cc2)n[nH]1
CHEMBL392573 hrh3_human Human No 9.0 EC50 = 1.1 nM Funct
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
385 4 0 5 4.6 Cc1cc2ncc(-c3ccc4cc(CCN5CCC[C@H]5C)ccc4n3)c(C)n2n1
CHEMBL4162793 hrh3_human Human No 9.0 EC50 = 1.1 nM Funct
Agonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assayAgonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assay
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
CHEMBL392573 hrh3_human Human No 9.0 EC50 = 1.1 nM Funct
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
385 4 0 5 4.6 Cc1cc2ncc(-c3ccc4cc(CCN5CCC[C@H]5C)ccc4n3)c(C)n2n1
CHEMBL4165989 hrh3_human Human No 8.9 EC50 = 1.2 nM Funct
Agonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assayAgonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assay
458 5 1 4 5.4 COc1ccc(NC2(c3ccc(F)cc3)C(=O)N(C(C)(C)C)C(=O)/C2=C/c2ccccc2)cc1
CHEMBL206000 hrh3_human Human Yes 8.9 EC50 = 1.3 nM Funct
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
167 5 1 2 1.3 CN(C)CCCCc1c[nH]cn1
CHEMBL4466700 hrh3_human Human No 8.9 EC50 = 1.3 nM Funct
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
179 2 2 5 -0.5 CNC1CN(c2ccnc(N)n2)C1
CHEMBL4594865 hrh3_human Human No 8.9 EC50 = 1.3 nM Funct
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
179 2 2 5 -0.5 CNC1CN(c2ccnc(N)n2)C1
CHEMBL4164467 hrh3_human Human No 8.9 EC50 = 1.3 nM Funct
Agonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assayAgonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assay
548 6 1 5 6.0 COc1ccc(NC2(c3ccc(Br)cc3)C(=O)N(C(C)(C)C)C(=O)/C2=C/c2ccccc2)cc1OC
CHEMBL351231 hrh3_human Human Yes 8.9 EC50 = 1.3 nM Funct
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
330 4 0 3 5.0 N#Cc1ccc(cc1)c1ccc2c(c1)cc(o2)CCN1CCC[C@H]1C
CHEMBL351231 hrh3_human Human Yes 8.9 EC50 = 1.3 nM Funct
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
330 4 0 3 5.0 N#Cc1ccc(cc1)c1ccc2c(c1)cc(o2)CCN1CCC[C@H]1C
CHEMBL4164467 hrh3_human Human No 8.9 EC50 = 1.3 nM Funct
Agonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assayAgonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assay
548 6 1 5 6.0 COc1ccc(NC2(c3ccc(Br)cc3)C(=O)N(C(C)(C)C)C(=O)/C2=C/c2ccccc2)cc1OC
CHEMBL4165989 hrh3_human Human No 8.9 EC50 = 1.3 nM Funct
Agonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assayAgonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assay
458 5 1 4 5.4 COc1ccc(NC2(c3ccc(F)cc3)C(=O)N(C(C)(C)C)C(=O)/C2=C/c2ccccc2)cc1
CHEMBL1829477 hrh3_human Human No 8.9 EC50 = 1.3 nM Funct
Antagonist activity at human histamine 3 receptor by [35S]GTPgammaS binding assayAntagonist activity at human histamine 3 receptor by [35S]GTPgammaS binding assay
345 6 0 5 2.8 C[C@@H]1CCCN1CCCOc1ccc(-c2ccc(=O)n(C)n2)cc1F
CHEMBL1950746 hrh3_human Human No 8.9 EC50 = 1.3 nM Funct
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
341 4 1 4 2.9 C[C@@H]1CC(=O)NN=C1c1ccc(OC2CCN(C3CCC3)CC2)cc1
CHEMBL1935111 hrh3_human Human No 8.9 EC50 = 1.3 nM Funct
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
329 6 1 4 2.8 CC1CC(=O)NN=C1c1ccc(OCCCN2CCC[C@H]2C)cc1
CHEMBL153061 hrh3_human Human Yes 8.9 EC50 = 1.3 nM Bind
Inhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H3 receptorInhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H3 receptor
151 2 2 2 0.6 c1nc(CC2CCNC2)c[nH]1
CHEMBL1935111 hrh3_human Human No 8.9 EC50 = 1.4 nM Funct
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
329 6 1 4 2.8 CC1CC(=O)NN=C1c1ccc(OCCCN2CCC[C@H]2C)cc1
CHEMBL393581 hrh3_human Human No 8.9 EC50 = 1.4 nM Funct
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
397 5 0 5 4.8 Cc1c(-c2ccc3cc(CCN4CCC[C@H]4C)ccc3n2)cnn1-c1ccccn1
CHEMBL471724 hrh3_human Human No 8.9 EC50 = 1.4 nM Bind
Agonist activity at human H3 receptor expressed in insect Sf9 cells co-expressing Gialpha2, Gbeta1gamma2 and RGS4 assessed as gamma[32P]GTP binding by liquid scintillation countingAgonist activity at human H3 receptor expressed in insect Sf9 cells co-expressing Gialpha2, Gbeta1gamma2 and RGS4 assessed as gamma[32P]GTP binding by liquid scintillation counting
237 5 3 2 0.4 CC(C)C(=O)/N=C(\N)NCCCc1c[nH]cn1
CHEMBL393581 hrh3_human Human No 8.9 EC50 = 1.4 nM Funct
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
397 5 0 5 4.8 Cc1c(-c2ccc3cc(CCN4CCC[C@H]4C)ccc3n2)cnn1-c1ccccn1
CHEMBL462605 hrh3_cavpo Guinea pig Yes 8.8 EC50 = 1.5 nM Funct
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
295 8 0 2 4.2 Clc1ccc(cc1)CCCOCCCN1CCCCC1
CHEMBL263101 hrh3_human Human No 8.8 EC50 = 1.6 nM Funct
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
382 4 0 4 5.2 Cc1nc2ncccc2cc1-c1ccc2cc(CCN3CCC[C@H]3C)ccc2n1
CHEMBL465170 hrh3_human Human No 8.8 EC50 = 1.6 nM Bind
Agonist activity at human H3 receptor expressed in insect Sf9 cells co-expressing Gialpha2, Gbeta1gamma2 and RGS4 assessed as gamma[32P]GTP binding by liquid scintillation countingAgonist activity at human H3 receptor expressed in insect Sf9 cells co-expressing Gialpha2, Gbeta1gamma2 and RGS4 assessed as gamma[32P]GTP binding by liquid scintillation counting
237 6 3 2 0.6 CCCC(=O)/N=C(\N)NCCCc1c[nH]cn1
CHEMBL475621 hrh3_human Human No 8.8 EC50 = 1.6 nM Bind
Agonist activity at human H3 receptor expressed in insect Sf9 cells co-expressing Gialpha2, Gbeta1gamma2 and RGS4 assessed as gamma[32P]GTP binding by liquid scintillation countingAgonist activity at human H3 receptor expressed in insect Sf9 cells co-expressing Gialpha2, Gbeta1gamma2 and RGS4 assessed as gamma[32P]GTP binding by liquid scintillation counting
223 5 3 2 0.2 CCC(=O)/N=C(\N)NCCCc1c[nH]cn1
CHEMBL263101 hrh3_human Human No 8.8 EC50 = 1.6 nM Funct
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
382 4 0 4 5.2 Cc1nc2ncccc2cc1-c1ccc2cc(CCN3CCC[C@H]3C)ccc2n1
CHEMBL3220124 hrh3_human Human No 8.8 EC50 = 1.6 nM Funct
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
383 8 0 5 4.6 c1cc(-c2nc(CN3CCCCC3)co2)ccc1OCCCN1CCCCC1
CHEMBL3220126 hrh3_human Human No 8.8 EC50 = 1.6 nM Funct
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
370 5 0 6 3.8 COC(=O)c1oc(-c2ccc(O[C@H]3C[C@H](N4CCCCC4)C3)cc2)nc1C
CHEMBL1096516 hrh3_human Human No 8.8 EC50 = 1.6 nM Funct
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
243 4 2 2 3.4 CC(C)(C)c1ccc(NCCc2c[nH]cn2)cc1
CHEMBL1173390 hrh3_human Human No 8.8 EC50 = 1.6 nM Funct
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
291 3 1 2 4.0 c1ccc2cc(N3CCC(Cc4c[nH]cn4)CC3)ccc2c1
CHEMBL1950747 hrh3_human Human No 8.8 EC50 = 1.6 nM Funct
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
341 4 1 4 2.9 C[C@H]1CC(=O)NN=C1c1ccc(OC2CCN(C3CCC3)CC2)cc1
CHEMBL502339 hrh3_human Human No 8.8 EC50 = 1.6 nM Bind
Activity at human recombinant histamine H3 receptor expressed in Sf9 cells coexpressing Galphai, G-beta-1-gamma-2 and RGS4 by steady-state GTPase activity assayActivity at human recombinant histamine H3 receptor expressed in Sf9 cells coexpressing Galphai, G-beta-1-gamma-2 and RGS4 by steady-state GTPase activity assay
319 7 4 4 2.2 CC(CC(=O)NC(=N)NCCCc1c[nH]cn1)c1cccs1
CHEMBL4635634 hrh3_human Human No 8.8 EC50 = 1.7 nM Funct
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
401 9 1 2 5.1 Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCCCc1c[nH]cn1
CHEMBL4650570 hrh3_human Human No 8.8 EC50 = 1.7 nM Funct
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
401 9 1 2 5.1 Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCCCc1c[nH]cn1
CHEMBL1169687 hrh3_human Human No 8.8 EC50 = 1.7 nM Funct
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
270 4 2 3 2.9 CNc1ccc(N2CCC(Cc3c[nH]cn3)CC2)cc1
CHEMBL2031470 hrh3_human Human No 8.8 EC50 = 1.7 nM Funct
Inverse agonist activity at human H3 receptor by [35S]GTPgamma binding assayInverse agonist activity at human H3 receptor by [35S]GTPgamma binding assay
353 5 0 5 2.8 C[C@@H]1CCCN1CCCOc1ccc2c(c1)CCc1cc(=O)n(C)nc1-2
CHEMBL14690 hrh3_mouse Mouse Yes 8.8 EC50 = 1.7 nM Funct
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
308 6 2 3 3.2 Clc1ccc(cc1)CN=C(SCCCc1cnc[nH]1)N
CHEMBL2165642 hrh3_human Human No 8.8 EC50 = 1.8 nM Funct
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
500 17 6 4 1.7 N/C(=N\C(=O)CCCCCCCCC(=O)/N=C(\N)NCCCc1c[nH]cn1)NCCCc1c[nH]cn1
CHEMBL2036643 hrh3_human Human No 8.7 EC50 = 1.8 nM Funct
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
380 8 0 4 3.9 C[C@@H]1CCCN1CCCOc1ccc(C(=O)CN2CCC(F)(F)CC2)cc1
CHEMBL1096429 hrh3_human Human No 8.7 EC50 = 1.9 nM Bind
Activity at human recombinant histamine H3 receptor expressed in Sf9 cells coexpressing Galphai, Gbeta1gamma2 and RGS4 by steady-state GTPase activity assayActivity at human recombinant histamine H3 receptor expressed in Sf9 cells coexpressing Galphai, Gbeta1gamma2 and RGS4 by steady-state GTPase activity assay
313 7 4 3 2.2 C[C@@H](CC(=O)NC(=N)NCCCc1c[nH]cn1)c1ccccc1
CHEMBL19439 hrh3_human Human Yes 8.7 EC50 = 1.9 nM Bind
Inhibition of human Histamine H3 receptor using [3H]N-alpha-methyl histamineInhibition of human Histamine H3 receptor using [3H]N-alpha-methyl histamine
170 3 3 3 0.6 NC(=N)SCCc1cnc[nH]1
CHEMBL4516714 hrh3_human Human No 8.7 EC50 = 2.0 nM Funct
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
221 4 2 5 0.6 CCC(C)NC1CN(c2ccnc(N)n2)C1
CHEMBL4595102 hrh3_human Human No 8.7 EC50 = 2.0 nM Funct
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
221 4 2 5 0.6 CCC(C)NC1CN(c2ccnc(N)n2)C1
CHEMBL494982 hrh3_human Human No 8.7 EC50 = 2.0 nM Funct
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
283 3 1 3 3.3 CC1CC(C)(C)N=C(c2cccc(Cc3c[nH]cn3)c2)O1
CHEMBL442242 hrh3_human Human No 8.7 EC50 = 2.0 nM Funct
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
334 4 0 4 4.0 Cc1nn(C)cc1-c1ccc2cc(CCN3CCC[C@H]3C)ccc2n1
CHEMBL3220122 hrh3_human Human No 8.7 EC50 = 2.0 nM Funct
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
368 4 0 4 4.6 c1cc(C2=NC3(CCCCC3)CO2)ccc1O[C@H]1C[C@H](N2CCCCC2)C1
CHEMBL381074 hrh3_human Human No 8.0 EC50 = 10 nM Funct
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
195 8 2 2 2.1 CCCNCCCCCc1c[nH]cn1
CHEMBL4174591 hrh3_human Human No 8.0 EC50 = 10 nM Funct
Agonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assayAgonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assay
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
CHEMBL4468740 hrh3_human Human No 8.0 EC50 = 10 nM Funct
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
193 2 2 5 -0.2 CNC1CN(c2cc(C)nc(N)n2)C1
CHEMBL4595912 hrh3_human Human No 8.0 EC50 = 10 nM Funct
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
193 2 2 5 -0.2 CNC1CN(c2cc(C)nc(N)n2)C1
CHEMBL11919 hrh3_human Human Yes 8.0 EC50 = 10 nM Funct
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
125 2 2 2 0.3 C[C@@H](Cc1cnc[nH]1)N
CHEMBL60716 hrh3_human Human Yes 8.0 EC50 = 10 nM Bind
Inhibition of human Histamine H3 receptor using [3H]N-alpha-methyl histamineInhibition of human Histamine H3 receptor using [3H]N-alpha-methyl histamine
151 3 2 2 0.9 NCC[C@@H]1C[C@@H]1c1c[nH]cn1
CHEMBL4174591 hrh3_human Human No 8.0 EC50 = 10.2 nM Funct
Agonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assayAgonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assay
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
CHEMBL2031874 hrh3_human Human No 8.0 EC50 = 10.7 nM Bind
Inverse agonist activity at human H3 receptor expressed in HEK293T cells assessed as inhibition of {35S]GTPgamma bindingInverse agonist activity at human H3 receptor expressed in HEK293T cells assessed as inhibition of {35S]GTPgamma binding
391 5 0 3 3.2 CN(C)C(=O)c1ccc(-c2ccc3c(c2)CCN(CCN2CCCC2)C3=O)cc1
CHEMBL474617 hrh3_human Human No 8.0 EC50 = 11.0 nM Bind
Agonist activity at human H3 receptor expressed in insect Sf9 cells co-expressing Gialpha2, Gbeta1gamma2 and RGS4 assessed as gamma[32P]GTP binding by liquid scintillation countingAgonist activity at human H3 receptor expressed in insect Sf9 cells co-expressing Gialpha2, Gbeta1gamma2 and RGS4 assessed as gamma[32P]GTP binding by liquid scintillation counting
395 8 4 3 1.4 CN(CCC(=O)/N=C(\N)NCCCc1c[nH]cn1)C(=O)c1cc2ccccc2[nH]1
CHEMBL4519616 hrh3_human Human No 7.0 EC50 = 100 nM Funct
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
235 3 1 5 0.9 CC(C)c1cc(N2CC(N(C)C)C2)nc(N)n1
CHEMBL105803 hrh3_human Human No 7.0 EC50 = 100 nM Funct
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
258 5 1 3 2.8 c1ccc(COC[C@H]2CC[C@H](c3c[nH]cn3)O2)cc1
CHEMBL106931 hrh3_human Human Yes 7.0 EC50 = 100 nM Funct
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
167 2 2 3 0.6 NC[C@@H]1CC[C@@H](c2c[nH]cn2)O1
CHEMBL260374 hrh3_human Human Yes 7.0 EC50 = 100 nM Funct
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
292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1
CHEMBL129198 hrh3_human Human Yes 6.0 EC50 = 1000 nM Bind
Effective concentration required against human histamine H3 receptor was determined by the inhibition of the cAMP stimulated beta-galactosidase transcription in SK-N-MC cellsEffective concentration required against human histamine H3 receptor was determined by the inhibition of the cAMP stimulated beta-galactosidase transcription in SK-N-MC cells
277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl
CHEMBL186456 hrh3_human Human No 6.0 EC50 = 1000 nM Bind
Effective concentration required against human histamine H3 receptor was determined by the inhibition of the cAMP stimulated beta-galactosidase transcription in SK-N-MC cellsEffective concentration required against human histamine H3 receptor was determined by the inhibition of the cAMP stimulated beta-galactosidase transcription in SK-N-MC cells
276 2 1 2 3.3 CN1CCC(C(=O)c2cc3cc(Cl)ccc3[nH]2)CC1
CHEMBL362163 hrh3_human Human No 6.0 EC50 = 1000 nM Bind
Effective concentration required against human histamine H3 receptor was determined by the inhibition of the cAMP stimulated beta-galactosidase transcription in SK-N-MC cellsEffective concentration required against human histamine H3 receptor was determined by the inhibition of the cAMP stimulated beta-galactosidase transcription in SK-N-MC cells
278 2 2 2 3.2 CN1CCC(C(O)c2cc3cc(Cl)ccc3[nH]2)CC1
CHEMBL106158 hrh3_human Human No 5.0 EC50 = 10000 nM Funct
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
248 3 3 4 0.3 C/N=C(\NC#N)NC[C@@H]1CC[C@H](c2c[nH]cn2)O1
CHEMBL1632410 hrh3_human Human No 5.0 EC50 = 10000 nM Funct
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
258 5 1 3 2.8 c1ccc(COC[C@H]2CC[C@@H](c3c[nH]cn3)O2)cc1
CHEMBL322256 hrh3_human Human No 5.0 EC50 = 10000 nM Funct
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
258 5 1 3 2.8 c1ccc(COC[C@@H]2CC[C@@H](c3c[nH]cn3)O2)cc1
CHEMBL106158 hrh3_human Human No 5.0 EC50 = 10232.9 nM Funct
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
248 3 3 4 0.3 C/N=C(\NC#N)NC[C@@H]1CC[C@H](c2c[nH]cn2)O1
CHEMBL4166645 hrh3_human Human No 7.0 EC50 = 104 nM Funct
Agonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assayAgonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assay
486 5 1 3 5.2 O=C1C=CC2(C=C1)C(c1ccccc1)=CC(=O)N2C(C(=O)NC1CCCCC1)c1ccc(Cl)cc1
CHEMBL4167482 hrh3_human Human No 7.0 EC50 = 104 nM Funct
Agonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assayAgonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assay
544 8 1 5 5.6 COc1cc(N2C(=O)/C(=C\c3ccccc3)C2(C(=O)NC2CCCCC2)c2ccc(F)cc2)cc(OC)c1OC
CHEMBL4166645 hrh3_human Human No 7.0 EC50 = 104.7 nM Funct
Agonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assayAgonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assay
486 5 1 3 5.2 O=C1C=CC2(C=C1)C(c1ccccc1)=CC(=O)N2C(C(=O)NC1CCCCC1)c1ccc(Cl)cc1
CHEMBL106931 hrh3_human Human Yes 7.0 EC50 = 104.7 nM Funct
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
167 2 2 3 0.6 NC[C@@H]1CC[C@@H](c2c[nH]cn2)O1
CHEMBL3220641 hrh3_human Human No 6.0 EC50 = 1071.5 nM Funct
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
234 5 3 3 0.7 CN/C(=N/C#N)NCCCCc1nc[nH]c1C
CHEMBL503070 hrh3_human Human No 8.0 EC50 = 11 nM Bind
Inverse agonist activity at human histamine H3 receptor expressed in CHO cells by GTPgamma[35S] binding assayInverse agonist activity at human histamine H3 receptor expressed in CHO cells by GTPgamma[35S] binding assay
563 6 0 6 5.1 CC(C)N1CCC(Oc2ccc3c(c2)cc(C(=O)N2CCC(F)(F)CC2)n3S(=O)(=O)c2ccc(F)cc2)CC1
CHEMBL260374 hrh3_mouse Mouse Yes 8.0 EC50 = 11 nM Funct
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
292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1
CHEMBL497632 hrh3_human Human No 7.0 EC50 = 112 nM Bind
Inverse agonist activity at human histamine H3 receptor expressed in CHO cells by GTPgamma[35S] binding assayInverse agonist activity at human histamine H3 receptor expressed in CHO cells by GTPgamma[35S] binding assay
389 4 1 4 3.0 CC(C)N1CCC(Oc2cc3[nH]c(C(=O)N4CCOCC4)cc3cc2F)CC1
CHEMBL1082296 hrh3_human Human No 6.9 EC50 = 119 nM Bind
Displacement of [125H]iodoproxyphan from human recombinant histamine H3 receptor expressed in human SK-N-MC cellsDisplacement of [125H]iodoproxyphan from human recombinant histamine H3 receptor expressed in human SK-N-MC cells
422 6 2 4 4.4 Cc1cc(OCCCN2C[C@H]3CCCN[C@H]3C2)ccc1-c1nc2c(C)c(F)ccc2[nH]1
CHEMBL1172712 hrh3_human Human No 7.9 EC50 = 12 nM Funct
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
283 4 1 2 4.0 CC(C)c1ccc(N2CCC(Cc3c[nH]cn3)CC2)cc1
CHEMBL1257487 hrh3_human Human No 7.9 EC50 = 12 nM Funct
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
418 5 0 5 3.9 CC(C)N1CCC(Oc2ccc3c(c2)cc2n3CCN(Cc3ccncc3)C2=O)CC1
CHEMBL4469111 hrh3_human Human No 7.9 EC50 = 12.6 nM Funct
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
207 3 2 5 0.2 CCNC1CN(c2cc(C)nc(N)n2)C1
CHEMBL4470781 hrh3_human Human No 7.9 EC50 = 12.6 nM Funct
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
221 3 2 5 0.6 CNC1CN(c2cc(C(C)C)nc(N)n2)C1
CHEMBL150701 hrh3_human Human Yes 7.9 EC50 = 12.6 nM Funct
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
179 3 2 2 1.3 c1nc(CCC2CCNCC2)c[nH]1
CHEMBL90 hrh3_human Human Yes 7.9 EC50 = 12.9 nM Bind
Activity at human recombinant histamine H3 receptor expressed in Sf9 cells coexpressing Galphai, Gbeta1gamma2 and RGS4 by steady-state GTPase activity assayActivity at human recombinant histamine H3 receptor expressed in Sf9 cells coexpressing Galphai, Gbeta1gamma2 and RGS4 by steady-state GTPase activity assay
111 2 2 2 -0.1 NCCc1cnc[nH]1
CHEMBL90 hrh3_human Human Yes 7.9 EC50 = 12.9 nM Funct
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
111 2 2 2 -0.1 NCCc1cnc[nH]1
CHEMBL275443 hrh3_human Human Yes 4.9 EC50 = 12400 nM Funct
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
125 2 2 2 0.2 Cc1c(CCN)nc[nH]1
CHEMBL4458116 hrh3_human Human No 6.9 EC50 = 125.9 nM Funct
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
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
CHEMBL112084 hrh3_rat Rat No 6.9 EC50 = 128 nM Bind
In vitro binding affinity against histamine H3 receptor from synaptosomes of rat cerebral cortexIn vitro binding affinity against histamine H3 receptor from synaptosomes of rat cerebral cortex
196 7 1 2 2.4 CC(C)CCOCCCc1c[nH]cn1
CHEMBL2145444 hrh3_rat Rat No 6.9 EC50 = 128 nM Bind
In vitro binding affinity against histamine H3 receptor from synaptosomes of rat cerebral cortexIn vitro binding affinity against histamine H3 receptor from synaptosomes of rat cerebral cortex
196 7 1 2 2.4 CC(C)CCOCCCc1c[nH]cn1
CHEMBL4161732 hrh3_human Human No 7.9 EC50 = 13 nM Funct
Agonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assayAgonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assay
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
CHEMBL90 hrh3_human Human Yes 7.9 EC50 = 13 nM Funct
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
111 2 2 2 -0.1 NCCc1cnc[nH]1
CHEMBL1257486 hrh3_human Human No 7.9 EC50 = 13 nM Funct
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
418 5 0 5 3.9 CC(C)N1CCC(Oc2ccc3c(c2)cc2n3CCN(Cc3cccnc3)C2=O)CC1
CHEMBL150701 hrh3_human Human Yes 7.9 EC50 = 13.2 nM Bind
Inhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H3 receptorInhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H3 receptor
179 3 2 2 1.3 c1nc(CCC2CCNCC2)c[nH]1
CHEMBL4161732 hrh3_human Human No 7.9 EC50 = 13.5 nM Funct
Agonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assayAgonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assay
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
CHEMBL81644 hrh3_human Human Yes 5.9 EC50 = 1300 nM Funct
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
159 2 1 2 1.4 c1ccc(Cc2c[nH]cn2)nc1
CHEMBL310360 hrh3_human Human Yes 5.9 EC50 = 1349.0 nM Bind
Inhibition of the cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H3 receptorInhibition of the cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H3 receptor
173 3 1 2 1.6 c1ccc(CCc2c[nH]cn2)nc1
CHEMBL1179608 hrh3_human Human No 6.9 EC50 = 135 nM Funct
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
164 5 1 2 1.0 C#CCOCCCc1c[nH]cn1
CHEMBL88958 hrh3_human Human No 6.9 EC50 = 135 nM Funct
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
164 5 1 2 1.0 C#CCOCCCc1c[nH]cn1
CHEMBL1257376 hrh3_human Human No 7.9 EC50 = 14 nM Funct
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
435 5 0 4 4.7 CC(C)N1CCC(Oc2ccc3c(c2)cc2n3CCN(Cc3ccc(F)cc3)C2=O)CC1
CHEMBL1257377 hrh3_human Human No 7.9 EC50 = 14 nM Funct
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
418 5 0 5 3.9 CC(C)N1CCC(Oc2ccc3c(c2)cc2n3CCN(Cc3ccccn3)C2=O)CC1
CHEMBL1257850 hrh3_human Human No 7.9 EC50 = 14 nM Funct
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
341 3 1 4 3.0 CC(C)N1CCC(Oc2ccc3c(c2)cc2n3C[C@H](C)NC2=O)CC1
CHEMBL4169663 hrh3_human Human No 7.8 EC50 = 14.4 nM Funct
Agonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assayAgonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assay
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
CHEMBL4169663 hrh3_human Human No 7.8 EC50 = 14.5 nM Funct
Agonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assayAgonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assay
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
CHEMBL1243367 hrh3_human Human No 6.9 EC50 = 140 nM Funct
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
349 5 1 3 4.7 FC(F)(F)c1ccc(SCC(c2ccncc2)c2c[nH]cn2)cc1
CHEMBL1243393 hrh3_human Human No 6.9 EC50 = 140 nM Funct
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
337 5 1 3 5.0 CC(C)(C)c1ccc(SCC(c2ccncc2)c2c[nH]cn2)cc1
CHEMBL78838 hrh3_human Human Yes 6.9 EC50 = 140 nM Funct
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
159 2 1 2 1.4 c1cncc(Cc2c[nH]cn2)c1
CHEMBL1258194 hrh3_human Human No 6.9 EC50 = 140 nM Funct
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
327 5 1 4 2.6 C[C@H]1CCCN1CCCOc1ccc2c(c1)cc1n2CCNC1=O
CHEMBL418470 hrh3_human Human Yes 5.9 EC50 = 1410 nM Bind
Inhibition of human Histamine H3 receptor using [3H]N-alpha-methyl histamineInhibition of human Histamine H3 receptor using [3H]N-alpha-methyl histamine
151 3 2 2 0.9 NCC[C@H]1C[C@H]1c1c[nH]cn1
CHEMBL1243335 hrh3_human Human No 7.8 EC50 = 15 nM Funct
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
337 5 1 3 5.0 CC(C)(C)c1ccc(SCC(c2ccccn2)c2c[nH]cn2)cc1
CHEMBL1195600 hrh3_rat Rat No 7.8 EC50 = 15 nM Funct
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
184 3 3 3 0.8 CNC(=N)SCCc1c[nH]cn1
CHEMBL554956 hrh3_rat Rat No 7.8 EC50 = 15 nM Funct
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
184 3 3 3 0.8 CNC(=N)SCCc1c[nH]cn1
CHEMBL205731 hrh3_human Human No 7.8 EC50 = 15.9 nM Funct
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
181 7 2 2 1.7 CCCNCCCCc1c[nH]cn1
CHEMBL474449 hrh3_human Human No 7.8 EC50 = 15.9 nM Bind
Agonist activity at human H3 receptor expressed in insect Sf9 cells co-expressing Gialpha2, Gbeta1gamma2 and RGS4 assessed as gamma[32P]GTP binding by liquid scintillation countingAgonist activity at human H3 receptor expressed in insect Sf9 cells co-expressing Gialpha2, Gbeta1gamma2 and RGS4 assessed as gamma[32P]GTP binding by liquid scintillation counting
367 7 5 3 0.7 N/C(=N\C(=O)CNC(=O)c1cc2ccccc2[nH]1)NCCCc1c[nH]cn1
CHEMBL4468827 hrh3_human Human No 7.8 EC50 = 15.9 nM Funct
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
179 1 2 5 -0.5 Cc1cc(N2CC(N)C2)nc(N)n1
CHEMBL495376 hrh3_human Human No 7.8 EC50 = 15.9 nM Funct
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
255 3 1 3 2.6 CC1(C)COC(c2cccc(Cc3c[nH]cn3)c2)=N1
CHEMBL90 hrh3_human Human Yes 7.8 EC50 = 15.9 nM Funct
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
111 2 2 2 -0.1 NCCc1cnc[nH]1
CHEMBL179479 hrh3_human Human No 7.8 EC50 = 15.9 nM Funct
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
267 4 1 2 3.1 C(=C1CCN(CCc2ccccc2)CC1)c1c[nH]cn1
CHEMBL369819 hrh3_human Human No 7.8 EC50 = 15.9 nM Funct
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
255 4 1 2 2.9 c1ccc(CN2CCC(Cc3c[nH]cn3)CC2)cc1
CHEMBL3220119 hrh3_human Human No 7.8 EC50 = 15.9 nM Funct
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
316 6 0 4 3.5 CC1(C)COC(c2ccc(OCCCN3CCCCC3)cc2)=N1
CHEMBL150243 hrh3_human Human Yes 5.8 EC50 = 1513.6 nM Bind
Inhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H3 receptorInhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H3 receptor
149 1 2 2 0.8 C1=C(c2c[nH]cn2)CCNC1
CHEMBL3806146 hrh3_human Human No 5.8 EC50 = 1530 nM Funct
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
272 4 3 3 1.5 N#C/N=C(\NC[C@@H]1CC[C@H](c2c[nH]cn2)C1)NC1CC1
CHEMBL4227989 hrh3_human Human No 6.8 EC50 = 157 nM Funct
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
317 9 0 2 5.4 CCC(C)(C)c1ccc(OCCCCCN2CCCCC2)cc1
CHEMBL4300613 hrh3_human Human No 6.8 EC50 = 157 nM Funct
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
317 9 0 2 5.4 CCC(C)(C)c1ccc(OCCCCCN2CCCCC2)cc1
CHEMBL4439165 hrh3_human Human No 6.8 EC50 = 158.5 nM Funct
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
235 4 2 5 1.0 CCNC1CN(c2cc(C(C)C)nc(N)n2)C1
CHEMBL128613 hrh3_human Human Yes 5.8 EC50 = 1584.9 nM Bind
Effective concentration required against human histamine H3 receptor was determined by the inhibition of the cAMP stimulated beta-galactosidase transcription in SK-N-MC cellsEffective concentration required against human histamine H3 receptor was determined by the inhibition of the cAMP stimulated beta-galactosidase transcription in SK-N-MC cells
321 1 1 2 2.3 CN1CCN(C(=O)c2cc3cc(Br)ccc3[nH]2)CC1
CHEMBL4225644 hrh3_human Human No 6.8 EC50 = 164 nM Funct
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
331 9 0 2 5.7 CCC(C)(C)c1ccc(OCCCCCN2CCCC(C)C2)cc1
CHEMBL4300100 hrh3_human Human No 6.8 EC50 = 164 nM Funct
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
331 9 0 2 5.7 CCC(C)(C)c1ccc(OCCCCCN2CCCC(C)C2)cc1
CHEMBL541483 hrh3_human Human No 7.8 EC50 = 17 nM Funct
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
382 4 0 4 3.6 CC(C)N1CCC(Oc2ccc3cc(C(=O)N4CCOCC4)ccc3c2)CC1
CHEMBL351231 hrh3_rat Rat Yes 7.8 EC50 = 17.4 nM Funct
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
330 4 0 3 5.0 N#Cc1ccc(cc1)c1ccc2c(c1)cc(o2)CCN1CCC[C@H]1C
CHEMBL351231 hrh3_rat Rat Yes 7.8 EC50 = 17.4 nM Funct
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
330 4 0 3 5.0 N#Cc1ccc(cc1)c1ccc2c(c1)cc(o2)CCN1CCC[C@H]1C
CHEMBL3805514 hrh3_human Human No 6.8 EC50 = 170 nM Funct
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
160 3 4 3 0.2 CC(=N)SCCNC(=N)N
CHEMBL1173033 hrh3_human Human No 6.8 EC50 = 177 nM Funct
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
242 3 1 3 2.3 c1cncc(N2CCC(Cc3c[nH]cn3)CC2)c1
CHEMBL1172776 hrh3_human Human No 7.8 EC50 = 18 nM Funct
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
297 3 1 2 4.2 CC(C)(C)c1ccc(N2CCC(Cc3c[nH]cn3)CC2)cc1
CHEMBL1257965 hrh3_human Human No 7.8 EC50 = 18 nM Funct
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
395 5 0 4 4.1 CC(C)N1CCC(Oc2ccc3c(c2)cc2n3C[C@@H](C)N(CC3CC3)C2=O)CC1
CHEMBL1257965 hrh3_rat Rat No 7.8 EC50 = 18 nM Funct
Inverse agonist activity at rat histamine H3 receptorInverse agonist activity at rat histamine H3 receptor
395 5 0 4 4.1 CC(C)N1CCC(Oc2ccc3c(c2)cc2n3C[C@@H](C)N(CC3CC3)C2=O)CC1
CHEMBL358028 hrh3_human Human Yes 5.7 EC50 = 1819.7 nM Bind
Inhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H3 receptorInhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H3 receptor
151 1 2 2 0.9 c1nc(C2CCNCC2)c[nH]1
CHEMBL4174017 hrh3_human Human No 6.7 EC50 = 186.2 nM Funct
Agonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assayAgonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assay
534 7 1 6 5.9 COc1cc(NC2(c3ccccc3Cl)C(=O)N(C(C)(C)C)C(=O)/C2=C/c2ccccc2)cc(OC)c1OC
CHEMBL4174017 hrh3_human Human No 6.7 EC50 = 187 nM Funct
Agonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assayAgonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assay
534 7 1 6 5.9 COc1cc(NC2(c3ccccc3Cl)C(=O)N(C(C)(C)C)C(=O)/C2=C/c2ccccc2)cc(OC)c1OC
CHEMBL1098002 hrh3_human Human No 7.7 EC50 = 19 nM Funct
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
272 4 1 2 3.8 FC(F)(F)c1ccc(SCCc2c[nH]cn2)cc1
CHEMBL309654 hrh3_human Human Yes 7.7 EC50 = 19.5 nM Bind
Inhibition of the cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H3 receptorInhibition of the cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H3 receptor
187 4 1 2 2.0 c1cc(CCCc2c[nH]cn2)ccn1
CHEMBL153284 hrh3_human Human Yes 7.7 EC50 = 19.5 nM Bind
Inhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H3 receptorInhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H3 receptor
137 2 2 2 0.5 NCC1CC1c1c[nH]cn1
CHEMBL203389 hrh3_human Human Yes 7.7 EC50 = 20.0 nM Funct
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
221 6 1 2 2.6 c1nc(CCCCCN2CCCCC2)c[nH]1
CHEMBL320331 hrh3_human Human No 6.7 EC50 = 190.6 nM Funct
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
258 5 1 3 2.8 c1ccc(COC[C@@H]2CC[C@H](c3c[nH]cn3)O2)cc1
CHEMBL493012 hrh3_human Human No 6.7 EC50 = 199.5 nM Funct
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
234 3 1 1 3.7 c1ccc(-c2cccc(Cc3c[nH]cn3)c2)cc1
CHEMBL320331 hrh3_human Human No 6.7 EC50 = 199.5 nM Funct
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
258 5 1 3 2.8 c1ccc(COC[C@@H]2CC[C@H](c3c[nH]cn3)O2)cc1
CHEMBL180061 hrh3_human Human Yes 6.7 EC50 = 199.5 nM Funct
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
221 4 1 2 2.5 CC(C)N1CCC(CCc2c[nH]cn2)CC1
CHEMBL442242 hrh3_human Human No 8.7 EC50 = 2 nM Funct
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
334 4 0 4 4.0 Cc1nn(C)cc1-c1ccc2cc(CCN3CCC[C@H]3C)ccc2n1
CHEMBL1170855 hrh3_human Human No 8.7 EC50 = 2 nM Funct
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
284 4 1 3 2.9 CN(C)c1ccc(N2CCC(Cc3c[nH]cn3)CC2)cc1
CHEMBL1917464 hrh3_human Human No 8.7 EC50 = 2 nM Funct
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
297 4 0 4 2.5 C[C@@H]1CCCN1CCc1ccc(-c2ccc(=O)n(C)n2)cc1
CHEMBL482844 hrh3_human Human No 8.7 EC50 = 2 nM Bind
Inverse agonist activity at human histamine H3 receptor expressed in CHO cells by GTPgamma[35S] binding assayInverse agonist activity at human histamine H3 receptor expressed in CHO cells by GTPgamma[35S] binding assay
451 5 0 5 3.7 O=C(c1cc2cc(OC3CCN(C4CC4)CC3)ccc2n1CC(F)(F)F)N1CCOCC1
CHEMBL483672 hrh3_human Human No 8.7 EC50 = 2 nM Bind
Inverse agonist activity at human histamine H3 receptor expressed in CHO cells by GTPgamma[35S] binding assayInverse agonist activity at human histamine H3 receptor expressed in CHO cells by GTPgamma[35S] binding assay
465 5 0 5 4.1 O=C(c1cc2cc(OC3CCN(C4CCC4)CC3)ccc2n1CC(F)(F)F)N1CCOCC1
CHEMBL521710 hrh3_human Human No 8.7 EC50 = 2 nM Bind
Inverse agonist activity at human histamine H3 receptor expressed in CHO cells by GTPgamma[35S] binding assayInverse agonist activity at human histamine H3 receptor expressed in CHO cells by GTPgamma[35S] binding assay
444 5 0 5 4.3 CC(C)N1CCC(Oc2ccc3c(c2)cc(C(=O)N2CCC(F)(F)CC2)n3CC#N)CC1
CHEMBL523948 hrh3_human Human No 8.7 EC50 = 2 nM Bind
Inverse agonist activity at human histamine H3 receptor expressed in CHO cells by GTPgamma[35S] binding assayInverse agonist activity at human histamine H3 receptor expressed in CHO cells by GTPgamma[35S] binding assay
549 5 0 4 7.1 CC(C)N1CCC(Oc2ccc3c(c2)cc(C(=O)N2CCC(F)(F)CC2)n3-c2ccc(Cl)c(Cl)c2)CC1
CHEMBL1258079 hrh3_human Human No 8.7 EC50 = 2 nM Funct
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
473 5 0 4 5.1 CC(C)N1CCC(Oc2cc3cc4n(c3cc2Br)[C@@H](C)CN(CC2CC2)C4=O)CC1
CHEMBL497031 hrh3_human Human Yes 8.7 EC50 = 2 nM Funct
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
447 5 0 4 5.3 CC(C)N1CCC(Oc2ccc3c(c2)cc(C(=O)N2CCC(F)(F)CC2)n3C(C)C)CC1
CHEMBL1829335 hrh3_rat Rat Yes 8.7 EC50 = 2 nM Funct
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
313 6 1 4 2.7 C[C@@H]1CCCN1CCCOc1ccc(-c2ccc(=O)[nH]n2)cc1
CHEMBL440730 hrh3_human Human Yes 8.7 EC50 = 2.1 nM Bind
Inhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H3 receptorInhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H3 receptor
151 2 2 2 0.6 c1nc(C[C@H]2CCNC2)c[nH]1
CHEMBL1829485 hrh3_human Human No 8.7 EC50 = 2.1 nM Funct
Antagonist activity at human histamine 3 receptor by [35S]GTPgammaS binding assayAntagonist activity at human histamine 3 receptor by [35S]GTPgammaS binding assay
341 6 0 5 2.9 C[C@H](COc1ccc(-c2ccc(=O)n(C)n2)cc1)CN1CCC[C@H]1C
CHEMBL1917468 hrh3_human Human No 8.7 EC50 = 2.1 nM Funct
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
377 5 0 4 4.1 C[C@@H]1CCCN1CCc1ccc(-c2ccc(=O)n(-c3ccc(F)cc3)n2)cc1
CHEMBL1813065 hrh3_rat Rat No 8.7 EC50 = 2.1 nM Funct
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
313 6 1 4 2.7 C[C@@H]1CCCN1CCCOc1ccc(-c2cn[nH]c(=O)c2)cc1
CHEMBL1813057 hrh3_rat Rat No 8.7 EC50 = 2.2 nM Funct
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
327 6 0 5 2.7 C[C@@H]1CCCN1CCCOc1ccc(-c2ccc(=O)n(C)n2)cc1
CHEMBL417096 hrh3_human Human Yes 8.6 EC50 = 2.3 nM Bind
Inhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H3 receptorInhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H3 receptor
153 5 2 2 1.1 NCCCCCc1cnc[nH]1
CHEMBL152936 hrh3_human Human Yes 8.6 EC50 = 2.3 nM Bind
Inhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H3 receptorInhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H3 receptor
177 2 2 2 1.4 C=C(c1c[nH]cn1)C1CCNCC1
CHEMBL19439 hrh3_human Human Yes 8.6 EC50 = 2.4 nM Funct
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
170 3 3 3 0.6 NC(=N)SCCc1cnc[nH]1
CHEMBL483406 hrh3_human Human No 8.6 EC50 = 2.5 nM Bind
Activity at human recombinant histamine H3 receptor expressed in Sf9 cells coexpressing Galphai, G-beta-1-gamma-2 and RGS4 by steady-state GTPase activity assayActivity at human recombinant histamine H3 receptor expressed in Sf9 cells coexpressing Galphai, G-beta-1-gamma-2 and RGS4 by steady-state GTPase activity assay
313 7 3 2 2.0 CC(CC(=O)/N=C(\N)NCCCc1c[nH]cn1)c1ccccc1
CHEMBL483406 hrh3_human Human No 8.6 EC50 = 2.5 nM Bind
Agonist activity at human H3 receptor expressed in insect Sf9 cells co-expressing Gialpha2, Gbeta1gamma2 and RGS4 assessed as gamma[32P]GTP binding by liquid scintillation countingAgonist activity at human H3 receptor expressed in insect Sf9 cells co-expressing Gialpha2, Gbeta1gamma2 and RGS4 assessed as gamma[32P]GTP binding by liquid scintillation counting
313 7 3 2 2.0 CC(CC(=O)/N=C(\N)NCCCc1c[nH]cn1)c1ccccc1
CHEMBL90 hrh3_human Human Yes 8.6 EC50 = 2.5 nM Funct
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
111 2 2 2 -0.1 NCCc1cnc[nH]1
CHEMBL470790 hrh3_human Human No 8.6 EC50 = 2.5 nM Funct
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
299 7 4 3 1.6 N=C(NCCCc1c[nH]cn1)NC(=O)CCc1ccccc1
CHEMBL483406 hrh3_human Human No 8.6 EC50 = 2.5 nM Funct
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
313 7 3 2 2.0 CC(CC(=O)/N=C(\N)NCCCc1c[nH]cn1)c1ccccc1
CHEMBL483406 hrh3_human Human No 8.6 EC50 = 2.5 nM Bind
Agonist activity at human recombinant histamine H3 receptor expressed in Sf9 cells coexpressing Galphai2,Gbeta1gamma2 and RGS4 preincubated for 2 mins before [gamma32P]GTP addition measured after 20 mins by steady-state GTPase activity assayAgonist activity at human recombinant histamine H3 receptor expressed in Sf9 cells coexpressing Galphai2,Gbeta1gamma2 and RGS4 preincubated for 2 mins before [gamma32P]GTP addition measured after 20 mins by steady-state GTPase activity assay
313 7 3 2 2.0 CC(CC(=O)/N=C(\N)NCCCc1c[nH]cn1)c1ccccc1
CHEMBL179302 hrh3_human Human Yes 8.6 EC50 = 2.5 nM Funct
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
177 1 1 2 1.5 CN1CCC(=Cc2c[nH]cn2)CC1
CHEMBL4166098 hrh3_human Human No 8.6 EC50 = 2.7 nM Funct
Agonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assayAgonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assay
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
CHEMBL4166098 hrh3_human Human No 8.6 EC50 = 2.7 nM Funct
Agonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assayAgonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assay
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
CHEMBL4175898 hrh3_human Human No 8.6 EC50 = 2.7 nM Funct
Agonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assayAgonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assay
530 7 1 5 6.5 COc1ccc(NC2(c3cccc(Cl)c3)C(=O)N(C3CCCCC3)C(=O)/C2=C/c2ccccc2)cc1OC
CHEMBL4175898 hrh3_human Human No 8.6 EC50 = 2.8 nM Funct
Agonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assayAgonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assay
530 7 1 5 6.5 COc1ccc(NC2(c3cccc(Cl)c3)C(=O)N(C3CCCCC3)C(=O)/C2=C/c2ccccc2)cc1OC
CHEMBL268229 hrh3_human Human Yes 8.6 EC50 = 2.8 nM Funct
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
125 2 2 2 0.3 C[C@H](Cc1cnc[nH]1)N
CHEMBL19439 hrh3_rat Rat Yes 8.6 EC50 = 2.8 nM Bind
In vitro binding affinity against histamine H3 receptor from synaptosomes of rat cerebral cortexIn vitro binding affinity against histamine H3 receptor from synaptosomes of rat cerebral cortex
170 3 3 3 0.6 NC(=N)SCCc1cnc[nH]1
CHEMBL1096430 hrh3_human Human No 8.5 EC50 = 2.9 nM Bind
Activity at human recombinant histamine H3 receptor expressed in Sf9 cells coexpressing Galphai, Gbeta1gamma2 and RGS4 by steady-state GTPase activity assayActivity at human recombinant histamine H3 receptor expressed in Sf9 cells coexpressing Galphai, Gbeta1gamma2 and RGS4 by steady-state GTPase activity assay
319 7 4 3 2.6 C[C@H](CC(=O)NC(=N)NCCCc1c[nH]cn1)C1CCCCC1
CHEMBL2165628 hrh3_human Human No 8.5 EC50 = 2.9 nM Funct
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
546 17 6 6 2.3 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)CCCCCCCCC(=O)/N=C(\N)NCCCc1c[nH]cn1
CHEMBL19439 hrh3_human Human Yes 8.5 EC50 = 2.9 nM Funct
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
170 3 3 3 0.6 NC(=N)SCCc1cnc[nH]1
CHEMBL557461 hrh3_human Human No 6.7 EC50 = 200 nM Funct
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
394 6 0 3 5.0 CC1CCN(C(=O)c2ccc3cc(OCCCN4CCCCC4)ccc3c2)CC1
CHEMBL477181 hrh3_human Human No 7.7 EC50 = 21 nM Funct
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
394 5 1 3 5.2 CC(C)N1CCC(Oc2ccc3cc(C(=O)NC4CCCCC4)ccc3c2)CC1
CHEMBL3806206 hrh3_human Human No 6.7 EC50 = 212 nM Funct
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
246 3 3 3 0.9 CN/C(=N\C#N)NC[C@@H]1CC[C@H](c2c[nH]cn2)C1
CHEMBL1243366 hrh3_human Human No 7.7 EC50 = 22 nM Funct
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
337 5 1 3 5.0 CC(C)(C)c1ccc(SCC(c2cccnc2)c2c[nH]cn2)cc1
CHEMBL4166386 hrh3_human Human No 7.6 EC50 = 22.9 nM Funct
Agonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assayAgonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assay
440 5 1 4 5.3 COc1ccc(NC2(c3ccccc3)C(=O)N(C(C)(C)C)C(=O)/C2=C/c2ccccc2)cc1
CHEMBL1243394 hrh3_human Human No 7.6 EC50 = 23 nM Funct
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
355 5 2 3 4.3 FC(F)(F)c1ccc(SC[C@H](c2c[nH]cn2)C2CCNCC2)cc1
CHEMBL522243 hrh3_human Human No 7.6 EC50 = 23 nM Bind
Inverse agonist activity at human histamine H3 receptor expressed in CHO cells by GTPgamma[35S] binding assayInverse agonist activity at human histamine H3 receptor expressed in CHO cells by GTPgamma[35S] binding assay
371 4 1 4 2.9 CC(C)N1CCC(Oc2ccc3cc(C(=O)N4CCOCC4)[nH]c3c2)CC1
CHEMBL1257257 hrh3_human Human No 7.6 EC50 = 23 nM Funct
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
435 5 0 4 4.7 CC(C)N1CCC(Oc2ccc3c(c2)cc2n3CCN(Cc3cccc(F)c3)C2=O)CC1
CHEMBL59389 hrh3_human Human No 5.6 EC50 = 2330 nM Bind
Inhibition of human H3-receptor using [3H]N-alpha-methyl histamineInhibition of human H3-receptor using [3H]N-alpha-methyl histamine
123 1 2 2 0.2 N[C@@H]1C[C@@H]1c1c[nH]cn1
CHEMBL4174766 hrh3_human Human No 7.6 EC50 = 24 nM Funct
Agonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assayAgonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assay
548 6 1 4 5.7 COc1ccc(N2C(=O)/C(=C\c3ccccc3)C2(C(=O)NC(C)(C)C)c2ccc(Br)cc2)cc1OC
CHEMBL1258309 hrh3_human Human No 7.6 EC50 = 24 nM Funct
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
341 5 1 4 3.0 C[C@H]1CC[C@H](C)N1CCCOc1ccc2c(c1)cc1n2CCNC1=O
CHEMBL1097658 hrh3_human Human No 7.6 EC50 = 25 nM Funct
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
215 4 2 2 2.7 Cc1ccc(NCCc2c[nH]cn2)cc1C
CHEMBL1258874 hrh3_human Human No 7.6 EC50 = 25 nM Funct
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
369 4 0 4 3.8 CC(C)N1CCC(Oc2ccc3c(c2)cc2n3CCN(C(C)C)C2=O)CC1
CHEMBL90 hrh3_human Human Yes 7.6 EC50 = 25.1 nM Bind
Activity at human recombinant histamine H3 receptor expressed in Sf9 cells coexpressing Galphai, G-beta-1-gamma-2 and RGS4 by steady-state GTPase activity assayActivity at human recombinant histamine H3 receptor expressed in Sf9 cells coexpressing Galphai, G-beta-1-gamma-2 and RGS4 by steady-state GTPase activity assay
111 2 2 2 -0.1 NCCc1cnc[nH]1
CHEMBL204843 hrh3_human Human Yes 7.6 EC50 = 25.1 nM Funct
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
167 6 2 2 1.3 CCNCCCCc1c[nH]cn1
CHEMBL90 hrh3_human Human Yes 7.6 EC50 = 25.1 nM Bind
Agonist activity at human H3 receptor expressed in insect Sf9 cells co-expressing Gialpha2, Gbeta1gamma2 and RGS4 assessed as gamma[32P]GTP binding by liquid scintillation countingAgonist activity at human H3 receptor expressed in insect Sf9 cells co-expressing Gialpha2, Gbeta1gamma2 and RGS4 assessed as gamma[32P]GTP binding by liquid scintillation counting
111 2 2 2 -0.1 NCCc1cnc[nH]1
CHEMBL4535363 hrh3_human Human No 7.6 EC50 = 25.1 nM Funct
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
207 3 2 5 0.0 CCc1cc(N2CC(NC)C2)nc(N)n1
CHEMBL90 hrh3_human Human Yes 7.6 EC50 = 25.1 nM Funct
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
111 2 2 2 -0.1 NCCc1cnc[nH]1
CHEMBL90 hrh3_human Human Yes 7.6 EC50 = 25.1 nM Bind
Agonist activity at human recombinant histamine H3 receptor expressed in Sf9 cells coexpressing Galphai2,Gbeta1gamma2 and RGS4 preincubated for 2 mins before [gamma32P]GTP addition measured after 20 mins by steady-state GTPase activity assayAgonist activity at human recombinant histamine H3 receptor expressed in Sf9 cells coexpressing Galphai2,Gbeta1gamma2 and RGS4 preincubated for 2 mins before [gamma32P]GTP addition measured after 20 mins by steady-state GTPase activity assay
111 2 2 2 -0.1 NCCc1cnc[nH]1
CHEMBL175741 hrh3_human Human No 7.6 EC50 = 25.1 nM Funct
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
191 2 1 2 1.9 CCN1CCC(=Cc2c[nH]cn2)CC1
CHEMBL4174766 hrh3_human Human No 7.6 EC50 = 25.7 nM Funct
Agonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assayAgonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assay
548 6 1 4 5.7 COc1ccc(N2C(=O)/C(=C\c3ccccc3)C2(C(=O)NC(C)(C)C)c2ccc(Br)cc2)cc1OC
CHEMBL1688969 hrh3_human Human No 6.6 EC50 = 251.2 nM Funct
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
259 5 1 4 2.4 C1CCC(CC1)CC2=CN(N=N2)CCC3=CN=CN3
CHEMBL1077861 hrh3_human Human Yes 6.6 EC50 = 251.2 nM Funct
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
206 5 3 3 0.1 N#C/N=C(\N)NCCCCc1c[nH]cn1
CHEMBL1258755 hrh3_human Human No 7.6 EC50 = 26 nM Funct
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
341 3 1 4 3.0 CC(C)N1CCC(Oc2ccc3c(c2)cc2n3CCCNC2=O)CC1
CHEMBL109130 hrh3_human Human Yes 6.6 EC50 = 269.2 nM Funct
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
165 2 2 3 0.4 NC[C@H]1C=C[C@H](c2c[nH]cn2)O1
CHEMBL320279 hrh3_human Human Yes 4.6 EC50 = 26915.4 nM Funct
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
165 2 2 3 0.4 NC[C@@H]1C=C[C@H](c2c[nH]cn2)O1
CHEMBL1094144 hrh3_human Human No 5.6 EC50 = 2754.2 nM Bind
Activity at human recombinant histamine H3 receptor expressed in Sf9 cells coexpressing Galphai, Gbeta1gamma2 and RGS4 by steady-state GTPase activity assayActivity at human recombinant histamine H3 receptor expressed in Sf9 cells coexpressing Galphai, Gbeta1gamma2 and RGS4 by steady-state GTPase activity assay
365 7 4 5 3.2 Cc1nc(N)sc1CCCNC(=N)NC(=O)C[C@H](C)C1CCCCC1
CHEMBL345954 hrh3_human Human Yes 5.6 EC50 = 2754.2 nM Bind
Inhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H3 receptorInhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H3 receptor
179 2 2 3 0.6 O=C(c1c[nH]cn1)C1CCNCC1
CHEMBL1257138 hrh3_human Human No 7.6 EC50 = 28 nM Funct
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
381 5 0 4 3.8 CC(C)N1CCC(Oc2ccc3c(c2)cc2n3CCN(CC3CC3)C2=O)CC1
CHEMBL1257256 hrh3_human Human No 7.6 EC50 = 28 nM Funct
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
435 5 0 4 4.7 CC(C)N1CCC(Oc2ccc3c(c2)cc2n3CCN(Cc3ccccc3F)C2=O)CC1
CHEMBL319658 hrh3_human Human Yes 5.6 EC50 = 2818.4 nM Funct
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
165 2 2 3 0.4 NC[C@@H]1C=C[C@@H](c2c[nH]cn2)O1
CHEMBL1257851 hrh3_human Human No 7.5 EC50 = 29 nM Funct
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
341 3 1 4 3.2 CC(C)N1CCC(Oc2ccc3c(c2)cc2n3[C@H](C)CNC2=O)CC1
CHEMBL4166386 hrh3_human Human No 8.5 EC50 = 3 nM Funct
Agonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assayAgonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assay
440 5 1 4 5.3 COc1ccc(NC2(c3ccccc3)C(=O)N(C(C)(C)C)C(=O)/C2=C/c2ccccc2)cc1
CHEMBL496617 hrh3_human Human No 8.5 EC50 = 3 nM Bind
Inverse agonist activity at human histamine H3 receptor expressed in CHO cells by GTPgamma[35S] binding assayInverse agonist activity at human histamine H3 receptor expressed in CHO cells by GTPgamma[35S] binding assay
405 4 1 3 4.3 CC(C)N1CCC(Oc2ccc3[nH]c(C(=O)N4CCCC(F)(F)C4)cc3c2)CC1
CHEMBL522739 hrh3_human Human No 8.5 EC50 = 3 nM Bind
Inverse agonist activity at human histamine H3 receptor expressed in CHO cells by GTPgamma[35S] binding assayInverse agonist activity at human histamine H3 receptor expressed in CHO cells by GTPgamma[35S] binding assay
478 4 0 5 3.0 O=C(c1ccc2c(c1)cc(C(=O)N1CCOCC1)n2CC(F)(F)F)N1CCN(C2CCC2)CC1
CHEMBL237191 hrh3_rat Rat No 8.5 EC50 = 3.0 nM Funct
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
401 5 0 5 4.6 Cc1nc(N2CCCC2)ncc1-c1ccc2cc(CCN3CCC[C@H]3C)ccc2n1
CHEMBL4476584 hrh3_human Human No 8.5 EC50 = 3.2 nM Funct
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
207 3 2 5 0.2 CC(C)NC1CN(c2ccnc(N)n2)C1
CHEMBL4596412 hrh3_human Human No 8.5 EC50 = 3.2 nM Funct
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
207 3 2 5 0.2 CC(C)NC1CN(c2ccnc(N)n2)C1
CHEMBL19173 hrh3_human Human Yes 8.5 EC50 = 3.2 nM Funct
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
216 6 1 2 2.6 C(CCc1cnc[nH]1)OCc1ccccc1
CHEMBL356666 hrh3_human Human Yes 8.5 EC50 = 3.2 nM Funct
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
163 1 2 2 1.2 C(=C1CCNCC1)c1c[nH]cn1
CHEMBL356666 hrh3_human Human Yes 8.5 EC50 = 3.2 nM Bind
Inhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H3 receptorInhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H3 receptor
163 1 2 2 1.2 C(=C1CCNCC1)c1c[nH]cn1
CHEMBL3220125 hrh3_human Human No 8.5 EC50 = 3.2 nM Funct
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
395 6 0 5 4.7 c1cc(-c2nc(CN3CCCCC3)co2)ccc1O[C@H]1C[C@H](N2CCCCC2)C1
CHEMBL451821 hrh3_human Human No 8.5 EC50 = 3.3 nM Bind
Antagonist activity at H3 receptor assessed as inhibition of [35S]gammaGTP binding relative to controlAntagonist activity at H3 receptor assessed as inhibition of [35S]gammaGTP binding relative to control
455 4 1 3 5.0 CN[C@@H](C(=O)N(C)[C@H]1CC[C@@]2(C)C(=CC[C@@H]3[C@@H]2CC[C@]24CN(C)[C@@H](C)[C@H]2CC[C@@H]34)C1)C(C)C
CHEMBL90 hrh3_human Human Yes 8.5 EC50 = 3.3 nM Funct
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
111 2 2 2 -0.1 NCCc1cnc[nH]1
CHEMBL393581 hrh3_rat Rat No 8.4 EC50 = 3.6 nM Funct
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
397 5 0 5 4.8 Cc1c(-c2ccc3cc(CCN4CCC[C@H]4C)ccc3n2)cnn1-c1ccccn1
CHEMBL443896 hrh3_human Human No 8.4 EC50 = 3.6 nM Bind
Agonist activity at human H3 receptor expressed in insect Sf9 cells co-expressing Gialpha2, Gbeta1gamma2 and RGS4 assessed as gamma[32P]GTP binding by liquid scintillation countingAgonist activity at human H3 receptor expressed in insect Sf9 cells co-expressing Gialpha2, Gbeta1gamma2 and RGS4 assessed as gamma[32P]GTP binding by liquid scintillation counting
209 4 3 2 -0.2 CC(=O)/N=C(\N)NCCCc1c[nH]cn1
CHEMBL393581 hrh3_rat Rat No 8.4 EC50 = 3.6 nM Funct
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
397 5 0 5 4.8 Cc1c(-c2ccc3cc(CCN4CCC[C@H]4C)ccc3n2)cnn1-c1ccccn1
CHEMBL4175106 hrh3_human Human No 8.4 EC50 = 3.8 nM Funct
Agonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assayAgonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assay
502 6 1 4 6.1 COc1ccc(NC2(c3cc(F)cc(F)c3)C(=O)N(C3CCCCC3)C(=O)/C2=C/c2ccccc2)cc1
CHEMBL4175106 hrh3_human Human No 8.4 EC50 = 3.8 nM Funct
Agonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assayAgonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assay
502 6 1 4 6.1 COc1ccc(NC2(c3cc(F)cc(F)c3)C(=O)N(C3CCCCC3)C(=O)/C2=C/c2ccccc2)cc1
CHEMBL4455352 hrh3_human Human No 8.4 EC50 = 4.0 nM Funct
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
193 2 1 5 -0.2 CN(C)C1CN(c2ccnc(N)n2)C1
CHEMBL4595913 hrh3_human Human No 8.4 EC50 = 4.0 nM Funct
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
193 2 1 5 -0.2 CN(C)C1CN(c2ccnc(N)n2)C1
CHEMBL4441731 hrh3_human Human Yes 8.4 EC50 = 4.0 nM Funct
Agonist activity at human H3R expressed on HEK293T cells by [35S]GTPgammaS binding assayAgonist activity at human H3R expressed on HEK293T cells by [35S]GTPgammaS binding assay
207 4 2 5 0.2 CCCNC1CN(c2ccnc(N)n2)C1
CHEMBL4596734 hrh3_human Human Yes 8.4 EC50 = 4.0 nM Funct
Agonist activity at human H3R expressed on HEK293T cells by [35S]GTPgammaS binding assayAgonist activity at human H3R expressed on HEK293T cells by [35S]GTPgammaS binding assay
207 4 2 5 0.2 CCCNC1CN(c2ccnc(N)n2)C1
CHEMBL417096 hrh3_human Human Yes 8.4 EC50 = 4.0 nM Funct
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
153 5 2 2 1.1 NCCCCCc1cnc[nH]1
CHEMBL176178 hrh3_human Human No 8.4 EC50 = 4.0 nM Funct
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
247 3 1 2 3.0 c1nc(CC2CCN(C3CCCCC3)CC2)c[nH]1
CHEMBL176269 hrh3_human Human No 8.4 EC50 = 4.0 nM Funct
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
193 3 1 2 1.7 CCN1CCC(Cc2c[nH]cn2)CC1
CHEMBL90 hrh3_human Human Yes 7.5 EC50 = 30 nM Funct
Agonist activity at human H3 receptor stably transfected in CHO-DUKX cells assessed as increase in cAMP accumulation by measuring reduction in forskolin level by HitHunter-cAMP assayAgonist activity at human H3 receptor stably transfected in CHO-DUKX cells assessed as increase in cAMP accumulation by measuring reduction in forskolin level by HitHunter-cAMP assay
111 2 2 2 -0.1 NCCc1cnc[nH]1
CHEMBL78497 hrh3_human Human Yes 7.5 EC50 = 30.9 nM Bind
Inhibition of the cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H3 receptorInhibition of the cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H3 receptor
187 4 1 2 2.0 c1cncc(CCCc2c[nH]cn2)c1
CHEMBL206548 hrh3_human Human Yes 7.5 EC50 = 31.6 nM Funct
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
181 6 1 2 1.7 CN(CCCCCc1[nH]cnc1)C
CHEMBL203228 hrh3_human Human No 7.5 EC50 = 31.6 nM Funct
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
207 6 1 2 2.2 c1nc(CCCCCN2CCCC2)c[nH]1
CHEMBL205583 hrh3_human Human No 7.5 EC50 = 31.6 nM Funct
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
207 5 1 2 2.2 c1nc(CCCCN2CCCCC2)c[nH]1
CHEMBL4459723 hrh3_human Human No 7.5 EC50 = 31.6 nM Funct
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
193 2 2 5 -0.2 CCc1cc(N2CC(N)C2)nc(N)n1
CHEMBL4570258 hrh3_human Human No 7.5 EC50 = 31.6 nM Funct
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
221 4 2 5 0.4 CCNC1CN(c2cc(CC)nc(N)n2)C1
CHEMBL453433 hrh3_human Human Yes 7.5 EC50 = 31.6 nM Funct
Agonist activity at human histamine H3 receptor assessed as beta galactosidase activityAgonist activity at human histamine H3 receptor assessed as beta galactosidase activity
124 3 1 1 1.8 CCCCc1c[nH]cn1
CHEMBL369096 hrh3_human Human No 7.5 EC50 = 31.6 nM Funct
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
283 6 1 2 3.3 c1ccc(CCCN2CCC(Cc3c[nH]cn3)CC2)cc1
CHEMBL1183715 hrh3_human Human No 6.5 EC50 = 311 nM Funct
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
182 7 1 2 2.2 CCCCOCCCc1c[nH]cn1
CHEMBL314526 hrh3_human Human No 6.5 EC50 = 311 nM Funct
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
182 7 1 2 2.2 CCCCOCCCc1c[nH]cn1
CHEMBL1196470 hrh3_human Human Yes 6.5 EC50 = 316.2 nM Funct
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
161 3 4 3 -1.1 NC(=N)SCCN=C(N)N
CHEMBL1196470 hrh3_human Human Yes 6.5 EC50 = 316.2 nM Funct
Agonist activity at human histamine H3 receptor in SK-N-MC cells assessed as inhibition of forskolin-induced cAMP-mediated CRE-beta galactosidase activityAgonist activity at human histamine H3 receptor in SK-N-MC cells assessed as inhibition of forskolin-induced cAMP-mediated CRE-beta galactosidase activity
161 3 4 3 -1.1 NC(=N)SCCN=C(N)N
CHEMBL369158 hrh3_human Human No 6.5 EC50 = 316.2 nM Funct
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
261 4 1 2 3.4 c1nc(CCC2CCN(C3CCCCC3)CC2)c[nH]1
CHEMBL321860 hrh3_human Human Yes 5.5 EC50 = 3162.3 nM Funct
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
248 3 3 4 0.3 C/N=C(\NC#N)NC[C@H]1CC[C@H](c2c[nH]cn2)O1
CHEMBL185951 hrh3_human Human Yes 5.5 EC50 = 3162.3 nM Bind
Effective concentration required against human histamine H3 receptor was determined by the inhibition of the cAMP stimulated beta-galactosidase transcription in SK-N-MC cellsEffective concentration required against human histamine H3 receptor was determined by the inhibition of the cAMP stimulated beta-galactosidase transcription in SK-N-MC cells
278 1 1 3 1.6 CN1CCN(CC1)C(=O)c1nc2c([nH]1)cc(cc2)Cl
CHEMBL186108 hrh3_human Human No 5.5 EC50 = 3162.3 nM Bind
Effective concentration required against human histamine H3 receptor was determined by the inhibition of the cAMP stimulated beta-galactosidase transcription in SK-N-MC cellsEffective concentration required against human histamine H3 receptor was determined by the inhibition of the cAMP stimulated beta-galactosidase transcription in SK-N-MC cells
369 1 1 2 2.2 CN1CCN(C(=O)c2cc3cc(I)ccc3[nH]2)CC1
CHEMBL187210 hrh3_human Human No 5.5 EC50 = 3162.3 nM Bind
Effective concentration required against human histamine H3 receptor was determined by the inhibition of the cAMP stimulated beta-galactosidase transcription in SK-N-MC cellsEffective concentration required against human histamine H3 receptor was determined by the inhibition of the cAMP stimulated beta-galactosidase transcription in SK-N-MC cells
266 4 2 3 1.5 CN(C)CCNC(=O)c1nc2cc(Cl)ccc2[nH]1
CHEMBL365257 hrh3_human Human Yes 5.5 EC50 = 3162.3 nM Bind
Effective concentration required against human histamine H3 receptor was determined by the inhibition of the cAMP stimulated beta-galactosidase transcription in SK-N-MC cellsEffective concentration required against human histamine H3 receptor was determined by the inhibition of the cAMP stimulated beta-galactosidase transcription in SK-N-MC cells
262 1 1 1 3.4 O=C(c1cc2cc(Cl)ccc2[nH]1)N1CCCCC1
CHEMBL321860 hrh3_human Human Yes 5.5 EC50 = 3162.3 nM Funct
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
248 3 3 4 0.3 C/N=C(\NC#N)NC[C@H]1CC[C@H](c2c[nH]cn2)O1
CHEMBL1096514 hrh3_human Human Yes 6.5 EC50 = 320 nM Funct
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
187 4 2 2 2.1 c1ccc(NCCc2c[nH]cn2)cc1
CHEMBL152948 hrh3_human Human No 6.5 EC50 = 323.6 nM Bind
Inhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H3 receptorInhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H3 receptor
193 4 2 2 1.9 c1nc(CCCC2CCCCN2)c[nH]1
CHEMBL554031 hrh3_human Human Yes 7.5 EC50 = 33.1 nM Bind
Inhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H3 receptorInhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H3 receptor
167 6 2 2 1.5 NCCCCCCc1c[nH]cn1
CHEMBL1096513 hrh3_human Human Yes 5.5 EC50 = 3400 nM Funct
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
193 4 2 2 1.9 c1nc(CCNC2CCCCC2)c[nH]1
CHEMBL82244 hrh3_human Human Yes 6.5 EC50 = 354.8 nM Bind
Inhibition of the cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H3 receptorInhibition of the cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H3 receptor
173 3 1 2 1.6 c1cncc(CCc2c[nH]cn2)c1
CHEMBL1257728 hrh3_human Human No 7.4 EC50 = 36 nM Funct
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
395 5 0 4 4.1 CC(C)N1CCC(Oc2ccc3c(c2)cc2n3CCCN(CC3CC3)C2=O)CC1
CHEMBL1179642 hrh3_human Human Yes 6.4 EC50 = 366 nM Funct
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
166 6 1 2 1.5 C=CCOCCCc1c[nH]cn1
CHEMBL91361 hrh3_human Human Yes 6.4 EC50 = 366 nM Funct
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
166 6 1 2 1.5 C=CCOCCCc1c[nH]cn1
CHEMBL3804906 hrh3_human Human No 6.4 EC50 = 370 nM Funct
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
246 3 3 3 0.9 CN/C(=N\C#N)NC[C@H]1CC[C@H](c2c[nH]cn2)C1
CHEMBL1086105 hrh3_human Human No 6.4 EC50 = 377 nM Bind
Displacement of [125H]iodoproxyphan from human recombinant histamine H3 receptor expressed in human SK-N-MC cellsDisplacement of [125H]iodoproxyphan from human recombinant histamine H3 receptor expressed in human SK-N-MC cells
419 6 2 4 4.5 Cc1cc(OCCCN2CCc3nc[nH]c3C2)ccc1-c1nc2c(C)c(F)ccc2[nH]1
CHEMBL1243305 hrh3_human Human No 7.4 EC50 = 38 nM Funct
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
355 5 2 3 4.3 FC(F)(F)c1ccc(SCC(c2c[nH]cn2)C2CCNCC2)cc1
CHEMBL1258754 hrh3_human Human No 7.4 EC50 = 38 nM Funct
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
327 3 1 4 2.6 CC(C)N1CCC(Oc2ccc3c(c2)cc2n3CCNC2=O)CC1
CHEMBL78838 hrh3_human Human Yes 7.4 EC50 = 38.9 nM Bind
Inhibition of the cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H3 receptorInhibition of the cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H3 receptor
159 2 1 2 1.4 c1cncc(Cc2c[nH]cn2)c1
CHEMBL204360 hrh3_human Human No 7.4 EC50 = 39.8 nM Funct
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
193 5 1 2 1.8 c1nc(CCCCN2CCCC2)c[nH]1
CHEMBL4579385 hrh3_human Human No 7.4 EC50 = 39.8 nM Funct
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
207 2 1 5 0.1 Cc1cc(N2CC(N(C)C)C2)nc(N)n1
CHEMBL106612 hrh3_human Human No 7.4 EC50 = 39.8 nM Funct
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
167 2 2 3 0.6 NC[C@H]1CC[C@H](c2c[nH]cn2)O1
CHEMBL4634086 hrh3_human Human Yes 7.4 EC50 = 39.8 nM Funct
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
125 3 2 2 0.3 NCCCc1c[nH]cn1
CHEMBL91353 hrh3_human Human Yes 7.4 EC50 = 39.8 nM Funct
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
125 3 2 2 0.3 NCCCc1c[nH]cn1
CHEMBL260374 hrh3_human Human Yes 7.4 EC50 = 39.8 nM Funct
Inverse agonist activity at human histamine H3 receptor expressed in HEK293 cells assessed by forskolin induced cAMP response element activation by luciferase reporter gene assayInverse agonist activity at human histamine H3 receptor expressed in HEK293 cells assessed by forskolin induced cAMP response element activation by luciferase reporter gene assay
292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1
CHEMBL90 hrh3_human Human Yes 8.4 EC50 = 4 nM Funct
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
111 2 2 2 -0.1 NCCc1cnc[nH]1
CHEMBL1193901 hrh3_rat Rat Yes 8.4 EC50 = 4 nM Funct
Compound was evaluated for agonistic effect on release of [3H]histamine from rat brain cortical slices with L-[3H]histidine at 0.3 uMCompound was evaluated for agonistic effect on release of [3H]histamine from rat brain cortical slices with L-[3H]histidine at 0.3 uM
125 2 2 2 0.5 C[C@H](CN)c1c[nH]cn1
CHEMBL545378 hrh3_rat Rat Yes 8.4 EC50 = 4 nM Funct
Compound was evaluated for agonistic effect on release of [3H]histamine from rat brain cortical slices with L-[3H]histidine at 0.3 uMCompound was evaluated for agonistic effect on release of [3H]histamine from rat brain cortical slices with L-[3H]histidine at 0.3 uM
125 2 2 2 0.5 C[C@H](CN)c1c[nH]cn1
CHEMBL489855 hrh3_human Human No 8.4 EC50 = 4 nM Bind
Inverse agonist activity at human histamine H3 receptor expressed in CHO cells by GTPgamma[35S] binding assayInverse agonist activity at human histamine H3 receptor expressed in CHO cells by GTPgamma[35S] binding assay
501 5 0 6 3.3 CC(C)N1CCC(Oc2ccc3c(c2)cc(C(=O)N2CCS(=O)(=O)CC2)n3CC(F)(F)F)CC1
CHEMBL495639 hrh3_human Human No 8.4 EC50 = 4 nM Bind
Inverse agonist activity at human histamine H3 receptor expressed in CHO cells by GTPgamma[35S] binding assayInverse agonist activity at human histamine H3 receptor expressed in CHO cells by GTPgamma[35S] binding assay
483 5 0 6 3.6 CC(C)N1CCC(Oc2ccc3c(c2)cc(C(=O)N2CCC(F)(F)CC2)n3S(C)(=O)=O)CC1
CHEMBL496008 hrh3_human Human No 8.4 EC50 = 4 nM Bind
Inverse agonist activity at human histamine H3 receptor expressed in CHO cells by GTPgamma[35S] binding assayInverse agonist activity at human histamine H3 receptor expressed in CHO cells by GTPgamma[35S] binding assay
369 4 1 4 2.6 O=C(c1cc2cc(OC3CCN(C4CC4)CC3)ccc2[nH]1)N1CCOCC1
CHEMBL496816 hrh3_human Human No 8.4 EC50 = 4 nM Bind
Inverse agonist activity at human histamine H3 receptor expressed in CHO cells by GTPgamma[35S] binding assayInverse agonist activity at human histamine H3 receptor expressed in CHO cells by GTPgamma[35S] binding assay
405 4 1 3 4.3 CC(C)N1CCC(Oc2ccc3[nH]c(C(=O)N4CCC(F)(F)CC4)cc3c2)CC1
CHEMBL497030 hrh3_human Human No 8.4 EC50 = 4 nM Bind
Inverse agonist activity at human histamine H3 receptor expressed in CHO cells by GTPgamma[35S] binding assayInverse agonist activity at human histamine H3 receptor expressed in CHO cells by GTPgamma[35S] binding assay
453 5 0 5 3.9 CC(C)N1CCC(Oc2ccc3c(c2)cc(C(=O)N2CCOCC2)n3CC(F)(F)F)CC1
CHEMBL524077 hrh3_human Human No 8.4 EC50 = 4 nM Bind
Inverse agonist activity at human histamine H3 receptor expressed in CHO cells by GTPgamma[35S] binding assayInverse agonist activity at human histamine H3 receptor expressed in CHO cells by GTPgamma[35S] binding assay
487 5 0 4 5.3 CC(C)N1CCC(Oc2ccc3c(c2)cc(C(=O)N2CCC(F)(F)CC2)n3CC(F)(F)F)CC1
CHEMBL1258078 hrh3_human Human No 8.4 EC50 = 4 nM Funct
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
419 3 1 4 4.0 CC(C)N1CCC(Oc2cc3cc4n(c3cc2Br)[C@@H](C)CNC4=O)CC1
CHEMBL1258308 hrh3_human Human No 8.4 EC50 = 4 nM Funct
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
327 5 1 4 2.6 C[C@@H]1CCCN1CCCOc1ccc2c(c1)cc1n2CCNC1=O
CHEMBL90 hrh3_human Human Yes 8.4 EC50 = 4.1 nM Funct
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
111 2 2 2 -0.1 NCCc1cnc[nH]1
CHEMBL2165641 hrh3_human Human No 8.4 EC50 = 4.2 nM Funct
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
472 15 6 4 0.9 N/C(=N\C(=O)CCCCCCC(=O)/N=C(\N)NCCCc1c[nH]cn1)NCCCc1c[nH]cn1
CHEMBL1096517 hrh3_human Human No 8.3 EC50 = 4.6 nM Funct
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
243 4 2 2 3.4 CC(C)(C)c1cccc(NCCc2c[nH]cn2)c1
CHEMBL268229 hrh3_human Human Yes 7.4 EC50 = 40 nM Funct
Agonist activity at human H3 receptor expressed in HEK293 cells preincubated for 30 mins followed by [35S]-GTPgammaS addition and measured after 30 mins by liquid scintillation counting methodAgonist activity at human H3 receptor expressed in HEK293 cells preincubated for 30 mins followed by [35S]-GTPgammaS addition and measured after 30 mins by liquid scintillation counting method
125 2 2 2 0.3 C[C@H](Cc1cnc[nH]1)N
CHEMBL1184057 hrh3_human Human No 7.4 EC50 = 40 nM Funct
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
210 9 1 2 2.9 CCCCCCOCCCc1c[nH]cn1
CHEMBL330688 hrh3_human Human No 7.4 EC50 = 40 nM Funct
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
210 9 1 2 2.9 CCCCCCOCCCc1c[nH]cn1
CHEMBL1257139 hrh3_human Human No 7.4 EC50 = 40 nM Funct
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
409 4 0 4 3.9 CC(C)N1CCC(Oc2ccc3c(c2)cc2n3CCN(CC(F)(F)F)C2=O)CC1
CHEMBL496814 hrh3_human Human No 6.4 EC50 = 405 nM Bind
Inverse agonist activity at human histamine H3 receptor expressed in CHO cells by GTPgamma[35S] binding assayInverse agonist activity at human histamine H3 receptor expressed in CHO cells by GTPgamma[35S] binding assay
385 4 1 4 3.2 Cc1[nH]c2ccc(OC3CCN(C(C)C)CC3)cc2c1C(=O)N1CCOCC1
CHEMBL1171443 hrh3_human Human No 7.4 EC50 = 41 nM Funct
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
241 3 1 2 2.9 c1ccc(N2CCC(Cc3c[nH]cn3)CC2)cc1
CHEMBL13795 hrh3_human Human Yes 7.4 EC50 = 42 nM Bind
Inhibition of human Histamine H3 receptor using [3H]N-alpha-methyl histamineInhibition of human Histamine H3 receptor using [3H]N-alpha-methyl histamine
123 1 2 2 0.2 N[C@H]1C[C@@H]1c1c[nH]cn1
CHEMBL4634086 hrh3_human Human Yes 7.4 EC50 = 42.7 nM Bind
Inhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H3 receptorInhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H3 receptor
125 3 2 2 0.3 NCCCc1c[nH]cn1
CHEMBL91353 hrh3_human Human Yes 7.4 EC50 = 42.7 nM Bind
Inhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H3 receptorInhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H3 receptor
125 3 2 2 0.3 NCCCc1c[nH]cn1
CHEMBL496209 hrh3_human Human No 7.4 EC50 = 44 nM Bind
Inverse agonist activity at human histamine H3 receptor expressed in CHO cells by GTPgamma[35S] binding assayInverse agonist activity at human histamine H3 receptor expressed in CHO cells by GTPgamma[35S] binding assay
370 4 2 4 2.9 CC(C)N1CCC(Nc2ccc3[nH]c(C(=O)N4CCOCC4)cc3c2)CC1
CHEMBL106612 hrh3_human Human No 7.4 EC50 = 44.7 nM Funct
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
167 2 2 3 0.6 NC[C@H]1CC[C@H](c2c[nH]cn2)O1
CHEMBL2165644 hrh3_human Human No 6.4 EC50 = 446.7 nM Funct
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
669 29 6 4 6.4 N/C(=N\C(=O)CCCCCCCCCCCCCCCCCCCCC(=O)/N=C(\N)NCCCc1c[nH]cn1)NCCCc1c[nH]cn1
CHEMBL1094142 hrh3_human Human No 5.4 EC50 = 4466.8 nM Bind
Activity at human recombinant histamine H3 receptor expressed in Sf9 cells coexpressing Galphai, Gbeta1gamma2 and RGS4 by steady-state GTPase activity assayActivity at human recombinant histamine H3 receptor expressed in Sf9 cells coexpressing Galphai, Gbeta1gamma2 and RGS4 by steady-state GTPase activity assay
365 7 4 5 3.2 Cc1nc(N)sc1CCCNC(=N)NC(=O)CC(C)C1CCCCC1
CHEMBL110098 hrh3_rat Rat No 7.4 EC50 = 45 nM Bind
In vitro binding affinity against histamine H3 receptor from synaptosomes of rat cerebral cortexIn vitro binding affinity against histamine H3 receptor from synaptosomes of rat cerebral cortex
210 6 1 2 2.8 CC(C)(C)CCOCCCc1c[nH]cn1
CHEMBL2145443 hrh3_rat Rat No 7.4 EC50 = 45 nM Bind
In vitro binding affinity against histamine H3 receptor from synaptosomes of rat cerebral cortexIn vitro binding affinity against histamine H3 receptor from synaptosomes of rat cerebral cortex
210 6 1 2 2.8 CC(C)(C)CCOCCCc1c[nH]cn1
CHEMBL1096428 hrh3_human Human No 7.3 EC50 = 45.7 nM Bind
Activity at human recombinant histamine H3 receptor expressed in Sf9 cells coexpressing Galphai, Gbeta1gamma2 and RGS4 by steady-state GTPase activity assayActivity at human recombinant histamine H3 receptor expressed in Sf9 cells coexpressing Galphai, Gbeta1gamma2 and RGS4 by steady-state GTPase activity assay
313 7 4 3 2.2 C[C@H](CC(=O)NC(=N)NCCCc1c[nH]cn1)c1ccccc1
CHEMBL1257729 hrh3_human Human No 7.3 EC50 = 46 nM Funct
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
341 3 1 4 3.0 CC(C)N1CCC(Oc2ccc3c(c2)cc2n3C[C@@H](C)NC2=O)CC1
CHEMBL1243334 hrh3_human Human No 7.3 EC50 = 48 nM Funct
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
349 5 1 3 4.7 FC(F)(F)c1ccc(SCC(c2ccccn2)c2c[nH]cn2)cc1
CHEMBL1258873 hrh3_human Human No 7.3 EC50 = 48 nM Funct
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
341 3 0 4 3.0 CC(C)N1CCC(Oc2ccc3c(c2)cc2n3CCN(C)C2=O)CC1
CHEMBL151467 hrh3_human Human Yes 7.3 EC50 = 49.0 nM Bind
Inhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H3 receptorInhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H3 receptor
165 2 2 2 1.0 c1nc(CC2CCCNC2)c[nH]1
CHEMBL497031 hrh3_human Human Yes 8.3 EC50 = 5 nM Bind
Inverse agonist activity at human histamine H3 receptor expressed in CHO cells by GTPgamma[35S] binding assayInverse agonist activity at human histamine H3 receptor expressed in CHO cells by GTPgamma[35S] binding assay
447 5 0 4 5.3 CC(C)N1CCC(Oc2ccc3c(c2)cc(C(=O)N2CCC(F)(F)CC2)n3C(C)C)CC1
CHEMBL503643 hrh3_human Human Yes 8.3 EC50 = 5 nM Bind
Inverse agonist activity at human histamine H3 receptor expressed in CHO cells by GTPgamma[35S] binding assayInverse agonist activity at human histamine H3 receptor expressed in CHO cells by GTPgamma[35S] binding assay
233 3 2 3 2.0 CCOC(=O)c1cc2cc(C(=O)O)ccc2[nH]1
CHEMBL392573 hrh3_rat Rat No 8.3 EC50 = 5.0 nM Funct
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
385 4 0 5 4.6 Cc1cc2ncc(-c3ccc4cc(CCN5CCC[C@H]5C)ccc4n3)c(C)n2n1
CHEMBL90019 hrh3_human Human Yes 8.3 EC50 = 5.0 nM Funct
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
139 4 2 2 0.7 NCCCCc1cnc[nH]1
CHEMBL417096 hrh3_human Human Yes 8.3 EC50 = 5.0 nM Funct
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
153 5 2 2 1.1 NCCCCCc1cnc[nH]1
CHEMBL203441 hrh3_human Human No 8.3 EC50 = 5.0 nM Funct
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
209 9 2 2 2.5 CCCCNCCCCCc1c[nH]cn1
CHEMBL206303 hrh3_human Human No 8.3 EC50 = 5.0 nM Funct
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
195 8 2 2 2.1 CCCCNCCCCc1c[nH]cn1
CHEMBL4579823 hrh3_human Human No 8.3 EC50 = 5.0 nM Funct
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
221 4 2 5 0.5 CC(C)CNC1CN(c2ccnc(N)n2)C1
CHEMBL4594651 hrh3_human Human No 8.3 EC50 = 5.0 nM Funct
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
221 4 2 5 0.5 CC(C)CNC1CN(c2ccnc(N)n2)C1
CHEMBL4459469 hrh3_human Human Yes 8.3 EC50 = 5.0 nM Funct
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
165 1 2 5 -0.8 Nc1nccc(N2CC(N)C2)n1
CHEMBL4596157 hrh3_human Human Yes 8.3 EC50 = 5.0 nM Funct
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
165 1 2 5 -0.8 Nc1nccc(N2CC(N)C2)n1
CHEMBL90 hrh3_human Human Yes 8.3 EC50 = 5.0 nM Funct
Agonist activity at human H3R expressed on SK-N-MC cells assessed as inhibition of forskolin-induced beta galactosidase activity preincubated with forskolin for 6 hrs followed compound addition by CRE-luciferase reporter gene assayAgonist activity at human H3R expressed on SK-N-MC cells assessed as inhibition of forskolin-induced beta galactosidase activity preincubated with forskolin for 6 hrs followed compound addition by CRE-luciferase reporter gene assay
111 2 2 2 -0.1 NCCc1cnc[nH]1
CHEMBL90 hrh3_human Human Yes 8.3 EC50 = 5.0 nM Funct
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
111 2 2 2 -0.1 NCCc1cnc[nH]1
CHEMBL392573 hrh3_rat Rat No 8.3 EC50 = 5.0 nM Funct
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
385 4 0 5 4.6 Cc1cc2ncc(-c3ccc4cc(CCN5CCC[C@H]5C)ccc4n3)c(C)n2n1
CHEMBL1951055 hrh3_human Human No 8.3 EC50 = 5.5 nM Funct
Inverse agonist activity at histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgamma bindingInverse agonist activity at histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgamma binding
346 8 0 5 2.5 C[C@@H]1CCCN1CCCOc1ccc(C(=O)CN2CCOCC2)cc1
CHEMBL4176601 hrh3_human Human No 8.3 EC50 = 5.6 nM Funct
Agonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assayAgonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assay
578 7 1 6 6.0 COc1cc(NC2(c3ccc(Br)cc3)C(=O)N(C(C)(C)C)C(=O)/C2=C/c2ccccc2)cc(OC)c1OC
CHEMBL4176601 hrh3_human Human No 8.2 EC50 = 5.7 nM Funct
Agonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assayAgonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assay
578 7 1 6 6.0 COc1cc(NC2(c3ccc(Br)cc3)C(=O)N(C(C)(C)C)C(=O)/C2=C/c2ccccc2)cc(OC)c1OC
CHEMBL442242 hrh3_rat Rat No 8.2 EC50 = 5.8 nM Funct
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
334 4 0 4 4.0 Cc1nn(C)cc1-c1ccc2cc(CCN3CCC[C@H]3C)ccc2n1
CHEMBL442242 hrh3_rat Rat No 8.2 EC50 = 5.8 nM Funct
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
334 4 0 4 4.0 Cc1nn(C)cc1-c1ccc2cc(CCN3CCC[C@H]3C)ccc2n1
CHEMBL1096431 hrh3_human Human No 8.2 EC50 = 5.9 nM Bind
Activity at human recombinant histamine H3 receptor expressed in Sf9 cells coexpressing Galphai, Gbeta1gamma2 and RGS4 by steady-state GTPase activity assayActivity at human recombinant histamine H3 receptor expressed in Sf9 cells coexpressing Galphai, Gbeta1gamma2 and RGS4 by steady-state GTPase activity assay
319 7 4 3 2.6 C[C@@H](CC(=O)NC(=N)NCCCc1c[nH]cn1)C1CCCCC1
CHEMBL13795 hrh3_human Human Yes 8.2 EC50 = 5.9 nM Bind
Inhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H3 receptorInhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H3 receptor
123 1 2 2 0.2 N[C@H]1C[C@@H]1c1c[nH]cn1
CHEMBL203390 hrh3_human Human No 7.3 EC50 = 50.1 nM Funct
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
235 6 1 2 3.0 c1nc(CCCCCN2CCCCCC2)c[nH]1
CHEMBL205868 hrh3_human Human No 7.3 EC50 = 50.1 nM Funct
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
221 5 1 2 2.6 c1nc(CCCCN2CCCCCC2)c[nH]1
CHEMBL175800 hrh3_human Human Yes 7.3 EC50 = 50.1 nM Funct
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
193 3 1 2 1.7 CN1CCC(CCc2c[nH]cn2)CC1
CHEMBL177612 hrh3_human Human No 7.3 EC50 = 50.1 nM Funct
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
245 2 1 2 3.2 C(=C1CCN(C2CCCCC2)CC1)c1c[nH]cn1
CHEMBL1257608 hrh3_human Human No 7.3 EC50 = 51 nM Funct
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
385 6 0 5 3.0 COCCN1CCn2c(cc3cc(OC4CCN(C(C)C)CC4)ccc32)C1=O
CHEMBL153207 hrh3_human Human Yes 6.3 EC50 = 512.9 nM Bind
Inhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H3 receptorInhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H3 receptor
179 3 2 2 1.3 c1nc(CCC2CCCNC2)c[nH]1
CHEMBL154529 hrh3_human Human No 6.3 EC50 = 512.9 nM Bind
Inhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H3 receptorInhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H3 receptor
193 4 2 2 1.7 c1nc(CCCC2CCCNC2)c[nH]1
CHEMBL522555 hrh3_human Human No 7.3 EC50 = 54 nM Bind
Inverse agonist activity at human histamine H3 receptor expressed in CHO cells by GTPgamma[35S] binding assayInverse agonist activity at human histamine H3 receptor expressed in CHO cells by GTPgamma[35S] binding assay
371 6 1 4 2.9 O=C(c1cc2cc(OCCCN3CCCCC3)ccc2[nH]1)N1CCOCC1
CHEMBL1243333 hrh3_human Human No 6.3 EC50 = 540 nM Funct
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
343 5 2 3 4.6 CC(C)(C)c1ccc(SCC(c2c[nH]cn2)C2CCNCC2)cc1
CHEMBL3806206 hrh3_human Human No 6.3 EC50 = 547 nM Funct
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
246 3 3 3 0.9 CN/C(=N\C#N)NC[C@@H]1CC[C@H](c2c[nH]cn2)C1
CHEMBL1257607 hrh3_human Human No 7.3 EC50 = 56 nM Funct
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
371 5 1 5 2.3 CC(C)N1CCC(Oc2ccc3c(c2)cc2n3CCN(CCO)C2=O)CC1
CHEMBL13559 hrh3_human Human Yes 7.2 EC50 = 57.5 nM Bind
Inhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H3 receptorInhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H3 receptor
123 1 2 2 0.2 N[C@@H]1C[C@H]1c1c[nH]cn1
CHEMBL3806255 hrh3_human Human No 6.2 EC50 = 578 nM Funct
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
288 5 3 3 2.0 CC(C)CN/C(=N/C#N)NC[C@H]1CC[C@H](c2c[nH]cn2)C1
CHEMBL495611 hrh3_human Human No 8.2 EC50 = 6 nM Bind
Inverse agonist activity at human histamine H3 receptor expressed in CHO cells by GTPgamma[35S] binding assayInverse agonist activity at human histamine H3 receptor expressed in CHO cells by GTPgamma[35S] binding assay
385 3 1 4 3.3 CC(C)(C)N1CCC(Oc2ccc3[nH]c(C(=O)N4CCOCC4)cc3c2)CC1
CHEMBL497025 hrh3_human Human No 8.2 EC50 = 6 nM Bind
Inverse agonist activity at human histamine H3 receptor expressed in CHO cells by GTPgamma[35S] binding assayInverse agonist activity at human histamine H3 receptor expressed in CHO cells by GTPgamma[35S] binding assay
419 4 1 5 2.3 CC(C)N1CCC(Oc2ccc3[nH]c(C(=O)N4CCS(=O)(=O)CC4)cc3c2)CC1
CHEMBL4165167 hrh3_human Human No 8.2 EC50 = 6.6 nM Funct
Agonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assayAgonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assay
746 11 1 8 7.1 COC1=CC2(C=C(OC)C1=O)C(c1ccccc1)=C(c1ccc(C(F)(F)F)cc1)C(=O)N2C(C(=O)NC1CCCCC1)c1ccc(OC)c(OC)c1OC
CHEMBL4165167 hrh3_human Human No 8.2 EC50 = 6.7 nM Funct
Agonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assayAgonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assay
746 11 1 8 7.1 COC1=CC2(C=C(OC)C1=O)C(c1ccccc1)=C(c1ccc(C(F)(F)F)cc1)C(=O)N2C(C(=O)NC1CCCCC1)c1ccc(OC)c(OC)c1OC
CHEMBL311473 hrh3_human Human Yes 8.2 EC50 = 6.8 nM Bind
Inhibition of the cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H3 receptorInhibition of the cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H3 receptor
173 3 1 2 1.6 c1cc(CCc2c[nH]cn2)ccn1
CHEMBL81644 hrh3_human Human Yes 6.2 EC50 = 602.6 nM Bind
Inhibition of the cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H3 receptorInhibition of the cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H3 receptor
159 2 1 2 1.4 c1ccc(Cc2c[nH]cn2)nc1
CHEMBL4167482 hrh3_human Human No 7.2 EC50 = 61.7 nM Funct
Agonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assayAgonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assay
544 8 1 5 5.6 COc1cc(N2C(=O)/C(=C\c3ccccc3)C2(C(=O)NC2CCCCC2)c2ccc(F)cc2)cc(OC)c1OC
CHEMBL90 hrh3_rat Rat Yes 7.2 EC50 = 62 nM Funct
Compound was evaluated for antagonistic effect on release of [3H]histamine from rat brain cortical slices with L-[3H]histidine at 0.3 uMCompound was evaluated for antagonistic effect on release of [3H]histamine from rat brain cortical slices with L-[3H]histidine at 0.3 uM
111 2 2 2 -0.1 NCCc1cnc[nH]1
CHEMBL4461302 hrh3_human Human No 7.2 EC50 = 63.1 nM Funct
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
221 3 1 5 0.4 CCc1cc(N2CC(N(C)C)C2)nc(N)n1
CHEMBL90 hrh3_human Human Yes 7.2 EC50 = 63.1 nM Funct
Agonist activity at human H3R expressed on HEK293T cells by [35S]GTPgammaS binding assayAgonist activity at human H3R expressed on HEK293T cells by [35S]GTPgammaS binding assay
111 2 2 2 -0.1 NCCc1cnc[nH]1
CHEMBL368774 hrh3_human Human No 7.2 EC50 = 63.1 nM Funct
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
205 2 1 2 2.3 CC(C)N1CCC(=Cc2c[nH]cn2)CC1
CHEMBL446011 hrh3_human Human Yes 6.2 EC50 = 631.0 nM Funct
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
236 2 1 1 2.8 Brc1ccc(Cc2c[nH]cn2)cc1
CHEMBL90 hrh3_human Human Yes 6.2 EC50 = 640 nM Funct
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
111 2 2 2 -0.1 NCCc1cnc[nH]1
CHEMBL1098527 hrh3_human Human No 7.2 EC50 = 65 nM Funct
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
234 5 1 3 2.8 COc1ccc(SCCc2c[nH]cn2)cc1
CHEMBL1243365 hrh3_human Human No 7.2 EC50 = 67 nM Funct
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
349 5 1 3 4.7 FC(F)(F)c1ccc(SCC(c2cccnc2)c2c[nH]cn2)cc1
CHEMBL496080 hrh3_human Human No 8.2 EC50 = 7 nM Bind
Inverse agonist activity at human histamine H3 receptor expressed in CHO cells by GTPgamma[35S] binding assayInverse agonist activity at human histamine H3 receptor expressed in CHO cells by GTPgamma[35S] binding assay
447 4 0 5 4.4 CC(=O)n1c(C(=O)N2CCC(F)(F)CC2)cc2cc(OC3CCN(C(C)C)CC3)ccc21
CHEMBL263101 hrh3_rat Rat No 8.1 EC50 = 7.2 nM Funct
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
382 4 0 4 5.2 Cc1nc2ncccc2cc1-c1ccc2cc(CCN3CCC[C@H]3C)ccc2n1
CHEMBL263101 hrh3_rat Rat No 8.1 EC50 = 7.2 nM Funct
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
382 4 0 4 5.2 Cc1nc2ncccc2cc1-c1ccc2cc(CCN3CCC[C@H]3C)ccc2n1
CHEMBL90019 hrh3_human Human Yes 8.1 EC50 = 7.4 nM Bind
Inhibition of the cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H3 receptorInhibition of the cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H3 receptor
139 4 2 2 0.7 NCCCCc1cnc[nH]1
CHEMBL90019 hrh3_human Human Yes 8.1 EC50 = 7.4 nM Bind
Inhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H3 receptorInhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H3 receptor
139 4 2 2 0.7 NCCCCc1cnc[nH]1
CHEMBL325327 hrh3_human Human Yes 8.1 EC50 = 7.6 nM Bind
Agonist activity at human H3 receptor expressed in insect Sf9 cells co-expressing Gialpha2, Gbeta1gamma2 and RGS4 assessed as gamma[32P]GTP binding by liquid scintillation countingAgonist activity at human H3 receptor expressed in insect Sf9 cells co-expressing Gialpha2, Gbeta1gamma2 and RGS4 assessed as gamma[32P]GTP binding by liquid scintillation counting
167 4 4 2 -0.2 N=C(N)NCCCc1c[nH]cn1
CHEMBL1172775 hrh3_human Human No 8.1 EC50 = 7.6 nM Funct
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
271 4 1 3 2.9 COc1ccc(N2CCC(Cc3c[nH]cn3)CC2)cc1
CHEMBL205834 hrh3_human Human No 8.1 EC50 = 7.9 nM Funct
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
209 8 2 2 2.4 CC(C)CNCCCCCc1c[nH]cn1
CHEMBL4555457 hrh3_human Human No 8.1 EC50 = 7.9 nM Funct
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
221 4 1 5 0.6 CCN(CC)C1CN(c2ccnc(N)n2)C1
CHEMBL4596532 hrh3_human Human No 8.1 EC50 = 7.9 nM Funct
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
221 4 1 5 0.6 CCN(CC)C1CN(c2ccnc(N)n2)C1
CHEMBL4539015 hrh3_human Human No 8.1 EC50 = 7.9 nM Funct
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
219 2 1 5 0.3 Nc1nccc(N2CC(N3CCCC3)C2)n1
CHEMBL4597818 hrh3_human Human No 8.1 EC50 = 7.9 nM Funct
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
219 2 1 5 0.3 Nc1nccc(N2CC(N3CCCC3)C2)n1
CHEMBL493014 hrh3_human Human No 8.1 EC50 = 7.9 nM Funct
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
238 2 1 1 3.4 CC(C)(C)C#Cc1cccc(Cc2c[nH]cn2)c1
CHEMBL176105 hrh3_human Human No 8.1 EC50 = 7.9 nM Funct
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
207 3 1 2 2.1 CC(C)N1CCC(Cc2c[nH]cn2)CC1
CHEMBL179873 hrh3_human Human No 8.1 EC50 = 7.9 nM Funct
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
269 5 1 2 2.9 c1ccc(CCN2CCC(Cc3c[nH]cn3)CC2)cc1
CHEMBL3220121 hrh3_human Human No 8.1 EC50 = 7.9 nM Funct
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
356 6 0 4 4.4 c1cc(C2=NC3(CCCCC3)CO2)ccc1OCCCN1CCCCC1
CHEMBL3745760 hrh3_human Human No 7.1 EC50 = 72 nM Funct
Antagonist activity at human recombinant histamine H3 receptor expressed in HEK293 cells assessed as inhibition of forskolin/(R)(-)-alpha-methylhistamine-induced cAMP accumulation after 1 hr by TR-FRET immunoassayAntagonist activity at human recombinant histamine H3 receptor expressed in HEK293 cells assessed as inhibition of forskolin/(R)(-)-alpha-methylhistamine-induced cAMP accumulation after 1 hr by TR-FRET immunoassay
295 7 0 2 4.6 CC1CCCN(CCCCCOc2ccc(Cl)cc2)C1
CHEMBL3747892 hrh3_human Human No 7.1 EC50 = 72 nM Funct
Antagonist activity at human recombinant histamine H3 receptor expressed in HEK293 cells assessed as inhibition of forskolin/(R)(-)-alpha-methylhistamine-induced cAMP accumulation after 1 hr by TR-FRET immunoassayAntagonist activity at human recombinant histamine H3 receptor expressed in HEK293 cells assessed as inhibition of forskolin/(R)(-)-alpha-methylhistamine-induced cAMP accumulation after 1 hr by TR-FRET immunoassay
295 7 0 2 4.6 CC1CCCN(CCCCCOc2ccc(Cl)cc2)C1
CHEMBL1078642 hrh3_human Human Yes 6.1 EC50 = 720 nM Funct
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
342 9 3 4 2.5 C1=CC=C(C=C1)SCCNC(=NCCCCC2=CN=CN2)NC#N
CHEMBL13559 hrh3_human Human Yes 6.1 EC50 = 724 nM Bind
Inhibition of human Histamine H3 receptor using [3H]N-alpha-methyl histamineInhibition of human Histamine H3 receptor using [3H]N-alpha-methyl histamine
123 1 2 2 0.2 N[C@@H]1C[C@H]1c1c[nH]cn1
CHEMBL1243395 hrh3_human Human No 7.1 EC50 = 74 nM Funct
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
355 5 2 3 4.3 FC(F)(F)c1ccc(SC[C@@H](c2c[nH]cn2)C2CCNCC2)cc1
CHEMBL1258193 hrh3_human Human No 7.1 EC50 = 74 nM Funct
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
327 5 1 4 2.6 O=C1NCCn2c1cc1cc(OCCCN3CCCCC3)ccc12
CHEMBL3747062 hrh3_human Human No 7.1 EC50 = 75 nM Funct
Antagonist activity at human recombinant histamine H3 receptor expressed in HEK293 cells assessed as inhibition of forskolin/(R)(-)-alpha-methylhistamine-induced cAMP accumulation after 1 hr by TR-FRET immunoassayAntagonist activity at human recombinant histamine H3 receptor expressed in HEK293 cells assessed as inhibition of forskolin/(R)(-)-alpha-methylhistamine-induced cAMP accumulation after 1 hr by TR-FRET immunoassay
309 9 0 2 5.2 Clc1ccc(OCCCCCCCN2CCCCC2)cc1
CHEMBL3747907 hrh3_human Human No 7.1 EC50 = 75 nM Funct
Antagonist activity at human recombinant histamine H3 receptor expressed in HEK293 cells assessed as inhibition of forskolin/(R)(-)-alpha-methylhistamine-induced cAMP accumulation after 1 hr by TR-FRET immunoassayAntagonist activity at human recombinant histamine H3 receptor expressed in HEK293 cells assessed as inhibition of forskolin/(R)(-)-alpha-methylhistamine-induced cAMP accumulation after 1 hr by TR-FRET immunoassay
309 9 0 2 5.2 Clc1ccc(OCCCCCCCN2CCCCC2)cc1
CHEMBL90 hrh3_human Human Yes 7.1 EC50 = 77 nM Bind
Inhibition of human Histamine H3 receptor using [3H]N-alpha-methyl histamineInhibition of human Histamine H3 receptor using [3H]N-alpha-methyl histamine
111 2 2 2 -0.1 NCCc1cnc[nH]1
CHEMBL321920 hrh3_human Human No 6.1 EC50 = 776.3 nM Funct
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
167 2 2 3 0.6 NC[C@@H]1CC[C@H](c2c[nH]cn2)O1
CHEMBL4452204 hrh3_human Human No 7.1 EC50 = 79.4 nM Funct
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
207 2 2 5 0.3 CC(C)c1cc(N2CC(N)C2)nc(N)n1
CHEMBL455266 hrh3_human Human No 7.1 EC50 = 79.4 nM Funct
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
317 5 1 3 3.4 c1ccc(C[C@@H]2COC(c3cccc(Cc4c[nH]cn4)c3)=N2)cc1
CHEMBL489493 hrh3_human Human No 7.1 EC50 = 79.4 nM Funct
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
256 4 1 2 3.6 CC(C)(C)CC(=O)c1cccc(Cc2c[nH]cn2)c1
CHEMBL179747 hrh3_human Human No 7.1 EC50 = 79.4 nM Funct
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
253 3 1 2 3.1 C(=C1CCN(Cc2ccccc2)CC1)c1c[nH]cn1
CHEMBL3220123 hrh3_human Human No 7.1 EC50 = 79.4 nM Funct
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
368 4 0 4 4.6 c1cc(C2=NC3(CCCCC3)CO2)ccc1O[C@H]1C[C@@H](N2CCCCC2)C1
CHEMBL106913 hrh3_human Human No 6.1 EC50 = 794.3 nM Funct
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
167 2 2 3 0.6 NC[C@H]1CC[C@@H](c2c[nH]cn2)O1
CHEMBL321920 hrh3_human Human No 6.1 EC50 = 794.3 nM Funct
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
167 2 2 3 0.6 NC[C@@H]1CC[C@H](c2c[nH]cn2)O1
CHEMBL150703 hrh3_human Human Yes 6.1 EC50 = 794.3 nM Bind
Inhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H3 receptorInhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H3 receptor
165 2 2 2 1.1 c1nc(CC2CCCCN2)c[nH]1
CHEMBL78498 hrh3_human Human Yes 8.1 EC50 = 8.3 nM Bind
Inhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H3 receptorInhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H3 receptor
193 4 2 2 1.7 c1nc(CCCC2CCNCC2)c[nH]1
CHEMBL1172753 hrh3_human Human No 8.1 EC50 = 8.8 nM Funct
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
286 4 1 4 2.8 O=[N+]([O-])c1ccc(N2CCC(Cc3c[nH]cn3)CC2)cc1
CHEMBL106913 hrh3_human Human No 6.1 EC50 = 812.8 nM Funct
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
167 2 2 3 0.6 NC[C@H]1CC[C@@H](c2c[nH]cn2)O1
CHEMBL3805003 hrh3_human Human No 6.1 EC50 = 858 nM Funct
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
288 5 3 3 2.0 CC(C)CN/C(=N/C#N)NC[C@@H]1CC[C@H](c2c[nH]cn2)C1
CHEMBL90 hrh3_human Human Yes 7.1 EC50 = 88 nM Funct
Agonist activity at human H3 receptor expressed in 293-EBNA cells by luciferase reporter gene assayAgonist activity at human H3 receptor expressed in 293-EBNA cells by luciferase reporter gene assay
111 2 2 2 -0.1 NCCc1cnc[nH]1
CHEMBL4470780 hrh3_human Human No 7.1 EC50 = 88 nM Bind
Agonist activity at human H3 receptor expressed in CHOK1 cells incubated for 10 mins by HTRF assayAgonist activity at human H3 receptor expressed in CHOK1 cells incubated for 10 mins by HTRF assay
1291 32 4 17 8.1 Cc1nn(CCOCCOCCNC(=O)CCCCCC2(C)C(/C=C/C=C/C=C3/N(CCCS(=O)(=O)O)c4ccc(S(=O)(=O)O)cc4C3(C)C)=[N+](CCCS(=O)(=O)[O-])c3ccc(S(=O)(=O)O)cc32)cc1-c1ccc2cc(CCN3CCC[C@H]3C)ccc2n1
CHEMBL1096515 hrh3_human Human Yes 7.1 EC50 = 88 nM Funct
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
201 4 2 2 2.4 Cc1ccc(NCCc2c[nH]cn2)cc1
CHEMBL520148 hrh3_human Human No 8.1 EC50 = 9 nM Bind
Inverse agonist activity at human histamine H3 receptor expressed in CHO cells by GTPgamma[35S] binding assayInverse agonist activity at human histamine H3 receptor expressed in CHO cells by GTPgamma[35S] binding assay
467 5 0 6 2.9 O=C(c1cc2cc(OC3CCN(C4COC4)CC3)ccc2n1CC(F)(F)F)N1CCOCC1
CHEMBL522236 hrh3_human Human No 8.1 EC50 = 9 nM Bind
Inverse agonist activity at human histamine H3 receptor expressed in CHO cells by GTPgamma[35S] binding assayInverse agonist activity at human histamine H3 receptor expressed in CHO cells by GTPgamma[35S] binding assay
399 5 1 4 3.7 COC1CCN(C(=O)c2cc3cc(OC4CCN(C(C)C)CC4)ccc3[nH]2)CC1
CHEMBL488248 hrh3_mouse Mouse No 8.0 EC50 = 9.6 nM Funct
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
363 6 0 5 3.5 Cn1c(-c2ccc(OCCCN3CCCC3)cc2)nc2ccccc2c1=O
CHEMBL557214 hrh3_mouse Mouse No 8.0 EC50 = 9.6 nM Funct
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
363 6 0 5 3.5 Cn1c(-c2ccc(OCCCN3CCCC3)cc2)nc2ccccc2c1=O
CHEMBL90 hrh3_human Human Yes 8.0 EC50 = 9.8 nM Bind
Inhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H3 receptorInhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H3 receptor
111 2 2 2 -0.1 NCCc1cnc[nH]1
CHEMBL1083162 hrh3_human Human No 5.1 EC50 = 9000 nM Bind
Displacement of [125H]iodoproxyphan from human recombinant histamine H3 receptor expressed in human SK-N-MC cellsDisplacement of [125H]iodoproxyphan from human recombinant histamine H3 receptor expressed in human SK-N-MC cells
407 9 3 4 4.3 Cc1cc(OCCCNCCc2c[nH]cn2)ccc1-c1nc2c(C)c(F)ccc2[nH]1
CHEMBL105803 hrh3_human Human No 7.0 EC50 = 91.2 nM Funct
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
258 5 1 3 2.8 c1ccc(COC[C@H]2CC[C@H](c3c[nH]cn3)O2)cc1
CHEMBL79126 hrh3_human Human Yes 6.0 EC50 = 912.0 nM Bind
Inhibition of the cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H3 receptorInhibition of the cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H3 receptor
187 4 1 2 2.0 c1ccc(CCCc2c[nH]cn2)nc1
CHEMBL3805437 hrh3_human Human No 5.0 EC50 = 9200 nM Funct
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
246 3 3 3 0.9 CN/C(=N\C#N)NC[C@@H]1CC[C@@H](c2c[nH]cn2)C1
CHEMBL4166675 hrh3_human Human No 7.0 EC50 = 93.3 nM Funct
Agonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assayAgonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assay
438 2 1 3 3.4 O=C1C=C[C@]23C(c4ccccc4)=CC(=O)N2[C@H](c2ccc(C(F)(F)F)cc2)C(=O)N[C@@H]3C1
CHEMBL4166675 hrh3_human Human No 7.0 EC50 = 94 nM Funct
Agonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assayAgonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assay
438 2 1 3 3.4 O=C1C=C[C@]23C(c4ccccc4)=CC(=O)N2[C@H](c2ccc(C(F)(F)F)cc2)C(=O)N[C@@H]3C1
CHEMBL1257964 hrh3_human Human No 7.0 EC50 = 94 nM Funct
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
341 3 1 4 3.2 CC(C)N1CCC(Oc2ccc3c(c2)cc2n3[C@@H](C)CNC2=O)CC1
CHEMBL322256 hrh3_human Human No 5.0 EC50 = 9549.9 nM Funct
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
258 5 1 3 2.8 c1ccc(COC[C@@H]2CC[C@@H](c3c[nH]cn3)O2)cc1
CHEMBL305135 hrh3_human Human No 7.0 EC50 = 96 nM Bind
Inhibition of human Histamine H3 receptor using [3H]N-alpha-methyl histamineInhibition of human Histamine H3 receptor using [3H]N-alpha-methyl histamine
137 2 2 2 0.5 NC[C@@H]1C[C@@H]1c1c[nH]cn1
CHEMBL1179604 hrh3_human Human No 7.0 EC50 = 97 nM Funct
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
196 8 1 2 2.5 CCCCCOCCCc1c[nH]cn1
CHEMBL88746 hrh3_human Human No 7.0 EC50 = 97 nM Funct
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
196 8 1 2 2.5 CCCCCOCCCc1c[nH]cn1
CHEMBL260374 hrh3_human Human Yes 7.0 EC50 = 97.7 nM Bind
Agonist activity at human H3 receptor expressed in insect Sf9 cells co-expressing Gialpha2, Gbeta1gamma2 and RGS4 assessed as gamma[32P]GTP binding by liquid scintillation countingAgonist activity at human H3 receptor expressed in insect Sf9 cells co-expressing Gialpha2, Gbeta1gamma2 and RGS4 assessed as gamma[32P]GTP binding by liquid scintillation counting
292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1
CHEMBL260374 hrh3_human Human Yes 7.0 EC50 = 97.7 nM Funct
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
292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1
CHEMBL1632410 hrh3_human Human No 5.0 EC50 = 9772.4 nM Funct
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
258 5 1 3 2.8 c1ccc(COC[C@H]2CC[C@@H](c3c[nH]cn3)O2)cc1
CHEMBL3804906 hrh3_human Human No 6.0 EC50 = 994 nM Funct
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
246 3 3 3 0.9 CN/C(=N\C#N)NC[C@H]1CC[C@H](c2c[nH]cn2)C1
CHEMBL2387288 hrh3_human Human No 10.0 IC50 = 0.1 nM Funct
Antagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of calcium mobilization by FLIPR assay
384 5 2 4 4.1 CC1CCCN1C1CCN(c2ccc(NC(=O)NCc3cccs3)cc2)C1
CHEMBL2387314 hrh3_human Human No 10.0 IC50 = 0.1 nM Funct
Antagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of calcium mobilization by FLIPR assay
370 4 2 3 4.2 CC1CCCN1C1CCN(c2ccc(NC(=O)NC3CCCCC3)cc2)C1
CHEMBL508712 hrh3_human Human No 10.0 IC50 = 0.1 nM Funct
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
403 4 0 5 4.3 Cc1cccc2c(=O)n(C)c(-c3ccc(OC4CCN(C5CCC5)CC4)cc3)nc12
CHEMBL550517 hrh3_human Human No 9.8 IC50 = 0.2 nM Funct
Inverse agonist activity at human cloned histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding by cell-based assayInverse agonist activity at human cloned histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding by cell-based assay
459 7 0 6 4.5 COc1cccc2c1OC(c1ccc(OCCCN3CCC[C@H](C)C3)cc1)C(C)S2(=O)=O
CHEMBL562870 hrh3_human Human No 9.8 IC50 = 0.2 nM Funct
Inverse agonist activity at human cloned histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding by cell-based assayInverse agonist activity at human cloned histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding by cell-based assay
457 5 0 6 4.4 COc1cccc2c1OC(c1ccc(OC3CCN(C4CCC4)CC3)cc1)C(C)S2(=O)=O
CHEMBL453893 hrh3_human Human No 9.7 IC50 = 0.2 nM Funct
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
423 4 0 5 4.7 Cn1c(-c2ccc(OC3CCN(C4CCC4)CC3)cc2)nc2c(Cl)cccc2c1=O
CHEMBL1222499 hrh3_human Human No 9.7 IC50 = 0.2 nM Funct
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
482 7 0 8 3.9 Cc1nccn1-c1ccc(C(c2nnnn2Cc2ccccc2)N2CCCN(C3CCC3)CC2)cc1
CHEMBL2387289 hrh3_human Human No 9.7 IC50 = 0.2 nM Funct
Antagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of calcium mobilization by FLIPR assay
398 5 2 4 4.4 Cc1cc(NC(=O)NCc2cccs2)ccc1N1CCC(N2CCCC2C)C1
CHEMBL2387290 hrh3_human Human No 9.7 IC50 = 0.2 nM Funct
Antagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of calcium mobilization by FLIPR assay
446 5 2 3 5.4 CC1CCCN1C1CCN(c2ccc(NC(=O)NCc3cc(Cl)cc(Cl)c3)cc2)C1
CHEMBL2387307 hrh3_human Human No 9.7 IC50 = 0.2 nM Funct
Antagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of calcium mobilization by FLIPR assay
435 7 2 3 6.2 Cc1c(Cl)cc(NC(=O)Nc2ccc(OCCCN3CCCCC3)cc2)cc1Cl
CHEMBL2387315 hrh3_human Human No 9.7 IC50 = 0.2 nM Funct
Antagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of calcium mobilization by FLIPR assay
384 4 2 3 4.5 Cc1cc(N2CCC(N3CCCC3C)C2)ccc1NC(=O)NC1CCCCC1
CHEMBL2387316 hrh3_human Human No 9.7 IC50 = 0.2 nM Funct
Antagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of calcium mobilization by FLIPR assay
384 4 2 3 4.5 Cc1cc(NC(=O)NC2CCCCC2)ccc1N1CCC(N2CCCC2C)C1
CHEMBL2387317 hrh3_human Human No 9.7 IC50 = 0.2 nM Funct
Antagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of calcium mobilization by FLIPR assay
371 3 1 4 2.5 CC1CCCN1C1CCN(c2ccc(NC(=O)N3CCN(C)CC3)cc2)C1
CHEMBL560863 hrh3_human Human No 9.7 IC50 = 0.2 nM Funct
Inverse agonist activity at human cloned histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding by cell-based assayInverse agonist activity at human cloned histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding by cell-based assay
445 7 0 6 4.2 COc1cccc2c1OC(c1ccc(OCCCN3CCC[C@H]3C)cc1)C(C)S2(=O)=O
CHEMBL488249 hrh3_human Human No 9.7 IC50 = 0.2 nM Funct
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
389 4 0 5 4.0 Cn1c(-c2ccc(OC3CCN(C4CCC4)CC3)cc2)nc2ccccc2c1=O
CHEMBL454642 hrh3_human Human No 9.6 IC50 = 0.3 nM Funct
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
407 4 0 5 4.1 Cn1c(-c2ccc(OC3CCN(C4CCC4)CC3)cc2)nc2c(F)cccc2c1=O
CHEMBL484946 hrh3_human Human No 9.6 IC50 = 0.3 nM Funct
Antagonist activity at human cloned histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS bindingAntagonist activity at human cloned histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding
403 4 0 5 4.4 Cc1cccc2nc(C)n(-c3ccc(OC4CCN(C5CCC5)CC4)cc3)c(=O)c12
CHEMBL1223513 hrh3_human Human No 9.5 IC50 = 0.3 nM Funct
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
521 8 1 7 4.6 O=C(Nc1ccccc1)c1ccc(C(c2nnnn2Cc2ccccc2)N2CCCN(C3CCC3)CC2)cc1
CHEMBL2387285 hrh3_human Human No 9.5 IC50 = 0.3 nM Funct
Antagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of calcium mobilization by FLIPR assay
356 3 1 3 3.8 CC1CCCN1C1CCN(c2ccc(NC(=O)N3CCCCC3)cc2)C1
CHEMBL453654 hrh3_human Human No 9.5 IC50 = 0.3 nM Funct
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
419 5 0 6 4.0 COc1ccc2nc(-c3ccc(OC4CCN(C5CCC5)CC4)cc3)n(C)c(=O)c2c1
CHEMBL487059 hrh3_human Human No 9.5 IC50 = 0.3 nM Funct
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
453 8 0 5 5.4 O=c1c2ccccc2nc(-c2ccc(OCCCN3CCCCC3)cc2)n1Cc1ccccc1
CHEMBL507360 hrh3_human Human Yes 9.5 IC50 = 0.3 nM Funct
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
420 5 0 7 3.4 COc1nccc2c(=O)n(C)c(-c3ccc(OC4CCN(C5CCC5)CC4)cc3)nc12
CHEMBL4740154 hrh3_human Human No 9.5 IC50 = 0.3 nM Funct
Antagonist activity at human H3 receptor expressed in HEK293 cells centrifuged for 3 mins followed by 60 mins incubation by LANCE Ultra cAMP assayAntagonist activity at human H3 receptor expressed in HEK293 cells centrifuged for 3 mins followed by 60 mins incubation by LANCE Ultra cAMP assay
234 5 1 4 0.8 C#CCN(C)CCCn1ccc(=O)c(O)c1C
CHEMBL561324 hrh3_human Human No 9.5 IC50 = 0.3 nM Funct
Inverse agonist activity at human cloned histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding by cell-based assayInverse agonist activity at human cloned histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding by cell-based assay
431 7 0 6 3.9 COc1ccc2c(c1)OC(c1ccc(OCCCN3CCCC3)cc1)C(C)S2(=O)=O
CHEMBL485543 hrh3_human Human No 9.5 IC50 = 0.3 nM Funct
Antagonist activity at human cloned histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS bindingAntagonist activity at human cloned histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding
457 4 0 5 5.1 Cc1nc2cccc(C(F)(F)F)c2c(=O)n1-c1ccc(OC2CCN(C3CCC3)CC2)cc1
CHEMBL458176 hrh3_human Human No 9.5 IC50 = 0.3 nM Funct
Antagonist activity at human cloned histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS bindingAntagonist activity at human cloned histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding
423 4 0 5 4.7 Cc1nc2cccc(Cl)c2c(=O)n1-c1ccc(OC2CCN(C3CCC3)CC2)cc1
CHEMBL550050 hrh3_human Human No 9.5 IC50 = 0.3 nM Funct
Inverse agonist activity at human cloned histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding by cell-based assayInverse agonist activity at human cloned histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding by cell-based assay
445 7 0 6 4.2 COc1cccc2c1OC(c1ccc(OCCCN3CCCCC3)cc1)C(C)S2(=O)=O
CHEMBL454879 hrh3_human Human No 9.5 IC50 = 0.3 nM Funct
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
419 5 0 6 4.0 COc1ccc2c(=O)n(C)c(-c3ccc(OC4CCN(C5CCC5)CC4)cc3)nc2c1
CHEMBL562722 hrh3_human Human No 9.4 IC50 = 0.4 nM Funct
Inverse agonist activity at human cloned histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding by cell-based assayInverse agonist activity at human cloned histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding by cell-based assay
431 7 0 6 3.9 COc1cccc2c1OC(c1ccc(OCCCN3CCCC3)cc1)C(C)S2(=O)=O
CHEMBL1222501 hrh3_human Human No 9.4 IC50 = 0.4 nM Funct
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
499 7 0 8 4.8 Cc1nc(-c2ccc(C(c3nnnn3Cc3ccccc3)N3CCCN(C4CCC4)CC3)cc2)cs1
CHEMBL1223158 hrh3_human Human No 9.4 IC50 = 0.4 nM Funct
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
514 8 0 8 3.1 CN1CCN(Cc2ccc(C(c3nnnn3Cc3ccccc3)N3CCCN(C4CCC4)CC3)cc2)CC1
CHEMBL2387284 hrh3_human Human No 9.4 IC50 = 0.4 nM Funct
Antagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of calcium mobilization by FLIPR assay
433 4 1 4 4.1 CC1CCCN1C1CCN(c2ccc(NC(=O)N3CCN(c4ccccc4)CC3)cc2)C1
CHEMBL1223158 hrh3_rat Rat No 9.4 IC50 = 0.4 nM Funct
Antagonist activity at rat histamine H3 receptorAntagonist activity at rat histamine H3 receptor
514 8 0 8 3.1 CN1CCN(Cc2ccc(C(c3nnnn3Cc3ccccc3)N3CCCN(C4CCC4)CC3)cc2)CC1
CHEMBL565007 hrh3_human Human No 9.4 IC50 = 0.4 nM Funct
Inverse agonist activity at human cloned histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding by cell-based assayInverse agonist activity at human cloned histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding by cell-based assay
431 7 0 6 3.9 COc1ccc2c(c1)S(=O)(=O)C(C)C(c1ccc(OCCCN3CCCC3)cc1)O2
CHEMBL560386 hrh3_human Human No 9.4 IC50 = 0.4 nM Funct
Inverse agonist activity at human cloned histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding by cell-based assayInverse agonist activity at human cloned histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding by cell-based assay
431 7 0 6 3.9 COc1cccc2c1O[C@@H](c1ccc(OCCCN3CCCC3)cc1)[C@H](C)S2(=O)=O
CHEMBL549639 hrh3_human Human No 9.4 IC50 = 0.4 nM Funct
Inverse agonist activity at human cloned histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding by cell-based assayInverse agonist activity at human cloned histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding by cell-based assay
431 7 0 6 3.9 COc1cccc2c1S(=O)(=O)C(C)C(c1ccc(OCCCN3CCCC3)cc1)O2
CHEMBL4752329 hrh3_human Human No 9.3 IC50 = 0.5 nM Funct
Antagonist activity at human histamine H3 receptor expressed in HEK293 cells preincubated for 5 mins followed by forskolin-stimulation and measured after 5 hrs by CRE-driven luciferase reporter gene assayAntagonist activity at human histamine H3 receptor expressed in HEK293 cells preincubated for 5 mins followed by forskolin-stimulation and measured after 5 hrs by CRE-driven luciferase reporter gene assay
368 5 0 5 3.6 COc1cn(-c2ccc(OC3CCN(C4CCCC4)CC3)cc2)ccc1=O
CHEMBL487230 hrh3_human Human No 9.3 IC50 = 0.5 nM Funct
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
405 8 0 5 4.7 CCCn1c(-c2ccc(OCCCN3CCCCC3)cc2)nc2ccccc2c1=O
CHEMBL2391151 hrh3_human Human No 9.3 IC50 = 0.5 nM Bind
Antagonist activity at human histamine H3 receptor by FLIPR assayAntagonist activity at human histamine H3 receptor by FLIPR assay
417 4 1 3 5.3 CC1CCCN1C1CCN(c2ccc(NC(=O)c3cc(Cl)cc(Cl)c3)cc2)C1
CHEMBL453892 hrh3_human Human Yes 9.3 IC50 = 0.5 nM Funct
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
419 5 0 6 4.0 COc1cccc2c(=O)n(C)c(-c3ccc(OC4CCN(C5CCC5)CC4)cc3)nc12
CHEMBL1222434 hrh3_human Human No 9.3 IC50 = 0.5 nM Funct
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
500 7 0 8 3.1 CN1CCN(c2ccc(C(c3nnnn3Cc3ccccc3)N3CCCN(C4CCC4)CC3)cc2)CC1
CHEMBL2387282 hrh3_human Human No 9.3 IC50 = 0.5 nM Funct
Antagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of calcium mobilization by FLIPR assay
399 3 1 4 2.4 CC(=O)N1CCN(C(=O)Nc2ccc(N3CCC(N4CCCC4C)C3)cc2)CC1
CHEMBL2387306 hrh3_human Human No 9.3 IC50 = 0.5 nM Funct
Antagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of calcium mobilization by FLIPR assay
421 7 2 3 5.9 O=C(Nc1ccc(OCCCN2CCCCC2)cc1)Nc1cc(Cl)cc(Cl)c1
CHEMBL2387309 hrh3_human Human No 9.3 IC50 = 0.5 nM Funct
Antagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of calcium mobilization by FLIPR assay
389 7 2 3 4.9 O=C(Nc1ccc(OCCCN2CCCCC2)cc1)Nc1ccc(F)cc1F
CHEMBL4748265 hrh3_human Human No 9.3 IC50 = 0.5 nM Funct
Antagonist activity at human histamine H3 receptor expressed in HEK293 cells preincubated for 5 mins followed by forskolin-stimulation and measured after 5 hrs by CRE-driven luciferase reporter gene assayAntagonist activity at human histamine H3 receptor expressed in HEK293 cells preincubated for 5 mins followed by forskolin-stimulation and measured after 5 hrs by CRE-driven luciferase reporter gene assay
328 7 0 5 2.7 COc1cn(-c2ccc(OCCCN3CCCC3)cc2)ccc1=O
CHEMBL129542 hrh3_human Human Yes 9.3 IC50 = 0.5 nM Bind
Inhibition of histamine H3 receptorInhibition of histamine H3 receptor
316 7 0 3 3.9 C1CCN(CC1)CCCOc1ccc(cc1)CN1CCCCC1
CHEMBL513893 hrh3_human Human No 9.3 IC50 = 0.5 nM Funct
Inverse agonist activity at human cloned histamine H3 receptor assessed as inhibition of (R)-alpha-methylhistamine-induced [35S]GTPgammaS bindingInverse agonist activity at human cloned histamine H3 receptor assessed as inhibition of (R)-alpha-methylhistamine-induced [35S]GTPgammaS binding
400 5 0 5 3.2 COc1ccc2c(c1)C(=O)O[C@]21CC[C@H](C(=O)N(C)CCN2CCCCC2)CC1
CHEMBL453653 hrh3_human Human No 9.3 IC50 = 0.5 nM Funct
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
419 5 0 6 4.0 COc1cccc2nc(-c3ccc(OC4CCN(C5CCC5)CC4)cc3)n(C)c(=O)c12
CHEMBL517140 hrh3_human Human Yes 9.3 IC50 = 0.6 nM Funct
Antagonist activity at human cloned histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS bindingAntagonist activity at human cloned histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding
351 4 1 4 3.2 CNC(=O)c1ccc(nc1)Oc1ccc2c(c1)CCN(CC2)C1CCC1
CHEMBL483400 hrh3_human Human No 9.3 IC50 = 0.6 nM Funct
Antagonist activity at human cloned histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS bindingAntagonist activity at human cloned histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding
407 4 0 5 4.2 Cc1nc2cccc(F)c2c(=O)n1-c1ccc(OC2CCN(C3CCC3)CC2)cc1
CHEMBL1222433 hrh3_human Human No 9.2 IC50 = 0.6 nM Funct
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
501 8 0 8 3.2 c1ccc(Cn2nnnc2C(c2ccc(CN3CCOCC3)cc2)N2CCCN(C3CCC3)CC2)cc1
CHEMBL2387293 hrh3_human Human No 9.2 IC50 = 0.6 nM Funct
Antagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of calcium mobilization by FLIPR assay
470 6 2 4 6.5 Cc1cc(NC(=O)Nc2ccc(Oc3ccccc3)cc2)ccc1N1CCC(N2CCCC2C)C1
CHEMBL2387310 hrh3_human Human Yes 9.2 IC50 = 0.6 nM Funct
Antagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of calcium mobilization by FLIPR assay
415 11 2 4 5.3 CCN(CC)CCOc1ccc(NC(=S)Nc2ccc(OCC(C)C)cc2)cc1
CHEMBL558248 hrh3_human Human No 9.2 IC50 = 0.6 nM Funct
Inverse agonist activity at human cloned histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding by cell-based assayInverse agonist activity at human cloned histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding by cell-based assay
401 6 0 5 3.8 C[C@@H]1[C@@H](c2ccc(OCCCN3CCCC3)cc2)Oc2ccccc2S1(=O)=O
CHEMBL562326 hrh3_human Human No 9.2 IC50 = 0.6 nM Funct
Inverse agonist activity at human cloned histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding by cell-based assayInverse agonist activity at human cloned histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding by cell-based assay
401 6 0 5 3.8 CC1C(c2ccc(OCCCN3CCCC3)cc2)Oc2ccccc2S1(=O)=O
CHEMBL557718 hrh3_human Human No 9.2 IC50 = 0.6 nM Funct
Inverse agonist activity at human cloned histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding by cell-based assayInverse agonist activity at human cloned histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding by cell-based assay
431 7 0 6 3.9 COc1cccc2c1O[C@H](c1ccc(OCCCN3CCCC3)cc1)[C@@H](C)S2(=O)=O
CHEMBL351231 hrh3_human Human Yes 9.2 IC50 = 0.6 nM Funct
Antagonist activity at human cloned histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS bindingAntagonist activity at human cloned histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding
330 4 0 3 5.0 N#Cc1ccc(cc1)c1ccc2c(c1)cc(o2)CCN1CCC[C@H]1C
CHEMBL1783890 hrh3_human Human No 9.2 IC50 = 0.6 nM Funct
Inverse agonist activity at human histamine H3 receptor by GTPgammaS binding assayInverse agonist activity at human histamine H3 receptor by GTPgammaS binding assay
352 4 1 5 2.6 CNC(=O)c1cnc(Oc2ccc3c(c2)CCN(C2CCC2)CC3)cn1
CHEMBL2403548 hrh3_human Human No 9.2 IC50 = 0.7 nM Bind
Antagonist activity at human histamine H3 receptor by FLIPR assayAntagonist activity at human histamine H3 receptor by FLIPR assay
395 4 1 3 4.8 Cc1cc(N2CC[C@H](N3CCC[C@H]3C)C2)ccc1NC(=O)c1cc(F)ccc1C
CHEMBL479241 hrh3_human Human No 9.2 IC50 = 0.7 nM Funct
Inverse agonist activity at human histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of N-alpha-methylhistamine-induced [35S]GTPgammaS bindingInverse agonist activity at human histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of N-alpha-methylhistamine-induced [35S]GTPgammaS binding
425 7 0 5 4.9 O=c1c2ccccc2nc(-c2ccccc2)n1-c1ccc(OCCCN2CCCC2)cc1
CHEMBL3427228 hrh3_human Human No 9.2 IC50 = 0.7 nM Funct
HTRF cAMP Assay: Compounds of the present invention were evaluated using the human H3 receptor (H3R) HTRF cAMP assay. In this assay, HEK293 cells expressing the human H3 receptor were suspended in PBS containing 100 μM IBMX and plated into 384-well assay plates (Perkin Elmer Proxiplate 384-Plus; 15,000 cells per well; 5 μL plating volume) and allowed to equilibrate for an hour. Test compounds were serially diluted in 100% DMSO and then further diluted in PBS containing forskolin (2 μM). Test compounds (5 μL) were then added to the assay plate and the mixture was incubated for 1 hour. HTRF assay reagents (Cisbio, Dynamic 2 cAMP Kit), cAMP-d2 and cryptate-labeled anti-cAMP antibody, are mixed with cell lysis buffer and added to the assay plate. After 1-hour incubation with these reagents, the assay plate was read on an HTRF-compatible microplate reader (Perkin Elmer EnVision or BMG Pherastar).HTRF cAMP Assay: Compounds of the present invention were evaluated using the human H3 receptor (H3R) HTRF cAMP assay. In this assay, HEK293 cells expressing the human H3 receptor were suspended in PBS containing 100 μM IBMX and plated into 384-well assay plates (Perkin Elmer Proxiplate 384-Plus; 15,000 cells per well; 5 μL plating volume) and allowed to equilibrate for an hour. Test compounds were serially diluted in 100% DMSO and then further diluted in PBS containing forskolin (2 μM). Test compounds (5 μL) were then added to the assay plate and the mixture was incubated for 1 hour. HTRF assay reagents (Cisbio, Dynamic 2 cAMP Kit), cAMP-d2 and cryptate-labeled anti-cAMP antibody, are mixed with cell lysis buffer and added to the assay plate. After 1-hour incubation with these reagents, the assay plate was read on an HTRF-compatible microplate reader (Perkin Elmer EnVision or BMG Pherastar).
381 9 0 4 4.5 CCOC(=O)COCc1ccc(-c2ccc(CCN3CCC[C@H]3C)cc2)cc1
CHEMBL3427228 hrh3_human Human No 9.2 IC50 = 0.7 nM Funct
Modulation of human histamine H3 receptor expressed in HEK293 cells assessed as change in forskolin-stimulated cAMP level after 1 hr by HTRF assayModulation of human histamine H3 receptor expressed in HEK293 cells assessed as change in forskolin-stimulated cAMP level after 1 hr by HTRF assay
381 9 0 4 4.5 CCOC(=O)COCc1ccc(-c2ccc(CCN3CCC[C@H]3C)cc2)cc1
CHEMBL488248 hrh3_human Human No 9.2 IC50 = 0.7 nM Funct
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
363 6 0 5 3.5 Cn1c(-c2ccc(OCCCN3CCCC3)cc2)nc2ccccc2c1=O
CHEMBL557214 hrh3_human Human No 9.2 IC50 = 0.7 nM Funct
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
363 6 0 5 3.5 Cn1c(-c2ccc(OCCCN3CCCC3)cc2)nc2ccccc2c1=O
CHEMBL515004 hrh3_human Human No 9.2 IC50 = 0.7 nM Funct
Inverse agonist activity at human histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of N-alpha-methylhistamine-induced [35S]GTPgammaS bindingInverse agonist activity at human histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of N-alpha-methylhistamine-induced [35S]GTPgammaS binding
391 8 0 5 4.2 CCCc1nc2ccccc2c(=O)n1-c1ccc(OCCCN2CCCC2)cc1
CHEMBL1222593 hrh3_human Human No 9.2 IC50 = 0.7 nM Funct
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
482 8 0 8 3.6 c1ccc(Cn2nnnc2C(c2ccc(Cn3cccn3)cc2)N2CCCN(C3CCC3)CC2)cc1
CHEMBL2387305 hrh3_human Human No 9.2 IC50 = 0.7 nM Funct
Antagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of calcium mobilization by FLIPR assay
387 7 2 3 5.2 O=C(Nc1ccc(Cl)cc1)Nc1ccc(OCCCN2CCCCC2)cc1
CHEMBL1934523 hrh3_human Human No 9.2 IC50 = 0.7 nM Funct
Inverse agonist activity at human cloned histamine H3 receptor by [35S]GTPgammaS binding assayInverse agonist activity at human cloned histamine H3 receptor by [35S]GTPgammaS binding assay
401 9 0 4 4.2 COCCCS(=O)(=O)c1ccc(-c2ccc(CCN3CCC[C@H]3C)cc2)cc1
CHEMBL453894 hrh3_human Human No 9.2 IC50 = 0.7 nM Funct
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
457 4 0 5 5.0 Cn1c(-c2ccc(OC3CCN(C4CCC4)CC3)cc2)nc2c(C(F)(F)F)cccc2c1=O
CHEMBL2403551 hrh3_human Human No 9.2 IC50 = 0.7 nM Bind
Antagonist activity at human histamine H3 receptor by FLIPR assayAntagonist activity at human histamine H3 receptor by FLIPR assay
395 4 1 3 4.8 Cc1cc(N2CC[C@@H](N3CCC[C@H]3C)C2)ccc1NC(=O)c1cc(F)ccc1C
CHEMBL129306 hrh3_human Human No 9.1 IC50 = 0.7 nM Bind
Inhibition of histamine H3 receptorInhibition of histamine H3 receptor
332 7 1 4 2.9 OC1CCN(Cc2ccc(OCCCN3CCCCC3)cc2)CC1
CHEMBL514217 hrh3_human Human No 9.1 IC50 = 0.7 nM Funct
Inverse agonist activity at human cloned histamine H3 receptor assessed as inhibition of (R)-alpha-methylhistamine-induced [35S]GTPgammaS bindingInverse agonist activity at human cloned histamine H3 receptor assessed as inhibition of (R)-alpha-methylhistamine-induced [35S]GTPgammaS binding
370 4 0 4 3.2 CN(CCN1CCCCC1)C(=O)[C@H]1CC[C@@]2(CC1)OC(=O)c1ccccc12
CHEMBL478395 hrh3_human Human No 9.1 IC50 = 0.7 nM Funct
Inverse agonist activity at human histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of N-alpha-methylhistamine-induced [35S]GTPgammaS bindingInverse agonist activity at human histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of N-alpha-methylhistamine-induced [35S]GTPgammaS binding
391 6 0 5 4.2 Cc1nc2ccccc2c(=O)n1-c1ccc(OCCCN2CCC[C@H](C)C2)cc1
CHEMBL4763867 hrh3_human Human No 9.1 IC50 = 0.7 nM Funct
Antagonist activity at human histamine H3 receptor expressed in HEK293 cells preincubated for 5 mins followed by forskolin-stimulation and measured after 5 hrs by CRE-driven luciferase reporter gene assayAntagonist activity at human histamine H3 receptor expressed in HEK293 cells preincubated for 5 mins followed by forskolin-stimulation and measured after 5 hrs by CRE-driven luciferase reporter gene assay
354 5 0 5 3.2 COc1cn(-c2ccc(OC3CCN(C4CCC4)CC3)cc2)ccc1=O
CHEMBL455681 hrh3_human Human No 9.1 IC50 = 0.7 nM Funct
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
403 4 0 5 4.4 Cn1c(-c2ccc(OC3CCN(C4CCCC4)CC3)cc2)nc2ccccc2c1=O
CHEMBL3427242 hrh3_human Human No 9.1 IC50 = 0.8 nM Funct
HTRF cAMP Assay: Compounds of the present invention were evaluated using the human H3 receptor (H3R) HTRF cAMP assay. In this assay, HEK293 cells expressing the human H3 receptor were suspended in PBS containing 100 μM IBMX and plated into 384-well assay plates (Perkin Elmer Proxiplate 384-Plus; 15,000 cells per well; 5 μL plating volume) and allowed to equilibrate for an hour. Test compounds were serially diluted in 100% DMSO and then further diluted in PBS containing forskolin (2 μM). Test compounds (5 μL) were then added to the assay plate and the mixture was incubated for 1 hour. HTRF assay reagents (Cisbio, Dynamic 2 cAMP Kit), cAMP-d2 and cryptate-labeled anti-cAMP antibody, are mixed with cell lysis buffer and added to the assay plate. After 1-hour incubation with these reagents, the assay plate was read on an HTRF-compatible microplate reader (Perkin Elmer EnVision or BMG Pherastar).HTRF cAMP Assay: Compounds of the present invention were evaluated using the human H3 receptor (H3R) HTRF cAMP assay. In this assay, HEK293 cells expressing the human H3 receptor were suspended in PBS containing 100 μM IBMX and plated into 384-well assay plates (Perkin Elmer Proxiplate 384-Plus; 15,000 cells per well; 5 μL plating volume) and allowed to equilibrate for an hour. Test compounds were serially diluted in 100% DMSO and then further diluted in PBS containing forskolin (2 μM). Test compounds (5 μL) were then added to the assay plate and the mixture was incubated for 1 hour. HTRF assay reagents (Cisbio, Dynamic 2 cAMP Kit), cAMP-d2 and cryptate-labeled anti-cAMP antibody, are mixed with cell lysis buffer and added to the assay plate. After 1-hour incubation with these reagents, the assay plate was read on an HTRF-compatible microplate reader (Perkin Elmer EnVision or BMG Pherastar).
347 6 1 4 3.5 C[C@@H]1CCCN1CCc1ccc(-c2ccc(Cc3nnn[nH]3)cc2)cc1
CHEMBL3427242 hrh3_human Human No 9.1 IC50 = 0.8 nM Funct
Modulation of human histamine H3 receptor expressed in HEK293 cells assessed as change in forskolin-stimulated cAMP level after 1 hr by HTRF assayModulation of human histamine H3 receptor expressed in HEK293 cells assessed as change in forskolin-stimulated cAMP level after 1 hr by HTRF assay
347 6 1 4 3.5 C[C@@H]1CCCN1CCc1ccc(-c2ccc(Cc3nnn[nH]3)cc2)cc1
CHEMBL4112593 hrh3_human Human No 9.1 IC50 = 0.8 nM Funct
HTRF cAMP Assay: Compounds of the present invention were evaluated using the human H3 receptor (H3R) HTRF cAMP assay. In this assay, HEK293 cells expressing the human H3 receptor were suspended in PBS containing 100 μM IBMX and plated into 384-well assay plates (Perkin Elmer Proxiplate 384-Plus; 15,000 cells per well; 5 μL plating volume) and allowed to equilibrate for an hour. Test compounds were serially diluted in 100% DMSO and then further diluted in PBS containing forskolin (2 μM). Test compounds (5 μL) were then added to the assay plate and the mixture was incubated for 1 hour. HTRF assay reagents (Cisbio, Dynamic 2 cAMP Kit), cAMP-d2 and cryptate-labeled anti-cAMP antibody, are mixed with cell lysis buffer and added to the assay plate. After 1-hour incubation with these reagents, the assay plate was read on an HTRF-compatible microplate reader (Perkin Elmer EnVision or BMG Pherastar).HTRF cAMP Assay: Compounds of the present invention were evaluated using the human H3 receptor (H3R) HTRF cAMP assay. In this assay, HEK293 cells expressing the human H3 receptor were suspended in PBS containing 100 μM IBMX and plated into 384-well assay plates (Perkin Elmer Proxiplate 384-Plus; 15,000 cells per well; 5 μL plating volume) and allowed to equilibrate for an hour. Test compounds were serially diluted in 100% DMSO and then further diluted in PBS containing forskolin (2 μM). Test compounds (5 μL) were then added to the assay plate and the mixture was incubated for 1 hour. HTRF assay reagents (Cisbio, Dynamic 2 cAMP Kit), cAMP-d2 and cryptate-labeled anti-cAMP antibody, are mixed with cell lysis buffer and added to the assay plate. After 1-hour incubation with these reagents, the assay plate was read on an HTRF-compatible microplate reader (Perkin Elmer EnVision or BMG Pherastar).
408 9 2 3 3.9 C[C@H](NC(=O)CCc1ccc(-c2ccc(CCN3CCC[C@H]3C)cc2)cc1)C(=O)O
CHEMBL14690 hrh3_human Human Yes 9.1 IC50 = 0.8 nM Funct
Antagonist activity at human histamine H3 receptor expressed in CHO cells assessed as inhibition of forskolin/R-alpha-methylhistamine-induced cAMP accumulation after 1.5 hrs by TR-FRET immunoassayAntagonist activity at human histamine H3 receptor expressed in CHO cells assessed as inhibition of forskolin/R-alpha-methylhistamine-induced cAMP accumulation after 1.5 hrs by TR-FRET immunoassay
308 6 2 3 3.2 Clc1ccc(cc1)CN=C(SCCCc1cnc[nH]1)N
CHEMBL2387318 hrh3_human Human No 9.1 IC50 = 0.8 nM Funct
Antagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of calcium mobilization by FLIPR assay
385 3 1 4 2.8 Cc1cc(N2CCC(N3CCCC3C)C2)ccc1NC(=O)N1CCN(C)CC1
CHEMBL3127674 hrh3_human Human No 9.1 IC50 = 0.8 nM Funct
Antagonist activity at human histamine H3 receptor long form expressed in CHOK1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding after 3 hrs by scintillation proximity assayAntagonist activity at human histamine H3 receptor long form expressed in CHOK1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding after 3 hrs by scintillation proximity assay
389 3 0 4 2.7 O=C(C1CC2(CCN(C3CCOCC3)CC2)C1)N1CCCN(C2CCC2)CC1
CHEMBL479036 hrh3_human Human No 9.1 IC50 = 0.8 nM Funct
Inverse agonist activity at human histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of N-alpha-methylhistamine-induced [35S]GTPgammaS bindingInverse agonist activity at human histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of N-alpha-methylhistamine-induced [35S]GTPgammaS binding
391 7 0 5 4.4 CC(C)c1nc2ccccc2c(=O)n1-c1ccc(OCCCN2CCCC2)cc1
CHEMBL563779 hrh3_human Human No 9.1 IC50 = 0.8 nM Funct
Inverse agonist activity at human cloned histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding by cell-based assayInverse agonist activity at human cloned histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding by cell-based assay
445 7 0 6 4.2 COc1cccc2c1OC(c1ccc(OCCCN3CCC[C@@H]3C)cc1)C(C)S2(=O)=O
CHEMBL3677895 hrh3_human Human No 9.1 IC50 = 0.8 nM Bind
SPA Assay: The H3 binding assay was/can be used to evaluate the ability of at least one compound in accordance with formula I, Ia, Ib, and/or Ic to inhibit [3H]-N-α-methylhistamine binding to CHO-K1 membranes expressing human histamine H3 receptors (full-length H3, the most prevalent brain isoform 445). In 200 μl 96-well SPA format, human H3 membranes (12.5 μg protein/well) and 1.4 nM [3H]-N-α-methylhistamine were/can be incubated with at least one compound in accordance with formula I, Ia, Ib, and/or Ic for 1.5 hrs to determine percent effect with respect to total (1% DMSO) and non-specific binding (10 μM imetit). Reproducibility of the assay is such that IC50 curves can be generated in singlicate.SPA Assay: The H3 binding assay was/can be used to evaluate the ability of at least one compound in accordance with formula I, Ia, Ib, and/or Ic to inhibit [3H]-N-α-methylhistamine binding to CHO-K1 membranes expressing human histamine H3 receptors (full-length H3, the most prevalent brain isoform 445). In 200 μl 96-well SPA format, human H3 membranes (12.5 μg protein/well) and 1.4 nM [3H]-N-α-methylhistamine were/can be incubated with at least one compound in accordance with formula I, Ia, Ib, and/or Ic for 1.5 hrs to determine percent effect with respect to total (1% DMSO) and non-specific binding (10 μM imetit). Reproducibility of the assay is such that IC50 curves can be generated in singlicate.
309 3 0 3 2.4 N#Cc1cccc(C2CC2C(=O)N2CCN(C3CCC3)CC2)c1
CHEMBL464599 hrh3_human Human No 9.1 IC50 = 0.8 nM Funct
Antagonist activity at human cloned histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS bindingAntagonist activity at human cloned histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding
407 4 0 5 4.2 Cc1nc2c(F)cccc2c(=O)n1-c1ccc(OC2CCN(C3CCC3)CC2)cc1
CHEMBL556100 hrh3_human Human No 9.1 IC50 = 0.8 nM Funct
Inverse agonist activity at human cloned histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding by cell-based assayInverse agonist activity at human cloned histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding by cell-based assay
399 6 0 5 4.1 CC1=C(c2ccc(OCCCN3CCCC3)cc2)Oc2ccccc2S1(=O)=O
CHEMBL488251 hrh3_human Human No 9.1 IC50 = 0.9 nM Funct
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
405 7 0 5 4.9 CC(C)n1c(-c2ccc(OCCCN3CCCCC3)cc2)nc2ccccc2c1=O
CHEMBL519067 hrh3_human Human No 9.1 IC50 = 0.9 nM Funct
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
391 7 0 5 4.3 CCn1c(-c2ccc(OCCCN3CCCCC3)cc2)nc2ccccc2c1=O
CHEMBL1222595 hrh3_human Human No 9.1 IC50 = 0.9 nM Funct
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
495 8 0 8 4.6 c1ccc(Cn2nnnc2C(c2ccc(Oc3ccccn3)cc2)N2CCCN(C3CCC3)CC2)cc1
CHEMBL2387312 hrh3_human Human No 9.1 IC50 = 0.9 nM Funct
Antagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of calcium mobilization by FLIPR assay
446 4 2 3 6.0 Cc1cc(N2CCC(N3CCCC3C)C2)ccc1NC(=O)Nc1cc(Cl)cc(Cl)c1
CHEMBL516697 hrh3_human Human No 9.0 IC50 = 0.9 nM Funct
Antagonist activity at human cloned histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS bindingAntagonist activity at human cloned histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding
425 4 0 5 4.4 Cc1nc2cc(F)c(F)cc2c(=O)n1-c1ccc(OC2CCN(C3CCC3)CC2)cc1
CHEMBL3427230 hrh3_human Human No 9.0 IC50 = 0.9 nM Funct
HTRF cAMP Assay: Compounds of the present invention were evaluated using the human H3 receptor (H3R) HTRF cAMP assay. In this assay, HEK293 cells expressing the human H3 receptor were suspended in PBS containing 100 μM IBMX and plated into 384-well assay plates (Perkin Elmer Proxiplate 384-Plus; 15,000 cells per well; 5 μL plating volume) and allowed to equilibrate for an hour. Test compounds were serially diluted in 100% DMSO and then further diluted in PBS containing forskolin (2 μM). Test compounds (5 μL) were then added to the assay plate and the mixture was incubated for 1 hour. HTRF assay reagents (Cisbio, Dynamic 2 cAMP Kit), cAMP-d2 and cryptate-labeled anti-cAMP antibody, are mixed with cell lysis buffer and added to the assay plate. After 1-hour incubation with these reagents, the assay plate was read on an HTRF-compatible microplate reader (Perkin Elmer EnVision or BMG Pherastar).HTRF cAMP Assay: Compounds of the present invention were evaluated using the human H3 receptor (H3R) HTRF cAMP assay. In this assay, HEK293 cells expressing the human H3 receptor were suspended in PBS containing 100 μM IBMX and plated into 384-well assay plates (Perkin Elmer Proxiplate 384-Plus; 15,000 cells per well; 5 μL plating volume) and allowed to equilibrate for an hour. Test compounds were serially diluted in 100% DMSO and then further diluted in PBS containing forskolin (2 μM). Test compounds (5 μL) were then added to the assay plate and the mixture was incubated for 1 hour. HTRF assay reagents (Cisbio, Dynamic 2 cAMP Kit), cAMP-d2 and cryptate-labeled anti-cAMP antibody, are mixed with cell lysis buffer and added to the assay plate. After 1-hour incubation with these reagents, the assay plate was read on an HTRF-compatible microplate reader (Perkin Elmer EnVision or BMG Pherastar).
361 7 0 5 3.6 C[C@@H]1CCCN1CCc1ccc(-c2ccc(CCn3cnnn3)cc2)cc1
CHEMBL3427230 hrh3_human Human No 9.0 IC50 = 0.9 nM Funct
Modulation of human histamine H3 receptor expressed in HEK293 cells assessed as change in forskolin-stimulated cAMP level after 1 hr by HTRF assayModulation of human histamine H3 receptor expressed in HEK293 cells assessed as change in forskolin-stimulated cAMP level after 1 hr by HTRF assay
361 7 0 5 3.6 C[C@@H]1CCCN1CCc1ccc(-c2ccc(CCn3cnnn3)cc2)cc1
CHEMBL2387311 hrh3_human Human No 9.0 IC50 = 1.0 nM Bind
Antagonist activity at human histamine H3 receptor by FLIPR assayAntagonist activity at human histamine H3 receptor by FLIPR assay
432 4 2 3 5.7 CC1CCCN1C1CCN(c2ccc(NC(=O)Nc3cc(Cl)cc(Cl)c3)cc2)C1
CHEMBL4110820 hrh3_human Human No 9.0 IC50 = 1.0 nM Funct
HTRF cAMP Assay: Compounds of the present invention were evaluated using the human H3 receptor (H3R) HTRF cAMP assay. In this assay, HEK293 cells expressing the human H3 receptor were suspended in PBS containing 100 μM IBMX and plated into 384-well assay plates (Perkin Elmer Proxiplate 384-Plus; 15,000 cells per well; 5 μL plating volume) and allowed to equilibrate for an hour. Test compounds were serially diluted in 100% DMSO and then further diluted in PBS containing forskolin (2 μM). Test compounds (5 μL) were then added to the assay plate and the mixture was incubated for 1 hour. HTRF assay reagents (Cisbio, Dynamic 2 cAMP Kit), cAMP-d2 and cryptate-labeled anti-cAMP antibody, are mixed with cell lysis buffer and added to the assay plate. After 1-hour incubation with these reagents, the assay plate was read on an HTRF-compatible microplate reader (Perkin Elmer EnVision or BMG Pherastar).HTRF cAMP Assay: Compounds of the present invention were evaluated using the human H3 receptor (H3R) HTRF cAMP assay. In this assay, HEK293 cells expressing the human H3 receptor were suspended in PBS containing 100 μM IBMX and plated into 384-well assay plates (Perkin Elmer Proxiplate 384-Plus; 15,000 cells per well; 5 μL plating volume) and allowed to equilibrate for an hour. Test compounds were serially diluted in 100% DMSO and then further diluted in PBS containing forskolin (2 μM). Test compounds (5 μL) were then added to the assay plate and the mixture was incubated for 1 hour. HTRF assay reagents (Cisbio, Dynamic 2 cAMP Kit), cAMP-d2 and cryptate-labeled anti-cAMP antibody, are mixed with cell lysis buffer and added to the assay plate. After 1-hour incubation with these reagents, the assay plate was read on an HTRF-compatible microplate reader (Perkin Elmer EnVision or BMG Pherastar).
478 9 1 4 5.6 C[C@@H]1CCCN1CCc1ccc(-c2ccc(CCC(=O)NC(C)(C)C(=O)OC(C)(C)C)cc2)cc1
CHEMBL3427235 hrh3_human Human No 9.0 IC50 = 1.0 nM Funct
Modulation of human histamine H3 receptor expressed in HEK293 cells assessed as change in forskolin-stimulated cAMP level after 1 hr by HTRF assayModulation of human histamine H3 receptor expressed in HEK293 cells assessed as change in forskolin-stimulated cAMP level after 1 hr by HTRF assay
478 9 1 4 5.4 C[C@@H]1CCCN1CCc1ccc(-c2ccc(CCNC(=O)C(C)(C)C(=O)OC(C)(C)C)cc2)cc1
CHEMBL4110757 hrh3_human Human No 9.0 IC50 = 1.0 nM Funct
HTRF cAMP Assay: Compounds of the present invention were evaluated using the human H3 receptor (H3R) HTRF cAMP assay. In this assay, HEK293 cells expressing the human H3 receptor were suspended in PBS containing 100 μM IBMX and plated into 384-well assay plates (Perkin Elmer Proxiplate 384-Plus; 15,000 cells per well; 5 μL plating volume) and allowed to equilibrate for an hour. Test compounds were serially diluted in 100% DMSO and then further diluted in PBS containing forskolin (2 μM). Test compounds (5 μL) were then added to the assay plate and the mixture was incubated for 1 hour. HTRF assay reagents (Cisbio, Dynamic 2 cAMP Kit), cAMP-d2 and cryptate-labeled anti-cAMP antibody, are mixed with cell lysis buffer and added to the assay plate. After 1-hour incubation with these reagents, the assay plate was read on an HTRF-compatible microplate reader (Perkin Elmer EnVision or BMG Pherastar).HTRF cAMP Assay: Compounds of the present invention were evaluated using the human H3 receptor (H3R) HTRF cAMP assay. In this assay, HEK293 cells expressing the human H3 receptor were suspended in PBS containing 100 μM IBMX and plated into 384-well assay plates (Perkin Elmer Proxiplate 384-Plus; 15,000 cells per well; 5 μL plating volume) and allowed to equilibrate for an hour. Test compounds were serially diluted in 100% DMSO and then further diluted in PBS containing forskolin (2 μM). Test compounds (5 μL) were then added to the assay plate and the mixture was incubated for 1 hour. HTRF assay reagents (Cisbio, Dynamic 2 cAMP Kit), cAMP-d2 and cryptate-labeled anti-cAMP antibody, are mixed with cell lysis buffer and added to the assay plate. After 1-hour incubation with these reagents, the assay plate was read on an HTRF-compatible microplate reader (Perkin Elmer EnVision or BMG Pherastar).
476 9 0 4 5.1 CCOC(=O)C1CCN(C(=O)CCc2ccc(-c3ccc(CCN4CCC[C@H]4C)cc3)cc2)CC1
CHEMBL477364 hrh3_human Human No 9.0 IC50 = 1.0 nM Funct
Inverse agonist activity at human histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of N-alpha-methylhistamine-induced [35S]GTPgammaS bindingInverse agonist activity at human histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of N-alpha-methylhistamine-induced [35S]GTPgammaS binding
431 6 0 5 4.6 Cc1nc2cc(C(F)(F)F)ccc2c(=O)n1-c1ccc(OCCCN2CCCC2)cc1
CHEMBL3427245 hrh3_human Human No 9.0 IC50 = 1.0 nM Funct
HTRF cAMP Assay: Compounds of the present invention were evaluated using the human H3 receptor (H3R) HTRF cAMP assay. In this assay, HEK293 cells expressing the human H3 receptor were suspended in PBS containing 100 μM IBMX and plated into 384-well assay plates (Perkin Elmer Proxiplate 384-Plus; 15,000 cells per well; 5 μL plating volume) and allowed to equilibrate for an hour. Test compounds were serially diluted in 100% DMSO and then further diluted in PBS containing forskolin (2 μM). Test compounds (5 μL) were then added to the assay plate and the mixture was incubated for 1 hour. HTRF assay reagents (Cisbio, Dynamic 2 cAMP Kit), cAMP-d2 and cryptate-labeled anti-cAMP antibody, are mixed with cell lysis buffer and added to the assay plate. After 1-hour incubation with these reagents, the assay plate was read on an HTRF-compatible microplate reader (Perkin Elmer EnVision or BMG Pherastar).HTRF cAMP Assay: Compounds of the present invention were evaluated using the human H3 receptor (H3R) HTRF cAMP assay. In this assay, HEK293 cells expressing the human H3 receptor were suspended in PBS containing 100 μM IBMX and plated into 384-well assay plates (Perkin Elmer Proxiplate 384-Plus; 15,000 cells per well; 5 μL plating volume) and allowed to equilibrate for an hour. Test compounds were serially diluted in 100% DMSO and then further diluted in PBS containing forskolin (2 μM). Test compounds (5 μL) were then added to the assay plate and the mixture was incubated for 1 hour. HTRF assay reagents (Cisbio, Dynamic 2 cAMP Kit), cAMP-d2 and cryptate-labeled anti-cAMP antibody, are mixed with cell lysis buffer and added to the assay plate. After 1-hour incubation with these reagents, the assay plate was read on an HTRF-compatible microplate reader (Perkin Elmer EnVision or BMG Pherastar).
351 8 1 2 4.8 C[C@@H]1CCCN1CCc1ccc(-c2ccc(CCCC(=O)O)cc2)cc1
CHEMBL3427245 hrh3_human Human No 9.0 IC50 = 1.0 nM Funct
Modulation of human histamine H3 receptor expressed in HEK293 cells assessed as change in forskolin-stimulated cAMP level after 1 hr by HTRF assayModulation of human histamine H3 receptor expressed in HEK293 cells assessed as change in forskolin-stimulated cAMP level after 1 hr by HTRF assay
351 8 1 2 4.8 C[C@@H]1CCCN1CCc1ccc(-c2ccc(CCCC(=O)O)cc2)cc1
CHEMBL259264 hrh3_human Human No 9.0 IC50 = 1.0 nM Bind
Inhibition of histamine H3 receptorInhibition of histamine H3 receptor
360 9 1 4 3.5 OCCC1CCN(Cc2ccc(OCCCN3CCCCC3)cc2)CC1
CHEMBL479242 hrh3_human Human No 9.0 IC50 = 1.0 nM Funct
Inverse agonist activity at human histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of N-alpha-methylhistamine-induced [35S]GTPgammaS bindingInverse agonist activity at human histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of N-alpha-methylhistamine-induced [35S]GTPgammaS binding
377 6 0 5 3.9 Cc1cccc2nc(C)n(-c3ccc(OCCCN4CCCC4)cc3)c(=O)c12
CHEMBL4111575 hrh3_human Human No 9.0 IC50 = 1.0 nM Funct
HTRF cAMP Assay: Compounds of the present invention were evaluated using the human H3 receptor (H3R) HTRF cAMP assay. In this assay, HEK293 cells expressing the human H3 receptor were suspended in PBS containing 100 μM IBMX and plated into 384-well assay plates (Perkin Elmer Proxiplate 384-Plus; 15,000 cells per well; 5 μL plating volume) and allowed to equilibrate for an hour. Test compounds were serially diluted in 100% DMSO and then further diluted in PBS containing forskolin (2 μM). Test compounds (5 μL) were then added to the assay plate and the mixture was incubated for 1 hour. HTRF assay reagents (Cisbio, Dynamic 2 cAMP Kit), cAMP-d2 and cryptate-labeled anti-cAMP antibody, are mixed with cell lysis buffer and added to the assay plate. After 1-hour incubation with these reagents, the assay plate was read on an HTRF-compatible microplate reader (Perkin Elmer EnVision or BMG Pherastar).HTRF cAMP Assay: Compounds of the present invention were evaluated using the human H3 receptor (H3R) HTRF cAMP assay. In this assay, HEK293 cells expressing the human H3 receptor were suspended in PBS containing 100 μM IBMX and plated into 384-well assay plates (Perkin Elmer Proxiplate 384-Plus; 15,000 cells per well; 5 μL plating volume) and allowed to equilibrate for an hour. Test compounds were serially diluted in 100% DMSO and then further diluted in PBS containing forskolin (2 μM). Test compounds (5 μL) were then added to the assay plate and the mixture was incubated for 1 hour. HTRF assay reagents (Cisbio, Dynamic 2 cAMP Kit), cAMP-d2 and cryptate-labeled anti-cAMP antibody, are mixed with cell lysis buffer and added to the assay plate. After 1-hour incubation with these reagents, the assay plate was read on an HTRF-compatible microplate reader (Perkin Elmer EnVision or BMG Pherastar).
408 9 1 4 3.6 COC(=O)CNC(=O)CCc1ccc(-c2ccc(CCN3CCC[C@H]3C)cc2)cc1
CHEMBL3427238 hrh3_human Human No 9.0 IC50 = 1.0 nM Funct
Modulation of human histamine H3 receptor expressed in HEK293 cells assessed as change in forskolin-stimulated cAMP level after 1 hr by HTRF assayModulation of human histamine H3 receptor expressed in HEK293 cells assessed as change in forskolin-stimulated cAMP level after 1 hr by HTRF assay
408 9 1 4 3.6 COC(=O)CC(=O)NCCc1ccc(-c2ccc(CCN3CCC[C@H]3C)cc2)cc1
CHEMBL14690 hrh3_human Human Yes 9.0 IC50 = 1 nM Funct
Antagonist activity against human histamine H3 receptor expressed in human HT1080 cells assessed as inhibition of (R)-alpha-methylhistamine-induced increase in intracellular calcium level by FLIPR assayAntagonist activity against human histamine H3 receptor expressed in human HT1080 cells assessed as inhibition of (R)-alpha-methylhistamine-induced increase in intracellular calcium level by FLIPR assay
308 6 2 3 3.2 Clc1ccc(cc1)CN=C(SCCCc1cnc[nH]1)N
CHEMBL14690 hrh3_mouse Mouse Yes 9.0 IC50 = 1 nM Funct
Antagonist activity against mouse histamine H3 receptor expressed in human HT1080 cells assessed as inhibition of (R)-alpha-methylhistamine-induced increase in intracellular calcium level by FLIPR assayAntagonist activity against mouse histamine H3 receptor expressed in human HT1080 cells assessed as inhibition of (R)-alpha-methylhistamine-induced increase in intracellular calcium level by FLIPR assay
308 6 2 3 3.2 Clc1ccc(cc1)CN=C(SCCCc1cnc[nH]1)N
CHEMBL4463918 hrh3_human Human No 9.0 IC50 = 1 nM Bind
Antagonist activity at human H3 receptor expressed in CHOK1 cells incubated for 10 mins by HTRF assayAntagonist activity at human H3 receptor expressed in CHOK1 cells incubated for 10 mins by HTRF assay
451 12 1 7 3.4 Cc1nn(CCOCCOCCN)cc1-c1ccc2cc(CCN3CCC[C@H]3C)ccc2n1
CHEMBL2387303 hrh3_human Human No 9.0 IC50 = 1 nM Funct
Antagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of calcium mobilization by FLIPR assay
395 8 2 3 5.4 CCN(CC)CCOc1ccc(NC(=O)Nc2c(Cl)cccc2Cl)cc1
CHEMBL2387286 hrh3_human Human No 9.0 IC50 = 1.1 nM Funct
Antagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of calcium mobilization by FLIPR assay
413 4 1 4 2.8 CC(=O)N(C)C1CCN(C(=O)Nc2ccc(N3CCC(N4CCCC4C)C3)cc2)C1
CHEMBL2387287 hrh3_human Human No 9.0 IC50 = 1.1 nM Funct
Antagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of calcium mobilization by FLIPR assay
427 4 1 4 3.1 CC(=O)N(C)C1CCN(C(=O)Nc2ccc(N3CCC(N4CCCC4C)C3)c(C)c2)C1
CHEMBL2387291 hrh3_human Human No 9.0 IC50 = 1.1 nM Funct
Antagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of calcium mobilization by FLIPR assay
460 5 2 3 5.7 Cc1cc(NC(=O)NCc2cc(Cl)cc(Cl)c2)ccc1N1CCC(N2CCCC2C)C1
CHEMBL2387319 hrh3_human Human No 9.0 IC50 = 1.1 nM Funct
Antagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of calcium mobilization by FLIPR assay
385 3 1 4 2.8 Cc1cc(NC(=O)N2CCN(C)CC2)ccc1N1CCC(N2CCCC2C)C1
CHEMBL3427232 hrh3_human Human No 9.0 IC50 = 1.1 nM Funct
HTRF cAMP Assay: Compounds of the present invention were evaluated using the human H3 receptor (H3R) HTRF cAMP assay. In this assay, HEK293 cells expressing the human H3 receptor were suspended in PBS containing 100 μM IBMX and plated into 384-well assay plates (Perkin Elmer Proxiplate 384-Plus; 15,000 cells per well; 5 μL plating volume) and allowed to equilibrate for an hour. Test compounds were serially diluted in 100% DMSO and then further diluted in PBS containing forskolin (2 μM). Test compounds (5 μL) were then added to the assay plate and the mixture was incubated for 1 hour. HTRF assay reagents (Cisbio, Dynamic 2 cAMP Kit), cAMP-d2 and cryptate-labeled anti-cAMP antibody, are mixed with cell lysis buffer and added to the assay plate. After 1-hour incubation with these reagents, the assay plate was read on an HTRF-compatible microplate reader (Perkin Elmer EnVision or BMG Pherastar).HTRF cAMP Assay: Compounds of the present invention were evaluated using the human H3 receptor (H3R) HTRF cAMP assay. In this assay, HEK293 cells expressing the human H3 receptor were suspended in PBS containing 100 μM IBMX and plated into 384-well assay plates (Perkin Elmer Proxiplate 384-Plus; 15,000 cells per well; 5 μL plating volume) and allowed to equilibrate for an hour. Test compounds were serially diluted in 100% DMSO and then further diluted in PBS containing forskolin (2 μM). Test compounds (5 μL) were then added to the assay plate and the mixture was incubated for 1 hour. HTRF assay reagents (Cisbio, Dynamic 2 cAMP Kit), cAMP-d2 and cryptate-labeled anti-cAMP antibody, are mixed with cell lysis buffer and added to the assay plate. After 1-hour incubation with these reagents, the assay plate was read on an HTRF-compatible microplate reader (Perkin Elmer EnVision or BMG Pherastar).
351 7 0 3 4.5 COC(=O)CCc1ccc(-c2ccc(CCN3CCC[C@H]3C)cc2)cc1
CHEMBL72156 hrh3_cavpo Guinea pig Yes 9.0 IC50 = 1.1 nM Funct
Histamine H3 receptor agonist activity was assessed by the inhibition of the electrically evoked twitch response of the guinea-pig ileum.Histamine H3 receptor agonist activity was assessed by the inhibition of the electrically evoked twitch response of the guinea-pig ileum.
152 4 3 2 0.7 N=C(N)CCCc1c[nH]cn1
CHEMBL477991 hrh3_human Human No 9.0 IC50 = 1.1 nM Funct
Inverse agonist activity at human histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of N-alpha-methylhistamine-induced [35S]GTPgammaS bindingInverse agonist activity at human histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of N-alpha-methylhistamine-induced [35S]GTPgammaS binding
393 7 0 6 3.6 COc1ccc2nc(C)n(-c3ccc(OCCCN4CCCC4)cc3)c(=O)c2c1
CHEMBL3427232 hrh3_human Human No 9.0 IC50 = 1.1 nM Funct
Modulation of human histamine H3 receptor expressed in HEK293 cells assessed as change in forskolin-stimulated cAMP level after 1 hr by HTRF assayModulation of human histamine H3 receptor expressed in HEK293 cells assessed as change in forskolin-stimulated cAMP level after 1 hr by HTRF assay
351 7 0 3 4.5 COC(=O)CCc1ccc(-c2ccc(CCN3CCC[C@H]3C)cc2)cc1
CHEMBL4744905 hrh3_human Human No 9.0 IC50 = 1.1 nM Funct
Antagonist activity at human histamine H3 receptor expressed in HEK293 cells preincubated for 5 mins followed by forskolin-stimulation and measured after 5 hrs by CRE-driven luciferase reporter gene assayAntagonist activity at human histamine H3 receptor expressed in HEK293 cells preincubated for 5 mins followed by forskolin-stimulation and measured after 5 hrs by CRE-driven luciferase reporter gene assay
356 8 0 5 3.3 CCc1c(OC)c(=O)ccn1-c1ccc(OCCCN2CCCC2)cc1
CHEMBL14690 hrh3_human Human Yes 8.9 IC50 = 1.2 nM Funct
Antagonist activity at human histamine H3 receptor expressed in HEK293 cells preincubated for 5 mins followed by forskolin-stimulation and measured after 5 hrs by CRE-driven luciferase reporter gene assayAntagonist activity at human histamine H3 receptor expressed in HEK293 cells preincubated for 5 mins followed by forskolin-stimulation and measured after 5 hrs by CRE-driven luciferase reporter gene assay
308 6 2 3 3.2 Clc1ccc(cc1)CN=C(SCCCc1cnc[nH]1)N
CHEMBL517937 hrh3_human Human No 8.9 IC50 = 1.2 nM Funct
Antagonist activity at human cloned histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS bindingAntagonist activity at human cloned histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding
407 4 0 5 4.2 Cc1nc2ccc(F)cc2c(=O)n1-c1ccc(OC2CCN(C3CCC3)CC2)cc1
CHEMBL520629 hrh3_human Human No 8.9 IC50 = 1.2 nM Funct
Antagonist activity at human cloned histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS bindingAntagonist activity at human cloned histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding
419 5 0 6 4.1 COc1cccc2nc(C)n(-c3ccc(OC4CCN(C5CCC5)CC4)cc3)c(=O)c12
CHEMBL1222436 hrh3_human Human No 8.9 IC50 = 1.2 nM Funct
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
468 7 0 8 3.6 c1ccc(Cn2nnnc2C(c2ccc(-n3cccn3)cc2)N2CCCN(C3CCC3)CC2)cc1
CHEMBL2387311 hrh3_human Human No 8.9 IC50 = 1.2 nM Funct
Antagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of calcium mobilization by FLIPR assay
432 4 2 3 5.7 CC1CCCN1C1CCN(c2ccc(NC(=O)Nc3cc(Cl)cc(Cl)c3)cc2)C1
CHEMBL3427231 hrh3_human Human No 8.9 IC50 = 1.2 nM Funct
HTRF cAMP Assay: Compounds of the present invention were evaluated using the human H3 receptor (H3R) HTRF cAMP assay. In this assay, HEK293 cells expressing the human H3 receptor were suspended in PBS containing 100 μM IBMX and plated into 384-well assay plates (Perkin Elmer Proxiplate 384-Plus; 15,000 cells per well; 5 μL plating volume) and allowed to equilibrate for an hour. Test compounds were serially diluted in 100% DMSO and then further diluted in PBS containing forskolin (2 μM). Test compounds (5 μL) were then added to the assay plate and the mixture was incubated for 1 hour. HTRF assay reagents (Cisbio, Dynamic 2 cAMP Kit), cAMP-d2 and cryptate-labeled anti-cAMP antibody, are mixed with cell lysis buffer and added to the assay plate. After 1-hour incubation with these reagents, the assay plate was read on an HTRF-compatible microplate reader (Perkin Elmer EnVision or BMG Pherastar).HTRF cAMP Assay: Compounds of the present invention were evaluated using the human H3 receptor (H3R) HTRF cAMP assay. In this assay, HEK293 cells expressing the human H3 receptor were suspended in PBS containing 100 μM IBMX and plated into 384-well assay plates (Perkin Elmer Proxiplate 384-Plus; 15,000 cells per well; 5 μL plating volume) and allowed to equilibrate for an hour. Test compounds were serially diluted in 100% DMSO and then further diluted in PBS containing forskolin (2 μM). Test compounds (5 μL) were then added to the assay plate and the mixture was incubated for 1 hour. HTRF assay reagents (Cisbio, Dynamic 2 cAMP Kit), cAMP-d2 and cryptate-labeled anti-cAMP antibody, are mixed with cell lysis buffer and added to the assay plate. After 1-hour incubation with these reagents, the assay plate was read on an HTRF-compatible microplate reader (Perkin Elmer EnVision or BMG Pherastar).
361 7 0 5 3.6 C[C@@H]1CCCN1CCc1ccc(-c2ccc(CCn3ncnn3)cc2)cc1
CHEMBL4113958 hrh3_human Human No 8.9 IC50 = 1.2 nM Funct
HTRF cAMP Assay: Compounds of the present invention were evaluated using the human H3 receptor (H3R) HTRF cAMP assay. In this assay, HEK293 cells expressing the human H3 receptor were suspended in PBS containing 100 μM IBMX and plated into 384-well assay plates (Perkin Elmer Proxiplate 384-Plus; 15,000 cells per well; 5 μL plating volume) and allowed to equilibrate for an hour. Test compounds were serially diluted in 100% DMSO and then further diluted in PBS containing forskolin (2 μM). Test compounds (5 μL) were then added to the assay plate and the mixture was incubated for 1 hour. HTRF assay reagents (Cisbio, Dynamic 2 cAMP Kit), cAMP-d2 and cryptate-labeled anti-cAMP antibody, are mixed with cell lysis buffer and added to the assay plate. After 1-hour incubation with these reagents, the assay plate was read on an HTRF-compatible microplate reader (Perkin Elmer EnVision or BMG Pherastar).HTRF cAMP Assay: Compounds of the present invention were evaluated using the human H3 receptor (H3R) HTRF cAMP assay. In this assay, HEK293 cells expressing the human H3 receptor were suspended in PBS containing 100 μM IBMX and plated into 384-well assay plates (Perkin Elmer Proxiplate 384-Plus; 15,000 cells per well; 5 μL plating volume) and allowed to equilibrate for an hour. Test compounds were serially diluted in 100% DMSO and then further diluted in PBS containing forskolin (2 μM). Test compounds (5 μL) were then added to the assay plate and the mixture was incubated for 1 hour. HTRF assay reagents (Cisbio, Dynamic 2 cAMP Kit), cAMP-d2 and cryptate-labeled anti-cAMP antibody, are mixed with cell lysis buffer and added to the assay plate. After 1-hour incubation with these reagents, the assay plate was read on an HTRF-compatible microplate reader (Perkin Elmer EnVision or BMG Pherastar).
408 7 1 4 4.1 COC(=O)C(C)(C)NC(=O)c1ccc(-c2ccc(CCN3CCC[C@H]3C)cc2)cc1
CHEMBL487064 hrh3_human Human No 8.9 IC50 = 1.2 nM Funct
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
377 6 0 5 3.9 Cn1c(-c2ccc(OCCCN3CCCCC3)cc2)nc2ccccc2c1=O
CHEMBL478615 hrh3_human Human No 8.9 IC50 = 1.2 nM Funct
Inverse agonist activity at human histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of N-alpha-methylhistamine-induced [35S]GTPgammaS bindingInverse agonist activity at human histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of N-alpha-methylhistamine-induced [35S]GTPgammaS binding
377 6 0 5 3.9 Cc1ccc2c(=O)n(-c3ccc(OCCCN4CCCC4)cc3)c(C)nc2c1
CHEMBL3427231 hrh3_human Human No 8.9 IC50 = 1.2 nM Funct
Modulation of human histamine H3 receptor expressed in HEK293 cells assessed as change in forskolin-stimulated cAMP level after 1 hr by HTRF assayModulation of human histamine H3 receptor expressed in HEK293 cells assessed as change in forskolin-stimulated cAMP level after 1 hr by HTRF assay
361 7 0 5 3.6 C[C@@H]1CCCN1CCc1ccc(-c2ccc(CCn3ncnn3)cc2)cc1
CHEMBL3427243 hrh3_human Human No 8.9 IC50 = 1.2 nM Funct
Modulation of human histamine H3 receptor expressed in HEK293 cells assessed as change in forskolin-stimulated cAMP level after 1 hr by HTRF assayModulation of human histamine H3 receptor expressed in HEK293 cells assessed as change in forskolin-stimulated cAMP level after 1 hr by HTRF assay
408 7 1 4 4.5 COC(=O)C(C)(C)C(=O)Nc1ccc(-c2ccc(CCN3CCC[C@H]3C)cc2)cc1
CHEMBL203263 hrh3_human Human No 8.9 IC50 = 1.3 nM Funct
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
277 8 2 2 3.6 Clc1ccc(CNCCCCCc2c[nH]cn2)cc1
CHEMBL464598 hrh3_human Human No 8.9 IC50 = 1.3 nM Funct
Antagonist activity at human cloned histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS bindingAntagonist activity at human cloned histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding
407 4 0 5 4.2 Cc1nc2cc(F)ccc2c(=O)n1-c1ccc(OC2CCN(C3CCC3)CC2)cc1
CHEMBL259482 hrh3_human Human No 8.9 IC50 = 1.3 nM Bind
Inhibition of histamine H3 receptorInhibition of histamine H3 receptor
346 8 1 4 3.1 OCC1CCN(Cc2ccc(OCCCN3CCCCC3)cc2)CC1
CHEMBL477363 hrh3_human Human No 8.9 IC50 = 1.3 nM Funct
Inverse agonist activity at human histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of N-alpha-methylhistamine-induced [35S]GTPgammaS bindingInverse agonist activity at human histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of N-alpha-methylhistamine-induced [35S]GTPgammaS binding
397 6 0 5 4.2 Cc1nc2cccc(Cl)c2c(=O)n1-c1ccc(OCCCN2CCCC2)cc1
CHEMBL477990 hrh3_human Human No 8.9 IC50 = 1.3 nM Funct
Inverse agonist activity at human histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of N-alpha-methylhistamine-induced [35S]GTPgammaS bindingInverse agonist activity at human histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of N-alpha-methylhistamine-induced [35S]GTPgammaS binding
393 7 0 6 3.6 COc1cccc2nc(C)n(-c3ccc(OCCCN4CCCC4)cc3)c(=O)c12
CHEMBL3677894 hrh3_human Human No 8.9 IC50 = 1.4 nM Bind
SPA Assay: The H3 binding assay was/can be used to evaluate the ability of at least one compound in accordance with formula I, Ia, Ib, and/or Ic to inhibit [3H]-N-α-methylhistamine binding to CHO-K1 membranes expressing human histamine H3 receptors (full-length H3, the most prevalent brain isoform 445). In 200 μl 96-well SPA format, human H3 membranes (12.5 μg protein/well) and 1.4 nM [3H]-N-α-methylhistamine were/can be incubated with at least one compound in accordance with formula I, Ia, Ib, and/or Ic for 1.5 hrs to determine percent effect with respect to total (1% DMSO) and non-specific binding (10 μM imetit). Reproducibility of the assay is such that IC50 curves can be generated in singlicate.SPA Assay: The H3 binding assay was/can be used to evaluate the ability of at least one compound in accordance with formula I, Ia, Ib, and/or Ic to inhibit [3H]-N-α-methylhistamine binding to CHO-K1 membranes expressing human histamine H3 receptors (full-length H3, the most prevalent brain isoform 445). In 200 μl 96-well SPA format, human H3 membranes (12.5 μg protein/well) and 1.4 nM [3H]-N-α-methylhistamine were/can be incubated with at least one compound in accordance with formula I, Ia, Ib, and/or Ic for 1.5 hrs to determine percent effect with respect to total (1% DMSO) and non-specific binding (10 μM imetit). Reproducibility of the assay is such that IC50 curves can be generated in singlicate.
362 3 0 2 3.2 O=C(C1CC1c1cccc(Br)c1)N1CCN(C2CCC2)CC1
CHEMBL4753961 hrh3_human Human No 8.9 IC50 = 1.4 nM Funct
Antagonist activity at human histamine H3 receptor expressed in HEK293 cells preincubated for 5 mins followed by forskolin-stimulation and measured after 5 hrs by CRE-driven luciferase reporter gene assayAntagonist activity at human histamine H3 receptor expressed in HEK293 cells preincubated for 5 mins followed by forskolin-stimulation and measured after 5 hrs by CRE-driven luciferase reporter gene assay
382 5 0 5 3.9 COc1c(C)n(-c2ccc(OC3CCN(C4CCCC4)CC3)cc2)ccc1=O
CHEMBL2387292 hrh3_human Human No 8.9 IC50 = 1.4 nM Funct
Antagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of calcium mobilization by FLIPR assay
456 6 2 4 6.2 CC1CCCN1C1CCN(c2ccc(NC(=O)Nc3ccc(Oc4ccccc4)cc3)cc2)C1
CHEMBL458359 hrh3_human Human No 8.8 IC50 = 1.5 nM Funct
Antagonist activity at human cloned histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS bindingAntagonist activity at human cloned histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding
423 4 0 5 4.7 Cc1nc2ccc(Cl)cc2c(=O)n1-c1ccc(OC2CCN(C3CCC3)CC2)cc1
CHEMBL483199 hrh3_human Human No 8.8 IC50 = 1.5 nM Funct
Antagonist activity at human cloned histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS bindingAntagonist activity at human cloned histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding
389 4 0 5 4.1 Cc1nc2ccccc2c(=O)n1-c1ccc(OC2CCN(C3CCC3)CC2)cc1
CHEMBL484189 hrh3_human Human No 8.8 IC50 = 1.5 nM Funct
Antagonist activity at human cloned histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS bindingAntagonist activity at human cloned histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding
419 5 0 6 4.1 COc1ccc2nc(C)n(-c3ccc(OC4CCN(C5CCC5)CC4)cc3)c(=O)c2c1
CHEMBL4110626 hrh3_human Human No 8.8 IC50 = 1.5 nM Funct
HTRF cAMP Assay: Compounds of the present invention were evaluated using the human H3 receptor (H3R) HTRF cAMP assay. In this assay, HEK293 cells expressing the human H3 receptor were suspended in PBS containing 100 μM IBMX and plated into 384-well assay plates (Perkin Elmer Proxiplate 384-Plus; 15,000 cells per well; 5 μL plating volume) and allowed to equilibrate for an hour. Test compounds were serially diluted in 100% DMSO and then further diluted in PBS containing forskolin (2 μM). Test compounds (5 μL) were then added to the assay plate and the mixture was incubated for 1 hour. HTRF assay reagents (Cisbio, Dynamic 2 cAMP Kit), cAMP-d2 and cryptate-labeled anti-cAMP antibody, are mixed with cell lysis buffer and added to the assay plate. After 1-hour incubation with these reagents, the assay plate was read on an HTRF-compatible microplate reader (Perkin Elmer EnVision or BMG Pherastar).HTRF cAMP Assay: Compounds of the present invention were evaluated using the human H3 receptor (H3R) HTRF cAMP assay. In this assay, HEK293 cells expressing the human H3 receptor were suspended in PBS containing 100 μM IBMX and plated into 384-well assay plates (Perkin Elmer Proxiplate 384-Plus; 15,000 cells per well; 5 μL plating volume) and allowed to equilibrate for an hour. Test compounds were serially diluted in 100% DMSO and then further diluted in PBS containing forskolin (2 μM). Test compounds (5 μL) were then added to the assay plate and the mixture was incubated for 1 hour. HTRF assay reagents (Cisbio, Dynamic 2 cAMP Kit), cAMP-d2 and cryptate-labeled anti-cAMP antibody, are mixed with cell lysis buffer and added to the assay plate. After 1-hour incubation with these reagents, the assay plate was read on an HTRF-compatible microplate reader (Perkin Elmer EnVision or BMG Pherastar).
476 10 1 4 5.3 COC(=O)CCCNC(=O)C1(c2ccc(-c3ccc(CCN4CCC[C@H]4C)cc3)cc2)CCCC1
CHEMBL268229 hrh3_rat Rat Yes 8.8 IC50 = 1.5 nM Bind
Inhibition of rat histamine H3 receptorInhibition of rat histamine H3 receptor
125 2 2 2 0.3 C[C@H](Cc1cnc[nH]1)N
CHEMBL515150 hrh3_human Human No 8.8 IC50 = 1.5 nM Funct
Inverse agonist activity at human histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of N-alpha-methylhistamine-induced [35S]GTPgammaS bindingInverse agonist activity at human histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of N-alpha-methylhistamine-induced [35S]GTPgammaS binding
381 6 0 5 3.7 Cc1nc2c(F)cccc2c(=O)n1-c1ccc(OCCCN2CCCC2)cc1
CHEMBL484611 hrh3_human Human No 8.8 IC50 = 1.6 nM Funct
Antagonist activity at human cloned histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS bindingAntagonist activity at human cloned histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding
390 4 0 6 3.5 Cc1nc2ncccc2c(=O)n1-c1ccc(OC2CCN(C3CCC3)CC2)cc1
CHEMBL1223157 hrh3_human Human No 8.8 IC50 = 1.6 nM Funct
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
480 7 0 8 2.8 CS(=O)(=O)c1ccc(C(c2nnnn2Cc2ccccc2)N2CCCN(C3CCC3)CC2)cc1
CHEMBL1223235 hrh3_human Human No 8.8 IC50 = 1.6 nM Funct
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
469 7 0 9 3.0 c1ccc(Cn2nnnc2C(c2ccc(-n3cncn3)cc2)N2CCCN(C3CCC3)CC2)cc1
CHEMBL3127676 hrh3_human Human No 8.8 IC50 = 1.6 nM Funct
Antagonist activity at human histamine H3 receptor long form expressed in CHOK1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding after 3 hrs by scintillation proximity assayAntagonist activity at human histamine H3 receptor long form expressed in CHOK1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding after 3 hrs by scintillation proximity assay
403 3 0 4 3.1 O=C(C1CC2(CCN(C3CCOCC3)CC2)C1)N1CCN(C2CCCCC2)CC1
CHEMBL487060 hrh3_human Human No 8.8 IC50 = 1.6 nM Funct
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
439 7 0 5 5.3 O=c1c2ccccc2nc(-c2ccc(OCCCN3CCCCC3)cc2)n1-c1ccccc1
CHEMBL476579 hrh3_human Human No 8.8 IC50 = 1.6 nM Funct
Inverse agonist activity at human histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of N-alpha-methylhistamine-induced [35S]GTPgammaS bindingInverse agonist activity at human histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of N-alpha-methylhistamine-induced [35S]GTPgammaS binding
391 6 0 5 4.3 Cc1nc2ccccc2c(=O)n1-c1ccc(OCCCN2CCCCCC2)cc1
CHEMBL476723 hrh3_human Human No 8.8 IC50 = 1.6 nM Funct
Inverse agonist activity at human histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of N-alpha-methylhistamine-induced [35S]GTPgammaS bindingInverse agonist activity at human histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of N-alpha-methylhistamine-induced [35S]GTPgammaS binding
377 7 0 5 3.8 CCc1nc2ccccc2c(=O)n1-c1ccc(OCCCN2CCCC2)cc1
CHEMBL479252 hrh3_human Human No 8.8 IC50 = 1.6 nM Funct
Inverse agonist activity at human histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of N-alpha-methylhistamine-induced [35S]GTPgammaS bindingInverse agonist activity at human histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of N-alpha-methylhistamine-induced [35S]GTPgammaS binding
381 6 0 5 3.7 Cc1nc2ccc(F)cc2c(=O)n1-c1ccc(OCCCN2CCCC2)cc1
CHEMBL3677882 hrh3_human Human No 8.8 IC50 = 1.6 nM Bind
SPA Assay: The H3 binding assay was/can be used to evaluate the ability of at least one compound in accordance with formula I, Ia, Ib, and/or Ic to inhibit [3H]-N-α-methylhistamine binding to CHO-K1 membranes expressing human histamine H3 receptors (full-length H3, the most prevalent brain isoform 445). In 200 μl 96-well SPA format, human H3 membranes (12.5 μg protein/well) and 1.4 nM [3H]-N-α-methylhistamine were/can be incubated with at least one compound in accordance with formula I, Ia, Ib, and/or Ic for 1.5 hrs to determine percent effect with respect to total (1% DMSO) and non-specific binding (10 μM imetit). Reproducibility of the assay is such that IC50 curves can be generated in singlicate.SPA Assay: The H3 binding assay was/can be used to evaluate the ability of at least one compound in accordance with formula I, Ia, Ib, and/or Ic to inhibit [3H]-N-α-methylhistamine binding to CHO-K1 membranes expressing human histamine H3 receptors (full-length H3, the most prevalent brain isoform 445). In 200 μl 96-well SPA format, human H3 membranes (12.5 μg protein/well) and 1.4 nM [3H]-N-α-methylhistamine were/can be incubated with at least one compound in accordance with formula I, Ia, Ib, and/or Ic for 1.5 hrs to determine percent effect with respect to total (1% DMSO) and non-specific binding (10 μM imetit). Reproducibility of the assay is such that IC50 curves can be generated in singlicate.
290 3 0 2 2.5 CC(C)N1CCN(C(=O)[C@H]2CC2c2ccc(F)cc2)CC1
CHEMBL4740932 hrh3_human Human No 8.8 IC50 = 1.7 nM Funct
Antagonist activity at human histamine H3 receptor expressed in HEK293 cells preincubated for 5 mins followed by forskolin-stimulation and measured after 5 hrs by CRE-driven luciferase reporter gene assayAntagonist activity at human histamine H3 receptor expressed in HEK293 cells preincubated for 5 mins followed by forskolin-stimulation and measured after 5 hrs by CRE-driven luciferase reporter gene assay
342 5 0 5 3.1 COc1cn(-c2ccc(OC3CCN(C(C)C)CC3)cc2)ccc1=O
CHEMBL458954 hrh3_human Human No 8.8 IC50 = 1.7 nM Funct
Antagonist activity at human cloned histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS bindingAntagonist activity at human cloned histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding
423 4 0 5 4.7 Cc1nc2c(Cl)cccc2c(=O)n1-c1ccc(OC2CCN(C3CCC3)CC2)cc1
CHEMBL476373 hrh3_human Human No 8.8 IC50 = 1.7 nM Funct
Antagonist activity at human cloned histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS bindingAntagonist activity at human cloned histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding
363 6 0 5 3.6 Cc1nc2ccccc2c(=O)n1-c1ccc(OCCCN2CCCC2)cc1
CHEMBL3127679 hrh3_human Human No 8.8 IC50 = 1.7 nM Funct
Antagonist activity at human histamine H3 receptor long form expressed in CHOK1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding after 3 hrs by scintillation proximity assayAntagonist activity at human histamine H3 receptor long form expressed in CHOK1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding after 3 hrs by scintillation proximity assay
363 3 0 4 2.2 CC(C)N1CCN(C(=O)C2CC3(CCN(C4CCOCC4)CC3)C2)CC1
CHEMBL476323 hrh3_human Human Yes 8.8 IC50 = 1.7 nM Funct
Inverse agonist activity at human histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of N-alpha-methylhistamine-induced [35S]GTPgammaS bindingInverse agonist activity at human histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of N-alpha-methylhistamine-induced [35S]GTPgammaS binding
431 6 0 5 4.6 Cc1nc2cccc(c2c(=O)n1c1ccc(cc1)OCCCN1CCCC1)C(F)(F)F
CHEMBL478616 hrh3_human Human No 8.8 IC50 = 1.7 nM Funct
Inverse agonist activity at human histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of N-alpha-methylhistamine-induced [35S]GTPgammaS bindingInverse agonist activity at human histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of N-alpha-methylhistamine-induced [35S]GTPgammaS binding
377 6 0 5 3.9 Cc1cccc2c(=O)n(-c3ccc(OCCCN4CCCC4)cc3)c(C)nc12
CHEMBL485388 hrh3_human Human No 8.7 IC50 = 1.8 nM Funct
Antagonist activity at human cloned histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS bindingAntagonist activity at human cloned histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding
419 5 0 6 4.1 COc1ccc2c(=O)n(-c3ccc(OC4CCN(C5CCC5)CC4)cc3)c(C)nc2c1
CHEMBL521327 hrh3_human Human No 8.7 IC50 = 1.8 nM Funct
Antagonist activity at human cloned histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS bindingAntagonist activity at human cloned histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding
390 4 0 6 3.5 Cc1nc2cnccc2c(=O)n1-c1ccc(OC2CCN(C3CCC3)CC2)cc1
CHEMBL3427234 hrh3_human Human No 8.7 IC50 = 1.8 nM Funct
HTRF cAMP Assay: Compounds of the present invention were evaluated using the human H3 receptor (H3R) HTRF cAMP assay. In this assay, HEK293 cells expressing the human H3 receptor were suspended in PBS containing 100 μM IBMX and plated into 384-well assay plates (Perkin Elmer Proxiplate 384-Plus; 15,000 cells per well; 5 μL plating volume) and allowed to equilibrate for an hour. Test compounds were serially diluted in 100% DMSO and then further diluted in PBS containing forskolin (2 μM). Test compounds (5 μL) were then added to the assay plate and the mixture was incubated for 1 hour. HTRF assay reagents (Cisbio, Dynamic 2 cAMP Kit), cAMP-d2 and cryptate-labeled anti-cAMP antibody, are mixed with cell lysis buffer and added to the assay plate. After 1-hour incubation with these reagents, the assay plate was read on an HTRF-compatible microplate reader (Perkin Elmer EnVision or BMG Pherastar).HTRF cAMP Assay: Compounds of the present invention were evaluated using the human H3 receptor (H3R) HTRF cAMP assay. In this assay, HEK293 cells expressing the human H3 receptor were suspended in PBS containing 100 μM IBMX and plated into 384-well assay plates (Perkin Elmer Proxiplate 384-Plus; 15,000 cells per well; 5 μL plating volume) and allowed to equilibrate for an hour. Test compounds were serially diluted in 100% DMSO and then further diluted in PBS containing forskolin (2 μM). Test compounds (5 μL) were then added to the assay plate and the mixture was incubated for 1 hour. HTRF assay reagents (Cisbio, Dynamic 2 cAMP Kit), cAMP-d2 and cryptate-labeled anti-cAMP antibody, are mixed with cell lysis buffer and added to the assay plate. After 1-hour incubation with these reagents, the assay plate was read on an HTRF-compatible microplate reader (Perkin Elmer EnVision or BMG Pherastar).
365 8 0 3 4.9 CCOC(=O)CCc1ccc(-c2ccc(CCN3CCC[C@H]3C)cc2)cc1
CHEMBL550393 hrh3_human Human No 8.7 IC50 = 1.8 nM Funct
Inverse agonist activity at human cloned histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding by cell-based assayInverse agonist activity at human cloned histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding by cell-based assay
369 6 0 4 5.2 C[C@H]1Sc2ccccc2O[C@@H]1c1ccc(OCCCN2CCCC2)cc1
CHEMBL476106 hrh3_human Human No 8.7 IC50 = 1.8 nM Funct
Inverse agonist activity at human histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of N-alpha-methylhistamine-induced [35S]GTPgammaS bindingInverse agonist activity at human histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of N-alpha-methylhistamine-induced [35S]GTPgammaS binding
381 6 0 5 3.7 Cc1nc2cc(F)ccc2c(=O)n1-c1ccc(OCCCN2CCCC2)cc1
CHEMBL3427234 hrh3_human Human No 8.7 IC50 = 1.8 nM Funct
Modulation of human histamine H3 receptor expressed in HEK293 cells assessed as change in forskolin-stimulated cAMP level after 1 hr by HTRF assayModulation of human histamine H3 receptor expressed in HEK293 cells assessed as change in forskolin-stimulated cAMP level after 1 hr by HTRF assay
365 8 0 3 4.9 CCOC(=O)CCc1ccc(-c2ccc(CCN3CCC[C@H]3C)cc2)cc1
CHEMBL257812 hrh3_rat Rat No 8.7 IC50 = 1.9 nM Funct
Antagonist activity at histamine H3 receptor in rat forebrain assessed as inhibition of [3H]histamine release from synaptosomesAntagonist activity at histamine H3 receptor in rat forebrain assessed as inhibition of [3H]histamine release from synaptosomes
356 6 0 6 1.8 C[C@H]1CCCN1CCN1CCN(CCN2CCC[C@@H]2C)C1=C(C#N)C#N
CHEMBL3127675 hrh3_human Human No 8.7 IC50 = 1.9 nM Funct
Antagonist activity at human histamine H3 receptor long form expressed in CHOK1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding after 3 hrs by scintillation proximity assayAntagonist activity at human histamine H3 receptor long form expressed in CHOK1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding after 3 hrs by scintillation proximity assay
375 3 0 4 2.4 O=C(C1CC2(CCN(C3CCOCC3)CC2)C1)N1CCN(C2CCC2)CC1
CHEMBL4106702 hrh3_human Human No 8.7 IC50 = 1.9 nM Funct
HTRF cAMP Assay: Compounds of the present invention were evaluated using the human H3 receptor (H3R) HTRF cAMP assay. In this assay, HEK293 cells expressing the human H3 receptor were suspended in PBS containing 100 μM IBMX and plated into 384-well assay plates (Perkin Elmer Proxiplate 384-Plus; 15,000 cells per well; 5 μL plating volume) and allowed to equilibrate for an hour. Test compounds were serially diluted in 100% DMSO and then further diluted in PBS containing forskolin (2 μM). Test compounds (5 μL) were then added to the assay plate and the mixture was incubated for 1 hour. HTRF assay reagents (Cisbio, Dynamic 2 cAMP Kit), cAMP-d2 and cryptate-labeled anti-cAMP antibody, are mixed with cell lysis buffer and added to the assay plate. After 1-hour incubation with these reagents, the assay plate was read on an HTRF-compatible microplate reader (Perkin Elmer EnVision or BMG Pherastar).HTRF cAMP Assay: Compounds of the present invention were evaluated using the human H3 receptor (H3R) HTRF cAMP assay. In this assay, HEK293 cells expressing the human H3 receptor were suspended in PBS containing 100 μM IBMX and plated into 384-well assay plates (Perkin Elmer Proxiplate 384-Plus; 15,000 cells per well; 5 μL plating volume) and allowed to equilibrate for an hour. Test compounds were serially diluted in 100% DMSO and then further diluted in PBS containing forskolin (2 μM). Test compounds (5 μL) were then added to the assay plate and the mixture was incubated for 1 hour. HTRF assay reagents (Cisbio, Dynamic 2 cAMP Kit), cAMP-d2 and cryptate-labeled anti-cAMP antibody, are mixed with cell lysis buffer and added to the assay plate. After 1-hour incubation with these reagents, the assay plate was read on an HTRF-compatible microplate reader (Perkin Elmer EnVision or BMG Pherastar).
448 8 1 4 4.5 COC(=O)CNC(=O)C1(c2ccc(-c3ccc(CCN4CCC[C@H]4C)cc3)cc2)CCCC1
CHEMBL3427240 hrh3_human Human No 8.7 IC50 = 1.9 nM Funct
Modulation of human histamine H3 receptor expressed in HEK293 cells assessed as change in forskolin-stimulated cAMP level after 1 hr by HTRF assayModulation of human histamine H3 receptor expressed in HEK293 cells assessed as change in forskolin-stimulated cAMP level after 1 hr by HTRF assay
448 8 1 4 4.8 COC(=O)CC(=O)NC1(c2ccc(-c3ccc(CCN4CCC[C@H]4C)cc3)cc2)CCCC1
CHEMBL4741097 hrh3_human Human No 8.7 IC50 = 1.9 nM Funct
Antagonist activity at human histamine H3 receptor expressed in HEK293 cells preincubated for 5 mins followed by forskolin-stimulation and measured after 5 hrs by CRE-driven luciferase reporter gene assayAntagonist activity at human histamine H3 receptor expressed in HEK293 cells preincubated for 5 mins followed by forskolin-stimulation and measured after 5 hrs by CRE-driven luciferase reporter gene assay
342 7 0 5 3.0 COc1cn(-c2ccc(OCCCN3CCCC3)cc2)c(C)cc1=O
CHEMBL2441945 hrh3_human Human No 8.7 IC50 = 2.0 nM Funct
Antagonist activity at human histamine H3 receptor expressed in CHO cells assessed as inhibition of forskolin/R-alpha-methylhistamine-induced cAMP accumulation after 1.5 hrs by TR-FRET immunoassayAntagonist activity at human histamine H3 receptor expressed in CHO cells assessed as inhibition of forskolin/R-alpha-methylhistamine-induced cAMP accumulation after 1.5 hrs by TR-FRET immunoassay
358 9 2 4 4.0 N#Cc1ccc(CCCCNC(=N)SCCCN2CCCCC2)cc1
CHEMBL3040738 hrh3_human Human No 8.7 IC50 = 2.0 nM Funct
Antagonist activity at human histamine H3 receptor expressed in CHO cells assessed as inhibition of forskolin/R-alpha-methylhistamine-induced cAMP accumulation after 1.5 hrs by TR-FRET immunoassayAntagonist activity at human histamine H3 receptor expressed in CHO cells assessed as inhibition of forskolin/R-alpha-methylhistamine-induced cAMP accumulation after 1.5 hrs by TR-FRET immunoassay
358 9 2 4 4.0 N#Cc1ccc(CCCCNC(=N)SCCCN2CCCCC2)cc1
CHEMBL377954 hrh3_human Human No 8.0 IC50 = 10 nM Funct
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
249 7 2 2 3.4 c1nc(CCCCCNC2CCCCCC2)c[nH]1
CHEMBL485242 hrh3_human Human No 8.0 IC50 = 10 nM Funct
Antagonist activity at human cloned histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS bindingAntagonist activity at human cloned histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding
403 4 0 5 4.5 Cc1nc2ccccc2c(=O)n1-c1ccc(OC2CCCN(C3CCC3)CC2)cc1
CHEMBL521022 hrh3_human Human No 8.0 IC50 = 10 nM Funct
Antagonist activity at human cloned histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS bindingAntagonist activity at human cloned histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding
403 4 0 5 4.5 Cc1nc2ccccc2c(=O)n1-c1ccc(O[C@H]2CC[C@@H](N3CCCC3)CC2)cc1
CHEMBL3127708 hrh3_human Human Yes 8.0 IC50 = 10 nM Funct
Antagonist activity at human histamine H3 receptor long form expressed in CHOK1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding after 3 hrs by scintillation proximity assayAntagonist activity at human histamine H3 receptor long form expressed in CHOK1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding after 3 hrs by scintillation proximity assay
387 3 0 3 3.9 O=C(C1CC12CCN(C1CCCCC1)CC2)N1CCN(C2CCCCC2)CC1
CHEMBL478621 hrh3_human Human No 8.0 IC50 = 10 nM Funct
Inverse agonist activity at human histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of N-alpha-methylhistamine-induced [35S]GTPgammaS bindingInverse agonist activity at human histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of N-alpha-methylhistamine-induced [35S]GTPgammaS binding
405 6 0 5 4.7 Cc1nc2ccccc2c(=O)n1-c1ccc(OCCCN2CCCCCCC2)cc1
CHEMBL3677882 hrh3_human Human No 8.0 IC50 = 10.2 nM Bind
SPA Assay: The H3 binding assay was/can be used to evaluate the ability of at least one compound in accordance with formula I, Ia, Ib, and/or Ic to inhibit [3H]-N-α-methylhistamine binding to CHO-K1 membranes expressing human histamine H3 receptors (full-length H3, the most prevalent brain isoform 445). In 200 μl 96-well SPA format, human H3 membranes (12.5 μg protein/well) and 1.4 nM [3H]-N-α-methylhistamine were/can be incubated with at least one compound in accordance with formula I, Ia, Ib, and/or Ic for 1.5 hrs to determine percent effect with respect to total (1% DMSO) and non-specific binding (10 μM imetit). Reproducibility of the assay is such that IC50 curves can be generated in singlicate.SPA Assay: The H3 binding assay was/can be used to evaluate the ability of at least one compound in accordance with formula I, Ia, Ib, and/or Ic to inhibit [3H]-N-α-methylhistamine binding to CHO-K1 membranes expressing human histamine H3 receptors (full-length H3, the most prevalent brain isoform 445). In 200 μl 96-well SPA format, human H3 membranes (12.5 μg protein/well) and 1.4 nM [3H]-N-α-methylhistamine were/can be incubated with at least one compound in accordance with formula I, Ia, Ib, and/or Ic for 1.5 hrs to determine percent effect with respect to total (1% DMSO) and non-specific binding (10 μM imetit). Reproducibility of the assay is such that IC50 curves can be generated in singlicate.
290 3 0 2 2.5 CC(C)N1CCN(C(=O)[C@H]2CC2c2ccc(F)cc2)CC1
CHEMBL2021979 hrh3_human Human No 5.0 IC50 = 10000 nM Bind
Displacement of [125H]iodoproxyphan from human histamine H3 receptor expressed in CHO-K1 cellsDisplacement of [125H]iodoproxyphan from human histamine H3 receptor expressed in CHO-K1 cells
499 9 2 5 4.9 O=C(Nc1ccc(C(F)(F)F)cc1)NS(=O)(=O)c1ccc(OCCCCN2CCCCC2)cc1
CHEMBL2024309 hrh3_human Human Yes 5.0 IC50 = 10000 nM Bind
Displacement of [125H]iodoproxyphan from human histamine H3 receptor expressed in CHO-K1 cellsDisplacement of [125H]iodoproxyphan from human histamine H3 receptor expressed in CHO-K1 cells
284 5 1 4 1.2 NS(=O)(=O)c1ccc(OCCN2CCCCC2)cc1
CHEMBL2024390 hrh3_human Human No 5.0 IC50 = 10000 nM Bind
Displacement of [125H]iodoproxyphan from human histamine H3 receptor expressed in CHO-K1 cellsDisplacement of [125H]iodoproxyphan from human histamine H3 receptor expressed in CHO-K1 cells
403 7 2 5 3.1 O=C(Nc1ccccc1)NS(=O)(=O)c1ccc(OCCN2CCCCC2)cc1
CHEMBL1222730 hrh3_human Human No 7.0 IC50 = 102 nM Funct
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
453 6 0 7 3.9 c1ccc(Cn2nnnc2C(c2ccc3ncccc3c2)N2CCCN(C3CCC3)CC2)cc1
CHEMBL485234 hrh3_human Human No 7.0 IC50 = 103 nM Funct
Antagonist activity at human cloned histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS bindingAntagonist activity at human cloned histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding
375 4 0 5 3.7 Cc1nc2ccccc2c(=O)n1-c1ccc(OC2CCN(C3CCC3)C2)cc1
CHEMBL260374 hrh3_human Human Yes 6.0 IC50 = 1030 nM Bind
Inhibition of human H3R expressed in methylhistamine-induced human H3-bla U2OS cells incubated for 30 mins by beta-lactamase complementation technologyInhibition of human H3R expressed in methylhistamine-induced human H3-bla U2OS cells incubated for 30 mins by beta-lactamase complementation technology
292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1
CHEMBL2419585 hrh3_human Human No 6.0 IC50 = 1040 nM Funct
Antagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed by forskolin induced cAMP response element activation after 5 hrs by luciferase reporter gene assayAntagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed by forskolin induced cAMP response element activation after 5 hrs by luciferase reporter gene assay
348 5 1 3 4.3 O=C(Cc1c[nH]c2ccccc12)Oc1ccc(CN2CCCCC2)cc1
CHEMBL2021987 hrh3_human Human No 5.0 IC50 = 10400 nM Bind
Displacement of [125H]iodoproxyphan from human histamine H3 receptor expressed in CHO-K1 cellsDisplacement of [125H]iodoproxyphan from human histamine H3 receptor expressed in CHO-K1 cells
485 8 2 5 4.5 O=C(Nc1ccccc1C(F)(F)F)NS(=O)(=O)c1ccc(OCCCN2CCCCC2)cc1
CHEMBL3677874 hrh3_human Human No 7.0 IC50 = 105 nM Bind
SPA Assay: The H3 binding assay was/can be used to evaluate the ability of at least one compound in accordance with formula I, Ia, Ib, and/or Ic to inhibit [3H]-N-α-methylhistamine binding to CHO-K1 membranes expressing human histamine H3 receptors (full-length H3, the most prevalent brain isoform 445). In 200 μl 96-well SPA format, human H3 membranes (12.5 μg protein/well) and 1.4 nM [3H]-N-α-methylhistamine were/can be incubated with at least one compound in accordance with formula I, Ia, Ib, and/or Ic for 1.5 hrs to determine percent effect with respect to total (1% DMSO) and non-specific binding (10 μM imetit). Reproducibility of the assay is such that IC50 curves can be generated in singlicate.SPA Assay: The H3 binding assay was/can be used to evaluate the ability of at least one compound in accordance with formula I, Ia, Ib, and/or Ic to inhibit [3H]-N-α-methylhistamine binding to CHO-K1 membranes expressing human histamine H3 receptors (full-length H3, the most prevalent brain isoform 445). In 200 μl 96-well SPA format, human H3 membranes (12.5 μg protein/well) and 1.4 nM [3H]-N-α-methylhistamine were/can be incubated with at least one compound in accordance with formula I, Ia, Ib, and/or Ic for 1.5 hrs to determine percent effect with respect to total (1% DMSO) and non-specific binding (10 μM imetit). Reproducibility of the assay is such that IC50 curves can be generated in singlicate.
312 3 0 2 3.3 O=C([C@H]1CC1c1ccccc1)N1CCN(C2CCCCC2)CC1
CHEMBL4765168 hrh3_human Human No 7.0 IC50 = 107.8 nM Funct
Antagonist activity at human histamine H3 receptor expressed in HEK293 cells preincubated for 5 mins followed by forskolin-stimulation and measured after 5 hrs by CRE-driven luciferase reporter gene assayAntagonist activity at human histamine H3 receptor expressed in HEK293 cells preincubated for 5 mins followed by forskolin-stimulation and measured after 5 hrs by CRE-driven luciferase reporter gene assay
358 7 0 6 2.3 COc1c(C)n(-c2ccc(OCCCN3CCOCC3)cc2)ccc1=O
CHEMBL1269843 hrh3_human Human Yes 8.0 IC50 = 11 nM Funct
Antagonist activity against human histamine H3 receptor expressed in human HT1080 cells assessed as inhibition of (R)-alpha-methylhistamine-induced increase in intracellular calcium level by FLIPR assayAntagonist activity against human histamine H3 receptor expressed in human HT1080 cells assessed as inhibition of (R)-alpha-methylhistamine-induced increase in intracellular calcium level by FLIPR assay
293 0 1 2 3.3 CC1CC(O)(C#Cc2cccc3ccccc23)C(C)CN1C
CHEMBL3127684 hrh3_human Human No 8.0 IC50 = 11 nM Funct
Antagonist activity at human histamine H3 receptor long form expressed in CHOK1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding after 3 hrs by scintillation proximity assayAntagonist activity at human histamine H3 receptor long form expressed in CHOK1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding after 3 hrs by scintillation proximity assay
369 3 0 4 1.1 CS(=O)(=O)N1CCC2(CC1)CC(C(=O)N1CCN(C3CCC3)CC1)C2
CHEMBL478628 hrh3_human Human No 8.0 IC50 = 11 nM Funct
Inverse agonist activity at human histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of N-alpha-methylhistamine-induced [35S]GTPgammaS bindingInverse agonist activity at human histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of N-alpha-methylhistamine-induced [35S]GTPgammaS binding
391 6 0 5 4.3 Cc1nc2ccccc2c(=O)n1-c1ccc(OCCCN2CCCCC2C)cc1
CHEMBL3677900 hrh3_human Human No 7.9 IC50 = 11.6 nM Bind
Guanosine 5'-O-(3-[35S]thio)triphosphate [GTP gamma S] Binding Assay: A GTP gamma S binding assay can be used to investigate antagonist properties of compounds in CHO cells (Chinese Hamster Ovary) transfected with human Histamine H3 receptor (hH3R). Membranes from CHO cells expressing hH3R (10 ug/well) are diluted in GTP gamma S assay buffer (20 mM Hepes, 10 mM MgCl2, 100 mM NaCl, pH 7.4) and preincubated with saponine (3 ug/ml), GDP (10 uM) and PVT-WGA SPA beads (125 ug/well) (Amersham) for 30 minutes. To determine antagonist activity, (R)-methyl histamine (30 nM) is added in 96 well SPA plate with [35S]GTP gamma S (0.2 nM) and various concentration of H3R antagonists. The GTP gamma S binding assay is started with addition of the mixture membrane/saponine/GDP and incubated for 90 minutes at room temperature. The amount of bound [35S]GTP gamma S is determined by using the MicroBeta Trilux counter (PerkinElmer). The percentage of [35S]GTP gamma S bound in each sample is calculated as a percentage of that bound control sample.Guanosine 5'-O-(3-[35S]thio)triphosphate [GTP gamma S] Binding Assay: A GTP gamma S binding assay can be used to investigate antagonist properties of compounds in CHO cells (Chinese Hamster Ovary) transfected with human Histamine H3 receptor (hH3R). Membranes from CHO cells expressing hH3R (10 ug/well) are diluted in GTP gamma S assay buffer (20 mM Hepes, 10 mM MgCl2, 100 mM NaCl, pH 7.4) and preincubated with saponine (3 ug/ml), GDP (10 uM) and PVT-WGA SPA beads (125 ug/well) (Amersham) for 30 minutes. To determine antagonist activity, (R)-methyl histamine (30 nM) is added in 96 well SPA plate with [35S]GTP gamma S (0.2 nM) and various concentration of H3R antagonists. The GTP gamma S binding assay is started with addition of the mixture membrane/saponine/GDP and incubated for 90 minutes at room temperature. The amount of bound [35S]GTP gamma S is determined by using the MicroBeta Trilux counter (PerkinElmer). The percentage of [35S]GTP gamma S bound in each sample is calculated as a percentage of that bound control sample.
367 4 0 3 2.6 O=C(C1CC1c1cccc(N2CCCC2=O)c1)N1CCN(C2CCC2)CC1
CHEMBL491614 hrh3_human Human No 7.0 IC50 = 110 nM Funct
Inverse agonist activity at human cloned histamine H3 receptor assessed as inhibition of (R)-alpha-methylhistamine-induced [35S]GTPgammaS bindingInverse agonist activity at human cloned histamine H3 receptor assessed as inhibition of (R)-alpha-methylhistamine-induced [35S]GTPgammaS binding
379 4 0 2 4.6 CN(CCN1CCCCC1)C(=O)N1CCC(c2ccc3ccccc3c2)CC1
CHEMBL3127697 hrh3_human Human Yes 6.0 IC50 = 1100 nM Funct
Antagonist activity at human histamine H3 receptor long form expressed in CHOK1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding after 3 hrs by scintillation proximity assayAntagonist activity at human histamine H3 receptor long form expressed in CHOK1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding after 3 hrs by scintillation proximity assay
321 2 0 4 1.0 CN1CCN(C(=O)C2CC23CCN(C2CCOCC2)CC3)CC1
CHEMBL4796300 hrh3_human Human No 5.0 IC50 = 11000 nM Bind
Displacement of [3H]-N-alpha-methylhistamine from recombinant human histamine H3 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting methodDisplacement of [3H]-N-alpha-methylhistamine from recombinant human histamine H3 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting method
317 1 0 7 1.5 CN1CCCN(c2nc3ncc(Cl)cc3n3cnnc23)CC1
CHEMBL2387300 hrh3_human Human No 7.0 IC50 = 111.4 nM Funct
Antagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of calcium mobilization by FLIPR assay
363 8 2 3 4.3 CCN(CC)CCOc1ccc(NC(=O)Nc2ccc(F)cc2F)cc1
CHEMBL1223449 hrh3_human Human No 6.9 IC50 = 115 nM Funct
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
480 6 0 6 4.1 Brc1ccc(C(c2nnnn2Cc2ccccc2)N2CCCN(C3CCC3)CC2)cc1
CHEMBL2021981 hrh3_human Human No 4.9 IC50 = 11800 nM Bind
Displacement of [125H]iodoproxyphan from human histamine H3 receptor expressed in CHO-K1 cellsDisplacement of [125H]iodoproxyphan from human histamine H3 receptor expressed in CHO-K1 cells
471 8 2 5 4.1 O=C(Nc1cccc(C(F)(F)F)c1)NS(=O)(=O)c1ccc(OCCCN2CCCC2)cc1
CHEMBL1269844 hrh3_mouse Mouse No 6.9 IC50 = 119 nM Funct
Antagonist activity against mouse histamine H3 receptor expressed in human HT1080 cells assessed as inhibition of (R)-alpha-methylhistamine-induced increase in intracellular calcium level by FLIPR assayAntagonist activity against mouse histamine H3 receptor expressed in human HT1080 cells assessed as inhibition of (R)-alpha-methylhistamine-induced increase in intracellular calcium level by FLIPR assay
293 0 1 2 3.3 C[C@H]1CN(C)[C@H](C)C[C@@]1(O)C#Cc1cccc2ccccc12
CHEMBL1222662 hrh3_human Human No 6.9 IC50 = 119 nM Funct
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
441 6 1 6 3.9 c1ccc(Cn2nnnc2C(c2ccc3[nH]ccc3c2)N2CCCN(C3CCC3)CC2)cc1
CHEMBL1270264 hrh3_human Human No 7.9 IC50 = 12 nM Funct
Antagonist activity against human histamine H3 receptor expressed in human HT1080 cells assessed as inhibition of (R)-alpha-methylhistamine-induced increase in intracellular calcium level by FLIPR assayAntagonist activity against human histamine H3 receptor expressed in human HT1080 cells assessed as inhibition of (R)-alpha-methylhistamine-induced increase in intracellular calcium level by FLIPR assay
294 0 1 3 2.7 CC1CC(O)(C#Cc2cccc3ncccc23)C(C)CN1C
CHEMBL462605 hrh3_human Human Yes 7.9 IC50 = 12 nM Funct
Antagonist activity at human cloned histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS bindingAntagonist activity at human cloned histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding
295 8 0 2 4.2 Clc1ccc(cc1)CCCOCCCN1CCCCC1
CHEMBL1222596 hrh3_human Human No 7.9 IC50 = 12 nM Funct
Antagonist activity at human histamine H3 receptorAntagonist activity at human histamine H3 receptor
496 8 0 9 4.0 c1ccc(Cn2nnnc2C(c2ccc(Oc3ncccn3)cc2)N2CCCN(C3CCC3)CC2)cc1
CHEMBL3127687 hrh3_human Human No 7.9 IC50 = 12 nM Funct
Antagonist activity at human histamine H3 receptor long form expressed in CHOK1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding after 3 hrs by scintillation proximity assayAntagonist activity at human histamine H3 receptor long form expressed in CHOK1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding after 3 hrs by scintillation proximity assay
397 3 0 3 3.3 CC(C)N1CCCN(C(=O)C2CC3(CCN(C(=O)c4ccccc4)CC3)C2)CC1
CHEMBL3127702 hrh3_human Human No 7.9 IC50 = 12 nM Funct
Antagonist activity at human histamine H3 receptor long form expressed in CHOK1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding after 3 hrs by scintillation proximity assayAntagonist activity at human histamine H3 receptor long form expressed in CHOK1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding after 3 hrs by scintillation proximity assay
389 3 0 4 2.7 O=C(C1CC12CCN(C1CCOCC1)CC2)N1CCN(C2CCCCC2)CC1
CHEMBL1221429 hrh3_rat Rat No 7.9 IC50 = 12 nM Funct
Antagonist activity at rat histamine H3 receptorAntagonist activity at rat histamine H3 receptor
459 7 1 7 2.7 CNC(=O)c1ccc(C(c2nnnn2Cc2ccccc2)N2CCCN(C3CCC3)CC2)cc1
CHEMBL206346 hrh3_human Human Yes 7.9 IC50 = 12.6 nM Funct
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
235 7 2 2 3.0 C(CCc1cnc[nH]1)CCNC1CCCCC1
CHEMBL4462662 hrh3_human Human No 7.9 IC50 = 12.8 nM Funct
Antagonist activity at human histamine H3 receptor stably expressed in HEK293 cells assessed as cAMP accumulation incubated for 60 mins by Eu-cAMP tracer based TR-FRET assayAntagonist activity at human histamine H3 receptor stably expressed in HEK293 cells assessed as cAMP accumulation incubated for 60 mins by Eu-cAMP tracer based TR-FRET assay
330 8 1 5 3.0 CCN(CC)CCCOc1ccc(-n2ccc(=O)c(O)c2C)cc1
CHEMBL260374 hrh3_human Human Yes 6.9 IC50 = 120 nM Funct
Antagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed by forskolin induced cAMP response element activation after 5 hrs by luciferase reporter gene assayAntagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed by forskolin induced cAMP response element activation after 5 hrs by luciferase reporter gene assay
292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1
CHEMBL2419569 hrh3_human Human No 5.9 IC50 = 1210 nM Funct
Antagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed by forskolin induced cAMP response element activation after 5 hrs by luciferase reporter gene assayAntagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed by forskolin induced cAMP response element activation after 5 hrs by luciferase reporter gene assay
333 4 2 2 4.4 O=C(Nc1ccc(CN2CCCCC2)cc1)c1c[nH]c2ccccc12
CHEMBL1270165 hrh3_mouse Mouse No 6.9 IC50 = 122 nM Funct
Antagonist activity against mouse histamine H3 receptor expressed in human HT1080 cells assessed as inhibition of (R)-alpha-methylhistamine-induced increase in intracellular calcium level by FLIPR assayAntagonist activity against mouse histamine H3 receptor expressed in human HT1080 cells assessed as inhibition of (R)-alpha-methylhistamine-induced increase in intracellular calcium level by FLIPR assay
297 3 1 2 3.9 CC1CC(O)(CCc2ccc3ccccc3c2)C(C)CN1C
CHEMBL4565419 hrh3_human Human No 4.9 IC50 = 12300 nM Funct
Antagonist activity at recombinant human Gi-coupled H3 receptor expressed in HEK293T cells assessed as reduction in histamine-induced inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by histamine addition for 10 mins and subsequent forskolin-stimulation by Glo-sensor assayAntagonist activity at recombinant human Gi-coupled H3 receptor expressed in HEK293T cells assessed as reduction in histamine-induced inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by histamine addition for 10 mins and subsequent forskolin-stimulation by Glo-sensor assay
284 2 1 5 3.1 CC1CCCc2c(-c3ccc([N+](=O)[O-])cc3)nc(N)nc21
CHEMBL4565419 hrh3_human Human No 4.9 IC50 = 12302.7 nM Funct
Antagonist activity at recombinant human Gi-coupled H3 receptor expressed in HEK293T cells assessed as reduction in histamine-induced inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by histamine addition for 10 mins and subsequent forskolin-stimulation by Glo-sensor assayAntagonist activity at recombinant human Gi-coupled H3 receptor expressed in HEK293T cells assessed as reduction in histamine-induced inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by histamine addition for 10 mins and subsequent forskolin-stimulation by Glo-sensor assay
284 2 1 5 3.1 CC1CCCc2c(-c3ccc([N+](=O)[O-])cc3)nc(N)nc21
CHEMBL2441947 hrh3_human Human No 6.9 IC50 = 125.9 nM Funct
Antagonist activity at human histamine H3 receptor expressed in CHO cells assessed as inhibition of forskolin/R-alpha-methylhistamine-induced cAMP accumulation after 1.5 hrs by TR-FRET immunoassayAntagonist activity at human histamine H3 receptor expressed in CHO cells assessed as inhibition of forskolin/R-alpha-methylhistamine-induced cAMP accumulation after 1.5 hrs by TR-FRET immunoassay
336 9 1 2 4.0 O=C(CCCN1CCCCC1)NCCCCc1ccc(Cl)cc1
CHEMBL3040649 hrh3_human Human No 6.9 IC50 = 125.9 nM Funct
Antagonist activity at human histamine H3 receptor expressed in CHO cells assessed as inhibition of forskolin/R-alpha-methylhistamine-induced cAMP accumulation after 1.5 hrs by TR-FRET immunoassayAntagonist activity at human histamine H3 receptor expressed in CHO cells assessed as inhibition of forskolin/R-alpha-methylhistamine-induced cAMP accumulation after 1.5 hrs by TR-FRET immunoassay
336 9 1 2 4.0 O=C(CCCN1CCCCC1)NCCCCc1ccc(Cl)cc1
CHEMBL2441948 hrh3_human Human No 6.9 IC50 = 125.9 nM Funct
Antagonist activity at human histamine H3 receptor expressed in CHO cells assessed as inhibition of forskolin/R-alpha-methylhistamine-induced cAMP accumulation after 1.5 hrs by TR-FRET immunoassayAntagonist activity at human histamine H3 receptor expressed in CHO cells assessed as inhibition of forskolin/R-alpha-methylhistamine-induced cAMP accumulation after 1.5 hrs by TR-FRET immunoassay
370 9 1 2 4.4 O=C(CCCN1CCCCC1)NCCCCc1ccc(C(F)(F)F)cc1
CHEMBL3040708 hrh3_human Human No 6.9 IC50 = 125.9 nM Funct
Antagonist activity at human histamine H3 receptor expressed in CHO cells assessed as inhibition of forskolin/R-alpha-methylhistamine-induced cAMP accumulation after 1.5 hrs by TR-FRET immunoassayAntagonist activity at human histamine H3 receptor expressed in CHO cells assessed as inhibition of forskolin/R-alpha-methylhistamine-induced cAMP accumulation after 1.5 hrs by TR-FRET immunoassay
370 9 1 2 4.4 O=C(CCCN1CCCCC1)NCCCCc1ccc(C(F)(F)F)cc1