Purchasability


Ligand source activities (1 row/activity)

Select all ChEMBL ID Receptor Species Purchasable p-value
(-log)		 Activity
Type		 Activity
Relation		 Activity
Value		 Unit Assay Type Assay Description Mol
weight		 Rot
Bonds		 H don H acc LogP Smiles
CHEMBL1083162 hrh4_human Human No 9.3 EC50 = 0.6 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 5 4.0 CC1=C(C=CC(=C1)OCCCNCCC2=CN=CN2)C3=NC4=C(N3)C=CC(=C4C)F
CHEMBL1083162 hrh4_human Human No 9.3 EC50 = 0.6 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 5 4.0 CC1=C(C=CC(=C1)OCCCNCCC2=CN=CN2)C3=NC4=C(N3)C=CC(=C4C)F
CHEMBL1688946 hrh4_human Human No 9.0 EC50 = 1 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 3 3.1 C1CCC(CC1)CC2=CN(N=N2)CCCC3=CN=CN3
CHEMBL1688946 hrh4_human Human No 9.0 EC50 = 1 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 3 3.1 C1CCC(CC1)CC2=CN(N=N2)CCCC3=CN=CN3
CHEMBL595180 hrh4_human Human Yes 9.0 EC50 = 1.1 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
367 4 2 6 3.2 CN1CCN(CC1)C2=CC(=NC(=N2)N)NCC3=C(C=CC=C3Cl)Cl
CHEMBL595180 hrh4_human Human Yes 9.0 EC50 = 1.1 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
367 4 2 6 3.2 CN1CCN(CC1)C2=CC(=NC(=N2)N)NCC3=C(C=CC=C3Cl)Cl
CHEMBL595180 hrh4_human Human Yes 8.9 EC50 = 1.4 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
367 4 2 6 3.2 CN1CCN(CC1)C2=CC(=NC(=N2)N)NCC3=C(C=CC=C3Cl)Cl
CHEMBL595180 hrh4_human Human Yes 8.9 EC50 = 1.4 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
367 4 2 6 3.2 CN1CCN(CC1)C2=CC(=NC(=N2)N)NCC3=C(C=CC=C3Cl)Cl
CHEMBL1632413 hrh4_mouse Mouse No 8.0 EC50 = 10 Funct
Agonist activity at mouse histamine H4 receptor by luciferase reporter gene assayAgonist activity at mouse histamine H4 receptor by luciferase reporter gene assay
293 2 2 5 1.5 CN1CCN(CC1)C(=C2C=C3C=C(C=CC3=N2)Cl)NO
CHEMBL1632413 hrh4_rat Rat No 8.0 EC50 = 10 Funct
Agonist activity at rat histamine H4 receptor by luciferase reporter gene assayAgonist activity at rat histamine H4 receptor by luciferase reporter gene assay
293 2 2 5 1.5 CN1CCN(CC1)C(=C2C=C3C=C(C=CC3=N2)Cl)NO
CHEMBL502347 hrh4_rat Rat No 8.0 EC50 = 10 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 2.1 C1CC2=CC=CC=C2C3=C(C1)C(=NC(=N3)N)N4CCC(C4)N
CHEMBL1632413 hrh4_mouse Mouse No 8.0 EC50 = 10 Funct
Agonist activity at mouse histamine H4 receptor by luciferase reporter gene assayAgonist activity at mouse histamine H4 receptor by luciferase reporter gene assay
293 2 2 5 1.5 CN1CCN(CC1)C(=C2C=C3C=C(C=CC3=N2)Cl)NO
CHEMBL1632413 hrh4_rat Rat No 8.0 EC50 = 10 Funct
Agonist activity at rat histamine H4 receptor by luciferase reporter gene assayAgonist activity at rat histamine H4 receptor by luciferase reporter gene assay
293 2 2 5 1.5 CN1CCN(CC1)C(=C2C=C3C=C(C=CC3=N2)Cl)NO
CHEMBL502347 hrh4_rat Rat No 8.0 EC50 = 10 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 2.1 C1CC2=CC=CC=C2C3=C(C1)C(=NC(=N3)N)N4CCC(C4)N
CHEMBL309819 hrh4_human Human No 7.0 EC50 = 100 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 0.8 CCNC(=S)NCCCCC1=CN=CN1
CHEMBL3804906 hrh4_human Human No 7.0 EC50 = 100 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 5 3 3 0.6 CN=C(NCC1CCC(C1)C2=CN=CN2)NC#N
CHEMBL1632412 hrh4_human Human No 7.0 EC50 = 100 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 4 1.5 CC1=CC2=CC(=C(C3CCN(CC3)C)NO)N=C2C=C1
CHEMBL309819 hrh4_human Human No 7.0 EC50 = 100 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 0.8 CCNC(=S)NCCCCC1=CN=CN1
CHEMBL3804906 hrh4_human Human No 7.0 EC50 = 100 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 5 3 3 0.6 CN=C(NCC1CCC(C1)C2=CN=CN2)NC#N
CHEMBL1632412 hrh4_human Human No 7.0 EC50 = 100 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 4 1.5 CC1=CC2=CC(=C(C3CCN(CC3)C)NO)N=C2C=C1
CHEMBL82298 hrh4_human Human Yes 6.0 EC50 = 1000 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 0.9 C1=CN=CC=C1CC2=CN=CN2
CHEMBL3393556 hrh4_human Human No 6.0 EC50 = 1000 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 1.8 CNC1CCN(C1)C2=CC(=NN=C2)NC3CC4CCC3C4
CHEMBL3220892 hrh4_human Human No 6.0 EC50 = 1000 Funct
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 8 2 3 1.7 CC(CC(=O)NC(=NCCCN1C=CN=C1)N)C2=CC=CC=C2
CHEMBL82298 hrh4_human Human Yes 6.0 EC50 = 1000 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 0.9 C1=CN=CC=C1CC2=CN=CN2
CHEMBL3393556 hrh4_human Human No 6.0 EC50 = 1000 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 1.8 CNC1CCN(C1)C2=CC(=NN=C2)NC3CC4CCC3C4
CHEMBL3220892 hrh4_human Human No 6.0 EC50 = 1000 Funct
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 8 2 3 1.7 CC(CC(=O)NC(=NCCCN1C=CN=C1)N)C2=CC=CC=C2
CHEMBL1771001 hrh4_human Human No 7.0 EC50 = 101 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 1.7 CN1CCN(CC1)C2=CC(=NC(=N2)N)NC3CCCC3
CHEMBL1771001 hrh4_human Human No 7.0 EC50 = 101 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 1.7 CN1CCN(CC1)C2=CC(=NC(=N2)N)NC3CCCC3
CHEMBL378788 hrh4_human Human No 7.0 EC50 = 102.3 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
362 1 0 3 3.7 CN1CCN(CC1)C2=NC3=C(C=CC(=C3)Cl)OC4=C2C=CC(=C4)Cl
CHEMBL596551 hrh4_human Human No 7.0 EC50 = 102.3 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 1.6 CN1CCN(CC1)C2=CC(=NC(=N2)N)NCC3=CC=C(C=C3)O
CHEMBL494890 hrh4_mouse Mouse No 7.0 EC50 = 102.3 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 C1CN(CCN1)C2=NC(=NC(=C2)C3=CC=C(C=C3)C#N)N
CHEMBL494576 hrh4_rat Rat No 7.0 EC50 = 102.3 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 6 -0.1 CN1CCN(CC1)C2=NC(=NC(=C2)C3=CN(C=N3)C)N
CHEMBL494724 hrh4_rat Rat No 7.0 EC50 = 102.3 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 1.8 CN1CCN(CC1)C2=NC(=NC(=C2)C3=CC(=CC=C3)OC)N
CHEMBL494890 hrh4_mouse Mouse No 7.0 EC50 = 102.3 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 C1CN(CCN1)C2=NC(=NC(=C2)C3=CC=C(C=C3)C#N)N
CHEMBL378788 hrh4_human Human No 7.0 EC50 = 102.3 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
362 1 0 3 3.7 CN1CCN(CC1)C2=NC3=C(C=CC(=C3)Cl)OC4=C2C=CC(=C4)Cl
CHEMBL596551 hrh4_human Human No 7.0 EC50 = 102.3 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 1.6 CN1CCN(CC1)C2=CC(=NC(=N2)N)NCC3=CC=C(C=C3)O
CHEMBL494890 hrh4_mouse Mouse No 7.0 EC50 = 102.3 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 C1CN(CCN1)C2=NC(=NC(=C2)C3=CC=C(C=C3)C#N)N
CHEMBL494576 hrh4_rat Rat No 7.0 EC50 = 102.3 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 6 -0.1 CN1CCN(CC1)C2=NC(=NC(=C2)C3=CN(C=N3)C)N
CHEMBL494724 hrh4_rat Rat No 7.0 EC50 = 102.3 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 1.8 CN1CCN(CC1)C2=NC(=NC(=C2)C3=CC(=CC=C3)OC)N
CHEMBL494890 hrh4_mouse Mouse No 7.0 EC50 = 102.3 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 C1CN(CCN1)C2=NC(=NC(=C2)C3=CC=C(C=C3)C#N)N
CHEMBL153051 hrh4_human Human Yes 6.0 EC50 = 1023.3 Funct
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 0.3 C1CNCC1CC2=CN=CN2
CHEMBL211242 hrh4_human Human No 7.0 EC50 = 104.7 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 1 0 3 2.8 CC1=CC2=C(C=C1)N=C(C3=CC=CC=C3O2)N4CCN(CC4)C
CHEMBL609161 hrh4_human Human No 7.0 EC50 = 104.7 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 2.3 CC1=CC=C(C=C1)CNC2=NC(=NC(=C2)N3CCN(CC3)C)N
CHEMBL211242 hrh4_human Human No 7.0 EC50 = 104.7 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 1 0 3 2.8 CC1=CC2=C(C=C1)N=C(C3=CC=CC=C3O2)N4CCN(CC4)C
CHEMBL609161 hrh4_human Human No 7.0 EC50 = 104.7 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 2.3 CC1=CC=C(C=C1)CNC2=NC(=NC(=C2)N3CCN(CC3)C)N
CHEMBL494910 hrh4_rat Rat Yes 5.0 EC50 = 10471.3 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 0.4 CN1CCN(CC1)C2=CC(=NC(=N2)N)OC
CHEMBL494910 hrh4_rat Rat Yes 5.0 EC50 = 10471.3 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 0.4 CN1CCN(CC1)C2=CC(=NC(=N2)N)OC
CHEMBL81644 hrh4_human Human Yes 5.0 EC50 = 10471.3 Funct
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 1.0 C1=CC=NC(=C1)CC2=CN=CN2
CHEMBL1078632 hrh4_human Human No 6.0 EC50 = 1096.5 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 10 3 3 2.3 C1=CC=C(C=C1)CCNC(=NCCCCC2=CN=CN2)NC#N
CHEMBL1078632 hrh4_human Human No 6.0 EC50 = 1096.5 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 10 3 3 2.3 C1=CC=C(C=C1)CCNC(=NCCCCC2=CN=CN2)NC#N
CHEMBL153284 hrh4_human Human Yes 6.0 EC50 = 1096.5 Funct
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 -0.4 C1C(C1C2=CN=CN2)CN
CHEMBL1770966 hrh4_human Human No 8.0 EC50 = 11 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 2.0 CN1CCN(CC1)C2=CC(=NC(=C2)NC3CCCC3)N
CHEMBL3805361 hrh4_human Human No 8.0 EC50 = 11 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
369 9 3 4 2.8 C1CC(CC1CN=C(NCCSC2=CC=CC=C2)NC#N)C3=CN=CN3
CHEMBL1770966 hrh4_human Human No 8.0 EC50 = 11 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 2.0 CN1CCN(CC1)C2=CC(=NC(=C2)NC3CCCC3)N
CHEMBL3805361 hrh4_human Human No 8.0 EC50 = 11 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
369 9 3 4 2.8 C1CC(CC1CN=C(NCCSC2=CC=CC=C2)NC#N)C3=CN=CN3
CHEMBL594731 hrh4_human Human No 7.9 EC50 = 11.8 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 2.3 CC1=CC=CC=C1CNC2=NC(=NC(=C2)N3CCN(CC3)C)N
CHEMBL594731 hrh4_human Human No 7.9 EC50 = 11.8 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 2.3 CC1=CC=CC=C1CNC2=NC(=NC(=C2)N3CCN(CC3)C)N
CHEMBL3805392 hrh4_human Human No 7.0 EC50 = 110 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
369 8 3 4 3.5 C1CC(CCC1C2=CN=CN2)NC(=NCCSC3=CC=CC=C3)NC#N
CHEMBL3805392 hrh4_human Human No 7.0 EC50 = 110 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
369 8 3 4 3.5 C1CC(CCC1C2=CN=CN2)NC(=NCCSC3=CC=CC=C3)NC#N
CHEMBL3805437 hrh4_human Human No 6.0 EC50 = 1100 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 5 3 3 0.6 CN=C(NCC1CCC(C1)C2=CN=CN2)NC#N
CHEMBL3805437 hrh4_human Human No 6.0 EC50 = 1100 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 5 3 3 0.6 CN=C(NCC1CCC(C1)C2=CN=CN2)NC#N
CHEMBL3806206 hrh4_human Human No 7.0 EC50 = 111 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 5 3 3 0.6 CN=C(NCC1CCC(C1)C2=CN=CN2)NC#N
CHEMBL3393536 hrh4_human Human Yes 7.0 EC50 = 112 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 1.6 CC(C)NC1=NC=CC(=N1)N2CCN(CC2)C
CHEMBL3393536 hrh4_human Human Yes 7.0 EC50 = 112 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 1.6 CC(C)NC1=NC=CC(=N1)N2CCN(CC2)C
CHEMBL493099 hrh4_rat Rat No 6.0 EC50 = 1122.0 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 5 1 5 2.1 CC(C)(C)C1=CC(=NC(=N1)N)N(C)CCN(C)C
CHEMBL493099 hrh4_rat Rat No 6.0 EC50 = 1122.0 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 5 1 5 2.1 CC(C)(C)C1=CC(=NC(=N1)N)N(C)CCN(C)C
CHEMBL268229 hrh4_human Human Yes 6.0 EC50 = 1122.0 Funct
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 CC(CC1=CN=CN1)N
CHEMBL494648 hrh4_rat Rat No 6.9 EC50 = 114.8 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 1.8 CN1CCN(CC1)C2=NC(=NC(=C2)C3=CC=C(C=C3)OC)N
CHEMBL501882 hrh4_rat Rat Yes 6.9 EC50 = 114.8 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 0.1 CN1CCN(CC1)C2=NC(=NC=C2)N
CHEMBL494648 hrh4_rat Rat No 6.9 EC50 = 114.8 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 1.8 CN1CCN(CC1)C2=NC(=NC(=C2)C3=CC=C(C=C3)OC)N
CHEMBL501882 hrh4_rat Rat Yes 6.9 EC50 = 114.8 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 0.1 CN1CCN(CC1)C2=NC(=NC=C2)N
CHEMBL449157 hrh4_human Human No 4.9 EC50 = 11481.5 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 3 0 5 2.6 CC(C)(C)C1=CC(=NC(=N1)N(C)C)N2CCN(CC2)C
CHEMBL449157 hrh4_human Human No 4.9 EC50 = 11481.5 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 3 0 5 2.6 CC(C)(C)C1=CC(=NC(=N1)N(C)C)N2CCN(CC2)C
CHEMBL1632410 hrh4_human Human No 4.9 EC50 = 11481.5 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 1.7 C1CC(OC1COCC2=CC=CC=C2)C3=CN=CN3
CHEMBL502104 hrh4_rat Rat No 6.9 EC50 = 117.5 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 2.0 CN1CCN(CC1)C2=NC(=NC(=C2)NC3=CC=CC=C3)N
CHEMBL502104 hrh4_rat Rat No 6.9 EC50 = 117.5 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 2.0 CN1CCN(CC1)C2=NC(=NC(=C2)NC3=CC=CC=C3)N
CHEMBL3806206 hrh4_human Human No 6.9 EC50 = 119 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 5 3 3 0.6 CN=C(NCC1CCC(C1)C2=CN=CN2)NC#N
CHEMBL3806206 hrh4_human Human No 6.9 EC50 = 119 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 5 3 3 0.6 CN=C(NCC1CCC(C1)C2=CN=CN2)NC#N
CHEMBL1082296 hrh4_mouse Mouse No 5.9 EC50 = 1197 Funct
Displacement of [3H]histamine from mouse recombinant histamine H4 receptorDisplacement of [3H]histamine from mouse recombinant histamine H4 receptor
423 6 2 5 4.5 CC1=C(C=CC(=C1)OCCCN2CC3CCCNC3C2)C4=NC5=C(N4)C=CC(=C5C)F
CHEMBL1082296 hrh4_mouse Mouse No 5.9 EC50 = 1197 Funct
Displacement of [3H]histamine from mouse recombinant histamine H4 receptorDisplacement of [3H]histamine from mouse recombinant histamine H4 receptor
423 6 2 5 4.5 CC1=C(C=CC(=C1)OCCCN2CC3CCCNC3C2)C4=NC5=C(N4)C=CC(=C5C)F
CHEMBL1770998 hrh4_human Human No 7.9 EC50 = 12 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 1.2 CC(C)NC1=NC(=NC(=C1)N2CCN(CC2)C)N
CHEMBL1086105 hrh4_mouse Mouse No 7.9 EC50 = 12 Funct
Displacement of [3H]histamine from mouse recombinant histamine H4 receptorDisplacement of [3H]histamine from mouse recombinant histamine H4 receptor
420 6 2 5 4.1 CC1=C(C=CC(=C1)OCCCN2CCC3=C(C2)NC=N3)C4=NC5=C(N4)C=CC(=C5C)F
CHEMBL1770998 hrh4_human Human No 7.9 EC50 = 12 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 1.2 CC(C)NC1=NC(=NC(=C1)N2CCN(CC2)C)N
CHEMBL1086105 hrh4_mouse Mouse No 7.9 EC50 = 12 Funct
Displacement of [3H]histamine from mouse recombinant histamine H4 receptorDisplacement of [3H]histamine from mouse recombinant histamine H4 receptor
420 6 2 5 4.1 CC1=C(C=CC(=C1)OCCCN2CCC3=C(C2)NC=N3)C4=NC5=C(N4)C=CC(=C5C)F
CHEMBL19439 hrh4_human Human Yes 7.9 EC50 = 12.6 Funct
Agonist activity at human histamine H4 receptorAgonist activity at human histamine H4 receptor
170 4 3 3 0.2 C1=C(NC=N1)CCSC(=N)N
CHEMBL19439 hrh4_human Human Yes 7.9 EC50 = 12.6 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 4 3 3 0.2 C1=C(NC=N1)CCSC(=N)N
CHEMBL281576 hrh4_human Human Yes 7.9 EC50 = 12.6 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 5 3 3 0.7 C1=C(NC=N1)CCCSC(=N)N
CHEMBL19439 hrh4_human Human Yes 7.9 EC50 = 12.6 Funct
Agonist activity at human histamine H4 receptorAgonist activity at human histamine H4 receptor
170 4 3 3 0.2 C1=C(NC=N1)CCSC(=N)N
CHEMBL19439 hrh4_human Human Yes 7.9 EC50 = 12.6 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 4 3 3 0.2 C1=C(NC=N1)CCSC(=N)N
CHEMBL281576 hrh4_human Human Yes 7.9 EC50 = 12.6 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 5 3 3 0.7 C1=C(NC=N1)CCCSC(=N)N
CHEMBL1078346 hrh4_human Human No 6.9 EC50 = 120.2 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 9 3 3 1.3 CC(C)CN=C(NCCCCC1=CN=CN1)NC#N
CHEMBL1078346 hrh4_human Human No 6.9 EC50 = 120.2 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 9 3 3 1.3 CC(C)CN=C(NCCCCC1=CN=CN1)NC#N
CHEMBL492489 hrh4_human Human No 5.9 EC50 = 1202.3 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 3 0 5 2.5 CC(C)(C)C1=CC(=NC(=N1)OC)N2CCN(CC2)C
CHEMBL1077737 hrh4_human Human No 5.9 EC50 = 1202.3 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 11 3 4 1.6 C1=CC(=CN=C1)CCCN=C(NCCCCC2=CN=CN2)NC#N
CHEMBL495083 hrh4_rat Rat No 5.9 EC50 = 1202.3 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 1.5 CN1CCN(CC1)C2=NC(=NC(=C2)C3=CC=CC=C3C#N)N
CHEMBL492489 hrh4_human Human No 5.9 EC50 = 1202.3 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 3 0 5 2.5 CC(C)(C)C1=CC(=NC(=N1)OC)N2CCN(CC2)C
CHEMBL1077737 hrh4_human Human No 5.9 EC50 = 1202.3 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 11 3 4 1.6 C1=CC(=CN=C1)CCCN=C(NCCCCC2=CN=CN2)NC#N
CHEMBL495083 hrh4_rat Rat No 5.9 EC50 = 1202.3 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 1.5 CN1CCN(CC1)C2=NC(=NC(=C2)C3=CC=CC=C3C#N)N
CHEMBL494678 hrh4_mouse Mouse Yes 6.9 EC50 = 123.0 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 1.5 CN1CCN(CC1)C2=NC(=NC(=C2)C3=CC=C(C=C3)C#N)N
CHEMBL494678 hrh4_mouse Mouse Yes 6.9 EC50 = 123.0 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 1.5 CN1CCN(CC1)C2=NC(=NC(=C2)C3=CC=C(C=C3)C#N)N
CHEMBL494678 hrh4_mouse Mouse Yes 6.9 EC50 = 123.0 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 1.5 CN1CCN(CC1)C2=NC(=NC(=C2)C3=CC=C(C=C3)C#N)N
CHEMBL494678 hrh4_mouse Mouse Yes 6.9 EC50 = 123.0 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 1.5 CN1CCN(CC1)C2=NC(=NC(=C2)C3=CC=C(C=C3)C#N)N
CHEMBL493663 hrh4_rat Rat No 4.9 EC50 = 12302.7 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 -0.6 CN1CCN(CC1)C2=NC(=NC(=C2)N3CCNC3=O)N
CHEMBL493663 hrh4_rat Rat No 4.9 EC50 = 12302.7 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 -0.6 CN1CCN(CC1)C2=NC(=NC(=C2)N3CCNC3=O)N
CHEMBL3806098 hrh4_human Human No 6.9 EC50 = 125 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 9 3 3 2.9 C1CC(CC1CN=C(NCCCC2=CC=CC=C2)NC#N)C3=CN=CN3
CHEMBL3806098 hrh4_human Human No 6.9 EC50 = 125 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 9 3 3 2.9 C1CC(CC1CN=C(NCCCC2=CC=CC=C2)NC#N)C3=CN=CN3
CHEMBL320331 hrh4_human Human No 6.9 EC50 = 125.9 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 1.7 C1CC(OC1COCC2=CC=CC=C2)C3=CN=CN3
CHEMBL320331 hrh4_human Human No 6.9 EC50 = 125.9 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 1.7 C1CC(OC1COCC2=CC=CC=C2)C3=CN=CN3
CHEMBL308913 hrh4_human Human No 5.9 EC50 = 1258.9 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 C1=CC=C(C=C1)CCNC(=S)NCCCCC2=CN=CN2
CHEMBL308913 hrh4_human Human No 5.9 EC50 = 1258.9 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 C1=CC=C(C=C1)CCNC(=S)NCCCCC2=CN=CN2
CHEMBL78497 hrh4_human Human No 5.9 EC50 = 1258.9 Funct
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 1.6 C1=CC(=CN=C1)CCCC2=CN=CN2
CHEMBL11919 hrh4_human Human Yes 4.9 EC50 = 12589.3 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 CC(CC1=CN=CN1)N
CHEMBL1632410 hrh4_human Human No 4.9 EC50 = 12589.3 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 1.7 C1CC(OC1COCC2=CC=CC=C2)C3=CN=CN3
CHEMBL322256 hrh4_human Human No 4.9 EC50 = 12589.3 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 1.7 C1CC(OC1COCC2=CC=CC=C2)C3=CN=CN3
CHEMBL11919 hrh4_human Human Yes 4.9 EC50 = 12589.3 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 CC(CC1=CN=CN1)N
CHEMBL1632410 hrh4_human Human No 4.9 EC50 = 12589.3 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 1.7 C1CC(OC1COCC2=CC=CC=C2)C3=CN=CN3
CHEMBL322256 hrh4_human Human No 4.9 EC50 = 12589.3 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 1.7 C1CC(OC1COCC2=CC=CC=C2)C3=CN=CN3
CHEMBL1078529 hrh4_human Human No 5.9 EC50 = 1288.3 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 10 3 4 2.2 C1=CC=C(C=C1)SCCNC(=NCCCC2=CN=CN2)NC#N
CHEMBL1078529 hrh4_human Human No 5.9 EC50 = 1288.3 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 10 3 4 2.2 C1=CC=C(C=C1)SCCNC(=NCCCC2=CN=CN2)NC#N
CHEMBL322256 hrh4_human Human No 4.9 EC50 = 12882.5 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 1.7 C1CC(OC1COCC2=CC=CC=C2)C3=CN=CN3
CHEMBL3806079 hrh4_human Human No 6.9 EC50 = 129 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
369 9 3 4 2.8 C1CC(CC1CN=C(NCCSC2=CC=CC=C2)NC#N)C3=CN=CN3
CHEMBL3806079 hrh4_human Human No 6.9 EC50 = 129 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
369 9 3 4 2.8 C1CC(CC1CN=C(NCCSC2=CC=CC=C2)NC#N)C3=CN=CN3
CHEMBL3236558 hrh4_human Human No 5.9 EC50 = 1300 Funct
Agonist activity at human H4 receptorAgonist activity at human H4 receptor
233 2 2 5 0.9 C1CCC(C1)C2=CC(=NC(=N2)N)N3CC(C3)N
CHEMBL3236558 hrh4_human Human No 5.9 EC50 = 1300 Funct
Agonist activity at human H4 receptorAgonist activity at human H4 receptor
233 2 2 5 0.9 C1CCC(C1)C2=CC(=NC(=N2)N)N3CC(C3)N
CHEMBL320331 hrh4_human Human No 6.9 EC50 = 134.9 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 1.7 C1CC(OC1COCC2=CC=CC=C2)C3=CN=CN3
CHEMBL492869 hrh4_rat Rat No 5.9 EC50 = 1349.0 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(CC1)C2=CC(=NC(=N2)N)N3CCN(CC3)C
CHEMBL492869 hrh4_rat Rat No 5.9 EC50 = 1349.0 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(CC1)C2=CC(=NC(=N2)N)N3CCN(CC3)C
CHEMBL1094144 hrh4_human Human No 5.9 EC50 = 1380.4 Funct
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
366 8 3 5 4.3 CC1=C(SC(=N1)N)CCCN=C(N)NC(=O)CC(C)C2CCCCC2
CHEMBL1094144 hrh4_human Human No 5.9 EC50 = 1380.4 Funct
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
366 8 3 5 4.3 CC1=C(SC(=N1)N)CCCN=C(N)NC(=O)CC(C)C2CCCCC2
CHEMBL3805361 hrh4_human Human No 7.9 EC50 = 14 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
369 9 3 4 2.8 C1CC(CC1CN=C(NCCSC2=CC=CC=C2)NC#N)C3=CN=CN3
CHEMBL209758 hrh4_human Human No 7.8 EC50 = 14.8 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
346 1 0 4 3.2 CN1CCN(CC1)C2=NC3=C(C=CC(=C3)Cl)OC4=C2C=CC=C4F
CHEMBL211170 hrh4_human Human No 7.8 EC50 = 14.8 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
362 1 0 3 3.7 CN1CCN(CC1)C2=NC3=C(C=C(C=C3)Cl)OC4=C2C=CC=C4Cl
CHEMBL509540 hrh4_rat Rat Yes 7.8 EC50 = 14.8 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 2.2 C1CC2=CC=CC=C2C3=C(C1)C(=NC(=N3)N)N4CCNCC4
CHEMBL209758 hrh4_human Human No 7.8 EC50 = 14.8 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
346 1 0 4 3.2 CN1CCN(CC1)C2=NC3=C(C=CC(=C3)Cl)OC4=C2C=CC=C4F
CHEMBL211170 hrh4_human Human No 7.8 EC50 = 14.8 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
362 1 0 3 3.7 CN1CCN(CC1)C2=NC3=C(C=C(C=C3)Cl)OC4=C2C=CC=C4Cl
CHEMBL509540 hrh4_rat Rat Yes 7.8 EC50 = 14.8 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 2.2 C1CC2=CC=CC=C2C3=C(C1)C(=NC(=N3)N)N4CCNCC4
CHEMBL1077860 hrh4_human Human No 6.9 EC50 = 141.3 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 11 3 3 3.0 CC(CCNC(=NCCCCC1=CN=CN1)NC#N)C2=CC=CC=C2
CHEMBL1077860 hrh4_human Human No 6.9 EC50 = 141.3 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 11 3 3 3.0 CC(CCNC(=NCCCCC1=CN=CN1)NC#N)C2=CC=CC=C2
CHEMBL493664 hrh4_rat Rat No 4.9 EC50 = 14125.4 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 6 0.5 CN1CCN(CC1)C2=NC(=NC(=C2)N3C=CC=CC3=O)N
CHEMBL493664 hrh4_rat Rat No 4.9 EC50 = 14125.4 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 6 0.5 CN1CCN(CC1)C2=NC(=NC(=C2)N3C=CC=CC3=O)N
CHEMBL494909 hrh4_rat Rat Yes 5.8 EC50 = 1479.1 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 3 -1.2 CN1CCN(CC1)C2=CC(=O)N=C(N2)N
CHEMBL494909 hrh4_rat Rat Yes 5.8 EC50 = 1479.1 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 3 -1.2 CN1CCN(CC1)C2=CC(=O)N=C(N2)N
CHEMBL3806255 hrh4_human Human No 7.8 EC50 = 15 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 7 3 3 1.9 CC(C)CN=C(NCC1CCC(C1)C2=CN=CN2)NC#N
CHEMBL3393539 hrh4_human Human No 7.8 EC50 = 15 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 2.1 CC(C)CNC1=NC=CC(=N1)N2CCC(C2)NC
CHEMBL3806255 hrh4_human Human No 7.8 EC50 = 15 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 7 3 3 1.9 CC(C)CN=C(NCC1CCC(C1)C2=CN=CN2)NC#N
CHEMBL3393539 hrh4_human Human No 7.8 EC50 = 15 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 2.1 CC(C)CNC1=NC=CC(=N1)N2CCC(C2)NC
CHEMBL483406 hrh4_human Human No 7.8 EC50 = 15.1 Funct
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 8 3 3 2.1 CC(CC(=O)NC(=NCCCC1=CN=CN1)N)C2=CC=CC=C2
CHEMBL483406 hrh4_human Human No 7.8 EC50 = 15.1 Funct
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 8 3 3 2.1 CC(CC(=O)NC(=NCCCC1=CN=CN1)N)C2=CC=CC=C2
CHEMBL483406 hrh4_human Human No 7.8 EC50 = 15.1 Funct
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 8 3 3 2.1 CC(CC(=O)NC(=NCCCC1=CN=CN1)N)C2=CC=CC=C2
CHEMBL483406 hrh4_human Human No 7.8 EC50 = 15.3 Funct
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 8 3 3 2.1 CC(CC(=O)NC(=NCCCC1=CN=CN1)N)C2=CC=CC=C2
CHEMBL483406 hrh4_human Human No 7.8 EC50 = 15.3 Funct
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 8 3 3 2.1 CC(CC(=O)NC(=NCCCC1=CN=CN1)N)C2=CC=CC=C2
CHEMBL492242 hrh4_rat Rat No 7.8 EC50 = 15.5 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 8 1.6 CN1CCN(CC1)C2=NC(=NC(=C2)C3=C(N=C(C=C3)F)F)N
CHEMBL494093 hrh4_rat Rat No 7.8 EC50 = 15.5 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 2.1 CN1CCN(CC1)C2=NC(=NC3=C2CCC4=CC=CC=C43)N
CHEMBL492242 hrh4_rat Rat No 7.8 EC50 = 15.5 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 8 1.6 CN1CCN(CC1)C2=NC(=NC(=C2)C3=C(N=C(C=C3)F)F)N
CHEMBL494093 hrh4_rat Rat No 7.8 EC50 = 15.5 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 2.1 CN1CCN(CC1)C2=NC(=NC3=C2CCC4=CC=CC=C43)N
CHEMBL483406 hrh4_human Human No 7.8 EC50 = 15.9 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 8 3 3 2.1 CC(CC(=O)NC(=NCCCC1=CN=CN1)N)C2=CC=CC=C2
CHEMBL470790 hrh4_human Human No 7.8 EC50 = 15.9 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 8 3 3 1.8 C1=CC=C(C=C1)CCC(=O)NC(=NCCCC2=CN=CN2)N
CHEMBL483406 hrh4_human Human No 7.8 EC50 = 15.9 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 8 3 3 2.1 CC(CC(=O)NC(=NCCCC1=CN=CN1)N)C2=CC=CC=C2
CHEMBL470790 hrh4_human Human No 7.8 EC50 = 15.9 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 8 3 3 1.8 C1=CC=C(C=C1)CCC(=O)NC(=NCCCC2=CN=CN2)N
CHEMBL3805995 hrh4_human Human No 6.8 EC50 = 150 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 0.3 C1CC(CC1CN)C2=CN=CN2
CHEMBL1083084 hrh4_human Human No 6.8 EC50 = 150 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
411 7 1 5 4.6 CC1=C(C=CC(=C1)OCCCN2CCC(C2)N(C)C)C3=NC4=C(N3)C=CC(=C4C)F
CHEMBL3805995 hrh4_human Human No 6.8 EC50 = 150 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 0.3 C1CC(CC1CN)C2=CN=CN2
CHEMBL1083084 hrh4_human Human No 6.8 EC50 = 150 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
411 7 1 5 4.6 CC1=C(C=CC(=C1)OCCCN2CCC(C2)N(C)C)C3=NC4=C(N3)C=CC(=C4C)F
CHEMBL474617 hrh4_human Human No 6.8 EC50 = 151.4 Funct
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 9 4 4 1.5 CN(CCC(=O)NC(=NCCCC1=CN=CN1)N)C(=O)C2=CC3=CC=CC=C3N2
CHEMBL1078631 hrh4_human Human No 6.8 EC50 = 151.4 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 11 3 3 2.7 C1=CC=C(C=C1)CCCN=C(NCCCCC2=CN=CN2)NC#N
CHEMBL474617 hrh4_human Human No 6.8 EC50 = 151.4 Funct
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 9 4 4 1.5 CN(CCC(=O)NC(=NCCCC1=CN=CN1)N)C(=O)C2=CC3=CC=CC=C3N2
CHEMBL1078631 hrh4_human Human No 6.8 EC50 = 151.4 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 11 3 3 2.7 C1=CC=C(C=C1)CCCN=C(NCCCCC2=CN=CN2)NC#N
CHEMBL311473 hrh4_human Human Yes 5.8 EC50 = 1513.6 Funct
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 1.2 C1=CN=CC=C1CCC2=CN=CN2
CHEMBL78838 hrh4_human Human Yes 4.8 EC50 = 15135.6 Funct
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 0.9 C1=CC(=CN=C1)CC2=CN=CN2
CHEMBL309654 hrh4_human Human No 5.8 EC50 = 1548.8 Funct
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 1.6 C1=CN=CC=C1CCCC2=CN=CN2
CHEMBL1688969 hrh4_human Human No 6.8 EC50 = 158.5 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 3 2.8 C1CCC(CC1)CC2=CN(N=N2)CCC3=CN=CN3
CHEMBL1688969 hrh4_human Human No 6.8 EC50 = 158.5 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 3 2.8 C1CCC(CC1)CC2=CN(N=N2)CCC3=CN=CN3
CHEMBL12344 hrh4_human Human Yes 5.8 EC50 = 1584.9 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 5 2 3 0.6 CN(C)CCCSC(=N)N
CHEMBL24665 hrh4_human Human Yes 5.8 EC50 = 1584.9 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 5 2.0 C1=CC(=CC(=C1)C(F)(F)F)C2=NC=C(N2)CCN
CHEMBL275443 hrh4_mouse Mouse Yes 5.8 EC50 = 1584.9 Funct
Agonist activity at mouse histamine H4 receptorAgonist activity at mouse histamine H4 receptor
125 2 2 2 -0.2 CC1=C(N=CN1)CCN
CHEMBL12344 hrh4_human Human Yes 5.8 EC50 = 1584.9 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 5 2 3 0.6 CN(C)CCCSC(=N)N
CHEMBL24665 hrh4_human Human Yes 5.8 EC50 = 1584.9 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 5 2.0 C1=CC(=CC(=C1)C(F)(F)F)C2=NC=C(N2)CCN
CHEMBL275443 hrh4_mouse Mouse Yes 5.8 EC50 = 1584.9 Funct
Agonist activity at mouse histamine H4 receptorAgonist activity at mouse histamine H4 receptor
125 2 2 2 -0.2 CC1=C(N=CN1)CCN
CHEMBL1770987 hrh4_human Human No 7.8 EC50 = 16 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 1.7 CN1CCN(CC1)C2=CC(=NC(=N2)NC3CCCC3)N
CHEMBL1770987 hrh4_human Human No 7.8 EC50 = 16 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 1.7 CN1CCN(CC1)C2=CC(=NC(=N2)NC3CCCC3)N
CHEMBL3805361 hrh4_mouse Mouse No 6.8 EC50 = 166 Funct
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
369 9 3 4 2.8 C1CC(CC1CN=C(NCCSC2=CC=CC=C2)NC#N)C3=CN=CN3
CHEMBL3805361 hrh4_mouse Mouse No 6.8 EC50 = 166 Funct
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
369 9 3 4 2.8 C1CC(CC1CN=C(NCCSC2=CC=CC=C2)NC#N)C3=CN=CN3
CHEMBL454007 hrh4_rat Rat Yes 4.8 EC50 = 16982.4 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
228 1 1 5 1.1 CN1CCN(CC1)C2=CC(=NC(=N2)N)Cl
CHEMBL454007 hrh4_rat Rat Yes 4.8 EC50 = 16982.4 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
228 1 1 5 1.1 CN1CCN(CC1)C2=CC(=NC(=N2)N)Cl
CHEMBL503605 hrh4_mouse Mouse Yes 7.8 EC50 = 17.8 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
264 1 2 2 1.8 C1CN(CCN1)C(=O)C2=CC3=C(N2)C=CC(=C3)Cl
CHEMBL503605 hrh4_mouse Mouse Yes 7.8 EC50 = 17.8 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
264 1 2 2 1.8 C1CN(CCN1)C(=O)C2=CC3=C(N2)C=CC(=C3)Cl
CHEMBL3805813 hrh4_human Human No 5.8 EC50 = 1710 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 0.3 C1CC(CC1CN)C2=CN=CN2
CHEMBL3805813 hrh4_human Human No 5.8 EC50 = 1710 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 0.3 C1CC(CC1CN)C2=CN=CN2
CHEMBL522841 hrh4_rat Rat No 6.8 EC50 = 173.8 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 3.0 CN1CCN(CC1)C2=NC(=NC(=C2)C3=CC4=CC=CC=C4C=C3)N
CHEMBL522841 hrh4_rat Rat No 6.8 EC50 = 173.8 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 3.0 CN1CCN(CC1)C2=NC(=NC(=C2)C3=CC4=CC=CC=C4C=C3)N
CHEMBL495280 hrh4_human Human No 6.8 EC50 = 177.8 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 6 1.6 CN1CCN(CC1)C2=NC(=NC(=C2)N3C=NC4=CC=CC=C43)N
CHEMBL494723 hrh4_rat Rat No 6.8 EC50 = 177.8 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 2.1 CC1=CC=CC=C1C2=CC(=NC(=N2)N)N3CCN(CC3)C
CHEMBL495280 hrh4_human Human No 6.8 EC50 = 177.8 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 6 1.6 CN1CCN(CC1)C2=NC(=NC(=C2)N3C=NC4=CC=CC=C43)N
CHEMBL494723 hrh4_rat Rat No 6.8 EC50 = 177.8 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 2.1 CC1=CC=CC=C1C2=CC(=NC(=N2)N)N3CCN(CC3)C
CHEMBL499631 hrh4_rat Rat No 5.8 EC50 = 1778.3 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 5 2 5 1.9 CC(C)(C)C1=CC(=NC(=N1)N)NCCN(C)C
CHEMBL499631 hrh4_rat Rat No 5.8 EC50 = 1778.3 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 5 2 5 1.9 CC(C)(C)C1=CC(=NC(=N1)N)NCCN(C)C
CHEMBL509540 hrh4_mouse Mouse Yes 7.7 EC50 = 18.2 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 2.2 C1CC2=CC=CC=C2C3=C(C1)C(=NC(=N3)N)N4CCNCC4
CHEMBL509540 hrh4_mouse Mouse Yes 7.7 EC50 = 18.2 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 2.2 C1CC2=CC=CC=C2C3=C(C1)C(=NC(=N3)N)N4CCNCC4
CHEMBL445091 hrh4_rat Rat Yes 5.7 EC50 = 1819.7 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 0.1 CN1CCN(CC1)C2=NC(=NC(=C2)C3=CNN=C3)N
CHEMBL445091 hrh4_rat Rat Yes 5.7 EC50 = 1819.7 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 0.1 CN1CCN(CC1)C2=NC(=NC(=C2)C3=CNN=C3)N
CHEMBL449157 hrh4_rat Rat No 4.7 EC50 = 18197.0 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 3 0 5 2.6 CC(C)(C)C1=CC(=NC(=N1)N(C)C)N2CCN(CC2)C
CHEMBL449157 hrh4_rat Rat No 4.7 EC50 = 18197.0 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 3 0 5 2.6 CC(C)(C)C1=CC(=NC(=N1)N(C)C)N2CCN(CC2)C
CHEMBL493461 hrh4_rat Rat No 5.7 EC50 = 1862.1 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 1.8 CN1CCN(CC1)C2=CC(=NC(=C2)N)C3=CC=C(C=C3)C#N
CHEMBL493461 hrh4_rat Rat No 5.7 EC50 = 1862.1 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 1.8 CN1CCN(CC1)C2=CC(=NC(=C2)N)C3=CC=C(C=C3)C#N
CHEMBL474447 hrh4_human Human No 7.7 EC50 = 19.1 Funct
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 7 4 3 1.6 C1=CC=C2C(=C1)C(=CN2)CC(=O)NC(=NCCCC3=CN=CN3)N
CHEMBL446269 hrh4_rat Rat No 7.7 EC50 = 19.1 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 1.7 CNC1CCN(C1)C2=NC(=NC3=C2CC4=CC=CC=C43)N
CHEMBL474447 hrh4_human Human No 7.7 EC50 = 19.1 Funct
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 7 4 3 1.6 C1=CC=C2C(=C1)C(=CN2)CC(=O)NC(=NCCCC3=CN=CN3)N
CHEMBL446269 hrh4_rat Rat No 7.7 EC50 = 19.1 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 1.7 CNC1CCN(C1)C2=NC(=NC3=C2CC4=CC=CC=C43)N
CHEMBL594721 hrh4_human Human No 7.7 EC50 = 19.5 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
333 4 2 6 2.6 CN1CCN(CC1)C2=CC(=NC(=N2)N)NCC3=CC=CC=C3Cl
CHEMBL594721 hrh4_human Human No 7.7 EC50 = 19.5 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
333 4 2 6 2.6 CN1CCN(CC1)C2=CC(=NC(=N2)N)NCC3=CC=CC=C3Cl
CHEMBL213912 hrh4_human Human No 7.7 EC50 = 20.0 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
328 1 0 3 3.1 CN1CCN(CC1)C2=NC3=C(C=C(C=C3)Cl)OC4=CC=CC=C42
CHEMBL12160 hrh4_human Human Yes 7.7 EC50 = 20.0 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 0.4 CNC(=S)NCCCCC1=CN=CN1
CHEMBL1632409 hrh4_human Human No 7.7 EC50 = 20.0 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
323 8 2 3 3.3 C1=CC(=CC=C1CN=C(N)SCCCCC2=CN=CN2)Cl
CHEMBL306077 hrh4_human Human No 7.7 EC50 = 20.0 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 1.2 CC(C)NC(=S)NCCCCC1=CN=CN1
CHEMBL521995 hrh4_rat Rat No 7.7 EC50 = 20.0 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 1.3 C1CN(CCN1)C2=NC(=NC3=C2CC4=CC=CC=C43)N
CHEMBL213912 hrh4_human Human No 7.7 EC50 = 20.0 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
328 1 0 3 3.1 CN1CCN(CC1)C2=NC3=C(C=C(C=C3)Cl)OC4=CC=CC=C42
CHEMBL12160 hrh4_human Human Yes 7.7 EC50 = 20.0 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 0.4 CNC(=S)NCCCCC1=CN=CN1
CHEMBL1632409 hrh4_human Human No 7.7 EC50 = 20.0 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
323 8 2 3 3.3 C1=CC(=CC=C1CN=C(N)SCCCCC2=CN=CN2)Cl
CHEMBL306077 hrh4_human Human No 7.7 EC50 = 20.0 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 1.2 CC(C)NC(=S)NCCCCC1=CN=CN1
CHEMBL521995 hrh4_rat Rat No 7.7 EC50 = 20.0 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 1.3 C1CN(CCN1)C2=NC(=NC3=C2CC4=CC=CC=C43)N
CHEMBL522679 hrh4_rat Rat No 6.7 EC50 = 195.0 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 1.7 CN1CCN(CC1)C2=NC(=NC(=C2)C3=C(C=CC=C3OC)OC)N
CHEMBL522679 hrh4_rat Rat No 6.7 EC50 = 195.0 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 1.7 CN1CCN(CC1)C2=NC(=NC(=C2)C3=C(C=CC=C3OC)OC)N
CHEMBL106158 hrh4_human Human No 6.7 EC50 = 199.5 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 5 3 4 -0.3 CN=C(NCC1CCC(O1)C2=CN=CN2)NC#N
CHEMBL91353 hrh4_human Human Yes 6.7 EC50 = 199.5 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 C1=C(NC=N1)CCCN
CHEMBL1632412 hrh4_mouse Mouse No 6.7 EC50 = 199.5 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 4 1.5 CC1=CC2=CC(=C(C3CCN(CC3)C)NO)N=C2C=C1
CHEMBL1632414 hrh4_rat Rat No 6.7 EC50 = 199.5 Funct
Agonist activity at rat histamine H4 receptor by luciferase reporter gene assayAgonist activity at rat histamine H4 receptor by luciferase reporter gene assay
293 1 2 5 2.5 CN1CCC(CC1)C(=C2NC3=C(N2)C=C(C=C3)Cl)N=O
CHEMBL595639 hrh4_human Human No 6.7 EC50 = 199.5 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
333 4 2 6 2.6 CN1CCN(CC1)C2=CC(=NC(=N2)N)NCC3=CC(=CC=C3)Cl
CHEMBL106158 hrh4_human Human No 6.7 EC50 = 199.5 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 5 3 4 -0.3 CN=C(NCC1CCC(O1)C2=CN=CN2)NC#N
CHEMBL91353 hrh4_human Human Yes 6.7 EC50 = 199.5 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 C1=C(NC=N1)CCCN
CHEMBL1632412 hrh4_mouse Mouse No 6.7 EC50 = 199.5 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 4 1.5 CC1=CC2=CC(=C(C3CCN(CC3)C)NO)N=C2C=C1
CHEMBL1632414 hrh4_rat Rat No 6.7 EC50 = 199.5 Funct
Agonist activity at rat histamine H4 receptor by luciferase reporter gene assayAgonist activity at rat histamine H4 receptor by luciferase reporter gene assay
293 1 2 5 2.5 CN1CCC(CC1)C(=C2NC3=C(N2)C=C(C=C3)Cl)N=O
CHEMBL595639 hrh4_human Human No 6.7 EC50 = 199.5 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
333 4 2 6 2.6 CN1CCN(CC1)C2=CC(=NC(=N2)N)NCC3=CC(=CC=C3)Cl
CHEMBL106612 hrh4_human Human No 5.7 EC50 = 1995.3 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 C1CC(OC1CN)C2=CN=CN2
CHEMBL106612 hrh4_human Human No 5.7 EC50 = 1995.3 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 C1CC(OC1CN)C2=CN=CN2
CHEMBL106612 hrh4_human Human No 5.7 EC50 = 1995.3 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 C1CC(OC1CN)C2=CN=CN2
CHEMBL106570 hrh4_human Human No 4.7 EC50 = 19952.6 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 5 3 4 -0.3 CN=C(NCC1CCC(O1)C2=CN=CN2)NC#N
CHEMBL106570 hrh4_human Human No 4.7 EC50 = 19952.6 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 5 3 4 -0.3 CN=C(NCC1CCC(O1)C2=CN=CN2)NC#N
CHEMBL465170 hrh4_human Human No 8.6 EC50 = 2.6 Funct
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 7 3 3 0.7 CCCC(=O)NC(=NCCCC1=CN=CN1)N
CHEMBL465170 hrh4_human Human No 8.6 EC50 = 2.6 Funct
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 7 3 3 0.7 CCCC(=O)NC(=NCCCC1=CN=CN1)N
CHEMBL1096429 hrh4_human Human No 8.6 EC50 = 2.6 Funct
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 8 3 3 2.1 CC(CC(=O)NC(=NCCCC1=CN=CN1)N)C2=CC=CC=C2
CHEMBL1096429 hrh4_human Human No 8.6 EC50 = 2.6 Funct
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 8 3 3 2.1 CC(CC(=O)NC(=NCCCC1=CN=CN1)N)C2=CC=CC=C2
CHEMBL3393546 hrh4_human Human No 7.7 EC50 = 20 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 2.5 CN1CCN(CC1)C2=NC(=NC=C2)NC3CC4CCC3C4
CHEMBL3393546 hrh4_human Human No 7.7 EC50 = 20 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 2.5 CN1CCN(CC1)C2=NC(=NC=C2)NC3CC4CCC3C4
CHEMBL209628 hrh4_human Human No 7.7 EC50 = 20.4 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
346 1 0 4 3.2 CN1CCN(CC1)C2=NC3=C(C=C(C=C3)Cl)OC4=C2C=CC=C4F
CHEMBL209628 hrh4_human Human No 7.7 EC50 = 20.4 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
346 1 0 4 3.2 CN1CCN(CC1)C2=NC3=C(C=C(C=C3)Cl)OC4=C2C=CC=C4F
CHEMBL593103 hrh4_human Human No 7.7 EC50 = 20.9 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 7 2.0 CN1CCN(CC1)C2=CC(=NC(=N2)N)NCC3=CC=C(C=C3)F
CHEMBL593103 hrh4_human Human No 7.7 EC50 = 20.9 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 7 2.0 CN1CCN(CC1)C2=CC(=NC(=N2)N)NCC3=CC=C(C=C3)F
CHEMBL3805003 hrh4_human Human No 6.7 EC50 = 202 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 7 3 3 1.9 CC(C)CN=C(NCC1CCC(C1)C2=CN=CN2)NC#N
CHEMBL3805003 hrh4_human Human No 6.7 EC50 = 202 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 7 3 3 1.9 CC(C)CN=C(NCC1CCC(C1)C2=CN=CN2)NC#N
CHEMBL492864 hrh4_rat Rat No 5.7 EC50 = 2041.7 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 0.8 CN1CCN(CC1)C2=CC(=NC(=N2)N)I
CHEMBL492864 hrh4_rat Rat No 5.7 EC50 = 2041.7 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 0.8 CN1CCN(CC1)C2=CC(=NC(=N2)N)I
CHEMBL153207 hrh4_human Human Yes 5.7 EC50 = 2041.7 Funct
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 1.0 C1CC(CNC1)CCC2=CN=CN2
CHEMBL3804906 hrh4_human Human No 6.7 EC50 = 206 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 5 3 3 0.6 CN=C(NCC1CCC(C1)C2=CN=CN2)NC#N
CHEMBL492227 hrh4_rat Rat No 6.7 EC50 = 208.9 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 0.7 CN1CCN(CC1)C2=NC(=NC(=C2)C3=CN=CC=C3)N
CHEMBL492227 hrh4_rat Rat No 6.7 EC50 = 208.9 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 0.7 CN1CCN(CC1)C2=NC(=NC(=C2)C3=CN=CC=C3)N
CHEMBL492677 hrh4_human Human No 7.7 EC50 = 21.4 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 1.9 CN1CCN(CC1)C2=NC(=NC(=C2)NCC3=CC=CC=C3)N
CHEMBL492677 hrh4_human Human No 7.7 EC50 = 21.4 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 1.9 CN1CCN(CC1)C2=NC(=NC(=C2)NCC3=CC=CC=C3)N
CHEMBL91353 hrh4_human Human Yes 6.7 EC50 = 213.8 Funct
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 C1=C(NC=N1)CCCN
CHEMBL106570 hrh4_human Human No 4.7 EC50 = 21379.6 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 5 3 4 -0.3 CN=C(NCC1CCC(O1)C2=CN=CN2)NC#N
CHEMBL473662 hrh4_rat Rat Yes 6.7 EC50 = 218.8 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 -0.2 CN1CCN(CC1)C2=CC(=NC(=N2)N)N
CHEMBL493229 hrh4_rat Rat No 6.7 EC50 = 218.8 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 6 0.1 CN1CCN(CC1)C2=NC(=NC(=C2)C3=CN(N=C3)C)N
CHEMBL473662 hrh4_rat Rat Yes 6.7 EC50 = 218.8 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 -0.2 CN1CCN(CC1)C2=CC(=NC(=N2)N)N
CHEMBL493229 hrh4_rat Rat No 6.7 EC50 = 218.8 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 6 0.1 CN1CCN(CC1)C2=NC(=NC(=C2)C3=CN(N=C3)C)N
CHEMBL1096428 hrh4_human Human No 7.6 EC50 = 22.9 Funct
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 8 3 3 2.1 CC(CC(=O)NC(=NCCCC1=CN=CN1)N)C2=CC=CC=C2
CHEMBL1096428 hrh4_human Human No 7.6 EC50 = 22.9 Funct
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 8 3 3 2.1 CC(CC(=O)NC(=NCCCC1=CN=CN1)N)C2=CC=CC=C2
CHEMBL106158 hrh4_human Human No 6.7 EC50 = 223.9 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 5 3 4 -0.3 CN=C(NCC1CCC(O1)C2=CN=CN2)NC#N
CHEMBL492241 hrh4_rat Rat Yes 6.6 EC50 = 229.1 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 0.7 CN1CCN(CC1)C2=NC(=NC(=C2)C3=CC=NC=C3)N
CHEMBL492241 hrh4_rat Rat Yes 6.6 EC50 = 229.1 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 0.7 CN1CCN(CC1)C2=NC(=NC(=C2)C3=CC=NC=C3)N
CHEMBL523335 hrh4_rat Rat No 5.6 EC50 = 2290.9 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 3 1 4 2.4 CC(C)(C)C1=CC(=NC(=N1)N2C=CC=C2)N3CCNCC3
CHEMBL523335 hrh4_rat Rat No 5.6 EC50 = 2290.9 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 3 1 4 2.4 CC(C)(C)C1=CC(=NC(=N1)N2C=CC=C2)N3CCNCC3
CHEMBL447151 hrh4_rat Rat No 4.6 EC50 = 22908.7 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 2 1 2 0.8 CC(C)(C)C1=CC(=NC(=O)N1)N2CCN(CC2)C
CHEMBL447151 hrh4_rat Rat No 4.6 EC50 = 22908.7 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 2 1 2 0.8 CC(C)(C)C1=CC(=NC(=O)N1)N2CCN(CC2)C
CHEMBL493281 hrh4_rat Rat No 7.6 EC50 = 24.0 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 1.6 C1CC2=C(C3=CC=CC=C31)N=C(N=C2N4CCNCC4)N
CHEMBL493281 hrh4_rat Rat No 7.6 EC50 = 24.0 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 1.6 C1CC2=C(C3=CC=CC=C31)N=C(N=C2N4CCNCC4)N
CHEMBL3804837 hrh4_human Human No 6.6 EC50 = 230 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 6 3 3 1.7 C1CC1NC(=NCC2CCC(C2)C3=CN=CN3)NC#N
CHEMBL3804837 hrh4_human Human No 6.6 EC50 = 230 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 6 3 3 1.7 C1CC1NC(=NCC2CCC(C2)C3=CN=CN3)NC#N
CHEMBL495082 hrh4_rat Rat No 6.6 EC50 = 234.4 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 1.5 CN1CCN(CC1)C2=NC(=NC(=C2)C3=CC=CC(=C3)C#N)N
CHEMBL522019 hrh4_rat Rat No 6.6 EC50 = 234.4 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 0.7 CN1CCN(CC1)C2=NC(=NC(=C2)C3=C(C=CN=C3)OC)N
CHEMBL495082 hrh4_rat Rat No 6.6 EC50 = 234.4 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 1.5 CN1CCN(CC1)C2=NC(=NC(=C2)C3=CC=CC(=C3)C#N)N
CHEMBL522019 hrh4_rat Rat No 6.6 EC50 = 234.4 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 0.7 CN1CCN(CC1)C2=NC(=NC(=C2)C3=C(C=CN=C3)OC)N
CHEMBL493262 hrh4_human Human No 5.6 EC50 = 2344.2 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 2.1 CN1CCN(CC1)C2=NC(=CC(=C2)C3=CC=C(C=C3)C#N)N
CHEMBL493262 hrh4_human Human No 5.6 EC50 = 2344.2 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 2.1 CN1CCN(CC1)C2=NC(=CC(=C2)C3=CC=C(C=C3)C#N)N
CHEMBL494687 hrh4_rat Rat No 4.6 EC50 = 23442.3 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 2 1 4 3.3 CC1CCN(CC1)C2=NC(=NC(=C2)C(C)(C)C)N
CHEMBL494687 hrh4_rat Rat No 4.6 EC50 = 23442.3 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 2 1 4 3.3 CC1CCN(CC1)C2=NC(=NC(=C2)C(C)(C)C)N
CHEMBL449021 hrh4_rat Rat No 5.6 EC50 = 2398.8 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 5 1 6 1.9 CC(C)(C)C1=CC(=NC(=N1)N)N2CCN(CC2)CCN(C)C
CHEMBL449021 hrh4_rat Rat No 5.6 EC50 = 2398.8 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 5 1 6 1.9 CC(C)(C)C1=CC(=NC(=N1)N)N2CCN(CC2)CCN(C)C
CHEMBL109130 hrh4_human Human No 4.6 EC50 = 23988.3 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 -0.7 C1=CC(OC1CN)C2=CN=CN2
CHEMBL3806146 hrh4_human Human No 6.6 EC50 = 245 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 6 3 3 1.7 C1CC1NC(=NCC2CCC(C2)C3=CN=CN3)NC#N
CHEMBL3806146 hrh4_human Human No 6.6 EC50 = 245 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 6 3 3 1.7 C1CC1NC(=NCC2CCC(C2)C3=CN=CN3)NC#N
CHEMBL494890 hrh4_rat Rat No 6.6 EC50 = 245.5 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 C1CN(CCN1)C2=NC(=NC(=C2)C3=CC=C(C=C3)C#N)N
CHEMBL506187 hrh4_rat Rat No 6.6 EC50 = 245.5 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 3 1 5 2.2 CCN1CCN(CC1)C2=NC(=NC(=C2)C(C)(C)C)N
CHEMBL494890 hrh4_rat Rat No 6.6 EC50 = 245.5 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 C1CN(CCN1)C2=NC(=NC(=C2)C3=CC=C(C=C3)C#N)N
CHEMBL3220642 hrh4_human Human No 6.6 EC50 = 245.5 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 11 3 4 3.0 CC1=C(N=CN1)CCCCN=C(NCCSC2=CC=CC=C2)NC#N
CHEMBL494890 hrh4_rat Rat No 6.6 EC50 = 245.5 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 C1CN(CCN1)C2=NC(=NC(=C2)C3=CC=C(C=C3)C#N)N
CHEMBL506187 hrh4_rat Rat No 6.6 EC50 = 245.5 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 3 1 5 2.2 CCN1CCN(CC1)C2=NC(=NC(=C2)C(C)(C)C)N
CHEMBL494890 hrh4_rat Rat No 6.6 EC50 = 245.5 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 C1CN(CCN1)C2=NC(=NC(=C2)C3=CC=C(C=C3)C#N)N
CHEMBL3805361 hrh4_human Human No 7.6 EC50 = 25 Funct
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
369 9 3 4 2.8 C1CC(CC1CN=C(NCCSC2=CC=CC=C2)NC#N)C3=CN=CN3
CHEMBL3354815 hrh4_human Human No 7.6 EC50 = 25 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 1.5 CC(C)NC1=NC=CC(=N1)N2CCC(C2)NC
CHEMBL3805361 hrh4_human Human No 7.6 EC50 = 25 Funct
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
369 9 3 4 2.8 C1CC(CC1CN=C(NCCSC2=CC=CC=C2)NC#N)C3=CN=CN3
CHEMBL3354815 hrh4_human Human No 7.6 EC50 = 25 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 1.5 CC(C)NC1=NC=CC(=N1)N2CCC(C2)NC
CHEMBL12608 hrh4_human Human Yes 7.6 EC50 = 25.1 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 10 4 4 0.3 CC1=C(N=CN1)CSCCNC(=NCCCC2=CN=CN2)N
CHEMBL12608 hrh4_human Human Yes 7.6 EC50 = 25.1 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 10 4 4 0.3 CC1=C(N=CN1)CSCCNC(=NCCCC2=CN=CN2)N
CHEMBL494679 hrh4_rat Rat Yes 6.6 EC50 = 251.2 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 2 1 6 1.6 CC(C)(C)C1=NC(=NC(=N1)N)N2CCN(CC2)C
CHEMBL494679 hrh4_rat Rat Yes 6.6 EC50 = 251.2 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 2 1 6 1.6 CC(C)(C)C1=NC(=NC(=N1)N)N2CCN(CC2)C
CHEMBL448085 hrh4_human Human No 5.6 EC50 = 2511.9 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 6 0.2 CN1CCN(CC1)C2=NC(=NC(=C2)N3C=CN=C3)N
CHEMBL275443 hrh4_rat Rat Yes 5.6 EC50 = 2511.9 Funct
Agonist activity at rat histamine H4 receptorAgonist activity at rat histamine H4 receptor
125 2 2 2 -0.2 CC1=C(N=CN1)CCN
CHEMBL448085 hrh4_human Human No 5.6 EC50 = 2511.9 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 6 0.2 CN1CCN(CC1)C2=NC(=NC(=C2)N3C=CN=C3)N
CHEMBL275443 hrh4_rat Rat Yes 5.6 EC50 = 2511.9 Funct
Agonist activity at rat histamine H4 receptorAgonist activity at rat histamine H4 receptor
125 2 2 2 -0.2 CC1=C(N=CN1)CCN
CHEMBL1077859 hrh4_human Human No 5.6 EC50 = 2570.4 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 11 3 4 1.6 C1=CN=CC=C1CCCN=C(NCCCCC2=CN=CN2)NC#N
CHEMBL1077859 hrh4_human Human No 5.6 EC50 = 2570.4 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 11 3 4 1.6 C1=CN=CC=C1CCCN=C(NCCCCC2=CN=CN2)NC#N
CHEMBL507063 hrh4_human Human Yes 7.6 EC50 = 26.9 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 1.0 CN1CCN(CC1)C2=NC(=NC(=C2)C3=C(N=CC=C3)OC)N
CHEMBL507063 hrh4_human Human Yes 7.6 EC50 = 26.9 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 1.0 CN1CCN(CC1)C2=NC(=NC(=C2)C3=C(N=CC=C3)OC)N
CHEMBL3806162 hrh4_human Human No 5.6 EC50 = 2675 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 5 3 3 0.6 CN=C(NCC1CCC(C1)C2=CN=CN2)NC#N
CHEMBL3806162 hrh4_human Human No 5.6 EC50 = 2675 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 5 3 3 0.6 CN=C(NCC1CCC(C1)C2=CN=CN2)NC#N
CHEMBL594949 hrh4_human Human No 6.6 EC50 = 269.2 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 2.3 CC1=CC(=CC=C1)CNC2=NC(=NC(=C2)N3CCN(CC3)C)N
CHEMBL594949 hrh4_human Human No 6.6 EC50 = 269.2 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 2.3 CC1=CC(=CC=C1)CNC2=NC(=NC(=C2)N3CCN(CC3)C)N
CHEMBL492288 hrh4_rat Rat No 6.6 EC50 = 275.4 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 2.4 CN1CCN(CC1)C2=NC(=NC(=C2)C3=CC=C(C=C3)I)N
CHEMBL492288 hrh4_rat Rat No 6.6 EC50 = 275.4 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 2.4 CN1CCN(CC1)C2=NC(=NC(=C2)C3=CC=C(C=C3)I)N
CHEMBL474449 hrh4_human Human No 7.6 EC50 = 28.2 Funct
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 8 5 4 1.4 C1=CC=C2C(=C1)C=C(N2)C(=O)NCC(=O)NC(=NCCCC3=CN=CN3)N
CHEMBL474449 hrh4_human Human No 7.6 EC50 = 28.2 Funct
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 8 5 4 1.4 C1=CC=C2C(=C1)C=C(N2)C(=O)NCC(=O)NC(=NCCCC3=CN=CN3)N
CHEMBL3220629 hrh4_human Human No 5.5 EC50 = 2884.0 Funct
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 8 3 3 2.1 CC(CC(=O)NC(=NCCCC1=NC=CN1)N)C2=CC=CC=C2
CHEMBL3806079 hrh4_human Human No 6.5 EC50 = 293 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
369 9 3 4 2.8 C1CC(CC1CN=C(NCCSC2=CC=CC=C2)NC#N)C3=CN=CN3
CHEMBL494093 hrh4_human Human No 6.5 EC50 = 295.1 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 2.1 CN1CCN(CC1)C2=NC(=NC3=C2CCC4=CC=CC=C43)N
CHEMBL494093 hrh4_human Human No 6.5 EC50 = 295.1 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 2.1 CN1CCN(CC1)C2=NC(=NC3=C2CCC4=CC=CC=C43)N
CHEMBL475621 hrh4_human Human No 8.5 EC50 = 3.0 Funct
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 6 3 3 0.4 CCC(=O)NC(=NCCCC1=CN=CN1)N
CHEMBL475621 hrh4_human Human No 8.5 EC50 = 3.0 Funct
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 6 3 3 0.4 CCC(=O)NC(=NCCCC1=CN=CN1)N
CHEMBL1086105 hrh4_human Human No 8.5 EC50 = 3.3 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
420 6 2 5 4.1 CC1=C(C=CC(=C1)OCCCN2CCC3=C(C2)NC=N3)C4=NC5=C(N4)C=CC(=C5C)F
CHEMBL1084355 hrh4_human Human No 8.5 EC50 = 3.3 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 5 4.3 CC1=C(C=CC(=C1)OCCCNCC2=CN=CC=C2)C3=NC4=C(N3)C=CC(=C4C)F
CHEMBL1086105 hrh4_human Human No 8.5 EC50 = 3.3 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
420 6 2 5 4.1 CC1=C(C=CC(=C1)OCCCN2CCC3=C(C2)NC=N3)C4=NC5=C(N4)C=CC(=C5C)F
CHEMBL1084355 hrh4_human Human No 8.5 EC50 = 3.3 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 5 4.3 CC1=C(C=CC(=C1)OCCCNCC2=CN=CC=C2)C3=NC4=C(N3)C=CC(=C4C)F
CHEMBL471724 hrh4_human Human No 8.4 EC50 = 3.7 Funct
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 3 0.9 CC(C)C(=O)NC(=NCCCC1=CN=CN1)N
CHEMBL471724 hrh4_human Human No 8.4 EC50 = 3.7 Funct
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 3 0.9 CC(C)C(=O)NC(=NCCCC1=CN=CN1)N
CHEMBL503605 hrh4_rat Rat Yes 7.5 EC50 = 30.9 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
264 1 2 2 1.8 C1CN(CCN1)C(=O)C2=CC3=C(N2)C=CC(=C3)Cl
CHEMBL503605 hrh4_rat Rat Yes 7.5 EC50 = 30.9 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
264 1 2 2 1.8 C1CN(CCN1)C(=O)C2=CC3=C(N2)C=CC(=C3)Cl
CHEMBL485802 hrh4_rat Rat No 5.5 EC50 = 3020.0 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 0.6 CN1CCN(CC1)C2=CC(=NC(=N2)N)N(C)C
CHEMBL485802 hrh4_rat Rat No 5.5 EC50 = 3020.0 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 0.6 CN1CCN(CC1)C2=CC(=NC(=N2)N)N(C)C
CHEMBL339414 hrh4_human Human No 6.5 EC50 = 302 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 1 0 3 2.4 CN1CCN(CC1)C2=NC3=CC=CC=C3OC4=CC=CC=C42
CHEMBL495341 hrh4_rat Rat No 6.5 EC50 = 302 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 5 1 5 1.9 CC(C)(C)C1=CC(=NC(=N1)N)OCCN(C)C
CHEMBL339414 hrh4_human Human No 6.5 EC50 = 302 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 1 0 3 2.4 CN1CCN(CC1)C2=NC3=CC=CC=C3OC4=CC=CC=C42
CHEMBL495341 hrh4_rat Rat No 6.5 EC50 = 302 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 5 1 5 1.9 CC(C)(C)C1=CC(=NC(=N1)N)OCCN(C)C
CHEMBL106931 hrh4_human Human No 4.5 EC50 = 30903.0 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 C1CC(OC1CN)C2=CN=CN2
CHEMBL594022 hrh4_human Human No 7.5 EC50 = 31.6 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
333 4 2 6 2.6 CN1CCN(CC1)C2=CC(=NC(=N2)N)NCC3=CC=C(C=C3)Cl
CHEMBL90019 hrh4_human Human Yes 7.5 EC50 = 31.6 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 -0.3 C1=C(NC=N1)CCCCN
CHEMBL275443 hrh4_human Human Yes 7.5 EC50 = 31.6 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 CC1=C(N=CN1)CCN
CHEMBL492287 hrh4_rat Rat No 7.5 EC50 = 31.6 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
304 2 1 5 2.4 CN1CCN(CC1)C2=NC(=NC(=C2)C3=CC(=CC=C3)Cl)N
CHEMBL594022 hrh4_human Human No 7.5 EC50 = 31.6 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
333 4 2 6 2.6 CN1CCN(CC1)C2=CC(=NC(=N2)N)NCC3=CC=C(C=C3)Cl
CHEMBL90019 hrh4_human Human Yes 7.5 EC50 = 31.6 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 -0.3 C1=C(NC=N1)CCCCN
CHEMBL275443 hrh4_human Human Yes 7.5 EC50 = 31.6 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 CC1=C(N=CN1)CCN
CHEMBL492287 hrh4_rat Rat No 7.5 EC50 = 31.6 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
304 2 1 5 2.4 CN1CCN(CC1)C2=NC(=NC(=C2)C3=CC(=CC=C3)Cl)N
CHEMBL522661 hrh4_rat Rat No 6.5 EC50 = 316.2 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 3.0 CN1CCN(CC1)C2=NC(=NC(=C2)C34CC5CC(C3)CC(C5)C4)N
CHEMBL522661 hrh4_rat Rat No 6.5 EC50 = 316.2 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 3.0 CN1CCN(CC1)C2=NC(=NC(=C2)C34CC5CC(C3)CC(C5)C4)N
CHEMBL3393550 hrh4_human Human No 5.5 EC50 = 3160 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 1.4 CC(C)CNC1=NN=CC(=C1)N2CCC(C2)NC
CHEMBL3393550 hrh4_human Human No 5.5 EC50 = 3160 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 1.4 CC(C)CNC1=NN=CC(=C1)N2CCC(C2)NC
CHEMBL3393547 hrh4_human Human No 5.5 EC50 = 3162 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 2.5 CNC1CCN(C1)C2=NC(=NC=C2)NC3CC4CCC3C4
CHEMBL3354816 hrh4_human Human No 5.5 EC50 = 3162 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 1.9 CC(C)NC1=NC=CC(=C1)N2CCC(C2)NC
CHEMBL3393547 hrh4_human Human No 5.5 EC50 = 3162 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 2.5 CNC1CCN(C1)C2=NC(=NC=C2)NC3CC4CCC3C4
CHEMBL3354816 hrh4_human Human No 5.5 EC50 = 3162 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 1.9 CC(C)NC1=NC=CC(=C1)N2CCC(C2)NC
CHEMBL79126 hrh4_human Human No 5.5 EC50 = 3162.3 Funct
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 1.6 C1=CC=NC(=C1)CCCC2=CN=CN2
CHEMBL106931 hrh4_human Human No 4.5 EC50 = 31622.8 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 C1CC(OC1CN)C2=CN=CN2
CHEMBL106931 hrh4_human Human No 4.5 EC50 = 31622.8 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 C1CC(OC1CN)C2=CN=CN2
CHEMBL523835 hrh4_rat Rat No 5.5 EC50 = 3235.9 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 0.4 CN1CCN(CC1)C2=NC(=NC(=C2)C3=CN=C(N=C3)OC)N
CHEMBL523835 hrh4_rat Rat No 5.5 EC50 = 3235.9 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 0.4 CN1CCN(CC1)C2=NC(=NC(=C2)C3=CN=C(N=C3)OC)N
CHEMBL82244 hrh4_human Human Yes 4.5 EC50 = 32359.4 Funct
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 1.2 C1=CC(=CN=C1)CCC2=CN=CN2
CHEMBL515428 hrh4_human Human No 7.5 EC50 = 33.1 Funct
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 9 5 4 1.3 C1=CC=C2C(=C1)C=C(N2)C(=O)NCCC(=O)NC(=NCCCC3=CN=CN3)N
CHEMBL515428 hrh4_human Human No 7.5 EC50 = 33.1 Funct
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 9 5 4 1.3 C1=CC=C2C(=C1)C=C(N2)C(=O)NCCC(=O)NC(=NCCCC3=CN=CN3)N
CHEMBL493478 hrh4_human Human No 7.5 EC50 = 33.9 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(CC1)C2=NC(=NC=C2N)N
CHEMBL493478 hrh4_human Human No 7.5 EC50 = 33.9 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(CC1)C2=NC(=NC=C2N)N
CHEMBL1083085 hrh4_human Human No 6.5 EC50 = 331 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
397 6 2 5 4.0 CC1=C(C=CC(=C1)OCCCN2CCCC(C2)N)C3=NC4=C(N3)C=CC(=C4C)F
CHEMBL1083085 hrh4_human Human No 6.5 EC50 = 331 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
397 6 2 5 4.0 CC1=C(C=CC(=C1)OCCCN2CCCC(C2)N)C3=NC4=C(N3)C=CC(=C4C)F
CHEMBL1077636 hrh4_human Human No 6.5 EC50 = 331.1 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 8 3 3 1.2 CC(C)NC(=NCCCCC1=CN=CN1)NC#N
CHEMBL1077636 hrh4_human Human No 6.5 EC50 = 331.1 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 8 3 3 1.2 CC(C)NC(=NCCCCC1=CN=CN1)NC#N
CHEMBL444484 hrh4_rat Rat No 6.5 EC50 = 338.8 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 0.2 CN1CCN(CC1)C2=CC(=NC(=N2)N)N3CCOCC3
CHEMBL2165643 hrh4_human Human No 6.5 EC50 = 338.8 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
585 25 6 6 5.6 C1=C(NC=N1)CCCN=C(N)NC(=O)CCCCCCCCCCCCCCC(=O)NC(=NCCCC2=CN=CN2)N
CHEMBL444484 hrh4_rat Rat No 6.5 EC50 = 338.8 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 0.2 CN1CCN(CC1)C2=CC(=NC(=N2)N)N3CCOCC3
CHEMBL492662 hrh4_rat Rat No 6.5 EC50 = 354.8 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 1.3 CCN(CC)C1=NC(=NC(=C1)N2CCN(CC2)C)N
CHEMBL492662 hrh4_rat Rat No 6.5 EC50 = 354.8 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 1.3 CCN(CC)C1=NC(=NC(=C1)N2CCN(CC2)C)N
CHEMBL493479 hrh4_rat Rat Yes 6.4 EC50 = 363.1 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 0.5 CC1=CC(=NC(=N1)N)N2CCN(CC2)C
CHEMBL493479 hrh4_rat Rat Yes 6.4 EC50 = 363.1 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 0.5 CC1=CC(=NC(=N1)N)N2CCN(CC2)C
CHEMBL494585 hrh4_rat Rat No 5.4 EC50 = 3630.8 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 2 1 4 2.2 CC(C)(C)C1=NC(=NC(=C1)C2CCN(CC2)C)N
CHEMBL492663 hrh4_rat Rat No 5.4 EC50 = 3630.8 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 0.8 CN1CCN(CC1)C2=NC(=NC(=C2)N3CCC(C3)N(C)C)N
CHEMBL3220641 hrh4_human Human No 5.4 EC50 = 3630.8 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 7 3 3 0.8 CC1=C(N=CN1)CCCCNC(=NC)NC#N
CHEMBL494585 hrh4_rat Rat No 5.4 EC50 = 3630.8 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 2 1 4 2.2 CC(C)(C)C1=NC(=NC(=C1)C2CCN(CC2)C)N
CHEMBL492663 hrh4_rat Rat No 5.4 EC50 = 3630.8 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 0.8 CN1CCN(CC1)C2=NC(=NC(=C2)N3CCC(C3)N(C)C)N
CHEMBL3805437 hrh4_mouse Mouse No 5.4 EC50 = 3631 Funct
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 5 3 3 0.6 CN=C(NCC1CCC(C1)C2=CN=CN2)NC#N
CHEMBL3805437 hrh4_mouse Mouse No 5.4 EC50 = 3631 Funct
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 5 3 3 0.6 CN=C(NCC1CCC(C1)C2=CN=CN2)NC#N
CHEMBL493720 hrh4_rat Rat No 7.4 EC50 = 37.2 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
304 2 1 5 2.4 CN1CCN(CC1)C2=NC(=NC(=C2)C3=CC=C(C=C3)Cl)N
CHEMBL594491 hrh4_human Human No 7.4 EC50 = 37.2 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 1.6 CN1CCN(CC1)C2=NC(=NC(=C2)N3CC4=CC=CC=C4C3)N
CHEMBL493720 hrh4_rat Rat No 7.4 EC50 = 37.2 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
304 2 1 5 2.4 CN1CCN(CC1)C2=NC(=NC(=C2)C3=CC=C(C=C3)Cl)N
CHEMBL594491 hrh4_human Human No 7.4 EC50 = 37.2 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 1.6 CN1CCN(CC1)C2=NC(=NC(=C2)N3CC4=CC=CC=C4C3)N
CHEMBL3805663 hrh4_human Human No 6.4 EC50 = 372 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 9 3 3 2.9 C1CC(CC1CN=C(NCCCC2=CC=CC=C2)NC#N)C3=CN=CN3
CHEMBL3805663 hrh4_human Human No 6.4 EC50 = 372 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 9 3 3 2.9 C1CC(CC1CN=C(NCCCC2=CC=CC=C2)NC#N)C3=CN=CN3
CHEMBL387054 hrh4_human Human No 7.4 EC50 = 38.9 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
346 1 0 4 3.2 CN1CCN(CC1)C2=NC3=C(C=C(C=C3)Cl)OC4=C2C=CC(=C4)F
CHEMBL387054 hrh4_human Human No 7.4 EC50 = 38.9 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
346 1 0 4 3.2 CN1CCN(CC1)C2=NC3=C(C=C(C=C3)Cl)OC4=C2C=CC(=C4)F
CHEMBL493664 hrh4_human Human No 5.4 EC50 = 3890.5 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 6 0.5 CN1CCN(CC1)C2=NC(=NC(=C2)N3C=CC=CC3=O)N
CHEMBL493664 hrh4_human Human No 5.4 EC50 = 3890.5 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 6 0.5 CN1CCN(CC1)C2=NC(=NC(=C2)N3C=CC=CC3=O)N
CHEMBL1083162 hrh4_mouse Mouse No 7.4 EC50 = 39 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 5 4.0 CC1=C(C=CC(=C1)OCCCNCCC2=CN=CN2)C3=NC4=C(N3)C=CC(=C4C)F
CHEMBL1083162 hrh4_mouse Mouse No 7.4 EC50 = 39 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 5 4.0 CC1=C(C=CC(=C1)OCCCNCCC2=CN=CN2)C3=NC4=C(N3)C=CC(=C4C)F
CHEMBL275443 hrh4_human Human Yes 7.4 EC50 = 39.8 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 CC1=C(N=CN1)CCN
CHEMBL1632413 hrh4_human Human No 7.4 EC50 = 39.8 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
293 2 2 5 1.5 CN1CCN(CC1)C(=C2C=C3C=C(C=CC3=N2)Cl)NO
CHEMBL275443 hrh4_human Human Yes 7.4 EC50 = 39.8 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 CC1=C(N=CN1)CCN
CHEMBL1632413 hrh4_human Human No 7.4 EC50 = 39.8 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
293 2 2 5 1.5 CN1CCN(CC1)C(=C2C=C3C=C(C=CC3=N2)Cl)NO
CHEMBL12620 hrh4_human Human Yes 5.4 EC50 = 3981.1 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 CC1=NC=C(N1)CCN
CHEMBL12620 hrh4_human Human Yes 5.4 EC50 = 3981.1 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 CC1=NC=C(N1)CCN
CHEMBL151467 hrh4_human Human Yes 5.4 EC50 = 3981.1 Funct
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 0.7 C1CC(CNC1)CC2=CN=CN2
CHEMBL3393542 hrh4_human Human No 8.4 EC50 = 4 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 2.0 CCCCNC1=NC=CC(=N1)N2CCC(C2)NC
CHEMBL3393542 hrh4_human Human No 8.4 EC50 = 4 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 2.0 CCCCNC1=NC=CC(=N1)N2CCC(C2)NC
CHEMBL521996 hrh4_mouse Mouse No 8.4 EC50 = 4.4 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 2.6 CNC1CCN(C1)C2=NC(=NC3=C2CCCC4=CC=CC=C43)N
CHEMBL521996 hrh4_mouse Mouse No 8.4 EC50 = 4.4 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 2.6 CNC1CCN(C1)C2=NC(=NC3=C2CCCC4=CC=CC=C43)N
CHEMBL1096431 hrh4_human Human No 8.3 EC50 = 4.6 Funct
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 8 3 3 3.4 CC(CC(=O)NC(=NCCCC1=CN=CN1)N)C2CCCCC2
CHEMBL1096431 hrh4_human Human No 8.3 EC50 = 4.6 Funct
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 8 3 3 3.4 CC(CC(=O)NC(=NCCCC1=CN=CN1)N)C2CCCCC2
CHEMBL523225 hrh4_mouse Mouse No 8.3 EC50 = 4.8 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 6 2.3 C1CC2=C(C=C(C=C2)F)C3=C(C1)C(=NC(=N3)N)N4CCNCC4
CHEMBL523225 hrh4_mouse Mouse No 8.3 EC50 = 4.8 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 6 2.3 C1CC2=C(C=C(C=C2)F)C3=C(C1)C(=NC(=N3)N)N4CCNCC4
CHEMBL443896 hrh4_human Human No 8.3 EC50 = 4.9 Funct
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 5 3 3 -0.1 CC(=O)NC(=NCCCC1=CN=CN1)N
CHEMBL443896 hrh4_human Human No 8.3 EC50 = 4.9 Funct
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 5 3 3 -0.1 CC(=O)NC(=NCCCC1=CN=CN1)N
CHEMBL320279 hrh4_human Human No 4.4 EC50 = 40738.0 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 -0.7 C1=CC(OC1CN)C2=CN=CN2
CHEMBL2165641 hrh4_human Human No 7.4 EC50 = 41.7 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
473 17 6 6 1.2 C1=C(NC=N1)CCCN=C(N)NC(=O)CCCCCCC(=O)NC(=NCCCC2=CN=CN2)N
CHEMBL440730 hrh4_human Human Yes 6.4 EC50 = 416.9 Funct
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 0.3 C1CNCC1CC2=CN=CN2
CHEMBL493478 hrh4_rat Rat No 7.4 EC50 = 42.7 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(CC1)C2=NC(=NC=C2N)N
CHEMBL492274 hrh4_rat Rat No 7.4 EC50 = 42.7 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 2.1 CC1=CC=CC(=C1)C2=CC(=NC(=N2)N)N3CCN(CC3)C
CHEMBL493478 hrh4_rat Rat No 7.4 EC50 = 42.7 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(CC1)C2=NC(=NC=C2N)N
CHEMBL492274 hrh4_rat Rat No 7.4 EC50 = 42.7 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 2.1 CC1=CC=CC(=C1)C2=CC(=NC(=N2)N)N3CCN(CC3)C
CHEMBL501882 hrh4_human Human Yes 7.4 EC50 = 43.7 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 0.1 CN1CCN(CC1)C2=NC(=NC=C2)N
CHEMBL493719 hrh4_rat Rat No 7.4 EC50 = 43.7 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 1.8 CN1CCN(CC1)C2=NC(=NC(=C2)C3=CC=CC=C3OC)N
CHEMBL594490 hrh4_human Human No 7.4 EC50 = 43.7 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 2.1 CN1CCN(CC1)C2=NC(=NC(=C2)N3CCC4=CC=CC=C4C3)N
CHEMBL501882 hrh4_human Human Yes 7.4 EC50 = 43.7 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 0.1 CN1CCN(CC1)C2=NC(=NC=C2)N
CHEMBL493719 hrh4_rat Rat No 7.4 EC50 = 43.7 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 1.8 CN1CCN(CC1)C2=NC(=NC(=C2)C3=CC=CC=C3OC)N
CHEMBL594490 hrh4_human Human No 7.4 EC50 = 43.7 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 2.1 CN1CCN(CC1)C2=NC(=NC(=C2)N3CCC4=CC=CC=C4C3)N
CHEMBL3805514 hrh4_human Human No 7.4 EC50 = 44 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 4 3 3 -0.8 CC(=N)SCCN=C(N)N
CHEMBL3805514 hrh4_human Human No 7.4 EC50 = 44 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 4 3 3 -0.8 CC(=N)SCCN=C(N)N
CHEMBL492231 hrh4_mouse Mouse No 7.3 EC50 = 45.7 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 2.9 C1CCC2=C(C(C1)C3=CC=CC=C3)N=C(N=C2N4CCNCC4)N
CHEMBL492231 hrh4_mouse Mouse No 7.3 EC50 = 45.7 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 2.9 C1CCC2=C(C(C1)C3=CC=CC=C3)N=C(N=C2N4CCNCC4)N
CHEMBL444782 hrh4_rat Rat No 7.3 EC50 = 46.8 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 1.4 CN1CCN(CC1)C2=NC(=NC(=C2)N3CCCCC3)N
CHEMBL444782 hrh4_rat Rat No 7.3 EC50 = 46.8 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 1.4 CN1CCN(CC1)C2=NC(=NC(=C2)N3CCCCC3)N
CHEMBL3220640 hrh4_human Human No 6.3 EC50 = 467.7 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 10 3 4 2.6 CC1=NC=C(N1)CCCN=C(NCCSC2=CC=CC=C2)NC#N
CHEMBL489663 hrh4_rat Rat Yes 5.3 EC50 = 4677.4 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 2 1 5 1.8 CC(C)(C)C1=NC(=CC(=N1)N)N2CCN(CC2)C
CHEMBL492489 hrh4_rat Rat No 5.3 EC50 = 4677.4 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 3 0 5 2.5 CC(C)(C)C1=CC(=NC(=N1)OC)N2CCN(CC2)C
CHEMBL494678 hrh4_rat Rat Yes 5.3 EC50 = 4677.4 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 1.5 CN1CCN(CC1)C2=NC(=NC(=C2)C3=CC=C(C=C3)C#N)N
CHEMBL489663 hrh4_rat Rat Yes 5.3 EC50 = 4677.4 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 2 1 5 1.8 CC(C)(C)C1=NC(=CC(=N1)N)N2CCN(CC2)C
CHEMBL492489 hrh4_rat Rat No 5.3 EC50 = 4677.4 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 3 0 5 2.5 CC(C)(C)C1=CC(=NC(=N1)OC)N2CCN(CC2)C
CHEMBL494678 hrh4_rat Rat Yes 5.3 EC50 = 4677.4 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 1.5 CN1CCN(CC1)C2=NC(=NC(=C2)C3=CC=C(C=C3)C#N)N
CHEMBL1082771 hrh4_human Human No 6.3 EC50 = 470 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 5 3.6 CC1=C(C=CC(=C1)OCCCN2CCC(C2)N)C3=NC4=C(N3)C=CC(=C4C)F
CHEMBL1082771 hrh4_human Human No 6.3 EC50 = 470 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 5 3.6 CC1=C(C=CC(=C1)OCCCN2CCC(C2)N)C3=NC4=C(N3)C=CC(=C4C)F
CHEMBL595880 hrh4_human Human No 6.3 EC50 = 478.6 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 4 2 8 1.8 CN1CCN(CC1)C2=CC(=NC(=N2)N)NCC3=CC(=CC=C3)[N+](=O)[O-]
CHEMBL595880 hrh4_human Human No 6.3 EC50 = 478.6 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 4 2 8 1.8 CN1CCN(CC1)C2=CC(=NC(=N2)N)NCC3=CC(=CC=C3)[N+](=O)[O-]
CHEMBL3393529 hrh4_human Human No 7.3 EC50 = 48 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 2.3 CCCCNC1=NC=CC(=C1)N2CCC(C2)NC
CHEMBL3393529 hrh4_human Human No 7.3 EC50 = 48 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 2.3 CCCCNC1=NC=CC(=C1)N2CCC(C2)NC
CHEMBL492677 hrh4_rat Rat No 6.3 EC50 = 489.8 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 1.9 CN1CCN(CC1)C2=NC(=NC(=C2)NCC3=CC=CC=C3)N
CHEMBL495112 hrh4_rat Rat Yes 6.3 EC50 = 489.8 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 0.4 CNC1=NC(=NC(=C1)N2CCN(CC2)C)N
CHEMBL492677 hrh4_rat Rat No 6.3 EC50 = 489.8 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 1.9 CN1CCN(CC1)C2=NC(=NC(=C2)NCC3=CC=CC=C3)N
CHEMBL495112 hrh4_rat Rat Yes 6.3 EC50 = 489.8 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 0.4 CNC1=NC(=NC(=C1)N2CCN(CC2)C)N
CHEMBL495265 hrh4_human Human No 5.3 EC50 = 4897.8 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
269 2 0 4 3.1 CC(C)(C)C1=CC(=NC(=N1)Cl)N2CCN(CC2)C
CHEMBL495265 hrh4_human Human No 5.3 EC50 = 4897.8 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
269 2 0 4 3.1 CC(C)(C)C1=CC(=NC(=N1)Cl)N2CCN(CC2)C
CHEMBL502347 hrh4_mouse Mouse No 8.2 EC50 = 5.8 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 2.1 C1CC2=CC=CC=C2C3=C(C1)C(=NC(=N3)N)N4CCC(C4)N
CHEMBL502347 hrh4_mouse Mouse No 8.2 EC50 = 5.8 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 2.1 C1CC2=CC=CC=C2C3=C(C1)C(=NC(=N3)N)N4CCC(C4)N
CHEMBL1770964 hrh4_human Human No 7.3 EC50 = 50 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 2.1 CC(C)CNC1=CC(=CC(=N1)N)N2CCN(CC2)C
CHEMBL1086460 hrh4_human Human No 7.3 EC50 = 50 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
397 6 1 5 4.2 CC1=C(C=CC(=C1)OCCCN2CCN(CC2)C)C3=NC4=C(N3)C=CC(=C4C)F
CHEMBL1770964 hrh4_human Human No 7.3 EC50 = 50 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 2.1 CC(C)CNC1=CC(=CC(=N1)N)N2CCN(CC2)C
CHEMBL1086460 hrh4_human Human No 7.3 EC50 = 50 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
397 6 1 5 4.2 CC1=C(C=CC(=C1)OCCCN2CCN(CC2)C)C3=NC4=C(N3)C=CC(=C4C)F
CHEMBL1196470 hrh4_human Human No 7.3 EC50 = 50.1 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 4 3 -1.4 C(CSC(=N)N)N=C(N)N
CHEMBL1196470 hrh4_human Human No 7.3 EC50 = 50.1 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 4 3 -1.4 C(CSC(=N)N)N=C(N)N
CHEMBL3805220 hrh4_human Human No 6.3 EC50 = 500 Funct
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
369 9 3 4 2.8 C1CC(CC1CN=C(NCCSC2=CC=CC=C2)NC#N)C3=CN=CN3
CHEMBL3805220 hrh4_human Human No 6.3 EC50 = 500 Funct
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
369 9 3 4 2.8 C1CC(CC1CN=C(NCCSC2=CC=CC=C2)NC#N)C3=CN=CN3
CHEMBL1632412 hrh4_rat Rat No 6.3 EC50 = 501.2 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 4 1.5 CC1=CC2=CC(=C(C3CCN(CC3)C)NO)N=C2C=C1
CHEMBL1632412 hrh4_rat Rat No 6.3 EC50 = 501.2 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 4 1.5 CC1=CC2=CC(=C(C3CCN(CC3)C)NO)N=C2C=C1
CHEMBL175782 hrh4_human Human Yes 5.3 EC50 = 5011.9 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 1.1 CN1CCC(CC1)CC2=CN=CN2
CHEMBL321920 hrh4_human Human No 5.3 EC50 = 5011.9 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 C1CC(OC1CN)C2=CN=CN2
CHEMBL175782 hrh4_human Human Yes 5.3 EC50 = 5011.9 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 1.1 CN1CCC(CC1)CC2=CN=CN2
CHEMBL321920 hrh4_human Human No 5.3 EC50 = 5011.9 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 C1CC(OC1CN)C2=CN=CN2
CHEMBL19439 hrh4_human Human Yes 7.3 EC50 = 51 Funct
Inhibition of human Histamine H4 receptorInhibition of human Histamine H4 receptor
170 4 3 3 0.2 C1=C(NC=N1)CCSC(=N)N
CHEMBL455016 hrh4_rat Rat No 5.3 EC50 = 5128.6 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 3 1 5 2.5 CC(C)(C)C1=CC(=NC(=N1)NC)N2CCN(CC2)C
CHEMBL493103 hrh4_rat Rat No 5.3 EC50 = 5128.6 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 1.5 CN1CCN(CC1)C2=NC(=NC(=C2OC)C3=CC=C(C=C3)C#N)N
CHEMBL455016 hrh4_rat Rat No 5.3 EC50 = 5128.6 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 3 1 5 2.5 CC(C)(C)C1=CC(=NC(=N1)NC)N2CCN(CC2)C
CHEMBL493103 hrh4_rat Rat No 5.3 EC50 = 5128.6 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 1.5 CN1CCN(CC1)C2=NC(=NC(=C2OC)C3=CC=C(C=C3)C#N)N
CHEMBL3804862 hrh4_human Human No 6.3 EC50 = 524 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 9 3 4 2.2 C1CC(CC1CN=C(NCCOC2=CC=CC=C2)NC#N)C3=CN=CN3
CHEMBL3804862 hrh4_human Human No 6.3 EC50 = 524 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 9 3 4 2.2 C1CC(CC1CN=C(NCCOC2=CC=CC=C2)NC#N)C3=CN=CN3
CHEMBL1770962 hrh4_human Human No 6.3 EC50 = 533 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 1.6 CC(C)NC1=CC(=CC(=N1)N)N2CCN(CC2)C
CHEMBL1770962 hrh4_human Human No 6.3 EC50 = 533 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 1.6 CC(C)NC1=CC(=CC(=N1)N)N2CCN(CC2)C
CHEMBL3804906 hrh4_mouse Mouse No 6.3 EC50 = 538 Funct
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 5 3 3 0.6 CN=C(NCC1CCC(C1)C2=CN=CN2)NC#N
CHEMBL3804906 hrh4_mouse Mouse No 6.3 EC50 = 538 Funct
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 5 3 3 0.6 CN=C(NCC1CCC(C1)C2=CN=CN2)NC#N
CHEMBL492231 hrh4_rat Rat No 7.3 EC50 = 55.0 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 2.9 C1CCC2=C(C(C1)C3=CC=CC=C3)N=C(N=C2N4CCNCC4)N
CHEMBL492231 hrh4_rat Rat No 7.3 EC50 = 55.0 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 2.9 C1CCC2=C(C(C1)C3=CC=CC=C3)N=C(N=C2N4CCNCC4)N
CHEMBL1083162 hrh4_mouse Mouse No 6.3 EC50 = 548 Funct
Displacement of [3H]histamine from mouse recombinant histamine H4 receptorDisplacement of [3H]histamine from mouse recombinant histamine H4 receptor
407 9 3 5 4.0 CC1=C(C=CC(=C1)OCCCNCCC2=CN=CN2)C3=NC4=C(N3)C=CC(=C4C)F
CHEMBL1083162 hrh4_mouse Mouse No 6.3 EC50 = 548 Funct
Displacement of [3H]histamine from mouse recombinant histamine H4 receptorDisplacement of [3H]histamine from mouse recombinant histamine H4 receptor
407 9 3 5 4.0 CC1=C(C=CC(=C1)OCCCNCCC2=CN=CN2)C3=NC4=C(N3)C=CC(=C4C)F
CHEMBL3805431 hrh4_human Human No 6.3 EC50 = 549 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
369 9 3 4 2.8 C1CC(CC1CN=C(NCCSC2=CC=CC=C2)NC#N)C3=CN=CN3
CHEMBL3805431 hrh4_human Human No 6.3 EC50 = 549 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
369 9 3 4 2.8 C1CC(CC1CN=C(NCCSC2=CC=CC=C2)NC#N)C3=CN=CN3
CHEMBL3220639 hrh4_human Human No 6.3 EC50 = 549.5 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 6 3 3 0.5 CC1=NC=C(N1)CCCNC(=NC)NC#N
CHEMBL322988 hrh4_human Human Yes 6.3 EC50 = 549.5 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 -0.3 CC(CN)C1=CN=CN1
CHEMBL321920 hrh4_human Human No 5.3 EC50 = 5495.4 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 C1CC(OC1CN)C2=CN=CN2
CHEMBL492885 hrh4_rat Rat No 7.3 EC50 = 56.2 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 2.1 CC1=CC=C(C=C1)C2=CC(=NC(=N2)N)N3CCN(CC3)C
CHEMBL595215 hrh4_human Human No 7.3 EC50 = 56.2 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
367 4 2 6 3.2 CN1CCN(CC1)C2=CC(=NC(=N2)N)NCC3=CC(=C(C=C3)Cl)Cl
CHEMBL492885 hrh4_rat Rat No 7.3 EC50 = 56.2 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 2.1 CC1=CC=C(C=C1)C2=CC(=NC(=N2)N)N3CCN(CC3)C
CHEMBL595215 hrh4_human Human No 7.3 EC50 = 56.2 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
367 4 2 6 3.2 CN1CCN(CC1)C2=CC(=NC(=N2)N)NCC3=CC(=C(C=C3)Cl)Cl
CHEMBL1077580 hrh4_human Human No 6.2 EC50 = 575.4 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 11 3 4 1.7 C1=CC=NC(=C1)CCCN=C(NCCCCC2=CN=CN2)NC#N
CHEMBL1077580 hrh4_human Human No 6.2 EC50 = 575.4 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 11 3 4 1.7 C1=CC=NC(=C1)CCCN=C(NCCCCC2=CN=CN2)NC#N
CHEMBL494678 hrh4_rat Rat Yes 7.2 EC50 = 58.9 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 1.5 CN1CCN(CC1)C2=NC(=NC(=C2)C3=CC=C(C=C3)C#N)N
CHEMBL492900 hrh4_rat Rat No 7.2 EC50 = 58.9 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 1.9 CC1=C(N=C(N=C1N2CCN(CC2)C)N)C3=CC=C(C=C3)C#N
CHEMBL494678 hrh4_rat Rat Yes 7.2 EC50 = 58.9 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 1.5 CN1CCN(CC1)C2=NC(=NC(=C2)C3=CC=C(C=C3)C#N)N
CHEMBL494678 hrh4_rat Rat Yes 7.2 EC50 = 58.9 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 1.5 CN1CCN(CC1)C2=NC(=NC(=C2)C3=CC=C(C=C3)C#N)N
CHEMBL492900 hrh4_rat Rat No 7.2 EC50 = 58.9 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 1.9 CC1=C(N=C(N=C1N2CCN(CC2)C)N)C3=CC=C(C=C3)C#N
CHEMBL494678 hrh4_rat Rat Yes 7.2 EC50 = 58.9 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 1.5 CN1CCN(CC1)C2=NC(=NC(=C2)C3=CC=C(C=C3)C#N)N
CHEMBL310360 hrh4_human Human Yes 4.2 EC50 = 58884.4 Funct
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 1.3 C1=CC=NC(=C1)CCC2=CN=CN2
CHEMBL3805220 hrh4_mouse Mouse No 6.2 EC50 = 589 Funct
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
369 9 3 4 2.8 C1CC(CC1CN=C(NCCSC2=CC=CC=C2)NC#N)C3=CN=CN3
CHEMBL3805220 hrh4_mouse Mouse No 6.2 EC50 = 589 Funct
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
369 9 3 4 2.8 C1CC(CC1CN=C(NCCSC2=CC=CC=C2)NC#N)C3=CN=CN3
CHEMBL594721 hrh4_human Human No 8.2 EC50 = 6.0 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
333 4 2 6 2.6 CN1CCN(CC1)C2=CC(=NC(=N2)N)NCC3=CC=CC=C3Cl
CHEMBL594721 hrh4_human Human No 8.2 EC50 = 6.0 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
333 4 2 6 2.6 CN1CCN(CC1)C2=CC(=NC(=N2)N)NCC3=CC=CC=C3Cl
CHEMBL523225 hrh4_rat Rat No 8.2 EC50 = 6.0 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 6 2.3 C1CC2=C(C=C(C=C2)F)C3=C(C1)C(=NC(=N3)N)N4CCNCC4
CHEMBL523225 hrh4_rat Rat No 8.2 EC50 = 6.0 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 6 2.3 C1CC2=C(C=C(C=C2)F)C3=C(C1)C(=NC(=N3)N)N4CCNCC4
CHEMBL502339 hrh4_human Human No 8.2 EC50 = 6.3 Funct
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 8 3 4 1.8 CC(CC(=O)NC(=NCCCC1=CN=CN1)N)C2=CC=CS2
CHEMBL502339 hrh4_human Human No 8.2 EC50 = 6.3 Funct
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 8 3 4 1.8 CC(CC(=O)NC(=NCCCC1=CN=CN1)N)C2=CC=CS2
CHEMBL521996 hrh4_rat Rat No 8.2 EC50 = 6.6 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 2.6 CNC1CCN(C1)C2=NC(=NC3=C2CCCC4=CC=CC=C43)N
CHEMBL521996 hrh4_rat Rat No 8.2 EC50 = 6.6 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 2.6 CNC1CCN(C1)C2=NC(=NC3=C2CCCC4=CC=CC=C43)N
CHEMBL1084869 hrh4_human Human No 8.2 EC50 = 6.9 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
411 8 3 5 4.2 CC1=C(C=CC(=C1)OCCCNCC2CCCNC2)C3=NC4=C(N3)C=CC(=C4C)F
CHEMBL1084869 hrh4_human Human No 8.2 EC50 = 6.9 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
411 8 3 5 4.2 CC1=C(C=CC(=C1)OCCCNCC2CCCNC2)C3=NC4=C(N3)C=CC(=C4C)F
CHEMBL609289 hrh4_human Human No 6.2 EC50 = 602.6 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 1.7 CN1CCN(CC1)C2=CC(=NC(=N2)N)NCC3=CC=C(C=C3)C#N
CHEMBL609289 hrh4_human Human No 6.2 EC50 = 602.6 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 1.7 CN1CCN(CC1)C2=CC(=NC(=N2)N)NCC3=CC=C(C=C3)C#N
CHEMBL1094142 hrh4_human Human No 5.2 EC50 = 6025.6 Funct
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
366 8 3 5 4.3 CC1=C(SC(=N1)N)CCCN=C(N)NC(=O)CC(C)C2CCCCC2
CHEMBL1094142 hrh4_human Human No 5.2 EC50 = 6025.6 Funct
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
366 8 3 5 4.3 CC1=C(SC(=N1)N)CCCN=C(N)NC(=O)CC(C)C2CCCCC2
CHEMBL1082772 hrh4_human Human No 7.2 EC50 = 62 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
397 7 2 5 4.1 CC1=C(C=CC(=C1)OCCCN2CCC(C2)NC)C3=NC4=C(N3)C=CC(=C4C)F
CHEMBL1082772 hrh4_human Human No 7.2 EC50 = 62 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
397 7 2 5 4.1 CC1=C(C=CC(=C1)OCCCN2CCC(C2)NC)C3=NC4=C(N3)C=CC(=C4C)F
CHEMBL3804906 hrh4_human Human No 7.2 EC50 = 63 Funct
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 5 3 3 0.6 CN=C(NCC1CCC(C1)C2=CN=CN2)NC#N
CHEMBL3804906 hrh4_human Human No 7.2 EC50 = 63 Funct
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 5 3 3 0.6 CN=C(NCC1CCC(C1)C2=CN=CN2)NC#N
CHEMBL19173 hrh4_human Human No 7.2 EC50 = 63.1 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 2.1 C1=CC=C(C=C1)COCCCC2=CN=CN2
CHEMBL72769 hrh4_human Human No 7.2 EC50 = 63.1 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 1.3 CCCNC(=S)NCCCCC1=CN=CN1
CHEMBL72372 hrh4_human Human No 7.2 EC50 = 63.1 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
337 8 3 2 2.9 C1=CC(=CC=C1CNC(=S)NCCCCCC2=CN=CN2)Cl
CHEMBL1632414 hrh4_mouse Mouse No 7.2 EC50 = 63.1 Funct
Agonist activity at mouse histamine H4 receptor by luciferase reporter gene assayAgonist activity at mouse histamine H4 receptor by luciferase reporter gene assay
293 1 2 5 2.5 CN1CCC(CC1)C(=C2NC3=C(N2)C=C(C=C3)Cl)N=O
CHEMBL19173 hrh4_human Human No 7.2 EC50 = 63.1 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 2.1 C1=CC=C(C=C1)COCCCC2=CN=CN2
CHEMBL72769 hrh4_human Human No 7.2 EC50 = 63.1 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 1.3 CCCNC(=S)NCCCCC1=CN=CN1
CHEMBL72372 hrh4_human Human No 7.2 EC50 = 63.1 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
337 8 3 2 2.9 C1=CC(=CC=C1CNC(=S)NCCCCCC2=CN=CN2)Cl
CHEMBL1632414 hrh4_mouse Mouse No 7.2 EC50 = 63.1 Funct
Agonist activity at mouse histamine H4 receptor by luciferase reporter gene assayAgonist activity at mouse histamine H4 receptor by luciferase reporter gene assay
293 1 2 5 2.5 CN1CCC(CC1)C(=C2NC3=C(N2)C=C(C=C3)Cl)N=O
CHEMBL268229 hrh4_human Human Yes 6.2 EC50 = 631.0 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 CC(CC1=CN=CN1)N
CHEMBL493477 hrh4_rat Rat No 6.2 EC50 = 631.0 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 0.1 CN1CCN(CC1)C2=NC(=NC=C2OC)N
CHEMBL268229 hrh4_human Human Yes 6.2 EC50 = 631.0 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 CC(CC1=CN=CN1)N
CHEMBL493477 hrh4_rat Rat No 6.2 EC50 = 631.0 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 0.1 CN1CCN(CC1)C2=NC(=NC=C2OC)N
CHEMBL492677 hrh4_human Human No 7.2 EC50 = 64.6 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 1.9 CN1CCN(CC1)C2=NC(=NC(=C2)NCC3=CC=CC=C3)N
CHEMBL492677 hrh4_human Human No 7.2 EC50 = 64.6 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 1.9 CN1CCN(CC1)C2=NC(=NC(=C2)NCC3=CC=CC=C3)N
CHEMBL446896 hrh4_rat Rat Yes 7.2 EC50 = 66.1 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 0.5 CC1=CN=C(N=C1N2CCN(CC2)C)N
CHEMBL446896 hrh4_rat Rat Yes 7.2 EC50 = 66.1 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 0.5 CC1=CN=C(N=C1N2CCN(CC2)C)N
CHEMBL472441 hrh4_human Human No 7.2 EC50 = 66.3 Funct
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 9 3 5 2.3 C1=CC=C(C=C1)C(CC(=O)NC(=NCCCC2=CN=CN2)N)C3=NC=CS3
CHEMBL472441 hrh4_human Human No 7.2 EC50 = 66.3 Funct
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 9 3 5 2.3 C1=CC=C(C=C1)C(CC(=O)NC(=NCCCC2=CN=CN2)N)C3=NC=CS3
CHEMBL492631 hrh4_rat Rat No 7.2 EC50 = 67.6 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 2 1 5 1.8 CC(C)(C)C1=CC(=NC(=N1)N)N2CCN(CC2)C
CHEMBL492631 hrh4_rat Rat No 7.2 EC50 = 67.6 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 2 1 5 1.8 CC(C)(C)C1=CC(=NC(=N1)N)N2CCN(CC2)C
CHEMBL505061 hrh4_rat Rat No 7.2 EC50 = 69.2 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 1.1 CN1CCN(CC1)C2=NC(=NC(=C2)N3CCCC3)N
CHEMBL505061 hrh4_rat Rat No 7.2 EC50 = 69.2 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 1.1 CN1CCN(CC1)C2=NC(=NC(=C2)N3CCCC3)N
CHEMBL514641 hrh4_human Human No 8.2 EC50 = 7.1 Funct
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 8 4 3 1.9 C1=CC=C2C(=C1)C(=CN2)CCC(=O)NC(=NCCCC3=CN=CN3)N
CHEMBL514641 hrh4_human Human No 8.2 EC50 = 7.1 Funct
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 8 4 3 1.9 C1=CC=C2C(=C1)C(=CN2)CCC(=O)NC(=NCCCC3=CN=CN3)N
CHEMBL3236553 hrh4_mouse Mouse No 8.1 EC50 = 7.3 Funct
Partial agonist activity at mouse histamine H4 receptorPartial agonist activity at mouse histamine H4 receptor
247 2 2 5 1.3 C1CCC(C1)C2=CC(=NC(=N2)N)N3CCNCC3
CHEMBL3236553 hrh4_mouse Mouse No 8.1 EC50 = 7.3 Funct
Partial agonist activity at mouse histamine H4 receptorPartial agonist activity at mouse histamine H4 receptor
247 2 2 5 1.3 C1CCC(C1)C2=CC(=NC(=N2)N)N3CCNCC3
CHEMBL471413 hrh4_human Human No 8.1 EC50 = 7.9 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 9 3 3 3.2 C1=CC=C(C=C1)C(CC(=O)NC(=NCCCC2=CN=CN2)N)C3=CC=CC=C3
CHEMBL471413 hrh4_human Human No 8.1 EC50 = 7.9 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 9 3 3 3.2 C1=CC=C(C=C1)C(CC(=O)NC(=NCCCC2=CN=CN2)N)C3=CC=CC=C3
CHEMBL275443 hrh4_human Human Yes 7.2 EC50 = 70.8 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 CC1=C(N=CN1)CCN
CHEMBL275443 hrh4_human Human Yes 7.2 EC50 = 70.8 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 CC1=C(N=CN1)CCN
CHEMBL1077756 hrh4_human Human No 6.2 EC50 = 708.0 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 8 3 3 0.7 CCNC(=NCCCCC1=CN=CN1)NC#N
CHEMBL1077756 hrh4_human Human No 6.2 EC50 = 708.0 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 8 3 3 0.7 CCNC(=NCCCCC1=CN=CN1)NC#N
CHEMBL13795 hrh4_human Human Yes 5.2 EC50 = 7079.5 Funct
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 -0.6 C1C(C1N)C2=CN=CN2
CHEMBL1086085 hrh4_human Human No 6.2 EC50 = 710 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 5 4.1 CC1=C(C=CC(=C1)OCCCN2C3C2CN(C3)C)C4=NC5=C(N4)C=CC(=C5C)F
CHEMBL1086085 hrh4_human Human No 6.2 EC50 = 710 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 5 4.1 CC1=C(C=CC(=C1)OCCCN2C3C2CN(C3)C)C4=NC5=C(N4)C=CC(=C5C)F
CHEMBL105803 hrh4_human Human No 6.1 EC50 = 741.3 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 1.7 C1CC(OC1COCC2=CC=CC=C2)C3=CN=CN3
CHEMBL153061 hrh4_human Human Yes 6.1 EC50 = 741.3 Funct
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 0.3 C1CNCC1CC2=CN=CN2
CHEMBL3393543 hrh4_human Human Yes 7.1 EC50 = 75 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 2.1 CN1CCN(CC1)C2=NC(=NC=C2)NC3CCCC3
CHEMBL3393543 hrh4_human Human Yes 7.1 EC50 = 75 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 2.1 CN1CCN(CC1)C2=NC(=NC=C2)NC3CCCC3
CHEMBL1078210 hrh4_human Human No 6.1 EC50 = 758.6 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 10 3 3 2.3 C1=CC=C(C=C1)CCCN=C(NCCCC2=CN=CN2)NC#N
CHEMBL1078210 hrh4_human Human No 6.1 EC50 = 758.6 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 10 3 3 2.3 C1=CC=C(C=C1)CCCN=C(NCCCC2=CN=CN2)NC#N
CHEMBL106913 hrh4_human Human No 5.1 EC50 = 7585.8 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 C1CC(OC1CN)C2=CN=CN2
CHEMBL108649 hrh4_human Human No 5.1 EC50 = 7585.8 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 5 3 4 -0.3 CN=C(NCC1CCC(O1)C2=CN=CN2)NC#N
CHEMBL107877 hrh4_human Human No 4.1 EC50 = 75857.8 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 -0.7 C1=CC(OC1CN)C2=CN=CN2
CHEMBL321860 hrh4_human Human No 7.1 EC50 = 77.6 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 5 3 4 -0.3 CN=C(NCC1CCC(O1)C2=CN=CN2)NC#N
CHEMBL3220630 hrh4_human Human No 6.1 EC50 = 776.3 Funct
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 8 3 4 1.8 CC(CC(=O)NC(=NCCCC1=NC=CN1)N)C2=CC=CS2
CHEMBL321860 hrh4_human Human No 7.1 EC50 = 78 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 5 3 4 -0.3 CN=C(NCC1CCC(O1)C2=CN=CN2)NC#N
CHEMBL321860 hrh4_human Human No 7.1 EC50 = 78 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 5 3 4 -0.3 CN=C(NCC1CCC(O1)C2=CN=CN2)NC#N
CHEMBL321860 hrh4_human Human No 7.1 EC50 = 79.4 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 5 3 4 -0.3 CN=C(NCC1CCC(O1)C2=CN=CN2)NC#N
CHEMBL72431 hrh4_human Human No 7.1 EC50 = 79.4 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 1.9 C1=CC=C(C=C1)CNC(=S)NCCCCC2=CN=CN2
CHEMBL1632414 hrh4_human Human No 7.1 EC50 = 79.4 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
293 1 2 5 2.5 CN1CCC(CC1)C(=C2NC3=C(N2)C=C(C=C3)Cl)N=O
CHEMBL2165640 hrh4_human Human No 7.1 EC50 = 79.4 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
445 15 6 6 0.2 C1=C(NC=N1)CCCN=C(N)NC(=O)CCCCC(=O)NC(=NCCCC2=CN=CN2)N
CHEMBL321860 hrh4_human Human No 7.1 EC50 = 79.4 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 5 3 4 -0.3 CN=C(NCC1CCC(O1)C2=CN=CN2)NC#N
CHEMBL72431 hrh4_human Human No 7.1 EC50 = 79.4 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 1.9 C1=CC=C(C=C1)CNC(=S)NCCCCC2=CN=CN2
CHEMBL1632414 hrh4_human Human No 7.1 EC50 = 79.4 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
293 1 2 5 2.5 CN1CCC(CC1)C(=C2NC3=C(N2)C=C(C=C3)Cl)N=O
CHEMBL105803 hrh4_human Human No 6.1 EC50 = 794.3 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 1.7 C1CC(OC1COCC2=CC=CC=C2)C3=CN=CN3
CHEMBL268490 hrh4_human Human Yes 6.1 EC50 = 794.3 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 CNCCC1=CN=CN1
CHEMBL105803 hrh4_human Human No 6.1 EC50 = 794.3 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 1.7 C1CC(OC1COCC2=CC=CC=C2)C3=CN=CN3
CHEMBL268490 hrh4_human Human Yes 6.1 EC50 = 794.3 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 CNCCC1=CN=CN1
CHEMBL106913 hrh4_human Human No 5.1 EC50 = 7943.3 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 C1CC(OC1CN)C2=CN=CN2
CHEMBL108649 hrh4_human Human No 5.1 EC50 = 7943.3 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 5 3 4 -0.3 CN=C(NCC1CCC(O1)C2=CN=CN2)NC#N
CHEMBL448085 hrh4_rat Rat No 5.1 EC50 = 7943.3 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 6 0.2 CN1CCN(CC1)C2=NC(=NC(=C2)N3C=CN=C3)N
CHEMBL493261 hrh4_rat Rat Yes 5.1 EC50 = 7943.3 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 2 1 5 1.8 CC(C)(C)C1=CC(=NC(=N1)N2CCN(CC2)C)N
CHEMBL505346 hrh4_rat Rat Yes 5.1 EC50 = 7943.3 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 0.1 CN1CCN(CC1)C2=NC(=NC(=C2)C3=CN=CN=C3)N
CHEMBL106913 hrh4_human Human No 5.1 EC50 = 7943.3 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 C1CC(OC1CN)C2=CN=CN2
CHEMBL108649 hrh4_human Human No 5.1 EC50 = 7943.3 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 5 3 4 -0.3 CN=C(NCC1CCC(O1)C2=CN=CN2)NC#N
CHEMBL448085 hrh4_rat Rat No 5.1 EC50 = 7943.3 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 6 0.2 CN1CCN(CC1)C2=NC(=NC(=C2)N3C=CN=C3)N
CHEMBL493261 hrh4_rat Rat Yes 5.1 EC50 = 7943.3 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 2 1 5 1.8 CC(C)(C)C1=CC(=NC(=N1)N2CCN(CC2)C)N
CHEMBL505346 hrh4_rat Rat Yes 5.1 EC50 = 7943.3 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 0.1 CN1CCN(CC1)C2=NC(=NC(=C2)C3=CN=CN=C3)N
CHEMBL325327 hrh4_human Human Yes 8.1 EC50 = 8.1 Funct
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 3 2 -0.8 C1=C(NC=N1)CCCN=C(N)N
CHEMBL325327 hrh4_human Human Yes 8.1 EC50 = 8.1 Funct
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 3 2 -0.8 C1=C(NC=N1)CCCN=C(N)N
CHEMBL1096430 hrh4_human Human No 8.1 EC50 = 8.3 Funct
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 8 3 3 3.4 CC(CC(=O)NC(=NCCCC1=CN=CN1)N)C2CCCCC2
CHEMBL1096430 hrh4_human Human No 8.1 EC50 = 8.3 Funct
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 8 3 3 3.4 CC(CC(=O)NC(=NCCCC1=CN=CN1)N)C2CCCCC2
CHEMBL2165628 hrh4_human Human No 8.1 EC50 = 8.5 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
547 19 6 8 3.3 CC1=C(SC(=N1)N)CCCN=C(N)NC(=O)CCCCCCCCC(=O)NC(=NCCCC2=CN=CN2)N
CHEMBL2165642 hrh4_human Human No 8.1 EC50 = 8.5 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
501 19 6 6 2.3 C1=C(NC=N1)CCCN=C(N)NC(=O)CCCCCCCCC(=O)NC(=NCCCC2=CN=CN2)N
CHEMBL594731 hrh4_human Human No 8.1 EC50 = 8.5 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 2.3 CC1=CC=CC=C1CNC2=NC(=NC(=C2)N3CCN(CC3)C)N
CHEMBL594731 hrh4_human Human No 8.1 EC50 = 8.5 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 2.3 CC1=CC=CC=C1CNC2=NC(=NC(=C2)N3CCN(CC3)C)N
CHEMBL471413 hrh4_human Human No 8.1 EC50 = 8.6 Funct
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 9 3 3 3.2 C1=CC=C(C=C1)C(CC(=O)NC(=NCCCC2=CN=CN2)N)C3=CC=CC=C3
CHEMBL471413 hrh4_human Human No 8.1 EC50 = 8.6 Funct
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 9 3 3 3.2 C1=CC=C(C=C1)C(CC(=O)NC(=NCCCC2=CN=CN2)N)C3=CC=CC=C3
CHEMBL379102 hrh4_human Human No 7.1 EC50 = 81.3 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
346 1 0 4 3.2 CN1CCN(CC1)C2=NC3=C(C=CC(=C3)Cl)OC4=C2C=C(C=C4)F
CHEMBL379102 hrh4_human Human No 7.1 EC50 = 81.3 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
346 1 0 4 3.2 CN1CCN(CC1)C2=NC3=C(C=CC(=C3)Cl)OC4=C2C=C(C=C4)F
CHEMBL451108 hrh4_rat Rat No 5.1 EC50 = 8317.6 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 1.7 CN1CCN(CC1)C2=NC(=NC=C2C3=CC=CC=C3)N
CHEMBL451108 hrh4_rat Rat No 5.1 EC50 = 8317.6 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 1.7 CN1CCN(CC1)C2=NC(=NC=C2C3=CC=CC=C3)N
CHEMBL3393538 hrh4_human Human Yes 7.1 EC50 = 84 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 2.1 CC(C)CNC1=NC=CC(=N1)N2CCN(CC2)C
CHEMBL3393538 hrh4_human Human Yes 7.1 EC50 = 84 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 2.1 CC(C)CNC1=NC=CC(=N1)N2CCN(CC2)C
CHEMBL319658 hrh4_human Human No 4.1 EC50 = 85113.8 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 -0.7 C1=CC(OC1CN)C2=CN=CN2
CHEMBL1770985 hrh4_human Human No 7.1 EC50 = 86 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 1.8 CC(C)CNC1=NC(=CC(=N1)N)N2CCN(CC2)C
CHEMBL3393544 hrh4_human Human No 7.1 EC50 = 86 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 2.0 CNC1CCN(C1)C2=NC(=NC=C2)NC3CCCC3
CHEMBL1770985 hrh4_human Human No 7.1 EC50 = 86 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 1.8 CC(C)CNC1=NC(=CC(=N1)N)N2CCN(CC2)C
CHEMBL3393544 hrh4_human Human No 7.1 EC50 = 86 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 2.0 CNC1CCN(C1)C2=NC(=NC=C2)NC3CCCC3
CHEMBL495265 hrh4_rat Rat No 5.1 EC50 = 8709.6 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 0 4 3.1 CC(C)(C)C1=CC(=NC(=N1)Cl)N2CCN(CC2)C
CHEMBL495265 hrh4_rat Rat No 5.1 EC50 = 8709.6 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 0 4 3.1 CC(C)(C)C1=CC(=NC(=N1)Cl)N2CCN(CC2)C
CHEMBL90019 hrh4_human Human Yes 7.1 EC50 = 89.1 Funct
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 -0.3 C1=C(NC=N1)CCCCN
CHEMBL90019 hrh4_human Human Yes 7.1 EC50 = 89.1 Funct
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 -0.3 C1=C(NC=N1)CCCCN
CHEMBL442865 hrh4_rat Rat No 6.1 EC50 = 891.3 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 2.4 CN1CCN(CC1)C2=NC(=NC(=C2)C3=CC(=CC=C3)I)N
CHEMBL442865 hrh4_rat Rat No 6.1 EC50 = 891.3 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 2.4 CN1CCN(CC1)C2=NC(=NC(=C2)C3=CC(=CC=C3)I)N
CHEMBL492652 hrh4_rat Rat No 5.1 EC50 = 8912.5 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 2.5 CN1CCN(CC1)C2=CC(=NC(=N2)N)SC3=CC=CC=C3
CHEMBL492652 hrh4_rat Rat No 5.1 EC50 = 8912.5 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 2.5 CN1CCN(CC1)C2=CC(=NC(=N2)N)SC3=CC=CC=C3
CHEMBL522673 hrh4_mouse Mouse No 8.0 EC50 = 9.1 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 2.2 CNC1CN(C1)C2=NC(=NC3=C2CCCC4=CC=CC=C43)N
CHEMBL522673 hrh4_mouse Mouse No 8.0 EC50 = 9.1 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 2.2 CNC1CN(C1)C2=NC(=NC3=C2CCCC4=CC=CC=C43)N
CHEMBL522673 hrh4_rat Rat No 8.0 EC50 = 9.3 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 2.2 CNC1CN(C1)C2=NC(=NC3=C2CCCC4=CC=CC=C43)N
CHEMBL522673 hrh4_rat Rat No 8.0 EC50 = 9.3 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 2.2 CNC1CN(C1)C2=NC(=NC3=C2CCCC4=CC=CC=C43)N
CHEMBL3393541 hrh4_human Human Yes 7.0 EC50 = 91 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 2.0 CCCCNC1=NC=CC(=N1)N2CCN(CC2)C
CHEMBL3393541 hrh4_human Human Yes 7.0 EC50 = 91 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 2.0 CCCCNC1=NC=CC(=N1)N2CCN(CC2)C
CHEMBL593103 hrh4_human Human No 7.0 EC50 = 91.2 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 7 2.0 CN1CCN(CC1)C2=CC(=NC(=N2)N)NCC3=CC=C(C=C3)F
CHEMBL593103 hrh4_human Human No 7.0 EC50 = 91.2 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 7 2.0 CN1CCN(CC1)C2=CC(=NC(=N2)N)NCC3=CC=C(C=C3)F
CHEMBL3752085 hrh4_human Human Yes 6.0 EC50 = 912.0 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 3.9 CN1CCN(CC1)C2=NC(=NC(=C2)C3=CC=CC=C3)NCC4=CC=CC=C4
CHEMBL3752085 hrh4_human Human Yes 6.0 EC50 = 912.0 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 3.9 CN1CCN(CC1)C2=NC(=NC(=C2)C3=CC=CC=C3)NCC4=CC=CC=C4
CHEMBL82298 hrh4_human Human Yes 6.0 EC50 = 912.0 Funct
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 0.9 C1=CN=CC=C1CC2=CN=CN2
CHEMBL507063 hrh4_rat Rat Yes 7.0 EC50 = 93.3 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 1.0 CN1CCN(CC1)C2=NC(=NC(=C2)C3=C(N=CC=C3)OC)N
CHEMBL507063 hrh4_rat Rat Yes 7.0 EC50 = 93.3 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 1.0 CN1CCN(CC1)C2=NC(=NC(=C2)C3=C(N=CC=C3)OC)N
CHEMBL495342 hrh4_rat Rat No 6.0 EC50 = 933.3 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 2 0 4 2.2 CC(C)(C)C1=CC(=NC=N1)N2CCN(CC2)C
CHEMBL3752270 hrh4_human Human No 6.0 EC50 = 933.3 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
386 4 1 5 4.2 CN1CCN(CC1)C2=NC(=NC3=C2CCC4=CC=CC=C43)NCC5=CC=CC=C5
CHEMBL495342 hrh4_rat Rat No 6.0 EC50 = 933.3 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 2 0 4 2.2 CC(C)(C)C1=CC(=NC=N1)N2CCN(CC2)C
CHEMBL3752270 hrh4_human Human No 6.0 EC50 = 933.3 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
386 4 1 5 4.2 CN1CCN(CC1)C2=NC(=NC3=C2CCC4=CC=CC=C43)NCC5=CC=CC=C5
CHEMBL493100 hrh4_rat Rat No 5.0 EC50 = 9772.4 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 6 1 5 2.4 CC(C)(C)C1=CC(=NC(=N1)N)N(C)CCCN(C)C
CHEMBL493100 hrh4_rat Rat No 5.0 EC50 = 9772.4 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 6 1 5 2.4 CC(C)(C)C1=CC(=NC(=N1)N)N(C)CCCN(C)C
CHEMBL1915540 hrh4_human Human Yes 9.2 IC50 = 0.7 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 1.1 CNC1CCN(C1)C2=CC(=NC(=N2)N)NCC3CC3
CHEMBL1915540 hrh4_human Human Yes 9.2 IC50 = 0.7 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 1.1 CNC1CCN(C1)C2=CC(=NC(=N2)N)NCC3CC3
CHEMBL1091874 hrh4_human Human No 9.0 IC50 = 1 Funct
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 2 2 6 2.5 CNC1CCN(C1)C2=NC(=NC3=C2OC4=C3C=C(C=C4)Cl)N
CHEMBL1091874 hrh4_human Human No 9.0 IC50 = 1 Funct
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 2 2 6 2.5 CNC1CCN(C1)C2=NC(=NC3=C2OC4=C3C=C(C=C4)Cl)N
CHEMBL1915540 hrh4_human Human Yes 8.9 IC50 = 1.3 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 1.1 CNC1CCN(C1)C2=CC(=NC(=N2)N)NCC3CC3
CHEMBL1915540 hrh4_human Human Yes 8.9 IC50 = 1.3 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 1.1 CNC1CCN(C1)C2=CC(=NC(=N2)N)NCC3CC3
CHEMBL591969 hrh4_human Human No 8.0 IC50 = 10 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
385 5 2 8 2.0 CN1CCN(CC1)C2=NC3=C(C=C(C=C3)Cl)C(=N2)NCCS(=O)(=O)N
CHEMBL591969 hrh4_human Human No 8.0 IC50 = 10 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
385 5 2 8 2.0 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 Funct
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
319 1 1 3 1.9 CN1CCN(CC1)C2=NC(=O)NC3=C2OC4=C3C=C(C=C4)Cl
CHEMBL1093438 hrh4_human Human No 6.0 IC50 = 1000 Funct
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
319 1 1 3 1.9 CN1CCN(CC1)C2=NC(=O)NC3=C2OC4=C3C=C(C=C4)Cl
CHEMBL1767164 hrh4_human Human Yes 5.0 IC50 = 10000 Funct
Binding affinity to human histamine H4 receptorBinding affinity to human histamine H4 receptor
641 14 0 5 8.3 C1CCCN(CC1)CCCOC2=CC=C(C=C2)CCCCN3CCCC3CN4C(=O)C5=CC=CC=C5C(=N4)CC6=CC=C(C=C6)Cl
CHEMBL1092331 hrh4_human Human No 5.0 IC50 = 10000 Funct
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
331 1 0 5 3.8 CC1CN(CC(N1C)C)C2=NC=NC3=C2OC4=C3C=C(C=C4)Cl
CHEMBL1767164 hrh4_human Human Yes 5.0 IC50 = 10000 Funct
Binding affinity to human histamine H4 receptorBinding affinity to human histamine H4 receptor
641 14 0 5 8.3 C1CCCN(CC1)CCCOC2=CC=C(C=C2)CCCCN3CCCC3CN4C(=O)C5=CC=CC=C5C(=N4)CC6=CC=C(C=C6)Cl
CHEMBL1092331 hrh4_human Human No 5.0 IC50 = 10000 Funct
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
331 1 0 5 3.8 CC1CN(CC(N1C)C)C2=NC=NC3=C2OC4=C3C=C(C=C4)Cl
CHEMBL1935574 hrh4_human Human No 7.0 IC50 = 106 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 1.7 C1CN(CCN1)C2=NC(=NC3=C2C=CC(=C3)C4=CC=CO4)N
CHEMBL1935574 hrh4_human Human No 7.0 IC50 = 106 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 1.7 C1CN(CCN1)C2=NC(=NC3=C2C=CC(=C3)C4=CC=CO4)N
CHEMBL213886 hrh4_human Human No 7.0 IC50 = 110 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
276 6 2 2 2.6 C1C(C1C2=CN=CN2)CCNCC3=CC=C(C=C3)Cl
CHEMBL213886 hrh4_human Human No 7.0 IC50 = 110 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
276 6 2 2 2.6 C1C(C1C2=CN=CN2)CCNCC3=CC=C(C=C3)Cl
CHEMBL657 hrh4_human Human Yes 5.0 IC50 = 11000 Funct
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 3.3 CN(C)CCOC(C1=CC=CC=C1)C2=CC=CC=C2
CHEMBL1092332 hrh4_human Human No 7.0 IC50 = 111 Funct
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
315 1 0 5 3.2 CN1CC2CC1CN2C3=NC=NC4=C3OC5=C4C=C(C=C5)Cl
CHEMBL1092332 hrh4_human Human No 7.0 IC50 = 111 Funct
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
315 1 0 5 3.2 CN1CC2CC1CN2C3=NC=NC4=C3OC5=C4C=C(C=C5)Cl
CHEMBL2376800 hrh4_human Human No 7.0 IC50 = 112.2 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 0.9 CCC1=CC2=C(C(=NC(=N2)N)N3CC(C3)NC)N=C1
CHEMBL2376801 hrh4_human Human No 6.9 IC50 = 125.9 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 1.2 CCC1=CC2=C(C(=NC(=N2)N)N3CCC(C3)NC)N=C1
CHEMBL1090532 hrh4_human Human No 6.9 IC50 = 126 Funct
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
289 1 1 5 2.4 C1CN(CC1N)C2=NC=NC3=C2OC4=C3C=C(C=C4)Cl
CHEMBL1090532 hrh4_human Human No 6.9 IC50 = 126 Funct
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
289 1 1 5 2.4 C1CN(CC1N)C2=NC=NC3=C2OC4=C3C=C(C=C4)Cl
CHEMBL1091875 hrh4_human Human No 7.9 IC50 = 13 Funct
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 2 2 6 2.5 CNC1CCN(C1)C2=NC(=NC3=C2OC4=C3C=C(C=C4)Cl)N
CHEMBL1091875 hrh4_human Human No 7.9 IC50 = 13 Funct
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 2 2 6 2.5 CNC1CCN(C1)C2=NC(=NC3=C2OC4=C3C=C(C=C4)Cl)N
CHEMBL185951 hrh4_human Human Yes 6.9 IC50 = 138 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
279 1 1 3 1.7 CN1CCN(CC1)C(=O)C2=NC3=C(N2)C=C(C=C3)Cl
CHEMBL185951 hrh4_human Human Yes 6.9 IC50 = 138 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
279 1 1 3 1.7 CN1CCN(CC1)C(=O)C2=NC3=C(N2)C=C(C=C3)Cl
CHEMBL1090520 hrh4_human Human No 5.9 IC50 = 1400 Funct
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
329 1 1 5 3.3 C1CC2CN(CC2NC1)C3=NC=NC4=C3OC5=C4C=C(C=C5)Cl
CHEMBL1090519 hrh4_human Human No 5.9 IC50 = 1400 Funct
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 1 5 3.1 CC1(CCN(C1)C2=NC=NC3=C2OC4=C3C=C(C=C4)Cl)NC
CHEMBL1090520 hrh4_human Human No 5.9 IC50 = 1400 Funct
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
329 1 1 5 3.3 C1CC2CN(CC2NC1)C3=NC=NC4=C3OC5=C4C=C(C=C5)Cl
CHEMBL1090519 hrh4_human Human No 5.9 IC50 = 1400 Funct
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 1 5 3.1 CC1(CCN(C1)C2=NC=NC3=C2OC4=C3C=C(C=C4)Cl)NC
CHEMBL1092543 hrh4_human Human No 4.9 IC50 = 14200 Funct
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
371 2 1 8 3.8 CNC1CCN(C1)C2=NC(=NC3=C2OC4=C3C=C(C=C4)Cl)C(F)(F)F
CHEMBL1092543 hrh4_human Human No 4.9 IC50 = 14200 Funct
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
371 2 1 8 3.8 CNC1CCN(C1)C2=NC(=NC3=C2OC4=C3C=C(C=C4)Cl)C(F)(F)F
CHEMBL454890 hrh4_human Human No 6.8 IC50 = 144.5 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
358 4 1 6 3.3 CN1CCN(CC1)C2=NC3=C(C=C(C=C3)Cl)C(=N2)NCC4=COC=C4
CHEMBL454890 hrh4_human Human No 6.8 IC50 = 144.5 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
358 4 1 6 3.3 CN1CCN(CC1)C2=NC3=C(C=C(C=C3)Cl)C(=N2)NCC4=COC=C4
CHEMBL214312 hrh4_human Human No 5.8 IC50 = 1500 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 2.8 C1CCC(CC1)CNCCC2CC2C3=CN=CN3
CHEMBL214312 hrh4_human Human No 5.8 IC50 = 1500 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 2.8 C1CCC(CC1)CNCCC2CC2C3=CN=CN3
CHEMBL1091559 hrh4_human Human No 5.8 IC50 = 1600 Funct
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 1 5 3.3 CC1=NC2=C(C(=N1)N3CCC(C3)NC)OC4=C2C=C(C=C4)Cl
CHEMBL1091559 hrh4_human Human No 5.8 IC50 = 1600 Funct
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 1 5 3.3 CC1=NC2=C(C(=N1)N3CCC(C3)NC)OC4=C2C=C(C=C4)Cl
CHEMBL1172 hrh4_human Human Yes 4.8 IC50 = 16000 Funct
Histamine H-4 Receptor Binding Assay: Histamine H-4 Receptor Binding AssayHistamine H-4 Receptor Binding Assay: Histamine H-4 Receptor Binding Assay
311 0 1 2 4.5 C1CC2=C(C=CC(=C2)Cl)C(=C3CCNCC3)C4=C1C=CC=N4
CHEMBL3290578 hrh4_human Human No 5.8 IC50 = 1630 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
349 2 1 6 2.2 CN1CCN(CC1)C2=NC(=NC(=N2)C3=CC=C(C=C3)Br)N
CHEMBL3290578 hrh4_human Human No 5.8 IC50 = 1630 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
349 2 1 6 2.2 CN1CCN(CC1)C2=NC(=NC(=N2)C3=CC=C(C=C3)Br)N
CHEMBL1092933 hrh4_human Human No 6.8 IC50 = 169 Funct
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
329 1 0 5 3.5 CN1CC2CCC1CN2C3=NC=NC4=C3OC5=C4C=C(C=C5)Cl
CHEMBL1092933 hrh4_human Human No 6.8 IC50 = 169 Funct
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
329 1 0 5 3.5 CN1CC2CCC1CN2C3=NC=NC4=C3OC5=C4C=C(C=C5)Cl
CHEMBL1092064 hrh4_human Human No 6.8 IC50 = 171 Funct
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
303 2 1 5 2.9 CNC1CCN(C1)C2=NC=NC3=C2OC4=C3C=CC(=C4)Cl
CHEMBL1092064 hrh4_human Human No 6.8 IC50 = 171 Funct
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
303 2 1 5 2.9 CNC1CCN(C1)C2=NC=NC3=C2OC4=C3C=CC(=C4)Cl
CHEMBL1093180 hrh4_human Human Yes 7.7 IC50 = 19 Funct
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
303 1 0 5 2.9 CN1CCN(CC1)C2=NC=NC3=C2OC4=C3C=C(C=C4)Cl
CHEMBL1093180 hrh4_human Human Yes 7.7 IC50 = 19 Funct
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
303 1 0 5 2.9 CN1CCN(CC1)C2=NC=NC3=C2OC4=C3C=C(C=C4)Cl
CHEMBL1092330 hrh4_human Human No 5.7 IC50 = 1900 Funct
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 1 0 5 3.4 CC1CN(CCN1C)C2=NC=NC3=C2OC4=C3C=C(C=C4)Cl
CHEMBL1092330 hrh4_human Human No 5.7 IC50 = 1900 Funct
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 1 0 5 3.4 CC1CN(CCN1C)C2=NC=NC3=C2OC4=C3C=C(C=C4)Cl
CHEMBL1222728 hrh4_human Human Yes 4.7 IC50 = 20000 Funct
Antagonist activity at human histamine H4 receptorAntagonist activity at human histamine H4 receptor
348 5 0 5 2.5 CN1CCN(CC1)C(C2=CC=CC=C2)C3=NN=NN3CC4=CC=CC=C4
CHEMBL1222728 hrh4_human Human Yes 4.7 IC50 = 20000 Funct
Antagonist activity at human histamine H4 receptorAntagonist activity at human histamine H4 receptor
348 5 0 5 2.5 CN1CCN(CC1)C(C2=CC=CC=C2)C3=NN=NN3CC4=CC=CC=C4
CHEMBL1088888 hrh4_human Human No 4.7 IC50 = 21000 Funct
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 0 5 3.4 CN(C)C1CCN(C1)C2=NC=NC3=C2OC4=C3C=C(C=C4)Cl
CHEMBL1088888 hrh4_human Human No 4.7 IC50 = 21000 Funct
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 0 5 3.4 CN(C)C1CCN(C1)C2=NC=NC3=C2OC4=C3C=C(C=C4)Cl
CHEMBL1090655 hrh4_human Human No 6.6 IC50 = 236 Funct
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
329 1 0 5 3.5 C1CC2CN(CCN2C1)C3=NC=NC4=C3OC5=C4C=C(C=C5)Cl
CHEMBL1090655 hrh4_human Human No 6.6 IC50 = 236 Funct
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
329 1 0 5 3.5 C1CC2CN(CCN2C1)C3=NC=NC4=C3OC5=C4C=C(C=C5)Cl
CHEMBL1090531 hrh4_human Human No 6.5 IC50 = 285 Funct
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
303 2 1 5 2.9 CNC1CCN(C1)C2=NC=NC3=C2OC4=C3C=C(C=C4)Cl
CHEMBL1090531 hrh4_human Human No 6.6 IC50 = 285 Funct
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
303 2 1 5 2.9 CNC1CCN(C1)C2=NC=NC3=C2OC4=C3C=C(C=C4)Cl
CHEMBL1090531 hrh4_human Human No 6.5 IC50 = 292 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
303 2 1 5 2.9 CNC1CCN(C1)C2=NC=NC3=C2OC4=C3C=C(C=C4)Cl
CHEMBL1090531 hrh4_human Human No 6.5 IC50 = 292 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
303 2 1 5 2.9 CNC1CCN(C1)C2=NC=NC3=C2OC4=C3C=C(C=C4)Cl
CHEMBL1091874 hrh4_human Human No 8.5 IC50 = 3 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
318 2 2 6 2.5 CNC1CCN(C1)C2=NC(=NC3=C2OC4=C3C=C(C=C4)Cl)N
CHEMBL1091874 hrh4_human Human No 8.5 IC50 = 3 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
318 2 2 6 2.5 CNC1CCN(C1)C2=NC(=NC3=C2OC4=C3C=C(C=C4)Cl)N
CHEMBL1088859 hrh4_human Human No 7.5 IC50 = 30 Funct
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 8 3.1 CNC1CCN(C1)C2=NC=NC3=C2OC4=C3C=C(C=C4)C(F)(F)F
CHEMBL1088859 hrh4_human Human No 7.5 IC50 = 30 Funct
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 8 3.1 CNC1CCN(C1)C2=NC=NC3=C2OC4=C3C=C(C=C4)C(F)(F)F
CHEMBL1093138 hrh4_human Human No 6.5 IC50 = 310 Funct
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
343 2 0 5 3.5 CN1CCN(CC1)C2=NC(=NC3=C2OC4=C3C=C(C=C4)Cl)C5CC5
CHEMBL1093138 hrh4_human Human No 6.5 IC50 = 310 Funct
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
343 2 0 5 3.5 CN1CCN(CC1)C2=NC(=NC3=C2OC4=C3C=C(C=C4)Cl)C5CC5
CHEMBL1090190 hrh4_human Human No 7.5 IC50 = 33 Funct
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
303 2 1 5 2.9 CNC1CCN(C1)C2=NC=NC3=C2OC4=C3C=C(C=C4)Cl
CHEMBL1090190 hrh4_human Human No 7.5 IC50 = 33 Funct
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
303 2 1 5 2.9 CNC1CCN(C1)C2=NC=NC3=C2OC4=C3C=C(C=C4)Cl
CHEMBL592379 hrh4_human Human No 7.5 IC50 = 33.1 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
461 7 2 8 4.0 CN1CCN(CC1)C2=NC3=C(C=C(C=C3)Cl)C(=N2)NCCS(=O)(=O)NC4=CC=CC=C4
CHEMBL592379 hrh4_human Human No 7.5 IC50 = 33.1 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
461 7 2 8 4.0 CN1CCN(CC1)C2=NC3=C(C=C(C=C3)Cl)C(=N2)NCCS(=O)(=O)NC4=CC=CC=C4
CHEMBL1091558 hrh4_human Human Yes 7.4 IC50 = 37 Funct
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 1 0 5 3.3 CC1=NC2=C(C(=N1)N3CCN(CC3)C)OC4=C2C=C(C=C4)Cl
CHEMBL1091558 hrh4_human Human Yes 7.4 IC50 = 37 Funct
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 1 0 5 3.3 CC1=NC2=C(C(=N1)N3CCN(CC3)C)OC4=C2C=C(C=C4)Cl
CHEMBL1092542 hrh4_human Human No 7.4 IC50 = 39 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
371 1 0 8 3.8 CN1CCN(CC1)C2=NC(=NC3=C2OC4=C3C=C(C=C4)Cl)C(F)(F)F
CHEMBL1092542 hrh4_human Human No 7.4 IC50 = 39 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
371 1 0 8 3.8 CN1CCN(CC1)C2=NC(=NC3=C2OC4=C3C=C(C=C4)Cl)C(F)(F)F
CHEMBL1091875 hrh4_human Human No 8.4 IC50 = 4 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
318 2 2 6 2.5 CNC1CCN(C1)C2=NC(=NC3=C2OC4=C3C=C(C=C4)Cl)N
CHEMBL1091875 hrh4_human Human No 8.4 IC50 = 4 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
318 2 2 6 2.5 CNC1CCN(C1)C2=NC(=NC3=C2OC4=C3C=C(C=C4)Cl)N
CHEMBL1915540 hrh4_human Human Yes 8.3 IC50 = 4.9 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 1.1 CNC1CCN(C1)C2=CC(=NC(=N2)N)NCC3CC3
CHEMBL1915540 hrh4_human Human Yes 8.3 IC50 = 4.9 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 1.1 CNC1CCN(C1)C2=CC(=NC(=N2)N)NCC3CC3
CHEMBL1090190 hrh4_human Human No 7.4 IC50 = 41 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
303 2 1 5 2.9 CNC1CCN(C1)C2=NC=NC3=C2OC4=C3C=C(C=C4)Cl
CHEMBL1090190 hrh4_human Human No 7.4 IC50 = 41 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
303 2 1 5 2.9 CNC1CCN(C1)C2=NC=NC3=C2OC4=C3C=C(C=C4)Cl
CHEMBL3628042 hrh4_human Human No 6.4 IC50 = 439 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
331 3 1 6 2.8 CN1CCN(CC1)C2=NC(=NC(=N2)C=CC3=CC(=CC=C3)Cl)N
CHEMBL3628042 hrh4_human Human No 6.4 IC50 = 439 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
331 3 1 6 2.8 CN1CCN(CC1)C2=NC(=NC(=N2)C=CC3=CC(=CC=C3)Cl)N
CHEMBL1092934 hrh4_human Human No 6.4 IC50 = 440 Funct
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
329 1 0 5 3.5 CN1C2CCC1CN(C2)C3=NC=NC4=C3OC5=C4C=C(C=C5)Cl
CHEMBL1092934 hrh4_human Human No 6.4 IC50 = 440 Funct
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
329 1 0 5 3.5 CN1C2CCC1CN(C2)C3=NC=NC4=C3OC5=C4C=C(C=C5)Cl
CHEMBL1935572 hrh4_human Human No 7.3 IC50 = 46 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 2.8 CN1CCN(CC1)C2=NC(=NC3=C2C=CC(=C3)C4=CSC=C4)N
CHEMBL1935572 hrh4_human Human No 7.3 IC50 = 46 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 2.8 CN1CCN(CC1)C2=NC(=NC3=C2C=CC(=C3)C4=CSC=C4)N
CHEMBL1935571 hrh4_human Human No 7.3 IC50 = 47 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(CC1)C2=NC(=NC3=C2C=CC(=C3)C4=COC=C4)N
CHEMBL3290576 hrh4_human Human No 6.3 IC50 = 512 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
305 2 1 6 2.9 CN1CCN(CC1)C2=NC(=NC(=N2)C3=CC=C(C=C3)Cl)N
CHEMBL3290576 hrh4_human Human No 6.3 IC50 = 512 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
305 2 1 6 2.9 CN1CCN(CC1)C2=NC(=NC(=N2)C3=CC=C(C=C3)Cl)N
CHEMBL1915540 hrh4_human Human Yes 7.3 IC50 = 53.7 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 1.1 CNC1CCN(C1)C2=CC(=NC(=N2)N)NCC3CC3
CHEMBL185951 hrh4_human Human Yes 6.3 IC50 = 530 Funct
Inhibition of human eosinophil chemotaxis mediated by histamine H4 receptorInhibition of human eosinophil chemotaxis mediated by histamine H4 receptor
279 1 1 3 1.7 CN1CCN(CC1)C(=O)C2=NC3=C(N2)C=C(C=C3)Cl
CHEMBL185951 hrh4_human Human Yes 6.3 IC50 = 530 Funct
Inhibition of human eosinophil chemotaxis mediated by histamine H4 receptorInhibition of human eosinophil chemotaxis mediated by histamine H4 receptor
279 1 1 3 1.7 CN1CCN(CC1)C(=O)C2=NC3=C(N2)C=C(C=C3)Cl
CHEMBL3629828 hrh4_human Human No 6.2 IC50 = 606 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 2.6 CC1=CC=CC(=C1)C=CC2=NC(=NC(=N2)N)N3CCN(CC3)C
CHEMBL3629828 hrh4_human Human No 6.2 IC50 = 606 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 2.6 CC1=CC=CC(=C1)C=CC2=NC(=NC(=N2)N)N3CCN(CC3)C
CHEMBL1092880 hrh4_human Human No 5.2 IC50 = 6200 Funct
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(C1)C2=NC=NC3=C2OC4=C3C=C(C=C4)C#N
CHEMBL1092880 hrh4_human Human No 5.2 IC50 = 6200 Funct
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(C1)C2=NC=NC3=C2OC4=C3C=C(C=C4)C#N
CHEMBL452847 hrh4_human Human No 7.2 IC50 = 69.2 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
374 4 1 6 4.0 CN1CCN(CC1)C2=NC3=C(C=C(C=C3)Cl)C(=N2)NCC4=CC=CS4
CHEMBL452847 hrh4_human Human No 7.2 IC50 = 69.2 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
374 4 1 6 4.0 CN1CCN(CC1)C2=NC3=C(C=C(C=C3)Cl)C(=N2)NCC4=CC=CS4
CHEMBL1092332 hrh4_human Human No 7.2 IC50 = 70 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
315 1 0 5 3.2 CN1CC2CC1CN2C3=NC=NC4=C3OC5=C4C=C(C=C5)Cl
CHEMBL1092332 hrh4_human Human No 7.2 IC50 = 70 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
315 1 0 5 3.2 CN1CC2CC1CN2C3=NC=NC4=C3OC5=C4C=C(C=C5)Cl
CHEMBL2376804 hrh4_human Human No 7.2 IC50 = 70.8 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 1.0 CNC1CN(C1)C2=NC(=NC3=C2N=CC(=C3)C4CC4)N
CHEMBL1091569 hrh4_human Human No 7.1 IC50 = 76 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
289 2 1 5 2.5 CNC1CN(C1)C2=NC=NC3=C2OC4=C3C=C(C=C4)Cl
CHEMBL1091569 hrh4_human Human No 7.1 IC50 = 76 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
289 2 1 5 2.5 CNC1CN(C1)C2=NC=NC3=C2OC4=C3C=C(C=C4)Cl
CHEMBL1935573 hrh4_human Human No 7.1 IC50 = 83 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