Ligand source activities (1 row/activity)



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Ligands Receptor Assay information Chemical information
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name		 GPCRdb ID #Vendors Reference
ligand		 Fold selectivity
(Potency)		 # tested GPCRs
(Potency)		 Species p-value
(-log)		 Type Activity
Relation		 Activity
Value		 Assay Type Assay Description Source Mol
weight		 Rot
Bonds		 H don H acc LogP Smiles DOI
155524115 176523 0 None -1 3 Rat 10.3 pEC50 = 10.3 Functional
Agonist activity at rat H4R expressed in HEK293-SF-rH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at rat H4R expressed in HEK293-SF-rH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 286 3 2 5 2.2 CC(C)(C)CNc1nccc(N2CCc3nc[nH]c3C2)n1 10.1021/acs.jmedchem.9b01342
CHEMBL4454158 176523 0 None -1 3 Rat 10.3 pEC50 = 10.3 Functional
Agonist activity at rat H4R expressed in HEK293-SF-rH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at rat H4R expressed in HEK293-SF-rH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 286 3 2 5 2.2 CC(C)(C)CNc1nccc(N2CCc3nc[nH]c3C2)n1 10.1021/acs.jmedchem.9b01342
CHEMBL4597218 176523 0 None -1 3 Rat 10.3 pEC50 = 10.3 Functional
Agonist activity at rat H4R expressed in HEK293-SF-rH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at rat H4R expressed in HEK293-SF-rH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 286 3 2 5 2.2 CC(C)(C)CNc1nccc(N2CCc3nc[nH]c3C2)n1 10.1021/acs.jmedchem.9b01342
155524115 176523 0 None 1 3 Human 9.9 pEC50 = 9.9 Functional
Agonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 286 3 2 5 2.2 CC(C)(C)CNc1nccc(N2CCc3nc[nH]c3C2)n1 10.1021/acs.jmedchem.9b01342
CHEMBL4454158 176523 0 None 1 3 Human 9.9 pEC50 = 9.9 Functional
Agonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 286 3 2 5 2.2 CC(C)(C)CNc1nccc(N2CCc3nc[nH]c3C2)n1 10.1021/acs.jmedchem.9b01342
CHEMBL4597218 176523 0 None 1 3 Human 9.9 pEC50 = 9.9 Functional
Agonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 286 3 2 5 2.2 CC(C)(C)CNc1nccc(N2CCc3nc[nH]c3C2)n1 10.1021/acs.jmedchem.9b01342
155524115 176523 0 None -4 3 Mouse 9.6 pEC50 = 9.6 Functional
Agonist activity at mouse H4R expressed in HEK293-SF-mH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at mouse H4R expressed in HEK293-SF-mH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 286 3 2 5 2.2 CC(C)(C)CNc1nccc(N2CCc3nc[nH]c3C2)n1 10.1021/acs.jmedchem.9b01342
CHEMBL4454158 176523 0 None -4 3 Mouse 9.6 pEC50 = 9.6 Functional
Agonist activity at mouse H4R expressed in HEK293-SF-mH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at mouse H4R expressed in HEK293-SF-mH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 286 3 2 5 2.2 CC(C)(C)CNc1nccc(N2CCc3nc[nH]c3C2)n1 10.1021/acs.jmedchem.9b01342
CHEMBL4597218 176523 0 None -4 3 Mouse 9.6 pEC50 = 9.6 Functional
Agonist activity at mouse H4R expressed in HEK293-SF-mH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at mouse H4R expressed in HEK293-SF-mH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 286 3 2 5 2.2 CC(C)(C)CNc1nccc(N2CCc3nc[nH]c3C2)n1 10.1021/acs.jmedchem.9b01342
46235428 6572 0 None 263 3 Human 9.3 pEC50 = 9.3 Functional
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
ChEMBL 407 9 3 4 4.3 Cc1cc(OCCCNCCc2c[nH]cn2)ccc1-c1nc2c(C)c(F)ccc2[nH]1 10.1016/j.bmcl.2010.04.017
CHEMBL1083162 6572 0 None 263 3 Human 9.3 pEC50 = 9.3 Functional
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
ChEMBL 407 9 3 4 4.3 Cc1cc(OCCCNCCc2c[nH]cn2)ccc1-c1nc2c(C)c(F)ccc2[nH]1 10.1016/j.bmcl.2010.04.017
58227401 176427 0 None 2 3 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 263 4 2 5 1.7 CN[C@@H]1CCN(c2ccnc(NCC(C)(C)C)n2)C1 10.1021/acs.jmedchem.9b01342
CHEMBL4443126 176427 0 None 2 3 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 263 4 2 5 1.7 CN[C@@H]1CCN(c2ccnc(NCC(C)(C)C)n2)C1 10.1021/acs.jmedchem.9b01342
CHEMBL4596409 176427 0 None 2 3 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 263 4 2 5 1.7 CN[C@@H]1CCN(c2ccnc(NCC(C)(C)C)n2)C1 10.1021/acs.jmedchem.9b01342
58227401 176427 0 None -2 3 Rat 9.2 pEC50 = 9.2 Functional
Agonist activity at rat H4R expressed in HEK293-SF-rH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at rat H4R expressed in HEK293-SF-rH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 263 4 2 5 1.7 CN[C@@H]1CCN(c2ccnc(NCC(C)(C)C)n2)C1 10.1021/acs.jmedchem.9b01342
CHEMBL4443126 176427 0 None -2 3 Rat 9.2 pEC50 = 9.2 Functional
Agonist activity at rat H4R expressed in HEK293-SF-rH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at rat H4R expressed in HEK293-SF-rH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 263 4 2 5 1.7 CN[C@@H]1CCN(c2ccnc(NCC(C)(C)C)n2)C1 10.1021/acs.jmedchem.9b01342
CHEMBL4596409 176427 0 None -2 3 Rat 9.2 pEC50 = 9.2 Functional
Agonist activity at rat H4R expressed in HEK293-SF-rH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at rat H4R expressed in HEK293-SF-rH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 263 4 2 5 1.7 CN[C@@H]1CCN(c2ccnc(NCC(C)(C)C)n2)C1 10.1021/acs.jmedchem.9b01342
155513612 176296 0 None -18 3 Rat 9.2 pEC50 = 9.2 Functional
Agonist activity at rat H4R expressed in HEK293-SF-rH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at rat H4R expressed in HEK293-SF-rH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 277 4 1 5 2.1 CN(C)[C@@H]1CCN(c2ccnc(NCC(C)(C)C)n2)C1 10.1021/acs.jmedchem.9b01342
CHEMBL4439142 176296 0 None -18 3 Rat 9.2 pEC50 = 9.2 Functional
Agonist activity at rat H4R expressed in HEK293-SF-rH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at rat H4R expressed in HEK293-SF-rH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 277 4 1 5 2.1 CN(C)[C@@H]1CCN(c2ccnc(NCC(C)(C)C)n2)C1 10.1021/acs.jmedchem.9b01342
CHEMBL4515149 176296 0 None -18 3 Rat 9.2 pEC50 = 9.2 Functional
Agonist activity at rat H4R expressed in HEK293-SF-rH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at rat H4R expressed in HEK293-SF-rH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 277 4 1 5 2.1 CN(C)[C@@H]1CCN(c2ccnc(NCC(C)(C)C)n2)C1 10.1021/acs.jmedchem.9b01342
CHEMBL4595327 176296 0 None -18 3 Rat 9.2 pEC50 = 9.2 Functional
Agonist activity at rat H4R expressed in HEK293-SF-rH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at rat H4R expressed in HEK293-SF-rH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 277 4 1 5 2.1 CN(C)[C@@H]1CCN(c2ccnc(NCC(C)(C)C)n2)C1 10.1021/acs.jmedchem.9b01342
51354300 58859 0 None - 1 Human 9.0 pEC50 = 9 Functional
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
ChEMBL 273 6 1 4 2.8 c1nc(CCCn2cc(CC3CCCCC3)nn2)c[nH]1 10.1021/jm1013488
CHEMBL1688946 58859 0 None - 1 Human 9.0 pEC50 = 9 Functional
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
ChEMBL 273 6 1 4 2.8 c1nc(CCCn2cc(CC3CCCCC3)nn2)c[nH]1 10.1021/jm1013488
155491015 176471 4 None -10 4 Mouse 9.0 pEC50 = 9 Functional
Agonist activity at mouse H4R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by luciferase reporter gene assayAgonist activity at mouse H4R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by luciferase reporter gene assay
ChEMBL 207 4 2 5 0.2 CCCNC1CN(c2ccnc(N)n2)C1 10.1021/acs.jmedchem.9b01462
CHEMBL4441731 176471 4 None -10 4 Mouse 9.0 pEC50 = 9 Functional
Agonist activity at mouse H4R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by luciferase reporter gene assayAgonist activity at mouse H4R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by luciferase reporter gene assay
ChEMBL 207 4 2 5 0.2 CCCNC1CN(c2ccnc(N)n2)C1 10.1021/acs.jmedchem.9b01462
CHEMBL4596734 176471 4 None -10 4 Mouse 9.0 pEC50 = 9 Functional
Agonist activity at mouse H4R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by luciferase reporter gene assayAgonist activity at mouse H4R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by luciferase reporter gene assay
ChEMBL 207 4 2 5 0.2 CCCNC1CN(c2ccnc(N)n2)C1 10.1021/acs.jmedchem.9b01462
155513612 176296 0 None -14 3 Mouse 9.0 pEC50 = 9.0 Functional
Agonist activity at mouse H4R expressed in HEK293-SF-mH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at mouse H4R expressed in HEK293-SF-mH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 277 4 1 5 2.1 CN(C)[C@@H]1CCN(c2ccnc(NCC(C)(C)C)n2)C1 10.1021/acs.jmedchem.9b01342
CHEMBL4439142 176296 0 None -14 3 Mouse 9.0 pEC50 = 9.0 Functional
Agonist activity at mouse H4R expressed in HEK293-SF-mH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at mouse H4R expressed in HEK293-SF-mH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 277 4 1 5 2.1 CN(C)[C@@H]1CCN(c2ccnc(NCC(C)(C)C)n2)C1 10.1021/acs.jmedchem.9b01342
CHEMBL4515149 176296 0 None -14 3 Mouse 9.0 pEC50 = 9.0 Functional
Agonist activity at mouse H4R expressed in HEK293-SF-mH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at mouse H4R expressed in HEK293-SF-mH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 277 4 1 5 2.1 CN(C)[C@@H]1CCN(c2ccnc(NCC(C)(C)C)n2)C1 10.1021/acs.jmedchem.9b01342
CHEMBL4595327 176296 0 None -14 3 Mouse 9.0 pEC50 = 9.0 Functional
Agonist activity at mouse H4R expressed in HEK293-SF-mH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at mouse H4R expressed in HEK293-SF-mH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 277 4 1 5 2.1 CN(C)[C@@H]1CCN(c2ccnc(NCC(C)(C)C)n2)C1 10.1021/acs.jmedchem.9b01342
58227401 176427 0 None -2 3 Mouse 9.0 pEC50 = 9.0 Functional
Agonist activity at mouse H4R expressed in HEK293-SF-mH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at mouse H4R expressed in HEK293-SF-mH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 263 4 2 5 1.7 CN[C@@H]1CCN(c2ccnc(NCC(C)(C)C)n2)C1 10.1021/acs.jmedchem.9b01342
CHEMBL4443126 176427 0 None -2 3 Mouse 9.0 pEC50 = 9.0 Functional
Agonist activity at mouse H4R expressed in HEK293-SF-mH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at mouse H4R expressed in HEK293-SF-mH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 263 4 2 5 1.7 CN[C@@H]1CCN(c2ccnc(NCC(C)(C)C)n2)C1 10.1021/acs.jmedchem.9b01342
CHEMBL4596409 176427 0 None -2 3 Mouse 9.0 pEC50 = 9.0 Functional
Agonist activity at mouse H4R expressed in HEK293-SF-mH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at mouse H4R expressed in HEK293-SF-mH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 263 4 2 5 1.7 CN[C@@H]1CCN(c2ccnc(NCC(C)(C)C)n2)C1 10.1021/acs.jmedchem.9b01342
45257132 3656 10 None - 1 Human 9.0 pEC50 = 9.0 Functional
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
ChEMBL 366 4 2 6 2.7 CN1CCN(CC1)c1cc(NCc2c(Cl)cccc2Cl)nc(n1)N 10.1016/j.bmc.2009.08.059
8983 3656 10 None - 1 Human 9.0 pEC50 = 9.0 Functional
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
ChEMBL 366 4 2 6 2.7 CN1CCN(CC1)c1cc(NCc2c(Cl)cccc2Cl)nc(n1)N 10.1016/j.bmc.2009.08.059
CHEMBL595180 3656 10 None - 1 Human 9.0 pEC50 = 9.0 Functional
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
ChEMBL 366 4 2 6 2.7 CN1CCN(CC1)c1cc(NCc2c(Cl)cccc2Cl)nc(n1)N 10.1016/j.bmc.2009.08.059
155552061 176454 0 None 2 3 Rat 8.9 pEC50 = 8.9 Functional
Agonist activity at rat H4R expressed in HEK293-SF-rH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at rat H4R expressed in HEK293-SF-rH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 277 3 1 5 2.1 CN1CCCN(c2ccnc(NCC(C)(C)C)n2)CC1 10.1021/acs.jmedchem.9b01342
CHEMBL4543119 176454 0 None 2 3 Rat 8.9 pEC50 = 8.9 Functional
Agonist activity at rat H4R expressed in HEK293-SF-rH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at rat H4R expressed in HEK293-SF-rH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 277 3 1 5 2.1 CN1CCCN(c2ccnc(NCC(C)(C)C)n2)CC1 10.1021/acs.jmedchem.9b01342
CHEMBL4596606 176454 0 None 2 3 Rat 8.9 pEC50 = 8.9 Functional
Agonist activity at rat H4R expressed in HEK293-SF-rH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at rat H4R expressed in HEK293-SF-rH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 277 3 1 5 2.1 CN1CCCN(c2ccnc(NCC(C)(C)C)n2)CC1 10.1021/acs.jmedchem.9b01342
155517880 176643 0 None 2 3 Rat 8.9 pEC50 = 8.9 Functional
Agonist activity at rat H4R expressed in HEK293-SF-rH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at rat H4R expressed in HEK293-SF-rH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 291 4 4 5 1.0 CC(C)(C)CNc1nccc(N2CC[C@@H](NC(=N)N)C2)n1 10.1021/acs.jmedchem.9b01342
CHEMBL4445423 176643 0 None 2 3 Rat 8.9 pEC50 = 8.9 Functional
Agonist activity at rat H4R expressed in HEK293-SF-rH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at rat H4R expressed in HEK293-SF-rH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 291 4 4 5 1.0 CC(C)(C)CNc1nccc(N2CC[C@@H](NC(=N)N)C2)n1 10.1021/acs.jmedchem.9b01342
CHEMBL4598198 176643 0 None 2 3 Rat 8.9 pEC50 = 8.9 Functional
Agonist activity at rat H4R expressed in HEK293-SF-rH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at rat H4R expressed in HEK293-SF-rH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 291 4 4 5 1.0 CC(C)(C)CNc1nccc(N2CC[C@@H](NC(=N)N)C2)n1 10.1021/acs.jmedchem.9b01342
45257132 3656 10 None - 1 Human 8.9 pEC50 = 8.9 Functional
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
ChEMBL 366 4 2 6 2.7 CN1CCN(CC1)c1cc(NCc2c(Cl)cccc2Cl)nc(n1)N 10.1016/j.bmc.2009.08.059
8983 3656 10 None - 1 Human 8.9 pEC50 = 8.9 Functional
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
ChEMBL 366 4 2 6 2.7 CN1CCN(CC1)c1cc(NCc2c(Cl)cccc2Cl)nc(n1)N 10.1016/j.bmc.2009.08.059
CHEMBL595180 3656 10 None - 1 Human 8.9 pEC50 = 8.9 Functional
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
ChEMBL 366 4 2 6 2.7 CN1CCN(CC1)c1cc(NCc2c(Cl)cccc2Cl)nc(n1)N 10.1016/j.bmc.2009.08.059
58227373 176484 0 None -1 3 Rat 8.8 pEC50 = 8.8 Functional
Agonist activity at rat H4R expressed in HEK293-SF-rH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at rat H4R expressed in HEK293-SF-rH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 249 3 2 5 1.5 CC(C)(C)CNc1nccc(N2CC[C@@H](N)C2)n1 10.1021/acs.jmedchem.9b01342
CHEMBL4455324 176484 0 None -1 3 Rat 8.8 pEC50 = 8.8 Functional
Agonist activity at rat H4R expressed in HEK293-SF-rH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at rat H4R expressed in HEK293-SF-rH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 249 3 2 5 1.5 CC(C)(C)CNc1nccc(N2CC[C@@H](N)C2)n1 10.1021/acs.jmedchem.9b01342
CHEMBL4596881 176484 0 None -1 3 Rat 8.8 pEC50 = 8.8 Functional
Agonist activity at rat H4R expressed in HEK293-SF-rH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at rat H4R expressed in HEK293-SF-rH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 249 3 2 5 1.5 CC(C)(C)CNc1nccc(N2CC[C@@H](N)C2)n1 10.1021/acs.jmedchem.9b01342
155513612 176296 0 None 14 3 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 277 4 1 5 2.1 CN(C)[C@@H]1CCN(c2ccnc(NCC(C)(C)C)n2)C1 10.1021/acs.jmedchem.9b01342
CHEMBL4439142 176296 0 None 14 3 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 277 4 1 5 2.1 CN(C)[C@@H]1CCN(c2ccnc(NCC(C)(C)C)n2)C1 10.1021/acs.jmedchem.9b01342
CHEMBL4515149 176296 0 None 14 3 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 277 4 1 5 2.1 CN(C)[C@@H]1CCN(c2ccnc(NCC(C)(C)C)n2)C1 10.1021/acs.jmedchem.9b01342
CHEMBL4595327 176296 0 None 14 3 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 277 4 1 5 2.1 CN(C)[C@@H]1CCN(c2ccnc(NCC(C)(C)C)n2)C1 10.1021/acs.jmedchem.9b01342
136030655 56452 0 None 1 3 Mouse 8.0 pEC50 = 8 Functional
Agonist activity at mouse histamine H4 receptor by luciferase reporter gene assayAgonist activity at mouse histamine H4 receptor by luciferase reporter gene assay
ChEMBL 292 1 2 3 2.2 CN1CCN(/C(=N\O)c2cc3cc(Cl)ccc3[nH]2)CC1 10.1016/j.bmcl.2010.10.041
CHEMBL1632413 56452 0 None 1 3 Mouse 8.0 pEC50 = 8 Functional
Agonist activity at mouse histamine H4 receptor by luciferase reporter gene assayAgonist activity at mouse histamine H4 receptor by luciferase reporter gene assay
ChEMBL 292 1 2 3 2.2 CN1CCN(/C(=N\O)c2cc3cc(Cl)ccc3[nH]2)CC1 10.1016/j.bmcl.2010.10.041
136030655 56452 0 None -1 3 Rat 8.0 pEC50 = 8 Functional
Agonist activity at rat histamine H4 receptor by luciferase reporter gene assayAgonist activity at rat histamine H4 receptor by luciferase reporter gene assay
ChEMBL 292 1 2 3 2.2 CN1CCN(/C(=N\O)c2cc3cc(Cl)ccc3[nH]2)CC1 10.1016/j.bmcl.2010.10.041
CHEMBL1632413 56452 0 None -1 3 Rat 8.0 pEC50 = 8 Functional
Agonist activity at rat histamine H4 receptor by luciferase reporter gene assayAgonist activity at rat histamine H4 receptor by luciferase reporter gene assay
ChEMBL 292 1 2 3 2.2 CN1CCN(/C(=N\O)c2cc3cc(Cl)ccc3[nH]2)CC1 10.1016/j.bmcl.2010.10.041
25068753 188414 19 None -1 2 Rat 8.0 pEC50 = 8 Functional
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
ChEMBL 295 1 2 5 1.8 Nc1nc2c(c(N3CC[C@@H](N)C3)n1)CCCc1ccccc1-2 10.1021/jm800670r
CHEMBL502347 188414 19 None -1 2 Rat 8.0 pEC50 = 8 Functional
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
ChEMBL 295 1 2 5 1.8 Nc1nc2c(c(N3CC[C@@H](N)C3)n1)CCCc1ccccc1-2 10.1021/jm800670r
10105117 104168 0 None - 1 Human 7.0 pEC50 = 7 Functional
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
ChEMBL 226 6 3 2 1.6 CC/N=C(\S)NCCCCc1c[nH]cn1 10.1016/j.bmcl.2010.10.041
CHEMBL309819 104168 0 None - 1 Human 7.0 pEC50 = 7 Functional
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
ChEMBL 226 6 3 2 1.6 CC/N=C(\S)NCCCCc1c[nH]cn1 10.1016/j.bmcl.2010.10.041
127051301 140175 0 None 4 3 Human 7.0 pEC50 = 7 Functional
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
ChEMBL 246 3 3 3 0.9 CN/C(=N\C#N)NC[C@H]1CC[C@H](c2c[nH]cn2)C1 10.1021/acs.jmedchem.6b00120
CHEMBL3804906 140175 0 None 4 3 Human 7.0 pEC50 = 7 Functional
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
ChEMBL 246 3 3 3 0.9 CN/C(=N\C#N)NC[C@H]1CC[C@H](c2c[nH]cn2)C1 10.1021/acs.jmedchem.6b00120
136141537 56451 3 None 1 3 Human 7.0 pEC50 = 7 Functional
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
ChEMBL 271 2 2 3 3.0 Cc1ccc2[nH]c(/C(=N\O)C3CCN(C)CC3)cc2c1 10.1016/j.bmcl.2010.10.041
CHEMBL1632412 56451 3 None 1 3 Human 7.0 pEC50 = 7 Functional
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
ChEMBL 271 2 2 3 3.0 Cc1ccc2[nH]c(/C(=N\O)C3CCN(C)CC3)cc2c1 10.1016/j.bmcl.2010.10.041
4024 2002 20 None -3388 2 Human 6.0 pEC50 = 6 Functional
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
ChEMBL 159 2 1 2 1.4 n1ccc(cc1)Cc1c[nH]cn1 10.1016/j.bmcl.2010.10.041
9989505 2002 20 None -3388 2 Human 6.0 pEC50 = 6 Functional
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
ChEMBL 159 2 1 2 1.4 n1ccc(cc1)Cc1c[nH]cn1 10.1016/j.bmcl.2010.10.041
CHEMBL82298 2002 20 None -3388 2 Human 6.0 pEC50 = 6 Functional
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
ChEMBL 159 2 1 2 1.4 n1ccc(cc1)Cc1c[nH]cn1 10.1016/j.bmcl.2010.10.041
58227259 117116 0 None - 1 Human 6.0 pEC50 = 6 Functional
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
ChEMBL 287 4 2 5 1.9 CN[C@@H]1CCN(c2cnnc(NC3CC4CCC3C4)c2)C1 10.1016/j.bmcl.2014.12.027
CHEMBL3393556 117116 0 None - 1 Human 6.0 pEC50 = 6 Functional
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
ChEMBL 287 4 2 5 1.9 CN[C@@H]1CCN(c2cnnc(NC3CC4CCC3C4)c2)C1 10.1016/j.bmcl.2014.12.027
1194 46 3 None -50 2 Human 5.0 pEC50 = 5 Functional
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
ChEMBL 265 3 2 2 2.3 NCCc1cnc([nH]1)c1cccc(c1)Br 10.1016/j.bmcl.2010.10.041
23786499 46 3 None -50 2 Human 5.0 pEC50 = 5 Functional
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
ChEMBL 265 3 2 2 2.3 NCCc1cnc([nH]1)c1cccc(c1)Br 10.1016/j.bmcl.2010.10.041
CHEMBL26116 46 3 None -50 2 Human 5.0 pEC50 = 5 Functional
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
ChEMBL 265 3 2 2 2.3 NCCc1cnc([nH]1)c1cccc(c1)Br 10.1016/j.bmcl.2010.10.041
24797598 61532 0 None - 1 Human 7.0 pEC50 = 7 Functional
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
ChEMBL 276 3 2 6 1.2 CN1CCN(c2cc(NC3CCCC3)nc(N)n2)CC1 10.1016/j.bmcl.2011.03.017
CHEMBL1771001 61532 0 None - 1 Human 7.0 pEC50 = 7 Functional
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
ChEMBL 276 3 2 6 1.2 CN1CCN(c2cc(NC3CCCC3)nc(N)n2)CC1 10.1016/j.bmcl.2011.03.017
11846299 139195 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
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
ChEMBL 361 0 0 4 4.4 CN1CCN(C2=Nc3cc(Cl)ccc3Oc3cc(Cl)ccc32)CC1 10.1021/jm051008s
CHEMBL378788 139195 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
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
ChEMBL 361 0 0 4 4.4 CN1CCN(C2=Nc3cc(Cl)ccc3Oc3cc(Cl)ccc32)CC1 10.1021/jm051008s
46228114 200153 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
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
ChEMBL 314 4 3 7 1.1 CN1CCN(c2cc(NCc3ccc(O)cc3)nc(N)n2)CC1 10.1016/j.bmc.2009.08.059
CHEMBL596551 200153 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
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
ChEMBL 314 4 3 7 1.1 CN1CCN(c2cc(NCc3ccc(O)cc3)nc(N)n2)CC1 10.1016/j.bmc.2009.08.059
25130576 187602 1 None 2 2 Mouse 7.0 pEC50 = 7.0 Functional
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
ChEMBL 280 2 2 6 1.0 N#Cc1ccc(-c2cc(N3CCNCC3)nc(N)n2)cc1 10.1021/jm8005959
CHEMBL494890 187602 1 None 2 2 Mouse 7.0 pEC50 = 7.0 Functional
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
ChEMBL 280 2 2 6 1.0 N#Cc1ccc(-c2cc(N3CCNCC3)nc(N)n2)cc1 10.1021/jm8005959
25130232 187539 0 None - 1 Rat 7.0 pEC50 = 7.0 Functional
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
ChEMBL 273 2 1 7 0.2 CN1CCN(c2cc(-c3cn(C)cn3)nc(N)n2)CC1 10.1021/jm8005959
CHEMBL494576 187539 0 None - 1 Rat 7.0 pEC50 = 7.0 Functional
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
ChEMBL 273 2 1 7 0.2 CN1CCN(c2cc(-c3cn(C)cn3)nc(N)n2)CC1 10.1021/jm8005959
25131229 187571 0 None - 1 Rat 7.0 pEC50 = 7.0 Functional
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
ChEMBL 299 3 1 6 1.5 COc1cccc(-c2cc(N3CCN(C)CC3)nc(N)n2)c1 10.1021/jm8005959
CHEMBL494724 187571 0 None - 1 Rat 7.0 pEC50 = 7.0 Functional
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
ChEMBL 299 3 1 6 1.5 COc1cccc(-c2cc(N3CCN(C)CC3)nc(N)n2)c1 10.1021/jm8005959
25130576 187602 1 None 2 2 Mouse 7.0 pEC50 = 7.0 Functional
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
ChEMBL 280 2 2 6 1.0 N#Cc1ccc(-c2cc(N3CCNCC3)nc(N)n2)cc1 10.1021/jm800670r
CHEMBL494890 187602 1 None 2 2 Mouse 7.0 pEC50 = 7.0 Functional
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
ChEMBL 280 2 2 6 1.0 N#Cc1ccc(-c2cc(N3CCNCC3)nc(N)n2)cc1 10.1021/jm800670r
11846635 78651 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
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
ChEMBL 307 0 0 4 3.4 Cc1ccc2c(c1)Oc1ccccc1C(N1CCN(C)CC1)=N2 10.1021/jm051008s
CHEMBL211242 78651 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
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
ChEMBL 307 0 0 4 3.4 Cc1ccc2c(c1)Oc1ccccc1C(N1CCN(C)CC1)=N2 10.1021/jm051008s
46228132 202122 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
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
ChEMBL 312 4 2 6 1.7 Cc1ccc(CNc2cc(N3CCN(C)CC3)nc(N)n2)cc1 10.1016/j.bmc.2009.08.059
CHEMBL609161 202122 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
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
ChEMBL 312 4 2 6 1.7 Cc1ccc(CNc2cc(N3CCN(C)CC3)nc(N)n2)cc1 10.1016/j.bmc.2009.08.059
25129178 187605 1 None - 1 Rat 5.0 pEC50 = 5.0 Functional
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
ChEMBL 223 2 1 6 -0.2 COc1cc(N2CCN(C)CC2)nc(N)n1 10.1021/jm8005959
CHEMBL494910 187605 1 None - 1 Rat 5.0 pEC50 = 5.0 Functional
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
ChEMBL 223 2 1 6 -0.2 COc1cc(N2CCN(C)CC2)nc(N)n1 10.1021/jm8005959
1267 3775 49 None -17 5 Human 7.0 pEC50 = 7.0 Functional
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
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1021/jm900526h
3035905 3775 49 None -17 5 Human 7.0 pEC50 = 7.0 Functional
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
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1021/jm900526h
CHEMBL260374 3775 49 None -17 5 Human 7.0 pEC50 = 7.0 Functional
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
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1021/jm900526h
44480708 5743 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
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
ChEMBL 310 8 3 3 2.0 N#C/N=C(/NCCCCc1c[nH]cn1)NCCc1ccccc1 10.1021/jm900526h
CHEMBL1078632 5743 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
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
ChEMBL 310 8 3 3 2.0 N#C/N=C(/NCCCCc1c[nH]cn1)NCCc1ccccc1 10.1021/jm900526h
53233804 61496 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
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
ChEMBL 275 3 2 5 1.8 CN1CCN(c2cc(N)nc(NC3CCCC3)c2)CC1 10.1016/j.bmcl.2011.03.017
CHEMBL1770966 61496 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
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
ChEMBL 275 3 2 5 1.8 CN1CCN(c2cc(N)nc(NC3CCCC3)c2)CC1 10.1016/j.bmcl.2011.03.017
1204 1919 119 None -3 11 Human 8.0 pEC50 = 8.0 Functional
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
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.6b00120
1247 1919 119 None -3 11 Human 8.0 pEC50 = 8.0 Functional
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
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.6b00120
1375 1919 119 None -3 11 Human 8.0 pEC50 = 8.0 Functional
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
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.6b00120
774 1919 119 None -3 11 Human 8.0 pEC50 = 8.0 Functional
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
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.6b00120
CHEMBL90 1919 119 None -3 11 Human 8.0 pEC50 = 8.0 Functional
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
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.6b00120
DB05381 1919 119 None -3 11 Human 8.0 pEC50 = 8.0 Functional
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
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.6b00120
127052293 140213 3 None 10 2 Human 8.0 pEC50 = 8.0 Functional
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
ChEMBL 368 7 3 4 3.1 N#C/N=C(/NCCSc1ccccc1)NC[C@H]1CC[C@H](c2c[nH]cn2)C1 10.1021/acs.jmedchem.6b00120
CHEMBL3805361 140213 3 None 10 2 Human 8.0 pEC50 = 8.0 Functional
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
ChEMBL 368 7 3 4 3.1 N#C/N=C(/NCCSc1ccccc1)NC[C@H]1CC[C@H](c2c[nH]cn2)C1 10.1021/acs.jmedchem.6b00120
1204 1919 119 None -3 11 Human 7.9 pEC50 = 7.9 Functional
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
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmc.2009.08.059
1247 1919 119 None -3 11 Human 7.9 pEC50 = 7.9 Functional
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
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmc.2009.08.059
1375 1919 119 None -3 11 Human 7.9 pEC50 = 7.9 Functional
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
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmc.2009.08.059
774 1919 119 None -3 11 Human 7.9 pEC50 = 7.9 Functional
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
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmc.2009.08.059
CHEMBL90 1919 119 None -3 11 Human 7.9 pEC50 = 7.9 Functional
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
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmc.2009.08.059
DB05381 1919 119 None -3 11 Human 7.9 pEC50 = 7.9 Functional
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
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmc.2009.08.059
45257131 199885 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
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
ChEMBL 312 4 2 6 1.7 Cc1ccccc1CNc1cc(N2CCN(C)CC2)nc(N)n1 10.1016/j.bmc.2009.08.059
CHEMBL594731 199885 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
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
ChEMBL 312 4 2 6 1.7 Cc1ccccc1CNc1cc(N2CCN(C)CC2)nc(N)n1 10.1016/j.bmc.2009.08.059
56593499 140217 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
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
ChEMBL 368 6 3 4 3.2 N#C/N=C(/NCCSc1ccccc1)N[C@H]1CC[C@@H](c2c[nH]cn2)CC1 10.1021/acs.jmedchem.6b00120
CHEMBL3805392 140217 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
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
ChEMBL 368 6 3 4 3.2 N#C/N=C(/NCCSc1ccccc1)N[C@H]1CC[C@@H](c2c[nH]cn2)CC1 10.1021/acs.jmedchem.6b00120
127050776 140222 0 None 3 3 Human 6.0 pEC50 = 6.0 Functional
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
ChEMBL 246 3 3 3 0.9 CN/C(=N\C#N)NC[C@@H]1CC[C@@H](c2c[nH]cn2)C1 10.1021/acs.jmedchem.6b00120
CHEMBL3805437 140222 0 None 3 3 Human 6.0 pEC50 = 6.0 Functional
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
ChEMBL 246 3 3 3 0.9 CN/C(=N\C#N)NC[C@@H]1CC[C@@H](c2c[nH]cn2)C1 10.1021/acs.jmedchem.6b00120
127050431 140290 0 None 3 2 Human 7.0 pEC50 = 7.0 Functional
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
ChEMBL 246 3 3 3 0.9 CN/C(=N\C#N)NC[C@@H]1CC[C@H](c2c[nH]cn2)C1 10.1021/acs.jmedchem.6b00120
CHEMBL3806206 140290 0 None 3 2 Human 7.0 pEC50 = 7.0 Functional
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
ChEMBL 246 3 3 3 0.9 CN/C(=N\C#N)NC[C@@H]1CC[C@H](c2c[nH]cn2)C1 10.1021/acs.jmedchem.6b00120
58227165 117096 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
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
ChEMBL 235 3 1 5 1.0 CC(C)Nc1nccc(N2CCN(C)CC2)n1 10.1016/j.bmcl.2014.12.027
CHEMBL3393536 117096 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
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
ChEMBL 235 3 1 5 1.0 CC(C)Nc1nccc(N2CCN(C)CC2)n1 10.1016/j.bmcl.2014.12.027
25130578 187309 0 None - 1 Rat 6.0 pEC50 = 6.0 Functional
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
ChEMBL 251 4 1 5 1.4 CN(C)CCN(C)c1cc(C(C)(C)C)nc(N)n1 10.1021/jm8005959
CHEMBL493099 187309 0 None - 1 Rat 6.0 pEC50 = 6.0 Functional
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
ChEMBL 251 4 1 5 1.4 CN(C)CCN(C)c1cc(C(C)(C)C)nc(N)n1 10.1021/jm8005959
25129525 187559 0 None - 1 Rat 6.9 pEC50 = 6.9 Functional
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
ChEMBL 299 3 1 6 1.5 COc1ccc(-c2cc(N3CCN(C)CC3)nc(N)n2)cc1 10.1021/jm8005959
CHEMBL494648 187559 0 None - 1 Rat 6.9 pEC50 = 6.9 Functional
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
ChEMBL 299 3 1 6 1.5 COc1ccc(-c2cc(N3CCN(C)CC3)nc(N)n2)cc1 10.1021/jm8005959
25128833 188378 38 None -2 2 Rat 6.9 pEC50 = 6.9 Functional
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
ChEMBL 193 1 1 5 -0.2 CN1CCN(c2ccnc(N)n2)CC1 10.1021/jm8005959
CHEMBL501882 188378 38 None -2 2 Rat 6.9 pEC50 = 6.9 Functional
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
ChEMBL 193 1 1 5 -0.2 CN1CCN(c2ccnc(N)n2)CC1 10.1021/jm8005959
25128831 172589 0 None 1 2 Human 4.9 pEC50 = 4.9 Functional
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
ChEMBL 277 2 0 5 1.6 CN1CCN(c2cc(C(C)(C)C)nc(N(C)C)n2)CC1 10.1021/jm8005959
CHEMBL449157 172589 0 None 1 2 Human 4.9 pEC50 = 4.9 Functional
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
ChEMBL 277 2 0 5 1.6 CN1CCN(c2cc(C(C)(C)C)nc(N(C)C)n2)CC1 10.1021/jm8005959
11043445 56449 1 None -1 2 Human 4.9 pEC50 = 4.9 Functional
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
ChEMBL 258 5 1 3 2.8 c1ccc(COC[C@H]2CC[C@@H](c3c[nH]cn3)O2)cc1 10.1021/jm0300025
CHEMBL1632410 56449 1 None -1 2 Human 4.9 pEC50 = 4.9 Functional
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
ChEMBL 258 5 1 3 2.8 c1ccc(COC[C@H]2CC[C@@H](c3c[nH]cn3)O2)cc1 10.1021/jm0300025
16061839 188394 0 None - 1 Rat 6.9 pEC50 = 6.9 Functional
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
ChEMBL 284 3 2 6 1.6 CN1CCN(c2cc(Nc3ccccc3)nc(N)n2)CC1 10.1021/jm8005959
CHEMBL502104 188394 0 None - 1 Rat 6.9 pEC50 = 6.9 Functional
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
ChEMBL 284 3 2 6 1.6 CN1CCN(c2cc(Nc3ccccc3)nc(N)n2)CC1 10.1021/jm8005959
127050431 140290 0 None 3 2 Human 6.9 pEC50 = 6.9 Functional
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
ChEMBL 246 3 3 3 0.9 CN/C(=N\C#N)NC[C@@H]1CC[C@H](c2c[nH]cn2)C1 10.1021/acs.jmedchem.6b00120
CHEMBL3806206 140290 0 None 3 2 Human 6.9 pEC50 = 6.9 Functional
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
ChEMBL 246 3 3 3 0.9 CN/C(=N\C#N)NC[C@@H]1CC[C@H](c2c[nH]cn2)C1 10.1021/acs.jmedchem.6b00120
54585780 61528 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
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
ChEMBL 250 3 2 6 0.6 CC(C)Nc1cc(N2CCN(C)CC2)nc(N)n1 10.1016/j.bmcl.2011.03.017
CHEMBL1770998 61528 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
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
ChEMBL 250 3 2 6 0.6 CC(C)Nc1cc(N2CCN(C)CC2)nc(N)n1 10.1016/j.bmcl.2011.03.017
1204 1919 119 None -3 11 Human 7.9 pEC50 = 7.9 Functional
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
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm900526h
1247 1919 119 None -3 11 Human 7.9 pEC50 = 7.9 Functional
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
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm900526h
1375 1919 119 None -3 11 Human 7.9 pEC50 = 7.9 Functional
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
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm900526h
774 1919 119 None -3 11 Human 7.9 pEC50 = 7.9 Functional
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
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm900526h
CHEMBL90 1919 119 None -3 11 Human 7.9 pEC50 = 7.9 Functional
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
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm900526h
DB05381 1919 119 None -3 11 Human 7.9 pEC50 = 7.9 Functional
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
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm900526h
25130914 187230 0 None 15 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at histamine H4 receptor (unknown origin) expressed in HEK293T cells harboring CRE-luciferase after 6 hrs by luciferase reporter gene assayAgonist activity at histamine H4 receptor (unknown origin) expressed in HEK293T cells harboring CRE-luciferase after 6 hrs by luciferase reporter gene assay
ChEMBL 298 4 2 6 1.4 CN1CCN(c2cc(NCc3ccccc3)nc(N)n2)CC1 10.1021/acs.jmedchem.8b00435
CHEMBL492677 187230 0 None 15 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at histamine H4 receptor (unknown origin) expressed in HEK293T cells harboring CRE-luciferase after 6 hrs by luciferase reporter gene assayAgonist activity at histamine H4 receptor (unknown origin) expressed in HEK293T cells harboring CRE-luciferase after 6 hrs by luciferase reporter gene assay
ChEMBL 298 4 2 6 1.4 CN1CCN(c2cc(NCc3ccccc3)nc(N)n2)CC1 10.1021/acs.jmedchem.8b00435
11957573 1997 34 None -54 5 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human histamine H4 receptorAgonist activity at human histamine H4 receptor
ChEMBL 170 3 3 3 0.6 NC(=N)SCCc1cnc[nH]1 10.1021/jm100064d
1250 1997 34 None -54 5 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human histamine H4 receptorAgonist activity at human histamine H4 receptor
ChEMBL 170 3 3 3 0.6 NC(=N)SCCc1cnc[nH]1 10.1021/jm100064d
3692 1997 34 None -54 5 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human histamine H4 receptorAgonist activity at human histamine H4 receptor
ChEMBL 170 3 3 3 0.6 NC(=N)SCCc1cnc[nH]1 10.1021/jm100064d
CHEMBL19439 1997 34 None -54 5 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human histamine H4 receptorAgonist activity at human histamine H4 receptor
ChEMBL 170 3 3 3 0.6 NC(=N)SCCc1cnc[nH]1 10.1021/jm100064d
11957573 1997 34 None -54 5 Human 7.9 pEC50 = 7.9 Functional
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
ChEMBL 170 3 3 3 0.6 NC(=N)SCCc1cnc[nH]1 10.1016/j.bmcl.2010.10.041
1250 1997 34 None -54 5 Human 7.9 pEC50 = 7.9 Functional
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
ChEMBL 170 3 3 3 0.6 NC(=N)SCCc1cnc[nH]1 10.1016/j.bmcl.2010.10.041
3692 1997 34 None -54 5 Human 7.9 pEC50 = 7.9 Functional
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
ChEMBL 170 3 3 3 0.6 NC(=N)SCCc1cnc[nH]1 10.1016/j.bmcl.2010.10.041
CHEMBL19439 1997 34 None -54 5 Human 7.9 pEC50 = 7.9 Functional
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
ChEMBL 170 3 3 3 0.6 NC(=N)SCCc1cnc[nH]1 10.1016/j.bmcl.2010.10.041
1253 2045 7 None -251 2 Human 7.9 pEC50 = 7.9 Functional
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
ChEMBL 342 6 1 2 3.2 Ic1ccc(cc1)COCCCc1cnc[nH]1 10.1016/j.bmcl.2010.10.041
132937 2045 7 None -251 2 Human 7.9 pEC50 = 7.9 Functional
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
ChEMBL 342 6 1 2 3.2 Ic1ccc(cc1)COCCCc1cnc[nH]1 10.1016/j.bmcl.2010.10.041
CHEMBL19010 2045 7 None -251 2 Human 7.9 pEC50 = 7.9 Functional
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
ChEMBL 342 6 1 2 3.2 Ic1ccc(cc1)COCCCc1cnc[nH]1 10.1016/j.bmcl.2010.10.041
10176414 4032 16 None -25 2 Human 7.9 pEC50 = 7.9 Functional
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
ChEMBL 184 4 3 3 1.0 NC(=N)SCCCc1cnc[nH]1 10.1016/j.bmcl.2010.10.041
1246 4032 16 None -25 2 Human 7.9 pEC50 = 7.9 Functional
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
ChEMBL 184 4 3 3 1.0 NC(=N)SCCCc1cnc[nH]1 10.1016/j.bmcl.2010.10.041
CHEMBL281576 4032 16 None -25 2 Human 7.9 pEC50 = 7.9 Functional
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
ChEMBL 184 4 3 3 1.0 NC(=N)SCCCc1cnc[nH]1 10.1016/j.bmcl.2010.10.041
1204 1919 119 None -3 11 Human 7.9 pEC50 = 7.9 Functional
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
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmcl.2010.10.041
1247 1919 119 None -3 11 Human 7.9 pEC50 = 7.9 Functional
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
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmcl.2010.10.041
1375 1919 119 None -3 11 Human 7.9 pEC50 = 7.9 Functional
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
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmcl.2010.10.041
774 1919 119 None -3 11 Human 7.9 pEC50 = 7.9 Functional
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
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmcl.2010.10.041
CHEMBL90 1919 119 None -3 11 Human 7.9 pEC50 = 7.9 Functional
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
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmcl.2010.10.041
DB05381 1919 119 None -3 11 Human 7.9 pEC50 = 7.9 Functional
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
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmcl.2010.10.041
1267 3775 49 None -17 5 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1021/acs.jmedchem.0c00160
3035905 3775 49 None -17 5 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1021/acs.jmedchem.0c00160
CHEMBL260374 3775 49 None -17 5 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1021/acs.jmedchem.0c00160
44482032 5700 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
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
ChEMBL 262 7 3 3 1.4 CC(C)CN/C(=N\C#N)NCCCCc1c[nH]cn1 10.1021/jm900526h
CHEMBL1078346 5700 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
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
ChEMBL 262 7 3 3 1.4 CC(C)CN/C(=N\C#N)NCCCCc1c[nH]cn1 10.1021/jm900526h
25130581 187201 0 None 3 2 Human 5.9 pEC50 = 5.9 Functional
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
ChEMBL 264 2 0 5 1.5 COc1nc(N2CCN(C)CC2)cc(C(C)(C)C)n1 10.1021/jm8005959
CHEMBL492489 187201 0 None 3 2 Human 5.9 pEC50 = 5.9 Functional
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
ChEMBL 264 2 0 5 1.5 COc1nc(N2CCN(C)CC2)cc(C(C)(C)C)n1 10.1021/jm8005959
44482029 5604 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
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
ChEMBL 325 9 3 4 1.8 N#C/N=C(/NCCCCc1c[nH]cn1)NCCCc1cccnc1 10.1021/jm900526h
CHEMBL1077737 5604 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
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
ChEMBL 325 9 3 4 1.8 N#C/N=C(/NCCCCc1c[nH]cn1)NCCCc1cccnc1 10.1021/jm900526h
25131234 187638 0 None - 1 Rat 5.9 pEC50 = 5.9 Functional
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
ChEMBL 294 2 1 6 1.3 CN1CCN(c2cc(-c3ccccc3C#N)nc(N)n2)CC1 10.1021/jm8005959
CHEMBL495083 187638 0 None - 1 Rat 5.9 pEC50 = 5.9 Functional
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
ChEMBL 294 2 1 6 1.3 CN1CCN(c2cc(-c3ccccc3C#N)nc(N)n2)CC1 10.1021/jm8005959
25130235 187563 1 None 4 3 Mouse 6.9 pEC50 = 6.9 Functional
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
ChEMBL 294 2 1 6 1.3 CN1CCN(c2cc(-c3ccc(C#N)cc3)nc(N)n2)CC1 10.1021/jm8005959
CHEMBL494678 187563 1 None 4 3 Mouse 6.9 pEC50 = 6.9 Functional
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
ChEMBL 294 2 1 6 1.3 CN1CCN(c2cc(-c3ccc(C#N)cc3)nc(N)n2)CC1 10.1021/jm8005959
25130235 187563 1 None 4 3 Mouse 6.9 pEC50 = 6.9 Functional
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
ChEMBL 294 2 1 6 1.3 CN1CCN(c2cc(-c3ccc(C#N)cc3)nc(N)n2)CC1 10.1021/jm800670r
CHEMBL494678 187563 1 None 4 3 Mouse 6.9 pEC50 = 6.9 Functional
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
ChEMBL 294 2 1 6 1.3 CN1CCN(c2cc(-c3ccc(C#N)cc3)nc(N)n2)CC1 10.1021/jm800670r
25130234 187379 0 None - 1 Rat 4.9 pEC50 = 4.9 Functional
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
ChEMBL 277 2 2 6 -0.7 CN1CCN(c2cc(N3CCNC3=O)nc(N)n2)CC1 10.1021/jm8005959
CHEMBL493663 187379 0 None - 1 Rat 4.9 pEC50 = 4.9 Functional
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
ChEMBL 277 2 2 6 -0.7 CN1CCN(c2cc(N3CCNC3=O)nc(N)n2)CC1 10.1021/jm8005959
127051986 140279 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
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
ChEMBL 350 7 3 3 2.9 N#C/N=C(/NCCCc1ccccc1)NC[C@H]1CC[C@H](c2c[nH]cn2)C1 10.1021/acs.jmedchem.6b00120
CHEMBL3806098 140279 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
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
ChEMBL 350 7 3 3 2.9 N#C/N=C(/NCCCc1ccccc1)NC[C@H]1CC[C@H](c2c[nH]cn2)C1 10.1021/acs.jmedchem.6b00120
51354301 58862 0 None -1 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at histamine H4 receptor (unknown origin) expressed in HEK293T cells harboring CRE-luciferase after 6 hrs by luciferase reporter gene assayAgonist activity at histamine H4 receptor (unknown origin) expressed in HEK293T cells harboring CRE-luciferase after 6 hrs by luciferase reporter gene assay
ChEMBL 259 5 1 4 2.4 c1nc(CCn2cc(CC3CCCCC3)nn2)c[nH]1 10.1021/acs.jmedchem.8b00435
CHEMBL1688969 58862 0 None -1 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at histamine H4 receptor (unknown origin) expressed in HEK293T cells harboring CRE-luciferase after 6 hrs by luciferase reporter gene assayAgonist activity at histamine H4 receptor (unknown origin) expressed in HEK293T cells harboring CRE-luciferase after 6 hrs by luciferase reporter gene assay
ChEMBL 259 5 1 4 2.4 c1nc(CCn2cc(CC3CCCCC3)nn2)c[nH]1 10.1021/acs.jmedchem.8b00435
10934158 108550 1 None 1 2 Human 6.9 pEC50 = 6.9 Functional
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
ChEMBL 258 5 1 3 2.8 c1ccc(COC[C@@H]2CC[C@H](c3c[nH]cn3)O2)cc1 10.1016/j.bmcl.2010.10.041
CHEMBL320331 108550 1 None 1 2 Human 6.9 pEC50 = 6.9 Functional
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
ChEMBL 258 5 1 3 2.8 c1ccc(COC[C@@H]2CC[C@H](c3c[nH]cn3)O2)cc1 10.1016/j.bmcl.2010.10.041
10017821 103759 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
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
ChEMBL 302 8 3 2 2.4 S=C(NCCCCc1c[nH]cn1)NCCc1ccccc1 10.1016/j.bmcl.2010.10.041
CHEMBL308913 103759 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
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
ChEMBL 302 8 3 2 2.4 S=C(NCCCCc1c[nH]cn1)NCCc1ccccc1 10.1016/j.bmcl.2010.10.041
1238 2069 13 None -1258 2 Human 4.9 pEC50 = 4.9 Functional
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
ChEMBL 125 2 2 2 0.3 C[C@@H](Cc1cnc[nH]1)N 10.1016/j.bmcl.2010.10.041
6603865 2069 13 None -1258 2 Human 4.9 pEC50 = 4.9 Functional
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
ChEMBL 125 2 2 2 0.3 C[C@@H](Cc1cnc[nH]1)N 10.1016/j.bmcl.2010.10.041
CHEMBL11919 2069 13 None -1258 2 Human 4.9 pEC50 = 4.9 Functional
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
ChEMBL 125 2 2 2 0.3 C[C@@H](Cc1cnc[nH]1)N 10.1016/j.bmcl.2010.10.041
11043445 56449 1 None -1 2 Human 4.9 pEC50 = 4.9 Functional
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
ChEMBL 258 5 1 3 2.8 c1ccc(COC[C@H]2CC[C@@H](c3c[nH]cn3)O2)cc1 10.1016/j.bmcl.2010.10.041
CHEMBL1632410 56449 1 None -1 2 Human 4.9 pEC50 = 4.9 Functional
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
ChEMBL 258 5 1 3 2.8 c1ccc(COC[C@H]2CC[C@@H](c3c[nH]cn3)O2)cc1 10.1016/j.bmcl.2010.10.041
10945113 109602 1 None -1 2 Human 4.9 pEC50 = 4.9 Functional
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
ChEMBL 258 5 1 3 2.8 c1ccc(COC[C@@H]2CC[C@@H](c3c[nH]cn3)O2)cc1 10.1016/j.bmcl.2010.10.041
CHEMBL322256 109602 1 None -1 2 Human 4.9 pEC50 = 4.9 Functional
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
ChEMBL 258 5 1 3 2.8 c1ccc(COC[C@@H]2CC[C@@H](c3c[nH]cn3)O2)cc1 10.1016/j.bmcl.2010.10.041
44480707 5731 0 None 5 2 Human 5.9 pEC50 = 5.9 Functional
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
ChEMBL 328 8 3 4 2.2 N#C/N=C(/NCCCc1c[nH]cn1)NCCSc1ccccc1 10.1021/jm900526h
CHEMBL1078529 5731 0 None 5 2 Human 5.9 pEC50 = 5.9 Functional
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
ChEMBL 328 8 3 4 2.2 N#C/N=C(/NCCCc1c[nH]cn1)NCCSc1ccccc1 10.1021/jm900526h
10945113 109602 1 None -1 2 Human 4.9 pEC50 = 4.9 Functional
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
ChEMBL 258 5 1 3 2.8 c1ccc(COC[C@@H]2CC[C@@H](c3c[nH]cn3)O2)cc1 10.1021/jm0300025
CHEMBL322256 109602 1 None -1 2 Human 4.9 pEC50 = 4.9 Functional
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
ChEMBL 258 5 1 3 2.8 c1ccc(COC[C@@H]2CC[C@@H](c3c[nH]cn3)O2)cc1 10.1021/jm0300025
127052294 140277 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
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
ChEMBL 368 7 3 4 3.1 N#C/N=C(/NCCSc1ccccc1)NC[C@@H]1CC[C@H](c2c[nH]cn2)C1 10.1021/acs.jmedchem.6b00120
CHEMBL3806079 140277 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
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
ChEMBL 368 7 3 4 3.1 N#C/N=C(/NCCSc1ccccc1)NC[C@@H]1CC[C@H](c2c[nH]cn2)C1 10.1021/acs.jmedchem.6b00120
1204 1919 119 None -3 11 Human 7.9 pEC50 = 7.9 Functional
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
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmc.2009.08.059
1247 1919 119 None -3 11 Human 7.9 pEC50 = 7.9 Functional
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
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmc.2009.08.059
1375 1919 119 None -3 11 Human 7.9 pEC50 = 7.9 Functional
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
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmc.2009.08.059
774 1919 119 None -3 11 Human 7.9 pEC50 = 7.9 Functional
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
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmc.2009.08.059
CHEMBL90 1919 119 None -3 11 Human 7.9 pEC50 = 7.9 Functional
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
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmc.2009.08.059
DB05381 1919 119 None -3 11 Human 7.9 pEC50 = 7.9 Functional
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
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmc.2009.08.059
10934158 108550 1 None 1 2 Human 6.9 pEC50 = 6.9 Functional
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
ChEMBL 258 5 1 3 2.8 c1ccc(COC[C@@H]2CC[C@H](c3c[nH]cn3)O2)cc1 10.1021/jm0300025
CHEMBL320331 108550 1 None 1 2 Human 6.9 pEC50 = 6.9 Functional
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
ChEMBL 258 5 1 3 2.8 c1ccc(COC[C@@H]2CC[C@H](c3c[nH]cn3)O2)cc1 10.1021/jm0300025
25129182 187259 0 None - 1 Rat 5.9 pEC50 = 5.9 Functional
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
ChEMBL 291 2 1 7 -0.4 CN1CCN(c2cc(N3CCN(C)CC3)nc(N)n2)CC1 10.1021/jm8005959
CHEMBL492869 187259 0 None - 1 Rat 5.9 pEC50 = 5.9 Functional
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
ChEMBL 291 2 1 7 -0.4 CN1CCN(c2cc(N3CCN(C)CC3)nc(N)n2)CC1 10.1021/jm8005959
127052293 140213 3 None 10 2 Human 7.9 pEC50 = 7.9 Functional
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
ChEMBL 368 7 3 4 3.1 N#C/N=C(/NCCSc1ccccc1)NC[C@H]1CC[C@H](c2c[nH]cn2)C1 10.1021/acs.jmedchem.6b00120
CHEMBL3805361 140213 3 None 10 2 Human 7.9 pEC50 = 7.9 Functional
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
ChEMBL 368 7 3 4 3.1 N#C/N=C(/NCCSc1ccccc1)NC[C@H]1CC[C@H](c2c[nH]cn2)C1 10.1021/acs.jmedchem.6b00120
11846634 77980 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
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
ChEMBL 345 0 0 4 3.9 CN1CCN(C2=Nc3cc(Cl)ccc3Oc3c(F)cccc32)CC1 10.1021/jm051008s
CHEMBL209758 77980 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
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
ChEMBL 345 0 0 4 3.9 CN1CCN(C2=Nc3cc(Cl)ccc3Oc3c(F)cccc32)CC1 10.1021/jm051008s
11846464 78431 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
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
ChEMBL 361 0 0 4 4.4 CN1CCN(C2=Nc3ccc(Cl)cc3Oc3c(Cl)cccc32)CC1 10.1021/jm051008s
CHEMBL211170 78431 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
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
ChEMBL 361 0 0 4 4.4 CN1CCN(C2=Nc3ccc(Cl)cc3Oc3c(Cl)cccc32)CC1 10.1021/jm051008s
25071319 189038 14 None 1 2 Rat 7.8 pEC50 = 7.8 Functional
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
ChEMBL 295 1 2 5 1.6 Nc1nc2c(c(N3CCNCC3)n1)CCCc1ccccc1-2 10.1021/jm800670r
CHEMBL509540 189038 14 None 1 2 Rat 7.8 pEC50 = 7.8 Functional
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
ChEMBL 295 1 2 5 1.6 Nc1nc2c(c(N3CCNCC3)n1)CCCc1ccccc1-2 10.1021/jm800670r
44482030 5643 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
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
ChEMBL 338 9 3 3 2.9 CC(CCN/C(=N\C#N)NCCCCc1c[nH]cn1)c1ccccc1 10.1021/jm900526h
CHEMBL1077860 5643 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
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
ChEMBL 338 9 3 3 2.9 CC(CCN/C(=N\C#N)NCCCCc1c[nH]cn1)c1ccccc1 10.1021/jm900526h
25131561 187380 0 None -3 2 Rat 4.9 pEC50 = 4.9 Functional
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
ChEMBL 286 2 1 7 -0.0 CN1CCN(c2cc(-n3ccccc3=O)nc(N)n2)CC1 10.1021/jm8005959
CHEMBL493664 187380 0 None -3 2 Rat 4.9 pEC50 = 4.9 Functional
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
ChEMBL 286 2 1 7 -0.0 CN1CCN(c2cc(-n3ccccc3=O)nc(N)n2)CC1 10.1021/jm8005959
135897837 187604 13 None - 1 Rat 5.8 pEC50 = 5.8 Functional
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
ChEMBL 209 1 2 6 -0.5 CN1CCN(c2cc(O)nc(N)n2)CC1 10.1021/jm8005959
CHEMBL494909 187604 13 None - 1 Rat 5.8 pEC50 = 5.8 Functional
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
ChEMBL 209 1 2 6 -0.5 CN1CCN(c2cc(O)nc(N)n2)CC1 10.1021/jm8005959
127048828 140295 0 None 38 2 Human 7.8 pEC50 = 7.8 Functional
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
ChEMBL 288 5 3 3 2.0 CC(C)CN/C(=N/C#N)NC[C@H]1CC[C@H](c2c[nH]cn2)C1 10.1021/acs.jmedchem.6b00120
CHEMBL3806255 140295 0 None 38 2 Human 7.8 pEC50 = 7.8 Functional
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
ChEMBL 288 5 3 3 2.0 CC(C)CN/C(=N/C#N)NC[C@H]1CC[C@H](c2c[nH]cn2)C1 10.1021/acs.jmedchem.6b00120
58227255 117099 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
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
ChEMBL 249 5 2 5 1.3 CN[C@@H]1CCN(c2ccnc(NCC(C)C)n2)C1 10.1016/j.bmcl.2014.12.027
CHEMBL3393539 117099 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
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
ChEMBL 249 5 2 5 1.3 CN[C@@H]1CCN(c2ccnc(NCC(C)C)n2)C1 10.1016/j.bmcl.2014.12.027
44568832 187159 0 None - 1 Rat 7.8 pEC50 = 7.8 Functional
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
ChEMBL 306 2 1 6 1.2 CN1CCN(c2cc(-c3ccc(F)nc3F)nc(N)n2)CC1 10.1021/jm8005959
CHEMBL492242 187159 0 None - 1 Rat 7.8 pEC50 = 7.8 Functional
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
ChEMBL 306 2 1 6 1.2 CN1CCN(c2cc(-c3ccc(F)nc3F)nc(N)n2)CC1 10.1021/jm8005959
25128822 187457 0 None 19 2 Rat 7.8 pEC50 = 7.8 Functional
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
ChEMBL 295 1 1 5 1.6 CN1CCN(c2nc(N)nc3c2CCc2ccccc2-3)CC1 10.1021/jm800670r
CHEMBL494093 187457 0 None 19 2 Rat 7.8 pEC50 = 7.8 Functional
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
ChEMBL 295 1 1 5 1.6 CN1CCN(c2nc(N)nc3c2CCc2ccccc2-3)CC1 10.1021/jm800670r
1251 2001 39 None -204 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human histamine H4 receptorAgonist activity at human histamine H4 receptor
ChEMBL 165 2 2 2 1.0 N1CCC(CC1)Cc1[nH]cnc1 10.1021/jm100064d
3035842 2001 39 None -204 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human histamine H4 receptorAgonist activity at human histamine H4 receptor
ChEMBL 165 2 2 2 1.0 N1CCC(CC1)Cc1[nH]cnc1 10.1021/jm100064d
CHEMBL18661 2001 39 None -204 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human histamine H4 receptorAgonist activity at human histamine H4 receptor
ChEMBL 165 2 2 2 1.0 N1CCC(CC1)Cc1[nH]cnc1 10.1021/jm100064d
1251 2001 39 None -204 2 Human 7.8 pEC50 = 7.8 Functional
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
ChEMBL 165 2 2 2 1.0 N1CCC(CC1)Cc1[nH]cnc1 10.1016/j.bmcl.2010.10.041
3035842 2001 39 None -204 2 Human 7.8 pEC50 = 7.8 Functional
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
ChEMBL 165 2 2 2 1.0 N1CCC(CC1)Cc1[nH]cnc1 10.1016/j.bmcl.2010.10.041
CHEMBL18661 2001 39 None -204 2 Human 7.8 pEC50 = 7.8 Functional
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
ChEMBL 165 2 2 2 1.0 N1CCC(CC1)Cc1[nH]cnc1 10.1016/j.bmcl.2010.10.041
25149712 178962 0 None -6 3 Human 7.8 pEC50 = 7.8 Functional
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
ChEMBL 299 7 4 3 1.6 N=C(NCCCc1c[nH]cn1)NC(=O)CCc1ccccc1 10.1016/j.bmcl.2010.10.041
CHEMBL470790 178962 0 None -6 3 Human 7.8 pEC50 = 7.8 Functional
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
ChEMBL 299 7 4 3 1.6 N=C(NCCCc1c[nH]cn1)NC(=O)CCc1ccccc1 10.1016/j.bmcl.2010.10.041
25149335 184201 0 None -6 3 Human 7.8 pEC50 = 7.8 Functional
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
ChEMBL 313 7 3 2 2.0 CC(CC(=O)/N=C(\N)NCCCc1c[nH]cn1)c1ccccc1 10.1016/j.bmcl.2010.10.041
CHEMBL483406 184201 0 None -6 3 Human 7.8 pEC50 = 7.8 Functional
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
ChEMBL 313 7 3 2 2.0 CC(CC(=O)/N=C(\N)NCCCc1c[nH]cn1)c1ccccc1 10.1016/j.bmcl.2010.10.041
1278 2137 84 None 1 4 Human 7.8 pEC50 = 7.8 Functional
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
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1016/j.bmc.2009.08.059
1279 2137 84 None 1 4 Human 7.8 pEC50 = 7.8 Functional
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
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1016/j.bmc.2009.08.059
4908365 2137 84 None 1 4 Human 7.8 pEC50 = 7.8 Functional
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
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1016/j.bmc.2009.08.059
CHEMBL129198 2137 84 None 1 4 Human 7.8 pEC50 = 7.8 Functional
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
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1016/j.bmc.2009.08.059
127048890 140270 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
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
ChEMBL 165 2 2 2 1.3 NC[C@@H]1CC[C@H](c2c[nH]cn2)C1 10.1021/acs.jmedchem.6b00120
CHEMBL3805995 140270 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
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
ChEMBL 165 2 2 2 1.3 NC[C@@H]1CC[C@H](c2c[nH]cn2)C1 10.1021/acs.jmedchem.6b00120
46890548 6552 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
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
ChEMBL 410 7 1 4 4.4 Cc1cc(OCCCN2CCC(N(C)C)C2)ccc1-c1nc2c(C)c(F)ccc2[nH]1 10.1016/j.bmcl.2010.04.017
CHEMBL1083084 6552 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
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
ChEMBL 410 7 1 4 4.4 Cc1cc(OCCCN2CCC(N(C)C)C2)ccc1-c1nc2c(C)c(F)ccc2[nH]1 10.1016/j.bmcl.2010.04.017
44481761 5742 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
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
ChEMBL 324 9 3 3 2.4 N#C/N=C(/NCCCCc1c[nH]cn1)NCCCc1ccccc1 10.1021/jm900526h
CHEMBL1078631 5742 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
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
ChEMBL 324 9 3 3 2.4 N#C/N=C(/NCCCCc1c[nH]cn1)NCCCc1ccccc1 10.1021/jm900526h
51354301 58862 0 None -1 2 Human 6.8 pEC50 = 6.8 Functional
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
ChEMBL 259 5 1 4 2.4 c1nc(CCn2cc(CC3CCCCC3)nn2)c[nH]1 10.1021/jm1013488
CHEMBL1688969 58862 0 None -1 2 Human 6.8 pEC50 = 6.8 Functional
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
ChEMBL 259 5 1 4 2.4 c1nc(CCn2cc(CC3CCCCC3)nn2)c[nH]1 10.1021/jm1013488
155513612 176296 0 None -18 3 Rat 6.8 pEC50 = 6.8 Functional
Agonist activity at rat H4R expressed in in HEK293T cells by CRE-luciferase reporter gene assayAgonist activity at rat H4R expressed in in HEK293T cells by CRE-luciferase reporter gene assay
ChEMBL 277 4 1 5 2.1 CN(C)[C@@H]1CCN(c2ccnc(NCC(C)(C)C)n2)C1 10.1021/acs.jmedchem.9b01342
CHEMBL4439142 176296 0 None -18 3 Rat 6.8 pEC50 = 6.8 Functional
Agonist activity at rat H4R expressed in in HEK293T cells by CRE-luciferase reporter gene assayAgonist activity at rat H4R expressed in in HEK293T cells by CRE-luciferase reporter gene assay
ChEMBL 277 4 1 5 2.1 CN(C)[C@@H]1CCN(c2ccnc(NCC(C)(C)C)n2)C1 10.1021/acs.jmedchem.9b01342
CHEMBL4515149 176296 0 None -18 3 Rat 6.8 pEC50 = 6.8 Functional
Agonist activity at rat H4R expressed in in HEK293T cells by CRE-luciferase reporter gene assayAgonist activity at rat H4R expressed in in HEK293T cells by CRE-luciferase reporter gene assay
ChEMBL 277 4 1 5 2.1 CN(C)[C@@H]1CCN(c2ccnc(NCC(C)(C)C)n2)C1 10.1021/acs.jmedchem.9b01342
CHEMBL4595327 176296 0 None -18 3 Rat 6.8 pEC50 = 6.8 Functional
Agonist activity at rat H4R expressed in in HEK293T cells by CRE-luciferase reporter gene assayAgonist activity at rat H4R expressed in in HEK293T cells by CRE-luciferase reporter gene assay
ChEMBL 277 4 1 5 2.1 CN(C)[C@@H]1CCN(c2ccnc(NCC(C)(C)C)n2)C1 10.1021/acs.jmedchem.9b01342
1204 1919 119 None -288 11 Rat 6.8 pEC50 = 6.8 Functional
Agonist activity at rat histamine H4 receptor by luciferase reporter gene assayAgonist activity at rat histamine H4 receptor by luciferase reporter gene assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmcl.2010.10.041
1247 1919 119 None -288 11 Rat 6.8 pEC50 = 6.8 Functional
Agonist activity at rat histamine H4 receptor by luciferase reporter gene assayAgonist activity at rat histamine H4 receptor by luciferase reporter gene assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmcl.2010.10.041
1375 1919 119 None -288 11 Rat 6.8 pEC50 = 6.8 Functional
Agonist activity at rat histamine H4 receptor by luciferase reporter gene assayAgonist activity at rat histamine H4 receptor by luciferase reporter gene assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmcl.2010.10.041
774 1919 119 None -288 11 Rat 6.8 pEC50 = 6.8 Functional
Agonist activity at rat histamine H4 receptor by luciferase reporter gene assayAgonist activity at rat histamine H4 receptor by luciferase reporter gene assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmcl.2010.10.041
CHEMBL90 1919 119 None -288 11 Rat 6.8 pEC50 = 6.8 Functional
Agonist activity at rat histamine H4 receptor by luciferase reporter gene assayAgonist activity at rat histamine H4 receptor by luciferase reporter gene assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmcl.2010.10.041
DB05381 1919 119 None -288 11 Rat 6.8 pEC50 = 6.8 Functional
Agonist activity at rat histamine H4 receptor by luciferase reporter gene assayAgonist activity at rat histamine H4 receptor by luciferase reporter gene assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmcl.2010.10.041
1248 1412 28 None - 1 Human 5.8 pEC50 = 5.8 Functional
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
ChEMBL 161 4 2 3 0.6 CN(CCCSC(=N)N)C 10.1016/j.bmcl.2010.10.041
3077 1412 28 None - 1 Human 5.8 pEC50 = 5.8 Functional
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
ChEMBL 161 4 2 3 0.6 CN(CCCSC(=N)N)C 10.1016/j.bmcl.2010.10.041
90045 1412 28 None - 1 Human 5.8 pEC50 = 5.8 Functional
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
ChEMBL 161 4 2 3 0.6 CN(CCCSC(=N)N)C 10.1016/j.bmcl.2010.10.041
CHEMBL12344 1412 28 None - 1 Human 5.8 pEC50 = 5.8 Functional
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
ChEMBL 161 4 2 3 0.6 CN(CCCSC(=N)N)C 10.1016/j.bmcl.2010.10.041
5310982 93583 4 None -3 2 Human 5.8 pEC50 = 5.8 Functional
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
ChEMBL 255 3 2 2 2.6 NCCc1c[nH]c(-c2cccc(C(F)(F)F)c2)n1 10.1016/j.bmcl.2010.10.041
CHEMBL24665 93583 4 None -3 2 Human 5.8 pEC50 = 5.8 Functional
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
ChEMBL 255 3 2 2 2.6 NCCc1c[nH]c(-c2cccc(C(F)(F)F)c2)n1 10.1016/j.bmcl.2010.10.041
1269 121 41 None -35 6 Mouse 5.8 pEC50 = 5.8 Functional
Agonist activity at mouse histamine H4 receptorAgonist activity at mouse histamine H4 receptor
ChEMBL 125 2 2 2 0.2 Cc1c(CCN)nc[nH]1 10.1016/j.bmcl.2010.10.041
37463 121 41 None -35 6 Mouse 5.8 pEC50 = 5.8 Functional
Agonist activity at mouse histamine H4 receptorAgonist activity at mouse histamine H4 receptor
ChEMBL 125 2 2 2 0.2 Cc1c(CCN)nc[nH]1 10.1016/j.bmcl.2010.10.041
CHEMBL275443 121 41 None -35 6 Mouse 5.8 pEC50 = 5.8 Functional
Agonist activity at mouse histamine H4 receptorAgonist activity at mouse histamine H4 receptor
ChEMBL 125 2 2 2 0.2 Cc1c(CCN)nc[nH]1 10.1016/j.bmcl.2010.10.041
53233802 61517 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
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
ChEMBL 276 3 2 6 1.2 CN1CCN(c2cc(N)nc(NC3CCCC3)n2)CC1 10.1016/j.bmcl.2011.03.017
CHEMBL1770987 61517 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
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
ChEMBL 276 3 2 6 1.2 CN1CCN(c2cc(N)nc(NC3CCCC3)n2)CC1 10.1016/j.bmcl.2011.03.017
25131559 187561 0 None 23 2 Human 7.8 pEC50 = 7.8 Functional
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
ChEMBL 259 2 2 6 0.2 CN1CCN(c2cc(-c3c[nH]cn3)nc(N)n2)CC1 10.1021/jm8005959
CHEMBL494667 187561 0 None 23 2 Human 7.8 pEC50 = 7.8 Functional
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
ChEMBL 259 2 2 6 0.2 CN1CCN(c2cc(-c3c[nH]cn3)nc(N)n2)CC1 10.1021/jm8005959
1204 1919 119 None -3 11 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.0c00160
1204 1919 119 None -3 11 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.9b01342
1247 1919 119 None -3 11 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.0c00160
1247 1919 119 None -3 11 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.9b01342
1375 1919 119 None -3 11 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.0c00160
1375 1919 119 None -3 11 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.9b01342
774 1919 119 None -3 11 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.0c00160
774 1919 119 None -3 11 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.9b01342
CHEMBL90 1919 119 None -3 11 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.0c00160
CHEMBL90 1919 119 None -3 11 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.9b01342
DB05381 1919 119 None -3 11 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.0c00160
DB05381 1919 119 None -3 11 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.9b01342
44480959 5644 2 None 1 2 Human 6.8 pEC50 = 6.8 Functional
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
ChEMBL 206 5 3 3 0.1 N#C/N=C(\N)NCCCCc1c[nH]cn1 10.1021/jm900526h
CHEMBL1077861 5644 2 None 1 2 Human 6.8 pEC50 = 6.8 Functional
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
ChEMBL 206 5 3 3 0.1 N#C/N=C(\N)NCCCCc1c[nH]cn1 10.1021/jm900526h
1484519 173872 60 None - 1 Rat 4.8 pEC50 = 4.8 Functional
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
ChEMBL 227 1 1 5 0.5 CN1CCN(c2cc(Cl)nc(N)n2)CC1 10.1021/jm8005959
CHEMBL454007 173872 60 None - 1 Rat 4.8 pEC50 = 4.8 Functional
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
ChEMBL 227 1 1 5 0.5 CN1CCN(c2cc(Cl)nc(N)n2)CC1 10.1021/jm8005959
21638785 188634 5 None 1 2 Mouse 7.8 pEC50 = 7.8 Functional
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
ChEMBL 263 1 2 2 1.9 O=C(c1cc2cc(Cl)ccc2[nH]1)N1CCNCC1 10.1021/jm800670r
CHEMBL503605 188634 5 None 1 2 Mouse 7.8 pEC50 = 7.8 Functional
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
ChEMBL 263 1 2 2 1.9 O=C(c1cc2cc(Cl)ccc2[nH]1)N1CCNCC1 10.1021/jm800670r
127051958 140253 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
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
ChEMBL 165 2 2 2 1.3 NC[C@H]1CC[C@H](c2c[nH]cn2)C1 10.1021/acs.jmedchem.6b00120
CHEMBL3805813 140253 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
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
ChEMBL 165 2 2 2 1.3 NC[C@H]1CC[C@H](c2c[nH]cn2)C1 10.1021/acs.jmedchem.6b00120
25129880 193106 0 None - 1 Rat 6.8 pEC50 = 6.8 Functional
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
ChEMBL 319 2 1 5 2.6 CN1CCN(c2cc(-c3ccc4ccccc4c3)nc(N)n2)CC1 10.1021/jm8005959
CHEMBL522841 193106 0 None - 1 Rat 6.8 pEC50 = 6.8 Functional
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
ChEMBL 319 2 1 5 2.6 CN1CCN(c2cc(-c3ccc4ccccc4c3)nc(N)n2)CC1 10.1021/jm8005959
25130231 187680 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
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
ChEMBL 309 2 1 7 1.2 CN1CCN(c2cc(-n3cnc4ccccc43)nc(N)n2)CC1 10.1021/jm8005959
CHEMBL495280 187680 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
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
ChEMBL 309 2 1 7 1.2 CN1CCN(c2cc(-n3cnc4ccccc43)nc(N)n2)CC1 10.1021/jm8005959
25131228 187570 0 None - 1 Rat 6.8 pEC50 = 6.8 Functional
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
ChEMBL 283 2 1 5 1.8 Cc1ccccc1-c1cc(N2CCN(C)CC2)nc(N)n1 10.1021/jm8005959
CHEMBL494723 187570 0 None - 1 Rat 6.8 pEC50 = 6.8 Functional
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
ChEMBL 283 2 1 5 1.8 Cc1ccccc1-c1cc(N2CCN(C)CC2)nc(N)n1 10.1021/jm8005959
25128828 188228 2 None - 1 Rat 5.8 pEC50 = 5.8 Functional
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
ChEMBL 237 4 2 5 1.3 CN(C)CCNc1cc(C(C)(C)C)nc(N)n1 10.1021/jm8005959
CHEMBL499631 188228 2 None - 1 Rat 5.8 pEC50 = 5.8 Functional
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
ChEMBL 237 4 2 5 1.3 CN(C)CCNc1cc(C(C)(C)C)nc(N)n1 10.1021/jm8005959
58227163 176439 0 None 4 3 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 263 3 2 5 1.7 CC(C)(C)CNc1nccc(N2CCCNCC2)n1 10.1021/acs.jmedchem.9b01342
CHEMBL4518374 176439 0 None 4 3 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 263 3 2 5 1.7 CC(C)(C)CNc1nccc(N2CCCNCC2)n1 10.1021/acs.jmedchem.9b01342
CHEMBL4596491 176439 0 None 4 3 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 263 3 2 5 1.7 CC(C)(C)CNc1nccc(N2CCCNCC2)n1 10.1021/acs.jmedchem.9b01342
25071319 189038 14 None -1 2 Mouse 7.7 pEC50 = 7.7 Functional
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
ChEMBL 295 1 2 5 1.6 Nc1nc2c(c(N3CCNCC3)n1)CCCc1ccccc1-2 10.1021/jm800670r
CHEMBL509540 189038 14 None -1 2 Mouse 7.7 pEC50 = 7.7 Functional
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
ChEMBL 295 1 2 5 1.6 Nc1nc2c(c(N3CCNCC3)n1)CCCc1ccccc1-2 10.1021/jm800670r
1204 1919 119 None -3 11 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human H4 receptor expressed in 293-EBNA cells by luciferase reporter gene assayAgonist activity at human H4 receptor expressed in 293-EBNA cells by luciferase reporter gene assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm0603318
1247 1919 119 None -3 11 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human H4 receptor expressed in 293-EBNA cells by luciferase reporter gene assayAgonist activity at human H4 receptor expressed in 293-EBNA cells by luciferase reporter gene assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm0603318
1375 1919 119 None -3 11 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human H4 receptor expressed in 293-EBNA cells by luciferase reporter gene assayAgonist activity at human H4 receptor expressed in 293-EBNA cells by luciferase reporter gene assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm0603318
774 1919 119 None -3 11 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human H4 receptor expressed in 293-EBNA cells by luciferase reporter gene assayAgonist activity at human H4 receptor expressed in 293-EBNA cells by luciferase reporter gene assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm0603318
CHEMBL90 1919 119 None -3 11 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human H4 receptor expressed in 293-EBNA cells by luciferase reporter gene assayAgonist activity at human H4 receptor expressed in 293-EBNA cells by luciferase reporter gene assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm0603318
DB05381 1919 119 None -3 11 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human H4 receptor expressed in 293-EBNA cells by luciferase reporter gene assayAgonist activity at human H4 receptor expressed in 293-EBNA cells by luciferase reporter gene assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm0603318
25130233 170589 7 None - 1 Rat 5.7 pEC50 = 5.7 Functional
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
ChEMBL 259 2 2 6 0.2 CN1CCN(c2cc(-c3cn[nH]c3)nc(N)n2)CC1 10.1021/jm8005959
CHEMBL445091 170589 7 None - 1 Rat 5.7 pEC50 = 5.7 Functional
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
ChEMBL 259 2 2 6 0.2 CN1CCN(c2cc(-c3cn[nH]c3)nc(N)n2)CC1 10.1021/jm8005959
25128831 172589 0 None -1 2 Rat 4.7 pEC50 = 4.7 Functional
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
ChEMBL 277 2 0 5 1.6 CN1CCN(c2cc(C(C)(C)C)nc(N(C)C)n2)CC1 10.1021/jm8005959
CHEMBL449157 172589 0 None -1 2 Rat 4.7 pEC50 = 4.7 Functional
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
ChEMBL 277 2 0 5 1.6 CN1CCN(c2cc(C(C)(C)C)nc(N(C)C)n2)CC1 10.1021/jm8005959
25130574 187352 0 None - 1 Rat 5.7 pEC50 = 5.7 Functional
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
ChEMBL 293 2 1 5 2.0 CN1CCN(c2cc(N)nc(-c3ccc(C#N)cc3)c2)CC1 10.1021/jm8005959
CHEMBL493461 187352 0 None - 1 Rat 5.7 pEC50 = 5.7 Functional
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
ChEMBL 293 2 1 5 2.0 CN1CCN(c2cc(N)nc(-c3ccc(C#N)cc3)c2)CC1 10.1021/jm8005959
44568790 171390 0 None - 1 Rat 7.7 pEC50 = 7.7 Functional
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
ChEMBL 281 2 2 5 1.4 CN[C@@H]1CCN(c2nc(N)nc3c2Cc2ccccc2-3)C1 10.1021/jm800670r
CHEMBL446269 171390 0 None - 1 Rat 7.7 pEC50 = 7.7 Functional
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
ChEMBL 281 2 2 5 1.4 CN[C@@H]1CCN(c2nc(N)nc3c2Cc2ccccc2-3)C1 10.1021/jm800670r
155552061 176454 0 None -2 3 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 277 3 1 5 2.1 CN1CCCN(c2ccnc(NCC(C)(C)C)n2)CC1 10.1021/acs.jmedchem.9b01342
CHEMBL4543119 176454 0 None -2 3 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 277 3 1 5 2.1 CN1CCCN(c2ccnc(NCC(C)(C)C)n2)CC1 10.1021/acs.jmedchem.9b01342
CHEMBL4596606 176454 0 None -2 3 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 277 3 1 5 2.1 CN1CCCN(c2ccnc(NCC(C)(C)C)n2)CC1 10.1021/acs.jmedchem.9b01342
45257133 199881 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
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
ChEMBL 332 4 2 6 2.1 CN1CCN(c2cc(NCc3ccccc3Cl)nc(N)n2)CC1 10.1016/j.bmc.2009.08.059
CHEMBL594721 199881 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
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
ChEMBL 332 4 2 6 2.1 CN1CCN(c2cc(NCc3ccccc3Cl)nc(N)n2)CC1 10.1016/j.bmc.2009.08.059
11846300 80237 3 None -2 2 Human 7.7 pEC50 = 7.7 Functional
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
ChEMBL 327 0 0 4 3.8 CN1CCN(C2=Nc3ccc(Cl)cc3Oc3ccccc32)CC1 10.1021/jm051008s
CHEMBL213912 80237 3 None -2 2 Human 7.7 pEC50 = 7.7 Functional
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
ChEMBL 327 0 0 4 3.8 CN1CCN(C2=Nc3ccc(Cl)cc3Oc3ccccc32)CC1 10.1021/jm051008s
1204 1919 119 None -3 11 Human 7.7 pEC50 = 7.7 Functional
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
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmcl.2010.10.041
1247 1919 119 None -3 11 Human 7.7 pEC50 = 7.7 Functional
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
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmcl.2010.10.041
1375 1919 119 None -3 11 Human 7.7 pEC50 = 7.7 Functional
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
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmcl.2010.10.041
774 1919 119 None -3 11 Human 7.7 pEC50 = 7.7 Functional
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
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmcl.2010.10.041
CHEMBL90 1919 119 None -3 11 Human 7.7 pEC50 = 7.7 Functional
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
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmcl.2010.10.041
DB05381 1919 119 None -3 11 Human 7.7 pEC50 = 7.7 Functional
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
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmcl.2010.10.041
3032915 15463 24 None - 1 Human 7.7 pEC50 = 7.7 Functional
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
ChEMBL 212 5 3 2 1.2 C/N=C(\S)NCCCCc1c[nH]cn1 10.1016/j.bmcl.2010.10.041
CHEMBL12160 15463 24 None - 1 Human 7.7 pEC50 = 7.7 Functional
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
ChEMBL 212 5 3 2 1.2 C/N=C(\S)NCCCCc1c[nH]cn1 10.1016/j.bmcl.2010.10.041
53321919 56448 0 None -50 2 Human 7.7 pEC50 = 7.7 Functional
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
ChEMBL 322 7 3 3 3.8 N=C(NCc1ccc(Cl)cc1)SCCCCc1c[nH]cn1 10.1016/j.bmcl.2010.10.041
CHEMBL1632409 56448 0 None -50 2 Human 7.7 pEC50 = 7.7 Functional
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
ChEMBL 322 7 3 3 3.8 N=C(NCc1ccc(Cl)cc1)SCCCCc1c[nH]cn1 10.1016/j.bmcl.2010.10.041
10060213 102884 1 None - 1 Human 7.7 pEC50 = 7.7 Functional
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
ChEMBL 240 6 3 2 2.0 CC(C)/N=C(\S)NCCCCc1c[nH]cn1 10.1016/j.bmcl.2010.10.041
CHEMBL306077 102884 1 None - 1 Human 7.7 pEC50 = 7.7 Functional
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
ChEMBL 240 6 3 2 2.0 CC(C)/N=C(\S)NCCCCc1c[nH]cn1 10.1016/j.bmcl.2010.10.041
25128823 192693 0 None - 1 Rat 7.7 pEC50 = 7.7 Functional
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
ChEMBL 267 1 2 5 1.0 Nc1nc2c(c(N3CCNCC3)n1)Cc1ccccc1-2 10.1021/jm800670r
CHEMBL521995 192693 0 None - 1 Rat 7.7 pEC50 = 7.7 Functional
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
ChEMBL 267 1 2 5 1.0 Nc1nc2c(c(N3CCNCC3)n1)Cc1ccccc1-2 10.1021/jm800670r
25131230 193085 0 None - 1 Rat 6.7 pEC50 = 6.7 Functional
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
ChEMBL 329 4 1 7 1.5 COc1cccc(OC)c1-c1cc(N2CCN(C)CC2)nc(N)n1 10.1021/jm8005959
CHEMBL522679 193085 0 None - 1 Rat 6.7 pEC50 = 6.7 Functional
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
ChEMBL 329 4 1 7 1.5 COc1cccc(OC)c1-c1cc(N2CCN(C)CC2)nc(N)n1 10.1021/jm8005959
10037650 5177 0 None 47 2 Human 6.7 pEC50 = 6.7 Functional
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
ChEMBL 248 3 3 4 0.3 C/N=C(\NC#N)NC[C@@H]1CC[C@H](c2c[nH]cn2)O1 10.1016/j.bmcl.2010.10.041
CHEMBL106158 5177 0 None 47 2 Human 6.7 pEC50 = 6.7 Functional
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
ChEMBL 248 3 3 4 0.3 C/N=C(\NC#N)NC[C@@H]1CC[C@H](c2c[nH]cn2)O1 10.1016/j.bmcl.2010.10.041
170389 206958 35 None -4 2 Human 6.7 pEC50 = 6.7 Functional
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
ChEMBL 125 3 2 2 0.3 NCCCc1c[nH]cn1 10.1016/j.bmcl.2010.10.041
CHEMBL4634086 206958 35 None -4 2 Human 6.7 pEC50 = 6.7 Functional
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
ChEMBL 125 3 2 2 0.3 NCCCc1c[nH]cn1 10.1016/j.bmcl.2010.10.041
CHEMBL91353 206958 35 None -4 2 Human 6.7 pEC50 = 6.7 Functional
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
ChEMBL 125 3 2 2 0.3 NCCCc1c[nH]cn1 10.1016/j.bmcl.2010.10.041
155513612 176296 0 None -14 3 Mouse 6.7 pEC50 = 6.7 Functional
Agonist activity at mouse H4R expressed in HEK293T cells by CRE-luciferase reporter gene assayAgonist activity at mouse H4R expressed in HEK293T cells by CRE-luciferase reporter gene assay
ChEMBL 277 4 1 5 2.1 CN(C)[C@@H]1CCN(c2ccnc(NCC(C)(C)C)n2)C1 10.1021/acs.jmedchem.9b01342
CHEMBL4439142 176296 0 None -14 3 Mouse 6.7 pEC50 = 6.7 Functional
Agonist activity at mouse H4R expressed in HEK293T cells by CRE-luciferase reporter gene assayAgonist activity at mouse H4R expressed in HEK293T cells by CRE-luciferase reporter gene assay
ChEMBL 277 4 1 5 2.1 CN(C)[C@@H]1CCN(c2ccnc(NCC(C)(C)C)n2)C1 10.1021/acs.jmedchem.9b01342
CHEMBL4515149 176296 0 None -14 3 Mouse 6.7 pEC50 = 6.7 Functional
Agonist activity at mouse H4R expressed in HEK293T cells by CRE-luciferase reporter gene assayAgonist activity at mouse H4R expressed in HEK293T cells by CRE-luciferase reporter gene assay
ChEMBL 277 4 1 5 2.1 CN(C)[C@@H]1CCN(c2ccnc(NCC(C)(C)C)n2)C1 10.1021/acs.jmedchem.9b01342
CHEMBL4595327 176296 0 None -14 3 Mouse 6.7 pEC50 = 6.7 Functional
Agonist activity at mouse H4R expressed in HEK293T cells by CRE-luciferase reporter gene assayAgonist activity at mouse H4R expressed in HEK293T cells by CRE-luciferase reporter gene assay
ChEMBL 277 4 1 5 2.1 CN(C)[C@@H]1CCN(c2ccnc(NCC(C)(C)C)n2)C1 10.1021/acs.jmedchem.9b01342
136141537 56451 3 None -1 3 Mouse 6.7 pEC50 = 6.7 Functional
Agonist activity at mouse histamine H4 receptor by luciferase reporter gene assayAgonist activity at mouse histamine H4 receptor by luciferase reporter gene assay
ChEMBL 271 2 2 3 3.0 Cc1ccc2[nH]c(/C(=N\O)C3CCN(C)CC3)cc2c1 10.1016/j.bmcl.2010.10.041
CHEMBL1632412 56451 3 None -1 3 Mouse 6.7 pEC50 = 6.7 Functional
Agonist activity at mouse histamine H4 receptor by luciferase reporter gene assayAgonist activity at mouse histamine H4 receptor by luciferase reporter gene assay
ChEMBL 271 2 2 3 3.0 Cc1ccc2[nH]c(/C(=N\O)C3CCN(C)CC3)cc2c1 10.1016/j.bmcl.2010.10.041
136192874 56453 0 None -3 3 Rat 6.7 pEC50 = 6.7 Functional
Agonist activity at rat histamine H4 receptor by luciferase reporter gene assayAgonist activity at rat histamine H4 receptor by luciferase reporter gene assay
ChEMBL 292 2 2 4 2.7 CN1CCC(/C(=N/O)c2nc3cc(Cl)ccc3[nH]2)CC1 10.1016/j.bmcl.2010.10.041
CHEMBL1632414 56453 0 None -3 3 Rat 6.7 pEC50 = 6.7 Functional
Agonist activity at rat histamine H4 receptor by luciferase reporter gene assayAgonist activity at rat histamine H4 receptor by luciferase reporter gene assay
ChEMBL 292 2 2 4 2.7 CN1CCC(/C(=N/O)c2nc3cc(Cl)ccc3[nH]2)CC1 10.1016/j.bmcl.2010.10.041
46228133 200031 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
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
ChEMBL 332 4 2 6 2.1 CN1CCN(c2cc(NCc3cccc(Cl)c3)nc(N)n2)CC1 10.1016/j.bmc.2009.08.059
CHEMBL595639 200031 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
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
ChEMBL 332 4 2 6 2.1 CN1CCN(c2cc(NCc3cccc(Cl)c3)nc(N)n2)CC1 10.1016/j.bmc.2009.08.059
10197870 5269 0 None -47 2 Human 5.7 pEC50 = 5.7 Functional
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
ChEMBL 167 2 2 3 0.6 NC[C@H]1CC[C@H](c2c[nH]cn2)O1 10.1016/j.bmcl.2010.10.041
CHEMBL106612 5269 0 None -47 2 Human 5.7 pEC50 = 5.7 Functional
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
ChEMBL 167 2 2 3 0.6 NC[C@H]1CC[C@H](c2c[nH]cn2)O1 10.1016/j.bmcl.2010.10.041
10197870 5269 0 None -47 2 Human 5.7 pEC50 = 5.7 Functional
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
ChEMBL 167 2 2 3 0.6 NC[C@H]1CC[C@H](c2c[nH]cn2)O1 10.1021/jm0300025
CHEMBL106612 5269 0 None -47 2 Human 5.7 pEC50 = 5.7 Functional
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
ChEMBL 167 2 2 3 0.6 NC[C@H]1CC[C@H](c2c[nH]cn2)O1 10.1021/jm0300025
10879463 5258 0 None - 1 Human 4.7 pEC50 = 4.7 Functional
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
ChEMBL 248 3 3 4 0.3 C/N=C(\NC#N)NC[C@@H]1CC[C@@H](c2c[nH]cn2)O1 10.1016/j.bmcl.2010.10.041
CHEMBL106570 5258 0 None - 1 Human 4.7 pEC50 = 4.7 Functional
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
ChEMBL 248 3 3 4 0.3 C/N=C(\NC#N)NC[C@@H]1CC[C@@H](c2c[nH]cn2)O1 10.1016/j.bmcl.2010.10.041
1278 2137 84 None -1 4 Mouse 8.6 pEC50 = 8.6 Functional
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
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/jm800670r
1279 2137 84 None -1 4 Mouse 8.6 pEC50 = 8.6 Functional
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
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/jm800670r
4908365 2137 84 None -1 4 Mouse 8.6 pEC50 = 8.6 Functional
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
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/jm800670r
CHEMBL129198 2137 84 None -1 4 Mouse 8.6 pEC50 = 8.6 Functional
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
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/jm800670r
1278 2137 84 None -1 4 Rat 8.6 pEC50 = 8.6 Functional
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
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/jm800670r
1279 2137 84 None -1 4 Rat 8.6 pEC50 = 8.6 Functional
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
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/jm800670r
4908365 2137 84 None -1 4 Rat 8.6 pEC50 = 8.6 Functional
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
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/jm800670r
CHEMBL129198 2137 84 None -1 4 Rat 8.6 pEC50 = 8.6 Functional
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
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/jm800670r
58227260 117106 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
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
ChEMBL 287 3 1 5 1.8 CN1CCN(c2ccnc(NC3CC4CCC3C4)n2)CC1 10.1016/j.bmcl.2014.12.027
CHEMBL3393546 117106 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
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
ChEMBL 287 3 1 5 1.8 CN1CCN(c2ccnc(NC3CC4CCC3C4)n2)CC1 10.1016/j.bmcl.2014.12.027
11846636 77923 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
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
ChEMBL 345 0 0 4 3.9 CN1CCN(C2=Nc3ccc(Cl)cc3Oc3c(F)cccc32)CC1 10.1021/jm051008s
CHEMBL209628 77923 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
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
ChEMBL 345 0 0 4 3.9 CN1CCN(C2=Nc3ccc(Cl)cc3Oc3c(F)cccc32)CC1 10.1021/jm051008s
1204 1919 119 None -3 11 Human 7.7 pEC50 = 7.7 Functional
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
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1039/C3MD00245D
1247 1919 119 None -3 11 Human 7.7 pEC50 = 7.7 Functional
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
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1039/C3MD00245D
1375 1919 119 None -3 11 Human 7.7 pEC50 = 7.7 Functional
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
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1039/C3MD00245D
774 1919 119 None -3 11 Human 7.7 pEC50 = 7.7 Functional
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
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1039/C3MD00245D
CHEMBL90 1919 119 None -3 11 Human 7.7 pEC50 = 7.7 Functional
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
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1039/C3MD00245D
DB05381 1919 119 None -3 11 Human 7.7 pEC50 = 7.7 Functional
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
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1039/C3MD00245D
16061961 199656 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
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
ChEMBL 316 4 2 6 1.6 CN1CCN(c2cc(NCc3ccc(F)cc3)nc(N)n2)CC1 10.1016/j.bmc.2009.08.059
CHEMBL593103 199656 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
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
ChEMBL 316 4 2 6 1.6 CN1CCN(c2cc(NCc3ccc(F)cc3)nc(N)n2)CC1 10.1016/j.bmc.2009.08.059
1204 1919 119 None -3 11 Human 7.7 pEC50 = 7.7 Functional
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
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm0300025
1247 1919 119 None -3 11 Human 7.7 pEC50 = 7.7 Functional
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
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm0300025
1375 1919 119 None -3 11 Human 7.7 pEC50 = 7.7 Functional
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
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm0300025
774 1919 119 None -3 11 Human 7.7 pEC50 = 7.7 Functional
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
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm0300025
CHEMBL90 1919 119 None -3 11 Human 7.7 pEC50 = 7.7 Functional
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
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm0300025
DB05381 1919 119 None -3 11 Human 7.7 pEC50 = 7.7 Functional
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
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm0300025
127052635 140182 0 None 4 2 Human 6.7 pEC50 = 6.7 Functional
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
ChEMBL 288 5 3 3 2.0 CC(C)CN/C(=N/C#N)NC[C@@H]1CC[C@H](c2c[nH]cn2)C1 10.1021/acs.jmedchem.6b00120
CHEMBL3805003 140182 0 None 4 2 Human 6.7 pEC50 = 6.7 Functional
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
ChEMBL 288 5 3 3 2.0 CC(C)CN/C(=N/C#N)NC[C@@H]1CC[C@H](c2c[nH]cn2)C1 10.1021/acs.jmedchem.6b00120
25130237 187258 2 None - 1 Rat 5.7 pEC50 = 5.7 Functional
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
ChEMBL 319 1 1 5 0.4 CN1CCN(c2cc(I)nc(N)n2)CC1 10.1021/jm8005959
CHEMBL492864 187258 2 None - 1 Rat 5.7 pEC50 = 5.7 Functional
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
ChEMBL 319 1 1 5 0.4 CN1CCN(c2cc(I)nc(N)n2)CC1 10.1021/jm8005959
127051301 140175 0 None 4 3 Human 6.7 pEC50 = 6.7 Functional
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
ChEMBL 246 3 3 3 0.9 CN/C(=N\C#N)NC[C@H]1CC[C@H](c2c[nH]cn2)C1 10.1021/acs.jmedchem.6b00120
CHEMBL3804906 140175 0 None 4 3 Human 6.7 pEC50 = 6.7 Functional
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
ChEMBL 246 3 3 3 0.9 CN/C(=N\C#N)NC[C@H]1CC[C@H](c2c[nH]cn2)C1 10.1021/acs.jmedchem.6b00120
25131555 187155 0 None - 1 Rat 6.7 pEC50 = 6.7 Functional
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
ChEMBL 270 2 1 6 0.9 CN1CCN(c2cc(-c3cccnc3)nc(N)n2)CC1 10.1021/jm8005959
CHEMBL492227 187155 0 None - 1 Rat 6.7 pEC50 = 6.7 Functional
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
ChEMBL 270 2 1 6 0.9 CN1CCN(c2cc(-c3cccnc3)nc(N)n2)CC1 10.1021/jm8005959
25130914 187230 0 None 15 2 Human 7.7 pEC50 = 7.7 Functional
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
ChEMBL 298 4 2 6 1.4 CN1CCN(c2cc(NCc3ccccc3)nc(N)n2)CC1 10.1016/j.bmc.2009.08.059
CHEMBL492677 187230 0 None 15 2 Human 7.7 pEC50 = 7.7 Functional
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
ChEMBL 298 4 2 6 1.4 CN1CCN(c2cc(NCc3ccccc3)nc(N)n2)CC1 10.1016/j.bmc.2009.08.059
10879463 5258 0 None - 1 Human 4.7 pEC50 = 4.7 Functional
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
ChEMBL 248 3 3 4 0.3 C/N=C(\NC#N)NC[C@@H]1CC[C@@H](c2c[nH]cn2)O1 10.1021/jm0300025
CHEMBL106570 5258 0 None - 1 Human 4.7 pEC50 = 4.7 Functional
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
ChEMBL 248 3 3 4 0.3 C/N=C(\NC#N)NC[C@@H]1CC[C@@H](c2c[nH]cn2)O1 10.1021/jm0300025
1613 2333 53 None -26 34 Human 6.7 pEC50 = 6.7 Functional
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
ChEMBL 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 10.1021/jm051008s
205 2333 53 None -26 34 Human 6.7 pEC50 = 6.7 Functional
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
ChEMBL 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 10.1021/jm051008s
3964 2333 53 None -26 34 Human 6.7 pEC50 = 6.7 Functional
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
ChEMBL 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 10.1021/jm051008s
CHEMBL831 2333 53 None -26 34 Human 6.7 pEC50 = 6.7 Functional
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
ChEMBL 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 10.1021/jm051008s
DB00408 2333 53 None -26 34 Human 6.7 pEC50 = 6.7 Functional
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
ChEMBL 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 10.1021/jm051008s
753256 179326 12 None - 1 Rat 6.7 pEC50 = 6.7 Functional
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
ChEMBL 208 1 2 6 -0.6 CN1CCN(c2cc(N)nc(N)n2)CC1 10.1021/jm8005959
CHEMBL473662 179326 12 None - 1 Rat 6.7 pEC50 = 6.7 Functional
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
ChEMBL 208 1 2 6 -0.6 CN1CCN(c2cc(N)nc(N)n2)CC1 10.1021/jm8005959
25131560 187322 0 None - 1 Rat 6.7 pEC50 = 6.7 Functional
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
ChEMBL 273 2 1 7 0.2 CN1CCN(c2cc(-c3cnn(C)c3)nc(N)n2)CC1 10.1021/jm8005959
CHEMBL493229 187322 0 None - 1 Rat 6.7 pEC50 = 6.7 Functional
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
ChEMBL 273 2 1 7 0.2 CN1CCN(c2cc(-c3cnn(C)c3)nc(N)n2)CC1 10.1021/jm8005959
1223 950 41 None -21 4 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human H4R by [35S]-GTPgammaS-binding assayAgonist activity at human H4R by [35S]-GTPgammaS-binding assay
ChEMBL 308 6 2 3 3.2 Clc1ccc(cc1)CN=C(SCCCc1cnc[nH]1)N 10.1021/acs.jmedchem.9b01342
2790 950 41 None -21 4 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human H4R by [35S]-GTPgammaS-binding assayAgonist activity at human H4R by [35S]-GTPgammaS-binding assay
ChEMBL 308 6 2 3 3.2 Clc1ccc(cc1)CN=C(SCCCc1cnc[nH]1)N 10.1021/acs.jmedchem.9b01342
CHEMBL14690 950 41 None -21 4 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human H4R by [35S]-GTPgammaS-binding assayAgonist activity at human H4R by [35S]-GTPgammaS-binding assay
ChEMBL 308 6 2 3 3.2 Clc1ccc(cc1)CN=C(SCCCc1cnc[nH]1)N 10.1021/acs.jmedchem.9b01342
155512725 176217 0 None -1 3 Rat 7.6 pEC50 = 7.6 Functional
Agonist activity at rat H4R expressed in HEK293-SF-rH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at rat H4R expressed in HEK293-SF-rH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 237 6 3 5 1.7 CC(C)(C)CNc1nccc(NCCCN)n1 10.1021/acs.jmedchem.9b01342
CHEMBL4437371 176217 0 None -1 3 Rat 7.6 pEC50 = 7.6 Functional
Agonist activity at rat H4R expressed in HEK293-SF-rH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at rat H4R expressed in HEK293-SF-rH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 237 6 3 5 1.7 CC(C)(C)CNc1nccc(NCCCN)n1 10.1021/acs.jmedchem.9b01342
CHEMBL4594753 176217 0 None -1 3 Rat 7.6 pEC50 = 7.6 Functional
Agonist activity at rat H4R expressed in HEK293-SF-rH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at rat H4R expressed in HEK293-SF-rH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 237 6 3 5 1.7 CC(C)(C)CNc1nccc(NCCCN)n1 10.1021/acs.jmedchem.9b01342
10037650 5177 0 None 47 2 Human 6.7 pEC50 = 6.7 Functional
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
ChEMBL 248 3 3 4 0.3 C/N=C(\NC#N)NC[C@@H]1CC[C@H](c2c[nH]cn2)O1 10.1021/jm0300025
CHEMBL106158 5177 0 None 47 2 Human 6.7 pEC50 = 6.7 Functional
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
ChEMBL 248 3 3 4 0.3 C/N=C(\NC#N)NC[C@@H]1CC[C@H](c2c[nH]cn2)O1 10.1021/jm0300025
25129881 187158 5 None - 1 Rat 6.6 pEC50 = 6.6 Functional
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
ChEMBL 270 2 1 6 0.9 CN1CCN(c2cc(-c3ccncc3)nc(N)n2)CC1 10.1021/jm8005959
CHEMBL492241 187158 5 None - 1 Rat 6.6 pEC50 = 6.6 Functional
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
ChEMBL 270 2 1 6 0.9 CN1CCN(c2cc(-c3ccncc3)nc(N)n2)CC1 10.1021/jm8005959
44568855 193170 0 None - 1 Rat 5.6 pEC50 = 5.6 Functional
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
ChEMBL 285 2 1 5 2.0 CC(C)(C)c1cc(N2CCNCC2)nc(-n2cccc2)n1 10.1021/jm8005959
CHEMBL523335 193170 0 None - 1 Rat 5.6 pEC50 = 5.6 Functional
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
ChEMBL 285 2 1 5 2.0 CC(C)(C)c1cc(N2CCNCC2)nc(-n2cccc2)n1 10.1021/jm8005959
25128832 171988 0 None - 1 Rat 4.6 pEC50 = 4.6 Functional
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
ChEMBL 250 1 1 5 1.2 CN1CCN(c2cc(C(C)(C)C)nc(O)n2)CC1 10.1021/jm8005959
CHEMBL447151 171988 0 None - 1 Rat 4.6 pEC50 = 4.6 Functional
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
ChEMBL 250 1 1 5 1.2 CN1CCN(c2cc(C(C)(C)C)nc(O)n2)CC1 10.1021/jm8005959
25071940 187330 0 None - 1 Rat 7.6 pEC50 = 7.6 Functional
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
ChEMBL 281 1 2 5 1.2 Nc1nc2c(c(N3CCNCC3)n1)CCc1ccccc1-2 10.1021/jm800670r
CHEMBL493281 187330 0 None - 1 Rat 7.6 pEC50 = 7.6 Functional
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
ChEMBL 281 1 2 5 1.2 Nc1nc2c(c(N3CCNCC3)n1)CCc1ccccc1-2 10.1021/jm800670r
127049156 140169 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
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
ChEMBL 272 4 3 3 1.5 N#C/N=C(\NC[C@H]1CC[C@H](c2c[nH]cn2)C1)NC1CC1 10.1021/acs.jmedchem.6b00120
CHEMBL3804837 140169 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
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
ChEMBL 272 4 3 3 1.5 N#C/N=C(\NC[C@H]1CC[C@H](c2c[nH]cn2)C1)NC1CC1 10.1021/acs.jmedchem.6b00120
11437850 187637 1 None - 1 Rat 6.6 pEC50 = 6.6 Functional
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
ChEMBL 294 2 1 6 1.3 CN1CCN(c2cc(-c3cccc(C#N)c3)nc(N)n2)CC1 10.1021/jm8005959
CHEMBL495082 187637 1 None - 1 Rat 6.6 pEC50 = 6.6 Functional
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
ChEMBL 294 2 1 6 1.3 CN1CCN(c2cc(-c3cccc(C#N)c3)nc(N)n2)CC1 10.1021/jm8005959
25129883 192699 0 None - 1 Rat 6.6 pEC50 = 6.6 Functional
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
ChEMBL 300 3 1 7 0.9 COc1ccncc1-c1cc(N2CCN(C)CC2)nc(N)n1 10.1021/jm8005959
CHEMBL522019 192699 0 None - 1 Rat 6.6 pEC50 = 6.6 Functional
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
ChEMBL 300 3 1 7 0.9 COc1ccncc1-c1cc(N2CCN(C)CC2)nc(N)n1 10.1021/jm8005959
25133972 187326 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
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
ChEMBL 293 2 1 5 2.0 CN1CCN(c2cc(-c3ccc(C#N)cc3)cc(N)n2)CC1 10.1021/jm8005959
CHEMBL493262 187326 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
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
ChEMBL 293 2 1 5 2.0 CN1CCN(c2cc(-c3ccc(C#N)cc3)cc(N)n2)CC1 10.1021/jm8005959
25130575 187565 1 None - 1 Rat 4.6 pEC50 = 4.6 Functional
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
ChEMBL 248 1 1 4 2.6 CC1CCN(c2cc(C(C)(C)C)nc(N)n2)CC1 10.1021/jm8005959
CHEMBL494687 187565 1 None - 1 Rat 4.6 pEC50 = 4.6 Functional
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
ChEMBL 248 1 1 4 2.6 CC1CCN(c2cc(C(C)(C)C)nc(N)n2)CC1 10.1021/jm8005959
25130577 172574 0 None - 1 Rat 5.6 pEC50 = 5.6 Functional
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
ChEMBL 306 4 1 6 1.0 CN(C)CCN1CCN(c2cc(C(C)(C)C)nc(N)n2)CC1 10.1021/jm8005959
CHEMBL449021 172574 0 None - 1 Rat 5.6 pEC50 = 5.6 Functional
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
ChEMBL 306 4 1 6 1.0 CN(C)CCN1CCN(c2cc(C(C)(C)C)nc(N)n2)CC1 10.1021/jm8005959
10773349 8059 1 None -89 2 Human 4.6 pEC50 = 4.6 Functional
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
ChEMBL 165 2 2 3 0.4 NC[C@H]1C=C[C@H](c2c[nH]cn2)O1 10.1021/jm0300025
CHEMBL109130 8059 1 None -89 2 Human 4.6 pEC50 = 4.6 Functional
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
ChEMBL 165 2 2 3 0.4 NC[C@H]1C=C[C@H](c2c[nH]cn2)O1 10.1021/jm0300025
127052634 140284 0 None 6 2 Human 6.6 pEC50 = 6.6 Functional
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
ChEMBL 272 4 3 3 1.5 N#C/N=C(\NC[C@@H]1CC[C@H](c2c[nH]cn2)C1)NC1CC1 10.1021/acs.jmedchem.6b00120
CHEMBL3806146 140284 0 None 6 2 Human 6.6 pEC50 = 6.6 Functional
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
ChEMBL 272 4 3 3 1.5 N#C/N=C(\NC[C@@H]1CC[C@H](c2c[nH]cn2)C1)NC1CC1 10.1021/acs.jmedchem.6b00120
90667240 109452 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
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
ChEMBL 356 9 3 4 2.8 Cc1[nH]cnc1CCCCN/C(=N\C#N)NCCSc1ccccc1 10.1039/C3MD00245D
CHEMBL3220642 109452 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
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
ChEMBL 356 9 3 4 2.8 Cc1[nH]cnc1CCCCN/C(=N\C#N)NCCSc1ccccc1 10.1039/C3MD00245D
25130576 187602 1 None -2 2 Rat 6.6 pEC50 = 6.6 Functional
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
ChEMBL 280 2 2 6 1.0 N#Cc1ccc(-c2cc(N3CCNCC3)nc(N)n2)cc1 10.1021/jm8005959
CHEMBL494890 187602 1 None -2 2 Rat 6.6 pEC50 = 6.6 Functional
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
ChEMBL 280 2 2 6 1.0 N#Cc1ccc(-c2cc(N3CCNCC3)nc(N)n2)cc1 10.1021/jm8005959
25128826 188792 0 None - 1 Rat 6.6 pEC50 = 6.6 Functional
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
ChEMBL 263 2 1 5 1.5 CCN1CCN(c2cc(C(C)(C)C)nc(N)n2)CC1 10.1021/jm8005959
CHEMBL506187 188792 0 None - 1 Rat 6.6 pEC50 = 6.6 Functional
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
ChEMBL 263 2 1 5 1.5 CCN1CCN(c2cc(C(C)(C)C)nc(N)n2)CC1 10.1021/jm8005959
25130576 187602 1 None -2 2 Rat 6.6 pEC50 = 6.6 Functional
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
ChEMBL 280 2 2 6 1.0 N#Cc1ccc(-c2cc(N3CCNCC3)nc(N)n2)cc1 10.1021/jm800670r
CHEMBL494890 187602 1 None -2 2 Rat 6.6 pEC50 = 6.6 Functional
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
ChEMBL 280 2 2 6 1.0 N#Cc1ccc(-c2cc(N3CCNCC3)nc(N)n2)cc1 10.1021/jm800670r
58227157 115891 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
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
ChEMBL 235 4 2 5 1.1 CN[C@@H]1CCN(c2ccnc(NC(C)C)n2)C1 10.1016/j.bmcl.2014.12.027
CHEMBL3354815 115891 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
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
ChEMBL 235 4 2 5 1.1 CN[C@@H]1CCN(c2ccnc(NC(C)C)n2)C1 10.1016/j.bmcl.2014.12.027
1204 1919 119 None -3 11 Human 7.6 pEC50 = 7.6 Functional
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
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm1013488
1247 1919 119 None -3 11 Human 7.6 pEC50 = 7.6 Functional
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
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm1013488
1375 1919 119 None -3 11 Human 7.6 pEC50 = 7.6 Functional
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
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm1013488
774 1919 119 None -3 11 Human 7.6 pEC50 = 7.6 Functional
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
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm1013488
CHEMBL90 1919 119 None -3 11 Human 7.6 pEC50 = 7.6 Functional
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
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm1013488
DB05381 1919 119 None -3 11 Human 7.6 pEC50 = 7.6 Functional
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
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm1013488
1226 2006 20 None - 1 Human 7.6 pEC50 = 7.6 Functional
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
ChEMBL 321 9 4 4 1.2 NC(=NCCCc1cnc[nH]1)NCCSCc1nc[nH]c1C 10.1016/j.bmcl.2010.10.041
41376 2006 20 None - 1 Human 7.6 pEC50 = 7.6 Functional
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
ChEMBL 321 9 4 4 1.2 NC(=NCCCc1cnc[nH]1)NCCSCc1nc[nH]c1C 10.1016/j.bmcl.2010.10.041
CHEMBL12608 2006 20 None - 1 Human 7.6 pEC50 = 7.6 Functional
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
ChEMBL 321 9 4 4 1.2 NC(=NCCCc1cnc[nH]1)NCCSCc1nc[nH]c1C 10.1016/j.bmcl.2010.10.041
25133970 187564 2 None - 1 Rat 6.6 pEC50 = 6.6 Functional
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
ChEMBL 250 1 1 6 0.5 CN1CCN(c2nc(N)nc(C(C)(C)C)n2)CC1 10.1021/jm8005959
CHEMBL494679 187564 2 None - 1 Rat 6.6 pEC50 = 6.6 Functional
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
ChEMBL 250 1 1 6 0.5 CN1CCN(c2nc(N)nc(C(C)(C)C)n2)CC1 10.1021/jm8005959
25130230 172432 2 None 3 2 Human 5.6 pEC50 = 5.6 Functional
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
ChEMBL 259 2 1 7 -0.0 CN1CCN(c2cc(-n3ccnc3)nc(N)n2)CC1 10.1021/jm8005959
CHEMBL448085 172432 2 None 3 2 Human 5.6 pEC50 = 5.6 Functional
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
ChEMBL 259 2 1 7 -0.0 CN1CCN(c2cc(-n3ccnc3)nc(N)n2)CC1 10.1021/jm8005959
1269 121 41 None -56 6 Rat 5.6 pEC50 = 5.6 Functional
Agonist activity at rat histamine H4 receptorAgonist activity at rat histamine H4 receptor
ChEMBL 125 2 2 2 0.2 Cc1c(CCN)nc[nH]1 10.1016/j.bmcl.2010.10.041
37463 121 41 None -56 6 Rat 5.6 pEC50 = 5.6 Functional
Agonist activity at rat histamine H4 receptorAgonist activity at rat histamine H4 receptor
ChEMBL 125 2 2 2 0.2 Cc1c(CCN)nc[nH]1 10.1016/j.bmcl.2010.10.041
CHEMBL275443 121 41 None -56 6 Rat 5.6 pEC50 = 5.6 Functional
Agonist activity at rat histamine H4 receptorAgonist activity at rat histamine H4 receptor
ChEMBL 125 2 2 2 0.2 Cc1c(CCN)nc[nH]1 10.1016/j.bmcl.2010.10.041
44480958 5641 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
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
ChEMBL 325 9 3 4 1.8 N#C/N=C(/NCCCCc1c[nH]cn1)NCCCc1ccncc1 10.1021/jm900526h
CHEMBL1077859 5641 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
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
ChEMBL 325 9 3 4 1.8 N#C/N=C(/NCCCCc1c[nH]cn1)NCCCc1ccncc1 10.1021/jm900526h
25131556 188847 7 None 3 2 Human 7.6 pEC50 = 7.6 Functional
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
ChEMBL 300 3 1 7 0.9 COc1ncccc1-c1cc(N2CCN(C)CC2)nc(N)n1 10.1021/jm8005959
CHEMBL507063 188847 7 None 3 2 Human 7.6 pEC50 = 7.6 Functional
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
ChEMBL 300 3 1 7 0.9 COc1ncccc1-c1cc(N2CCN(C)CC2)nc(N)n1 10.1021/jm8005959
127051047 140286 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
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
ChEMBL 246 3 3 3 0.9 CN/C(=N\C#N)NC[C@H]1CC[C@@H](c2c[nH]cn2)C1 10.1021/acs.jmedchem.6b00120
CHEMBL3806162 140286 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
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
ChEMBL 246 3 3 3 0.9 CN/C(=N\C#N)NC[C@H]1CC[C@@H](c2c[nH]cn2)C1 10.1021/acs.jmedchem.6b00120
45257134 199920 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
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
ChEMBL 312 4 2 6 1.7 Cc1cccc(CNc2cc(N3CCN(C)CC3)nc(N)n2)c1 10.1016/j.bmc.2009.08.059
CHEMBL594949 199920 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
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
ChEMBL 312 4 2 6 1.7 Cc1cccc(CNc2cc(N3CCN(C)CC3)nc(N)n2)c1 10.1016/j.bmc.2009.08.059
25131231 187163 0 None - 1 Rat 6.6 pEC50 = 6.6 Functional
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
ChEMBL 395 2 1 5 2.1 CN1CCN(c2cc(-c3ccc(I)cc3)nc(N)n2)CC1 10.1021/jm8005959
CHEMBL492288 187163 0 None - 1 Rat 6.6 pEC50 = 6.6 Functional
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
ChEMBL 395 2 1 5 2.1 CN1CCN(c2cc(-c3ccc(I)cc3)nc(N)n2)CC1 10.1021/jm8005959
10381810 205151 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
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
ChEMBL 327 0 0 4 3.8 CN1CCN(C2=Nc3cc(Cl)ccc3Oc3ccccc32)CC1 10.1021/jm051008s
CHEMBL7828 205151 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
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
ChEMBL 327 0 0 4 3.8 CN1CCN(C2=Nc3cc(Cl)ccc3Oc3ccccc32)CC1 10.1021/jm051008s
155512725 176217 0 None 1 3 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 237 6 3 5 1.7 CC(C)(C)CNc1nccc(NCCCN)n1 10.1021/acs.jmedchem.9b01342
CHEMBL4437371 176217 0 None 1 3 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 237 6 3 5 1.7 CC(C)(C)CNc1nccc(NCCCN)n1 10.1021/acs.jmedchem.9b01342
CHEMBL4594753 176217 0 None 1 3 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 237 6 3 5 1.7 CC(C)(C)CNc1nccc(NCCCN)n1 10.1021/acs.jmedchem.9b01342
127052294 140277 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
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
ChEMBL 368 7 3 4 3.1 N#C/N=C(/NCCSc1ccccc1)NC[C@@H]1CC[C@H](c2c[nH]cn2)C1 10.1021/acs.jmedchem.6b00120
CHEMBL3806079 140277 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
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
ChEMBL 368 7 3 4 3.1 N#C/N=C(/NCCSc1ccccc1)NC[C@@H]1CC[C@H](c2c[nH]cn2)C1 10.1021/acs.jmedchem.6b00120
1204 1919 119 None -288 11 Rat 6.5 pEC50 = 6.5 Functional
Agonist activity at rat H4R expressed in HEK293-SF-rH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at rat H4R expressed in HEK293-SF-rH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.9b01342
1247 1919 119 None -288 11 Rat 6.5 pEC50 = 6.5 Functional
Agonist activity at rat H4R expressed in HEK293-SF-rH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at rat H4R expressed in HEK293-SF-rH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.9b01342
1375 1919 119 None -288 11 Rat 6.5 pEC50 = 6.5 Functional
Agonist activity at rat H4R expressed in HEK293-SF-rH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at rat H4R expressed in HEK293-SF-rH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.9b01342
774 1919 119 None -288 11 Rat 6.5 pEC50 = 6.5 Functional
Agonist activity at rat H4R expressed in HEK293-SF-rH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at rat H4R expressed in HEK293-SF-rH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.9b01342
CHEMBL90 1919 119 None -288 11 Rat 6.5 pEC50 = 6.5 Functional
Agonist activity at rat H4R expressed in HEK293-SF-rH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at rat H4R expressed in HEK293-SF-rH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.9b01342
DB05381 1919 119 None -288 11 Rat 6.5 pEC50 = 6.5 Functional
Agonist activity at rat H4R expressed in HEK293-SF-rH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at rat H4R expressed in HEK293-SF-rH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.9b01342
25128822 187457 0 None -19 2 Human 6.5 pEC50 = 6.5 Functional
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
ChEMBL 295 1 1 5 1.6 CN1CCN(c2nc(N)nc3c2CCc2ccccc2-3)CC1 10.1016/j.bmcl.2015.12.035
CHEMBL494093 187457 0 None -19 2 Human 6.5 pEC50 = 6.5 Functional
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
ChEMBL 295 1 1 5 1.6 CN1CCN(c2nc(N)nc3c2CCc2ccccc2-3)CC1 10.1016/j.bmcl.2015.12.035
155491015 176471 4 None -31 4 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human H4R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by CRE-luciferase reporter gene assayAgonist activity at human H4R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by CRE-luciferase reporter gene assay
ChEMBL 207 4 2 5 0.2 CCCNC1CN(c2ccnc(N)n2)C1 10.1021/acs.jmedchem.9b01462
CHEMBL4441731 176471 4 None -31 4 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human H4R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by CRE-luciferase reporter gene assayAgonist activity at human H4R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by CRE-luciferase reporter gene assay
ChEMBL 207 4 2 5 0.2 CCCNC1CN(c2ccnc(N)n2)C1 10.1021/acs.jmedchem.9b01462
CHEMBL4596734 176471 4 None -31 4 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human H4R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by CRE-luciferase reporter gene assayAgonist activity at human H4R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by CRE-luciferase reporter gene assay
ChEMBL 207 4 2 5 0.2 CCCNC1CN(c2ccnc(N)n2)C1 10.1021/acs.jmedchem.9b01462
46890072 6878 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
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
ChEMBL 404 8 2 4 4.9 Cc1cc(OCCCNCc2cccnc2)ccc1-c1nc2c(C)c(F)ccc2[nH]1 10.1016/j.bmcl.2010.04.017
CHEMBL1084355 6878 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
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
ChEMBL 404 8 2 4 4.9 Cc1cc(OCCCNCc2cccnc2)ccc1-c1nc2c(C)c(F)ccc2[nH]1 10.1016/j.bmcl.2010.04.017
46890166 7284 0 None 3 4 Human 8.5 pEC50 = 8.5 Functional
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
ChEMBL 419 6 2 4 4.5 Cc1cc(OCCCN2CCc3nc[nH]c3C2)ccc1-c1nc2c(C)c(F)ccc2[nH]1 10.1016/j.bmcl.2010.04.017
CHEMBL1086105 7284 0 None 3 4 Human 8.5 pEC50 = 8.5 Functional
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
ChEMBL 419 6 2 4 4.5 Cc1cc(OCCCN2CCc3nc[nH]c3C2)ccc1-c1nc2c(C)c(F)ccc2[nH]1 10.1016/j.bmcl.2010.04.017
58227373 176484 0 None 1 3 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 249 3 2 5 1.5 CC(C)(C)CNc1nccc(N2CC[C@@H](N)C2)n1 10.1021/acs.jmedchem.9b01342
CHEMBL4455324 176484 0 None 1 3 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 249 3 2 5 1.5 CC(C)(C)CNc1nccc(N2CC[C@@H](N)C2)n1 10.1021/acs.jmedchem.9b01342
CHEMBL4596881 176484 0 None 1 3 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 249 3 2 5 1.5 CC(C)(C)CNc1nccc(N2CC[C@@H](N)C2)n1 10.1021/acs.jmedchem.9b01342
21638785 188634 5 None -1 2 Rat 7.5 pEC50 = 7.5 Functional
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
ChEMBL 263 1 2 2 1.9 O=C(c1cc2cc(Cl)ccc2[nH]1)N1CCNCC1 10.1021/jm800670r
CHEMBL503605 188634 5 None -1 2 Rat 7.5 pEC50 = 7.5 Functional
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
ChEMBL 263 1 2 2 1.9 O=C(c1cc2cc(Cl)ccc2[nH]1)N1CCNCC1 10.1021/jm800670r
25130911 185206 0 None - 1 Rat 5.5 pEC50 = 5.5 Functional
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
ChEMBL 236 2 1 6 -0.1 CN1CCN(c2cc(N(C)C)nc(N)n2)CC1 10.1021/jm8005959
CHEMBL485802 185206 0 None - 1 Rat 5.5 pEC50 = 5.5 Functional
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
ChEMBL 236 2 1 6 -0.1 CN1CCN(c2cc(N(C)C)nc(N)n2)CC1 10.1021/jm8005959
16352 117159 13 None - 1 Human 6.5 pEC50 = 6.5 Functional
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
ChEMBL 293 0 0 4 3.1 CN1CCN(C2=Nc3ccccc3Oc3ccccc32)CC1 10.1021/jm051008s
CHEMBL339414 117159 13 None - 1 Human 6.5 pEC50 = 6.5 Functional
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
ChEMBL 293 0 0 4 3.1 CN1CCN(C2=Nc3ccccc3Oc3ccccc32)CC1 10.1021/jm051008s
1267 3775 49 None -8 5 Mouse 6.5 pEC50 = 6.5 Functional
Agonist activity at mouse H4R expressed in HEK293-SF-mH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at mouse H4R expressed in HEK293-SF-mH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1021/acs.jmedchem.0c00160
3035905 3775 49 None -8 5 Mouse 6.5 pEC50 = 6.5 Functional
Agonist activity at mouse H4R expressed in HEK293-SF-mH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at mouse H4R expressed in HEK293-SF-mH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1021/acs.jmedchem.0c00160
CHEMBL260374 3775 49 None -8 5 Mouse 6.5 pEC50 = 6.5 Functional
Agonist activity at mouse H4R expressed in HEK293-SF-mH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at mouse H4R expressed in HEK293-SF-mH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1021/acs.jmedchem.0c00160
25130579 187688 2 None - 1 Rat 6.5 pEC50 = 6.5 Functional
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
ChEMBL 238 4 1 5 1.3 CN(C)CCOc1cc(C(C)(C)C)nc(N)n1 10.1021/jm8005959
CHEMBL495341 187688 2 None - 1 Rat 6.5 pEC50 = 6.5 Functional
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
ChEMBL 238 4 1 5 1.3 CN(C)CCOc1cc(C(C)(C)C)nc(N)n1 10.1021/jm8005959
10678661 5330 1 None -309 2 Human 4.5 pEC50 = 4.5 Functional
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
ChEMBL 167 2 2 3 0.6 NC[C@@H]1CC[C@@H](c2c[nH]cn2)O1 10.1021/jm0300025
CHEMBL106931 5330 1 None -309 2 Human 4.5 pEC50 = 4.5 Functional
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
ChEMBL 167 2 2 3 0.6 NC[C@@H]1CC[C@@H](c2c[nH]cn2)O1 10.1021/jm0300025
46228101 199775 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
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
ChEMBL 332 4 2 6 2.1 CN1CCN(c2cc(NCc3ccc(Cl)cc3)nc(N)n2)CC1 10.1016/j.bmc.2009.08.059
CHEMBL594022 199775 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
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
ChEMBL 332 4 2 6 2.1 CN1CCN(c2cc(NCc3ccc(Cl)cc3)nc(N)n2)CC1 10.1016/j.bmc.2009.08.059
1249 1996 16 None -18 2 Human 7.5 pEC50 = 7.5 Functional
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
ChEMBL 139 4 2 2 0.7 NCCCCc1cnc[nH]1 10.1016/j.bmcl.2010.10.041
13499360 1996 16 None -18 2 Human 7.5 pEC50 = 7.5 Functional
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
ChEMBL 139 4 2 2 0.7 NCCCCc1cnc[nH]1 10.1016/j.bmcl.2010.10.041
CHEMBL90019 1996 16 None -18 2 Human 7.5 pEC50 = 7.5 Functional
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
ChEMBL 139 4 2 2 0.7 NCCCCc1cnc[nH]1 10.1016/j.bmcl.2010.10.041
1269 121 41 None 35 6 Human 7.5 pEC50 = 7.5 Functional
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
ChEMBL 125 2 2 2 0.2 Cc1c(CCN)nc[nH]1 10.1016/j.bmcl.2010.10.041
37463 121 41 None 35 6 Human 7.5 pEC50 = 7.5 Functional
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
ChEMBL 125 2 2 2 0.2 Cc1c(CCN)nc[nH]1 10.1016/j.bmcl.2010.10.041
CHEMBL275443 121 41 None 35 6 Human 7.5 pEC50 = 7.5 Functional
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
ChEMBL 125 2 2 2 0.2 Cc1c(CCN)nc[nH]1 10.1016/j.bmcl.2010.10.041
25129528 187162 0 None - 1 Rat 7.5 pEC50 = 7.5 Functional
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
ChEMBL 303 2 1 5 2.1 CN1CCN(c2cc(-c3cccc(Cl)c3)nc(N)n2)CC1 10.1021/jm8005959
CHEMBL492287 187162 0 None - 1 Rat 7.5 pEC50 = 7.5 Functional
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
ChEMBL 303 2 1 5 2.1 CN1CCN(c2cc(-c3cccc(Cl)c3)nc(N)n2)CC1 10.1021/jm8005959
44568923 193079 0 None - 1 Rat 6.5 pEC50 = 6.5 Functional
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
ChEMBL 327 2 1 5 2.3 CN1CCN(c2cc(C34CC5CC(CC(C5)C3)C4)nc(N)n2)CC1 10.1021/jm8005959
CHEMBL522661 193079 0 None - 1 Rat 6.5 pEC50 = 6.5 Functional
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
ChEMBL 327 2 1 5 2.3 CN1CCN(c2cc(C34CC5CC(CC(C5)C3)C4)nc(N)n2)CC1 10.1021/jm8005959
67087450 117110 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
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
ChEMBL 249 5 2 5 1.3 CN[C@@H]1CCN(c2cnnc(NCC(C)C)c2)C1 10.1016/j.bmcl.2014.12.027
CHEMBL3393550 117110 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
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
ChEMBL 249 5 2 5 1.3 CN[C@@H]1CCN(c2cnnc(NCC(C)C)c2)C1 10.1016/j.bmcl.2014.12.027
44547127 115892 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
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
ChEMBL 234 4 2 4 1.7 CN[C@@H]1CCN(c2ccnc(NC(C)C)c2)C1 10.1016/j.bmcl.2014.12.027
CHEMBL3354816 115892 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
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
ChEMBL 234 4 2 4 1.7 CN[C@@H]1CCN(c2ccnc(NC(C)C)c2)C1 10.1016/j.bmcl.2014.12.027
58227148 117107 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
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
ChEMBL 287 4 2 5 1.9 CN[C@@H]1CCN(c2ccnc(NC3CC4CCC3C4)n2)C1 10.1016/j.bmcl.2014.12.027
CHEMBL3393547 117107 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
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
ChEMBL 287 4 2 5 1.9 CN[C@@H]1CCN(c2ccnc(NC3CC4CCC3C4)n2)C1 10.1016/j.bmcl.2014.12.027
10678661 5330 1 None -309 2 Human 4.5 pEC50 = 4.5 Functional
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
ChEMBL 167 2 2 3 0.6 NC[C@@H]1CC[C@@H](c2c[nH]cn2)O1 10.1016/j.bmcl.2010.10.041
CHEMBL106931 5330 1 None -309 2 Human 4.5 pEC50 = 4.5 Functional
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
ChEMBL 167 2 2 3 0.6 NC[C@@H]1CC[C@@H](c2c[nH]cn2)O1 10.1016/j.bmcl.2010.10.041
25131557 193235 0 None - 1 Rat 5.5 pEC50 = 5.5 Functional
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
ChEMBL 301 3 1 8 0.3 COc1ncc(-c2cc(N3CCN(C)CC3)nc(N)n2)cn1 10.1021/jm8005959
CHEMBL523835 193235 0 None - 1 Rat 5.5 pEC50 = 5.5 Functional
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
ChEMBL 301 3 1 8 0.3 COc1ncc(-c2cc(N3CCN(C)CC3)nc(N)n2)cn1 10.1021/jm8005959
25130909 187356 0 None 1 2 Human 7.5 pEC50 = 7.5 Functional
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
ChEMBL 208 1 2 6 -0.6 CN1CCN(c2nc(N)ncc2N)CC1 10.1021/jm8005959
CHEMBL493478 187356 0 None 1 2 Human 7.5 pEC50 = 7.5 Functional
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
ChEMBL 208 1 2 6 -0.6 CN1CCN(c2nc(N)ncc2N)CC1 10.1021/jm8005959
44478385 5744 6 None 20 2 Human 7.5 pEC50 = 7.5 Functional
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
ChEMBL 342 9 3 4 2.5 N#C/N=C(/NCCCCc1c[nH]cn1)NCCSc1ccccc1 10.1021/jm900526h
CHEMBL1078642 5744 6 None 20 2 Human 7.5 pEC50 = 7.5 Functional
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
ChEMBL 342 9 3 4 2.5 N#C/N=C(/NCCCCc1c[nH]cn1)NCCSc1ccccc1 10.1021/jm900526h
46890549 6553 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
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
ChEMBL 396 6 2 4 4.2 Cc1cc(OCCCN2CCCC(N)C2)ccc1-c1nc2c(C)c(F)ccc2[nH]1 10.1016/j.bmcl.2010.04.017
CHEMBL1083085 6553 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
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
ChEMBL 396 6 2 4 4.2 Cc1cc(OCCCN2CCCC(N)C2)ccc1-c1nc2c(C)c(F)ccc2[nH]1 10.1016/j.bmcl.2010.04.017
44480960 5598 2 None - 1 Human 6.5 pEC50 = 6.5 Functional
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
ChEMBL 248 6 3 3 1.2 CC(C)N/C(=N\C#N)NCCCCc1c[nH]cn1 10.1021/jm900526h
CHEMBL1077636 5598 2 None - 1 Human 6.5 pEC50 = 6.5 Functional
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
ChEMBL 248 6 3 3 1.2 CC(C)N/C(=N\C#N)NCCCCc1c[nH]cn1 10.1021/jm900526h
42625303 180742 0 None -2089 6 Rat 5.5 pEC50 = 5.5 Functional
Agonist activity at rat H4R by [35S]-GTPgammaS-binding assayAgonist activity at rat H4R by [35S]-GTPgammaS-binding assay
ChEMBL 223 5 3 2 0.2 CCC(=O)/N=C(\N)NCCCc1c[nH]cn1 10.1021/acs.jmedchem.9b01342
CHEMBL475621 180742 0 None -2089 6 Rat 5.5 pEC50 = 5.5 Functional
Agonist activity at rat H4R by [35S]-GTPgammaS-binding assayAgonist activity at rat H4R by [35S]-GTPgammaS-binding assay
ChEMBL 223 5 3 2 0.2 CCC(=O)/N=C(\N)NCCCc1c[nH]cn1 10.1021/acs.jmedchem.9b01342
56954425 82052 0 None -13 2 Human 6.5 pEC50 = 6.5 Functional
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
ChEMBL 584 23 6 4 4.0 N/C(=N\C(=O)CCCCCCCCCCCCCCC(=O)/N=C(\N)NCCCc1c[nH]cn1)NCCCc1c[nH]cn1 10.1021/jm201128q
CHEMBL2165643 82052 0 None -13 2 Human 6.5 pEC50 = 6.5 Functional
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
ChEMBL 584 23 6 4 4.0 N/C(=N\C(=O)CCCCCCCCCCCCCCC(=O)/N=C(\N)NCCCc1c[nH]cn1)NCCCc1c[nH]cn1 10.1021/jm201128q
25130913 170163 0 None - 1 Rat 6.5 pEC50 = 6.5 Functional
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
ChEMBL 278 2 1 7 -0.4 CN1CCN(c2cc(N3CCOCC3)nc(N)n2)CC1 10.1021/jm8005959
CHEMBL444484 170163 0 None - 1 Rat 6.5 pEC50 = 6.5 Functional
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
ChEMBL 278 2 1 7 -0.4 CN1CCN(c2cc(N3CCOCC3)nc(N)n2)CC1 10.1021/jm8005959
1274 4033 16 None -776 4 Rat 4.5 pEC50 = 4.5 Functional
Agonist activity at rat H4R by [35S]-GTPgammaS-binding assayAgonist activity at rat H4R by [35S]-GTPgammaS-binding assay
ChEMBL 161 3 4 3 -1.1 NC(=N)SCCN=C(N)N 10.1021/acs.jmedchem.9b01342
3063228 4033 16 None -776 4 Rat 4.5 pEC50 = 4.5 Functional
Agonist activity at rat H4R by [35S]-GTPgammaS-binding assayAgonist activity at rat H4R by [35S]-GTPgammaS-binding assay
ChEMBL 161 3 4 3 -1.1 NC(=N)SCCN=C(N)N 10.1021/acs.jmedchem.9b01342
CHEMBL1196470 4033 16 None -776 4 Rat 4.5 pEC50 = 4.5 Functional
Agonist activity at rat H4R by [35S]-GTPgammaS-binding assayAgonist activity at rat H4R by [35S]-GTPgammaS-binding assay
ChEMBL 161 3 4 3 -1.1 NC(=N)SCCN=C(N)N 10.1021/acs.jmedchem.9b01342
155517880 176643 0 None -3 3 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 291 4 4 5 1.0 CC(C)(C)CNc1nccc(N2CC[C@@H](NC(=N)N)C2)n1 10.1021/acs.jmedchem.9b01342
CHEMBL4445423 176643 0 None -3 3 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 291 4 4 5 1.0 CC(C)(C)CNc1nccc(N2CC[C@@H](NC(=N)N)C2)n1 10.1021/acs.jmedchem.9b01342
CHEMBL4598198 176643 0 None -3 3 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 291 4 4 5 1.0 CC(C)(C)CNc1nccc(N2CC[C@@H](NC(=N)N)C2)n1 10.1021/acs.jmedchem.9b01342
155552061 176454 0 None -8 3 Mouse 7.5 pEC50 = 7.5 Functional
Agonist activity at mouse H4R expressed in HEK293-SF-mH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at mouse H4R expressed in HEK293-SF-mH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 277 3 1 5 2.1 CN1CCCN(c2ccnc(NCC(C)(C)C)n2)CC1 10.1021/acs.jmedchem.9b01342
CHEMBL4543119 176454 0 None -8 3 Mouse 7.5 pEC50 = 7.5 Functional
Agonist activity at mouse H4R expressed in HEK293-SF-mH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at mouse H4R expressed in HEK293-SF-mH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 277 3 1 5 2.1 CN1CCCN(c2ccnc(NCC(C)(C)C)n2)CC1 10.1021/acs.jmedchem.9b01342
CHEMBL4596606 176454 0 None -8 3 Mouse 7.5 pEC50 = 7.5 Functional
Agonist activity at mouse H4R expressed in HEK293-SF-mH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at mouse H4R expressed in HEK293-SF-mH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 277 3 1 5 2.1 CN1CCCN(c2ccnc(NCC(C)(C)C)n2)CC1 10.1021/acs.jmedchem.9b01342
25129180 187227 0 None - 1 Rat 6.5 pEC50 = 6.5 Functional
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
ChEMBL 264 4 1 6 0.7 CCN(CC)c1cc(N2CCN(C)CC2)nc(N)n1 10.1021/jm8005959
CHEMBL492662 187227 0 None - 1 Rat 6.5 pEC50 = 6.5 Functional
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
ChEMBL 264 4 1 6 0.7 CCN(CC)c1cc(N2CCN(C)CC2)nc(N)n1 10.1021/jm8005959
3228743 187357 5 None - 1 Rat 6.4 pEC50 = 6.4 Functional
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
ChEMBL 207 1 1 5 0.1 Cc1cc(N2CCN(C)CC2)nc(N)n1 10.1021/jm8005959
CHEMBL493479 187357 5 None - 1 Rat 6.4 pEC50 = 6.4 Functional
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
ChEMBL 207 1 1 5 0.1 Cc1cc(N2CCN(C)CC2)nc(N)n1 10.1021/jm8005959
12769844 109451 0 None -3 2 Human 5.4 pEC50 = 5.4 Functional
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
ChEMBL 234 5 3 3 0.7 CN/C(=N/C#N)NCCCCc1nc[nH]c1C 10.1039/C3MD00245D
CHEMBL3220641 109451 0 None -3 2 Human 5.4 pEC50 = 5.4 Functional
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
ChEMBL 234 5 3 3 0.7 CN/C(=N/C#N)NCCCCc1nc[nH]c1C 10.1039/C3MD00245D
25129181 187228 0 None - 1 Rat 5.4 pEC50 = 5.4 Functional
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
ChEMBL 305 3 1 7 -0.0 CN1CCN(c2cc(N3CCC(N(C)C)C3)nc(N)n2)CC1 10.1021/jm8005959
CHEMBL492663 187228 0 None - 1 Rat 5.4 pEC50 = 5.4 Functional
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
ChEMBL 305 3 1 7 -0.0 CN1CCN(c2cc(N3CCC(N(C)C)C3)nc(N)n2)CC1 10.1021/jm8005959
25128825 187540 0 None - 1 Rat 5.4 pEC50 = 5.4 Functional
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
ChEMBL 248 1 1 4 2.2 CN1CCC(c2cc(C(C)(C)C)nc(N)n2)CC1 10.1021/jm8005959
CHEMBL494585 187540 0 None - 1 Rat 5.4 pEC50 = 5.4 Functional
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
ChEMBL 248 1 1 4 2.2 CN1CCC(c2cc(C(C)(C)C)nc(N)n2)CC1 10.1021/jm8005959
44478385 5744 6 None 20 2 Human 7.4 pEC50 = 7.4 Functional
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
ChEMBL 342 9 3 4 2.5 N#C/N=C(/NCCCCc1c[nH]cn1)NCCSc1ccccc1 10.1021/acs.jmedchem.6b00120
CHEMBL1078642 5744 6 None 20 2 Human 7.4 pEC50 = 7.4 Functional
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
ChEMBL 342 9 3 4 2.5 N#C/N=C(/NCCCCc1c[nH]cn1)NCCSc1ccccc1 10.1021/acs.jmedchem.6b00120
44478385 5744 6 None 20 2 Human 7.4 pEC50 = 7.4 Functional
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
ChEMBL 342 9 3 4 2.5 N#C/N=C(/NCCCCc1c[nH]cn1)NCCSc1ccccc1 10.1039/C3MD00245D
CHEMBL1078642 5744 6 None 20 2 Human 7.4 pEC50 = 7.4 Functional
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
ChEMBL 342 9 3 4 2.5 N#C/N=C(/NCCCCc1c[nH]cn1)NCCSc1ccccc1 10.1039/C3MD00245D
25129527 187390 0 None - 1 Rat 7.4 pEC50 = 7.4 Functional
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
ChEMBL 303 2 1 5 2.1 CN1CCN(c2cc(-c3ccc(Cl)cc3)nc(N)n2)CC1 10.1021/jm8005959
CHEMBL493720 187390 0 None - 1 Rat 7.4 pEC50 = 7.4 Functional
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
ChEMBL 303 2 1 5 2.1 CN1CCN(c2cc(-c3ccc(Cl)cc3)nc(N)n2)CC1 10.1021/jm8005959
24798596 199844 2 None - 1 Human 7.4 pEC50 = 7.4 Functional
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
ChEMBL 310 2 1 6 1.3 CN1CCN(c2cc(N3Cc4ccccc4C3)nc(N)n2)CC1 10.1016/j.bmc.2009.08.059
CHEMBL594491 199844 2 None - 1 Human 7.4 pEC50 = 7.4 Functional
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
ChEMBL 310 2 1 6 1.3 CN1CCN(c2cc(N3Cc4ccccc4C3)nc(N)n2)CC1 10.1016/j.bmc.2009.08.059
127052292 140241 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
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
ChEMBL 350 7 3 3 2.9 N#C/N=C(/NCCCc1ccccc1)NC[C@@H]1CC[C@H](c2c[nH]cn2)C1 10.1021/acs.jmedchem.6b00120
CHEMBL3805663 140241 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
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
ChEMBL 350 7 3 3 2.9 N#C/N=C(/NCCCc1ccccc1)NC[C@@H]1CC[C@H](c2c[nH]cn2)C1 10.1021/acs.jmedchem.6b00120
1274 4033 16 None 7 4 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human H4R by [35S]-GTPgammaS-binding assayAgonist activity at human H4R by [35S]-GTPgammaS-binding assay
ChEMBL 161 3 4 3 -1.1 NC(=N)SCCN=C(N)N 10.1021/acs.jmedchem.9b01342
3063228 4033 16 None 7 4 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human H4R by [35S]-GTPgammaS-binding assayAgonist activity at human H4R by [35S]-GTPgammaS-binding assay
ChEMBL 161 3 4 3 -1.1 NC(=N)SCCN=C(N)N 10.1021/acs.jmedchem.9b01342
CHEMBL1196470 4033 16 None 7 4 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human H4R by [35S]-GTPgammaS-binding assayAgonist activity at human H4R by [35S]-GTPgammaS-binding assay
ChEMBL 161 3 4 3 -1.1 NC(=N)SCCN=C(N)N 10.1021/acs.jmedchem.9b01342
11846465 141907 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
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
ChEMBL 345 0 0 4 3.9 CN1CCN(C2=Nc3ccc(Cl)cc3Oc3cc(F)ccc32)CC1 10.1021/jm051008s
CHEMBL387054 141907 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
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
ChEMBL 345 0 0 4 3.9 CN1CCN(C2=Nc3ccc(Cl)cc3Oc3cc(F)ccc32)CC1 10.1021/jm051008s
25131559 187561 0 None -23 2 Rat 6.4 pEC50 = 6.4 Functional
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
ChEMBL 259 2 2 6 0.2 CN1CCN(c2cc(-c3c[nH]cn3)nc(N)n2)CC1 10.1021/jm8005959
CHEMBL494667 187561 0 None -23 2 Rat 6.4 pEC50 = 6.4 Functional
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
ChEMBL 259 2 2 6 0.2 CN1CCN(c2cc(-c3c[nH]cn3)nc(N)n2)CC1 10.1021/jm8005959
25131561 187380 0 None 3 2 Human 5.4 pEC50 = 5.4 Functional
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
ChEMBL 286 2 1 7 -0.0 CN1CCN(c2cc(-n3ccccc3=O)nc(N)n2)CC1 10.1021/jm8005959
CHEMBL493664 187380 0 None 3 2 Human 5.4 pEC50 = 5.4 Functional
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
ChEMBL 286 2 1 7 -0.0 CN1CCN(c2cc(-n3ccccc3=O)nc(N)n2)CC1 10.1021/jm8005959
46235428 6572 0 None -263 3 Mouse 7.4 pEC50 = 7.4 Functional
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
ChEMBL 407