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
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H don H acc LogP Smiles
CHEMBL4454158 hrh4_rat Rat No 10.3 EC50 = 0.1 nM Funct
Agonist activity at rat H4R expressed in HEK293-SF-rH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at rat H4R expressed in HEK293-SF-rH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
286 3 2 5 2.2 CC(C)(C)CNc1nccc(N2CCc3nc[nH]c3C2)n1
CHEMBL4597218 hrh4_rat Rat No 10.3 EC50 = 0.1 nM Funct
Agonist activity at rat H4R expressed in HEK293-SF-rH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at rat H4R expressed in HEK293-SF-rH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
286 3 2 5 2.2 CC(C)(C)CNc1nccc(N2CCc3nc[nH]c3C2)n1
CHEMBL4454158 hrh4_human Human No 9.9 EC50 = 0.1 nM Funct
Agonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
286 3 2 5 2.2 CC(C)(C)CNc1nccc(N2CCc3nc[nH]c3C2)n1
CHEMBL4597218 hrh4_human Human No 9.9 EC50 = 0.1 nM Funct
Agonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
286 3 2 5 2.2 CC(C)(C)CNc1nccc(N2CCc3nc[nH]c3C2)n1
CHEMBL4454158 hrh4_mouse Mouse No 9.6 EC50 = 0.3 nM Funct
Agonist activity at mouse H4R expressed in HEK293-SF-mH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at mouse H4R expressed in HEK293-SF-mH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
286 3 2 5 2.2 CC(C)(C)CNc1nccc(N2CCc3nc[nH]c3C2)n1
CHEMBL4597218 hrh4_mouse Mouse No 9.6 EC50 = 0.3 nM Funct
Agonist activity at mouse H4R expressed in HEK293-SF-mH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at mouse H4R expressed in HEK293-SF-mH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
286 3 2 5 2.2 CC(C)(C)CNc1nccc(N2CCc3nc[nH]c3C2)n1
CHEMBL1083162 hrh4_human Human No 9.3 EC50 = 0.6 nM Funct
Agonist activity at human histamine H4 receptor in SK-N-MC cells assessed as forskolin-stimulated cAMP release preincubated for 10 mins before forskolin challengeAgonist activity at human histamine H4 receptor in SK-N-MC cells assessed as forskolin-stimulated cAMP release preincubated for 10 mins before forskolin challenge
407 9 3 4 4.3 Cc1cc(OCCCNCCc2c[nH]cn2)ccc1-c1nc2c(C)c(F)ccc2[nH]1
CHEMBL4443126 hrh4_human Human No 9.2 EC50 = 0.6 nM Funct
Agonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
263 4 2 5 1.7 CN[C@@H]1CCN(c2ccnc(NCC(C)(C)C)n2)C1
CHEMBL4596409 hrh4_human Human No 9.2 EC50 = 0.6 nM Funct
Agonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
263 4 2 5 1.7 CN[C@@H]1CCN(c2ccnc(NCC(C)(C)C)n2)C1
CHEMBL4443126 hrh4_rat Rat No 9.2 EC50 = 0.6 nM Funct
Agonist activity at rat H4R expressed in HEK293-SF-rH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at rat H4R expressed in HEK293-SF-rH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
263 4 2 5 1.7 CN[C@@H]1CCN(c2ccnc(NCC(C)(C)C)n2)C1
CHEMBL4596409 hrh4_rat Rat No 9.2 EC50 = 0.6 nM Funct
Agonist activity at rat H4R expressed in HEK293-SF-rH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at rat H4R expressed in HEK293-SF-rH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
263 4 2 5 1.7 CN[C@@H]1CCN(c2ccnc(NCC(C)(C)C)n2)C1
CHEMBL4439142 hrh4_rat Rat No 9.2 EC50 = 0.6 nM Funct
Agonist activity at rat H4R expressed in HEK293-SF-rH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at rat H4R expressed in HEK293-SF-rH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
277 4 1 5 2.1 CN(C)[C@@H]1CCN(c2ccnc(NCC(C)(C)C)n2)C1
CHEMBL4515149 hrh4_rat Rat No 9.2 EC50 = 0.6 nM Funct
Agonist activity at rat H4R expressed in HEK293-SF-rH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at rat H4R expressed in HEK293-SF-rH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
277 4 1 5 2.1 CN(C)[C@@H]1CCN(c2ccnc(NCC(C)(C)C)n2)C1
CHEMBL4595327 hrh4_rat Rat No 9.2 EC50 = 0.6 nM Funct
Agonist activity at rat H4R expressed in HEK293-SF-rH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at rat H4R expressed in HEK293-SF-rH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
277 4 1 5 2.1 CN(C)[C@@H]1CCN(c2ccnc(NCC(C)(C)C)n2)C1
CHEMBL1688946 hrh4_human Human No 9.0 EC50 = 1 nM Funct
Agonist activity at human histamine H4 receptor expressed in HEK293 cells assessed by forskolin induced cAMP response element activation by luciferase reporter gene assayAgonist activity at human histamine H4 receptor expressed in HEK293 cells assessed by forskolin induced cAMP response element activation by luciferase reporter gene assay
273 6 1 4 2.8 C1CCC(CC1)CC2=CN(N=N2)CCCC3=CN=CN3
CHEMBL4441731 hrh4_mouse Mouse Yes 9.0 EC50 = 1 nM Funct
Agonist activity at mouse H4R expressed on HEK293T 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 H4R expressed on HEK293T 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 hrh4_mouse Mouse Yes 9.0 EC50 = 1 nM Funct
Agonist activity at mouse H4R expressed on HEK293T 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 H4R expressed on HEK293T 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
CHEMBL4439142 hrh4_mouse Mouse No 9.0 EC50 = 1.0 nM Funct
Agonist activity at mouse H4R expressed in HEK293-SF-mH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at mouse H4R expressed in HEK293-SF-mH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
277 4 1 5 2.1 CN(C)[C@@H]1CCN(c2ccnc(NCC(C)(C)C)n2)C1
CHEMBL4515149 hrh4_mouse Mouse No 9.0 EC50 = 1.0 nM Funct
Agonist activity at mouse H4R expressed in HEK293-SF-mH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at mouse H4R expressed in HEK293-SF-mH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
277 4 1 5 2.1 CN(C)[C@@H]1CCN(c2ccnc(NCC(C)(C)C)n2)C1
CHEMBL4595327 hrh4_mouse Mouse No 9.0 EC50 = 1.0 nM Funct
Agonist activity at mouse H4R expressed in HEK293-SF-mH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at mouse H4R expressed in HEK293-SF-mH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
277 4 1 5 2.1 CN(C)[C@@H]1CCN(c2ccnc(NCC(C)(C)C)n2)C1
CHEMBL4443126 hrh4_mouse Mouse No 9.0 EC50 = 1.1 nM Funct
Agonist activity at mouse H4R expressed in HEK293-SF-mH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at mouse H4R expressed in HEK293-SF-mH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
263 4 2 5 1.7 CN[C@@H]1CCN(c2ccnc(NCC(C)(C)C)n2)C1
CHEMBL4596409 hrh4_mouse Mouse No 9.0 EC50 = 1.1 nM Funct
Agonist activity at mouse H4R expressed in HEK293-SF-mH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at mouse H4R expressed in HEK293-SF-mH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
263 4 2 5 1.7 CN[C@@H]1CCN(c2ccnc(NCC(C)(C)C)n2)C1
CHEMBL595180 hrh4_human Human No 9.0 EC50 = 1.1 nM Funct
Agonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of [35S]GTPgammaS binding
366 4 2 6 2.7 CN1CCN(CC1)c1cc(NCc2c(Cl)cccc2Cl)nc(n1)N
CHEMBL4543119 hrh4_rat Rat No 8.9 EC50 = 1.2 nM Funct
Agonist activity at rat H4R expressed in HEK293-SF-rH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at rat H4R expressed in HEK293-SF-rH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
277 3 1 5 2.1 CN1CCCN(c2ccnc(NCC(C)(C)C)n2)CC1
CHEMBL4596606 hrh4_rat Rat No 8.9 EC50 = 1.2 nM Funct
Agonist activity at rat H4R expressed in HEK293-SF-rH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at rat H4R expressed in HEK293-SF-rH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
277 3 1 5 2.1 CN1CCCN(c2ccnc(NCC(C)(C)C)n2)CC1
CHEMBL4445423 hrh4_rat Rat No 8.9 EC50 = 1.4 nM Funct
Agonist activity at rat H4R expressed in HEK293-SF-rH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at rat H4R expressed in HEK293-SF-rH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
291 4 4 5 1.0 CC(C)(C)CNc1nccc(N2CC[C@@H](NC(=N)N)C2)n1
CHEMBL4598198 hrh4_rat Rat No 8.9 EC50 = 1.4 nM Funct
Agonist activity at rat H4R expressed in HEK293-SF-rH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at rat H4R expressed in HEK293-SF-rH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
291 4 4 5 1.0 CC(C)(C)CNc1nccc(N2CC[C@@H](NC(=N)N)C2)n1
CHEMBL595180 hrh4_human Human No 8.9 EC50 = 1.4 nM Funct
Agonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of GTPase by [gamma-32P]GTP spontaneous degradation assayAgonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of GTPase by [gamma-32P]GTP spontaneous degradation assay
366 4 2 6 2.7 CN1CCN(CC1)c1cc(NCc2c(Cl)cccc2Cl)nc(n1)N
CHEMBL4455324 hrh4_rat Rat No 8.8 EC50 = 1.8 nM Funct
Agonist activity at rat H4R expressed in HEK293-SF-rH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at rat H4R expressed in HEK293-SF-rH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
249 3 2 5 1.5 CC(C)(C)CNc1nccc(N2CC[C@@H](N)C2)n1
CHEMBL4596881 hrh4_rat Rat No 8.8 EC50 = 1.8 nM Funct
Agonist activity at rat H4R expressed in HEK293-SF-rH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at rat H4R expressed in HEK293-SF-rH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
249 3 2 5 1.5 CC(C)(C)CNc1nccc(N2CC[C@@H](N)C2)n1
CHEMBL4439142 hrh4_human Human No 8.7 EC50 = 1.9 nM Funct
Agonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
277 4 1 5 2.1 CN(C)[C@@H]1CCN(c2ccnc(NCC(C)(C)C)n2)C1
CHEMBL4515149 hrh4_human Human No 8.7 EC50 = 1.9 nM Funct
Agonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
277 4 1 5 2.1 CN(C)[C@@H]1CCN(c2ccnc(NCC(C)(C)C)n2)C1
CHEMBL4595327 hrh4_human Human No 8.7 EC50 = 1.9 nM Funct
Agonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
277 4 1 5 2.1 CN(C)[C@@H]1CCN(c2ccnc(NCC(C)(C)C)n2)C1
CHEMBL1632413 hrh4_mouse Mouse No 8.0 EC50 = 10 nM Funct
Agonist activity at mouse histamine H4 receptor by luciferase reporter gene assayAgonist activity at mouse histamine H4 receptor by luciferase reporter gene assay
292 1 2 3 2.2 CN1CCN(/C(=N\O)c2cc3cc(Cl)ccc3[nH]2)CC1
CHEMBL1632413 hrh4_rat Rat No 8.0 EC50 = 10 nM Funct
Agonist activity at rat histamine H4 receptor by luciferase reporter gene assayAgonist activity at rat histamine H4 receptor by luciferase reporter gene assay
292 1 2 3 2.2 CN1CCN(/C(=N\O)c2cc3cc(Cl)ccc3[nH]2)CC1
CHEMBL502347 hrh4_rat Rat Yes 8.0 EC50 = 10 nM Funct
Antagonist activity at rat histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assayAntagonist activity at rat histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assay
295 1 2 5 1.8 Nc1nc2c(c(N3CC[C@@H](N)C3)n1)CCCc1ccccc1-2
CHEMBL309819 hrh4_human Human No 7.0 EC50 = 100 nM Funct
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
226 6 3 2 1.6 CC/N=C(\S)NCCCCc1c[nH]cn1
CHEMBL3804906 hrh4_human Human No 7.0 EC50 = 100 nM Funct
Agonist activity at human histamine H4 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 H4 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
CHEMBL1632412 hrh4_human Human No 7.0 EC50 = 100 nM Funct
Agonist activity at human recombinant histamine H4 receptor expressed in human SK-N-MC cells co-expressing SRE-Luc by luciferase reporter gene assayAgonist activity at human recombinant histamine H4 receptor expressed in human SK-N-MC cells co-expressing SRE-Luc by luciferase reporter gene assay
271 2 2 3 3.0 Cc1ccc2[nH]c(/C(=N\O)C3CCN(C)CC3)cc2c1
CHEMBL1688969 hrh4_human Human No 6.0 EC50 = 1000 nM Bind
Agonist activity at histamine H4 receptor (unknown origin) expressed in human U2OS cells increase in beta-arrestin2 recruitment after 2 hrs by luminescence assayAgonist activity at histamine H4 receptor (unknown origin) expressed in human U2OS cells increase in beta-arrestin2 recruitment after 2 hrs by luminescence assay
259 5 1 4 2.4 C1CCC(CC1)CC2=CN(N=N2)CCC3=CN=CN3
CHEMBL2047474 hrh4_human Human No 6.0 EC50 = 1000 nM Bind
Agonist activity at histamine H4 receptor (unknown origin) expressed in human U2OS cells increase in beta-arrestin2 recruitment after 2 hrs by luminescence assayAgonist activity at histamine H4 receptor (unknown origin) expressed in human U2OS cells increase in beta-arrestin2 recruitment after 2 hrs by luminescence assay
322 2 1 4 2.1 CN1CCN(C(=O)c2cc3cc(Cl)cc([N+](=O)[O-])c3[nH]2)CC1
CHEMBL82298 hrh4_human Human Yes 6.0 EC50 = 1000 nM Funct
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H4 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
CHEMBL3393556 hrh4_human Human No 6.0 EC50 = 1000 nM Funct
Agonist activity at human recombinant histamine H4 receptor expressed in SK-N-MC cells assessed as effect on forskolin-stimulated cAMP-mediated reporter gene activityAgonist activity at human recombinant histamine H4 receptor expressed in SK-N-MC cells assessed as effect on forskolin-stimulated cAMP-mediated reporter gene activity
287 4 2 5 1.9 CN[C@@H]1CCN(c2cnnc(NC3CC4CCC3C4)c2)C1
CHEMBL3220892 hrh4_human Human No 6.0 EC50 = 1000 nM Bind
Agonist activity at human recombinant histamine H4 receptor-RGS19 fusion protein expressed in Sf9 cells coexpressing Galphai2,Gbeta1gamma2 preincubated for 2 mins before [gamma32P]GTP addition measured after 20 mins by steady-state GTPase activity assayAgonist activity at human recombinant histamine H4 receptor-RGS19 fusion protein expressed in Sf9 cells coexpressing Galphai2,Gbeta1gamma2 preincubated for 2 mins before [gamma32P]GTP addition measured after 20 mins by steady-state GTPase activity assay
313 7 2 3 1.9 CC(CC(=O)/N=C(\N)NCCCn1ccnc1)c1ccccc1
CHEMBL26116 hrh4_human Human Yes 5.0 EC50 = 10000 nM Funct
Agonist activity at human recombinant histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2 by steady-state GTPase activity assayAgonist activity at human recombinant histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2 by steady-state GTPase activity assay
265 3 2 2 2.3 NCCc1cnc([nH]1)c1cccc(c1)Br
CHEMBL1771001 hrh4_human Human No 7.0 EC50 = 101 nM Funct
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells assessed as effect on forskolin-induced cAMP accumulation after 6 hrsAgonist activity at human histamine H4 receptor expressed in human SK-N-MC cells assessed as effect on forskolin-induced cAMP accumulation after 6 hrs
276 3 2 6 1.2 CN1CCN(c2cc(NC3CCCC3)nc(N)n2)CC1
CHEMBL378788 hrh4_human Human No 7.0 EC50 = 102.3 nM Funct
Activity at human histamine H4 receptor transfected in SK-N-MC cells by cAMP assayActivity at human histamine H4 receptor transfected in SK-N-MC cells by cAMP assay
361 0 0 4 4.4 CN1CCN(C2=Nc3cc(Cl)ccc3Oc3cc(Cl)ccc32)CC1
CHEMBL596551 hrh4_human Human No 7.0 EC50 = 102.3 nM Funct
Agonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of [35S]GTPgammaS binding
314 4 3 7 1.1 CN1CCN(c2cc(NCc3ccc(O)cc3)nc(N)n2)CC1
CHEMBL494890 hrh4_mouse Mouse Yes 7.0 EC50 = 102.3 nM Funct
Agonist activity at mouse histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at mouse histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
280 2 2 6 1.0 N#Cc1ccc(-c2cc(N3CCNCC3)nc(N)n2)cc1
CHEMBL494576 hrh4_rat Rat No 7.0 EC50 = 102.3 nM Funct
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
273 2 1 7 0.2 CN1CCN(c2cc(-c3cn(C)cn3)nc(N)n2)CC1
CHEMBL494724 hrh4_rat Rat No 7.0 EC50 = 102.3 nM Funct
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
299 3 1 6 1.5 COc1cccc(-c2cc(N3CCN(C)CC3)nc(N)n2)c1
CHEMBL494890 hrh4_mouse Mouse Yes 7.0 EC50 = 102.3 nM Funct
Antagonist activity at mouse histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assayAntagonist activity at mouse histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assay
280 2 2 6 1.0 N#Cc1ccc(-c2cc(N3CCNCC3)nc(N)n2)cc1
CHEMBL153051 hrh4_human Human Yes 6.0 EC50 = 1023.3 nM Bind
Inhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H4 receptorInhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H4 receptor
151 2 2 2 0.6 c1nc(C[C@@H]2CCNC2)c[nH]1
CHEMBL211242 hrh4_human Human No 7.0 EC50 = 104.7 nM Funct
Activity at human histamine H4 receptor transfected in SK-N-MC cells by cAMP assayActivity at human histamine H4 receptor transfected in SK-N-MC cells by cAMP assay
307 0 0 4 3.4 Cc1ccc2c(c1)Oc1ccccc1C(N1CCN(C)CC1)=N2
CHEMBL609161 hrh4_human Human No 7.0 EC50 = 104.7 nM Funct
Antagonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as inhibition of 100 nM dopamine-induced stimulation of [35S]GTPgammaS bindingAntagonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as inhibition of 100 nM dopamine-induced stimulation of [35S]GTPgammaS binding
312 4 2 6 1.7 Cc1ccc(CNc2cc(N3CCN(C)CC3)nc(N)n2)cc1
CHEMBL494910 hrh4_rat Rat Yes 5.0 EC50 = 10471.3 nM Funct
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
223 2 1 6 -0.2 COc1cc(N2CCN(C)CC2)nc(N)n1
CHEMBL81644 hrh4_human Human Yes 5.0 EC50 = 10471.3 nM Bind
Inhibition of the cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H4 receptorInhibition of the cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H4 receptor
159 2 1 2 1.4 c1ccc(Cc2c[nH]cn2)nc1
CHEMBL4437371 hrh4_mouse Mouse No 6.0 EC50 = 1071.5 nM Bind
Agonist activity at mouse H4R expressed in HEK293T-beta-arr2-mH4R cells by beta-arrestin2 recruitment assayAgonist activity at mouse H4R expressed in HEK293T-beta-arr2-mH4R cells by beta-arrestin2 recruitment assay
237 6 3 5 1.7 CC(C)(C)CNc1nccc(NCCCN)n1
CHEMBL4594753 hrh4_mouse Mouse No 6.0 EC50 = 1071.5 nM Bind
Agonist activity at mouse H4R expressed in HEK293T-beta-arr2-mH4R cells by beta-arrestin2 recruitment assayAgonist activity at mouse H4R expressed in HEK293T-beta-arr2-mH4R cells by beta-arrestin2 recruitment assay
237 6 3 5 1.7 CC(C)(C)CNc1nccc(NCCCN)n1
CHEMBL260374 hrh4_human Human Yes 7.0 EC50 = 109.7 nM Bind
Agonist activity at human H4 receptor expressed in insect Sf9 cells co-expressing RGS19 fusion protein and Gialpha2, Gbeta1gamma2 assessed as gamma[32P]GTP binding by liquid scintillation countingAgonist activity at human H4 receptor expressed in insect Sf9 cells co-expressing RGS19 fusion protein and Gialpha2, Gbeta1gamma2 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 hrh4_human Human Yes 7.0 EC50 = 109.7 nM Funct
Agonist activity at human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19 protein by steady-state GTPase assayAgonist activity at human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19 protein by steady-state GTPase assay
292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1
CHEMBL1078632 hrh4_human Human No 6.0 EC50 = 1096.5 nM Funct
Agonist activity at human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19 protein by steady-state GTPase assayAgonist activity at human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19 protein by steady-state GTPase assay
310 8 3 3 2.0 N#C/N=C(/NCCCCc1c[nH]cn1)NCCc1ccccc1
CHEMBL153284 hrh4_human Human Yes 6.0 EC50 = 1096.5 nM Bind
Inhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H4 receptorInhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H4 receptor
137 2 2 2 0.5 NCC1CC1c1c[nH]cn1
CHEMBL1770966 hrh4_human Human No 8.0 EC50 = 11 nM Funct
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells assessed as effect on forskolin-induced cAMP accumulation after 6 hrsAgonist activity at human histamine H4 receptor expressed in human SK-N-MC cells assessed as effect on forskolin-induced cAMP accumulation after 6 hrs
275 3 2 5 1.8 CN1CCN(c2cc(N)nc(NC3CCCC3)c2)CC1
CHEMBL90 hrh4_human Human Yes 8.0 EC50 = 11 nM Funct
Agonist activity at human histamine H4 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 H4 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
CHEMBL3805361 hrh4_human Human No 8.0 EC50 = 11 nM Funct
Agonist activity at human histamine H4 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 H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assay
368 7 3 4 3.1 N#C/N=C(/NCCSc1ccccc1)NC[C@H]1CC[C@H](c2c[nH]cn2)C1
CHEMBL4454158 hrh4_mouse Mouse No 7.9 EC50 = 11.5 nM Bind
Agonist activity at mouse H4R expressed in HEK293T-beta-arr2-mH4R cells by beta-arrestin2 recruitment assayAgonist activity at mouse H4R expressed in HEK293T-beta-arr2-mH4R cells by beta-arrestin2 recruitment assay
286 3 2 5 2.2 CC(C)(C)CNc1nccc(N2CCc3nc[nH]c3C2)n1
CHEMBL4597218 hrh4_mouse Mouse No 7.9 EC50 = 11.5 nM Bind
Agonist activity at mouse H4R expressed in HEK293T-beta-arr2-mH4R cells by beta-arrestin2 recruitment assayAgonist activity at mouse H4R expressed in HEK293T-beta-arr2-mH4R cells by beta-arrestin2 recruitment assay
286 3 2 5 2.2 CC(C)(C)CNc1nccc(N2CCc3nc[nH]c3C2)n1
CHEMBL90 hrh4_human Human Yes 7.9 EC50 = 11.6 nM Bind
Activity at human recombinant histamine H4 receptor-RGS4 fusion protein expressed in Sf9 cells coexpressing Galphai2 and G-beta-1-gamma-2 by steady-state GTPase activity assayActivity at human recombinant histamine H4 receptor-RGS4 fusion protein expressed in Sf9 cells coexpressing Galphai2 and G-beta-1-gamma-2 by steady-state GTPase activity assay
111 2 2 2 -0.1 NCCc1cnc[nH]1
CHEMBL90 hrh4_human Human Yes 7.9 EC50 = 11.8 nM Funct
Agonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of GTPase by [gamma-32P]GTP spontaneous degradation assayAgonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of GTPase by [gamma-32P]GTP spontaneous degradation assay
111 2 2 2 -0.1 NCCc1cnc[nH]1
CHEMBL594731 hrh4_human Human No 7.9 EC50 = 11.8 nM Funct
Agonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of GTPase by [gamma-32P]GTP spontaneous degradation assayAgonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of GTPase by [gamma-32P]GTP spontaneous degradation assay
312 4 2 6 1.7 Cc1ccccc1CNc1cc(N2CCN(C)CC2)nc(N)n1
CHEMBL3805392 hrh4_human Human No 7.0 EC50 = 110 nM Funct
Agonist activity at human histamine H4 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 H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assay
368 6 3 4 3.2 N#C/N=C(/NCCSc1ccccc1)N[C@H]1CC[C@@H](c2c[nH]cn2)CC1
CHEMBL3805437 hrh4_human Human No 6.0 EC50 = 1100 nM Funct
Agonist activity at human histamine H4 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 H4 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
CHEMBL3806206 hrh4_human Human No 7.0 EC50 = 111 nM Funct
Agonist activity at human histamine H4 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 H4 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
CHEMBL3393536 hrh4_human Human No 7.0 EC50 = 112 nM Funct
Agonist activity at human recombinant histamine H4 receptor expressed in SK-N-MC cells assessed as effect on forskolin-stimulated cAMP-mediated reporter gene activityAgonist activity at human recombinant histamine H4 receptor expressed in SK-N-MC cells assessed as effect on forskolin-stimulated cAMP-mediated reporter gene activity
235 3 1 5 1.0 CC(C)Nc1nccc(N2CCN(C)CC2)n1
CHEMBL493099 hrh4_rat Rat No 6.0 EC50 = 1122.0 nM Funct
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
251 4 1 5 1.4 CN(C)CCN(C)c1cc(C(C)(C)C)nc(N)n1
CHEMBL268229 hrh4_human Human Yes 6.0 EC50 = 1122.0 nM Bind
Inhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H4 receptorInhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H4 receptor
125 2 2 2 0.3 C[C@H](Cc1cnc[nH]1)N
CHEMBL494648 hrh4_rat Rat No 6.9 EC50 = 114.8 nM Funct
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
299 3 1 6 1.5 COc1ccc(-c2cc(N3CCN(C)CC3)nc(N)n2)cc1
CHEMBL501882 hrh4_rat Rat Yes 6.9 EC50 = 114.8 nM Funct
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
193 1 1 5 -0.2 CN1CCN(c2ccnc(N)n2)CC1
CHEMBL449157 hrh4_human Human No 4.9 EC50 = 11481.5 nM Funct
Agonist activity at human histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at human histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
277 2 0 5 1.6 CN1CCN(c2cc(C(C)(C)C)nc(N(C)C)n2)CC1
CHEMBL1632410 hrh4_human Human No 4.9 EC50 = 11481.5 nM Funct
Inhibition of the forskolin-stimulated cAMP production in SK-N-MC cells expressing human Histamine H4 receptorInhibition of the forskolin-stimulated cAMP production in SK-N-MC cells expressing human Histamine H4 receptor
258 5 1 3 2.8 c1ccc(COC[C@H]2CC[C@@H](c3c[nH]cn3)O2)cc1
CHEMBL502104 hrh4_rat Rat No 6.9 EC50 = 117.5 nM Funct
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
284 3 2 6 1.6 CN1CCN(CC1)C2=NC(=NC(=C2)NC3=CC=CC=C3)N
CHEMBL3806206 hrh4_human Human No 6.9 EC50 = 119 nM Funct
Agonist activity at human histamine H4 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 H4 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
CHEMBL1082296 hrh4_mouse Mouse No 5.9 EC50 = 1197 nM Bind
Displacement of [3H]histamine from mouse recombinant histamine H4 receptorDisplacement of [3H]histamine from mouse recombinant histamine H4 receptor
422 6 2 4 4.4 Cc1cc(OCCCN2C[C@H]3CCCN[C@H]3C2)ccc1-c1nc2c(C)c(F)ccc2[nH]1
CHEMBL1770998 hrh4_human Human No 7.9 EC50 = 12 nM Funct
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells assessed as effect on forskolin-induced cAMP accumulation after 6 hrsAgonist activity at human histamine H4 receptor expressed in human SK-N-MC cells assessed as effect on forskolin-induced cAMP accumulation after 6 hrs
250 3 2 6 0.6 CC(C)Nc1cc(N2CCN(C)CC2)nc(N)n1
CHEMBL1086105 hrh4_mouse Mouse No 7.9 EC50 = 12 nM Bind
Displacement of [3H]histamine from mouse recombinant histamine H4 receptorDisplacement of [3H]histamine from mouse recombinant histamine H4 receptor
419 6 2 4 4.5 Cc1cc(OCCCN2CCc3nc[nH]c3C2)ccc1-c1nc2c(C)c(F)ccc2[nH]1
CHEMBL90 hrh4_human Human Yes 7.9 EC50 = 12.0 nM Bind
Agonist activity at human H4 receptor expressed in insect Sf9 cells co-expressing RGS19 fusion protein and Gialpha2, Gbeta1gamma2 assessed as gamma[32P]GTP binding by liquid scintillation countingAgonist activity at human H4 receptor expressed in insect Sf9 cells co-expressing RGS19 fusion protein and Gialpha2, Gbeta1gamma2 assessed as gamma[32P]GTP binding by liquid scintillation counting
111 2 2 2 -0.1 NCCc1cnc[nH]1
CHEMBL90 hrh4_human Human Yes 7.9 EC50 = 12.0 nM Funct
Agonist activity at human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19 protein by steady-state GTPase assayAgonist activity at human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19 protein by steady-state GTPase assay
111 2 2 2 -0.1 NCCc1cnc[nH]1
CHEMBL90 hrh4_human Human Yes 7.9 EC50 = 12.0 nM Bind
Agonist activity at human recombinant histamine H4 receptor-RGS19 fusion protein expressed in Sf9 cells coexpressing Galphai2,Gbeta1gamma2 preincubated for 2 mins before [gamma32P]GTP addition measured after 20 mins by steady-state GTPase activity assayAgonist activity at human recombinant histamine H4 receptor-RGS19 fusion protein expressed in Sf9 cells coexpressing Galphai2,Gbeta1gamma2 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
CHEMBL129198 hrh4_human Human Yes 7.9 EC50 = 12.6 nM Bind
Agonist activity at histamine H4 receptor (unknown origin) assessed as increase in beta-arrestin recruitmentAgonist activity at histamine H4 receptor (unknown origin) assessed as increase in beta-arrestin recruitment
277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl
CHEMBL492677 hrh4_human Human No 7.9 EC50 = 12.6 nM Funct
Agonist activity at histamine H4 receptor (unknown origin) expressed in HEK293T cells harboring CRE-luciferase after 6 hrs by luciferase reporter gene assayAgonist activity at histamine H4 receptor (unknown origin) expressed in HEK293T cells harboring CRE-luciferase after 6 hrs by luciferase reporter gene assay
298 4 2 6 1.4 CN1CCN(CC1)C2=NC(=NC(=C2)NCC3=CC=CC=C3)N
CHEMBL19439 hrh4_human Human Yes 7.9 EC50 = 12.6 nM Funct
Agonist activity at human histamine H4 receptorAgonist activity at human histamine H4 receptor
170 3 3 3 0.6 NC(=N)SCCc1cnc[nH]1
CHEMBL19439 hrh4_human Human Yes 7.9 EC50 = 12.6 nM Funct
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H4 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
CHEMBL19010 hrh4_human Human Yes 7.9 EC50 = 12.6 nM Funct
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H4 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
CHEMBL281576 hrh4_human Human Yes 7.9 EC50 = 12.6 nM Funct
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H4 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
CHEMBL90 hrh4_human Human Yes 7.9 EC50 = 12.6 nM Funct
Agonist activity at human recombinant histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2 by steady-state GTPase activity assayAgonist activity at human recombinant histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2 by steady-state GTPase activity assay
111 2 2 2 -0.1 NCCc1cnc[nH]1
CHEMBL4454158 hrh4_mouse Mouse No 7.9 EC50 = 12.6 nM Bind
Agonist activity at mouse recombinant H4R expressed in HEK293T cells by beta-arrestin recruitment assayAgonist activity at mouse recombinant H4R expressed in HEK293T cells by beta-arrestin recruitment assay
286 3 2 5 2.2 CC(C)(C)CNc1nccc(N2CCc3nc[nH]c3C2)n1
CHEMBL4597218 hrh4_mouse Mouse No 7.9 EC50 = 12.6 nM Bind
Agonist activity at mouse recombinant H4R expressed in HEK293T cells by beta-arrestin recruitment assayAgonist activity at mouse recombinant H4R expressed in HEK293T cells by beta-arrestin recruitment assay
286 3 2 5 2.2 CC(C)(C)CNc1nccc(N2CCc3nc[nH]c3C2)n1
CHEMBL260374 hrh4_human Human Yes 6.9 EC50 = 120.2 nM Funct
Agonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1
CHEMBL1078346 hrh4_human Human No 6.9 EC50 = 120.2 nM Funct
Agonist activity at human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19 protein by steady-state GTPase assayAgonist activity at human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19 protein by steady-state GTPase assay
262 7 3 3 1.4 CC(C)CN/C(=N\C#N)NCCCCc1c[nH]cn1
CHEMBL492489 hrh4_human Human No 5.9 EC50 = 1202.3 nM Funct
Agonist activity at human histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at human histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
264 2 0 5 1.5 COc1nc(N2CCN(C)CC2)cc(C(C)(C)C)n1
CHEMBL1077737 hrh4_human Human No 5.9 EC50 = 1202.3 nM Funct
Agonist activity at human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19 protein by steady-state GTPase assayAgonist activity at human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19 protein by steady-state GTPase assay
325 9 3 4 1.8 N#C/N=C(/NCCCCc1c[nH]cn1)NCCCc1cccnc1
CHEMBL495083 hrh4_rat Rat No 5.9 EC50 = 1202.3 nM Funct
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
294 2 1 6 1.3 CN1CCN(c2cc(-c3ccccc3C#N)nc(N)n2)CC1
CHEMBL494678 hrh4_mouse Mouse No 6.9 EC50 = 123.0 nM Funct
Agonist activity at mouse histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at mouse histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
294 2 1 6 1.3 CN1CCN(c2cc(-c3ccc(C#N)cc3)nc(N)n2)CC1
CHEMBL494678 hrh4_mouse Mouse No 6.9 EC50 = 123.0 nM Funct
Antagonist activity at mouse histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assayAntagonist activity at mouse histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assay
294 2 1 6 1.3 CN1CCN(c2cc(-c3ccc(C#N)cc3)nc(N)n2)CC1
CHEMBL493663 hrh4_rat Rat No 4.9 EC50 = 12302.7 nM Funct
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
277 2 2 6 -0.7 CN1CCN(c2cc(N3CCNC3=O)nc(N)n2)CC1
CHEMBL3806098 hrh4_human Human No 6.9 EC50 = 125 nM Funct
Agonist activity at human histamine H4 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 H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assay
350 7 3 3 2.9 N#C/N=C(/NCCCc1ccccc1)NC[C@H]1CC[C@H](c2c[nH]cn2)C1
CHEMBL1688969 hrh4_human Human No 6.9 EC50 = 125.9 nM Funct
Agonist activity at histamine H4 receptor (unknown origin) expressed in HEK293T cells harboring CRE-luciferase after 6 hrs by luciferase reporter gene assayAgonist activity at histamine H4 receptor (unknown origin) expressed in HEK293T cells harboring CRE-luciferase after 6 hrs by luciferase reporter gene assay
259 5 1 4 2.4 C1CCC(CC1)CC2=CN(N=N2)CCC3=CN=CN3
CHEMBL320331 hrh4_human Human No 6.9 EC50 = 125.9 nM Funct
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H4 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
CHEMBL308913 hrh4_human Human No 5.9 EC50 = 1258.9 nM Funct
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
302 8 3 2 2.4 S=C(NCCCCc1c[nH]cn1)NCCc1ccccc1
CHEMBL78497 hrh4_human Human Yes 5.9 EC50 = 1258.9 nM Bind
Inhibition of the cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H4 receptorInhibition of the cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H4 receptor
187 4 1 2 2.0 c1cncc(CCCc2c[nH]cn2)c1
CHEMBL11919 hrh4_human Human Yes 4.9 EC50 = 12589.3 nM Funct
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H4 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
CHEMBL1632410 hrh4_human Human No 4.9 EC50 = 12589.3 nM Funct
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H4 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 hrh4_human Human No 4.9 EC50 = 12589.3 nM Funct
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H4 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
CHEMBL1078529 hrh4_human Human No 5.9 EC50 = 1288.3 nM Funct
Agonist activity at human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19 protein by steady-state GTPase assayAgonist activity at human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19 protein by steady-state GTPase assay
328 8 3 4 2.2 N#C/N=C(/NCCCc1c[nH]cn1)NCCSc1ccccc1
CHEMBL322256 hrh4_human Human No 4.9 EC50 = 12882.5 nM Funct
Inhibition of the forskolin-stimulated cAMP production in SK-N-MC cells expressing human Histamine H4 receptorInhibition of the forskolin-stimulated cAMP production in SK-N-MC cells expressing human Histamine H4 receptor
258 5 1 3 2.8 c1ccc(COC[C@@H]2CC[C@@H](c3c[nH]cn3)O2)cc1
CHEMBL3806079 hrh4_human Human No 6.9 EC50 = 129 nM Funct
Agonist activity at human histamine H4 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 H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assay
368 7 3 4 3.1 N#C/N=C(/NCCSc1ccccc1)NC[C@@H]1CC[C@H](c2c[nH]cn2)C1
CHEMBL90 hrh4_human Human Yes 7.9 EC50 = 13 nM Bind
Agonist activity at human SF-His6-tagged histamine H4 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated response incubated for 5 hrs by luciferase reporter gene assayAgonist activity at human SF-His6-tagged histamine H4 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated response incubated for 5 hrs by luciferase reporter gene assay
111 2 2 2 -0.1 NCCc1cnc[nH]1
CHEMBL90 hrh4_human Human Yes 7.9 EC50 = 13.8 nM Funct
Agonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of [35S]GTPgammaS binding
111 2 2 2 -0.1 NCCc1cnc[nH]1
CHEMBL3236558 hrh4_human Human Yes 5.9 EC50 = 1300 nM Bind
Agonist activity at human H4 receptorAgonist activity at human H4 receptor
233 2 2 5 0.9 Nc1nc(C2CCCC2)cc(N2CC(N)C2)n1
CHEMBL4455324 hrh4_mouse Mouse No 6.9 EC50 = 134.9 nM Bind
Agonist activity at mouse H4R expressed in HEK293T-beta-arr2-mH4R cells by beta-arrestin2 recruitment assayAgonist activity at mouse H4R expressed in HEK293T-beta-arr2-mH4R cells by beta-arrestin2 recruitment assay
249 3 2 5 1.5 CC(C)(C)CNc1nccc(N2CC[C@@H](N)C2)n1
CHEMBL4596881 hrh4_mouse Mouse No 6.9 EC50 = 134.9 nM Bind
Agonist activity at mouse H4R expressed in HEK293T-beta-arr2-mH4R cells by beta-arrestin2 recruitment assayAgonist activity at mouse H4R expressed in HEK293T-beta-arr2-mH4R cells by beta-arrestin2 recruitment assay
249 3 2 5 1.5 CC(C)(C)CNc1nccc(N2CC[C@@H](N)C2)n1
CHEMBL320331 hrh4_human Human No 6.9 EC50 = 134.9 nM Funct
Inhibition of the forskolin-stimulated cAMP production in SK-N-MC cells expressing human Histamine H4 receptorInhibition of the forskolin-stimulated cAMP production in SK-N-MC cells expressing human Histamine H4 receptor
258 5 1 3 2.8 c1ccc(COC[C@@H]2CC[C@H](c3c[nH]cn3)O2)cc1
CHEMBL492869 hrh4_rat Rat No 5.9 EC50 = 1349.0 nM Funct
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
291 2 1 7 -0.4 CN1CCN(c2cc(N3CCN(C)CC3)nc(N)n2)CC1
CHEMBL4543119 hrh4_human Human No 6.9 EC50 = 138.0 nM Bind
Agonist activity at human H4R expressed in HEK293T-beta-arr2-hH4R cells by beta-arrestin2 recruitment assayAgonist activity at human H4R expressed in HEK293T-beta-arr2-hH4R cells by beta-arrestin2 recruitment assay
277 3 1 5 2.1 CN1CCCN(c2ccnc(NCC(C)(C)C)n2)CC1
CHEMBL4596606 hrh4_human Human No 6.9 EC50 = 138.0 nM Bind
Agonist activity at human H4R expressed in HEK293T-beta-arr2-hH4R cells by beta-arrestin2 recruitment assayAgonist activity at human H4R expressed in HEK293T-beta-arr2-hH4R cells by beta-arrestin2 recruitment assay
277 3 1 5 2.1 CN1CCCN(c2ccnc(NCC(C)(C)C)n2)CC1
CHEMBL1094144 hrh4_human Human No 5.9 EC50 = 1380.4 nM Bind
Activity at human recombinant GAIP-fused histamine H4 receptor expressed in Sf9 cells coexpressing Galphai, Gbeta1gamma2 by steady-state GTPase activity assayActivity at human recombinant GAIP-fused histamine H4 receptor expressed in Sf9 cells coexpressing Galphai, Gbeta1gamma2 by steady-state GTPase activity assay
365 7 4 5 3.2 Cc1nc(N)sc1CCCNC(=N)NC(=O)C[C@H](C)C1CCCCC1
CHEMBL3805361 hrh4_human Human No 7.9 EC50 = 14 nM Funct
Agonist activity at human histamine H4 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 H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assay
368 7 3 4 3.1 N#C/N=C(/NCCSc1ccccc1)NC[C@H]1CC[C@H](c2c[nH]cn2)C1
CHEMBL4455324 hrh4_human Human No 7.8 EC50 = 14.5 nM Bind
Agonist activity at human H4R expressed in HEK293T-beta-arr2-hH4R cells by beta-arrestin2 recruitment assayAgonist activity at human H4R expressed in HEK293T-beta-arr2-hH4R cells by beta-arrestin2 recruitment assay
249 3 2 5 1.5 CC(C)(C)CNc1nccc(N2CC[C@@H](N)C2)n1
CHEMBL4596881 hrh4_human Human No 7.8 EC50 = 14.5 nM Bind
Agonist activity at human H4R expressed in HEK293T-beta-arr2-hH4R cells by beta-arrestin2 recruitment assayAgonist activity at human H4R expressed in HEK293T-beta-arr2-hH4R cells by beta-arrestin2 recruitment assay
249 3 2 5 1.5 CC(C)(C)CNc1nccc(N2CC[C@@H](N)C2)n1
CHEMBL209758 hrh4_human Human No 7.8 EC50 = 14.8 nM Funct
Activity at human histamine H4 receptor transfected in SK-N-MC cells by cAMP assayActivity at human histamine H4 receptor transfected in SK-N-MC cells by cAMP assay
345 0 0 4 3.9 CN1CCN(C2=Nc3cc(Cl)ccc3Oc3c(F)cccc32)CC1
CHEMBL211170 hrh4_human Human No 7.8 EC50 = 14.8 nM Funct
Activity at human histamine H4 receptor transfected in SK-N-MC cells by cAMP assayActivity at human histamine H4 receptor transfected in SK-N-MC cells by cAMP assay
361 0 0 4 4.4 CN1CCN(C2=Nc3ccc(Cl)cc3Oc3c(Cl)cccc32)CC1
CHEMBL509540 hrh4_rat Rat Yes 7.8 EC50 = 14.8 nM Funct
Antagonist activity at rat histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assayAntagonist activity at rat histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assay
295 1 2 5 1.6 C1CC2=CC=CC=C2C3=C(C1)C(=NC(=N3)N)N4CCNCC4
CHEMBL1077860 hrh4_human Human No 6.9 EC50 = 141.3 nM Funct
Agonist activity at human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19 protein by steady-state GTPase assayAgonist activity at human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19 protein by steady-state GTPase assay
338 9 3 3 2.9 CC(CCN/C(=N\C#N)NCCCCc1c[nH]cn1)c1ccccc1
CHEMBL493664 hrh4_rat Rat No 4.9 EC50 = 14125.4 nM Funct
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
286 2 1 7 -0.0 CN1CCN(c2cc(-n3ccccc3=O)nc(N)n2)CC1
CHEMBL4445423 hrh4_rat Rat No 6.8 EC50 = 144.5 nM Bind
Agonist activity at rat H4R expressed in HEK293T-beta-arr2-rH4R cells by beta-arrestin2 recruitment assayAgonist activity at rat H4R expressed in HEK293T-beta-arr2-rH4R cells by beta-arrestin2 recruitment assay
291 4 4 5 1.0 CC(C)(C)CNc1nccc(N2CC[C@@H](NC(=N)N)C2)n1
CHEMBL4598198 hrh4_rat Rat No 6.8 EC50 = 144.5 nM Bind
Agonist activity at rat H4R expressed in HEK293T-beta-arr2-rH4R cells by beta-arrestin2 recruitment assayAgonist activity at rat H4R expressed in HEK293T-beta-arr2-rH4R cells by beta-arrestin2 recruitment assay
291 4 4 5 1.0 CC(C)(C)CNc1nccc(N2CC[C@@H](NC(=N)N)C2)n1
CHEMBL494909 hrh4_rat Rat Yes 5.8 EC50 = 1479.1 nM Funct
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
209 1 2 6 -0.5 CN1CCN(c2cc(O)nc(N)n2)CC1
CHEMBL3806255 hrh4_human Human No 7.8 EC50 = 15 nM Funct
Agonist activity at human histamine H4 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 H4 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
CHEMBL3393539 hrh4_human Human No 7.8 EC50 = 15 nM Funct
Agonist activity at human recombinant histamine H4 receptor expressed in SK-N-MC cells assessed as effect on forskolin-stimulated cAMP-mediated reporter gene activityAgonist activity at human recombinant histamine H4 receptor expressed in SK-N-MC cells assessed as effect on forskolin-stimulated cAMP-mediated reporter gene activity
249 5 2 5 1.3 CN[C@@H]1CCN(c2ccnc(NCC(C)C)n2)C1
CHEMBL483406 hrh4_human Human No 7.8 EC50 = 15.1 nM Bind
Agonist activity at human H4 receptor expressed in insect Sf9 cells co-expressing RGS19 fusion protein and Gialpha2, Gbeta1gamma2 assessed as gamma[32P]GTP binding by liquid scintillation countingAgonist activity at human H4 receptor expressed in insect Sf9 cells co-expressing RGS19 fusion protein and Gialpha2, Gbeta1gamma2 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
CHEMBL483406 hrh4_human Human No 7.8 EC50 = 15.1 nM Bind
Agonist activity at human recombinant histamine H4 receptor-RGS19 fusion protein expressed in Sf9 cells coexpressing Galphai2,Gbeta1gamma2 preincubated for 2 mins before [gamma32P]GTP addition measured after 20 mins by steady-state GTPase activity assayAgonist activity at human recombinant histamine H4 receptor-RGS19 fusion protein expressed in Sf9 cells coexpressing Galphai2,Gbeta1gamma2 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
CHEMBL483406 hrh4_human Human No 7.8 EC50 = 15.3 nM Bind
Activity at human recombinant histamine H4 receptor-RGS4 fusion protein expressed in Sf9 cells coexpressing Galphai2 and G-beta-1-gamma-2 by steady-state GTPase activity assayActivity at human recombinant histamine H4 receptor-RGS4 fusion protein expressed in Sf9 cells coexpressing Galphai2 and G-beta-1-gamma-2 by steady-state GTPase activity assay
313 7 3 2 2.0 CC(CC(=O)/N=C(\N)NCCCc1c[nH]cn1)c1ccccc1
CHEMBL492242 hrh4_rat Rat No 7.8 EC50 = 15.5 nM Funct
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
306 2 1 6 1.2 CN1CCN(c2cc(-c3ccc(F)nc3F)nc(N)n2)CC1
CHEMBL494093 hrh4_rat Rat No 7.8 EC50 = 15.5 nM Funct
Antagonist activity at rat histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assayAntagonist activity at rat histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assay
295 1 1 5 1.6 CN1CCN(c2nc(N)nc3c2CCc2ccccc2-3)CC1
CHEMBL563342 hrh4_human Human No 7.8 EC50 = 15.9 nM Bind
Agonist activity at histamine H4 receptor (unknown origin) expressed in human U2OS cells increase in beta-arrestin2 recruitment after 2 hrs by luminescence assayAgonist activity at histamine H4 receptor (unknown origin) expressed in human U2OS cells increase in beta-arrestin2 recruitment after 2 hrs by luminescence assay
308 6 2 3 3.2 C1=CC=C(C(=C1)CN=C(N)SCCCC2=CN=CN2)Cl
CHEMBL18661 hrh4_human Human Yes 7.8 EC50 = 15.9 nM Funct
Agonist activity at human histamine H4 receptorAgonist activity at human histamine H4 receptor
165 2 2 2 1.0 N1CCC(CC1)Cc1[nH]cnc1
CHEMBL18661 hrh4_human Human Yes 7.8 EC50 = 15.9 nM Funct
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H4 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
CHEMBL470790 hrh4_human Human No 7.8 EC50 = 15.9 nM Funct
Agonist activity at human recombinant histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2 by steady-state GTPase activity assayAgonist activity at human recombinant histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2 by steady-state GTPase activity assay
299 7 4 3 1.6 N=C(NCCCc1c[nH]cn1)NC(=O)CCc1ccccc1
CHEMBL483406 hrh4_human Human No 7.8 EC50 = 15.9 nM Funct
Agonist activity at human recombinant histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2 by steady-state GTPase activity assayAgonist activity at human recombinant histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2 by steady-state GTPase activity assay
313 7 3 2 2.0 CC(CC(=O)/N=C(\N)NCCCc1c[nH]cn1)c1ccccc1
CHEMBL129198 hrh4_human Human Yes 7.8 EC50 = 15.9 nM Funct
Inverse agonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of [35S]GTPgammaS bindingInverse agonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of [35S]GTPgammaS binding
277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl
CHEMBL3805995 hrh4_human Human No 6.8 EC50 = 150 nM Funct
Agonist activity at human histamine H4 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 H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assay
165 2 2 2 1.3 NC[C@@H]1CC[C@H](c2c[nH]cn2)C1
CHEMBL1083084 hrh4_human Human No 6.8 EC50 = 150 nM Funct
Agonist activity at human histamine H4 receptor in SK-N-MC cells assessed as forskolin-stimulated cAMP release preincubated for 10 mins before forskolin challengeAgonist activity at human histamine H4 receptor in SK-N-MC cells assessed as forskolin-stimulated cAMP release preincubated for 10 mins before forskolin challenge
410 7 1 4 4.4 Cc1cc(OCCCN2CCC(N(C)C)C2)ccc1-c1nc2c(C)c(F)ccc2[nH]1
CHEMBL474617 hrh4_human Human No 6.8 EC50 = 151.4 nM Bind
Agonist activity at human H4 receptor expressed in insect Sf9 cells co-expressing RGS19 fusion protein and Gialpha2, Gbeta1gamma2 assessed as gamma[32P]GTP binding by liquid scintillation countingAgonist activity at human H4 receptor expressed in insect Sf9 cells co-expressing RGS19 fusion protein and Gialpha2, Gbeta1gamma2 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
CHEMBL1078631 hrh4_human Human No 6.8 EC50 = 151.4 nM Funct
Agonist activity at human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19 protein by steady-state GTPase assayAgonist activity at human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19 protein by steady-state GTPase assay
324 9 3 3 2.4 N#C/N=C(/NCCCCc1c[nH]cn1)NCCCc1ccccc1
CHEMBL311473 hrh4_human Human Yes 5.8 EC50 = 1513.6 nM Bind
Inhibition of the cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H4 receptorInhibition of the cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H4 receptor
173 3 1 2 1.6 c1cc(CCc2c[nH]cn2)ccn1
CHEMBL78838 hrh4_human Human Yes 4.8 EC50 = 15135.6 nM Bind
Inhibition of the cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H4 receptorInhibition of the cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H4 receptor
159 2 1 2 1.4 c1cncc(Cc2c[nH]cn2)c1
CHEMBL309654 hrh4_human Human Yes 5.8 EC50 = 1548.8 nM Bind
Inhibition of the cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H4 receptorInhibition of the cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H4 receptor
187 4 1 2 2.0 c1cc(CCCc2c[nH]cn2)ccn1
CHEMBL1688969 hrh4_human Human No 6.8 EC50 = 158.5 nM Funct
Agonist activity at human histamine H4 receptor expressed in HEK293 cells assessed by forskolin induced cAMP response element activation by luciferase reporter gene assayAgonist activity at human histamine H4 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
CHEMBL4439142 hrh4_rat Rat No 6.8 EC50 = 158.5 nM Funct
Agonist activity at rat H4R expressed in in HEK293T cells by CRE-luciferase reporter gene assayAgonist activity at rat H4R expressed in in HEK293T cells by CRE-luciferase reporter gene assay
277 4 1 5 2.1 CN(C)[C@@H]1CCN(c2ccnc(NCC(C)(C)C)n2)C1
CHEMBL4515149 hrh4_rat Rat No 6.8 EC50 = 158.5 nM Funct
Agonist activity at rat H4R expressed in in HEK293T cells by CRE-luciferase reporter gene assayAgonist activity at rat H4R expressed in in HEK293T cells by CRE-luciferase reporter gene assay
277 4 1 5 2.1 CN(C)[C@@H]1CCN(c2ccnc(NCC(C)(C)C)n2)C1
CHEMBL4595327 hrh4_rat Rat No 6.8 EC50 = 158.5 nM Funct
Agonist activity at rat H4R expressed in in HEK293T cells by CRE-luciferase reporter gene assayAgonist activity at rat H4R expressed in in HEK293T cells by CRE-luciferase reporter gene assay
277 4 1 5 2.1 CN(C)[C@@H]1CCN(c2ccnc(NCC(C)(C)C)n2)C1
CHEMBL90 hrh4_rat Rat Yes 6.8 EC50 = 158.5 nM Funct
Agonist activity at rat histamine H4 receptor by luciferase reporter gene assayAgonist activity at rat histamine H4 receptor by luciferase reporter gene assay
111 2 2 2 -0.1 NCCc1cnc[nH]1
CHEMBL12344 hrh4_human Human Yes 5.8 EC50 = 1584.9 nM Funct
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
161 4 2 3 0.6 CN(CCCSC(=N)N)C
CHEMBL24665 hrh4_human Human Yes 5.8 EC50 = 1584.9 nM Funct
Agonist activity at human recombinant histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2 by steady-state GTPase activity assayAgonist activity at human recombinant histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2 by steady-state GTPase activity assay
255 3 2 2 2.6 NCCc1c[nH]c(-c2cccc(C(F)(F)F)c2)n1
CHEMBL275443 hrh4_mouse Mouse Yes 5.8 EC50 = 1584.9 nM Funct
Agonist activity at mouse histamine H4 receptorAgonist activity at mouse histamine H4 receptor
125 2 2 2 0.2 Cc1c(CCN)nc[nH]1
CHEMBL1770987 hrh4_human Human No 7.8 EC50 = 16 nM Funct
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells assessed as effect on forskolin-induced cAMP accumulation after 6 hrsAgonist activity at human histamine H4 receptor expressed in human SK-N-MC cells assessed as effect on forskolin-induced cAMP accumulation after 6 hrs
276 3 2 6 1.2 CN1CCN(c2cc(N)nc(NC3CCCC3)n2)CC1
CHEMBL494667 hrh4_human Human No 7.8 EC50 = 16.2 nM Funct
Agonist activity at human histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at human histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
259 2 2 6 0.2 CN1CCN(c2cc(-c3c[nH]cn3)nc(N)n2)CC1
CHEMBL4454158 hrh4_rat Rat No 7.8 EC50 = 16.6 nM Bind
Agonist activity at rat H4R expressed in HEK293T-beta-arr2-rH4R cells by beta-arrestin2 recruitment assayAgonist activity at rat H4R expressed in HEK293T-beta-arr2-rH4R cells by beta-arrestin2 recruitment assay
286 3 2 5 2.2 CC(C)(C)CNc1nccc(N2CCc3nc[nH]c3C2)n1
CHEMBL4597218 hrh4_rat Rat No 7.8 EC50 = 16.6 nM Bind
Agonist activity at rat H4R expressed in HEK293T-beta-arr2-rH4R cells by beta-arrestin2 recruitment assayAgonist activity at rat H4R expressed in HEK293T-beta-arr2-rH4R cells by beta-arrestin2 recruitment assay
286 3 2 5 2.2 CC(C)(C)CNc1nccc(N2CCc3nc[nH]c3C2)n1
CHEMBL90 hrh4_human Human Yes 7.8 EC50 = 17.0 nM Funct
Agonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
111 2 2 2 -0.1 NCCc1cnc[nH]1
CHEMBL3805361 hrh4_mouse Mouse No 6.8 EC50 = 166 nM Bind
Agonist activity at mouse SF-His6-tagged histamine H4 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated response incubated for 5 hrs by luciferase reporter gene assayAgonist activity at mouse SF-His6-tagged histamine H4 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated response incubated for 5 hrs by luciferase reporter gene assay
368 7 3 4 3.1 N#C/N=C(/NCCSc1ccccc1)NC[C@H]1CC[C@H](c2c[nH]cn2)C1
CHEMBL1077861 hrh4_human Human Yes 6.8 EC50 = 169.8 nM Funct
Agonist activity at human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19 protein by steady-state GTPase assayAgonist activity at human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19 protein by steady-state GTPase assay
206 5 3 3 0.1 N#C/N=C(\N)NCCCCc1c[nH]cn1
CHEMBL454007 hrh4_rat Rat Yes 4.8 EC50 = 16982.4 nM Funct
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
227 1 1 5 0.5 CN1CCN(c2cc(Cl)nc(N)n2)CC1
CHEMBL503605 hrh4_mouse Mouse Yes 7.8 EC50 = 17.8 nM Funct
Antagonist activity at mouse histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assayAntagonist activity at mouse histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assay
263 1 2 2 1.9 O=C(c1cc2cc(Cl)ccc2[nH]1)N1CCNCC1
CHEMBL3805813 hrh4_human Human No 5.8 EC50 = 1710 nM Funct
Agonist activity at human histamine H4 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 H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assay
165 2 2 2 1.3 NC[C@H]1CC[C@H](c2c[nH]cn2)C1
CHEMBL522841 hrh4_rat Rat No 6.8 EC50 = 173.8 nM Funct
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
319 2 1 5 2.6 CN1CCN(c2cc(-c3ccc4ccccc4c3)nc(N)n2)CC1
CHEMBL495280 hrh4_human Human No 6.8 EC50 = 177.8 nM Funct
Agonist activity at human histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at human histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
309 2 1 7 1.2 CN1CCN(c2cc(-n3cnc4ccccc43)nc(N)n2)CC1
CHEMBL494723 hrh4_rat Rat No 6.8 EC50 = 177.8 nM Funct
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
283 2 1 5 1.8 Cc1ccccc1-c1cc(N2CCN(C)CC2)nc(N)n1
CHEMBL499631 hrh4_rat Rat Yes 5.8 EC50 = 1778.3 nM Funct
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
237 4 2 5 1.3 CN(C)CCNc1cc(C(C)(C)C)nc(N)n1
CHEMBL4518374 hrh4_human Human No 7.7 EC50 = 18.2 nM Funct
Agonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
263 3 2 5 1.7 CC(C)(C)CNc1nccc(N2CCCNCC2)n1
CHEMBL4596491 hrh4_human Human No 7.7 EC50 = 18.2 nM Funct
Agonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
263 3 2 5 1.7 CC(C)(C)CNc1nccc(N2CCCNCC2)n1
CHEMBL509540 hrh4_mouse Mouse Yes 7.7 EC50 = 18.2 nM Funct
Antagonist activity at mouse histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assayAntagonist activity at mouse histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assay
295 1 2 5 1.6 C1CC2=CC=CC=C2C3=C(C1)C(=NC(=N3)N)N4CCNCC4
CHEMBL4439142 hrh4_human Human No 7.7 EC50 = 18.6 nM Bind
Agonist activity at human H4R expressed in HEK293T-beta-arr2-hH4R cells by beta-arrestin2 recruitment assayAgonist activity at human H4R expressed in HEK293T-beta-arr2-hH4R cells by beta-arrestin2 recruitment assay
277 4 1 5 2.1 CN(C)[C@@H]1CCN(c2ccnc(NCC(C)(C)C)n2)C1
CHEMBL4515149 hrh4_human Human No 7.7 EC50 = 18.6 nM Bind
Agonist activity at human H4R expressed in HEK293T-beta-arr2-hH4R cells by beta-arrestin2 recruitment assayAgonist activity at human H4R expressed in HEK293T-beta-arr2-hH4R cells by beta-arrestin2 recruitment assay
277 4 1 5 2.1 CN(C)[C@@H]1CCN(c2ccnc(NCC(C)(C)C)n2)C1
CHEMBL4595327 hrh4_human Human No 7.7 EC50 = 18.6 nM Bind
Agonist activity at human H4R expressed in HEK293T-beta-arr2-hH4R cells by beta-arrestin2 recruitment assayAgonist activity at human H4R expressed in HEK293T-beta-arr2-hH4R cells by beta-arrestin2 recruitment assay
277 4 1 5 2.1 CN(C)[C@@H]1CCN(c2ccnc(NCC(C)(C)C)n2)C1
CHEMBL90 hrh4_human Human Yes 5.8 EC50 = 1800 nM Funct
Agonist activity at human H4 receptor expressed in 293-EBNA cells by luciferase reporter gene assayAgonist activity at human H4 receptor expressed in 293-EBNA cells by luciferase reporter gene assay
111 2 2 2 -0.1 NCCc1cnc[nH]1
CHEMBL445091 hrh4_rat Rat Yes 5.7 EC50 = 1819.7 nM Funct
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
259 2 2 6 0.2 CN1CCN(c2cc(-c3cn[nH]c3)nc(N)n2)CC1
CHEMBL449157 hrh4_rat Rat No 4.7 EC50 = 18197.0 nM Funct
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
277 2 0 5 1.6 CN1CCN(c2cc(C(C)(C)C)nc(N(C)C)n2)CC1
CHEMBL493461 hrh4_rat Rat No 5.7 EC50 = 1862.1 nM Funct
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
293 2 1 5 2.0 CN1CCN(c2cc(N)nc(-c3ccc(C#N)cc3)c2)CC1
CHEMBL474447 hrh4_human Human No 7.7 EC50 = 19.1 nM Bind
Agonist activity at human H4 receptor expressed in insect Sf9 cells co-expressing RGS19 fusion protein and Gialpha2, Gbeta1gamma2 assessed as gamma[32P]GTP binding by liquid scintillation countingAgonist activity at human H4 receptor expressed in insect Sf9 cells co-expressing RGS19 fusion protein and Gialpha2, Gbeta1gamma2 assessed as gamma[32P]GTP binding by liquid scintillation counting
324 6 4 2 1.5 N/C(=N\C(=O)Cc1c[nH]c2ccccc12)NCCCc1c[nH]cn1
CHEMBL446269 hrh4_rat Rat No 7.7 EC50 = 19.1 nM Funct
Antagonist activity at rat histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assayAntagonist activity at rat histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assay
281 2 2 5 1.4 CN[C@@H]1CCN(c2nc(N)nc3c2Cc2ccccc2-3)C1
CHEMBL4543119 hrh4_human Human No 7.7 EC50 = 19.5 nM Funct
Agonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
277 3 1 5 2.1 CN1CCCN(c2ccnc(NCC(C)(C)C)n2)CC1
CHEMBL4596606 hrh4_human Human No 7.7 EC50 = 19.5 nM Funct
Agonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
277 3 1 5 2.1 CN1CCCN(c2ccnc(NCC(C)(C)C)n2)CC1
CHEMBL594721 hrh4_human Human No 7.7 EC50 = 19.5 nM Funct
Agonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of GTPase by [gamma-32P]GTP spontaneous degradation assayAgonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of GTPase by [gamma-32P]GTP spontaneous degradation assay
332 4 2 6 2.1 CN1CCN(c2cc(NCc3ccccc3Cl)nc(N)n2)CC1
CHEMBL213912 hrh4_human Human Yes 7.7 EC50 = 20.0 nM Funct
Activity at human histamine H4 receptor transfected in SK-N-MC cells by cAMP assayActivity at human histamine H4 receptor transfected in SK-N-MC cells by cAMP assay
327 0 0 4 3.8 CN1CCN(CC1)C2=NC3=C(C=C(C=C3)Cl)OC4=CC=CC=C42
CHEMBL90 hrh4_human Human Yes 7.7 EC50 = 20.0 nM Funct
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
111 2 2 2 -0.1 NCCc1cnc[nH]1
CHEMBL12160 hrh4_human Human Yes 7.7 EC50 = 20.0 nM Funct
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
212 5 3 2 1.2 C/N=C(\S)NCCCCc1c[nH]cn1
CHEMBL1632409 hrh4_human Human No 7.7 EC50 = 20.0 nM Funct
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H4 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
CHEMBL306077 hrh4_human Human Yes 7.7 EC50 = 20.0 nM Funct
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
240 6 3 2 2.0 CC(C)/N=C(\S)NCCCCc1c[nH]cn1
CHEMBL521995 hrh4_rat Rat No 7.7 EC50 = 20.0 nM Funct
Antagonist activity at rat histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assayAntagonist activity at rat histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assay
267 1 2 5 1.0 Nc1nc2c(c(N3CCNCC3)n1)Cc1ccccc1-2
CHEMBL4437371 hrh4_rat Rat No 6.7 EC50 = 190.6 nM Bind
Agonist activity at rat H4R expressed in HEK293T-beta-arr2-rH4R cells by beta-arrestin2 recruitment assayAgonist activity at rat H4R expressed in HEK293T-beta-arr2-rH4R cells by beta-arrestin2 recruitment assay
237 6 3 5 1.7 CC(C)(C)CNc1nccc(NCCCN)n1
CHEMBL4594753 hrh4_rat Rat No 6.7 EC50 = 190.6 nM Bind
Agonist activity at rat H4R expressed in HEK293T-beta-arr2-rH4R cells by beta-arrestin2 recruitment assayAgonist activity at rat H4R expressed in HEK293T-beta-arr2-rH4R cells by beta-arrestin2 recruitment assay
237 6 3 5 1.7 CC(C)(C)CNc1nccc(NCCCN)n1
CHEMBL522679 hrh4_rat Rat No 6.7 EC50 = 195.0 nM Funct
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
329 4 1 7 1.5 COc1cccc(OC)c1-c1cc(N2CCN(C)CC2)nc(N)n1
CHEMBL106158 hrh4_human Human No 6.7 EC50 = 199.5 nM Funct
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H4 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
CHEMBL4634086 hrh4_human Human Yes 6.7 EC50 = 199.5 nM Funct
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H4 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 hrh4_human Human Yes 6.7 EC50 = 199.5 nM Funct
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
125 3 2 2 0.3 NCCCc1c[nH]cn1
CHEMBL4439142 hrh4_mouse Mouse No 6.7 EC50 = 199.5 nM Funct
Agonist activity at mouse H4R expressed in HEK293T cells by CRE-luciferase reporter gene assayAgonist activity at mouse H4R expressed in HEK293T cells by CRE-luciferase reporter gene assay
277 4 1 5 2.1 CN(C)[C@@H]1CCN(c2ccnc(NCC(C)(C)C)n2)C1
CHEMBL4515149 hrh4_mouse Mouse No 6.7 EC50 = 199.5 nM Funct
Agonist activity at mouse H4R expressed in HEK293T cells by CRE-luciferase reporter gene assayAgonist activity at mouse H4R expressed in HEK293T cells by CRE-luciferase reporter gene assay
277 4 1 5 2.1 CN(C)[C@@H]1CCN(c2ccnc(NCC(C)(C)C)n2)C1
CHEMBL4595327 hrh4_mouse Mouse No 6.7 EC50 = 199.5 nM Funct
Agonist activity at mouse H4R expressed in HEK293T cells by CRE-luciferase reporter gene assayAgonist activity at mouse H4R expressed in HEK293T cells by CRE-luciferase reporter gene assay
277 4 1 5 2.1 CN(C)[C@@H]1CCN(c2ccnc(NCC(C)(C)C)n2)C1
CHEMBL1632412 hrh4_mouse Mouse No 6.7 EC50 = 199.5 nM Funct
Agonist activity at mouse histamine H4 receptor by luciferase reporter gene assayAgonist activity at mouse histamine H4 receptor by luciferase reporter gene assay
271 2 2 3 3.0 Cc1ccc2[nH]c(/C(=N\O)C3CCN(C)CC3)cc2c1
CHEMBL1632414 hrh4_rat Rat No 6.7 EC50 = 199.5 nM Funct
Agonist activity at rat histamine H4 receptor by luciferase reporter gene assayAgonist activity at rat histamine H4 receptor by luciferase reporter gene assay
292 2 2 4 2.7 CN1CCC(/C(=N/O)c2nc3cc(Cl)ccc3[nH]2)CC1
CHEMBL595639 hrh4_human Human No 6.7 EC50 = 199.5 nM Funct
Inverse agonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of [35S]GTPgammaS bindingInverse agonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of [35S]GTPgammaS binding
332 4 2 6 2.1 CN1CCN(c2cc(NCc3cccc(Cl)c3)nc(N)n2)CC1
CHEMBL106612 hrh4_human Human No 5.7 EC50 = 1995.3 nM Funct
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H4 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
CHEMBL106612 hrh4_human Human No 5.7 EC50 = 1995.3 nM Funct
Inhibition of the forskolin-stimulated cAMP production in SK-N-MC cells expressing human Histamine H4 receptorInhibition of the forskolin-stimulated cAMP production in SK-N-MC cells expressing human Histamine H4 receptor
167 2 2 3 0.6 NC[C@H]1CC[C@H](c2c[nH]cn2)O1
CHEMBL106570 hrh4_human Human No 4.7 EC50 = 19952.6 nM Funct
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H4 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
CHEMBL129198 hrh4_mouse Mouse Yes 8.6 EC50 = 2.4 nM Funct
Antagonist activity at mouse histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assayAntagonist activity at mouse histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assay
277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl
CHEMBL465170 hrh4_human Human No 8.6 EC50 = 2.6 nM Bind
Agonist activity at human H4 receptor expressed in insect Sf9 cells co-expressing RGS19 fusion protein and Gialpha2, Gbeta1gamma2 assessed as gamma[32P]GTP binding by liquid scintillation countingAgonist activity at human H4 receptor expressed in insect Sf9 cells co-expressing RGS19 fusion protein and Gialpha2, Gbeta1gamma2 assessed as gamma[32P]GTP binding by liquid scintillation counting
237 6 3 2 0.6 CCCC(=O)/N=C(\N)NCCCc1c[nH]cn1
CHEMBL129198 hrh4_rat Rat Yes 8.6 EC50 = 2.6 nM Funct
Antagonist activity at rat histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assayAntagonist activity at rat histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assay
277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl
CHEMBL1096429 hrh4_human Human No 8.6 EC50 = 2.6 nM Bind
Activity at human recombinant GAIP-fused histamine H4 receptor expressed in Sf9 cells coexpressing Galphai, Gbeta1gamma2 by steady-state GTPase activity assayActivity at human recombinant GAIP-fused histamine H4 receptor expressed in Sf9 cells coexpressing Galphai, Gbeta1gamma2 by steady-state GTPase activity assay
313 7 4 3 2.2 C[C@@H](CC(=O)NC(=N)NCCCc1c[nH]cn1)c1ccccc1
CHEMBL3393546 hrh4_human Human No 7.7 EC50 = 20 nM Funct
Agonist activity at human recombinant histamine H4 receptor expressed in SK-N-MC cells assessed as effect on forskolin-stimulated cAMP-mediated reporter gene activityAgonist activity at human recombinant histamine H4 receptor expressed in SK-N-MC cells assessed as effect on forskolin-stimulated cAMP-mediated reporter gene activity
287 3 1 5 1.8 CN1CCN(c2ccnc(NC3CC4CCC3C4)n2)CC1
CHEMBL209628 hrh4_human Human No 7.7 EC50 = 20.4 nM Funct
Activity at human histamine H4 receptor transfected in SK-N-MC cells by cAMP assayActivity at human histamine H4 receptor transfected in SK-N-MC cells by cAMP assay
345 0 0 4 3.9 CN1CCN(C2=Nc3ccc(Cl)cc3Oc3c(F)cccc32)CC1
CHEMBL90 hrh4_human Human Yes 7.7 EC50 = 20.4 nM Funct
Agonist activity at human recombinant histamine H4 receptor-RGS19 fusion protein expressed in Sf9 cells coexpressing Galphai2,Gbeta1gamma2 assessed as [35S]GTPgammaS binding after 90 mins by liquid scintillation countingAgonist activity at human recombinant histamine H4 receptor-RGS19 fusion protein expressed in Sf9 cells coexpressing Galphai2,Gbeta1gamma2 assessed as [35S]GTPgammaS binding after 90 mins by liquid scintillation counting
111 2 2 2 -0.1 NCCc1cnc[nH]1
CHEMBL593103 hrh4_human Human No 7.7 EC50 = 20.9 nM Funct
Agonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of [35S]GTPgammaS binding
316 4 2 6 1.6 CN1CCN(c2cc(NCc3ccc(F)cc3)nc(N)n2)CC1
CHEMBL90 hrh4_human Human Yes 7.7 EC50 = 20.9 nM Funct
Inhibition of the forskolin-stimulated cAMP production in SK-N-MC cells expressing human Histamine H4 receptorInhibition of the forskolin-stimulated cAMP production in SK-N-MC cells expressing human Histamine H4 receptor
111 2 2 2 -0.1 NCCc1cnc[nH]1
CHEMBL3805003 hrh4_human Human No 6.7 EC50 = 202 nM Funct
Agonist activity at human histamine H4 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 H4 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
CHEMBL492864 hrh4_rat Rat Yes 5.7 EC50 = 2041.7 nM Funct
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
319 1 1 5 0.4 CN1CCN(c2cc(I)nc(N)n2)CC1
CHEMBL153207 hrh4_human Human Yes 5.7 EC50 = 2041.7 nM Bind
Inhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H4 receptorInhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H4 receptor
179 3 2 2 1.3 c1nc(CCC2CCCNC2)c[nH]1
CHEMBL3804906 hrh4_human Human No 6.7 EC50 = 206 nM Funct
Agonist activity at human histamine H4 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 H4 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
CHEMBL492227 hrh4_rat Rat No 6.7 EC50 = 208.9 nM Funct
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
270 2 1 6 0.9 CN1CCN(c2cc(-c3cccnc3)nc(N)n2)CC1
CHEMBL492677 hrh4_human Human No 7.7 EC50 = 21.4 nM Funct
Agonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of [35S]GTPgammaS binding
298 4 2 6 1.4 CN1CCN(CC1)C2=NC(=NC(=C2)NCC3=CC=CC=C3)N
CHEMBL4634086 hrh4_human Human Yes 6.7 EC50 = 213.8 nM Bind
Inhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H4 receptorInhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H4 receptor
125 3 2 2 0.3 NCCCc1c[nH]cn1
CHEMBL91353 hrh4_human Human Yes 6.7 EC50 = 213.8 nM Bind
Inhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H4 receptorInhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H4 receptor
125 3 2 2 0.3 NCCCc1c[nH]cn1
CHEMBL106570 hrh4_human Human No 4.7 EC50 = 21379.6 nM Funct
Inhibition of the forskolin-stimulated cAMP production in SK-N-MC cells expressing human Histamine H4 receptorInhibition of the forskolin-stimulated cAMP production in SK-N-MC cells expressing human Histamine H4 receptor
248 3 3 4 0.3 C/N=C(\NC#N)NC[C@@H]1CC[C@@H](c2c[nH]cn2)O1
CHEMBL831 hrh4_human Human Yes 6.7 EC50 = 218.8 nM Funct
Activity at human histamine H4 receptor transfected in SK-N-MC cells by cAMP assayActivity at human histamine H4 receptor transfected in SK-N-MC cells by cAMP assay
327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2
CHEMBL473662 hrh4_rat Rat Yes 6.7 EC50 = 218.8 nM Funct
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
208 1 2 6 -0.6 CN1CCN(c2cc(N)nc(N)n2)CC1
CHEMBL493229 hrh4_rat Rat No 6.7 EC50 = 218.8 nM Funct
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
273 2 1 7 0.2 CN1CCN(c2cc(-c3cnn(C)c3)nc(N)n2)CC1
CHEMBL14690 hrh4_human Human Yes 7.7 EC50 = 22.4 nM Funct
Agonist activity at human H4R by [35S]-GTPgammaS-binding assayAgonist activity at human H4R by [35S]-GTPgammaS-binding assay
308 6 2 3 3.2 Clc1ccc(cc1)CN=C(SCCCc1cnc[nH]1)N
CHEMBL1096428 hrh4_human Human No 7.6 EC50 = 22.9 nM Bind
Activity at human recombinant GAIP-fused histamine H4 receptor expressed in Sf9 cells coexpressing Galphai, Gbeta1gamma2 by steady-state GTPase activity assayActivity at human recombinant GAIP-fused histamine H4 receptor expressed in Sf9 cells coexpressing Galphai, Gbeta1gamma2 by steady-state GTPase activity assay
313 7 4 3 2.2 C[C@H](CC(=O)NC(=N)NCCCc1c[nH]cn1)c1ccccc1
CHEMBL4437371 hrh4_rat Rat No 7.6 EC50 = 22.9 nM Funct
Agonist activity at rat H4R expressed in HEK293-SF-rH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at rat H4R expressed in HEK293-SF-rH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
237 6 3 5 1.7 CC(C)(C)CNc1nccc(NCCCN)n1
CHEMBL4594753 hrh4_rat Rat No 7.6 EC50 = 22.9 nM Funct
Agonist activity at rat H4R expressed in HEK293-SF-rH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at rat H4R expressed in HEK293-SF-rH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
237 6 3 5 1.7 CC(C)(C)CNc1nccc(NCCCN)n1
CHEMBL106158 hrh4_human Human No 6.7 EC50 = 223.9 nM Funct
Inhibition of the forskolin-stimulated cAMP production in SK-N-MC cells expressing human Histamine H4 receptorInhibition of the forskolin-stimulated cAMP production in SK-N-MC cells expressing human Histamine H4 receptor
248 3 3 4 0.3 C/N=C(\NC#N)NC[C@@H]1CC[C@H](c2c[nH]cn2)O1
CHEMBL4445423 hrh4_mouse Mouse No 6.6 EC50 = 229.1 nM Bind
Agonist activity at mouse H4R expressed in HEK293T-beta-arr2-mH4R cells by beta-arrestin2 recruitment assayAgonist activity at mouse H4R expressed in HEK293T-beta-arr2-mH4R cells by beta-arrestin2 recruitment assay
291 4 4 5 1.0 CC(C)(C)CNc1nccc(N2CC[C@@H](NC(=N)N)C2)n1
CHEMBL4598198 hrh4_mouse Mouse No 6.6 EC50 = 229.1 nM Bind
Agonist activity at mouse H4R expressed in HEK293T-beta-arr2-mH4R cells by beta-arrestin2 recruitment assayAgonist activity at mouse H4R expressed in HEK293T-beta-arr2-mH4R cells by beta-arrestin2 recruitment assay
291 4 4 5 1.0 CC(C)(C)CNc1nccc(N2CC[C@@H](NC(=N)N)C2)n1
CHEMBL492241 hrh4_rat Rat Yes 6.6 EC50 = 229.1 nM Funct
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
270 2 1 6 0.9 CN1CCN(c2cc(-c3ccncc3)nc(N)n2)CC1
CHEMBL523335 hrh4_rat Rat No 5.6 EC50 = 2290.9 nM Funct
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
285 2 1 5 2.0 CC(C)(C)c1cc(N2CCNCC2)nc(-n2cccc2)n1
CHEMBL447151 hrh4_rat Rat No 4.6 EC50 = 22908.7 nM Funct
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
250 1 1 5 1.2 CN1CCN(c2cc(C(C)(C)C)nc(O)n2)CC1
CHEMBL493281 hrh4_rat Rat No 7.6 EC50 = 24.0 nM Funct
Antagonist activity at rat histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assayAntagonist activity at rat histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assay
281 1 2 5 1.2 Nc1nc2c(c(N3CCNCC3)n1)CCc1ccccc1-2
CHEMBL3804837 hrh4_human Human No 6.6 EC50 = 230 nM Funct
Agonist activity at human histamine H4 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 H4 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
CHEMBL495082 hrh4_rat Rat Yes 6.6 EC50 = 234.4 nM Funct
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
294 2 1 6 1.3 CN1CCN(c2cc(-c3cccc(C#N)c3)nc(N)n2)CC1
CHEMBL522019 hrh4_rat Rat No 6.6 EC50 = 234.4 nM Funct
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
300 3 1 7 0.9 COc1ccncc1-c1cc(N2CCN(C)CC2)nc(N)n1
CHEMBL493262 hrh4_human Human No 5.6 EC50 = 2344.2 nM Funct
Agonist activity at human histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at human histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
293 2 1 5 2.0 CN1CCN(c2cc(-c3ccc(C#N)cc3)cc(N)n2)CC1
CHEMBL90 hrh4_mouse Mouse Yes 5.6 EC50 = 2344.2 nM Bind
Agonist activity at mouse H4R expressed in HEK293 cells co-expressing ELucC/ELucN-beta-arrestin2 assessed as induction of beta-arrestin recruitment by luciferase reporter gene assayAgonist activity at mouse H4R expressed in HEK293 cells co-expressing ELucC/ELucN-beta-arrestin2 assessed as induction of beta-arrestin recruitment by luciferase reporter gene assay
111 2 2 2 -0.1 NCCc1cnc[nH]1
CHEMBL90 hrh4_mouse Mouse Yes 5.6 EC50 = 2344.2 nM Bind
Agonist activity at mouse H4R expressed in HEK293T-beta-arr2-mH4R cells by beta-arrestin2 recruitment assayAgonist activity at mouse H4R expressed in HEK293T-beta-arr2-mH4R cells by beta-arrestin2 recruitment assay
111 2 2 2 -0.1 NCCc1cnc[nH]1
CHEMBL494687 hrh4_rat Rat Yes 4.6 EC50 = 23442.3 nM Funct
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
248 1 1 4 2.6 CC1CCN(c2cc(C(C)(C)C)nc(N)n2)CC1
CHEMBL449021 hrh4_rat Rat No 5.6 EC50 = 2398.8 nM Funct
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
306 4 1 6 1.0 CN(C)CCN1CCN(c2cc(C(C)(C)C)nc(N)n2)CC1
CHEMBL109130 hrh4_human Human Yes 4.6 EC50 = 23988.3 nM Funct
Inhibition of the forskolin-stimulated cAMP production in SK-N-MC cells expressing human Histamine H4 receptorInhibition of the forskolin-stimulated cAMP production in SK-N-MC cells expressing human Histamine H4 receptor
165 2 2 3 0.4 NC[C@H]1C=C[C@H](c2c[nH]cn2)O1
CHEMBL3806146 hrh4_human Human No 6.6 EC50 = 245 nM Funct
Agonist activity at human histamine H4 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 H4 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
CHEMBL3220642 hrh4_human Human No 6.6 EC50 = 245.5 nM Funct
Agonist activity at human recombinant histamine H4 receptor-RGS19 fusion protein expressed in Sf9 cells coexpressing Galphai2,Gbeta1gamma2 assessed as [35S]GTPgammaS binding after 90 mins by liquid scintillation countingAgonist activity at human recombinant histamine H4 receptor-RGS19 fusion protein expressed in Sf9 cells coexpressing Galphai2,Gbeta1gamma2 assessed as [35S]GTPgammaS binding after 90 mins by liquid scintillation counting
356 9 3 4 2.8 Cc1[nH]cnc1CCCCN/C(=N\C#N)NCCSc1ccccc1
CHEMBL494890 hrh4_rat Rat Yes 6.6 EC50 = 245.5 nM Funct
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
280 2 2 6 1.0 N#Cc1ccc(-c2cc(N3CCNCC3)nc(N)n2)cc1
CHEMBL506187 hrh4_rat Rat No 6.6 EC50 = 245.5 nM Funct
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
263 2 1 5 1.5 CCN1CCN(c2cc(C(C)(C)C)nc(N)n2)CC1
CHEMBL494890 hrh4_rat Rat Yes 6.6 EC50 = 245.5 nM Funct
Antagonist activity at rat histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assayAntagonist activity at rat histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assay
280 2 2 6 1.0 N#Cc1ccc(-c2cc(N3CCNCC3)nc(N)n2)cc1
CHEMBL3805361 hrh4_human Human No 7.6 EC50 = 25 nM Bind
Agonist activity at human SF-His6-tagged histamine H4 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated response incubated for 5 hrs by luciferase reporter gene assayAgonist activity at human SF-His6-tagged histamine H4 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated response incubated for 5 hrs by luciferase reporter gene assay
368 7 3 4 3.1 N#C/N=C(/NCCSc1ccccc1)NC[C@H]1CC[C@H](c2c[nH]cn2)C1
CHEMBL3354815 hrh4_human Human No 7.6 EC50 = 25 nM Funct
Agonist activity at human recombinant histamine H4 receptor expressed in SK-N-MC cells assessed as effect on forskolin-stimulated cAMP-mediated reporter gene activityAgonist activity at human recombinant histamine H4 receptor expressed in SK-N-MC cells assessed as effect on forskolin-stimulated cAMP-mediated reporter gene activity
235 4 2 5 1.1 CN[C@@H]1CCN(c2ccnc(NC(C)C)n2)C1
CHEMBL260549 hrh4_human Human Yes 7.6 EC50 = 25.1 nM Bind
Agonist activity at histamine H4 receptor (unknown origin) expressed in human U2OS cells increase in beta-arrestin2 recruitment after 2 hrs by luminescence assayAgonist activity at histamine H4 receptor (unknown origin) expressed in human U2OS cells increase in beta-arrestin2 recruitment after 2 hrs by luminescence assay
312 1 1 4 2.0 CN1CCN(CC1)C2=NC3=CC(=C(C=C3NC2=O)Cl)Cl
CHEMBL129198 hrh4_human Human Yes 7.6 EC50 = 25.1 nM Bind
Agonist activity at human H4R expressed in human U2OS cells assessed as recruitment of beta-arrestin after 2 hrs by PathHunter beta-galactosidase enzyme fragment complementation assayAgonist activity at human H4R expressed in human U2OS cells assessed as recruitment of beta-arrestin after 2 hrs by PathHunter beta-galactosidase enzyme fragment complementation assay
277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl
CHEMBL90 hrh4_human Human Yes 7.6 EC50 = 25.1 nM Funct
Agonist activity at human histamine H4 receptor expressed in HEK293 cells assessed by forskolin induced cAMP response element activation by luciferase reporter gene assayAgonist activity at human histamine H4 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
CHEMBL12608 hrh4_human Human Yes 7.6 EC50 = 25.1 nM Funct
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
321 9 4 4 1.2 NC(=NCCCc1cnc[nH]1)NCCSCc1nc[nH]c1C
CHEMBL4443126 hrh4_mouse Mouse No 7.6 EC50 = 25.7 nM Bind
Agonist activity at mouse H4R expressed in HEK293T-beta-arr2-mH4R cells by beta-arrestin2 recruitment assayAgonist activity at mouse H4R expressed in HEK293T-beta-arr2-mH4R cells by beta-arrestin2 recruitment assay
263 4 2 5 1.7 CN[C@@H]1CCN(c2ccnc(NCC(C)(C)C)n2)C1
CHEMBL4596409 hrh4_mouse Mouse No 7.6 EC50 = 25.7 nM Bind
Agonist activity at mouse H4R expressed in HEK293T-beta-arr2-mH4R cells by beta-arrestin2 recruitment assayAgonist activity at mouse H4R expressed in HEK293T-beta-arr2-mH4R cells by beta-arrestin2 recruitment assay
263 4 2 5 1.7 CN[C@@H]1CCN(c2ccnc(NCC(C)(C)C)n2)C1
CHEMBL4439142 hrh4_rat Rat No 7.6 EC50 = 25.7 nM Bind
Agonist activity at rat H4R expressed in HEK293T-beta-arr2-rH4R cells by beta-arrestin2 recruitment assayAgonist activity at rat H4R expressed in HEK293T-beta-arr2-rH4R cells by beta-arrestin2 recruitment assay
277 4 1 5 2.1 CN(C)[C@@H]1CCN(c2ccnc(NCC(C)(C)C)n2)C1
CHEMBL4515149 hrh4_rat Rat No 7.6 EC50 = 25.7 nM Bind
Agonist activity at rat H4R expressed in HEK293T-beta-arr2-rH4R cells by beta-arrestin2 recruitment assayAgonist activity at rat H4R expressed in HEK293T-beta-arr2-rH4R cells by beta-arrestin2 recruitment assay
277 4 1 5 2.1 CN(C)[C@@H]1CCN(c2ccnc(NCC(C)(C)C)n2)C1
CHEMBL4595327 hrh4_rat Rat No 7.6 EC50 = 25.7 nM Bind
Agonist activity at rat H4R expressed in HEK293T-beta-arr2-rH4R cells by beta-arrestin2 recruitment assayAgonist activity at rat H4R expressed in HEK293T-beta-arr2-rH4R cells by beta-arrestin2 recruitment assay
277 4 1 5 2.1 CN(C)[C@@H]1CCN(c2ccnc(NCC(C)(C)C)n2)C1
CHEMBL494679 hrh4_rat Rat Yes 6.6 EC50 = 251.2 nM Funct
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
250 1 1 6 0.5 CN1CCN(c2nc(N)nc(C(C)(C)C)n2)CC1
CHEMBL448085 hrh4_human Human Yes 5.6 EC50 = 2511.9 nM Funct
Agonist activity at human histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at human histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
259 2 1 7 -0.0 CN1CCN(c2cc(-n3ccnc3)nc(N)n2)CC1
CHEMBL275443 hrh4_rat Rat Yes 5.6 EC50 = 2511.9 nM Funct
Agonist activity at rat histamine H4 receptorAgonist activity at rat histamine H4 receptor
125 2 2 2 0.2 Cc1c(CCN)nc[nH]1
CHEMBL1077859 hrh4_human Human No 5.6 EC50 = 2570.4 nM Funct
Agonist activity at human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19 protein by steady-state GTPase assayAgonist activity at human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19 protein by steady-state GTPase assay
325 9 3 4 1.8 N#C/N=C(/NCCCCc1c[nH]cn1)NCCCc1ccncc1
CHEMBL507063 hrh4_human Human Yes 7.6 EC50 = 26.9 nM Funct
Agonist activity at human histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at human histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
300 3 1 7 0.9 COc1ncccc1-c1cc(N2CCN(C)CC2)nc(N)n1
CHEMBL3806162 hrh4_human Human No 5.6 EC50 = 2675 nM Funct
Agonist activity at human histamine H4 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 H4 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
CHEMBL594949 hrh4_human Human No 6.6 EC50 = 269.2 nM Funct
Inverse agonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of [35S]GTPgammaS bindingInverse agonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of [35S]GTPgammaS binding
312 4 2 6 1.7 Cc1cccc(CNc2cc(N3CCN(C)CC3)nc(N)n2)c1
CHEMBL492288 hrh4_rat Rat No 6.6 EC50 = 275.4 nM Funct
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
395 2 1 5 2.1 CN1CCN(c2cc(-c3ccc(I)cc3)nc(N)n2)CC1
CHEMBL7828 hrh4_human Human No 7.6 EC50 = 28.2 nM Funct
Activity at human histamine H4 receptor transfected in SK-N-MC cells by cAMP assayActivity at human histamine H4 receptor transfected in SK-N-MC cells by cAMP assay
327 0 0 4 3.8 CN1CCN(C2=Nc3cc(Cl)ccc3Oc3ccccc32)CC1
CHEMBL474449 hrh4_human Human No 7.6 EC50 = 28.2 nM Bind
Agonist activity at human H4 receptor expressed in insect Sf9 cells co-expressing RGS19 fusion protein and Gialpha2, Gbeta1gamma2 assessed as gamma[32P]GTP binding by liquid scintillation countingAgonist activity at human H4 receptor expressed in insect Sf9 cells co-expressing RGS19 fusion protein and Gialpha2, Gbeta1gamma2 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
CHEMBL260374 hrh4_mouse Mouse Yes 7.6 EC50 = 28.2 nM Bind
Antagonist activity at mouse H4R expressed in HEK293 cells co-expressing ELucC/ELucN-beta-arrestin2 assessed as inhibition of histamine-induced beta-arrestin recruitment preincubated for 15 mins followed by histamine addition by luciferase reporter gene assayAntagonist activity at mouse H4R expressed in HEK293 cells co-expressing ELucC/ELucN-beta-arrestin2 assessed as inhibition of histamine-induced beta-arrestin recruitment preincubated for 15 mins followed by histamine addition by luciferase reporter gene assay
292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1
CHEMBL3220629 hrh4_human Human No 5.5 EC50 = 2884.0 nM Bind
Agonist activity at human recombinant histamine H4 receptor-RGS19 fusion protein expressed in Sf9 cells coexpressing Galphai2,Gbeta1gamma2 preincubated for 2 mins before [gamma32P]GTP addition measured after 20 mins by steady-state GTPase activity assayAgonist activity at human recombinant histamine H4 receptor-RGS19 fusion protein expressed in Sf9 cells coexpressing Galphai2,Gbeta1gamma2 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)NCCCc1ncc[nH]1)c1ccccc1
CHEMBL4437371 hrh4_human Human No 7.5 EC50 = 29.5 nM Funct
Agonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
237 6 3 5 1.7 CC(C)(C)CNc1nccc(NCCCN)n1
CHEMBL4594753 hrh4_human Human No 7.5 EC50 = 29.5 nM Funct
Agonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
237 6 3 5 1.7 CC(C)(C)CNc1nccc(NCCCN)n1
CHEMBL4443126 hrh4_rat Rat No 7.5 EC50 = 29.5 nM Bind
Agonist activity at rat H4R expressed in HEK293T-beta-arr2-rH4R cells by beta-arrestin2 recruitment assayAgonist activity at rat H4R expressed in HEK293T-beta-arr2-rH4R cells by beta-arrestin2 recruitment assay
263 4 2 5 1.7 CN[C@@H]1CCN(c2ccnc(NCC(C)(C)C)n2)C1
CHEMBL4596409 hrh4_rat Rat No 7.5 EC50 = 29.5 nM Bind
Agonist activity at rat H4R expressed in HEK293T-beta-arr2-rH4R cells by beta-arrestin2 recruitment assayAgonist activity at rat H4R expressed in HEK293T-beta-arr2-rH4R cells by beta-arrestin2 recruitment assay
263 4 2 5 1.7 CN[C@@H]1CCN(c2ccnc(NCC(C)(C)C)n2)C1
CHEMBL3806079 hrh4_human Human No 6.5 EC50 = 293 nM Funct
Agonist activity at human histamine H4 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 H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assay
368 7 3 4 3.1 N#C/N=C(/NCCSc1ccccc1)NC[C@@H]1CC[C@H](c2c[nH]cn2)C1
CHEMBL90 hrh4_rat Rat Yes 6.5 EC50 = 295.1 nM Funct
Agonist activity at rat H4R expressed in HEK293-SF-rH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at rat H4R expressed in HEK293-SF-rH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
111 2 2 2 -0.1 NCCc1cnc[nH]1
CHEMBL494093 hrh4_human Human No 6.5 EC50 = 295.1 nM Funct
Antagonist activity at human histamine 4 receptor expressed in Sf9 cell membranes co-expressing Galphai2 and Gbeta1gamma2 assessed as [35S]GTPgammaS binding by scintillation countingAntagonist activity at human histamine 4 receptor expressed in Sf9 cell membranes co-expressing Galphai2 and Gbeta1gamma2 assessed as [35S]GTPgammaS binding by scintillation counting
295 1 1 5 1.6 CN1CCN(c2nc(N)nc3c2CCc2ccccc2-3)CC1
CHEMBL475621 hrh4_human Human No 8.5 EC50 = 3.0 nM Bind
Agonist activity at human H4 receptor expressed in insect Sf9 cells co-expressing RGS19 fusion protein and Gialpha2, Gbeta1gamma2 assessed as gamma[32P]GTP binding by liquid scintillation countingAgonist activity at human H4 receptor expressed in insect Sf9 cells co-expressing RGS19 fusion protein and Gialpha2, Gbeta1gamma2 assessed as gamma[32P]GTP binding by liquid scintillation counting
223 5 3 2 0.2 CCC(=O)/N=C(\N)NCCCc1c[nH]cn1
CHEMBL4441731 hrh4_human Human Yes 8.5 EC50 = 3.2 nM Funct
Agonist activity at human H4R expressed on HEK293T cells assessed as inhibition 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 H4R expressed on HEK293T cells assessed as inhibition 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 hrh4_human Human Yes 8.5 EC50 = 3.2 nM Funct
Agonist activity at human H4R expressed on HEK293T cells assessed as inhibition 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 H4R expressed on HEK293T cells assessed as inhibition 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
CHEMBL1084355 hrh4_human Human No 8.5 EC50 = 3.3 nM Funct
Agonist activity at human histamine H4 receptor in SK-N-MC cells assessed as forskolin-stimulated cAMP release preincubated for 10 mins before forskolin challengeAgonist activity at human histamine H4 receptor in SK-N-MC cells assessed as forskolin-stimulated cAMP release preincubated for 10 mins before forskolin challenge
404 8 2 4 4.9 Cc1cc(OCCCNCc2cccnc2)ccc1-c1nc2c(C)c(F)ccc2[nH]1
CHEMBL1086105 hrh4_human Human No 8.5 EC50 = 3.3 nM Funct
Agonist activity at human histamine H4 receptor in SK-N-MC cells assessed as forskolin-stimulated cAMP release preincubated for 10 mins before forskolin challengeAgonist activity at human histamine H4 receptor in SK-N-MC cells assessed as forskolin-stimulated cAMP release preincubated for 10 mins before forskolin challenge
419 6 2 4 4.5 Cc1cc(OCCCN2CCc3nc[nH]c3C2)ccc1-c1nc2c(C)c(F)ccc2[nH]1
CHEMBL4455324 hrh4_human Human No 8.5 EC50 = 3.5 nM Funct
Agonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
249 3 2 5 1.5 CC(C)(C)CNc1nccc(N2CC[C@@H](N)C2)n1
CHEMBL4596881 hrh4_human Human No 8.5 EC50 = 3.5 nM Funct
Agonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
249 3 2 5 1.5 CC(C)(C)CNc1nccc(N2CC[C@@H](N)C2)n1
CHEMBL471724 hrh4_human Human No 8.4 EC50 = 3.7 nM Bind
Agonist activity at human H4 receptor expressed in insect Sf9 cells co-expressing RGS19 fusion protein and Gialpha2, Gbeta1gamma2 assessed as gamma[32P]GTP binding by liquid scintillation countingAgonist activity at human H4 receptor expressed in insect Sf9 cells co-expressing RGS19 fusion protein and Gialpha2, Gbeta1gamma2 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
CHEMBL503605 hrh4_rat Rat Yes 7.5 EC50 = 30.9 nM Funct
Antagonist activity at rat histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assayAntagonist activity at rat histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assay
263 1 2 2 1.9 O=C(c1cc2cc(Cl)ccc2[nH]1)N1CCNCC1
CHEMBL485802 hrh4_rat Rat No 5.5 EC50 = 3020.0 nM Funct
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
236 2 1 6 -0.1 CN1CCN(c2cc(N(C)C)nc(N)n2)CC1
CHEMBL339414 hrh4_human Human Yes 6.5 EC50 = 302 nM Funct
Activity at human histamine H4 receptor transfected in SK-N-MC cells by cAMP assayActivity at human histamine H4 receptor transfected in SK-N-MC cells by cAMP assay
293 0 0 4 3.1 CN1CCN(C2=Nc3ccccc3Oc3ccccc32)CC1
CHEMBL260374 hrh4_mouse Mouse Yes 6.5 EC50 = 302 nM Funct
Agonist activity at mouse H4R expressed in HEK293-SF-mH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at mouse H4R expressed in HEK293-SF-mH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1
CHEMBL495341 hrh4_rat Rat Yes 6.5 EC50 = 302 nM Funct
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
238 4 1 5 1.3 CN(C)CCOc1cc(C(C)(C)C)nc(N)n1
CHEMBL106931 hrh4_human Human Yes 4.5 EC50 = 30903.0 nM Funct
Inhibition of the forskolin-stimulated cAMP production in SK-N-MC cells expressing human Histamine H4 receptorInhibition of the forskolin-stimulated cAMP production in SK-N-MC cells expressing human Histamine H4 receptor
167 2 2 3 0.6 NC[C@@H]1CC[C@@H](c2c[nH]cn2)O1
CHEMBL594022 hrh4_human Human No 7.5 EC50 = 31.6 nM Funct
Agonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of [35S]GTPgammaS binding
332 4 2 6 2.1 CN1CCN(c2cc(NCc3ccc(Cl)cc3)nc(N)n2)CC1
CHEMBL90019 hrh4_human Human Yes 7.5 EC50 = 31.6 nM Funct
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
139 4 2 2 0.7 NCCCCc1cnc[nH]1
CHEMBL275443 hrh4_human Human Yes 7.5 EC50 = 31.6 nM Funct
Agonist activity at human recombinant histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2 by steady-state GTPase activity assayAgonist activity at human recombinant histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2 by steady-state GTPase activity assay
125 2 2 2 0.2 Cc1c(CCN)nc[nH]1
CHEMBL492287 hrh4_rat Rat No 7.5 EC50 = 31.6 nM Funct
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
303 2 1 5 2.1 CN1CCN(c2cc(-c3cccc(Cl)c3)nc(N)n2)CC1
CHEMBL522661 hrh4_rat Rat No 6.5 EC50 = 316.2 nM Funct
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
327 2 1 5 2.3 CN1CCN(c2cc(C34CC5CC(CC(C5)C3)C4)nc(N)n2)CC1
CHEMBL3393550 hrh4_human Human No 5.5 EC50 = 3160 nM Funct
Agonist activity at human recombinant histamine H4 receptor expressed in SK-N-MC cells assessed as effect on forskolin-stimulated cAMP-mediated reporter gene activityAgonist activity at human recombinant histamine H4 receptor expressed in SK-N-MC cells assessed as effect on forskolin-stimulated cAMP-mediated reporter gene activity
249 5 2 5 1.3 CN[C@@H]1CCN(c2cnnc(NCC(C)C)c2)C1
CHEMBL3354816 hrh4_human Human No 5.5 EC50 = 3162 nM Funct
Agonist activity at human recombinant histamine H4 receptor expressed in SK-N-MC cells assessed as effect on forskolin-stimulated cAMP-mediated reporter gene activityAgonist activity at human recombinant histamine H4 receptor expressed in SK-N-MC cells assessed as effect on forskolin-stimulated cAMP-mediated reporter gene activity
234 4 2 4 1.7 CN[C@@H]1CCN(c2ccnc(NC(C)C)c2)C1
CHEMBL3393547 hrh4_human Human No 5.5 EC50 = 3162 nM Funct
Agonist activity at human recombinant histamine H4 receptor expressed in SK-N-MC cells assessed as effect on forskolin-stimulated cAMP-mediated reporter gene activityAgonist activity at human recombinant histamine H4 receptor expressed in SK-N-MC cells assessed as effect on forskolin-stimulated cAMP-mediated reporter gene activity
287 4 2 5 1.9 CN[C@@H]1CCN(c2ccnc(NC3CC4CCC3C4)n2)C1
CHEMBL79126 hrh4_human Human Yes 5.5 EC50 = 3162.3 nM Bind
Inhibition of the cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H4 receptorInhibition of the cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H4 receptor
187 4 1 2 2.0 c1ccc(CCCc2c[nH]cn2)nc1
CHEMBL106931 hrh4_human Human Yes 4.5 EC50 = 31622.8 nM Funct
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H4 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
CHEMBL523835 hrh4_rat Rat No 5.5 EC50 = 3235.9 nM Funct
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
301 3 1 8 0.3 COc1ncc(-c2cc(N3CCN(C)CC3)nc(N)n2)cn1
CHEMBL82244 hrh4_human Human Yes 4.5 EC50 = 32359.4 nM Bind
Inhibition of the cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H4 receptorInhibition of the cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H4 receptor
173 3 1 2 1.6 c1cncc(CCc2c[nH]cn2)c1
CHEMBL515428 hrh4_human Human No 7.5 EC50 = 33.1 nM Bind
Agonist activity at human H4 receptor expressed in insect Sf9 cells co-expressing RGS19 fusion protein and Gialpha2, Gbeta1gamma2 assessed as gamma[32P]GTP binding by liquid scintillation countingAgonist activity at human H4 receptor expressed in insect Sf9 cells co-expressing RGS19 fusion protein and Gialpha2, Gbeta1gamma2 assessed as gamma[32P]GTP binding by liquid scintillation counting
381 8 5 3 1.1 N/C(=N\C(=O)CCNC(=O)c1cc2ccccc2[nH]1)NCCCc1c[nH]cn1
CHEMBL90 hrh4_human Human Yes 7.5 EC50 = 33.9 nM Bind
Agonist activity at human H4R expressed in HEK293 cells co-expressing ELucC/ELucN-beta-arrestin2 assessed as induction of beta-arrestin recruitment by luciferase reporter gene assayAgonist activity at human H4R expressed in HEK293 cells co-expressing ELucC/ELucN-beta-arrestin2 assessed as induction of beta-arrestin recruitment by luciferase reporter gene assay
111 2 2 2 -0.1 NCCc1cnc[nH]1
CHEMBL90 hrh4_human Human Yes 7.5 EC50 = 33.9 nM Bind
Agonist activity at human H4R expressed in HEK293T-beta-arr2-hH4R cells by beta-arrestin2 recruitment assayAgonist activity at human H4R expressed in HEK293T-beta-arr2-hH4R cells by beta-arrestin2 recruitment assay
111 2 2 2 -0.1 NCCc1cnc[nH]1
CHEMBL493478 hrh4_human Human No 7.5 EC50 = 33.9 nM Funct
Agonist activity at human histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at human histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
208 1 2 6 -0.6 CN1CCN(c2nc(N)ncc2N)CC1
CHEMBL1078642 hrh4_human Human Yes 7.5 EC50 = 33.9 nM Funct
Agonist activity at human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19 protein by steady-state GTPase assayAgonist activity at human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19 protein by steady-state GTPase assay
342 9 3 4 2.5 C1=CC=C(C=C1)SCCNC(=NCCCCC2=CN=CN2)NC#N
CHEMBL4455324 hrh4_rat Rat No 7.5 EC50 = 33.9 nM Bind
Agonist activity at rat H4R expressed in HEK293T-beta-arr2-rH4R cells by beta-arrestin2 recruitment assayAgonist activity at rat H4R expressed in HEK293T-beta-arr2-rH4R cells by beta-arrestin2 recruitment assay
249 3 2 5 1.5 CC(C)(C)CNc1nccc(N2CC[C@@H](N)C2)n1
CHEMBL4596881 hrh4_rat Rat No 7.5 EC50 = 33.9 nM Bind
Agonist activity at rat H4R expressed in HEK293T-beta-arr2-rH4R cells by beta-arrestin2 recruitment assayAgonist activity at rat H4R expressed in HEK293T-beta-arr2-rH4R cells by beta-arrestin2 recruitment assay
249 3 2 5 1.5 CC(C)(C)CNc1nccc(N2CC[C@@H](N)C2)n1
CHEMBL1083085 hrh4_human Human No 6.5 EC50 = 331 nM Funct
Agonist activity at human histamine H4 receptor in SK-N-MC cells assessed as forskolin-stimulated cAMP release preincubated for 10 mins before forskolin challengeAgonist activity at human histamine H4 receptor in SK-N-MC cells assessed as forskolin-stimulated cAMP release preincubated for 10 mins before forskolin challenge
396 6 2 4 4.2 Cc1cc(OCCCN2CCCC(N)C2)ccc1-c1nc2c(C)c(F)ccc2[nH]1
CHEMBL1077636 hrh4_human Human Yes 6.5 EC50 = 331.1 nM Funct
Agonist activity at human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19 protein by steady-state GTPase assayAgonist activity at human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19 protein by steady-state GTPase assay
248 6 3 3 1.2 CC(C)N/C(=N\C#N)NCCCCc1c[nH]cn1
CHEMBL4543119 hrh4_rat Rat No 6.5 EC50 = 331.1 nM Bind
Agonist activity at rat H4R expressed in HEK293T-beta-arr2-rH4R cells by beta-arrestin2 recruitment assayAgonist activity at rat H4R expressed in HEK293T-beta-arr2-rH4R cells by beta-arrestin2 recruitment assay
277 3 1 5 2.1 CN1CCCN(c2ccnc(NCC(C)(C)C)n2)CC1
CHEMBL4596606 hrh4_rat Rat No 6.5 EC50 = 331.1 nM Bind
Agonist activity at rat H4R expressed in HEK293T-beta-arr2-rH4R cells by beta-arrestin2 recruitment assayAgonist activity at rat H4R expressed in HEK293T-beta-arr2-rH4R cells by beta-arrestin2 recruitment assay
277 3 1 5 2.1 CN1CCCN(c2ccnc(NCC(C)(C)C)n2)CC1
CHEMBL475621 hrh4_rat Rat No 5.5 EC50 = 3311.3 nM Funct
Agonist activity at rat H4R by [35S]-GTPgammaS-binding assayAgonist activity at rat H4R by [35S]-GTPgammaS-binding assay
223 5 3 2 0.2 CCC(=O)/N=C(\N)NCCCc1c[nH]cn1
CHEMBL2165643 hrh4_human Human No 6.5 EC50 = 338.8 nM Funct
Agonist activity at human H4R-RGS19 Galphai2 Gbeta1gamma2 expressed in Sf9 cells at 0.1 nM to 1 mM by steady state GTPase activity assayAgonist activity at human H4R-RGS19 Galphai2 Gbeta1gamma2 expressed in Sf9 cells at 0.1 nM to 1 mM by steady state GTPase activity assay
584 23 6 4 4.0 N/C(=N\C(=O)CCCCCCCCCCCCCCC(=O)/N=C(\N)NCCCc1c[nH]cn1)NCCCc1c[nH]cn1
CHEMBL444484 hrh4_rat Rat No 6.5 EC50 = 338.8 nM Funct
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
278 2 1 7 -0.4 CN1CCN(c2cc(N3CCOCC3)nc(N)n2)CC1
CHEMBL1196470 hrh4_rat Rat Yes 4.5 EC50 = 33884.4 nM Funct
Agonist activity at rat H4R by [35S]-GTPgammaS-binding assayAgonist activity at rat H4R by [35S]-GTPgammaS-binding assay
161 3 4 3 -1.1 NC(=N)SCCN=C(N)N
CHEMBL4445423 hrh4_human Human No 7.5 EC50 = 35.5 nM Funct
Agonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
291 4 4 5 1.0 CC(C)(C)CNc1nccc(N2CC[C@@H](NC(=N)N)C2)n1
CHEMBL4598198 hrh4_human Human No 7.5 EC50 = 35.5 nM Funct
Agonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
291 4 4 5 1.0 CC(C)(C)CNc1nccc(N2CC[C@@H](NC(=N)N)C2)n1
CHEMBL4543119 hrh4_mouse Mouse No 7.5 EC50 = 35.5 nM Funct
Agonist activity at mouse H4R expressed in HEK293-SF-mH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at mouse H4R expressed in HEK293-SF-mH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
277 3 1 5 2.1 CN1CCCN(c2ccnc(NCC(C)(C)C)n2)CC1
CHEMBL4596606 hrh4_mouse Mouse No 7.5 EC50 = 35.5 nM Funct
Agonist activity at mouse H4R expressed in HEK293-SF-mH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at mouse H4R expressed in HEK293-SF-mH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
277 3 1 5 2.1 CN1CCCN(c2ccnc(NCC(C)(C)C)n2)CC1
CHEMBL4518374 hrh4_mouse Mouse No 6.5 EC50 = 354.8 nM Bind
Agonist activity at mouse H4R expressed in HEK293T-beta-arr2-mH4R cells by beta-arrestin2 recruitment assayAgonist activity at mouse H4R expressed in HEK293T-beta-arr2-mH4R cells by beta-arrestin2 recruitment assay
263 3 2 5 1.7 CC(C)(C)CNc1nccc(N2CCCNCC2)n1
CHEMBL4596491 hrh4_mouse Mouse No 6.5 EC50 = 354.8 nM Bind
Agonist activity at mouse H4R expressed in HEK293T-beta-arr2-mH4R cells by beta-arrestin2 recruitment assayAgonist activity at mouse H4R expressed in HEK293T-beta-arr2-mH4R cells by beta-arrestin2 recruitment assay
263 3 2 5 1.7 CC(C)(C)CNc1nccc(N2CCCNCC2)n1
CHEMBL492662 hrh4_rat Rat No 6.5 EC50 = 354.8 nM Funct
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
264 4 1 6 0.7 CCN(CC)c1cc(N2CCN(C)CC2)nc(N)n1
CHEMBL493479 hrh4_rat Rat Yes 6.4 EC50 = 363.1 nM Funct
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
207 1 1 5 0.1 Cc1cc(N2CCN(C)CC2)nc(N)n1
CHEMBL3220641 hrh4_human Human No 5.4 EC50 = 3630.8 nM Funct
Agonist activity at human recombinant histamine H4 receptor-RGS19 fusion protein expressed in Sf9 cells coexpressing Galphai2,Gbeta1gamma2 assessed as [35S]GTPgammaS binding after 90 mins by liquid scintillation countingAgonist activity at human recombinant histamine H4 receptor-RGS19 fusion protein expressed in Sf9 cells coexpressing Galphai2,Gbeta1gamma2 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
CHEMBL492663 hrh4_rat Rat No 5.4 EC50 = 3630.8 nM Funct
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
305 3 1 7 -0.0 CN1CCN(c2cc(N3CCC(N(C)C)C3)nc(N)n2)CC1
CHEMBL494585 hrh4_rat Rat No 5.4 EC50 = 3630.8 nM Funct
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
248 1 1 4 2.2 CN1CCC(c2cc(C(C)(C)C)nc(N)n2)CC1
CHEMBL3805437 hrh4_mouse Mouse No 5.4 EC50 = 3631 nM Bind
Agonist activity at mouse SF-His6-tagged histamine H4 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated response incubated for 5 hrs by luciferase reporter gene assayAgonist activity at mouse SF-His6-tagged histamine H4 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated response incubated for 5 hrs by luciferase reporter gene assay
246 3 3 3 0.9 CN/C(=N\C#N)NC[C@@H]1CC[C@@H](c2c[nH]cn2)C1
CHEMBL1078642 hrh4_human Human Yes 7.4 EC50 = 37 nM Funct
Agonist activity at human histamine H4 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 H4 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
CHEMBL1078642 hrh4_human Human Yes 7.4 EC50 = 37.2 nM Funct
Agonist activity at human recombinant histamine H4 receptor-RGS19 fusion protein expressed in Sf9 cells coexpressing Galphai2,Gbeta1gamma2 assessed as [35S]GTPgammaS binding after 90 mins by liquid scintillation countingAgonist activity at human recombinant histamine H4 receptor-RGS19 fusion protein expressed in Sf9 cells coexpressing Galphai2,Gbeta1gamma2 assessed as [35S]GTPgammaS binding after 90 mins by liquid scintillation counting
342 9 3 4 2.5 C1=CC=C(C=C1)SCCNC(=NCCCCC2=CN=CN2)NC#N
CHEMBL493720 hrh4_rat Rat No 7.4 EC50 = 37.2 nM Funct
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
303 2 1 5 2.1 CN1CCN(c2cc(-c3ccc(Cl)cc3)nc(N)n2)CC1
CHEMBL594491 hrh4_human Human Yes 7.4 EC50 = 37.2 nM Funct
Inverse agonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of [35S]GTPgammaS bindingInverse agonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of [35S]GTPgammaS binding
310 2 1 6 1.3 CN1CCN(c2cc(N3Cc4ccccc4C3)nc(N)n2)CC1
CHEMBL90 hrh4_rat Rat Yes 5.4 EC50 = 3715.4 nM Bind
Agonist activity at rat H4R expressed in HEK293T-beta-arr2-rH4R cells by beta-arrestin2 recruitment assayAgonist activity at rat H4R expressed in HEK293T-beta-arr2-rH4R cells by beta-arrestin2 recruitment assay
111 2 2 2 -0.1 NCCc1cnc[nH]1
CHEMBL3805663 hrh4_human Human No 6.4 EC50 = 372 nM Funct
Agonist activity at human histamine H4 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 H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assay
350 7 3 3 2.9 N#C/N=C(/NCCCc1ccccc1)NC[C@@H]1CC[C@H](c2c[nH]cn2)C1
CHEMBL1196470 hrh4_human Human Yes 7.4 EC50 = 38.0 nM Funct
Agonist activity at human H4R by [35S]-GTPgammaS-binding assayAgonist activity at human H4R by [35S]-GTPgammaS-binding assay
161 3 4 3 -1.1 NC(=N)SCCN=C(N)N
CHEMBL387054 hrh4_human Human No 7.4 EC50 = 38.9 nM Funct
Activity at human histamine H4 receptor transfected in SK-N-MC cells by cAMP assayActivity at human histamine H4 receptor transfected in SK-N-MC cells by cAMP assay
345 0 0 4 3.9 CN1CCN(C2=Nc3ccc(Cl)cc3Oc3cc(F)ccc32)CC1
CHEMBL494667 hrh4_rat Rat No 6.4 EC50 = 389.1 nM Funct
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
259 2 2 6 0.2 CN1CCN(c2cc(-c3c[nH]cn3)nc(N)n2)CC1
CHEMBL493664 hrh4_human Human No 5.4 EC50 = 3890.5 nM Funct
Agonist activity at human histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at human histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
286 2 1 7 -0.0 CN1CCN(c2cc(-n3ccccc3=O)nc(N)n2)CC1
CHEMBL1083162 hrh4_mouse Mouse No 7.4 EC50 = 39 nM Funct
Intrinsic activity at mouse histamine H4 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-induced cAMP responsive element-beta-galactosidase activity after 6 hrs by colorimetric cAMP assayIntrinsic activity at mouse histamine H4 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-induced cAMP responsive element-beta-galactosidase activity after 6 hrs by colorimetric cAMP assay
407 9 3 4 4.3 Cc1cc(OCCCNCCc2c[nH]cn2)ccc1-c1nc2c(C)c(F)ccc2[nH]1
CHEMBL551790 hrh4_human Human No 7.4 EC50 = 39.8 nM Bind
Agonist activity at histamine H4 receptor (unknown origin) expressed in human U2OS cells increase in beta-arrestin2 recruitment after 2 hrs by luminescence assayAgonist activity at histamine H4 receptor (unknown origin) expressed in human U2OS cells increase in beta-arrestin2 recruitment after 2 hrs by luminescence assay
308 6 2 3 3.2 C1=CC(=CC(=C1)Cl)CN=C(N)SCCCC2=CN=CN2
CHEMBL4437371 hrh4_human Human No 7.4 EC50 = 39.8 nM Bind
Agonist activity at human H4R expressed in HEK293T-beta-arr2-hH4R cells by beta-arrestin2 recruitment assayAgonist activity at human H4R expressed in HEK293T-beta-arr2-hH4R cells by beta-arrestin2 recruitment assay
237 6 3 5 1.7 CC(C)(C)CNc1nccc(NCCCN)n1
CHEMBL4594753 hrh4_human Human No 7.4 EC50 = 39.8 nM Bind
Agonist activity at human H4R expressed in HEK293T-beta-arr2-hH4R cells by beta-arrestin2 recruitment assayAgonist activity at human H4R expressed in HEK293T-beta-arr2-hH4R cells by beta-arrestin2 recruitment assay
237 6 3 5 1.7 CC(C)(C)CNc1nccc(NCCCN)n1
CHEMBL275443 hrh4_human Human Yes 7.4 EC50 = 39.8 nM Funct
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
125 2 2 2 0.2 Cc1c(CCN)nc[nH]1
CHEMBL1632413 hrh4_human Human No 7.4 EC50 = 39.8 nM Funct
Agonist activity at human recombinant histamine H4 receptor expressed in human SK-N-MC cells co-expressing SRE-Luc by luciferase reporter gene assayAgonist activity at human recombinant histamine H4 receptor expressed in human SK-N-MC cells co-expressing SRE-Luc by luciferase reporter gene assay
292 1 2 3 2.2 CN1CCN(/C(=N\O)c2cc3cc(Cl)ccc3[nH]2)CC1
CHEMBL492884 hrh4_rat Rat Yes 7.4 EC50 = 39.8 nM Funct
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
269 2 1 5 1.5 CN1CCN(CC1)C2=NC(=NC(=C2)C3=CC=CC=C3)N
CHEMBL492884 hrh4_rat Rat Yes 7.4 EC50 = 39.8 nM Funct
Antagonist activity at rat histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assayAntagonist activity at rat histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assay
269 2 1 5 1.5 CN1CCN(CC1)C2=NC(=NC(=C2)C3=CC=CC=C3)N
CHEMBL2047474 hrh4_human Human No 6.4 EC50 = 398.1 nM Funct
Agonist activity at histamine H4 receptor (unknown origin) expressed in HEK293T cells harboring CRE-luciferase after 6 hrs by luciferase reporter gene assayAgonist activity at histamine H4 receptor (unknown origin) expressed in HEK293T cells harboring CRE-luciferase after 6 hrs by luciferase reporter gene assay
322 2 1 4 2.1 CN1CCN(C(=O)c2cc3cc(Cl)cc([N+](=O)[O-])c3[nH]2)CC1
CHEMBL12620 hrh4_human Human Yes 5.4 EC50 = 3981.1 nM Funct
Agonist activity at human recombinant histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2 by steady-state GTPase activity assayAgonist activity at human recombinant histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2 by steady-state GTPase activity assay
125 2 2 2 0.2 Cc1ncc(CCN)[nH]1
CHEMBL151467 hrh4_human Human Yes 5.4 EC50 = 3981.1 nM Bind
Inhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H4 receptorInhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H4 receptor
165 2 2 2 1.0 c1nc(CC2CCCNC2)c[nH]1
CHEMBL3393542 hrh4_human Human No 8.4 EC50 = 4 nM Funct
Agonist activity at human recombinant histamine H4 receptor expressed in SK-N-MC cells assessed as effect on forskolin-stimulated cAMP-mediated reporter gene activityAgonist activity at human recombinant histamine H4 receptor expressed in SK-N-MC cells assessed as effect on forskolin-stimulated cAMP-mediated reporter gene activity
249 6 2 5 1.5 CCCCNc1nccc(N2CC[C@@H](NC)C2)n1
CHEMBL4454158 hrh4_human Human No 8.4 EC50 = 4.2 nM Bind
Agonist activity at human H4R expressed in HEK293T-beta-arr2-hH4R cells by beta-arrestin2 recruitment assayAgonist activity at human H4R expressed in HEK293T-beta-arr2-hH4R cells by beta-arrestin2 recruitment assay
286 3 2 5 2.2 CC(C)(C)CNc1nccc(N2CCc3nc[nH]c3C2)n1
CHEMBL4597218 hrh4_human Human No 8.4 EC50 = 4.2 nM Bind
Agonist activity at human H4R expressed in HEK293T-beta-arr2-hH4R cells by beta-arrestin2 recruitment assayAgonist activity at human H4R expressed in HEK293T-beta-arr2-hH4R cells by beta-arrestin2 recruitment assay
286 3 2 5 2.2 CC(C)(C)CNc1nccc(N2CCc3nc[nH]c3C2)n1
CHEMBL4455324 hrh4_mouse Mouse No 8.4 EC50 = 4.2 nM Funct
Agonist activity at mouse H4R expressed in HEK293-SF-mH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at mouse H4R expressed in HEK293-SF-mH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
249 3 2 5 1.5 CC(C)(C)CNc1nccc(N2CC[C@@H](N)C2)n1
CHEMBL4596881 hrh4_mouse Mouse No 8.4 EC50 = 4.2 nM Funct
Agonist activity at mouse H4R expressed in HEK293-SF-mH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at mouse H4R expressed in HEK293-SF-mH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
249 3 2 5 1.5 CC(C)(C)CNc1nccc(N2CC[C@@H](N)C2)n1
CHEMBL521996 hrh4_mouse Mouse No 8.4 EC50 = 4.4 nM Funct
Antagonist activity at mouse histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assayAntagonist activity at mouse histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assay
309 2 2 5 2.0 CN[C@@H]1CCN(c2nc(N)nc3c2CCCc2ccccc2-3)C1
CHEMBL475621 hrh4_human Human No 8.4 EC50 = 4.5 nM Funct
Agonist activity at human H4R by [35S]-GTPgammaS-binding assayAgonist activity at human H4R by [35S]-GTPgammaS-binding assay
223 5 3 2 0.2 CCC(=O)/N=C(\N)NCCCc1c[nH]cn1
CHEMBL1096431 hrh4_human Human No 8.3 EC50 = 4.6 nM Bind
Activity at human recombinant GAIP-fused histamine H4 receptor expressed in Sf9 cells coexpressing Galphai, Gbeta1gamma2 by steady-state GTPase activity assayActivity at human recombinant GAIP-fused histamine H4 receptor expressed in Sf9 cells coexpressing Galphai, Gbeta1gamma2 by steady-state GTPase activity assay
319 7 4 3 2.6 C[C@@H](CC(=O)NC(=N)NCCCc1c[nH]cn1)C1CCCCC1
CHEMBL523225 hrh4_mouse Mouse No 8.3 EC50 = 4.8 nM Funct
Antagonist activity at mouse histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assayAntagonist activity at mouse histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assay
313 1 2 5 1.8 Nc1nc2c(c(N3CCNCC3)n1)CCCc1ccc(F)cc1-2
CHEMBL443896 hrh4_human Human No 8.3 EC50 = 4.9 nM Bind
Agonist activity at human H4 receptor expressed in insect Sf9 cells co-expressing RGS19 fusion protein and Gialpha2, Gbeta1gamma2 assessed as gamma[32P]GTP binding by liquid scintillation countingAgonist activity at human H4 receptor expressed in insect Sf9 cells co-expressing RGS19 fusion protein and Gialpha2, Gbeta1gamma2 assessed as gamma[32P]GTP binding by liquid scintillation counting
209 4 3 2 -0.2 CC(=O)/N=C(\N)NCCCc1c[nH]cn1
CHEMBL320279 hrh4_human Human Yes 4.4 EC50 = 40738.0 nM Funct
Inhibition of the forskolin-stimulated cAMP production in SK-N-MC cells expressing human Histamine H4 receptorInhibition of the forskolin-stimulated cAMP production in SK-N-MC cells expressing human Histamine H4 receptor
165 2 2 3 0.4 NC[C@@H]1C=C[C@H](c2c[nH]cn2)O1
CHEMBL2165641 hrh4_human Human No 7.4 EC50 = 41.7 nM Funct
Agonist activity at human H4R-RGS19 Galphai2 Gbeta1gamma2 expressed in Sf9 cells at 0.1 nM to 1 mM by steady state GTPase activity assayAgonist activity at human H4R-RGS19 Galphai2 Gbeta1gamma2 expressed in Sf9 cells at 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
CHEMBL260374 hrh4_human Human Yes 6.4 EC50 = 416.9 nM Funct
Antagonist activity at human histamine 4 receptor expressed in Sf9 cell membranes co-expressing Galphai2 and Gbeta1gamma2 assessed as [35S]GTPgammaS binding by scintillation countingAntagonist activity at human histamine 4 receptor expressed in Sf9 cell membranes co-expressing Galphai2 and Gbeta1gamma2 assessed as [35S]GTPgammaS binding by scintillation counting
292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1
CHEMBL440730 hrh4_human Human Yes 6.4 EC50 = 416.9 nM Bind
Inhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H4 receptorInhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H4 receptor
151 2 2 2 0.6 c1nc(C[C@H]2CCNC2)c[nH]1
CHEMBL4518374 hrh4_human Human No 7.4 EC50 = 42.7 nM Bind
Agonist activity at human H4R expressed in HEK293T-beta-arr2-hH4R cells by beta-arrestin2 recruitment assayAgonist activity at human H4R expressed in HEK293T-beta-arr2-hH4R cells by beta-arrestin2 recruitment assay
263 3 2 5 1.7 CC(C)(C)CNc1nccc(N2CCCNCC2)n1
CHEMBL4596491 hrh4_human Human No 7.4 EC50 = 42.7 nM Bind
Agonist activity at human H4R expressed in HEK293T-beta-arr2-hH4R cells by beta-arrestin2 recruitment assayAgonist activity at human H4R expressed in HEK293T-beta-arr2-hH4R cells by beta-arrestin2 recruitment assay
263 3 2 5 1.7 CC(C)(C)CNc1nccc(N2CCCNCC2)n1
CHEMBL492274 hrh4_rat Rat No 7.4 EC50 = 42.7 nM Funct
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
283 2 1 5 1.8 Cc1cccc(-c2cc(N3CCN(C)CC3)nc(N)n2)c1
CHEMBL493478 hrh4_rat Rat No 7.4 EC50 = 42.7 nM Funct
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
208 1 2 6 -0.6 CN1CCN(c2nc(N)ncc2N)CC1
CHEMBL129198 hrh4_rat Rat Yes 7.4 EC50 = 42.7 nM Funct
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein by GTPgammaS assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein by GTPgammaS assay
277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl
CHEMBL501882 hrh4_human Human Yes 7.4 EC50 = 43.7 nM Funct
Agonist activity at human histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at human histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
193 1 1 5 -0.2 CN1CCN(c2ccnc(N)n2)CC1
CHEMBL493719 hrh4_rat Rat No 7.4 EC50 = 43.7 nM Funct
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
299 3 1 6 1.5 COc1ccccc1-c1cc(N2CCN(C)CC2)nc(N)n1
CHEMBL594490 hrh4_human Human Yes 7.4 EC50 = 43.7 nM Funct
Inverse agonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of [35S]GTPgammaS bindingInverse agonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of [35S]GTPgammaS binding
324 2 1 6 1.4 CN1CCN(c2cc(N3CCc4ccccc4C3)nc(N)n2)CC1
CHEMBL3805514 hrh4_human Human No 7.4 EC50 = 44 nM Funct
Agonist activity at human histamine H4 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 H4 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
CHEMBL492231 hrh4_mouse Mouse No 7.3 EC50 = 45.7 nM Funct
Antagonist activity at mouse histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assayAntagonist activity at mouse histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assay
323 2 2 5 2.3 Nc1nc2c(c(N3CCNCC3)n1)CCCCC2c1ccccc1
CHEMBL444782 hrh4_rat Rat Yes 7.3 EC50 = 46.8 nM Funct
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
276 2 1 6 0.8 CN1CCN(c2cc(N3CCCCC3)nc(N)n2)CC1
CHEMBL3220640 hrh4_human Human No 6.3 EC50 = 467.7 nM Funct
Agonist activity at human recombinant histamine H4 receptor-RGS19 fusion protein expressed in Sf9 cells coexpressing Galphai2,Gbeta1gamma2 assessed as [35S]GTPgammaS binding after 90 mins by liquid scintillation countingAgonist activity at human recombinant histamine H4 receptor-RGS19 fusion protein expressed in Sf9 cells coexpressing Galphai2,Gbeta1gamma2 assessed as [35S]GTPgammaS binding after 90 mins by liquid scintillation counting
342 8 3 4 2.5 Cc1nc(CCCN/C(=N\C#N)NCCSc2ccccc2)c[nH]1
CHEMBL489663 hrh4_rat Rat Yes 5.3 EC50 = 4677.4 nM Funct
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
249 1 1 5 1.1 CN1CCN(c2cc(N)nc(C(C)(C)C)n2)CC1
CHEMBL492489 hrh4_rat Rat No 5.3 EC50 = 4677.4 nM Funct
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
264 2 0 5 1.5 COc1nc(N2CCN(C)CC2)cc(C(C)(C)C)n1
CHEMBL494678 hrh4_rat Rat No 5.3 EC50 = 4677.4 nM Funct
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein by GTPgammaS assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein by GTPgammaS assay
294 2 1 6 1.3 CN1CCN(c2cc(-c3ccc(C#N)cc3)nc(N)n2)CC1
CHEMBL1082771 hrh4_human Human No 6.3 EC50 = 470 nM Funct
Agonist activity at human histamine H4 receptor in SK-N-MC cells assessed as forskolin-stimulated cAMP release preincubated for 10 mins before forskolin challengeAgonist activity at human histamine H4 receptor in SK-N-MC cells assessed as forskolin-stimulated cAMP release preincubated for 10 mins before forskolin challenge
382 6 2 4 3.8 Cc1cc(OCCCN2CCC(N)C2)ccc1-c1nc2c(C)c(F)ccc2[nH]1
CHEMBL595880 hrh4_human Human No 6.3 EC50 = 478.6 nM Funct
Inverse agonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of [35S]GTPgammaS bindingInverse agonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of [35S]GTPgammaS binding
343 5 2 8 1.3 CN1CCN(c2cc(NCc3cccc([N+](=O)[O-])c3)nc(N)n2)CC1
CHEMBL3393529 hrh4_human Human Yes 7.3 EC50 = 48 nM Funct
Agonist activity at human recombinant histamine H4 receptor expressed in SK-N-MC cells assessed as effect on forskolin-stimulated cAMP-mediated reporter gene activityAgonist activity at human recombinant histamine H4 receptor expressed in SK-N-MC cells assessed as effect on forskolin-stimulated cAMP-mediated reporter gene activity
248 6 2 4 2.1 CCCCNc1cc(N2CC[C@@H](NC)C2)ccn1
CHEMBL492677 hrh4_rat Rat No 6.3 EC50 = 489.8 nM Funct
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
298 4 2 6 1.4 CN1CCN(CC1)C2=NC(=NC(=C2)NCC3=CC=CC=C3)N
CHEMBL495112 hrh4_rat Rat Yes 6.3 EC50 = 489.8 nM Funct
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
222 2 2 6 -0.1 CNc1cc(N2CCN(C)CC2)nc(N)n1
CHEMBL495265 hrh4_human Human No 5.3 EC50 = 4897.8 nM Funct
Agonist activity at human histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at human histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
268 1 0 4 2.2 CN1CCN(c2cc(C(C)(C)C)nc(Cl)n2)CC1
CHEMBL502347 hrh4_mouse Mouse Yes 8.2 EC50 = 5.8 nM Funct
Antagonist activity at mouse histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assayAntagonist activity at mouse histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assay
295 1 2 5 1.8 Nc1nc2c(c(N3CC[C@@H](N)C3)n1)CCCc1ccccc1-2
CHEMBL1770964 hrh4_human Human No 7.3 EC50 = 50 nM Funct
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells assessed as effect on forskolin-induced cAMP accumulation after 6 hrsAgonist activity at human histamine H4 receptor expressed in human SK-N-MC cells assessed as effect on forskolin-induced cAMP accumulation after 6 hrs
263 4 2 5 1.5 CC(C)CNc1cc(N2CCN(C)CC2)cc(N)n1
CHEMBL1086460 hrh4_human Human No 7.3 EC50 = 50 nM Funct
Agonist activity at human histamine H4 receptor in SK-N-MC cells assessed as forskolin-stimulated cAMP release preincubated for 10 mins before forskolin challengeAgonist activity at human histamine H4 receptor in SK-N-MC cells assessed as forskolin-stimulated cAMP release preincubated for 10 mins before forskolin challenge
396 6 1 4 4.0 Cc1cc(OCCCN2CCN(C)CC2)ccc1-c1nc2c(C)c(F)ccc2[nH]1
CHEMBL1196470 hrh4_human Human Yes 7.3 EC50 = 50.1 nM Funct
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H4 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 hrh4_human Human Yes 7.3 EC50 = 50.1 nM Funct
Agonist activity at human histamine H4 receptor in SK-N-MC cells assessed as inhibition of forskolin-induced cAMP-mediated CRE-beta galactosidase activityAgonist activity at human histamine H4 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
CHEMBL4439142 hrh4_mouse Mouse No 7.3 EC50 = 50.1 nM Bind
Agonist activity at mouse recombinant H4R expressed in HEK293T cells by beta-arrestin recruitment assayAgonist activity at mouse recombinant H4R expressed in HEK293T cells by beta-arrestin recruitment assay
277 4 1 5 2.1 CN(C)[C@@H]1CCN(c2ccnc(NCC(C)(C)C)n2)C1
CHEMBL4515149 hrh4_mouse Mouse No 7.3 EC50 = 50.1 nM Bind
Agonist activity at mouse recombinant H4R expressed in HEK293T cells by beta-arrestin recruitment assayAgonist activity at mouse recombinant H4R expressed in HEK293T cells by beta-arrestin recruitment assay
277 4 1 5 2.1 CN(C)[C@@H]1CCN(c2ccnc(NCC(C)(C)C)n2)C1
CHEMBL4595327 hrh4_mouse Mouse No 7.3 EC50 = 50.1 nM Bind
Agonist activity at mouse recombinant H4R expressed in HEK293T cells by beta-arrestin recruitment assayAgonist activity at mouse recombinant H4R expressed in HEK293T cells by beta-arrestin recruitment assay
277 4 1 5 2.1 CN(C)[C@@H]1CCN(c2ccnc(NCC(C)(C)C)n2)C1
CHEMBL4635634 hrh4_mouse Mouse No 7.3 EC50 = 50.1 nM Bind
Antagonist activity at mouse H4R expressed in HEK293 cells co-expressing ELucC/ELucN-beta-arrestin2 assessed as inhibition of histamine-induced beta-arrestin recruitment preincubated for 15 mins followed by histamine addition by luciferase reporter gene assayAntagonist activity at mouse H4R expressed in HEK293 cells co-expressing ELucC/ELucN-beta-arrestin2 assessed as inhibition of histamine-induced beta-arrestin recruitment preincubated for 15 mins followed by histamine addition 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 hrh4_mouse Mouse No 7.3 EC50 = 50.1 nM Bind
Antagonist activity at mouse H4R expressed in HEK293 cells co-expressing ELucC/ELucN-beta-arrestin2 assessed as inhibition of histamine-induced beta-arrestin recruitment preincubated for 15 mins followed by histamine addition by luciferase reporter gene assayAntagonist activity at mouse H4R expressed in HEK293 cells co-expressing ELucC/ELucN-beta-arrestin2 assessed as inhibition of histamine-induced beta-arrestin recruitment preincubated for 15 mins followed by histamine addition 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
CHEMBL3805220 hrh4_human Human No 6.3 EC50 = 500 nM Bind
Agonist activity at human SF-His6-tagged histamine H4 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated response incubated for 5 hrs by luciferase reporter gene assayAgonist activity at human SF-His6-tagged histamine H4 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated response incubated for 5 hrs by luciferase reporter gene assay
368 7 3 4 3.1 N#C/N=C(/NCCSc1ccccc1)NC[C@@H]1CC[C@@H](c2c[nH]cn2)C1
CHEMBL1632412 hrh4_rat Rat No 6.3 EC50 = 501.2 nM Funct
Agonist activity at rat histamine H4 receptor by luciferase reporter gene assayAgonist activity at rat histamine H4 receptor by luciferase reporter gene assay
271 2 2 3 3.0 Cc1ccc2[nH]c(/C(=N\O)C3CCN(C)CC3)cc2c1
CHEMBL175782 hrh4_human Human Yes 5.3 EC50 = 5011.9 nM Funct
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H4 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
CHEMBL321920 hrh4_human Human No 5.3 EC50 = 5011.9 nM Funct
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H4 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
CHEMBL90 hrh4_mouse Mouse Yes 5.3 EC50 = 5011.9 nM Funct
Agonist activity at mouse histamine H4 receptor by luciferase reporter gene assayAgonist activity at mouse histamine H4 receptor by luciferase reporter gene assay
111 2 2 2 -0.1 NCCc1cnc[nH]1
CHEMBL4439142 hrh4_rat Rat No 4.3 EC50 = 50118.7 nM Funct
Agonist activity at rat H4R expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 by [35S]-GTPgammaS-binding assayAgonist activity at rat H4R expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 by [35S]-GTPgammaS-binding assay
277 4 1 5 2.1 CN(C)[C@@H]1CCN(c2ccnc(NCC(C)(C)C)n2)C1
CHEMBL4515149 hrh4_rat Rat No 4.3 EC50 = 50118.7 nM Funct
Agonist activity at rat H4R expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 by [35S]-GTPgammaS-binding assayAgonist activity at rat H4R expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 by [35S]-GTPgammaS-binding assay
277 4 1 5 2.1 CN(C)[C@@H]1CCN(c2ccnc(NCC(C)(C)C)n2)C1
CHEMBL4595327 hrh4_rat Rat No 4.3 EC50 = 50118.7 nM Funct
Agonist activity at rat H4R expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 by [35S]-GTPgammaS-binding assayAgonist activity at rat H4R expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 by [35S]-GTPgammaS-binding assay
277 4 1 5 2.1 CN(C)[C@@H]1CCN(c2ccnc(NCC(C)(C)C)n2)C1
CHEMBL19439 hrh4_human Human Yes 7.3 EC50 = 51 nM Bind
Inhibition of human Histamine H4 receptorInhibition of human Histamine H4 receptor
170 3 3 3 0.6 NC(=N)SCCc1cnc[nH]1
CHEMBL4437371 hrh4_mouse Mouse No 7.3 EC50 = 51.3 nM Funct
Agonist activity at mouse H4R expressed in HEK293-SF-mH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at mouse H4R expressed in HEK293-SF-mH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
237 6 3 5 1.7 CC(C)(C)CNc1nccc(NCCCN)n1
CHEMBL4594753 hrh4_mouse Mouse No 7.3 EC50 = 51.3 nM Funct
Agonist activity at mouse H4R expressed in HEK293-SF-mH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at mouse H4R expressed in HEK293-SF-mH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
237 6 3 5 1.7 CC(C)(C)CNc1nccc(NCCCN)n1
CHEMBL4518374 hrh4_mouse Mouse No 7.3 EC50 = 51.3 nM Funct
Agonist activity at mouse H4R expressed in HEK293-SF-mH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at mouse H4R expressed in HEK293-SF-mH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
263 3 2 5 1.7 CC(C)(C)CNc1nccc(N2CCCNCC2)n1
CHEMBL4596491 hrh4_mouse Mouse No 7.3 EC50 = 51.3 nM Funct
Agonist activity at mouse H4R expressed in HEK293-SF-mH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at mouse H4R expressed in HEK293-SF-mH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
263 3 2 5 1.7 CC(C)(C)CNc1nccc(N2CCCNCC2)n1
CHEMBL4439142 hrh4_mouse Mouse No 7.3 EC50 = 51.3 nM Bind
Agonist activity at mouse H4R expressed in HEK293T-beta-arr2-mH4R cells by beta-arrestin2 recruitment assayAgonist activity at mouse H4R expressed in HEK293T-beta-arr2-mH4R cells by beta-arrestin2 recruitment assay
277 4 1 5 2.1 CN(C)[C@@H]1CCN(c2ccnc(NCC(C)(C)C)n2)C1
CHEMBL4515149 hrh4_mouse Mouse No 7.3 EC50 = 51.3 nM Bind
Agonist activity at mouse H4R expressed in HEK293T-beta-arr2-mH4R cells by beta-arrestin2 recruitment assayAgonist activity at mouse H4R expressed in HEK293T-beta-arr2-mH4R cells by beta-arrestin2 recruitment assay
277 4 1 5 2.1 CN(C)[C@@H]1CCN(c2ccnc(NCC(C)(C)C)n2)C1
CHEMBL4595327 hrh4_mouse Mouse No 7.3 EC50 = 51.3 nM Bind
Agonist activity at mouse H4R expressed in HEK293T-beta-arr2-mH4R cells by beta-arrestin2 recruitment assayAgonist activity at mouse H4R expressed in HEK293T-beta-arr2-mH4R cells by beta-arrestin2 recruitment assay
277 4 1 5 2.1 CN(C)[C@@H]1CCN(c2ccnc(NCC(C)(C)C)n2)C1
CHEMBL455016 hrh4_rat Rat No 5.3 EC50 = 5128.6 nM Funct
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
263 2 1 5 1.6 CNc1nc(N2CCN(C)CC2)cc(C(C)(C)C)n1
CHEMBL493103 hrh4_rat Rat No 5.3 EC50 = 5128.6 nM Funct
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
324 3 1 7 1.4 COc1c(-c2ccc(C#N)cc2)nc(N)nc1N1CCN(C)CC1
CHEMBL3804862 hrh4_human Human No 6.3 EC50 = 524 nM Funct
Agonist activity at human histamine H4 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 H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assay
352 7 3 4 2.4 N#C/N=C(/NCCOc1ccccc1)NC[C@H]1CC[C@H](c2c[nH]cn2)C1
CHEMBL90 hrh4_rat Rat Yes 4.3 EC50 = 52480.8 nM Funct
Agonist activity at rat H4R by [35S]-GTPgammaS-binding assayAgonist activity at rat H4R by [35S]-GTPgammaS-binding assay
111 2 2 2 -0.1 NCCc1cnc[nH]1
CHEMBL1770962 hrh4_human Human No 6.3 EC50 = 533 nM Funct
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells assessed as effect on forskolin-induced cAMP accumulation after 6 hrsAgonist activity at human histamine H4 receptor expressed in human SK-N-MC cells assessed as effect on forskolin-induced cAMP accumulation after 6 hrs
249 3 2 5 1.2 CC(C)Nc1cc(N2CCN(C)CC2)cc(N)n1
CHEMBL3804906 hrh4_mouse Mouse No 6.3 EC50 = 538 nM Bind
Agonist activity at mouse SF-His6-tagged histamine H4 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated response incubated for 5 hrs by luciferase reporter gene assayAgonist activity at mouse SF-His6-tagged histamine H4 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated response incubated for 5 hrs by luciferase reporter gene assay
246 3 3 3 0.9 CN/C(=N\C#N)NC[C@H]1CC[C@H](c2c[nH]cn2)C1
CHEMBL492231 hrh4_rat Rat No 7.3 EC50 = 55.0 nM Funct
Antagonist activity at rat histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assayAntagonist activity at rat histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assay
323 2 2 5 2.3 Nc1nc2c(c(N3CCNCC3)n1)CCCCC2c1ccccc1
CHEMBL90 hrh4_human Human Yes 7.3 EC50 = 55.0 nM Bind
Inhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H4 receptorInhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H4 receptor
111 2 2 2 -0.1 NCCc1cnc[nH]1
CHEMBL1083162 hrh4_mouse Mouse No 6.3 EC50 = 548 nM Bind
Displacement of [3H]histamine from mouse recombinant histamine H4 receptorDisplacement of [3H]histamine from mouse recombinant histamine H4 receptor
407 9 3 4 4.3 Cc1cc(OCCCNCCc2c[nH]cn2)ccc1-c1nc2c(C)c(F)ccc2[nH]1
CHEMBL3805431 hrh4_human Human No 6.3 EC50 = 549 nM Funct
Agonist activity at human histamine H4 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 H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assay
368 7 3 4 3.1 N#C/N=C(/NCCSc1ccccc1)NC[C@H]1CC[C@@H](c2c[nH]cn2)C1
CHEMBL3220639 hrh4_human Human No 6.3 EC50 = 549.5 nM Funct
Agonist activity at human recombinant histamine H4 receptor-RGS19 fusion protein expressed in Sf9 cells coexpressing Galphai2,Gbeta1gamma2 assessed as [35S]GTPgammaS binding after 90 mins by liquid scintillation countingAgonist activity at human recombinant histamine H4 receptor-RGS19 fusion protein expressed in Sf9 cells coexpressing Galphai2,Gbeta1gamma2 assessed as [35S]GTPgammaS binding after 90 mins by liquid scintillation counting
220 4 3 3 0.3 CN/C(=N/C#N)NCCCc1c[nH]c(C)n1
CHEMBL322988 hrh4_human Human Yes 6.3 EC50 = 549.5 nM Funct
Inhibition of the forskolin-stimulated cAMP production for human Histamine H4 receptorInhibition of the forskolin-stimulated cAMP production for human Histamine H4 receptor
125 2 2 2 0.5 CC(CN)c1cnc[nH]1
CHEMBL321920 hrh4_human Human No 5.3 EC50 = 5495.4 nM Funct
Inhibition of the forskolin-stimulated cAMP production in SK-N-MC cells expressing human Histamine H4 receptorInhibition of the forskolin-stimulated cAMP production in SK-N-MC cells expressing human Histamine H4 receptor
167 2 2 3 0.6 NC[C@@H]1CC[C@H](c2c[nH]cn2)O1
CHEMBL492885 hrh4_rat Rat No 7.3 EC50 = 56.2 nM Funct
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
283 2 1 5 1.8 Cc1ccc(-c2cc(N3CCN(C)CC3)nc(N)n2)cc1
CHEMBL18661 hrh4_human Human Yes 7.3 EC50 = 56.2 nM Bind
Inhibition of the cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H4 receptorInhibition of the cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H4 receptor
165 2 2 2 1.0 N1CCC(CC1)Cc1[nH]cnc1
CHEMBL18661 hrh4_human Human Yes 7.3 EC50 = 56.2 nM Bind
Inhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H4 receptorInhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H4 receptor
165 2 2 2 1.0 N1CCC(CC1)Cc1[nH]cnc1
CHEMBL595215 hrh4_human Human No 7.3 EC50 = 56.2 nM Funct
Inverse agonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of [35S]GTPgammaS bindingInverse agonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of [35S]GTPgammaS binding
366 4 2 6 2.7 CN1CCN(c2cc(NCc3ccc(Cl)c(Cl)c3)nc(N)n2)CC1
CHEMBL1077580 hrh4_human Human No 6.2 EC50 = 575.4 nM Funct
Agonist activity at human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19 protein by steady-state GTPase assayAgonist activity at human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19 protein by steady-state GTPase assay
325 9 3 4 1.8 N#C/N=C(/NCCCCc1c[nH]cn1)NCCCc1ccccn1
CHEMBL492900 hrh4_rat Rat No 7.2 EC50 = 58.9 nM Funct
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
308 2 1 6 1.7 Cc1c(-c2ccc(C#N)cc2)nc(N)nc1N1CCN(C)CC1
CHEMBL494678 hrh4_rat Rat No 7.2 EC50 = 58.9 nM Funct
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
294 2 1 6 1.3 CN1CCN(c2cc(-c3ccc(C#N)cc3)nc(N)n2)CC1
CHEMBL494678 hrh4_rat Rat No 7.2 EC50 = 58.9 nM Funct
Antagonist activity at rat histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assayAntagonist activity at rat histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assay
294 2 1 6 1.3 CN1CCN(c2cc(-c3ccc(C#N)cc3)nc(N)n2)CC1
CHEMBL310360 hrh4_human Human Yes 4.2 EC50 = 58884.4 nM Bind
Inhibition of the cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H4 receptorInhibition of the cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H4 receptor
173 3 1 2 1.6 c1ccc(CCc2c[nH]cn2)nc1
CHEMBL3805220 hrh4_mouse Mouse No 6.2 EC50 = 589 nM Bind
Agonist activity at mouse SF-His6-tagged histamine H4 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated response incubated for 5 hrs by luciferase reporter gene assayAgonist activity at mouse SF-His6-tagged histamine H4 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated response incubated for 5 hrs by luciferase reporter gene assay
368 7 3 4 3.1 N#C/N=C(/NCCSc1ccccc1)NC[C@@H]1CC[C@@H](c2c[nH]cn2)C1
CHEMBL594721 hrh4_human Human No 8.2 EC50 = 6.0 nM Funct
Agonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of [35S]GTPgammaS binding
332 4 2 6 2.1 CN1CCN(c2cc(NCc3ccccc3Cl)nc(N)n2)CC1
CHEMBL523225 hrh4_rat Rat No 8.2 EC50 = 6.0 nM Funct
Antagonist activity at rat histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assayAntagonist activity at rat histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assay
313 1 2 5 1.8 Nc1nc2c(c(N3CCNCC3)n1)CCCc1ccc(F)cc1-2
CHEMBL4445423 hrh4_mouse Mouse No 8.2 EC50 = 6.2 nM Funct
Agonist activity at mouse H4R expressed in HEK293-SF-mH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at mouse H4R expressed in HEK293-SF-mH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
291 4 4 5 1.0 CC(C)(C)CNc1nccc(N2CC[C@@H](NC(=N)N)C2)n1
CHEMBL4598198 hrh4_mouse Mouse No 8.2 EC50 = 6.2 nM Funct
Agonist activity at mouse H4R expressed in HEK293-SF-mH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at mouse H4R expressed in HEK293-SF-mH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
291 4 4 5 1.0 CC(C)(C)CNc1nccc(N2CC[C@@H](NC(=N)N)C2)n1
CHEMBL502339 hrh4_human Human No 8.2 EC50 = 6.3 nM Bind
Activity at human recombinant histamine H4 receptor-RGS4 fusion protein expressed in Sf9 cells coexpressing Galphai2 and G-beta-1-gamma-2 by steady-state GTPase activity assayActivity at human recombinant histamine H4 receptor-RGS4 fusion protein expressed in Sf9 cells coexpressing Galphai2 and G-beta-1-gamma-2 by steady-state GTPase activity assay
319 7 4 4 2.2 CC(CC(=O)NC(=N)NCCCc1c[nH]cn1)c1cccs1
CHEMBL551790 hrh4_human Human No 8.2 EC50 = 6.3 nM Funct
Agonist activity at histamine H4 receptor (unknown origin) expressed in HEK293T cells harboring CRE-luciferase after 6 hrs by luciferase reporter gene assayAgonist activity at histamine H4 receptor (unknown origin) expressed in HEK293T cells harboring CRE-luciferase after 6 hrs by luciferase reporter gene assay
308 6 2 3 3.2 C1=CC(=CC(=C1)Cl)CN=C(N)SCCCC2=CN=CN2
CHEMBL521996 hrh4_rat Rat No 8.2 EC50 = 6.6 nM Funct
Antagonist activity at rat histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assayAntagonist activity at rat histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assay
309 2 2 5 2.0 CN[C@@H]1CCN(c2nc(N)nc3c2CCCc2ccccc2-3)C1
CHEMBL1084869 hrh4_human Human No 8.2 EC50 = 6.9 nM Funct
Agonist activity at human histamine H4 receptor in SK-N-MC cells assessed as forskolin-stimulated cAMP release preincubated for 10 mins before forskolin challengeAgonist activity at human histamine H4 receptor in SK-N-MC cells assessed as forskolin-stimulated cAMP release preincubated for 10 mins before forskolin challenge
410 8 3 4 4.3 Cc1cc(OCCCNCC2CCCNC2)ccc1-c1nc2c(C)c(F)ccc2[nH]1
CHEMBL4443126 hrh4_human Human No 8.2 EC50 = 6.9 nM Bind
Agonist activity at human H4R expressed in HEK293T-beta-arr2-hH4R cells by beta-arrestin2 recruitment assayAgonist activity at human H4R expressed in HEK293T-beta-arr2-hH4R cells by beta-arrestin2 recruitment assay
263 4 2 5 1.7 CN[C@@H]1CCN(c2ccnc(NCC(C)(C)C)n2)C1
CHEMBL4596409 hrh4_human Human No 8.2 EC50 = 6.9 nM Bind
Agonist activity at human H4R expressed in HEK293T-beta-arr2-hH4R cells by beta-arrestin2 recruitment assayAgonist activity at human H4R expressed in HEK293T-beta-arr2-hH4R cells by beta-arrestin2 recruitment assay
263 4 2 5 1.7 CN[C@@H]1CCN(c2ccnc(NCC(C)(C)C)n2)C1
CHEMBL609289 hrh4_human Human No 6.2 EC50 = 602.6 nM Funct
Agonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of [35S]GTPgammaS binding
323 4 2 7 1.3 CN1CCN(c2cc(NCc3ccc(C#N)cc3)nc(N)n2)CC1
CHEMBL1094142 hrh4_human Human No 5.2 EC50 = 6025.6 nM Bind
Activity at human recombinant GAIP-fused histamine H4 receptor expressed in Sf9 cells coexpressing Galphai, Gbeta1gamma2 by steady-state GTPase activity assayActivity at human recombinant GAIP-fused histamine H4 receptor expressed in Sf9 cells coexpressing Galphai, Gbeta1gamma2 by steady-state GTPase activity assay
365 7 4 5 3.2 Cc1nc(N)sc1CCCNC(=N)NC(=O)CC(C)C1CCCCC1
CHEMBL1082772 hrh4_human Human No 7.2 EC50 = 62 nM Funct
Agonist activity at human histamine H4 receptor in SK-N-MC cells assessed as forskolin-stimulated cAMP release preincubated for 10 mins before forskolin challengeAgonist activity at human histamine H4 receptor in SK-N-MC cells assessed as forskolin-stimulated cAMP release preincubated for 10 mins before forskolin challenge
396 7 2 4 4.0 CNC1CCN(CCCOc2ccc(-c3nc4c(C)c(F)ccc4[nH]3)c(C)c2)C1
CHEMBL3804906 hrh4_human Human No 7.2 EC50 = 63 nM Bind
Agonist activity at human SF-His6-tagged histamine H4 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated response incubated for 5 hrs by luciferase reporter gene assayAgonist activity at human SF-His6-tagged histamine H4 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated response incubated for 5 hrs by luciferase reporter gene assay
246 3 3 3 0.9 CN/C(=N\C#N)NC[C@H]1CC[C@H](c2c[nH]cn2)C1
CHEMBL492677 hrh4_human Human No 7.2 EC50 = 63.1 nM Bind
Agonist activity at histamine H4 receptor (unknown origin) expressed in human U2OS cells increase in beta-arrestin2 recruitment after 2 hrs by luminescence assayAgonist activity at histamine H4 receptor (unknown origin) expressed in human U2OS cells increase in beta-arrestin2 recruitment after 2 hrs by luminescence assay
298 4 2 6 1.4 CN1CCN(CC1)C2=NC(=NC(=C2)NCC3=CC=CC=C3)N
CHEMBL19173 hrh4_human Human Yes 7.2 EC50 = 63.1 nM Funct
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H4 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
CHEMBL72372 hrh4_human Human No 7.2 EC50 = 63.1 nM Funct
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
336 8 3 2 3.4 S=C(NCCCCCc1c[nH]cn1)NCc1ccc(Cl)cc1
CHEMBL72769 hrh4_human Human No 7.2 EC50 = 63.1 nM Funct
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
240 7 3 2 2.0 CCC/N=C(\S)NCCCCc1c[nH]cn1
CHEMBL1632414 hrh4_mouse Mouse No 7.2 EC50 = 63.1 nM Funct
Agonist activity at mouse histamine H4 receptor by luciferase reporter gene assayAgonist activity at mouse histamine H4 receptor by luciferase reporter gene assay
292 2 2 4 2.7 CN1CCC(/C(=N/O)c2nc3cc(Cl)ccc3[nH]2)CC1
CHEMBL268229 hrh4_human Human Yes 6.2 EC50 = 631.0 nM Funct
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H4 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
CHEMBL493477 hrh4_rat Rat No 6.2 EC50 = 631.0 nM Funct
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
223 2 1 6 -0.2 COc1cnc(N)nc1N1CCN(C)CC1
CHEMBL4642520 hrh4_human Human No 7.2 EC50 = 64.6 nM Bind
Agonist activity at human H4R expressed in HEK293 cells co-expressing ELucC/ELucN-beta-arrestin2 assessed as induction of beta-arrestin recruitment by luciferase reporter gene assayAgonist activity at human H4R expressed in HEK293 cells co-expressing ELucC/ELucN-beta-arrestin2 assessed as induction of beta-arrestin recruitment by luciferase reporter gene assay
415 10 1 2 5.5 Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCCCCc1c[nH]cn1
CHEMBL4650832 hrh4_human Human No 7.2 EC50 = 64.6 nM Bind
Agonist activity at human H4R expressed in HEK293 cells co-expressing ELucC/ELucN-beta-arrestin2 assessed as induction of beta-arrestin recruitment by luciferase reporter gene assayAgonist activity at human H4R expressed in HEK293 cells co-expressing ELucC/ELucN-beta-arrestin2 assessed as induction of beta-arrestin recruitment by luciferase reporter gene assay
415 10 1 2 5.5 Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCCCCc1c[nH]cn1
CHEMBL492677 hrh4_human Human No 7.2 EC50 = 64.6 nM Funct
Agonist activity at human histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at human histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
298 4 2 6 1.4 CN1CCN(CC1)C2=NC(=NC(=C2)NCC3=CC=CC=C3)N
CHEMBL4518374 hrh4_rat Rat No 6.2 EC50 = 645.7 nM Bind
Agonist activity at rat H4R expressed in HEK293T-beta-arr2-rH4R cells by beta-arrestin2 recruitment assayAgonist activity at rat H4R expressed in HEK293T-beta-arr2-rH4R cells by beta-arrestin2 recruitment assay
263 3 2 5 1.7 CC(C)(C)CNc1nccc(N2CCCNCC2)n1
CHEMBL4596491 hrh4_rat Rat No 6.2 EC50 = 645.7 nM Bind
Agonist activity at rat H4R expressed in HEK293T-beta-arr2-rH4R cells by beta-arrestin2 recruitment assayAgonist activity at rat H4R expressed in HEK293T-beta-arr2-rH4R cells by beta-arrestin2 recruitment assay
263 3 2 5 1.7 CC(C)(C)CNc1nccc(N2CCCNCC2)n1
CHEMBL446896 hrh4_rat Rat Yes 7.2 EC50 = 66.1 nM Funct
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
207 1 1 5 0.1 Cc1cnc(N)nc1N1CCN(C)CC1
CHEMBL472441 hrh4_human Human No 7.2 EC50 = 66.3 nM Bind
Activity at human recombinant histamine H4 receptor-RGS4 fusion protein expressed in Sf9 cells coexpressing Galphai2 and G-beta-1-gamma-2 by steady-state GTPase activity assayActivity at human recombinant histamine H4 receptor-RGS4 fusion protein expressed in Sf9 cells coexpressing Galphai2 and G-beta-1-gamma-2 by steady-state GTPase activity assay
382 8 4 5 2.7 N=C(NCCCc1c[nH]cn1)NC(=O)CC(c1ccccc1)c1nccs1
CHEMBL492631 hrh4_rat Rat No 7.2 EC50 = 67.6 nM Funct
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
249 1 1 5 1.1 CN1CCN(c2cc(C(C)(C)C)nc(N)n2)CC1
CHEMBL4077914 hrh4_human Human No 5.2 EC50 = 6750 nM Bind
Agonist activity at human H4 receptor expressed in CHO cell membranes co-expressing Galphai2 by GTPgamma[35S] binding assayAgonist activity at human H4 receptor expressed in CHO cell membranes co-expressing Galphai2 by GTPgamma[35S] binding assay
335 6 2 4 3.6 COc1ccc(/C(=N/[C@H](C)Cc2cnc[nH]2)c2ccccc2)c(O)c1
CHEMBL90 hrh4_mouse Mouse Yes 5.2 EC50 = 6760.8 nM Funct
Agonist activity at mouse H4R by [35S]-GTPgammaS-binding assayAgonist activity at mouse H4R by [35S]-GTPgammaS-binding assay
111 2 2 2 -0.1 NCCc1cnc[nH]1
CHEMBL505061 hrh4_rat Rat No 7.2 EC50 = 69.2 nM Funct
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
262 2 1 6 0.4 CN1CCN(c2cc(N3CCCC3)nc(N)n2)CC1
CHEMBL514641 hrh4_human Human No 8.2 EC50 = 7.1 nM Bind
Agonist activity at human H4 receptor expressed in insect Sf9 cells co-expressing RGS19 fusion protein and Gialpha2, Gbeta1gamma2 assessed as gamma[32P]GTP binding by liquid scintillation countingAgonist activity at human H4 receptor expressed in insect Sf9 cells co-expressing RGS19 fusion protein and Gialpha2, Gbeta1gamma2 assessed as gamma[32P]GTP binding by liquid scintillation counting
338 7 4 2 1.9 N/C(=N\C(=O)CCc1c[nH]c2ccccc12)NCCCc1c[nH]cn1
CHEMBL3236553 hrh4_mouse Mouse Yes 8.1 EC50 = 7.3 nM Bind
Partial agonist activity at mouse histamine H4 receptorPartial agonist activity at mouse histamine H4 receptor
247 2 2 5 1.1 Nc1nc(C2CCCC2)cc(N2CCNCC2)n1
CHEMBL90 hrh4_human Human Yes 8.1 EC50 = 7.4 nM Funct
Agonist activity at human H4R by [35S]-GTPgammaS-binding assayAgonist activity at human H4R by [35S]-GTPgammaS-binding assay
111 2 2 2 -0.1 NCCc1cnc[nH]1
CHEMBL471413 hrh4_human Human No 8.1 EC50 = 7.9 nM Funct
Agonist activity at human recombinant histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2 by steady-state GTPase activity assayAgonist activity at human recombinant histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2 by steady-state GTPase activity assay
375 8 4 3 3.2 N=C(NCCCc1c[nH]cn1)NC(=O)CC(c1ccccc1)c1ccccc1
CHEMBL90 hrh4_human Human Yes 8.1 EC50 = 7.9 nM Funct
Antagonist activity at human histamine 4 receptor expressed in Sf9 cell membranes co-expressing Galphai2 and Gbeta1gamma2 assessed as [35S]GTPgammaS binding by scintillation countingAntagonist activity at human histamine 4 receptor expressed in Sf9 cell membranes co-expressing Galphai2 and Gbeta1gamma2 assessed as [35S]GTPgammaS binding by scintillation counting
111 2 2 2 -0.1 NCCc1cnc[nH]1
CHEMBL260374 hrh4_human Human Yes 7.2 EC50 = 70.8 nM Funct
Agonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of [35S]GTPgammaS binding
292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1
CHEMBL275443 hrh4_human Human Yes 7.2 EC50 = 70.8 nM Funct
Agonist activity at human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19 protein by steady-state GTPase assayAgonist activity at human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19 protein by steady-state GTPase assay
125 2 2 2 0.2 Cc1c(CCN)nc[nH]1
CHEMBL260374 hrh4_human Human Yes 7.2 EC50 = 70.8 nM Funct
Inverse agonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of [35S]GTPgammaS bindingInverse agonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of [35S]GTPgammaS binding
292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1
CHEMBL1077756 hrh4_human Human Yes 6.2 EC50 = 708.0 nM Funct
Agonist activity at human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19 protein by steady-state GTPase assayAgonist activity at human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19 protein by steady-state GTPase assay
234 6 3 3 0.8 CCN/C(=N\C#N)NCCCCc1c[nH]cn1
CHEMBL13795 hrh4_human Human Yes 5.2 EC50 = 7079.5 nM Bind
Inhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H4 receptorInhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H4 receptor
123 1 2 2 0.2 N[C@H]1C[C@@H]1c1c[nH]cn1
CHEMBL1086085 hrh4_human Human No 6.2 EC50 = 710 nM Funct
Agonist activity at human histamine H4 receptor in SK-N-MC cells assessed as forskolin-stimulated cAMP release preincubated for 10 mins before forskolin challengeAgonist activity at human histamine H4 receptor in SK-N-MC cells assessed as forskolin-stimulated cAMP release preincubated for 10 mins before forskolin challenge
394 6 1 4 3.8 Cc1cc(OCCCN2C3CN(C)CC32)ccc1-c1nc2c(C)c(F)ccc2[nH]1
CHEMBL4642520 hrh4_human Human No 7.1 EC50 = 72.4 nM Funct
Agonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
415 10 1 2 5.5 Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCCCCc1c[nH]cn1
CHEMBL4650832 hrh4_human Human No 7.1 EC50 = 72.4 nM Funct
Agonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
415 10 1 2 5.5 Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCCCCc1c[nH]cn1
CHEMBL129198 hrh4_rat Rat Yes 6.1 EC50 = 741.3 nM Funct
Agonist activity at rat H4R by [35S]-GTPgammaS-binding assayAgonist activity at rat H4R by [35S]-GTPgammaS-binding assay
277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl
CHEMBL105803 hrh4_human Human No 6.1 EC50 = 741.3 nM Funct
Inhibition of the forskolin-stimulated cAMP production in SK-N-MC cells expressing human Histamine H4 receptorInhibition of the forskolin-stimulated cAMP production in SK-N-MC cells expressing human Histamine H4 receptor
258 5 1 3 2.8 c1ccc(COC[C@H]2CC[C@H](c3c[nH]cn3)O2)cc1
CHEMBL153061 hrh4_human Human Yes 6.1 EC50 = 741.3 nM Bind
Inhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H4 receptorInhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H4 receptor
151 2 2 2 0.6 c1nc(CC2CCNC2)c[nH]1
CHEMBL3393543 hrh4_human Human Yes 7.1 EC50 = 75 nM Funct
Agonist activity at human recombinant histamine H4 receptor expressed in SK-N-MC cells assessed as effect on forskolin-stimulated cAMP-mediated reporter gene activityAgonist activity at human recombinant histamine H4 receptor expressed in SK-N-MC cells assessed as effect on forskolin-stimulated cAMP-mediated reporter gene activity
261 3 1 5 1.6 CN1CCN(c2ccnc(NC3CCCC3)n2)CC1
CHEMBL90 hrh4_human Human Yes 7.1 EC50 = 75 nM Bind
Inhibition of human Histamine H4 receptorInhibition of human Histamine H4 receptor
111 2 2 2 -0.1 NCCc1cnc[nH]1
CHEMBL1078210 hrh4_human Human No 6.1 EC50 = 758.6 nM Funct
Agonist activity at human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19 protein by steady-state GTPase assayAgonist activity at human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19 protein by steady-state GTPase assay
310 8 3 3 2.0 N#C/N=C(\NCCCc1ccccc1)NCCCc1c[nH]cn1
CHEMBL106913 hrh4_human Human No 5.1 EC50 = 7585.8 nM Funct
Inhibition of the forskolin-stimulated cAMP production in SK-N-MC cells expressing human Histamine H4 receptorInhibition of the forskolin-stimulated cAMP production in SK-N-MC cells expressing human Histamine H4 receptor
167 2 2 3 0.6 NC[C@H]1CC[C@@H](c2c[nH]cn2)O1
CHEMBL108649 hrh4_human Human No 5.1 EC50 = 7585.8 nM Funct
Inhibition of the forskolin-stimulated cAMP production in SK-N-MC cells expressing human Histamine H4 receptorInhibition of the forskolin-stimulated cAMP production in SK-N-MC cells expressing human Histamine H4 receptor
248 3 3 4 0.3 C/N=C(\NC#N)NC[C@H]1CC[C@@H](c2c[nH]cn2)O1
CHEMBL107877 hrh4_human Human No 4.1 EC50 = 75857.8 nM Funct
Inhibition of the forskolin-stimulated cAMP production in SK-N-MC cells expressing human Histamine H4 receptorInhibition of the forskolin-stimulated cAMP production in SK-N-MC cells expressing human Histamine H4 receptor
165 2 2 3 0.4 NC[C@H]1C=C[C@@H](c2c[nH]cn2)O1
CHEMBL321860 hrh4_human Human Yes 7.1 EC50 = 77.6 nM Funct
Inhibition of the forskolin-stimulated cAMP production in SK-N-MC cells expressing human Histamine H4 receptorInhibition of the forskolin-stimulated cAMP production in SK-N-MC cells expressing human Histamine H4 receptor
248 3 3 4 0.3 C/N=C(\NC#N)NC[C@H]1CC[C@H](c2c[nH]cn2)O1
CHEMBL3220630 hrh4_human Human No 6.1 EC50 = 776.3 nM Bind
Agonist activity at human recombinant histamine H4 receptor-RGS19 fusion protein expressed in Sf9 cells coexpressing Galphai2,Gbeta1gamma2 preincubated for 2 mins before [gamma32P]GTP addition measured after 20 mins by steady-state GTPase activity assayAgonist activity at human recombinant histamine H4 receptor-RGS19 fusion protein expressed in Sf9 cells coexpressing Galphai2,Gbeta1gamma2 preincubated for 2 mins before [gamma32P]GTP addition measured after 20 mins by steady-state GTPase activity assay
319 7 3 3 2.0 CC(CC(=O)/N=C(\N)NCCCc1ncc[nH]1)c1cccs1
CHEMBL25725 hrh4_human Human Yes 5.1 EC50 = 7780 nM Bind
Agonist activity at human H4 receptor expressed in CHO cell membranes co-expressing Galphai2 by GTPgamma[35S] binding assayAgonist activity at human H4 receptor expressed in CHO cell membranes co-expressing Galphai2 by GTPgamma[35S] binding assay
414 7 2 5 3.3 COc1ccc2c(c1)c(CC(=O)NCCCO)c(C)n2C(=O)c1ccc(Cl)cc1
CHEMBL321860 hrh4_human Human Yes 7.1 EC50 = 78 nM Funct
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-stimulated cAMP production incubated for 6 hrs by CRE/beta-galactosidase reporter gene assayAgonist activity at human histamine H4 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-stimulated cAMP production incubated for 6 hrs 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
CHEMBL2165640 hrh4_human Human No 7.1 EC50 = 79.4 nM Funct
Agonist activity at human H4R-RGS19 Galphai2 Gbeta1gamma2 expressed in Sf9 cells at 0.1 nM to 1 mM by steady state GTPase activity assayAgonist activity at human H4R-RGS19 Galphai2 Gbeta1gamma2 expressed in Sf9 cells at 0.1 nM to 1 mM by steady state GTPase activity assay
444 13 6 4 0.1 N/C(=N\C(=O)CCCCC(=O)/N=C(\N)NCCCc1c[nH]cn1)NCCCc1c[nH]cn1
CHEMBL321860 hrh4_human Human Yes 7.1 EC50 = 79.4 nM Funct
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H4 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
CHEMBL72431 hrh4_human Human No 7.1 EC50 = 79.4 nM Funct
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
288 7 3 2 2.4 S=C(NCCCCc1c[nH]cn1)NCc1ccccc1
CHEMBL90 hrh4_human Human Yes 7.1 EC50 = 79.4 nM Funct
Agonist activity at human recombinant histamine H4 receptor expressed in human SK-N-MC cells co-expressing SRE-Luc by luciferase reporter gene assayAgonist activity at human recombinant histamine H4 receptor expressed in human SK-N-MC cells co-expressing SRE-Luc by luciferase reporter gene assay
111 2 2 2 -0.1 NCCc1cnc[nH]1
CHEMBL1632414 hrh4_human Human No 7.1 EC50 = 79.4 nM Funct
Agonist activity at human recombinant histamine H4 receptor expressed in human SK-N-MC cells co-expressing SRE-Luc by luciferase reporter gene assayAgonist activity at human recombinant histamine H4 receptor expressed in human SK-N-MC cells co-expressing SRE-Luc by luciferase reporter gene assay
292 2 2 4 2.7 CN1CCC(/C(=N/O)c2nc3cc(Cl)ccc3[nH]2)CC1
CHEMBL260374 hrh4_human Human Yes 7.1 EC50 = 79.4 nM Funct
Inverse agonist activity at human histamine H4 receptor expressed in HEK293 cells assessed by forskolin induced cAMP response element activation by luciferase reporter gene assayInverse agonist activity at human histamine H4 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
CHEMBL268490 hrh4_human Human Yes 6.1 EC50 = 794.3 nM Funct
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
125 3 2 2 0.2 CNCCc1cnc[nH]1
CHEMBL105803 hrh4_human Human No 6.1 EC50 = 794.3 nM Funct
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H4 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
CHEMBL129198 hrh4_mouse Mouse Yes 6.1 EC50 = 794.3 nM Funct
Agonist activity at mouse H4R by [35S]-GTPgammaS-binding assayAgonist activity at mouse H4R by [35S]-GTPgammaS-binding assay
277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl
CHEMBL475621 hrh4_mouse Mouse No 6.1 EC50 = 794.3 nM Funct
Agonist activity at mouse H4R by [35S]-GTPgammaS-binding assayAgonist activity at mouse H4R by [35S]-GTPgammaS-binding assay
223 5 3 2 0.2 CCC(=O)/N=C(\N)NCCCc1c[nH]cn1
CHEMBL106913 hrh4_human Human No 5.1 EC50 = 7943.3 nM Funct
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H4 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
CHEMBL108649 hrh4_human Human No 5.1 EC50 = 7943.3 nM Funct
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H4 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
CHEMBL4439142 hrh4_mouse Mouse No 5.1 EC50 = 7943.3 nM Funct
Agonist activity at mouse H4R expressed in Sf9 cells by [35S]-GTPgammaS-binding assayAgonist activity at mouse H4R expressed in Sf9 cells by [35S]-GTPgammaS-binding assay
277 4 1 5 2.1 CN(C)[C@@H]1CCN(c2ccnc(NCC(C)(C)C)n2)C1
CHEMBL4515149 hrh4_mouse Mouse No 5.1 EC50 = 7943.3 nM Funct
Agonist activity at mouse H4R expressed in Sf9 cells by [35S]-GTPgammaS-binding assayAgonist activity at mouse H4R expressed in Sf9 cells by [35S]-GTPgammaS-binding assay
277 4 1 5 2.1 CN(C)[C@@H]1CCN(c2ccnc(NCC(C)(C)C)n2)C1
CHEMBL4595327 hrh4_mouse Mouse No 5.1 EC50 = 7943.3 nM Funct
Agonist activity at mouse H4R expressed in Sf9 cells by [35S]-GTPgammaS-binding assayAgonist activity at mouse H4R expressed in Sf9 cells by [35S]-GTPgammaS-binding assay
277 4 1 5 2.1 CN(C)[C@@H]1CCN(c2ccnc(NCC(C)(C)C)n2)C1
CHEMBL448085 hrh4_rat Rat Yes 5.1 EC50 = 7943.3 nM Funct
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
259 2 1 7 -0.0 CN1CCN(c2cc(-n3ccnc3)nc(N)n2)CC1
CHEMBL493261 hrh4_rat Rat Yes 5.1 EC50 = 7943.3 nM Funct
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
249 1 1 5 1.1 CN1CCN(c2nc(N)cc(C(C)(C)C)n2)CC1
CHEMBL505346 hrh4_rat Rat Yes 5.1 EC50 = 7943.3 nM Funct
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
271 2 1 7 0.3 CN1CCN(c2cc(-c3cncnc3)nc(N)n2)CC1
CHEMBL325327 hrh4_human Human Yes 8.1 EC50 = 8.1 nM Bind
Agonist activity at human H4 receptor expressed in insect Sf9 cells co-expressing RGS19 fusion protein and Gialpha2, Gbeta1gamma2 assessed as gamma[32P]GTP binding by liquid scintillation countingAgonist activity at human H4 receptor expressed in insect Sf9 cells co-expressing RGS19 fusion protein and Gialpha2, Gbeta1gamma2 assessed as gamma[32P]GTP binding by liquid scintillation counting
167 4 4 2 -0.2 N=C(N)NCCCc1c[nH]cn1
CHEMBL1096430 hrh4_human Human No 8.1 EC50 = 8.3 nM Bind
Activity at human recombinant GAIP-fused histamine H4 receptor expressed in Sf9 cells coexpressing Galphai, Gbeta1gamma2 by steady-state GTPase activity assayActivity at human recombinant GAIP-fused histamine H4 receptor expressed in Sf9 cells coexpressing Galphai, Gbeta1gamma2 by steady-state GTPase activity assay
319 7 4 3 2.6 C[C@H](CC(=O)NC(=N)NCCCc1c[nH]cn1)C1CCCCC1
CHEMBL2165628 hrh4_human Human No 8.1 EC50 = 8.5 nM Funct
Agonist activity at human H4R-RGS19 Galphai2 Gbeta1gamma2 expressed in Sf9 cells at 0.1 nM to 1 mM by steady state GTPase activity assayAgonist activity at human H4R-RGS19 Galphai2 Gbeta1gamma2 expressed in Sf9 cells at 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
CHEMBL2165642 hrh4_human Human No 8.1 EC50 = 8.5 nM Funct
Agonist activity at human H4R-RGS19 Galphai2 Gbeta1gamma2 expressed in Sf9 cells at 0.1 nM to 1 mM by steady state GTPase activity assayAgonist activity at human H4R-RGS19 Galphai2 Gbeta1gamma2 expressed in Sf9 cells at 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
CHEMBL594731 hrh4_human Human No 8.1 EC50 = 8.5 nM Funct
Agonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of [35S]GTPgammaS binding
312 4 2 6 1.7 Cc1ccccc1CNc1cc(N2CCN(C)CC2)nc(N)n1
CHEMBL471413 hrh4_human Human No 8.1 EC50 = 8.6 nM Bind
Activity at human recombinant histamine H4 receptor-RGS4 fusion protein expressed in Sf9 cells coexpressing Galphai2 and G-beta-1-gamma-2 by steady-state GTPase activity assayActivity at human recombinant histamine H4 receptor-RGS4 fusion protein expressed in Sf9 cells coexpressing Galphai2 and G-beta-1-gamma-2 by steady-state GTPase activity assay
375 8 4 3 3.2 N=C(NCCCc1c[nH]cn1)NC(=O)CC(c1ccccc1)c1ccccc1
CHEMBL379102 hrh4_human Human No 7.1 EC50 = 81.3 nM Funct
Activity at human histamine H4 receptor transfected in SK-N-MC cells by cAMP assayActivity at human histamine H4 receptor transfected in SK-N-MC cells by cAMP assay
345 0 0 4 3.9 CN1CCN(C2=Nc3cc(Cl)ccc3Oc3ccc(F)cc32)CC1
CHEMBL4543119 hrh4_mouse Mouse No 6.1 EC50 = 831.8 nM Bind
Agonist activity at mouse H4R expressed in HEK293T-beta-arr2-mH4R cells by beta-arrestin2 recruitment assayAgonist activity at mouse H4R expressed in HEK293T-beta-arr2-mH4R cells by beta-arrestin2 recruitment assay
277 3 1 5 2.1 CN1CCCN(c2ccnc(NCC(C)(C)C)n2)CC1
CHEMBL4596606 hrh4_mouse Mouse No 6.1 EC50 = 831.8 nM Bind
Agonist activity at mouse H4R expressed in HEK293T-beta-arr2-mH4R cells by beta-arrestin2 recruitment assayAgonist activity at mouse H4R expressed in HEK293T-beta-arr2-mH4R cells by beta-arrestin2 recruitment assay
277 3 1 5 2.1 CN1CCCN(c2ccnc(NCC(C)(C)C)n2)CC1
CHEMBL451108 hrh4_rat Rat No 5.1 EC50 = 8317.6 nM Funct
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
269 2 1 5 1.5 CN1CCN(c2nc(N)ncc2-c2ccccc2)CC1
CHEMBL3393538 hrh4_human Human Yes 7.1 EC50 = 84 nM Funct
Agonist activity at human recombinant histamine H4 receptor expressed in SK-N-MC cells assessed as effect on forskolin-stimulated cAMP-mediated reporter gene activityAgonist activity at human recombinant histamine H4 receptor expressed in SK-N-MC cells assessed as effect on forskolin-stimulated cAMP-mediated reporter gene activity
249 4 1 5 1.3 CC(C)CNc1nccc(N2CCN(C)CC2)n1
CHEMBL14690 hrh4_mouse Mouse Yes 6.1 EC50 = 851.1 nM Funct
Agonist activity at mouse H4R by [35S]-GTPgammaS-binding assayAgonist activity at mouse H4R by [35S]-GTPgammaS-binding assay
308 6 2 3 3.2 Clc1ccc(cc1)CN=C(SCCCc1cnc[nH]1)N
CHEMBL319658 hrh4_human Human Yes 4.1 EC50 = 85113.8 nM Funct
Inhibition of the forskolin-stimulated cAMP production in SK-N-MC cells expressing human Histamine H4 receptorInhibition of the forskolin-stimulated cAMP production in SK-N-MC cells expressing human Histamine H4 receptor
165 2 2 3 0.4 NC[C@@H]1C=C[C@@H](c2c[nH]cn2)O1
CHEMBL1770985 hrh4_human Human No 7.1 EC50 = 86 nM Funct
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells assessed as effect on forskolin-induced cAMP accumulation after 6 hrsAgonist activity at human histamine H4 receptor expressed in human SK-N-MC cells assessed as effect on forskolin-induced cAMP accumulation after 6 hrs
264 4 2 6 0.9 CC(C)CNc1nc(N)cc(N2CCN(C)CC2)n1
CHEMBL3393544 hrh4_human Human No 7.1 EC50 = 86 nM Funct
Agonist activity at human recombinant histamine H4 receptor expressed in SK-N-MC cells assessed as effect on forskolin-stimulated cAMP-mediated reporter gene activityAgonist activity at human recombinant histamine H4 receptor expressed in SK-N-MC cells assessed as effect on forskolin-stimulated cAMP-mediated reporter gene activity
261 4 2 5 1.6 CN[C@@H]1CCN(c2ccnc(NC3CCCC3)n2)C1
CHEMBL90 hrh4_mouse Mouse Yes 7.1 EC50 = 87.1 nM Funct
Agonist activity at mouse H4R expressed in HEK293-SF-mH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at mouse H4R expressed in HEK293-SF-mH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
111 2 2 2 -0.1 NCCc1cnc[nH]1
CHEMBL1196470 hrh4_mouse Mouse Yes 5.1 EC50 = 8709.6 nM Funct
Agonist activity at mouse H4R by [35S]-GTPgammaS-binding assayAgonist activity at mouse H4R by [35S]-GTPgammaS-binding assay
161 3 4 3 -1.1 NC(=N)SCCN=C(N)N
CHEMBL495265 hrh4_rat Rat No 5.1 EC50 = 8709.6 nM Funct
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
268 1 0 4 2.2 CN1CCN(c2cc(C(C)(C)C)nc(Cl)n2)CC1
CHEMBL4445423 hrh4_human Human No 7.1 EC50 = 89.1 nM Bind
Agonist activity at human H4R expressed in HEK293T-beta-arr2-hH4R cells by beta-arrestin2 recruitment assayAgonist activity at human H4R expressed in HEK293T-beta-arr2-hH4R cells by beta-arrestin2 recruitment assay
291 4 4 5 1.0 CC(C)(C)CNc1nccc(N2CC[C@@H](NC(=N)N)C2)n1
CHEMBL4598198 hrh4_human Human No 7.1 EC50 = 89.1 nM Bind
Agonist activity at human H4R expressed in HEK293T-beta-arr2-hH4R cells by beta-arrestin2 recruitment assayAgonist activity at human H4R expressed in HEK293T-beta-arr2-hH4R cells by beta-arrestin2 recruitment assay
291 4 4 5 1.0 CC(C)(C)CNc1nccc(N2CC[C@@H](NC(=N)N)C2)n1
CHEMBL260374 hrh4_human Human Yes 7.1 EC50 = 89.1 nM Funct
Agonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of GTPase by [gamma-32P]GTP spontaneous degradation assayAgonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of GTPase by [gamma-32P]GTP spontaneous degradation assay
292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1
CHEMBL90019 hrh4_human Human Yes 7.1 EC50 = 89.1 nM Bind
Inhibition of the cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H4 receptorInhibition of the cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H4 receptor
139 4 2 2 0.7 NCCCCc1cnc[nH]1
CHEMBL90019 hrh4_human Human Yes 7.1 EC50 = 89.1 nM Bind
Inhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H4 receptorInhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H4 receptor
139 4 2 2 0.7 NCCCCc1cnc[nH]1
CHEMBL442865 hrh4_rat Rat No 6.1 EC50 = 891.3 nM Funct
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
395 2 1 5 2.1 CN1CCN(c2cc(-c3cccc(I)c3)nc(N)n2)CC1
CHEMBL492652 hrh4_rat Rat No 5.1 EC50 = 8912.5 nM Funct
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
301 3 1 6 2.0 CN1CCN(c2cc(Sc3ccccc3)nc(N)n2)CC1
CHEMBL90 hrh4_human Human Yes 8.0 EC50 = 9.1 nM Bind
Activity at human recombinant GAIP-fused histamine H4 receptor expressed in Sf9 cells coexpressing Galphai, Gbeta1gamma2 by steady-state GTPase activity assayActivity at human recombinant GAIP-fused histamine H4 receptor expressed in Sf9 cells coexpressing Galphai, Gbeta1gamma2 by steady-state GTPase activity assay
111 2 2 2 -0.1 NCCc1cnc[nH]1
CHEMBL522673 hrh4_mouse Mouse No 8.0 EC50 = 9.1 nM Funct
Antagonist activity at mouse histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assayAntagonist activity at mouse histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assay
295 2 2 5 1.6 CNC1CN(c2nc(N)nc3c2CCCc2ccccc2-3)C1
CHEMBL522673 hrh4_rat Rat No 8.0 EC50 = 9.3 nM Funct
Antagonist activity at rat histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assayAntagonist activity at rat histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assay
295 2 2 5 1.6 CNC1CN(c2nc(N)nc3c2CCCc2ccccc2-3)C1
CHEMBL3393541 hrh4_human Human Yes 7.0 EC50 = 91 nM Funct
Agonist activity at human recombinant histamine H4 receptor expressed in SK-N-MC cells assessed as effect on forskolin-stimulated cAMP-mediated reporter gene activityAgonist activity at human recombinant histamine H4 receptor expressed in SK-N-MC cells assessed as effect on forskolin-stimulated cAMP-mediated reporter gene activity
249 5 1 5 1.4 CCCCNc1nccc(N2CCN(C)CC2)n1
CHEMBL593103 hrh4_human Human No 7.0 EC50 = 91.2 nM Funct
Agonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of GTPase by [gamma-32P]GTP spontaneous degradation assayAgonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of GTPase by [gamma-32P]GTP spontaneous degradation assay
316 4 2 6 1.6 CN1CCN(c2cc(NCc3ccc(F)cc3)nc(N)n2)CC1
CHEMBL3752085 hrh4_human Human Yes 6.0 EC50 = 912.0 nM Funct
Antagonist activity at human histamine 4 receptor expressed in Sf9 cell membranes co-expressing Galphai2 and Gbeta1gamma2 assessed as [35S]GTPgammaS binding by scintillation countingAntagonist activity at human histamine 4 receptor expressed in Sf9 cell membranes co-expressing Galphai2 and Gbeta1gamma2 assessed as [35S]GTPgammaS binding by scintillation counting
359 5 1 5 3.5 CN1CCN(c2cc(-c3ccccc3)nc(NCc3ccccc3)n2)CC1
CHEMBL82298 hrh4_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 H4 receptorInhibition of the cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H4 receptor
159 2 1 2 1.4 n1ccc(cc1)Cc1c[nH]cn1
CHEMBL4518374 hrh4_rat Rat No 7.0 EC50 = 93.3 nM Funct
Agonist activity at rat H4R expressed in HEK293-SF-rH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at rat H4R expressed in HEK293-SF-rH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
263 3 2 5 1.7 CC(C)(C)CNc1nccc(N2CCCNCC2)n1
CHEMBL4596491 hrh4_rat Rat No 7.0 EC50 = 93.3 nM Funct
Agonist activity at rat H4R expressed in HEK293-SF-rH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at rat H4R expressed in HEK293-SF-rH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
263 3 2 5 1.7 CC(C)(C)CNc1nccc(N2CCCNCC2)n1
CHEMBL507063 hrh4_rat Rat Yes 7.0 EC50 = 93.3 nM Funct
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
300 3 1 7 0.9 COc1ncccc1-c1cc(N2CCN(C)CC2)nc(N)n1
CHEMBL495342 hrh4_rat Rat No 6.0 EC50 = 933.3 nM Funct
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
234 1 0 4 1.5 CN1CCN(c2cc(C(C)(C)C)ncn2)CC1
CHEMBL3752270 hrh4_human Human No 6.0 EC50 = 933.3 nM Funct
Antagonist activity at human histamine 4 receptor expressed in Sf9 cell membranes co-expressing Galphai2 and Gbeta1gamma2 assessed as [35S]GTPgammaS binding by scintillation countingAntagonist activity at human histamine 4 receptor expressed in Sf9 cell membranes co-expressing Galphai2 and Gbeta1gamma2 assessed as [35S]GTPgammaS binding by scintillation counting
385 4 1 5 3.6 CN1CCN(c2nc(NCc3ccccc3)nc3c2CCc2ccccc2-3)CC1
CHEMBL90 hrh4_mouse Mouse Yes 7.0 EC50 = 94 nM Bind
Agonist activity at mouse SF-His6-tagged histamine H4 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated response incubated for 5 hrs by luciferase reporter gene assayAgonist activity at mouse SF-His6-tagged histamine H4 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated response incubated for 5 hrs by luciferase reporter gene assay
111 2 2 2 -0.1 NCCc1cnc[nH]1
CHEMBL1077862 hrh4_human Human Yes 6.0 EC50 = 955.0 nM Funct
Agonist activity at human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19 protein by steady-state GTPase assayAgonist activity at human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19 protein by steady-state GTPase assay
220 5 3 3 0.4 CN/C(=N\C#N)NCCCCc1c[nH]cn1
CHEMBL493100 hrh4_rat Rat No 5.0 EC50 = 9772.4 nM Funct
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
265 5 1 5 1.7 CN(C)CCCN(C)c1cc(C(C)(C)C)nc(N)n1
CHEMBL1915540 hrh4_human Human Yes 9.2 IC50 = 0.7 nM Funct
Antagonist activity at H4R in human eosinophils assessed as inhibition of histamine-induced shape change by GAFS assayAntagonist activity at H4R in human eosinophils assessed as inhibition of histamine-induced shape change by GAFS assay
262 5 3 6 0.7 CN[C@@H]1CCN(C1)c1cc(NCC2CC2)nc(n1)N
CHEMBL1091874 hrh4_human Human No 9.0 IC50 = 1 nM Bind
Displacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assayDisplacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assay
317 2 2 6 2.4 CN[C@@H]1CCN(c2nc(N)nc3c2oc2ccc(Cl)cc23)C1
CHEMBL1915540 hrh4_human Human Yes 8.9 IC50 = 1.3 nM Funct
Antagonist activity at H4R in human eosinophils assessed as inhibition of histamine-induced actin polymerisationAntagonist activity at H4R in human eosinophils assessed as inhibition of histamine-induced actin polymerisation
262 5 3 6 0.7 CN[C@@H]1CCN(C1)c1cc(NCC2CC2)nc(n1)N
CHEMBL4635634 hrh4_human Human No 8.8 IC50 = 1.7 nM Funct
Inverse agonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells assessed as reduction in histamine-induced inhibition of forskolin stimulated luciferase activity by luciferase reporter gene assayInverse agonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells assessed as reduction in histamine-induced inhibition of forskolin stimulated luciferase activity 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 hrh4_human Human No 8.8 IC50 = 1.7 nM Funct
Inverse agonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells assessed as reduction in histamine-induced inhibition of forskolin stimulated luciferase activity by luciferase reporter gene assayInverse agonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells assessed as reduction in histamine-induced inhibition of forskolin stimulated luciferase activity 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
CHEMBL591969 hrh4_human Human No 8.0 IC50 = 10 nM Funct
Inverse agonist activity at human histamine H4 receptor expressed in HEK293T cells by CRE-beta-galactosidase assayInverse agonist activity at human histamine H4 receptor expressed in HEK293T cells by CRE-beta-galactosidase assay
384 5 2 7 0.7 CN1CCN(CC1)C2=NC3=C(C=C(C=C3)Cl)C(=N2)NCCS(=O)(=O)N
CHEMBL1093438 hrh4_human Human No 6.0 IC50 = 1000 nM Bind
Displacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assayDisplacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assay
318 1 1 6 2.5 CN1CCN(c2nc(O)nc3c2oc2ccc(Cl)cc23)CC1
CHEMBL1767164 hrh4_human Human Yes 5.0 IC50 = 10000 nM Bind
Binding affinity to human histamine H4 receptorBinding affinity to human histamine H4 receptor
640 14 0 6 7.8 O=c1c2ccccc2c(Cc2ccc(Cl)cc2)nn1C[C@H]1CCCN1CCCCc1ccc(OCCCN2CCCCCC2)cc1
CHEMBL1092331 hrh4_human Human No 5.0 IC50 = 10000 nM Bind
Displacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assayDisplacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assay
330 1 0 5 3.6 CC1CN(c2ncnc3c2oc2ccc(Cl)cc23)CC(C)N1C
CHEMBL1935574 hrh4_human Human No 7.0 IC50 = 106 nM Funct
Antagonist activity at human H4 receptor expressed in HEK293T cells assessed as inhibition of histamine-induced [35S]GTPgammaS bindingAntagonist activity at human H4 receptor expressed in HEK293T cells assessed as inhibition of histamine-induced [35S]GTPgammaS binding
295 2 2 6 1.9 Nc1nc(N2CCNCC2)c2ccc(-c3ccco3)cc2n1
CHEMBL213886 hrh4_human Human No 7.0 IC50 = 110 nM Funct
Antagonist activity at human H4 receptor expressed in 293-EBNA cells assessed as inhibition of histamine agonist activity by luciferase reporter gene assayAntagonist activity at human H4 receptor expressed in 293-EBNA cells assessed as inhibition of histamine agonist activity by luciferase reporter gene assay
275 6 2 2 3.3 Clc1ccc(CNCC[C@@H]2C[C@H]2c2c[nH]cn2)cc1
CHEMBL4794724 hrh4_human Human No 6.0 IC50 = 1100 nM Bind
Displacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting methodDisplacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting method
289 2 1 7 0.7 CNC1CN(c2nc3ncc(Cl)cc3c3ncnn23)C1
CHEMBL4115693 hrh4_human Human No 6.0 IC50 = 1100 nM Bind
Histamine H-4 Receptor Binding Assay: Histamine H-4 Receptor Binding AssayHistamine H-4 Receptor Binding Assay: Histamine H-4 Receptor Binding Assay
297 0 2 3 3.5 O[C@@H]1Cc2ccccc2C(=C2CCNCC2)c2ccsc21
CHEMBL657 hrh4_human Human Yes 5.0 IC50 = 11000 nM Bind
Histamine H-4 Receptor Binding Assay: Histamine H-4 Receptor Binding AssayHistamine H-4 Receptor Binding Assay: Histamine H-4 Receptor Binding Assay
255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C
CHEMBL1092332 hrh4_human Human No 7.0 IC50 = 111 nM Bind
Displacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assayDisplacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assay
314 1 0 5 2.9 CN1C[C@@H]2C[C@H]1CN2c1ncnc2c1oc1ccc(Cl)cc12
CHEMBL2376800 hrh4_human Human No 7.0 IC50 = 112.2 nM Funct
Antagonist activity at human histamine H4 receptor expressed in HEK cells assessed as inhibition of histamine-induced [35S]GTPgammaS bindingAntagonist activity at human histamine H4 receptor expressed in HEK cells assessed as inhibition of histamine-induced [35S]GTPgammaS binding
258 3 2 6 0.6 CCc1cnc2c(N3CC(NC)C3)nc(N)nc2c1
CHEMBL4782441 hrh4_human Human No 5.9 IC50 = 1200 nM Bind
Displacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting methodDisplacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting method
303 2 0 7 1.1 CN(C)C1CN(c2nc3ncc(Cl)cc3n3cnnc23)C1
CHEMBL2376801 hrh4_human Human No 6.9 IC50 = 125.9 nM Funct
Antagonist activity at human histamine H4 receptor expressed in HEK cells assessed as inhibition of histamine-induced [35S]GTPgammaS bindingAntagonist activity at human histamine H4 receptor expressed in HEK cells assessed as inhibition of histamine-induced [35S]GTPgammaS binding
272 3 2 6 1.0 CCc1cnc2c(N3CC[C@@H](NC)C3)nc(N)nc2c1
CHEMBL1090532 hrh4_human Human No 6.9 IC50 = 126 nM Bind
Displacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assayDisplacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assay
288 1 1 5 2.6 NC1CCN(c2ncnc3c2oc2ccc(Cl)cc23)C1
CHEMBL129198 hrh4_human Human Yes 7.9 IC50 = 13 nM Funct
Antagonist activity at recombinant human H4 receptor expressed in CHOK1 cells co-expressing Galpha16/aequorin assessed as inhibition of histamine-induced intracellular calcium flux preincubated for 30 mins followed by histamine addition and measured for 30 secs in presence of coelenterazine by luminescence assayAntagonist activity at recombinant human H4 receptor expressed in CHOK1 cells co-expressing Galpha16/aequorin assessed as inhibition of histamine-induced intracellular calcium flux preincubated for 30 mins followed by histamine addition and measured for 30 secs in presence of coelenterazine by luminescence assay
277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl
CHEMBL1091875 hrh4_human Human No 7.9 IC50 = 13 nM Bind
Displacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assayDisplacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assay
317 2 2 6 2.4 CN[C@H]1CCN(c2nc(N)nc3c2oc2ccc(Cl)cc23)C1
CHEMBL4792733 hrh4_human Human No 6.9 IC50 = 130 nM Bind
Displacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting methodDisplacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting method
289 1 1 7 0.7 Clc1cnc2nc(N3CCNCC3)c3nncn3c2c1
CHEMBL185951 hrh4_human Human Yes 6.9 IC50 = 138 nM Funct
Inhibition of mouse bone-marrow mast cell chemotaxis mediated by histamine H4 receptorInhibition of mouse bone-marrow mast cell chemotaxis mediated by histamine H4 receptor
278 1 1 3 1.6 CN1CCN(CC1)C(=O)c1nc2c([nH]1)cc(cc2)Cl
CHEMBL4573309 hrh4_human Human No 5.9 IC50 = 1400 nM Funct
Antagonist activity at human H4 receptor expressed in CHO-K1 cells co-expressing G protein alpha16 assessed as inhibition of histamine-induced calcium mobilization incubated for 16 hrs by aequorin-based functional assayAntagonist activity at human H4 receptor expressed in CHO-K1 cells co-expressing G protein alpha16 assessed as inhibition of histamine-induced calcium mobilization incubated for 16 hrs by aequorin-based functional assay
498 12 1 7 5.1 CCOC(=O)C1=C(C)NC(C)=C(C(=O)OCC)C1c1ccc(OCCCCCN2CCCCC2)cc1
CHEMBL1090519 hrh4_human Human No 5.9 IC50 = 1400 nM Bind
Displacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assayDisplacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assay
316 2 1 5 3.2 CNC1(C)CCN(c2ncnc3c2oc2ccc(Cl)cc23)C1
CHEMBL1090520 hrh4_human Human No 5.9 IC50 = 1400 nM Bind
Displacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assayDisplacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assay
328 1 1 5 3.2 Clc1ccc2oc3c(N4CC5CCCNC5C4)ncnc3c2c1
CHEMBL1092543 hrh4_human Human No 4.9 IC50 = 14200 nM Bind
Displacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assayDisplacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assay
370 2 1 5 3.8 CN[C@@H]1CCN(c2nc(C(F)(F)F)nc3c2oc2ccc(Cl)cc23)C1
CHEMBL454890 hrh4_human Human No 6.8 IC50 = 144.5 nM Funct
Inverse agonist activity at human histamine H4 receptor expressed in HEK293T cells by CRE-beta-galactosidase assayInverse agonist activity at human histamine H4 receptor expressed in HEK293T cells by CRE-beta-galactosidase assay
357 4 1 6 3.2 CN1CCN(c2nc(NCc3ccoc3)c3cc(Cl)ccc3n2)CC1
CHEMBL4635634 hrh4_human Human No 7.8 IC50 = 15.5 nM Bind
Inverse agonist activity at human H4R expressed in HEK293 cells co-expressing ELucC/ELucN-beta-arrestin2 assessed as inhibition of histamine-induced beta-arrestin recruitment by luciferase reporter gene assayInverse agonist activity at human H4R expressed in HEK293 cells co-expressing ELucC/ELucN-beta-arrestin2 assessed as inhibition of histamine-induced beta-arrestin recruitment 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 hrh4_human Human No 7.8 IC50 = 15.5 nM Bind
Inverse agonist activity at human H4R expressed in HEK293 cells co-expressing ELucC/ELucN-beta-arrestin2 assessed as inhibition of histamine-induced beta-arrestin recruitment by luciferase reporter gene assayInverse agonist activity at human H4R expressed in HEK293 cells co-expressing ELucC/ELucN-beta-arrestin2 assessed as inhibition of histamine-induced beta-arrestin recruitment 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
CHEMBL214312 hrh4_human Human No 5.8 IC50 = 1500 nM Funct
Antagonist activity at human H4 receptor expressed in 293-EBNA cells assessed as inhibition of histamine agonist activity by luciferase reporter gene assayAntagonist activity at human H4 receptor expressed in 293-EBNA cells assessed as inhibition of histamine agonist activity by luciferase reporter gene assay
247 6 2 2 3.1 c1nc([C@H]2C[C@@H]2CCNCC2CCCCC2)c[nH]1
CHEMBL1091559 hrh4_human Human No 5.8 IC50 = 1600 nM Bind
Displacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assayDisplacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assay
316 2 1 5 3.1 CNC1CCN(c2nc(C)nc3c2oc2ccc(Cl)cc23)C1
CHEMBL1172 hrh4_human Human Yes 4.8 IC50 = 16000 nM Bind
Histamine H-4 Receptor Binding Assay: Histamine H-4 Receptor Binding AssayHistamine H-4 Receptor Binding Assay: Histamine H-4 Receptor Binding Assay
310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1
CHEMBL3290578 hrh4_human Human No 5.8 IC50 = 1630 nM Funct
Antagonist activity at human histamine H4 receptor expressed in gamma-irradiated recombinant CHO cells assessed as inhibition of forskolin/histamine-induced intracellular cAMP accumulation preincubated for 30 mins followed by Eu chelate-labeled cAMP/anti-cAMP mAb addition measured after 1 hr by TR-FRET immunoassayAntagonist activity at human histamine H4 receptor expressed in gamma-irradiated recombinant CHO cells assessed as inhibition of forskolin/histamine-induced intracellular cAMP accumulation preincubated for 30 mins followed by Eu chelate-labeled cAMP/anti-cAMP mAb addition measured after 1 hr by TR-FRET immunoassay
348 2 1 6 1.6 CN1CCN(c2nc(N)nc(-c3ccc(Br)cc3)n2)CC1
CHEMBL1092933 hrh4_human Human No 6.8 IC50 = 169 nM Bind
Displacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assayDisplacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assay
328 1 0 5 3.3 CN1CC2CCC1CN2c1ncnc2c1oc1ccc(Cl)cc12
CHEMBL4790239 hrh4_human Human No 6.8 IC50 = 170 nM Bind
Displacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting methodDisplacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting method
303 1 0 7 1.1 CN1CCN(c2nc3ncc(Cl)cc3c3ncnn23)CC1
CHEMBL4798729 hrh4_human Human No 6.8 IC50 = 170 nM Bind
Displacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting methodDisplacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting method
313 2 0 8 0.9 CN1CCN(c2nc3ccc([N+](=O)[O-])cc3n3cnnc23)CC1
CHEMBL1092064 hrh4_human Human No 6.8 IC50 = 171 nM Bind
Displacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assayDisplacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assay
302 2 1 5 2.8 CN[C@@H]1CCN(c2ncnc3c2oc2cc(Cl)ccc23)C1
CHEMBL4789645 hrh4_human Human No 6.8 IC50 = 180 nM Bind
Displacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting methodDisplacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting method
337 1 0 7 1.7 CN1CCN(c2nc3nc(Cl)c(Cl)cc3n3cnnc23)CC1
CHEMBL260374 hrh4_human Human Yes 7.7 IC50 = 19 nM Funct
Antagonist activity at human H4 receptor expressed in CHO-K1 cells co-expressing G protein alpha16 assessed as inhibition of histamine-induced calcium mobilization incubated for 16 hrs by aequorin-based functional assayAntagonist activity at human H4 receptor expressed in CHO-K1 cells co-expressing G protein alpha16 assessed as inhibition of histamine-induced calcium mobilization incubated for 16 hrs by aequorin-based functional assay
292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1
CHEMBL1093180 hrh4_human Human Yes 7.7 IC50 = 19 nM Bind
Displacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assayDisplacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assay
302 1 0 5 2.8 CN1CCN(c2ncnc3c2oc2ccc(Cl)cc23)CC1
CHEMBL1092330 hrh4_human Human No 5.7 IC50 = 1900 nM Bind
Displacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assayDisplacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assay
316 1 0 5 3.2 CC1CN(c2ncnc3c2oc2ccc(Cl)cc23)CCN1C
CHEMBL129198 hrh4_human Human Yes 6.7 IC50 = 199 nM Funct
Antagonist activity at H4R in human eosinophils assessed as inhibition of histamine-induced shape change by GAFS assayAntagonist activity at H4R in human eosinophils assessed as inhibition of histamine-induced shape change by GAFS assay
277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl
CHEMBL129198 hrh4_human Human Yes 6.7 IC50 = 199.5 nM Funct
Antagonist actiivty at human H4R expressed in human U2OS cells assessed as inhibition of [35S]GTPgammaS binding after 30 mins by scintillation proximity assayAntagonist actiivty at human H4R expressed in human U2OS cells assessed as inhibition of [35S]GTPgammaS binding after 30 mins by scintillation proximity assay
277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl
CHEMBL1197564 hrh4_human Human Yes 5.7 IC50 = 2000 nM Bind
Histamine H-4 Receptor Binding Assay: Histamine H-4 Receptor Binding AssayHistamine H-4 Receptor Binding Assay: Histamine H-4 Receptor Binding Assay
295 0 1 3 3.7 O=C1Cc2ccccc2C(=C2CCNCC2)c2ccsc21
CHEMBL1222728 hrh4_human Human Yes 4.7 IC50 = 20000 nM Funct
Antagonist activity at human histamine H4 receptorAntagonist activity at human histamine H4 receptor
348 5 0 6 2.1 CN1CCN(C(c2ccccc2)c2nnnn2Cc2ccccc2)CC1
CHEMBL1088888 hrh4_human Human No 4.7 IC50 = 21000 nM Bind
Displacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assayDisplacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assay
316 2 0 5 3.2 CN(C)C1CCN(c2ncnc3c2oc2ccc(Cl)cc23)C1
CHEMBL534 hrh4_human Human Yes 4.7 IC50 = 21000 nM Bind
Histamine H-4 Receptor Binding Assay: Histamine H-4 Receptor Binding AssayHistamine H-4 Receptor Binding Assay: Histamine H-4 Receptor Binding Assay
309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1
CHEMBL4778864 hrh4_human Human Yes 7.7 IC50 = 22 nM Bind
Displacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting methodDisplacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting method
302 1 0 6 1.7 CN1CCN(c2nc3ccc(Cl)cc3n3cnnc23)CC1
CHEMBL129198 hrh4_human Human Yes 6.7 IC50 = 221.4 nM Funct
Antagonist activity at H4R in human eosinophils assessed as inhibition of histamine-induced CD11b upregulationAntagonist activity at H4R in human eosinophils assessed as inhibition of histamine-induced CD11b upregulation
277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl
CHEMBL306316 hrh4_human Human Yes 5.6 IC50 = 2300 nM Bind
Displacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting methodDisplacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting method
268 1 0 6 1.0 CN1CCN(c2nc3ccccc3n3cnnc23)CC1
CHEMBL3929465 hrh4_human Human No 5.6 IC50 = 2300 nM Bind
Histamine H-4 Receptor Binding Assay: Histamine H-4 Receptor Binding AssayHistamine H-4 Receptor Binding Assay: Histamine H-4 Receptor Binding Assay
297 0 2 3 3.5 O[C@H]1Cc2ccccc2C(=C2CCNCC2)c2ccsc21
CHEMBL1090655 hrh4_human Human No 6.6 IC50 = 236 nM Bind
Displacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assayDisplacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assay
328 1 0 5 3.3 Clc1ccc2oc3c(N4CCN5CCCC5C4)ncnc3c2c1
CHEMBL4778712 hrh4_human Human No 6.6 IC50 = 240 nM Bind
Displacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting methodDisplacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting method
401 3 0 8 2.0 CN1CCN(c2nc3nc(OCC(F)(F)F)c(Cl)cc3n3cnnc23)CC1
CHEMBL4793425 hrh4_human Human No 6.6 IC50 = 240 nM Bind
Displacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting methodDisplacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting method
294 1 0 8 0.3 CN1CCN(c2nc3ncc(C#N)cc3n3cnnc23)CC1
CHEMBL4549015 hrh4_human Human Yes 6.6 IC50 = 265 nM Funct
Antagonist activity at recombinant human H4 receptor expressed in CHOK1 cells co-expressing Galpha16/aequorin assessed as inhibition of histamine-induced intracellular calcium flux preincubated for 30 mins followed by histamine addition and measured for 30 secs in presence of coelenterazine by luminescence assayAntagonist activity at recombinant human H4 receptor expressed in CHOK1 cells co-expressing Galpha16/aequorin assessed as inhibition of histamine-induced intracellular calcium flux preincubated for 30 mins followed by histamine addition and measured for 30 secs in presence of coelenterazine by luminescence assay
236 3 1 6 0.2 CCCc1nc(N)nc(N2CCN(C)CC2)n1
CHEMBL4790724 hrh4_human Human Yes 7.6 IC50 = 27 nM Bind
Displacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting methodDisplacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting method
334 2 1 8 0.2 CNC1CN(C1)c1nc2ncc(cc2n2c1nnn2)Br
CHEMBL4784683 hrh4_human Human No 6.6 IC50 = 270 nM Bind
Displacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting methodDisplacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting method
328 1 0 8 0.9 CN1CCN(c2nc3nc(C#N)c(Cl)cc3n3cnnc23)CC1
CHEMBL4790724 hrh4_human Human Yes 7.6 IC50 = 28 nM Funct
Antagonist activity at recombinant human histamine H4 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine induced stimulation of [35S]-GTPgammaS binding by scintillation proximity assayAntagonist activity at recombinant human histamine H4 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine induced stimulation of [35S]-GTPgammaS binding by scintillation proximity assay
334 2 1 8 0.2 CNC1CN(C1)c1nc2ncc(cc2n2c1nnn2)Br
CHEMBL4783487 hrh4_human Human No 7.6 IC50 = 28 nM Bind
Displacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting methodDisplacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting method
348 1 0 8 0.6 CN1CCN(c2nc3ncc(Br)cc3n3nnnc23)CC1
CHEMBL4792352 hrh4_human Human No 6.6 IC50 = 280 nM Bind
Displacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting methodDisplacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting method
337 1 0 7 1.4 CN1CCN(c2nc3ncc(C(F)(F)F)cc3n3cnnc23)CC1
CHEMBL1090531 hrh4_human Human No 6.5 IC50 = 285 nM Bind
Displacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assayDisplacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assay
302 2 1 5 2.8 CN[C@H]1CCN(c2ncnc3c2oc2ccc(Cl)cc23)C1
CHEMBL129198 hrh4_human Human Yes 7.5 IC50 = 29 nM Bind
Displacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting methodDisplacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting method
277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl
CHEMBL4790724 hrh4_mouse Mouse Yes 6.5 IC50 = 290 nM Bind
Displacement of [3H]-histamine from recombinant mouse histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting methodDisplacement of [3H]-histamine from recombinant mouse histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting method
334 2 1 8 0.2 CNC1CN(C1)c1nc2ncc(cc2n2c1nnn2)Br
CHEMBL4796300 hrh4_human Human No 5.5 IC50 = 2900 nM Bind
Displacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting methodDisplacement of [3H]-histamine from recombinant human histamine H4 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
CHEMBL1090531 hrh4_human Human No 6.5 IC50 = 292 nM Funct
Inverse agonist activity at human histamine H4 receptor assessed as inhibition of [35S]GTPgammaS binding after 15 mins by scintillation proximity assayInverse agonist activity at human histamine H4 receptor assessed as inhibition of [35S]GTPgammaS binding after 15 mins by scintillation proximity assay
302 2 1 5 2.8 CN[C@H]1CCN(c2ncnc3c2oc2ccc(Cl)cc23)C1
CHEMBL1091874 hrh4_human Human No 8.5 IC50 = 3 nM Funct
Inverse agonist activity at human histamine H4 receptor assessed as inhibition of [35S]GTPgammaS binding after 15 mins by scintillation proximity assayInverse agonist activity at human histamine H4 receptor assessed as inhibition of [35S]GTPgammaS binding after 15 mins by scintillation proximity assay
317 2 2 6 2.4 CN[C@@H]1CCN(c2nc(N)nc3c2oc2ccc(Cl)cc23)C1
CHEMBL129198 hrh4_human Human Yes 7.5 IC50 = 30 nM Funct
Antagonist activity at H4R in human eosinophils assessed as inhibition of imetit-induced shape change by GAFS assayAntagonist activity at H4R in human eosinophils assessed as inhibition of imetit-induced shape change by GAFS assay
277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl
CHEMBL1088859 hrh4_human Human No 7.5 IC50 = 30 nM Bind
Displacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assayDisplacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assay
336 2 1 5 3.2 CN[C@@H]1CCN(c2ncnc3c2oc2ccc(C(F)(F)F)cc23)C1
CHEMBL4787243 hrh4_human Human No 6.5 IC50 = 300 nM Bind
Displacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting methodDisplacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting method
361 1 0 7 1.5 Cc1c(Br)cnc2nc(N3CCN(C)CC3)c3nncn3c12
CHEMBL4781409 hrh4_human Human No 5.5 IC50 = 3000 nM Bind
Displacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting methodDisplacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting method
269 1 0 7 0.4 CN1CCN(c2nc3ncccc3n3cnnc23)CC1
CHEMBL4791152 hrh4_human Human No 5.5 IC50 = 3000 nM Bind
Displacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting methodDisplacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting method
269 1 0 7 0.4 CN1CCN(c2nc3cccnc3n3cnnc23)CC1
CHEMBL1093138 hrh4_human Human No 6.5 IC50 = 310 nM Bind
Displacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assayDisplacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assay
342 2 0 5 3.7 CN1CCN(c2nc(C3CC3)nc3c2oc2ccc(Cl)cc23)CC1
CHEMBL4483783 hrh4_human Human No 7.5 IC50 = 32 nM Funct
Antagonist activity at recombinant human H4 receptor expressed in CHOK1 cells co-expressing Galpha16/aequorin assessed as inhibition of histamine-induced intracellular calcium flux preincubated for 30 mins followed by histamine addition and measured for 30 secs in presence of coelenterazine by luminescence assayAntagonist activity at recombinant human H4 receptor expressed in CHOK1 cells co-expressing Galpha16/aequorin assessed as inhibition of histamine-induced intracellular calcium flux preincubated for 30 mins followed by histamine addition and measured for 30 secs in presence of coelenterazine by luminescence assay
290 3 1 6 1.3 CN1CCN(c2nc(N)nc(CC3CCCCC3)n2)CC1
CHEMBL1090190 hrh4_human Human No 7.5 IC50 = 33 nM Bind
Displacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assayDisplacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assay
302 2 1 5 2.8 CN[C@@H]1CCN(c2ncnc3c2oc2ccc(Cl)cc23)C1
CHEMBL592379 hrh4_human Human No 7.5 IC50 = 33.1 nM Funct
Inverse agonist activity at human histamine H4 receptor expressed in HEK293T cells by CRE-beta-galactosidase assayInverse agonist activity at human histamine H4 receptor expressed in HEK293T cells by CRE-beta-galactosidase assay
460 7 2 7 2.9 CN1CCN(CC1)C2=NC3=C(C=C(C=C3)Cl)C(=N2)NCCS(=O)(=O)NC4=CC=CC=C4
CHEMBL4778591 hrh4_human Human No 7.5 IC50 = 34 nM Bind
Displacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting methodDisplacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting method
395 1 0 7 1.0 CN1CCN(c2nc3ncc(I)cc3n3cnnc23)CC1
CHEMBL1091558 hrh4_human Human Yes 7.4 IC50 = 37 nM Bind
Displacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assayDisplacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assay
316 1 0 5 3.1 Cc1nc(N2CCN(C)CC2)c2oc3ccc(Cl)cc3c2n1
CHEMBL4794336 hrh4_human Human No 6.4 IC50 = 380 nM Bind
Displacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting methodDisplacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting method
317 1 0 7 1.5 C[C@H]1CN(c2nc3ncc(Cl)cc3n3cnnc23)CCN1C
CHEMBL1092542 hrh4_human Human No 7.4 IC50 = 39 nM Funct
Inverse agonist activity at human histamine H4 receptor assessed as inhibition of [35S]GTPgammaS binding after 15 mins by scintillation proximity assayInverse agonist activity at human histamine H4 receptor assessed as inhibition of [35S]GTPgammaS binding after 15 mins by scintillation proximity assay
370 1 0 5 3.8 CN1CCN(c2nc(C(F)(F)F)nc3c2oc2ccc(Cl)cc23)CC1
CHEMBL1091875 hrh4_human Human No 8.4 IC50 = 4 nM Funct
Inverse agonist activity at human histamine H4 receptor assessed as inhibition of [35S]GTPgammaS binding after 15 mins by scintillation proximity assayInverse agonist activity at human histamine H4 receptor assessed as inhibition of [35S]GTPgammaS binding after 15 mins by scintillation proximity assay
317 2 2 6 2.4 CN[C@H]1CCN(c2nc(N)nc3c2oc2ccc(Cl)cc23)C1
CHEMBL1915540 hrh4_human Human Yes 8.3 IC50 = 4.9 nM Funct
Antagonist activity at H4R in human eosinophils assessed as inhibition of histamine-induced CD11b upregulationAntagonist activity at H4R in human eosinophils assessed as inhibition of histamine-induced CD11b upregulation
262 5 3 6 0.7 CN[C@@H]1CCN(C1)c1cc(NCC2CC2)nc(n1)N
CHEMBL129198 hrh4_mouse Mouse Yes 7.4 IC50 = 40 nM Bind
Inhibition of histamine H4 receptor-mediated chemotaxis in mouse bone marrow cellsInhibition of histamine H4 receptor-mediated chemotaxis in mouse bone marrow cells
277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl
CHEMBL129198 hrh4_human Human Yes 7.4 IC50 = 40 nM Funct
Inhibition of mouse bone-marrow mast cell chemotaxis mediated by histamine H4 receptorInhibition of mouse bone-marrow mast cell chemotaxis mediated by histamine H4 receptor
277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl
CHEMBL1090190 hrh4_human Human No 7.4 IC50 = 41 nM Funct
Inverse agonist activity at human histamine H4 receptor assessed as inhibition of [35S]GTPgammaS binding after 15 mins by scintillation proximity assayInverse agonist activity at human histamine H4 receptor assessed as inhibition of [35S]GTPgammaS binding after 15 mins by scintillation proximity assay
302 2 1 5 2.8 CN[C@@H]1CCN(c2ncnc3c2oc2ccc(Cl)cc23)C1
CHEMBL4800462 hrh4_human Human No 5.4 IC50 = 4100 nM Bind
Displacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting methodDisplacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting method
303 2 1 7 1.1 CN[C@@H]1CCN(c2nc3ncc(Cl)cc3n3cnnc23)C1
CHEMBL4798915 hrh4_human Human No 6.4 IC50 = 430 nM Bind
Displacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting methodDisplacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting method
315 1 0 7 1.2 CN1C[C@@H]2C[C@H]1CN2c1nc2ncc(Cl)cc2n2cnnc12
CHEMBL3628042 hrh4_human Human No 6.4 IC50 = 439 nM Funct
Antagonist activity at human H4R expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by TR-FRET immunoassayAntagonist activity at human H4R expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by TR-FRET immunoassay
330 3 1 6 2.0 CN1CCN(c2nc(N)nc(/C=C/c3cccc(Cl)c3)n2)CC1
CHEMBL1092934 hrh4_human Human No 6.4 IC50 = 440 nM Bind
Displacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assayDisplacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assay
328 1 0 5 3.3 CN1C2CCC1CN(c1ncnc3c1oc1ccc(Cl)cc13)C2
CHEMBL1935572 hrh4_human Human No 7.3 IC50 = 46 nM Funct
Antagonist activity at human H4 receptor expressed in HEK293T cells assessed as inhibition of histamine-induced [35S]GTPgammaS bindingAntagonist activity at human H4 receptor expressed in HEK293T cells assessed as inhibition of histamine-induced [35S]GTPgammaS binding
325 2 1 6 2.7 CN1CCN(c2nc(N)nc3cc(-c4ccsc4)ccc23)CC1
CHEMBL1935571 hrh4_human Human No 7.3 IC50 = 47 nM Funct
Antagonist activity at human H4 receptor expressed in HEK293T cells assessed as inhibition of histamine-induced [35S]GTPgammaS bindingAntagonist activity at human H4 receptor expressed in HEK293T cells assessed as inhibition of histamine-induced [35S]GTPgammaS binding
309 2 1 6 2.2 CN1CCN(c2nc(N)nc3cc(-c4ccoc4)ccc23)CC1
CHEMBL4796842 hrh4_human Human No 5.3 IC50 = 4800 nM Bind
Displacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting methodDisplacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting method
317 2 0 7 1.5 CN(C)[C@@H]1CCN(c2nc3ncc(Cl)cc3n3cnnc23)C1
CHEMBL260374 hrh4_human Human Yes 6.3 IC50 = 489.8 nM Bind
Inverse agonist activity at human H4R expressed in HEK293 cells co-expressing ELucC/ELucN-beta-arrestin2 assessed as inhibition of histamine-induced beta-arrestin recruitment by luciferase reporter gene assayInverse agonist activity at human H4R expressed in HEK293 cells co-expressing ELucC/ELucN-beta-arrestin2 assessed as inhibition of histamine-induced beta-arrestin recruitment by luciferase reporter gene assay
292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1
CHEMBL4789385 hrh4_human Human No 6.3 IC50 = 490 nM Bind
Displacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting methodDisplacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting method
301 1 1 7 0.9 Clc1cnc2nc(N3C[C@@H]4C[C@H]3CN4)c3nncn3c2c1
CHEMBL129198 hrh4_human Human Yes 8.3 IC50 = 5.3 nM Funct
Antagonist activity at H4R in human eosinophils assessed as inhibition of histamine-induced actin polymerisationAntagonist activity at H4R in human eosinophils assessed as inhibition of histamine-induced actin polymerisation
277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl
CHEMBL4795091 hrh4_human Human No 6.3 IC50 = 510 nM Bind
Displacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting methodDisplacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting method
283 1 0 7 0.7 Cc1cnc2nc(N3CCN(C)CC3)c3nncn3c2c1
CHEMBL3290576 hrh4_human Human No 6.3 IC50 = 512 nM Funct
Antagonist activity at human histamine H4 receptor expressed in gamma-irradiated recombinant CHO cells assessed as inhibition of forskolin/histamine-induced intracellular cAMP accumulation preincubated for 30 mins followed by Eu chelate-labeled cAMP/anti-cAMP mAb addition measured after 1 hr by TR-FRET immunoassayAntagonist activity at human histamine H4 receptor expressed in gamma-irradiated recombinant CHO cells assessed as inhibition of forskolin/histamine-induced intracellular cAMP accumulation preincubated for 30 mins followed by Eu chelate-labeled cAMP/anti-cAMP mAb addition measured after 1 hr by TR-FRET immunoassay
304 2 1 6 1.5 CN1CCN(c2nc(N)nc(-c3ccc(Cl)cc3)n2)CC1
CHEMBL4793974 hrh4_human Human No 7.3 IC50 = 52 nM Bind
Displacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting methodDisplacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting method
329 1 0 7 1.6 Clc1cnc2nc(N3CCN4CCCC4C3)c3nncn3c2c1
CHEMBL4786816 hrh4_human Human No 6.3 IC50 = 520 nM Bind
Displacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting methodDisplacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting method
347 3 0 8 1.5 CCOc1nc2nc(N3CCN(C)CC3)c3nncn3c2cc1Cl
CHEMBL4782945 hrh4_human Human No 5.3 IC50 = 5200 nM Bind
Displacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting methodDisplacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting method
275 1 1 7 0.5 NC1CN(c2nc3ncc(Cl)cc3n3cnnc23)C1
CHEMBL4781484 hrh4_human Human No 7.3 IC50 = 53 nM Bind
Displacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting methodDisplacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting method
290 2 1 8 0.1 CNC1CN(c2nc3ncc(Cl)cc3n3nnnc23)C1
CHEMBL1915540 hrh4_human Human Yes 7.3 IC50 = 53.7 nM Funct
Antagonist activity at human histamine H4 receptor expressed in HEK cells assessed as inhibition of histamine-induced [35S]GTPgammaS bindingAntagonist activity at human histamine H4 receptor expressed in HEK cells assessed as inhibition of histamine-induced [35S]GTPgammaS binding
262 5 3 6 0.7 CN[C@@H]1CCN(C1)c1cc(NCC2CC2)nc(n1)N
CHEMBL185951 hrh4_human Human Yes 6.3 IC50 = 530 nM Funct
Inhibition of human eosinophil chemotaxis mediated by histamine H4 receptorInhibition of human eosinophil chemotaxis mediated by histamine H4 receptor
278 1 1 3 1.6 CN1CCN(CC1)C(=O)c1nc2c([nH]1)cc(cc2)Cl
CHEMBL4776004 hrh4_human Human No 6.2 IC50 = 570 nM Bind
Displacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting methodDisplacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting method
282 1 0 6 1.3 Cc1ccc2nc(N3CCN(C)CC3)c3nncn3c2c1
CHEMBL3629828 hrh4_human Human No 6.2 IC50 = 606 nM Funct
Antagonist activity at human H4R expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by TR-FRET immunoassayAntagonist activity at human H4R expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by TR-FRET immunoassay
310 3 1 6 1.7 Cc1cccc(/C=C/c2nc(N)nc(N3CCN(C)CC3)n2)c1
CHEMBL4787983 hrh4_human Human No 7.2 IC50 = 62 nM Bind
Displacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting methodDisplacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting method
304 1 0 8 0.5 CN1CCN(c2nc3ncc(Cl)cc3n3nnnc23)CC1
CHEMBL4790726 hrh4_human Human No 5.2 IC50 = 6200 nM Bind
Displacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting methodDisplacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting method
301 1 0 5 2.3 CN1CCN(c2cc3ccc(Cl)cc3n3cnnc23)CC1
CHEMBL1092880 hrh4_human Human No 5.2 IC50 = 6200 nM Bind
Displacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assayDisplacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assay
293 2 1 6 2.0 CNC1CCN(c2ncnc3c2oc2ccc(C#N)cc23)C1
CHEMBL4789543 hrh4_human Human No 5.2 IC50 = 6300 nM Bind
Displacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting methodDisplacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting method
289 1 1 7 0.9 N[C@@H]1CCN(c2nc3ncc(Cl)cc3n3cnnc23)C1
CHEMBL4782303 hrh4_human Human No 7.2 IC50 = 65 nM Bind
Displacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting methodDisplacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting method
289 2 1 7 0.7 CNC1CN(c2nc3ncc(Cl)cc3n3cnnc23)C1
CHEMBL260374 hrh4_human Human Yes 6.2 IC50 = 667 nM Funct
Antagonist activity at histamine H4 receptor expressed in HEK293 cells co-transfected with pCRE-Luc gene assessed as inhibition of forskolin/histamine-induced cAMP accumulation after 5 hrs by luciferase reporter gene assayAntagonist activity at histamine H4 receptor expressed in HEK293 cells co-transfected with pCRE-Luc gene assessed as inhibition of forskolin/histamine-induced cAMP accumulation after 5 hrs by luciferase reporter gene assay
292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1
CHEMBL4778068 hrh4_human Human No 7.2 IC50 = 67 nM Bind
Displacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting methodDisplacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting method
347 1 0 7 1.2 CN1CCN(c2nc3ncc(Br)cc3n3cnnc23)CC1
CHEMBL260374 hrh4_human Human Yes 6.2 IC50 = 680 nM Funct
Antagonist activity at human H4 receptor expressed in 293-EBNA cells assessed as inhibition of histamine agonist activity by luciferase reporter gene assayAntagonist activity at human H4 receptor expressed in 293-EBNA cells assessed as inhibition of histamine agonist activity by luciferase reporter gene assay
292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1
CHEMBL452847 hrh4_human Human Yes 7.2 IC50 = 69.2 nM Funct
Inverse agonist activity at human histamine H4 receptor expressed in HEK293T cells by CRE-beta-galactosidase assayInverse agonist activity at human histamine H4 receptor expressed in HEK293T cells by CRE-beta-galactosidase assay
373 4 1 6 3.7 CN1CCN(c2nc(NCc3cccs3)c3cc(Cl)ccc3n2)CC1
CHEMBL4790724 hrh4_mouse Mouse Yes 6.2 IC50 = 690 nM Funct
Antagonist activity at recombinant mouse histamine H4 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine induced stimulation of [35S]-GTPgammaS binding by scintillation proximity assayAntagonist activity at recombinant mouse histamine H4 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine induced stimulation of [35S]-GTPgammaS binding by scintillation proximity assay
334 2 1 8 0.2 CNC1CN(C1)c1nc2ncc(cc2n2c1nnn2)Br
CHEMBL1092332 hrh4_human Human No 7.2 IC50 = 70 nM Funct
Inverse agonist activity at human histamine H4 receptor assessed as inhibition of [35S]GTPgammaS binding after 15 mins by scintillation proximity assayInverse agonist activity at human histamine H4 receptor assessed as inhibition of [35S]GTPgammaS binding after 15 mins by scintillation proximity assay
314 1 0 5 2.9 CN1C[C@@H]2C[C@H]1CN2c1ncnc2c1oc1ccc(Cl)cc12
CHEMBL2376804 hrh4_human Human No 7.2 IC50 = 70.8 nM Funct
Antagonist activity at human histamine H4 receptor expressed in HEK cells assessed as inhibition of histamine-induced [35S]GTPgammaS bindingAntagonist activity at human histamine H4 receptor expressed in HEK cells assessed as inhibition of histamine-induced [35S]GTPgammaS binding
270 3 2 6 0.9 CNC1CN(c2nc(N)nc3cc(C4CC4)cnc23)C1
CHEMBL1091569 hrh4_human Human No 7.1 IC50 = 76 nM Funct
Inverse agonist activity at human histamine H4 receptor assessed as inhibition of [35S]GTPgammaS binding after 15 mins by scintillation proximity assayInverse agonist activity at human histamine H4 receptor assessed as inhibition of [35S]GTPgammaS binding after 15 mins by scintillation proximity assay
288 2 1 5 2.4 CNC1CN(c2ncnc3c2oc2ccc(Cl)cc23)C1
CHEMBL4781143 hrh4_human Human No 6.1 IC50 = 760 nM Bind
Displacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting methodDisplacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting method
303 1 1 7 1.1 C[C@H]1CN(c2nc3ncc(Cl)cc3n3cnnc23)CCN1
CHEMBL4797517 hrh4_human Human No 7.1 IC50 = 77 nM Bind
Displacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting methodDisplacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting method
303 1 0 7 1.1 CN1CCN(c2nc3ncc(Cl)cc3n3cnnc23)CC1
CHEMBL1935573 hrh4_human Human No 7.1 IC50 = 83 nM Funct
Antagonist activity at human H4 receptor expressed in HEK293T cells assessed as inhibition of histamine-induced [35S]GTPgammaS bindingAntagonist activity at human H4 receptor expressed in HEK293T cells assessed as inhibition of histamine-induced [35S]GTPgammaS binding
309 2 1 6 2.2 CN1CCN(c2nc(N)nc3cc(-c4ccco4)ccc23)CC1
CHEMBL1092542 hrh4_human Human No 7.1 IC50 = 83 nM Bind
Displacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assayDisplacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assay
370 1 0 5 3.8 CN1CCN(c2nc(C(F)(F)F)nc3c2oc2ccc(Cl)cc23)CC1
CHEMBL4635634 hrh4_mouse Mouse No 7.1 IC50 = 83.2 nM Funct
Inverse agonist activity at mouse H4R expressed in HEK293-SF-mH4R-His6-CRE-Luc cells assessed as reduction in histamine-induced inhibition of forskolin stimulated luciferase activity by luciferase reporter gene assayInverse agonist activity at mouse H4R expressed in HEK293-SF-mH4R-His6-CRE-Luc cells assessed as reduction in histamine-induced inhibition of forskolin stimulated luciferase activity 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 hrh4_mouse Mouse No 7.1 IC50 = 83.2 nM Funct
Inverse agonist activity at mouse H4R expressed in HEK293-SF-mH4R-His6-CRE-Luc cells assessed as reduction in histamine-induced inhibition of forskolin stimulated luciferase activity by luciferase reporter gene assayInverse agonist activity at mouse H4R expressed in HEK293-SF-mH4R-His6-CRE-Luc cells assessed as reduction in histamine-induced inhibition of forskolin stimulated luciferase activity 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
CHEMBL1091729 hrh4_human Human No 7.1 IC50 = 86 nM Bind
Displacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assayDisplacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assay
282 2 1 5 2.5 CN[C@@H]1CCN(c2ncnc3c2oc2ccc(C)cc23)C1
CHEMBL129198 hrh4_human Human Yes 7.1 IC50 = 86 nM Bind
Inhibition of histamine H4 receptor-mediated chemotaxis in human eosinophilsInhibition of histamine H4 receptor-mediated chemotaxis in human eosinophils
277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl
CHEMBL129198 hrh4_human Human Yes 7.1 IC50 = 86 nM Funct
Inhibition of human eosinophil chemotaxis mediated by histamine H4 receptorInhibition of human eosinophil chemotaxis mediated by histamine H4 receptor
277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl
CHEMBL214311 hrh4_human Human No 6.1 IC50 = 860 nM Funct
Antagonist activity at human H4 receptor expressed in 293-EBNA cells assessed as inhibition of histamine agonist activity by luciferase reporter gene assayAntagonist activity at human H4 receptor expressed in 293-EBNA cells assessed as inhibition of histamine agonist activity by luciferase reporter gene assay
275 6 2 2 3.3 Clc1ccc(CNCC[C@H]2C[C@@H]2c2c[nH]cn2)cc1
CHEMBL1091569 hrh4_human Human No 7.1 IC50 = 87 nM Bind
Displacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assayDisplacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assay
288 2 1 5 2.4 CNC1CN(c2ncnc3c2oc2ccc(Cl)cc23)C1
CHEMBL1093439 hrh4_human Human No 7.1 IC50 = 90 nM Bind
Displacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assayDisplacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assay
332 2 0 6 2.8 COc1nc(N2CCN(C)CC2)c2oc3ccc(Cl)cc3c2n1
CHEMBL1088889 hrh4_human Human No 7.0 IC50 = 95 nM Bind
Displacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assayDisplacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assay
302 2 1 5 2.8 CNC1CCN(c2ncnc3c2oc2ccc(Cl)cc23)C1
CHEMBL2376803 hrh4_human Human No 7.0 IC50 = 97.7 nM Funct
Antagonist activity at human histamine H4 receptor expressed in HEK cells assessed as inhibition of histamine-induced [35S]GTPgammaS bindingAntagonist activity at human histamine H4 receptor expressed in HEK cells assessed as inhibition of histamine-induced [35S]GTPgammaS binding
298 3 2 6 1.7 CNC1CN(c2nc(N)nc3cc(C4CCCC4)cnc23)C1
CHEMBL260374 hrh4_human Human Yes 6.0 IC50 = 977 nM Funct
Antagonist activity at human H4 receptor expressed in HEK293T cells assessed as inhibition of histamine-induced [35S]GTPgammaS bindingAntagonist activity at human H4 receptor expressed in HEK293T cells assessed as inhibition of histamine-induced [35S]GTPgammaS binding
292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1
CHEMBL3393547 hrh4_human Human No 10.1 Kd = 0.1 nM Funct
Antagonist activity at human recombinant histamine H4 receptor expressed in SK-N-MC cells assessed as inhibition of forskolin-stimulated cAMP-mediated reporter gene activityAntagonist activity at human recombinant histamine H4 receptor expressed in SK-N-MC cells assessed as inhibition of forskolin-stimulated cAMP-mediated reporter gene activity
287 4 2 5 1.9 CN[C@@H]1CCN(c2ccnc(NC3CC4CCC3C4)n2)C1
CHEMBL3236561 hrh4_human Human No 10.0 Kd = 0.1 nM Funct
Antagonist activity at human histamine H4 receptor expressed in SK-N-MC cells assessed as reduction of histamine-induced inhibition of cAMP-mediated beta-galactosidase reporter gene activity treated 10 mins prior to histamine challenge by microplate reader analysisAntagonist activity at human histamine H4 receptor expressed in SK-N-MC cells assessed as reduction of histamine-induced inhibition of cAMP-mediated beta-galactosidase reporter gene activity treated 10 mins prior to histamine challenge by microplate reader analysis
273 2 2 5 1.5 Nc1nc(C2CCCC2)cc(N2C[C@H]3CCN[C@H]3C2)n1
CHEMBL3236552 hrh4_human Human Yes 9.9 Kd = 0.1 nM Funct
Antagonist activity at human histamine H4 receptor expressed in SK-N-MC cells assessed as reduction of histamine-induced inhibition of cAMP-mediated beta-galactosidase reporter gene activity treated 10 mins prior to histamine challenge by microplate reader analysisAntagonist activity at human histamine H4 receptor expressed in SK-N-MC cells assessed as reduction of histamine-induced inhibition of cAMP-mediated beta-galactosidase reporter gene activity treated 10 mins prior to histamine challenge by microplate reader analysis
261 2 1 5 1.5 CN1CCN(c2cc(C3CCCC3)nc(N)n2)CC1
CHEMBL3236554 hrh4_human Human No 9.6 Kd = 0.3 nM Funct
Antagonist activity at human histamine H4 receptor expressed in SK-N-MC cells assessed as reduction of histamine-induced inhibition of cAMP-mediated beta-galactosidase reporter gene activity treated 10 mins prior to histamine challenge by microplate reader analysisAntagonist activity at human histamine H4 receptor expressed in SK-N-MC cells assessed as reduction of histamine-induced inhibition of cAMP-mediated beta-galactosidase reporter gene activity treated 10 mins prior to histamine challenge by microplate reader analysis
261 3 2 5 1.5 CN[C@@H]1CCN(c2cc(C3CCCC3)nc(N)n2)C1
CHEMBL3236553 hrh4_human Human Yes 9.5 Kd = 0.3 nM Funct
Antagonist activity at human histamine H4 receptor expressed in SK-N-MC cells assessed as reduction of histamine-induced inhibition of cAMP-mediated beta-galactosidase reporter gene activity treated 10 mins prior to histamine challenge by microplate reader analysisAntagonist activity at human histamine H4 receptor expressed in SK-N-MC cells assessed as reduction of histamine-induced inhibition of cAMP-mediated beta-galactosidase reporter gene activity treated 10 mins prior to histamine challenge by microplate reader analysis
247 2 2 5 1.1 Nc1nc(C2CCCC2)cc(N2CCNCC2)n1
CHEMBL3236575 hrh4_human Human No 9.4 Kd = 0.4 nM Funct
Antagonist activity at human histamine H4 receptor expressed in SK-N-MC cells assessed as reduction of histamine-induced inhibition of cAMP-mediated beta-galactosidase reporter gene activity treated 10 mins prior to histamine challenge by microplate reader analysisAntagonist activity at human histamine H4 receptor expressed in SK-N-MC cells assessed as reduction of histamine-induced inhibition of cAMP-mediated beta-galactosidase reporter gene activity treated 10 mins prior to histamine challenge by microplate reader analysis
247 3 2 5 1.1 CN[C@@H]1CCN(c2cc(C3CCC3)nc(N)n2)C1
CHEMBL1770980 hrh4_human Human No 9.4 Kd = 0.4 nM Funct
Antagonist activity at human histamine H4 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 6 hrsAntagonist activity at human histamine H4 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 6 hrs
276 4 3 6 1.2 CN[C@@H]1CCN(c2cc(NC3CCCC3)nc(N)n2)C1
CHEMBL1770979 hrh4_human Human No 9.3 Kd = 0.5 nM Funct
Antagonist activity at human histamine H4 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 6 hrsAntagonist activity at human histamine H4 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 6 hrs
264 5 3 6 0.9 CN[C@@H]1CCN(c2cc(NCC(C)C)nc(N)n2)C1
CHEMBL3236556 hrh4_human Human No 9.2 Kd = 0.6 nM Funct
Antagonist activity at human histamine H4 receptor expressed in SK-N-MC cells assessed as reduction of histamine-induced inhibition of cAMP-mediated beta-galactosidase reporter gene activity treated 10 mins prior to histamine challenge by microplate reader analysisAntagonist activity at human histamine H4 receptor expressed in SK-N-MC cells assessed as reduction of histamine-induced inhibition of cAMP-mediated beta-galactosidase reporter gene activity treated 10 mins prior to histamine challenge by microplate reader analysis
247 2 2 5 1.3 Nc1nc(C2CCCC2)cc(N2CC[C@@H](N)C2)n1
CHEMBL3393526 hrh4_human Human No 9.2 Kd = 0.6 nM Funct
Antagonist activity at human recombinant histamine H4 receptor expressed in SK-N-MC cells assessed as inhibition of forskolin-stimulated cAMP-mediated reporter gene activityAntagonist activity at human recombinant histamine H4 receptor expressed in SK-N-MC cells assessed as inhibition of forskolin-stimulated cAMP-mediated reporter gene activity
248 5 2 4 1.9 CN[C@@H]1CCN(c2ccnc(NCC(C)C)c2)C1
CHEMBL3393532 hrh4_human Human No 9.0 Kd = 1 nM Funct
Antagonist activity at human recombinant histamine H4 receptor expressed in SK-N-MC cells assessed as inhibition of forskolin-stimulated cAMP-mediated reporter gene activityAntagonist activity at human recombinant histamine H4 receptor expressed in SK-N-MC cells assessed as inhibition of forskolin-stimulated cAMP-mediated reporter gene activity
260 4 2 4 2.2 CN[C@@H]1CCN(c2ccnc(NC3CCCC3)c2)C1
CHEMBL3393535 hrh4_human Human No 9.0 Kd = 1 nM Funct
Antagonist activity at human recombinant histamine H4 receptor expressed in SK-N-MC cells assessed as inhibition of forskolin-stimulated cAMP-mediated reporter gene activityAntagonist activity at human recombinant histamine H4 receptor expressed in SK-N-MC cells assessed as inhibition of forskolin-stimulated cAMP-mediated reporter gene activity
286 4 2 4 2.5 CN[C@H]1CCN(c2ccnc(NC3CC4CCC3C4)c2)C1
CHEMBL1771000 hrh4_human Human No 8.9 Kd = 1.3 nM Funct
Antagonist activity at human histamine H4 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 6 hrsAntagonist activity at human histamine H4 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 6 hrs
264 4 2 6 0.9 CC(C)CNc1cc(N2CCN(C)CC2)nc(N)n1
CHEMBL1770969 hrh4_human Human No 8.8 Kd = 1.6 nM Funct
Antagonist activity at human histamine H4 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 6 hrsAntagonist activity at human histamine H4 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 6 hrs
249 4 3 5 1.3 CN[C@@H]1CCN(c2cc(N)nc(NC(C)C)c2)C1
CHEMBL1770971 hrh4_human Human No 8.8 Kd = 1.6 nM Funct
Antagonist activity at human histamine H4 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 6 hrsAntagonist activity at human histamine H4 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 6 hrs
263 5 3 5 1.5 CN[C@@H]1CCN(c2cc(N)nc(NCC(C)C)c2)C1
CHEMBL1770992 hrh4_human Human No 8.8 Kd = 1.6 nM Funct
Antagonist activity at human histamine H4 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 6 hrsAntagonist activity at human histamine H4 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 6 hrs
264 5 3 6 0.9 CN[C@@H]1CCN(c2cc(N)nc(NCC(C)C)n2)C1
CHEMBL505061 hrh4_human Human No 8.7 Kd = 2.0 nM Funct
Antagonist activity at human histamine H4 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 6 hrsAntagonist activity at human histamine H4 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 6 hrs
262 2 1 6 0.4 CN1CCN(c2cc(N3CCCC3)nc(N)n2)CC1
CHEMBL1914541 hrh4_human Human Yes 8.7 Kd = 2.0 nM Funct
Antagonist activity at recombinant human histamine H4 receptorAntagonist activity at recombinant human histamine H4 receptor
317 1 1 6 2.4 CN1CCN(c2nc(N)nc3c2oc2ccc(Cl)cc23)CC1
CHEMBL3236565 hrh4_human Human No 8.0 Kd = 10 nM Funct
Antagonist activity at human histamine H4 receptor expressed in SK-N-MC cells assessed as reduction of histamine-induced inhibition of cAMP-mediated beta-galactosidase reporter gene activity treated 10 mins prior to histamine challenge by microplate reader analysisAntagonist activity at human histamine H4 receptor expressed in SK-N-MC cells assessed as reduction of histamine-induced inhibition of cAMP-mediated beta-galactosidase reporter gene activity treated 10 mins prior to histamine challenge by microplate reader analysis
277 3 3 6 0.5 CN[C@H]1CN(c2cc(C3CCCC3)nc(N)n2)C[C@@H]1O
CHEMBL3236568 hrh4_human Human Yes 8.0 Kd = 10 nM Funct
Antagonist activity at human histamine H4 receptor expressed in SK-N-MC cells assessed as reduction of histamine-induced inhibition of cAMP-mediated beta-galactosidase reporter gene activity treated 10 mins prior to histamine challenge by microplate reader analysisAntagonist activity at human histamine H4 receptor expressed in SK-N-MC cells assessed as reduction of histamine-induced inhibition of cAMP-mediated beta-galactosidase reporter gene activity treated 10 mins prior to histamine challenge by microplate reader analysis
221 3 2 5 0.4 CCc1cc(N2CC[C@@H](NC)C2)nc(N)n1
CHEMBL3236572 hrh4_human Human No 8.0 Kd = 10 nM Funct
Antagonist activity at human histamine H4 receptor expressed in SK-N-MC cells assessed as reduction of histamine-induced inhibition of cAMP-mediated beta-galactosidase reporter gene activity treated 10 mins prior to histamine challenge by microplate reader analysisAntagonist activity at human histamine H4 receptor expressed in SK-N-MC cells assessed as reduction of histamine-induced inhibition of cAMP-mediated beta-galactosidase reporter gene activity treated 10 mins prior to histamine challenge by microplate reader analysis
283 4 2 5 1.4 CN[C@@H]1CCN(c2cc(Cc3ccccc3)nc(N)n2)C1
CHEMBL1770977 hrh4_human Human No 8.0 Kd = 10 nM Funct
Antagonist activity at human histamine H4 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 6 hrsAntagonist activity at human histamine H4 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 6 hrs
250 4 3 6 0.7 CN[C@@H]1CCN(c2cc(NC(C)C)nc(N)n2)C1
CHEMBL3393553 hrh4_human Human No 8.0 Kd = 10 nM Funct
Antagonist activity at human recombinant histamine H4 receptor expressed in SK-N-MC cells assessed as inhibition of forskolin-stimulated cAMP-mediated reporter gene activityAntagonist activity at human recombinant histamine H4 receptor expressed in SK-N-MC cells assessed as inhibition of forskolin-stimulated cAMP-mediated reporter gene activity
261 4 2 5 1.6 CN[C@@H]1CCN(c2cnnc(NC3CCCC3)c2)C1
CHEMBL3393556 hrh4_human Human No 8.0 Kd = 10 nM Funct
Antagonist activity at human recombinant histamine H4 receptor expressed in SK-N-MC cells assessed as inhibition of forskolin-stimulated cAMP-mediated reporter gene activityAntagonist activity at human recombinant histamine H4 receptor expressed in SK-N-MC cells assessed as inhibition of forskolin-stimulated cAMP-mediated reporter gene activity
287 4 2 5 1.9 CN[C@@H]1CCN(c2cnnc(NC3CC4CCC3C4)c2)C1
CHEMBL3236553 hrh4_mouse Mouse Yes 8.0 Kd = 10 nM Funct
Antagonist activity at mouse histamine H4 receptor expressed in SK-N-MC cells assessed as reduction of histamine-induced inhibition of cAMP-mediated beta-galactosidase reporter gene activity treated 10 mins prior to histamine challenge by microplate reader analysisAntagonist activity at mouse histamine H4 receptor expressed in SK-N-MC cells assessed as reduction of histamine-induced inhibition of cAMP-mediated beta-galactosidase reporter gene activity treated 10 mins prior to histamine challenge by microplate reader analysis
247 2 2 5 1.1 Nc1nc(C2CCCC2)cc(N2CCNCC2)n1
CHEMBL1914750 hrh4_human Human No 8.0 Kd = 10 nM Funct
Antagonist activity at recombinant human histamine H4 receptorAntagonist activity at recombinant human histamine H4 receptor
317 2 2 6 2.4 CNC1CCN(c2nc(N)nc3c2oc2ccc(Cl)cc23)C1
CHEMBL338937 hrh4_human Human No 8.0 Kd = 10 nM Funct
Antagonistic activity at human histamine H4 receptor in SK-N-MC cells by inhibition of forskolin-stimulated cAMP-mediated reporter gene activityAntagonistic activity at human histamine H4 receptor in SK-N-MC cells by inhibition of forskolin-stimulated cAMP-mediated reporter gene activity
311 1 1 2 2.9 CN1CCN(C(=O)c2cc3cc(Cl)cc(Cl)c3[nH]2)CC1
CHEMBL129198 hrh4_human Human Yes 8.0 Kd = 10 nM Bind
pA2 value against histamine h4 receptorpA2 value against histamine h4 receptor
277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl
CHEMBL2376803 hrh4_human Human No 8.0 Kd = 10.2 nM Bind
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells by competitive kinetic analysisDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells by competitive kinetic analysis
298 3 2 6 1.7 CNC1CN(c2nc(N)nc3cc(C4CCCC4)cnc23)C1
CHEMBL213912 hrh4_human Human Yes 8.0 Kd = 10.7 nM Bind
Displacement of [3H]histamine from human histamine H4 receptor transfected in SK-N-MC cellsDisplacement of [3H]histamine from human histamine H4 receptor transfected in SK-N-MC cells
327 0 0 4 3.8 CN1CCN(CC1)C2=NC3=C(C=C(C=C3)Cl)OC4=CC=CC=C42
CHEMBL4635634 hrh4_human Human No 8.0 Kd = 10.7 nM Bind
Binding affinity to human recombinant NLuc/GPCR-fused H4R expressed in HEK293T cells assessed as dissociation constant measured after 30 mins in presence of thioperamide by furimazine substrate based BRET assayBinding affinity to human recombinant NLuc/GPCR-fused H4R expressed in HEK293T cells assessed as dissociation constant measured after 30 mins in presence of thioperamide by furimazine substrate based BRET assay
401 9 1 2 5.1 Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCCCc1c[nH]cn1
CHEMBL4650570 hrh4_human Human No 8.0 Kd = 10.7 nM Bind
Binding affinity to human recombinant NLuc/GPCR-fused H4R expressed in HEK293T cells assessed as dissociation constant measured after 30 mins in presence of thioperamide by furimazine substrate based BRET assayBinding affinity to human recombinant NLuc/GPCR-fused H4R expressed in HEK293T cells assessed as dissociation constant measured after 30 mins in presence of thioperamide by furimazine substrate based BRET assay
401 9 1 2 5.1 Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCCCc1c[nH]cn1
CHEMBL42 hrh4_human Human Yes 7.9 Kd = 11.9 nM Bind
Displacement of [3H]histamine from human histamine H4 receptor transfected in SK-N-MC cellsDisplacement of [3H]histamine from human histamine H4 receptor transfected in SK-N-MC cells
326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2
CHEMBL3236549 hrh4_human Human Yes 7.9 Kd = 12.6 nM Funct
Antagonist activity at human histamine H4 receptor expressed in SK-N-MC cells assessed as reduction of histamine-induced inhibition of cAMP-mediated beta-galactosidase reporter gene activity treated 10 mins prior to histamine challenge by microplate reader analysisAntagonist activity at human histamine H4 receptor expressed in SK-N-MC cells assessed as reduction of histamine-induced inhibition of cAMP-mediated beta-galactosidase reporter gene activity treated 10 mins prior to histamine challenge by microplate reader analysis
221 2 2 5 0.7 N[C@@H]1CCN(C1)c1cc(nc(n1)N)C(C)C
CHEMBL3236569 hrh4_human Human No 7.9 Kd = 12.6 nM Funct
Antagonist activity at human histamine H4 receptor expressed in SK-N-MC cells assessed as reduction of histamine-induced inhibition of cAMP-mediated beta-galactosidase reporter gene activity treated 10 mins prior to histamine challenge by microplate reader analysisAntagonist activity at human histamine H4 receptor expressed in SK-N-MC cells assessed as reduction of histamine-induced inhibition of cAMP-mediated beta-galactosidase reporter gene activity treated 10 mins prior to histamine challenge by microplate reader analysis
207 2 2 5 0.2 CCc1cc(N2CC[C@@H](N)C2)nc(N)n1
CHEMBL3236570 hrh4_human Human No 7.9 Kd = 12.6 nM Funct
Antagonist activity at human histamine H4 receptor expressed in SK-N-MC cells assessed as reduction of histamine-induced inhibition of cAMP-mediated beta-galactosidase reporter gene activity treated 10 mins prior to histamine challenge by microplate reader analysisAntagonist activity at human histamine H4 receptor expressed in SK-N-MC cells assessed as reduction of histamine-induced inhibition of cAMP-mediated beta-galactosidase reporter gene activity treated 10 mins prior to histamine challenge by microplate reader analysis
235 3 2 5 1.0 CN[C@@H]1CCN(c2cc(C(C)C)nc(N)n2)C1
CHEMBL1770959 hrh4_human Human No 7.9 Kd = 12.6 nM Funct
Antagonist activity at human histamine H4 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 6 hrsAntagonist activity at human histamine H4 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 6 hrs
276 4 3 6 1.2 CN[C@@H]1CCN(c2cc(N)nc(NC3CCCC3)n2)C1
CHEMBL1770990 hrh4_human Human No 7.9 Kd = 12.6 nM Funct
Antagonist activity at human histamine H4 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 6 hrsAntagonist activity at human histamine H4 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 6 hrs
250 4 3 6 0.7 CN[C@@H]1CCN(c2cc(N)nc(NC(C)C)n2)C1
CHEMBL364400 hrh4_human Human Yes 7.9 Kd = 12.6 nM Funct
Antagonistic activity at human histamine H4 receptor in SK-N-MC cells by inhibition of forskolin-stimulated cAMP-mediated reporter gene activityAntagonistic activity at human histamine H4 receptor in SK-N-MC cells by inhibition of forskolin-stimulated cAMP-mediated reporter gene activity
283 1 1 3 2.3 CN1CCN(C(=O)c2cc3cc(Cl)sc3[nH]2)CC1
CHEMBL1083098 hrh4_human Human No 7.9 Kd = 12.6 nM Funct
Intrinsic activity at human histamine H4 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-induced cAMP responsive element-beta-galactosidase activity after 6 hrs by colorimetric cAMP assayIntrinsic activity at human histamine H4 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-induced cAMP responsive element-beta-galactosidase activity after 6 hrs by colorimetric cAMP assay
408 6 2 4 4.0 Cc1cc(OCCCN2CC3CCNC3C2)ccc1-c1nc2c(C)c(F)ccc2[nH]1
CHEMBL3233048 hrh4_human Human No 6.9 Kd = 125.9 nM Funct
Antagonist activity at human histamine H4 receptor expressed in SK-N-MC cells assessed as reduction of histamine-induced inhibition of cAMP-mediated beta-galactosidase reporter gene activity treated 10 mins prior to histamine challenge by microplate reader analysisAntagonist activity at human histamine H4 receptor expressed in SK-N-MC cells assessed as reduction of histamine-induced inhibition of cAMP-mediated beta-galactosidase reporter gene activity treated 10 mins prior to histamine challenge by microplate reader analysis
289 2 2 6 0.9 Nc1nc(C2CCCC2)cc(N2C[C@H]3NCCO[C@@H]3C2)n1
CHEMBL120854 hrh4_human Human No 6.9 Kd = 125.9 nM Funct
Antagonistic activity at human histamine H4 receptor in SK-N-MC cells by inhibition of forskolin-stimulated cAMP-mediated reporter gene activityAntagonistic activity at human histamine H4 receptor in SK-N-MC cells by inhibition of forskolin-stimulated cAMP-mediated reporter gene activity
292 1 1 3 1.9 Cc1cc(Cl)c2nc(C(=O)N3CCN(C)CC3)[nH]c2c1
CHEMBL128252 hrh4_human Human Yes 6.9 Kd = 125.9 nM Funct
Antagonistic activity at human histamine H4 receptor in SK-N-MC cells by inhibition of forskolin-stimulated cAMP-mediated reporter gene activityAntagonistic activity at human histamine H4 receptor in SK-N-MC cells by inhibition of forskolin-stimulated cAMP-mediated reporter gene activity
321 1 1 2 2.3 CN1CCN(C(=O)c2cc3cccc(Br)c3[nH]2)CC1
CHEMBL213912 hrh4_human Human Yes 7.9 Kd = 13 nM Bind
Displacement of [3H]histamine from human histamine H4 receptor transfected in SK-N-MC cells at 10 nMDisplacement of [3H]histamine from human histamine H4 receptor transfected in SK-N-MC cells at 10 nM
327 0 0 4 3.8 CN1CCN(CC1)C2=NC3=C(C=C(C=C3)Cl)OC4=CC=CC=C42