Ligand source activities (1 row/activity)



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Ligands (move mouse cursor over ligand name to see structure) Receptor Activity Chemical information
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 Activity
Type		 Activity
Relation		 Activity
Value		 p-value
(-log)		 Fold
selectivity		 Tested
GPCRs		 Assay
Description		 Source

 Mol
weight		 Rot
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 DOI
155524115 176652 None 0 Rat Functional pEC50 = 10.3 10.3 -1 3
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 176652 None 0 Rat Functional pEC50 = 10.3 10.3 -1 3
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 176652 None 0 Rat Functional pEC50 = 10.3 10.3 -1 3
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 176652 None 0 Human Functional pEC50 = 9.9 9.9 1 3
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 176652 None 0 Human Functional pEC50 = 9.9 9.9 1 3
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 176652 None 0 Human Functional pEC50 = 9.9 9.9 1 3
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 176652 None 0 Mouse Functional pEC50 = 9.6 9.6 -4 3
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 176652 None 0 Mouse Functional pEC50 = 9.6 9.6 -4 3
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 176652 None 0 Mouse Functional pEC50 = 9.6 9.6 -4 3
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 6606 None 0 Human Functional pEC50 = 9.3 9.3 263 3
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 6606 None 0 Human Functional pEC50 = 9.3 9.3 263 3
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 176556 None 0 Human Functional pEC50 = 9.2 9.2 2 3
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 176556 None 0 Human Functional pEC50 = 9.2 9.2 2 3
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 176556 None 0 Human Functional pEC50 = 9.2 9.2 2 3
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 176556 None 0 Rat Functional pEC50 = 9.2 9.2 -2 3
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 176556 None 0 Rat Functional pEC50 = 9.2 9.2 -2 3
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 176556 None 0 Rat Functional pEC50 = 9.2 9.2 -2 3
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 176425 None 0 Rat Functional pEC50 = 9.2 9.2 -18 3
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 176425 None 0 Rat Functional pEC50 = 9.2 9.2 -18 3
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 176425 None 0 Rat Functional pEC50 = 9.2 9.2 -18 3
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 176425 None 0 Rat Functional pEC50 = 9.2 9.2 -18 3
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 58906 None 0 Human Functional pEC50 = 9 9.0 - 1
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 58906 None 0 Human Functional pEC50 = 9 9.0 - 1
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 176600 None 5 Mouse Functional pEC50 = 9 9.0 -10 4
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 176600 None 5 Mouse Functional pEC50 = 9 9.0 -10 4
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 176600 None 5 Mouse Functional pEC50 = 9 9.0 -10 4
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 176425 None 0 Mouse Functional pEC50 = 9.0 9.0 -14 3
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 176425 None 0 Mouse Functional pEC50 = 9.0 9.0 -14 3
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 176425 None 0 Mouse Functional pEC50 = 9.0 9.0 -14 3
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 176425 None 0 Mouse Functional pEC50 = 9.0 9.0 -14 3
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 176556 None 0 Mouse Functional pEC50 = 9.0 9.0 -2 3
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 176556 None 0 Mouse Functional pEC50 = 9.0 9.0 -2 3
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 176556 None 0 Mouse Functional pEC50 = 9.0 9.0 -2 3
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 3682 None 14 Human Functional pEC50 = 9.0 9.0 - 1
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 3682 None 14 Human Functional pEC50 = 9.0 9.0 - 1
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 3682 None 14 Human Functional pEC50 = 9.0 9.0 - 1
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 176583 None 0 Rat Functional pEC50 = 8.9 8.9 2 3
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 176583 None 0 Rat Functional pEC50 = 8.9 8.9 2 3
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 176583 None 0 Rat Functional pEC50 = 8.9 8.9 2 3
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 176772 None 0 Rat Functional pEC50 = 8.9 8.9 2 3
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 176772 None 0 Rat Functional pEC50 = 8.9 8.9 2 3
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 176772 None 0 Rat Functional pEC50 = 8.9 8.9 2 3
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 3682 None 14 Human Functional pEC50 = 8.9 8.9 - 1
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 3682 None 14 Human Functional pEC50 = 8.9 8.9 - 1
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 3682 None 14 Human Functional pEC50 = 8.9 8.9 - 1
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 176613 None 0 Rat Functional pEC50 = 8.8 8.8 -1 3
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 176613 None 0 Rat Functional pEC50 = 8.8 8.8 -1 3
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 176613 None 0 Rat Functional pEC50 = 8.8 8.8 -1 3
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 176425 None 0 Human Functional pEC50 = 8.7 8.7 14 3
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 176425 None 0 Human Functional pEC50 = 8.7 8.7 14 3
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 176425 None 0 Human Functional pEC50 = 8.7 8.7 14 3
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 176425 None 0 Human Functional pEC50 = 8.7 8.7 14 3
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 56498 None 0 Mouse Functional pEC50 = 8 8.0 1 3
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 56498 None 0 Mouse Functional pEC50 = 8 8.0 1 3
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 56498 None 0 Rat Functional pEC50 = 8 8.0 -1 3
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 56498 None 0 Rat Functional pEC50 = 8 8.0 -1 3
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 188545 None 19 Rat Functional pEC50 = 8 8.0 -1 2
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 188545 None 19 Rat Functional pEC50 = 8 8.0 -1 2
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 104250 None 0 Human Functional pEC50 = 7 7.0 - 1
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 104250 None 0 Human Functional pEC50 = 7 7.0 - 1
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 140287 None 0 Human Functional pEC50 = 7 7.0 4 3
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 140287 None 0 Human Functional pEC50 = 7 7.0 4 3
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 56497 None 3 Human Functional pEC50 = 7 7.0 1 3
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 56497 None 3 Human Functional pEC50 = 7 7.0 1 3
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 2015 None 18 Human Functional pEC50 = 6 6.0 -3388 2
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 2015 None 18 Human Functional pEC50 = 6 6.0 -3388 2
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 2015 None 18 Human Functional pEC50 = 6 6.0 -3388 2
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 117206 None 0 Human Functional pEC50 = 6 6.0 - 1
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 117206 None 0 Human Functional pEC50 = 6 6.0 - 1
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 45 None 1 Human Functional pEC50 = 5 5.0 -50 2
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 45 None 1 Human Functional pEC50 = 5 5.0 -50 2
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 45 None 1 Human Functional pEC50 = 5 5.0 -50 2
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 61582 None 0 Human Functional pEC50 = 7 7.0 - 1
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 61582 None 0 Human Functional pEC50 = 7 7.0 - 1
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 139307 None 0 Human Functional pEC50 = 7.0 7.0 - 1
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 139307 None 0 Human Functional pEC50 = 7.0 7.0 - 1
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 202632 None 0 Human Functional pEC50 = 7.0 7.0 - 1
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 202632 None 0 Human Functional pEC50 = 7.0 7.0 - 1
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 187732 None 0 Mouse Functional pEC50 = 7.0 7.0 2 2
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 187732 None 0 Mouse Functional pEC50 = 7.0 7.0 2 2
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 187669 None 0 Rat Functional pEC50 = 7.0 7.0 - 1
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium 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 187669 None 0 Rat Functional pEC50 = 7.0 7.0 - 1
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium 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 187701 None 0 Rat Functional pEC50 = 7.0 7.0 - 1
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium 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 187701 None 0 Rat Functional pEC50 = 7.0 7.0 - 1
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium 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 187732 None 0 Mouse Functional pEC50 = 7.0 7.0 2 2
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 187732 None 0 Mouse Functional pEC50 = 7.0 7.0 2 2
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 78711 None 0 Human Functional pEC50 = 7.0 7.0 - 1
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 78711 None 0 Human Functional pEC50 = 7.0 7.0 - 1
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 204602 None 0 Human Functional pEC50 = 7.0 7.0 - 1
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 204602 None 0 Human Functional pEC50 = 7.0 7.0 - 1
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 187735 None 0 Rat Functional pEC50 = 5.0 5.0 - 1
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium 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 187735 None 0 Rat Functional pEC50 = 5.0 5.0 - 1
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium 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 3804 None 32 Human Functional pEC50 = 7.0 7.0 -17 5
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 3804 None 32 Human Functional pEC50 = 7.0 7.0 -17 5
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 3804 None 32 Human Functional pEC50 = 7.0 7.0 -17 5
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 5777 None 0 Human Functional pEC50 = 6.0 6.0 - 1
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 5777 None 0 Human Functional pEC50 = 6.0 6.0 - 1
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 61546 None 0 Human Functional pEC50 = 8.0 8.0 - 1
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 61546 None 0 Human Functional pEC50 = 8.0 8.0 - 1
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 1932 None 74 Human Functional pEC50 = 8.0 8.0 -3 11
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 1932 None 74 Human Functional pEC50 = 8.0 8.0 -3 11
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 1932 None 74 Human Functional pEC50 = 8.0 8.0 -3 11
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 1932 None 74 Human Functional pEC50 = 8.0 8.0 -3 11
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
774.0 1932 None 74 Human Functional pEC50 = 8.0 8.0 -3 11
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 1932 None 74 Human Functional pEC50 = 8.0 8.0 -3 11
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 1932 None 74 Human Functional pEC50 = 8.0 8.0 -3 11
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 140325 None 3 Human Functional pEC50 = 8.0 8.0 10 2
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 140325 None 3 Human Functional pEC50 = 8.0 8.0 10 2
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 1932 None 74 Human Functional pEC50 = 7.9 7.9 -3 11
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 1932 None 74 Human Functional pEC50 = 7.9 7.9 -3 11
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 1932 None 74 Human Functional pEC50 = 7.9 7.9 -3 11
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 1932 None 74 Human Functional pEC50 = 7.9 7.9 -3 11
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
774.0 1932 None 74 Human Functional pEC50 = 7.9 7.9 -3 11
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 1932 None 74 Human Functional pEC50 = 7.9 7.9 -3 11
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 1932 None 74 Human Functional pEC50 = 7.9 7.9 -3 11
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 202364 None 0 Human Functional pEC50 = 7.9 7.9 - 1
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 202364 None 0 Human Functional pEC50 = 7.9 7.9 - 1
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 140329 None 0 Human Functional pEC50 = 7.0 7.0 - 1
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 140329 None 0 Human Functional pEC50 = 7.0 7.0 - 1
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 140334 None 0 Human Functional pEC50 = 6.0 6.0 3 3
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 140334 None 0 Human Functional pEC50 = 6.0 6.0 3 3
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 140402 None 0 Human Functional pEC50 = 7.0 7.0 3 2
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 140402 None 0 Human Functional pEC50 = 7.0 7.0 3 2
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 117186 None 0 Human Functional pEC50 = 7.0 7.0 - 1
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 117186 None 0 Human Functional pEC50 = 7.0 7.0 - 1
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 187439 None 0 Rat Functional pEC50 = 6.0 6.0 - 1
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium 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 187439 None 0 Rat Functional pEC50 = 6.0 6.0 - 1
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium 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 187689 None 0 Rat Functional pEC50 = 6.9 6.9 - 1
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium 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 187689 None 0 Rat Functional pEC50 = 6.9 6.9 - 1
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium 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 188509 None 25 Rat Functional pEC50 = 6.9 6.9 -2 2
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium 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 188509 None 25 Rat Functional pEC50 = 6.9 6.9 -2 2
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium 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 172716 None 0 Human Functional pEC50 = 4.9 4.9 1 2
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 172716 None 0 Human Functional pEC50 = 4.9 4.9 1 2
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 56495 None 0 Human Functional pEC50 = 4.9 4.9 -1 2
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 56495 None 0 Human Functional pEC50 = 4.9 4.9 -1 2
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 188525 None 0 Rat Functional pEC50 = 6.9 6.9 - 1
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium 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 188525 None 0 Rat Functional pEC50 = 6.9 6.9 - 1
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium 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 140402 None 0 Human Functional pEC50 = 6.9 6.9 3 2
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 140402 None 0 Human Functional pEC50 = 6.9 6.9 3 2
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 61578 None 0 Human Functional pEC50 = 7.9 7.9 - 1
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 61578 None 0 Human Functional pEC50 = 7.9 7.9 - 1
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 1932 None 74 Human Functional pEC50 = 7.9 7.9 -3 11
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 1932 None 74 Human Functional pEC50 = 7.9 7.9 -3 11
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 1932 None 74 Human Functional pEC50 = 7.9 7.9 -3 11
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 1932 None 74 Human Functional pEC50 = 7.9 7.9 -3 11
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
774.0 1932 None 74 Human Functional pEC50 = 7.9 7.9 -3 11
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 1932 None 74 Human Functional pEC50 = 7.9 7.9 -3 11
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 1932 None 74 Human Functional pEC50 = 7.9 7.9 -3 11
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 187360 None 0 Human Functional pEC50 = 7.9 7.9 15 2
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 187360 None 0 Human Functional pEC50 = 7.9 7.9 15 2
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 2010 None 25 Human Functional pEC50 = 7.9 7.9 -54 5
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 2010 None 25 Human Functional pEC50 = 7.9 7.9 -54 5
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 2010 None 25 Human Functional pEC50 = 7.9 7.9 -54 5
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 2010 None 25 Human Functional pEC50 = 7.9 7.9 -54 5
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 2010 None 25 Human Functional pEC50 = 7.9 7.9 -54 5
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 2010 None 25 Human Functional pEC50 = 7.9 7.9 -54 5
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 2010 None 25 Human Functional pEC50 = 7.9 7.9 -54 5
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 2010 None 25 Human Functional pEC50 = 7.9 7.9 -54 5
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 2058 None 4 Human Functional pEC50 = 7.9 7.9 -251 2
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 2058 None 4 Human Functional pEC50 = 7.9 7.9 -251 2
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 2058 None 4 Human Functional pEC50 = 7.9 7.9 -251 2
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 4063 None 15 Human Functional pEC50 = 7.9 7.9 -25 2
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 4063 None 15 Human Functional pEC50 = 7.9 7.9 -25 2
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 4063 None 15 Human Functional pEC50 = 7.9 7.9 -25 2
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 1932 None 74 Human Functional pEC50 = 7.9 7.9 -3 11
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 1932 None 74 Human Functional pEC50 = 7.9 7.9 -3 11
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 1932 None 74 Human Functional pEC50 = 7.9 7.9 -3 11
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 1932 None 74 Human Functional pEC50 = 7.9 7.9 -3 11
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
774.0 1932 None 74 Human Functional pEC50 = 7.9 7.9 -3 11
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 1932 None 74 Human Functional pEC50 = 7.9 7.9 -3 11
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 1932 None 74 Human Functional pEC50 = 7.9 7.9 -3 11
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 3804 None 32 Human Functional pEC50 = 6.9 6.9 -17 5
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 3804 None 32 Human Functional pEC50 = 6.9 6.9 -17 5
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 3804 None 32 Human Functional pEC50 = 6.9 6.9 -17 5
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 5734 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 5734 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 187331 None 0 Human Functional pEC50 = 5.9 5.9 3 2
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 187331 None 0 Human Functional pEC50 = 5.9 5.9 3 2
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 5638 None 0 Human Functional pEC50 = 5.9 5.9 - 1
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 5638 None 0 Human Functional pEC50 = 5.9 5.9 - 1
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 187768 None 0 Rat Functional pEC50 = 5.9 5.9 - 1
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium 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 187768 None 0 Rat Functional pEC50 = 5.9 5.9 - 1
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium 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 187693 None 1 Mouse Functional pEC50 = 6.9 6.9 4 3
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 187693 None 1 Mouse Functional pEC50 = 6.9 6.9 4 3
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 187693 None 1 Mouse Functional pEC50 = 6.9 6.9 4 3
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 187693 None 1 Mouse Functional pEC50 = 6.9 6.9 4 3
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 187509 None 0 Rat Functional pEC50 = 4.9 4.9 - 1
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium 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 187509 None 0 Rat Functional pEC50 = 4.9 4.9 - 1
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium 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 140391 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 140391 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 58909 None 0 Human Functional pEC50 = 6.9 6.9 -1 2
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 58909 None 0 Human Functional pEC50 = 6.9 6.9 -1 2
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 108633 None 0 Human Functional pEC50 = 6.9 6.9 1 2
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 108633 None 0 Human Functional pEC50 = 6.9 6.9 1 2
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 103841 None 0 Human Functional pEC50 = 5.9 5.9 - 1
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 103841 None 0 Human Functional pEC50 = 5.9 5.9 - 1
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 2082 None 7 Human Functional pEC50 = 4.9 4.9 -1258 2
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 2082 None 7 Human Functional pEC50 = 4.9 4.9 -1258 2
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 2082 None 7 Human Functional pEC50 = 4.9 4.9 -1258 2
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 56495 None 0 Human Functional pEC50 = 4.9 4.9 -1 2
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 56495 None 0 Human Functional pEC50 = 4.9 4.9 -1 2
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 109685 None 0 Human Functional pEC50 = 4.9 4.9 -1 2
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 109685 None 0 Human Functional pEC50 = 4.9 4.9 -1 2
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 5765 None 0 Human Functional pEC50 = 5.9 5.9 5 2
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 5765 None 0 Human Functional pEC50 = 5.9 5.9 5 2
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 109685 None 0 Human Functional pEC50 = 4.9 4.9 -1 2
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 109685 None 0 Human Functional pEC50 = 4.9 4.9 -1 2
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 140389 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 140389 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 1932 None 74 Human Functional pEC50 = 7.9 7.9 -3 11
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 1932 None 74 Human Functional pEC50 = 7.9 7.9 -3 11
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 1932 None 74 Human Functional pEC50 = 7.9 7.9 -3 11
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 1932 None 74 Human Functional pEC50 = 7.9 7.9 -3 11
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
774.0 1932 None 74 Human Functional pEC50 = 7.9 7.9 -3 11
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 1932 None 74 Human Functional pEC50 = 7.9 7.9 -3 11
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 1932 None 74 Human Functional pEC50 = 7.9 7.9 -3 11
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 108633 None 0 Human Functional pEC50 = 6.9 6.9 1 2
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 108633 None 0 Human Functional pEC50 = 6.9 6.9 1 2
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 187389 None 0 Rat Functional pEC50 = 5.9 5.9 - 1
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium 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 187389 None 0 Rat Functional pEC50 = 5.9 5.9 - 1
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium 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 140325 None 3 Human Functional pEC50 = 7.9 7.9 10 2
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 140325 None 3 Human Functional pEC50 = 7.9 7.9 10 2
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 78038 None 0 Human Functional pEC50 = 7.8 7.8 - 1
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 78038 None 0 Human Functional pEC50 = 7.8 7.8 - 1
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 78491 None 0 Human Functional pEC50 = 7.8 7.8 - 1
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 78491 None 0 Human Functional pEC50 = 7.8 7.8 - 1
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 189171 None 15 Rat Functional pEC50 = 7.8 7.8 1 2
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 189171 None 15 Rat Functional pEC50 = 7.8 7.8 1 2
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 5677 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 5677 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 187510 None 0 Rat Functional pEC50 = 4.9 4.9 -3 2
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium 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 187510 None 0 Rat Functional pEC50 = 4.9 4.9 -3 2
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium 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 187734 None 10 Rat Functional pEC50 = 5.8 5.8 - 1
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium 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 187734 None 10 Rat Functional pEC50 = 5.8 5.8 - 1
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium 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 140407 None 0 Human Functional pEC50 = 7.8 7.8 38 2
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 140407 None 0 Human Functional pEC50 = 7.8 7.8 38 2
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 117189 None 0 Human Functional pEC50 = 7.8 7.8 - 1
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 117189 None 0 Human Functional pEC50 = 7.8 7.8 - 1
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 187289 None 0 Rat Functional pEC50 = 7.8 7.8 - 1
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium 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 187289 None 0 Rat Functional pEC50 = 7.8 7.8 - 1
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium 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 187587 None 0 Rat Functional pEC50 = 7.8 7.8 19 2
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 187587 None 0 Rat Functional pEC50 = 7.8 7.8 19 2
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 2014 None 28 Human Functional pEC50 = 7.8 7.8 -204 2
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 2014 None 28 Human Functional pEC50 = 7.8 7.8 -204 2
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 2014 None 28 Human Functional pEC50 = 7.8 7.8 -204 2
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 2014 None 28 Human Functional pEC50 = 7.8 7.8 -204 2
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 2014 None 28 Human Functional pEC50 = 7.8 7.8 -204 2
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 2014 None 28 Human Functional pEC50 = 7.8 7.8 -204 2
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 179092 None 0 Human Functional pEC50 = 7.8 7.8 -6 3
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 179092 None 0 Human Functional pEC50 = 7.8 7.8 -6 3
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 184331 None 0 Human Functional pEC50 = 7.8 7.8 -6 3
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 184331 None 0 Human Functional pEC50 = 7.8 7.8 -6 3
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 2150 None 56 Human Functional pEC50 = 7.8 7.8 1 4
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 2150 None 56 Human Functional pEC50 = 7.8 7.8 1 4
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 2150 None 56 Human Functional pEC50 = 7.8 7.8 1 4
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 2150 None 56 Human Functional pEC50 = 7.8 7.8 1 4
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 140382 None 0 Human Functional pEC50 = 6.8 6.8 - 1
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 140382 None 0 Human Functional pEC50 = 6.8 6.8 - 1
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 6586 None 0 Human Functional pEC50 = 6.8 6.8 - 1
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 6586 None 0 Human Functional pEC50 = 6.8 6.8 - 1
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 5776 None 0 Human Functional pEC50 = 6.8 6.8 - 1
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 5776 None 0 Human Functional pEC50 = 6.8 6.8 - 1
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 58909 None 0 Human Functional pEC50 = 6.8 6.8 -1 2
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 58909 None 0 Human Functional pEC50 = 6.8 6.8 -1 2
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 176425 None 0 Rat Functional pEC50 = 6.8 6.8 -18 3
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 176425 None 0 Rat Functional pEC50 = 6.8 6.8 -18 3
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 176425 None 0 Rat Functional pEC50 = 6.8 6.8 -18 3
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 176425 None 0 Rat Functional pEC50 = 6.8 6.8 -18 3
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 1932 None 74 Rat Functional pEC50 = 6.8 6.8 -288 11
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 1932 None 74 Rat Functional pEC50 = 6.8 6.8 -288 11
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 1932 None 74 Rat Functional pEC50 = 6.8 6.8 -288 11
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 1932 None 74 Rat Functional pEC50 = 6.8 6.8 -288 11
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
774.0 1932 None 74 Rat Functional pEC50 = 6.8 6.8 -288 11
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 1932 None 74 Rat Functional pEC50 = 6.8 6.8 -288 11
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 1932 None 74 Rat Functional pEC50 = 6.8 6.8 -288 11
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 1424 None 16 Human Functional pEC50 = 5.8 5.8 - 1
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 1424 None 16 Human Functional pEC50 = 5.8 5.8 - 1
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 1424 None 16 Human Functional pEC50 = 5.8 5.8 - 1
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 1424 None 16 Human Functional pEC50 = 5.8 5.8 - 1
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 93665 None 1 Human Functional pEC50 = 5.8 5.8 -3 2
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 93665 None 1 Human Functional pEC50 = 5.8 5.8 -3 2
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 None 34 Mouse Functional pEC50 = 5.8 5.8 -35 6
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 None 34 Mouse Functional pEC50 = 5.8 5.8 -35 6
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 None 34 Mouse Functional pEC50 = 5.8 5.8 -35 6
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 61567 None 0 Human Functional pEC50 = 7.8 7.8 - 1
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 61567 None 0 Human Functional pEC50 = 7.8 7.8 - 1
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 187691 None 0 Human Functional pEC50 = 7.8 7.8 23 2
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 187691 None 0 Human Functional pEC50 = 7.8 7.8 23 2
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 1932 None 74 Human Functional pEC50 = 7.8 7.8 -3 11
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 1932 None 74 Human Functional pEC50 = 7.8 7.8 -3 11
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 1932 None 74 Human Functional pEC50 = 7.8 7.8 -3 11
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 1932 None 74 Human Functional pEC50 = 7.8 7.8 -3 11
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 1932 None 74 Human Functional pEC50 = 7.8 7.8 -3 11
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 1932 None 74 Human Functional pEC50 = 7.8 7.8 -3 11
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 1932 None 74 Human Functional pEC50 = 7.8 7.8 -3 11
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 1932 None 74 Human Functional pEC50 = 7.8 7.8 -3 11
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
774.0 1932 None 74 Human Functional pEC50 = 7.8 7.8 -3 11
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
774.0 1932 None 74 Human Functional pEC50 = 7.8 7.8 -3 11
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 1932 None 74 Human Functional pEC50 = 7.8 7.8 -3 11
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 1932 None 74 Human Functional pEC50 = 7.8 7.8 -3 11
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 1932 None 74 Human Functional pEC50 = 7.8 7.8 -3 11
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 1932 None 74 Human Functional pEC50 = 7.8 7.8 -3 11
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 5678 None 0 Human Functional pEC50 = 6.8 6.8 1 2
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 5678 None 0 Human Functional pEC50 = 6.8 6.8 1 2
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 174000 None 42 Rat Functional pEC50 = 4.8 4.8 - 1
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium 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 174000 None 42 Rat Functional pEC50 = 4.8 4.8 - 1
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium 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 188765 None 2 Mouse Functional pEC50 = 7.8 7.8 1 2
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 188765 None 2 Mouse Functional pEC50 = 7.8 7.8 1 2
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 140365 None 0 Human Functional pEC50 = 5.8 5.8 - 1
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 140365 None 0 Human Functional pEC50 = 5.8 5.8 - 1
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 193239 None 0 Rat Functional pEC50 = 6.8 6.8 - 1
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium 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 193239 None 0 Rat Functional pEC50 = 6.8 6.8 - 1
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium 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 187810 None 0 Human Functional pEC50 = 6.8 6.8 - 1
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 187810 None 0 Human Functional pEC50 = 6.8 6.8 - 1
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 187700 None 0 Rat Functional pEC50 = 6.8 6.8 - 1
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium 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 187700 None 0 Rat Functional pEC50 = 6.8 6.8 - 1
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium 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 188359 None 0 Rat Functional pEC50 = 5.8 5.8 - 1
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium 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 188359 None 0 Rat Functional pEC50 = 5.8 5.8 - 1
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium 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 176568 None 0 Human Functional pEC50 = 7.7 7.7 4 3
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 176568 None 0 Human Functional pEC50 = 7.7 7.7 4 3
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 176568 None 0 Human Functional pEC50 = 7.7 7.7 4 3
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 189171 None 15 Mouse Functional pEC50 = 7.7 7.7 -1 2
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 189171 None 15 Mouse Functional pEC50 = 7.7 7.7 -1 2
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 1932 None 74 Human Functional pEC50 = 5.8 5.8 -3 11
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 1932 None 74 Human Functional pEC50 = 5.8 5.8 -3 11
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 1932 None 74 Human Functional pEC50 = 5.8 5.8 -3 11
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 1932 None 74 Human Functional pEC50 = 5.8 5.8 -3 11
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
774.0 1932 None 74 Human Functional pEC50 = 5.8 5.8 -3 11
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 1932 None 74 Human Functional pEC50 = 5.8 5.8 -3 11
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 1932 None 74 Human Functional pEC50 = 5.8 5.8 -3 11
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 170716 None 5 Rat Functional pEC50 = 5.7 5.7 - 1
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium 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 170716 None 5 Rat Functional pEC50 = 5.7 5.7 - 1
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium 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 172716 None 0 Rat Functional pEC50 = 4.7 4.7 -1 2
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium 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 172716 None 0 Rat Functional pEC50 = 4.7 4.7 -1 2
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium 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 187482 None 0 Rat Functional pEC50 = 5.7 5.7 - 1
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium 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 187482 None 0 Rat Functional pEC50 = 5.7 5.7 - 1
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium 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 171517 None 0 Rat Functional pEC50 = 7.7 7.7 - 1
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 171517 None 0 Rat Functional pEC50 = 7.7 7.7 - 1
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 176583 None 0 Human Functional pEC50 = 7.7 7.7 -2 3
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 176583 None 0 Human Functional pEC50 = 7.7 7.7 -2 3
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 176583 None 0 Human Functional pEC50 = 7.7 7.7 -2 3
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 202360 None 0 Human Functional pEC50 = 7.7 7.7 - 1
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 202360 None 0 Human Functional pEC50 = 7.7 7.7 - 1
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 80297 None 3 Human Functional pEC50 = 7.7 7.7 -2 2
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 80297 None 3 Human Functional pEC50 = 7.7 7.7 -2 2
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 1932 None 74 Human Functional pEC50 = 7.7 7.7 -3 11
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 1932 None 74 Human Functional pEC50 = 7.7 7.7 -3 11
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 1932 None 74 Human Functional pEC50 = 7.7 7.7 -3 11
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 1932 None 74 Human Functional pEC50 = 7.7 7.7 -3 11
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
774.0 1932 None 74 Human Functional pEC50 = 7.7 7.7 -3 11
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 1932 None 74 Human Functional pEC50 = 7.7 7.7 -3 11
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 1932 None 74 Human Functional pEC50 = 7.7 7.7 -3 11
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 15502 None 19 Human Functional pEC50 = 7.7 7.7 - 1
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 15502 None 19 Human Functional pEC50 = 7.7 7.7 - 1
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 56494 None 0 Human Functional pEC50 = 7.7 7.7 -50 2
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 56494 None 0 Human Functional pEC50 = 7.7 7.7 -50 2
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 102966 None 0 Human Functional pEC50 = 7.7 7.7 - 1
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 102966 None 0 Human Functional pEC50 = 7.7 7.7 - 1
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 192826 None 0 Rat Functional pEC50 = 7.7 7.7 - 1
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 192826 None 0 Rat Functional pEC50 = 7.7 7.7 - 1
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 193218 None 0 Rat Functional pEC50 = 6.7 6.7 - 1
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium 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 193218 None 0 Rat Functional pEC50 = 6.7 6.7 - 1
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium 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 5211 None 0 Human Functional pEC50 = 6.7 6.7 47 2
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 5211 None 0 Human Functional pEC50 = 6.7 6.7 47 2
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 209439 None 25 Human Functional pEC50 = 6.7 6.7 -4 2
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 209439 None 25 Human Functional pEC50 = 6.7 6.7 -4 2
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 209439 None 25 Human Functional pEC50 = 6.7 6.7 -4 2
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 176425 None 0 Mouse Functional pEC50 = 6.7 6.7 -14 3
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 176425 None 0 Mouse Functional pEC50 = 6.7 6.7 -14 3
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 176425 None 0 Mouse Functional pEC50 = 6.7 6.7 -14 3
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 176425 None 0 Mouse Functional pEC50 = 6.7 6.7 -14 3
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 56497 None 3 Mouse Functional pEC50 = 6.7 6.7 -1 3
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 56497 None 3 Mouse Functional pEC50 = 6.7 6.7 -1 3
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 56499 None 0 Rat Functional pEC50 = 6.7 6.7 -3 3
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 56499 None 0 Rat Functional pEC50 = 6.7 6.7 -3 3
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 202510 None 0 Human Functional pEC50 = 6.7 6.7 - 1
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 202510 None 0 Human Functional pEC50 = 6.7 6.7 - 1
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 5303 None 0 Human Functional pEC50 = 5.7 5.7 -47 2
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 5303 None 0 Human Functional pEC50 = 5.7 5.7 -47 2
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 5303 None 0 Human Functional pEC50 = 5.7 5.7 -47 2
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 5303 None 0 Human Functional pEC50 = 5.7 5.7 -47 2
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 5292 None 0 Human Functional pEC50 = 4.7 4.7 - 1
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 5292 None 0 Human Functional pEC50 = 4.7 4.7 - 1
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 2150 None 56 Mouse Functional pEC50 = 8.6 8.6 -1 4
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 2150 None 56 Mouse Functional pEC50 = 8.6 8.6 -1 4
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 2150 None 56 Mouse Functional pEC50 = 8.6 8.6 -1 4
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 2150 None 56 Mouse Functional pEC50 = 8.6 8.6 -1 4
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 2150 None 56 Rat Functional pEC50 = 8.6 8.6 -1 4
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 2150 None 56 Rat Functional pEC50 = 8.6 8.6 -1 4
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 2150 None 56 Rat Functional pEC50 = 8.6 8.6 -1 4
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 2150 None 56 Rat Functional pEC50 = 8.6 8.6 -1 4
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 117196 None 0 Human Functional pEC50 = 7.7 7.7 - 1
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 117196 None 0 Human Functional pEC50 = 7.7 7.7 - 1
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 77981 None 0 Human Functional pEC50 = 7.7 7.7 - 1
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 77981 None 0 Human Functional pEC50 = 7.7 7.7 - 1
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 1932 None 74 Human Functional pEC50 = 7.7 7.7 -3 11
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 1932 None 74 Human Functional pEC50 = 7.7 7.7 -3 11
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 1932 None 74 Human Functional pEC50 = 7.7 7.7 -3 11
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 1932 None 74 Human Functional pEC50 = 7.7 7.7 -3 11
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
774.0 1932 None 74 Human Functional pEC50 = 7.7 7.7 -3 11
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 1932 None 74 Human Functional pEC50 = 7.7 7.7 -3 11
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 1932 None 74 Human Functional pEC50 = 7.7 7.7 -3 11
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 202135 None 0 Human Functional pEC50 = 7.7 7.7 - 1
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 202135 None 0 Human Functional pEC50 = 7.7 7.7 - 1
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 1932 None 74 Human Functional pEC50 = 7.7 7.7 -3 11
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 1932 None 74 Human Functional pEC50 = 7.7 7.7 -3 11
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 1932 None 74 Human Functional pEC50 = 7.7 7.7 -3 11
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 1932 None 74 Human Functional pEC50 = 7.7 7.7 -3 11
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
774.0 1932 None 74 Human Functional pEC50 = 7.7 7.7 -3 11
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 1932 None 74 Human Functional pEC50 = 7.7 7.7 -3 11
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 1932 None 74 Human Functional pEC50 = 7.7 7.7 -3 11
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 140294 None 0 Human Functional pEC50 = 6.7 6.7 4 2
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 140294 None 0 Human Functional pEC50 = 6.7 6.7 4 2
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 187388 None 0 Rat Functional pEC50 = 5.7 5.7 - 1
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium 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 187388 None 0 Rat Functional pEC50 = 5.7 5.7 - 1
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium 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 140287 None 0 Human Functional pEC50 = 6.7 6.7 4 3
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 140287 None 0 Human Functional pEC50 = 6.7 6.7 4 3
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 187285 None 0 Rat Functional pEC50 = 6.7 6.7 - 1
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium 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 187285 None 0 Rat Functional pEC50 = 6.7 6.7 - 1
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium 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 187360 None 0 Human Functional pEC50 = 7.7 7.7 15 2
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 187360 None 0 Human Functional pEC50 = 7.7 7.7 15 2
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 5292 None 0 Human Functional pEC50 = 4.7 4.7 - 1
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 5292 None 0 Human Functional pEC50 = 4.7 4.7 - 1
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 2348 None 42 Human Functional pEC50 = 6.7 6.7 -18 33
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 2348 None 42 Human Functional pEC50 = 6.7 6.7 -18 33
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 2348 None 42 Human Functional pEC50 = 6.7 6.7 -18 33
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
3964.0 2348 None 42 Human Functional pEC50 = 6.7 6.7 -18 33
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 2348 None 42 Human Functional pEC50 = 6.7 6.7 -18 33
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 2348 None 42 Human Functional pEC50 = 6.7 6.7 -18 33
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 179456 None 6 Rat Functional pEC50 = 6.7 6.7 - 1
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium 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 179456 None 6 Rat Functional pEC50 = 6.7 6.7 - 1
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium 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 187452 None 0 Rat Functional pEC50 = 6.7 6.7 - 1
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium 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 187452 None 0 Rat Functional pEC50 = 6.7 6.7 - 1
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium 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 953 None 33 Human Functional pEC50 = 7.7 7.7 -21 4
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 953 None 33 Human Functional pEC50 = 7.7 7.7 -21 4
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 953 None 33 Human Functional pEC50 = 7.7 7.7 -21 4
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 176346 None 0 Rat Functional pEC50 = 7.6 7.6 -1 3
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 176346 None 0 Rat Functional pEC50 = 7.6 7.6 -1 3
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 176346 None 0 Rat Functional pEC50 = 7.6 7.6 -1 3
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 5211 None 0 Human Functional pEC50 = 6.7 6.7 47 2
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 5211 None 0 Human Functional pEC50 = 6.7 6.7 47 2
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 187288 None 4 Rat Functional pEC50 = 6.6 6.6 - 1
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium 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 187288 None 4 Rat Functional pEC50 = 6.6 6.6 - 1
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium 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 193303 None 0 Rat Functional pEC50 = 5.6 5.6 - 1
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium 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 193303 None 0 Rat Functional pEC50 = 5.6 5.6 - 1
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium 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 172115 None 0 Rat Functional pEC50 = 4.6 4.6 - 1
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium 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 172115 None 0 Rat Functional pEC50 = 4.6 4.6 - 1
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium 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 187460 None 0 Rat Functional pEC50 = 7.6 7.6 - 1
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 187460 None 0 Rat Functional pEC50 = 7.6 7.6 - 1
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 140281 None 0 Human Functional pEC50 = 6.6 6.6 - 1
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 140281 None 0 Human Functional pEC50 = 6.6 6.6 - 1
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 187767 None 0 Rat Functional pEC50 = 6.6 6.6 - 1
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium 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 187767 None 0 Rat Functional pEC50 = 6.6 6.6 - 1
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium 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 192832 None 0 Rat Functional pEC50 = 6.6 6.6 - 1
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium 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 192832 None 0 Rat Functional pEC50 = 6.6 6.6 - 1
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium 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 187456 None 0 Human Functional pEC50 = 5.6 5.6 - 1
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 187456 None 0 Human Functional pEC50 = 5.6 5.6 - 1
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 187695 None 1 Rat Functional pEC50 = 4.6 4.6 - 1
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium 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 187695 None 1 Rat Functional pEC50 = 4.6 4.6 - 1
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium 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 172701 None 0 Rat Functional pEC50 = 5.6 5.6 - 1
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium 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 172701 None 0 Rat Functional pEC50 = 5.6 5.6 - 1
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium 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 8093 None 1 Human Functional pEC50 = 4.6 4.6 -89 2
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 8093 None 1 Human Functional pEC50 = 4.6 4.6 -89 2
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 140396 None 0 Human Functional pEC50 = 6.6 6.6 6 2
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 140396 None 0 Human Functional pEC50 = 6.6 6.6 6 2
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 109535 None 0 Human Functional pEC50 = 6.6 6.6 - 1
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 109535 None 0 Human Functional pEC50 = 6.6 6.6 - 1
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 187732 None 0 Rat Functional pEC50 = 6.6 6.6 -2 2
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium 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 187732 None 0 Rat Functional pEC50 = 6.6 6.6 -2 2
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium 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 188924 None 0 Rat Functional pEC50 = 6.6 6.6 - 1
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium 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 188924 None 0 Rat Functional pEC50 = 6.6 6.6 - 1
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium 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 187732 None 0 Rat Functional pEC50 = 6.6 6.6 -2 2
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 187732 None 0 Rat Functional pEC50 = 6.6 6.6 -2 2
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 115981 None 0 Human Functional pEC50 = 7.6 7.6 - 1
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 115981 None 0 Human Functional pEC50 = 7.6 7.6 - 1
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 1932 None 74 Human Functional pEC50 = 7.6 7.6 -3 11
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 1932 None 74 Human Functional pEC50 = 7.6 7.6 -3 11
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 1932 None 74 Human Functional pEC50 = 7.6 7.6 -3 11
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 1932 None 74 Human Functional pEC50 = 7.6 7.6 -3 11
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
774.0 1932 None 74 Human Functional pEC50 = 7.6 7.6 -3 11
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 1932 None 74 Human Functional pEC50 = 7.6 7.6 -3 11
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 1932 None 74 Human Functional pEC50 = 7.6 7.6 -3 11
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 2019 None 19 Human Functional pEC50 = 7.6 7.6 - 1
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 2019 None 19 Human Functional pEC50 = 7.6 7.6 - 1
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 2019 None 19 Human Functional pEC50 = 7.6 7.6 - 1
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 187694 None 1 Rat Functional pEC50 = 6.6 6.6 - 1
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium 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 187694 None 1 Rat Functional pEC50 = 6.6 6.6 - 1
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium 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 172559 None 0 Human Functional pEC50 = 5.6 5.6 3 2
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 172559 None 0 Human Functional pEC50 = 5.6 5.6 3 2
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 None 34 Rat Functional pEC50 = 5.6 5.6 -56 6
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 None 34 Rat Functional pEC50 = 5.6 5.6 -56 6
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 None 34 Rat Functional pEC50 = 5.6 5.6 -56 6
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 5675 None 0 Human Functional pEC50 = 5.6 5.6 - 1
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 5675 None 0 Human Functional pEC50 = 5.6 5.6 - 1
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 188979 None 5 Human Functional pEC50 = 7.6 7.6 3 2
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 188979 None 5 Human Functional pEC50 = 7.6 7.6 3 2
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 140398 None 0 Human Functional pEC50 = 5.6 5.6 - 1
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 140398 None 0 Human Functional pEC50 = 5.6 5.6 - 1
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 202399 None 0 Human Functional pEC50 = 6.6 6.6 - 1
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 202399 None 0 Human Functional pEC50 = 6.6 6.6 - 1
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 187293 None 0 Rat Functional pEC50 = 6.6 6.6 - 1
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium 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 187293 None 0 Rat Functional pEC50 = 6.6 6.6 - 1
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium 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 207632 None 0 Human Functional pEC50 = 7.6 7.6 - 1
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 207632 None 0 Human Functional pEC50 = 7.6 7.6 - 1
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 176346 None 0 Human Functional pEC50 = 7.5 7.5 1 3
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 176346 None 0 Human Functional pEC50 = 7.5 7.5 1 3
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 176346 None 0 Human Functional pEC50 = 7.5 7.5 1 3
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 140389 None 0 Human Functional pEC50 = 6.5 6.5 - 1
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 140389 None 0 Human Functional pEC50 = 6.5 6.5 - 1
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 1932 None 74 Rat Functional pEC50 = 6.5 6.5 -288 11
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 1932 None 74 Rat Functional pEC50 = 6.5 6.5 -288 11
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 1932 None 74 Rat Functional pEC50 = 6.5 6.5 -288 11
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 1932 None 74 Rat Functional pEC50 = 6.5 6.5 -288 11
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
774.0 1932 None 74 Rat Functional pEC50 = 6.5 6.5 -288 11
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 1932 None 74 Rat Functional pEC50 = 6.5 6.5 -288 11
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 1932 None 74 Rat Functional pEC50 = 6.5 6.5 -288 11
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 187587 None 0 Human Functional pEC50 = 6.5 6.5 -19 2
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 187587 None 0 Human Functional pEC50 = 6.5 6.5 -19 2
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 176600 None 5 Human Functional pEC50 = 8.5 8.5 -31 4
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 176600 None 5 Human Functional pEC50 = 8.5 8.5 -31 4
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 176600 None 5 Human Functional pEC50 = 8.5 8.5 -31 4
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 6912 None 0 Human Functional pEC50 = 8.5 8.5 - 1
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 6912 None 0 Human Functional pEC50 = 8.5 8.5 - 1
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 7318 None 0 Human Functional pEC50 = 8.5 8.5 3 4
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 7318 None 0 Human Functional pEC50 = 8.5 8.5 3 4
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 176613 None 0 Human Functional pEC50 = 8.5 8.5 1 3
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 176613 None 0 Human Functional pEC50 = 8.5 8.5 1 3
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 176613 None 0 Human Functional pEC50 = 8.5 8.5 1 3
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 188765 None 2 Rat Functional pEC50 = 7.5 7.5 -1 2
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 188765 None 2 Rat Functional pEC50 = 7.5 7.5 -1 2
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 185336 None 0 Rat Functional pEC50 = 5.5 5.5 - 1
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium 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 185336 None 0 Rat Functional pEC50 = 5.5 5.5 - 1
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium 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 117249 None 9 Human Functional pEC50 = 6.5 6.5 - 1
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 117249 None 9 Human Functional pEC50 = 6.5 6.5 - 1
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 3804 None 32 Mouse Functional pEC50 = 6.5 6.5 -8 5
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 3804 None 32 Mouse Functional pEC50 = 6.5 6.5 -8 5
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 3804 None 32 Mouse Functional pEC50 = 6.5 6.5 -8 5
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 187818 None 0 Rat Functional pEC50 = 6.5 6.5 - 1
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium 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 187818 None 0 Rat Functional pEC50 = 6.5 6.5 - 1
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium 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 5364 None 1 Human Functional pEC50 = 4.5 4.5 -309 2
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 5364 None 1 Human Functional pEC50 = 4.5 4.5 -309 2
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 202254 None 0 Human Functional pEC50 = 7.5 7.5 - 1
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 202254 None 0 Human Functional pEC50 = 7.5 7.5 - 1
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 2009 None 10 Human Functional pEC50 = 7.5 7.5 -18 2
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 2009 None 10 Human Functional pEC50 = 7.5 7.5 -18 2
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 2009 None 10 Human Functional pEC50 = 7.5 7.5 -18 2
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 None 34 Human Functional pEC50 = 7.5 7.5 35 6
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 None 34 Human Functional pEC50 = 7.5 7.5 35 6
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 None 34 Human Functional pEC50 = 7.5 7.5 35 6
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 187292 None 0 Rat Functional pEC50 = 7.5 7.5 - 1
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium 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 187292 None 0 Rat Functional pEC50 = 7.5 7.5 - 1
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium 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 193212 None 0 Rat Functional pEC50 = 6.5 6.5 - 1
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium 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 193212 None 0 Rat Functional pEC50 = 6.5 6.5 - 1
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium 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 117200 None 0 Human Functional pEC50 = 5.5 5.5 - 1
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 117200 None 0 Human Functional pEC50 = 5.5 5.5 - 1
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 115982 None 0 Human Functional pEC50 = 5.5 5.5 - 1
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 115982 None 0 Human Functional pEC50 = 5.5 5.5 - 1
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 117197 None 0 Human Functional pEC50 = 5.5 5.5 - 1
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 117197 None 0 Human Functional pEC50 = 5.5 5.5 - 1
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 5364 None 1 Human Functional pEC50 = 4.5 4.5 -309 2
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 5364 None 1 Human Functional pEC50 = 4.5 4.5 -309 2
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 193368 None 0 Rat Functional pEC50 = 5.5 5.5 - 1
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium 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 193368 None 0 Rat Functional pEC50 = 5.5 5.5 - 1
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium 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 187486 None 0 Human Functional pEC50 = 7.5 7.5 1 2
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 187486 None 0 Human Functional pEC50 = 7.5 7.5 1 2
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 5778 None 7 Human Functional pEC50 = 7.5 7.5 20 2
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 5778 None 7 Human Functional pEC50 = 7.5 7.5 20 2
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 6587 None 0 Human Functional pEC50 = 6.5 6.5 - 1
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 6587 None 0 Human Functional pEC50 = 6.5 6.5 - 1
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 5632 None 0 Human Functional pEC50 = 6.5 6.5 - 1
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 5632 None 0 Human Functional pEC50 = 6.5 6.5 - 1
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 180872 None 0 Rat Functional pEC50 = 5.5 5.5 -2089 6
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 180872 None 0 Rat Functional pEC50 = 5.5 5.5 -2089 6
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 82112 None 0 Human Functional pEC50 = 6.5 6.5 -13 2
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 82112 None 0 Human Functional pEC50 = 6.5 6.5 -13 2
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 170290 None 0 Rat Functional pEC50 = 6.5 6.5 - 1
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium 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 170290 None 0 Rat Functional pEC50 = 6.5 6.5 - 1
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium 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 4064 None 14 Rat Functional pEC50 = 4.5 4.5 -776 4
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 4064 None 14 Rat Functional pEC50 = 4.5 4.5 -776 4
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 4064 None 14 Rat Functional pEC50 = 4.5 4.5 -776 4
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 176772 None 0 Human Functional pEC50 = 7.5 7.5 -3 3
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 176772 None 0 Human Functional pEC50 = 7.5 7.5 -3 3
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 176772 None 0 Human Functional pEC50 = 7.5 7.5 -3 3
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 176583 None 0 Mouse Functional pEC50 = 7.5 7.5 -8 3
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 176583 None 0 Mouse Functional pEC50 = 7.5 7.5 -8 3
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 176583 None 0 Mouse Functional pEC50 = 7.5 7.5 -8 3
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 187357 None 0 Rat Functional pEC50 = 6.5 6.5 - 1
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium 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 187357 None 0 Rat Functional pEC50 = 6.5 6.5 - 1
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium 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 187487 None 0 Rat Functional pEC50 = 6.4 6.4 - 1
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium 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 187487 None 0 Rat Functional pEC50 = 6.4 6.4 - 1
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium 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 109534 None 0 Human Functional pEC50 = 5.4 5.4 -3 2
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 109534 None 0 Human Functional pEC50 = 5.4 5.4 -3 2
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 187358 None 0 Rat Functional pEC50 = 5.4 5.4 - 1
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium 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 187358 None 0 Rat Functional pEC50 = 5.4 5.4 - 1
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium 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 187670 None 0 Rat Functional pEC50 = 5.4 5.4 - 1
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium 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 187670 None 0 Rat Functional pEC50 = 5.4 5.4 - 1
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium 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 5778 None 7 Human Functional pEC50 = 7.4 7.4 20 2
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 5778 None 7 Human Functional pEC50 = 7.4 7.4 20 2
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 5778 None 7 Human Functional pEC50 = 7.4 7.4 20 2
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 5778 None 7 Human Functional pEC50 = 7.4 7.4 20 2
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 187520 None 0 Rat Functional pEC50 = 7.4 7.4 - 1
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium 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 187520 None 0 Rat Functional pEC50 = 7.4 7.4 - 1
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium 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 202323 None 0 Human Functional pEC50 = 7.4 7.4 - 1
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 202323 None 0 Human Functional pEC50 = 7.4 7.4 - 1
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 140353 None 0 Human Functional pEC50 = 6.4 6.4 - 1
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 140353 None 0 Human Functional pEC50 = 6.4 6.4 - 1
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 4064 None 14 Human Functional pEC50 = 7.4 7.4 7 4
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 4064 None 14 Human Functional pEC50 = 7.4 7.4 7 4
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 4064 None 14 Human Functional pEC50 = 7.4 7.4 7 4
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 142019 None 0 Human Functional pEC50 = 7.4 7.4 - 1
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 142019 None 0 Human Functional pEC50 = 7.4 7.4 - 1
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 187691 None 0 Rat Functional pEC50 = 6.4 6.4 -23 2
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium 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 187691 None 0 Rat Functional pEC50 = 6.4 6.4 -23 2
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium 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 187510 None 0 Human Functional pEC50 = 5.4 5.4 3 2
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 187510 None 0 Human Functional pEC50 = 5.4 5.4 3 2
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 6606 None 0 Mouse Functional pEC50 = 7.4 7.4 -263 3
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 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 6606 None 0 Mouse Functional pEC50 = 7.4 7.4 -263 3
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 9 3 4 4.3 Cc1cc(OCCCNCCc2c[nH]cn2)ccc1-c1nc2c(C)c(F)ccc2[nH]1 10.1016/j.bmcl.2010.04.017
1269 121 None 34 Human Functional pEC50 = 7.4 7.4 35 6
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 0.2 Cc1c(CCN)nc[nH]1 10.1016/j.bmcl.2010.10.041
37463 121 None 34 Human Functional pEC50 = 7.4 7.4 35 6
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 0.2 Cc1c(CCN)nc[nH]1 10.1016/j.bmcl.2010.10.041
CHEMBL275443 121 None 34 Human Functional pEC50 = 7.4 7.4 35 6
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 0.2 Cc1c(CCN)nc[nH]1 10.1016/j.bmcl.2010.10.041
136030655 56498 None 0 Human Functional pEC50 = 7.4 7.4 -3 3
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 292 1 2 3 2.2 CN1CCN(/C(=N\O)c2cc3cc(Cl)ccc3[nH]2)CC1 10.1016/j.bmcl.2010.10.041
CHEMBL1632413 56498 None 0 Human Functional pEC50 = 7.4 7.4 -3 3
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 292 1 2 3 2.2 CN1CCN(/C(=N\O)c2cc3cc(Cl)ccc3[nH]2)CC1 10.1016/j.bmcl.2010.10.041
25129523 187393 None 38 Rat Functional pEC50 = 7.4 7.4 - 1
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium 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 269 2 1 5 1.5 CN1CCN(c2cc(-c3ccccc3)nc(N)n2)CC1 10.1021/jm8005959
CHEMBL492884 187393 None 38 Rat Functional pEC50 = 7.4 7.4 - 1
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium 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 269 2 1 5 1.5 CN1CCN(c2cc(-c3ccccc3)nc(N)n2)CC1 10.1021/jm8005959
25129523 187393 None 38 Rat Functional pEC50 = 7.4 7.4 - 1
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 269 2 1 5 1.5 CN1CCN(c2cc(-c3ccccc3)nc(N)n2)CC1 10.1021/jm800670r
CHEMBL492884 187393 None 38 Rat Functional pEC50 = 7.4 7.4 - 1
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 269 2 1 5 1.5 CN1CCN(c2cc(-c3ccccc3)nc(N)n2)CC1 10.1021/jm800670r
70692530 75718 None 0 Human Functional pEC50 = 6.4 6.4 - 1
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 322 2 1 4 2.1 CN1CCN(C(=O)c2cc3cc(Cl)cc([N+](=O)[O-])c3[nH]2)CC1 10.1021/acs.jmedchem.8b00435
CHEMBL2047474 75718 None 0 Human Functional pEC50 = 6.4 6.4 - 1
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 322 2 1 4 2.1 CN1CCN(C(=O)c2cc3cc(Cl)cc([N+](=O)[O-])c3[nH]2)CC1 10.1021/acs.jmedchem.8b00435
91613 17994 None 20 Human Functional pEC50 = 5.4 5.4 -5 2
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 Cc1ncc(CCN)[nH]1 10.1016/j.bmcl.2010.10.041
CHEMBL12620 17994 None 20 Human Functional pEC50 = 5.4 5.4 -5 2
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 Cc1ncc(CCN)[nH]1 10.1016/j.bmcl.2010.10.041
58227326 117192 None 0 Human Functional pEC50 = 8.4 8.4 - 1
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 6 2 5 1.5 CCCCNc1nccc(N2CC[C@@H](NC)C2)n1 10.1016/j.bmcl.2014.12.027
CHEMBL3393542 117192 None 0 Human Functional pEC50 = 8.4 8.4 - 1
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 6 2 5 1.5 CCCCNc1nccc(N2CC[C@@H](NC)C2)n1 10.1016/j.bmcl.2014.12.027
58227373 176613 None 0 Mouse Functional pEC50 = 8.4 8.4 -3 3
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 249 3 2 5 1.5 CC(C)(C)CNc1nccc(N2CC[C@@H](N)C2)n1 10.1021/acs.jmedchem.9b01342
CHEMBL4455324 176613 None 0 Mouse Functional pEC50 = 8.4 8.4 -3 3
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 249 3 2 5 1.5 CC(C)(C)CNc1nccc(N2CC[C@@H](N)C2)n1 10.1021/acs.jmedchem.9b01342
CHEMBL4596881 176613 None 0 Mouse Functional pEC50 = 8.4 8.4 -3 3
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 249 3 2 5 1.5 CC(C)(C)CNc1nccc(N2CC[C@@H](N)C2)n1 10.1021/acs.jmedchem.9b01342
25071004 192827 None 0 Mouse Functional pEC50 = 8.4 8.4 1 2
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 309 2 2 5 2.0 CN[C@@H]1CCN(c2nc(N)nc3c2CCCc2ccccc2-3)C1 10.1021/jm800670r
CHEMBL521996 192827 None 0 Mouse Functional pEC50 = 8.4 8.4 1 2
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 309 2 2 5 2.0 CN[C@@H]1CCN(c2nc(N)nc3c2CCCc2ccccc2-3)C1 10.1021/jm800670r
42625303 180872 None 0 Human Functional pEC50 = 8.4 8.4 -2 6
Agonist activity at human H4R by [35S]-GTPgammaS-binding assayAgonist activity at human 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 180872 None 0 Human Functional pEC50 = 8.4 8.4 -2 6
Agonist activity at human H4R by [35S]-GTPgammaS-binding assayAgonist activity at human 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
25128824 193287 None 0 Mouse Functional pEC50 = 8.3 8.3 1 2
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 313 1 2 5 1.8 Nc1nc2c(c(N3CCNCC3)n1)CCCc1ccc(F)cc1-2 10.1021/jm800670r
CHEMBL523225 193287 None 0 Mouse Functional pEC50 = 8.3 8.3 1 2
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 313 1 2 5 1.8 Nc1nc2c(c(N3CCNCC3)n1)CCCc1ccc(F)cc1-2 10.1021/jm800670r
10702196 108624 None 1 Human Functional pEC50 = 4.4 4.4 -1 2
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
CHEMBL320279 108624 None 1 Human Functional pEC50 = 4.4 4.4 -1 2
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
56954320 82110 None 0 Human Functional pEC50 = 7.4 7.4 -10 3
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 472 15 6 4 0.9 N/C(=N\C(=O)CCCCCCC(=O)/N=C(\N)NCCCc1c[nH]cn1)NCCCc1c[nH]cn1 10.1021/jm201128q
CHEMBL2165641 82110 None 0 Human Functional pEC50 = 7.4 7.4 -10 3
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 472 15 6 4 0.9 N/C(=N\C(=O)CCCCCCC(=O)/N=C(\N)NCCCc1c[nH]cn1)NCCCc1c[nH]cn1 10.1021/jm201128q
1267 3804 None 32 Human Functional pEC50 = 6.4 6.4 -17 5
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 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1016/j.bmcl.2015.12.035
3035905 3804 None 32 Human Functional pEC50 = 6.4 6.4 -17 5
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 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1016/j.bmcl.2015.12.035
CHEMBL260374 3804 None 32 Human Functional pEC50 = 6.4 6.4 -17 5
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 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1016/j.bmcl.2015.12.035
25129524 187290 None 0 Rat Functional pEC50 = 7.4 7.4 - 1
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium 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 Cc1cccc(-c2cc(N3CCN(C)CC3)nc(N)n2)c1 10.1021/jm8005959
CHEMBL492274 187290 None 0 Rat Functional pEC50 = 7.4 7.4 - 1
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium 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 Cc1cccc(-c2cc(N3CCN(C)CC3)nc(N)n2)c1 10.1021/jm8005959
25130909 187486 None 0 Rat Functional pEC50 = 7.4 7.4 -1 2
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium 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(c2nc(N)ncc2N)CC1 10.1021/jm8005959
CHEMBL493478 187486 None 0 Rat Functional pEC50 = 7.4 7.4 -1 2
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium 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(c2nc(N)ncc2N)CC1 10.1021/jm8005959
1278 2150 None 56 Rat Functional pEC50 = 7.4 7.4 -1 4
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein by GTPgammaS assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein by GTPgammaS assay
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/jm8005959
1279 2150 None 56 Rat Functional pEC50 = 7.4 7.4 -1 4
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein by GTPgammaS assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein by GTPgammaS assay
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/jm8005959
4908365 2150 None 56 Rat Functional pEC50 = 7.4 7.4 -1 4
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein by GTPgammaS assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein by GTPgammaS assay
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/jm8005959
CHEMBL129198 2150 None 56 Rat Functional pEC50 = 7.4 7.4 -1 4
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein by GTPgammaS assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein by GTPgammaS assay
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/jm8005959
25128833 188509 None 25 Human Functional pEC50 = 7.4 7.4 2 2
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 193 1 1 5 -0.2 CN1CCN(c2ccnc(N)n2)CC1 10.1021/jm8005959
CHEMBL501882 188509 None 25 Human Functional pEC50 = 7.4 7.4 2 2
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 193 1 1 5 -0.2 CN1CCN(c2ccnc(N)n2)CC1 10.1021/jm8005959
25129526 187519 None 0 Rat Functional pEC50 = 7.4 7.4 - 1
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium 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 COc1ccccc1-c1cc(N2CCN(C)CC2)nc(N)n1 10.1021/jm8005959
CHEMBL493719 187519 None 0 Rat Functional pEC50 = 7.4 7.4 - 1
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium 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 COc1ccccc1-c1cc(N2CCN(C)CC2)nc(N)n1 10.1021/jm8005959
24797248 202322 None 0 Human Functional pEC50 = 7.4 7.4 - 1
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 324 2 1 6 1.4 CN1CCN(c2cc(N3CCc4ccccc4C3)nc(N)n2)CC1 10.1016/j.bmc.2009.08.059
CHEMBL594490 202322 None 0 Human Functional pEC50 = 7.4 7.4 - 1
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 324 2 1 6 1.4 CN1CCN(c2cc(N3CCc4ccccc4C3)nc(N)n2)CC1 10.1016/j.bmc.2009.08.059
127050434 140337 None 0 Human Functional pEC50 = 7.4 7.4 3 2
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 160 3 4 3 0.2 CC(=N)SCCNC(=N)N 10.1021/acs.jmedchem.6b00120
CHEMBL3805514 140337 None 0 Human Functional pEC50 = 7.4 7.4 3 2
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 160 3 4 3 0.2 CC(=N)SCCNC(=N)N 10.1021/acs.jmedchem.6b00120
25129169 187287 None 0 Mouse Functional pEC50 = 7.3 7.3 1 2
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 323 2 2 5 2.3 Nc1nc2c(c(N3CCNCC3)n1)CCCCC2c1ccccc1 10.1021/jm800670r
CHEMBL492231 187287 None 0 Mouse Functional pEC50 = 7.3 7.3 1 2
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 323 2 2 5 2.3 Nc1nc2c(c(N3CCNCC3)n1)CCCCC2c1ccccc1 10.1021/jm800670r
24798595 170479 None 0 Rat Functional pEC50 = 7.3 7.3 - 1
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium 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 276 2 1 6 0.8 CN1CCN(c2cc(N3CCCCC3)nc(N)n2)CC1 10.1021/jm8005959
CHEMBL444782 170479 None 0 Rat Functional pEC50 = 7.3 7.3 - 1
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium 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 276 2 1 6 0.8 CN1CCN(c2cc(N3CCCCC3)nc(N)n2)CC1 10.1021/jm8005959
90667239 109533 None 0 Human Functional pEC50 = 6.3 6.3 - 1
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 8 3 4 2.5 Cc1nc(CCCN/C(=N\C#N)NCCSc2ccccc2)c[nH]1 10.1039/C3MD00245D
CHEMBL3220640 109533 None 0 Human Functional pEC50 = 6.3 6.3 - 1
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 8 3 4 2.5 Cc1nc(CCCN/C(=N\C#N)NCCSc2ccccc2)c[nH]1 10.1039/C3MD00245D
25130573 186991 None 1 Rat Functional pEC50 = 5.3 5.3 - 1
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium 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 249 1 1 5 1.1 CN1CCN(c2cc(N)nc(C(C)(C)C)n2)CC1 10.1021/jm8005959
CHEMBL489663 186991 None 1 Rat Functional pEC50 = 5.3 5.3 - 1
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium 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 249 1 1 5 1.1 CN1CCN(c2cc(N)nc(C(C)(C)C)n2)CC1 10.1021/jm8005959
25130581 187331 None 0 Rat Functional pEC50 = 5.3 5.3 -3 2
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium 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 2 0 5 1.5 COc1nc(N2CCN(C)CC2)cc(C(C)(C)C)n1 10.1021/jm8005959
CHEMBL492489 187331 None 0 Rat Functional pEC50 = 5.3 5.3 -3 2
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium 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 2 0 5 1.5 COc1nc(N2CCN(C)CC2)cc(C(C)(C)C)n1 10.1021/jm8005959
25130235 187693 None 1 Rat Functional pEC50 = 5.3 5.3 -4 3
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein by GTPgammaS assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein by GTPgammaS assay
ChEMBL 294 2 1 6 1.3 CN1CCN(c2cc(-c3ccc(C#N)cc3)nc(N)n2)CC1 10.1021/jm8005959
CHEMBL494678 187693 None 1 Rat Functional pEC50 = 5.3 5.3 -4 3
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein by GTPgammaS assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein by GTPgammaS assay
ChEMBL 294 2 1 6 1.3 CN1CCN(c2cc(-c3ccc(C#N)cc3)nc(N)n2)CC1 10.1021/jm8005959
46890546 6517 None 0 Human Functional pEC50 = 6.3 6.3 - 1
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 382 6 2 4 3.8 Cc1cc(OCCCN2CCC(N)C2)ccc1-c1nc2c(C)c(F)ccc2[nH]1 10.1016/j.bmcl.2010.04.017
CHEMBL1082771 6517 None 0 Human Functional pEC50 = 6.3 6.3 - 1
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 382 6 2 4 3.8 Cc1cc(OCCCN2CCC(N)C2)ccc1-c1nc2c(C)c(F)ccc2[nH]1 10.1016/j.bmcl.2010.04.017
46228143 202539 None 0 Human Functional pEC50 = 6.3 6.3 - 1
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 343 5 2 8 1.3 CN1CCN(c2cc(NCc3cccc([N+](=O)[O-])c3)nc(N)n2)CC1 10.1016/j.bmc.2009.08.059
CHEMBL595880 202539 None 0 Human Functional pEC50 = 6.3 6.3 - 1
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 343 5 2 8 1.3 CN1CCN(c2cc(NCc3cccc([N+](=O)[O-])c3)nc(N)n2)CC1 10.1016/j.bmc.2009.08.059
117724523 117179 None 0 Human Functional pEC50 = 7.3 7.3 - 1
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 248 6 2 4 2.1 CCCCNc1cc(N2CC[C@@H](NC)C2)ccn1 10.1016/j.bmcl.2014.12.027
CHEMBL3393529 117179 None 0 Human Functional pEC50 = 7.3 7.3 - 1
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 248 6 2 4 2.1 CCCCNc1cc(N2CC[C@@H](NC)C2)ccn1 10.1016/j.bmcl.2014.12.027
25130914 187360 None 0 Rat Functional pEC50 = 6.3 6.3 -15 2
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium 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 298 4 2 6 1.4 CN1CCN(c2cc(NCc3ccccc3)nc(N)n2)CC1 10.1021/jm8005959
CHEMBL492677 187360 None 0 Rat Functional pEC50 = 6.3 6.3 -15 2
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium 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 298 4 2 6 1.4 CN1CCN(c2cc(NCc3ccccc3)nc(N)n2)CC1 10.1021/jm8005959
25129179 187774 None 1 Rat Functional pEC50 = 6.3 6.3 - 1
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium 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 222 2 2 6 -0.1 CNc1cc(N2CCN(C)CC2)nc(N)n1 10.1021/jm8005959
CHEMBL495112 187774 None 1 Rat Functional pEC50 = 6.3 6.3 - 1
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium 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 222 2 2 6 -0.1 CNc1cc(N2CCN(C)CC2)nc(N)n1 10.1021/jm8005959
25130236 187807 None 0 Human Functional pEC50 = 5.3 5.3 1 2
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 268 1 0 4 2.2 CN1CCN(c2cc(C(C)(C)C)nc(Cl)n2)CC1 10.1021/jm8005959
CHEMBL495265 187807 None 0 Human Functional pEC50 = 5.3 5.3 1 2
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 268 1 0 4 2.2 CN1CCN(c2cc(C(C)(C)C)nc(Cl)n2)CC1 10.1021/jm8005959
25068753 188545 None 19 Mouse Functional pEC50 = 8.2 8.2 1 2
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 1.8 Nc1nc2c(c(N3CC[C@@H](N)C3)n1)CCCc1ccccc1-2 10.1021/jm800670r
CHEMBL502347 188545 None 19 Mouse Functional pEC50 = 8.2 8.2 1 2
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 1.8 Nc1nc2c(c(N3CC[C@@H](N)C3)n1)CCCc1ccccc1-2 10.1021/jm800670r
53233805 61544 None 0 Human Functional pEC50 = 7.3 7.3 - 1
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 263 4 2 5 1.5 CC(C)CNc1cc(N2CCN(C)CC2)cc(N)n1 10.1016/j.bmcl.2011.03.017
CHEMBL1770964 61544 None 0 Human Functional pEC50 = 7.3 7.3 - 1
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 263 4 2 5 1.5 CC(C)CNc1cc(N2CCN(C)CC2)cc(N)n1 10.1016/j.bmcl.2011.03.017
46890545 7387 None 0 Human Functional pEC50 = 7.3 7.3 - 1
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 1 4 4.0 Cc1cc(OCCCN2CCN(C)CC2)ccc1-c1nc2c(C)c(F)ccc2[nH]1 10.1016/j.bmcl.2010.04.017
CHEMBL1086460 7387 None 0 Human Functional pEC50 = 7.3 7.3 - 1
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 1 4 4.0 Cc1cc(OCCCN2CCN(C)CC2)ccc1-c1nc2c(C)c(F)ccc2[nH]1 10.1016/j.bmcl.2010.04.017
1274 4064 None 14 Human Functional pEC50 = 7.3 7.3 7 4
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 3 4 3 -1.1 NC(=N)SCCN=C(N)N 10.1016/j.bmcl.2010.10.041
3063228 4064 None 14 Human Functional pEC50 = 7.3 7.3 7 4
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 3 4 3 -1.1 NC(=N)SCCN=C(N)N 10.1016/j.bmcl.2010.10.041
CHEMBL1196470 4064 None 14 Human Functional pEC50 = 7.3 7.3 7 4
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 3 4 3 -1.1 NC(=N)SCCN=C(N)N 10.1016/j.bmcl.2010.10.041
1274 4064 None 14 Human Functional pEC50 = 7.3 7.3 7 4
Agonist activity at human histamine H4 receptor in SK-N-MC cells assessed as inhibition of forskolin-induced cAMP-mediated CRE-beta galactosidase activityAgonist activity at human histamine H4 receptor in SK-N-MC cells assessed as inhibition of forskolin-induced cAMP-mediated CRE-beta galactosidase activity
ChEMBL 161 3 4 3 -1.1 NC(=N)SCCN=C(N)N 10.1021/jm060880d
3063228 4064 None 14 Human Functional pEC50 = 7.3 7.3 7 4
Agonist activity at human histamine H4 receptor in SK-N-MC cells assessed as inhibition of forskolin-induced cAMP-mediated CRE-beta galactosidase activityAgonist activity at human histamine H4 receptor in SK-N-MC cells assessed as inhibition of forskolin-induced cAMP-mediated CRE-beta galactosidase activity
ChEMBL 161 3 4 3 -1.1 NC(=N)SCCN=C(N)N 10.1021/jm060880d
CHEMBL1196470 4064 None 14 Human Functional pEC50 = 7.3 7.3 7 4
Agonist activity at human histamine H4 receptor in SK-N-MC cells assessed as inhibition of forskolin-induced cAMP-mediated CRE-beta galactosidase activityAgonist activity at human histamine H4 receptor in SK-N-MC cells assessed as inhibition of forskolin-induced cAMP-mediated CRE-beta galactosidase activity
ChEMBL 161 3 4 3 -1.1 NC(=N)SCCN=C(N)N 10.1021/jm060880d
136141537 56497 None 3 Rat Functional pEC50 = 6.3 6.3 -5 3
Agonist activity at rat histamine H4 receptor by luciferase reporter gene assayAgonist activity at rat 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 56497 None 3 Rat Functional pEC50 = 6.3 6.3 -5 3
Agonist activity at rat histamine H4 receptor by luciferase reporter gene assayAgonist activity at rat 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
11313837 2500 None 6 Human Functional pEC50 = 5.3 5.3 -15848 2
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 179 2 1 2 1.3 CN1CCC(CC1)Cc1[nH]cnc1 10.1016/j.bmcl.2010.10.041
1254 2500 None 6 Human Functional pEC50 = 5.3 5.3 -15848 2
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 179 2 1 2 1.3 CN1CCC(CC1)Cc1[nH]cnc1 10.1016/j.bmcl.2010.10.041
CHEMBL175782 2500 None 6 Human Functional pEC50 = 5.3 5.3 -15848 2
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 179 2 1 2 1.3 CN1CCC(CC1)Cc1[nH]cnc1 10.1016/j.bmcl.2010.10.041
10583206 109416 None 0 Human Functional pEC50 = 5.3 5.3 -6 2
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
CHEMBL321920 109416 None 0 Human Functional pEC50 = 5.3 5.3 -6 2
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
1204 1932 None 74 Mouse Functional pEC50 = 5.3 5.3 -151 11
Agonist activity at mouse histamine H4 receptor by luciferase reporter gene assayAgonist activity at mouse 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 1932 None 74 Mouse Functional pEC50 = 5.3 5.3 -151 11
Agonist activity at mouse histamine H4 receptor by luciferase reporter gene assayAgonist activity at mouse 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 1932 None 74 Mouse Functional pEC50 = 5.3 5.3 -151 11
Agonist activity at mouse histamine H4 receptor by luciferase reporter gene assayAgonist activity at mouse 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 1932 None 74 Mouse Functional pEC50 = 5.3 5.3 -151 11
Agonist activity at mouse histamine H4 receptor by luciferase reporter gene assayAgonist activity at mouse 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
774.0 1932 None 74 Mouse Functional pEC50 = 5.3 5.3 -151 11
Agonist activity at mouse histamine H4 receptor by luciferase reporter gene assayAgonist activity at mouse 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 1932 None 74 Mouse Functional pEC50 = 5.3 5.3 -151 11
Agonist activity at mouse histamine H4 receptor by luciferase reporter gene assayAgonist activity at mouse 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 1932 None 74 Mouse Functional pEC50 = 5.3 5.3 -151 11
Agonist activity at mouse histamine H4 receptor by luciferase reporter gene assayAgonist activity at mouse 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
155513612 176425 None 0 Rat Functional pEC50 = 4.3 4.3 -18 3
Agonist activity at rat H4R expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 by [35S]-GTPgammaS-binding assayAgonist activity at rat H4R expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 by [35S]-GTPgammaS-binding assay
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 176425 None 0 Rat Functional pEC50 = 4.3 4.3 -18 3
Agonist activity at rat H4R expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 by [35S]-GTPgammaS-binding assayAgonist activity at rat H4R expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 by [35S]-GTPgammaS-binding assay
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 176425 None 0 Rat Functional pEC50 = 4.3 4.3 -18 3
Agonist activity at rat H4R expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 by [35S]-GTPgammaS-binding assayAgonist activity at rat H4R expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 by [35S]-GTPgammaS-binding assay
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 176425 None 0 Rat Functional pEC50 = 4.3 4.3 -18 3
Agonist activity at rat H4R expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 by [35S]-GTPgammaS-binding assayAgonist activity at rat H4R expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 by [35S]-GTPgammaS-binding assay
ChEMBL 277 4 1 5 2.1 CN(C)[C@@H]1CCN(c2ccnc(NCC(C)(C)C)n2)C1 10.1021/acs.jmedchem.9b01342
155512725 176346 None 0 Mouse Functional pEC50 = 7.3 7.3 -6 3
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 237 6 3 5 1.7 CC(C)(C)CNc1nccc(NCCCN)n1 10.1021/acs.jmedchem.9b01342
CHEMBL4437371 176346 None 0 Mouse Functional pEC50 = 7.3 7.3 -6 3
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 237 6 3 5 1.7 CC(C)(C)CNc1nccc(NCCCN)n1 10.1021/acs.jmedchem.9b01342
CHEMBL4594753 176346 None 0 Mouse Functional pEC50 = 7.3 7.3 -6 3
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 237 6 3 5 1.7 CC(C)(C)CNc1nccc(NCCCN)n1 10.1021/acs.jmedchem.9b01342
58227163 176568 None 0 Mouse Functional pEC50 = 7.3 7.3 -4 3
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 3 2 5 1.7 CC(C)(C)CNc1nccc(N2CCCNCC2)n1 10.1021/acs.jmedchem.9b01342
CHEMBL4518374 176568 None 0 Mouse Functional pEC50 = 7.3 7.3 -4 3
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 3 2 5 1.7 CC(C)(C)CNc1nccc(N2CCCNCC2)n1 10.1021/acs.jmedchem.9b01342
CHEMBL4596491 176568 None 0 Mouse Functional pEC50 = 7.3 7.3 -4 3
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 3 2 5 1.7 CC(C)(C)CNc1nccc(N2CCCNCC2)n1 10.1021/acs.jmedchem.9b01342
25130580 174406 None 0 Rat Functional pEC50 = 5.3 5.3 - 1
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium 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 1.6 CNc1nc(N2CCN(C)CC2)cc(C(C)(C)C)n1 10.1021/jm8005959
CHEMBL455016 174406 None 0 Rat Functional pEC50 = 5.3 5.3 - 1
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium 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 1.6 CNc1nc(N2CCN(C)CC2)cc(C(C)(C)C)n1 10.1021/jm8005959
25129878 187441 None 0 Rat Functional pEC50 = 5.3 5.3 - 1
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium 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 324 3 1 7 1.4 COc1c(-c2ccc(C#N)cc2)nc(N)nc1N1CCN(C)CC1 10.1021/jm8005959
CHEMBL493103 187441 None 0 Rat Functional pEC50 = 5.3 5.3 - 1
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium 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 324 3 1 7 1.4 COc1c(-c2ccc(C#N)cc2)nc(N)nc1N1CCN(C)CC1 10.1021/jm8005959
127052295 140284 None 0 Human Functional pEC50 = 6.3 6.3 - 1
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 352 7 3 4 2.4 N#C/N=C(/NCCOc1ccccc1)NC[C@H]1CC[C@H](c2c[nH]cn2)C1 10.1021/acs.jmedchem.6b00120
CHEMBL3804862 140284 None 0 Human Functional pEC50 = 6.3 6.3 - 1
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 352 7 3 4 2.4 N#C/N=C(/NCCOc1ccccc1)NC[C@H]1CC[C@H](c2c[nH]cn2)C1 10.1021/acs.jmedchem.6b00120
1204 1932 None 74 Rat Functional pEC50 = 4.3 4.3 -288 11
Agonist activity at rat H4R by [35S]-GTPgammaS-binding assayAgonist activity at rat H4R by [35S]-GTPgammaS-binding assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.9b01342
1247 1932 None 74 Rat Functional pEC50 = 4.3 4.3 -288 11
Agonist activity at rat H4R by [35S]-GTPgammaS-binding assayAgonist activity at rat H4R by [35S]-GTPgammaS-binding assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.9b01342
1375 1932 None 74 Rat Functional pEC50 = 4.3 4.3 -288 11
Agonist activity at rat H4R by [35S]-GTPgammaS-binding assayAgonist activity at rat H4R by [35S]-GTPgammaS-binding assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.9b01342
774 1932 None 74 Rat Functional pEC50 = 4.3 4.3 -288 11
Agonist activity at rat H4R by [35S]-GTPgammaS-binding assayAgonist activity at rat H4R by [35S]-GTPgammaS-binding assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.9b01342
774.0 1932 None 74 Rat Functional pEC50 = 4.3 4.3 -288 11
Agonist activity at rat H4R by [35S]-GTPgammaS-binding assayAgonist activity at rat H4R by [35S]-GTPgammaS-binding assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.9b01342
CHEMBL90 1932 None 74 Rat Functional pEC50 = 4.3 4.3 -288 11
Agonist activity at rat H4R by [35S]-GTPgammaS-binding assayAgonist activity at rat H4R by [35S]-GTPgammaS-binding assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.9b01342
DB05381 1932 None 74 Rat Functional pEC50 = 4.3 4.3 -288 11
Agonist activity at rat H4R by [35S]-GTPgammaS-binding assayAgonist activity at rat H4R by [35S]-GTPgammaS-binding assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.9b01342
53233803 61542 None 0 Human Functional pEC50 = 6.3 6.3 - 1
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 249 3 2 5 1.2 CC(C)Nc1cc(N2CCN(C)CC2)cc(N)n1 10.1016/j.bmcl.2011.03.017
CHEMBL1770962 61542 None 0 Human Functional pEC50 = 6.3 6.3 - 1
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 249 3 2 5 1.2 CC(C)Nc1cc(N2CCN(C)CC2)cc(N)n1 10.1016/j.bmcl.2011.03.017
25129169 187287 None 0 Rat Functional pEC50 = 7.3 7.3 -1 2
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 323 2 2 5 2.3 Nc1nc2c(c(N3CCNCC3)n1)CCCCC2c1ccccc1 10.1021/jm800670r
CHEMBL492231 187287 None 0 Rat Functional pEC50 = 7.3 7.3 -1 2
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 323 2 2 5 2.3 Nc1nc2c(c(N3CCNCC3)n1)CCCCC2c1ccccc1 10.1021/jm800670r
127049856 140332 None 0 Human Functional pEC50 = 6.3 6.3 - 1
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
CHEMBL3805431 140332 None 0 Human Functional pEC50 = 6.3 6.3 - 1
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
90667238 109532 None 0 Human Functional pEC50 = 6.3 6.3 - 1
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 220 4 3 3 0.3 CN/C(=N/C#N)NCCCc1c[nH]c(C)n1 10.1039/C3MD00245D
CHEMBL3220639 109532 None 0 Human Functional pEC50 = 6.3 6.3 - 1
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 220 4 3 3 0.3 CN/C(=N/C#N)NCCCc1c[nH]c(C)n1 10.1039/C3MD00245D
565544 109799 None 8 Human Functional pEC50 = 6.3 6.3 -4466 2
Inhibition of the forskolin-stimulated cAMP production for human Histamine H4 receptorInhibition of the forskolin-stimulated cAMP production for human Histamine H4 receptor
ChEMBL 125 2 2 2 0.5 CC(CN)c1cnc[nH]1 10.1021/jm0300025
CHEMBL322988 109799 None 8 Human Functional pEC50 = 6.3 6.3 -4466 2
Inhibition of the forskolin-stimulated cAMP production for human Histamine H4 receptorInhibition of the forskolin-stimulated cAMP production for human Histamine H4 receptor
ChEMBL 125 2 2 2 0.5 CC(CN)c1cnc[nH]1 10.1021/jm0300025
10583206 109416 None 0 Human Functional pEC50 = 5.3 5.3 -6 2
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
CHEMBL321920 109416 None 0 Human Functional pEC50 = 5.3 5.3 -6 2
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
25130915 187394 None 1 Rat Functional pEC50 = 7.3 7.3 - 1
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium 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 Cc1ccc(-c2cc(N3CCN(C)CC3)nc(N)n2)cc1 10.1021/jm8005959
CHEMBL492885 187394 None 1 Rat Functional pEC50 = 7.3 7.3 - 1
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium 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 Cc1ccc(-c2cc(N3CCN(C)CC3)nc(N)n2)cc1 10.1021/jm8005959
46228125 202444 None 0 Human Functional pEC50 = 7.3 7.3 - 1
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 366 4 2 6 2.7 CN1CCN(c2cc(NCc3ccc(Cl)c(Cl)c3)nc(N)n2)CC1 10.1016/j.bmc.2009.08.059
CHEMBL595215 202444 None 0 Human Functional pEC50 = 7.3 7.3 - 1
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 366 4 2 6 2.7 CN1CCN(c2cc(NCc3ccc(Cl)c(Cl)c3)nc(N)n2)CC1 10.1016/j.bmc.2009.08.059
44482028 5626 None 0 Human Functional pEC50 = 6.2 6.2 - 1
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)NCCCc1ccccn1 10.1021/jm900526h
CHEMBL1077580 5626 None 0 Human Functional pEC50 = 6.2 6.2 - 1
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)NCCCc1ccccn1 10.1021/jm900526h
25131232 187396 None 0 Rat Functional pEC50 = 7.2 7.2 - 1
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium 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 308 2 1 6 1.7 Cc1c(-c2ccc(C#N)cc2)nc(N)nc1N1CCN(C)CC1 10.1021/jm8005959
CHEMBL492900 187396 None 0 Rat Functional pEC50 = 7.2 7.2 - 1
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium 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 308 2 1 6 1.7 Cc1c(-c2ccc(C#N)cc2)nc(N)nc1N1CCN(C)CC1 10.1021/jm8005959
25130235 187693 None 1 Rat Functional pEC50 = 7.2 7.2 -4 3
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium 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(-c3ccc(C#N)cc3)nc(N)n2)CC1 10.1021/jm8005959
CHEMBL494678 187693 None 1 Rat Functional pEC50 = 7.2 7.2 -4 3
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium 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(-c3ccc(C#N)cc3)nc(N)n2)CC1 10.1021/jm8005959
25130235 187693 None 1 Rat Functional pEC50 = 7.2 7.2 -4 3
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 294 2 1 6 1.3 CN1CCN(c2cc(-c3ccc(C#N)cc3)nc(N)n2)CC1 10.1021/jm800670r
CHEMBL494678 187693 None 1 Rat Functional pEC50 = 7.2 7.2 -4 3
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 294 2 1 6 1.3 CN1CCN(c2cc(-c3ccc(C#N)cc3)nc(N)n2)CC1 10.1021/jm800670r
45257133 202360 None 0 Human Functional pEC50 = 8.2 8.2 - 1
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(NCc3ccccc3Cl)nc(N)n2)CC1 10.1016/j.bmc.2009.08.059
CHEMBL594721 202360 None 0 Human Functional pEC50 = 8.2 8.2 - 1
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(NCc3ccccc3Cl)nc(N)n2)CC1 10.1016/j.bmc.2009.08.059
25128824 193287 None 0 Rat Functional pEC50 = 8.2 8.2 -1 2
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 313 1 2 5 1.8 Nc1nc2c(c(N3CCNCC3)n1)CCCc1ccc(F)cc1-2 10.1021/jm800670r
CHEMBL523225 193287 None 0 Rat Functional pEC50 = 8.2 8.2 -1 2
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 313 1 2 5 1.8 Nc1nc2c(c(N3CCNCC3)n1)CCCc1ccc(F)cc1-2 10.1021/jm800670r
155517880 176772 None 0 Mouse Functional pEC50 = 8.2 8.2 -2 3
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 291 4 4 5 1.0 CC(C)(C)CNc1nccc(N2CC[C@@H](NC(=N)N)C2)n1 10.1021/acs.jmedchem.9b01342
CHEMBL4445423 176772 None 0 Mouse Functional pEC50 = 8.2 8.2 -2 3
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 291 4 4 5 1.0 CC(C)(C)CNc1nccc(N2CC[C@@H](NC(=N)N)C2)n1 10.1021/acs.jmedchem.9b01342
CHEMBL4598198 176772 None 0 Mouse Functional pEC50 = 8.2 8.2 -2 3
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 291 4 4 5 1.0 CC(C)(C)CNc1nccc(N2CC[C@@H](NC(=N)N)C2)n1 10.1021/acs.jmedchem.9b01342
45269820 197805 None 0 Human Functional pEC50 = 8.2 8.2 - 1
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 308 6 3 3 3.5 N=C(NCc1cccc(Cl)c1)SCCCc1c[nH]cn1 10.1021/acs.jmedchem.8b00435
CHEMBL1202326 197805 None 0 Human Functional pEC50 = 8.2 8.2 - 1
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 308 6 3 3 3.5 N=C(NCc1cccc(Cl)c1)SCCCc1c[nH]cn1 10.1021/acs.jmedchem.8b00435
CHEMBL551790 197805 None 0 Human Functional pEC50 = 8.2 8.2 - 1
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 308 6 3 3 3.5 N=C(NCc1cccc(Cl)c1)SCCCc1c[nH]cn1 10.1021/acs.jmedchem.8b00435
25071004 192827 None 0 Rat Functional pEC50 = 8.2 8.2 -1 2
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 309 2 2 5 2.0 CN[C@@H]1CCN(c2nc(N)nc3c2CCCc2ccccc2-3)C1 10.1021/jm800670r
CHEMBL521996 192827 None 0 Rat Functional pEC50 = 8.2 8.2 -1 2
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 309 2 2 5 2.0 CN[C@@H]1CCN(c2nc(N)nc3c2CCCc2ccccc2-3)C1 10.1021/jm800670r
46890022 7048 None 0 Human Functional pEC50 = 8.2 8.2 - 1
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 8 3 4 4.3 Cc1cc(OCCCNCC2CCCNC2)ccc1-c1nc2c(C)c(F)ccc2[nH]1 10.1016/j.bmcl.2010.04.017
CHEMBL1084869 7048 None 0 Human Functional pEC50 = 8.2 8.2 - 1
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 8 3 4 4.3 Cc1cc(OCCCNCC2CCCNC2)ccc1-c1nc2c(C)c(F)ccc2[nH]1 10.1016/j.bmcl.2010.04.017
46228158 204615 None 0 Human Functional pEC50 = 6.2 6.2 - 1
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 323 4 2 7 1.3 CN1CCN(c2cc(NCc3ccc(C#N)cc3)nc(N)n2)CC1 10.1016/j.bmc.2009.08.059
CHEMBL609289 204615 None 0 Human Functional pEC50 = 6.2 6.2 - 1
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 323 4 2 7 1.3 CN1CCN(c2cc(NCc3ccc(C#N)cc3)nc(N)n2)CC1 10.1016/j.bmc.2009.08.059
46890547 6518 None 0 Human Functional pEC50 = 7.2 7.2 - 1
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 7 2 4 4.0 CNC1CCN(CCCOc2ccc(-c3nc4c(C)c(F)ccc4[nH]3)c(C)c2)C1 10.1016/j.bmcl.2010.04.017
CHEMBL1082772 6518 None 0 Human Functional pEC50 = 7.2 7.2 - 1
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 7 2 4 4.0 CNC1CCN(CCCOc2ccc(-c3nc4c(C)c(F)ccc4[nH]3)c(C)c2)C1 10.1016/j.bmcl.2010.04.017
1255 3195 None 17 Human Functional pEC50 = 7.2 7.2 -19 2
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 216 6 1 2 2.6 C(CCc1cnc[nH]1)OCc1ccccc1 10.1016/j.bmcl.2010.10.041
6421522 3195 None 17 Human Functional pEC50 = 7.2 7.2 -19 2
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 216 6 1 2 2.6 C(CCc1cnc[nH]1)OCc1ccccc1 10.1016/j.bmcl.2010.10.041
CHEMBL19173 3195 None 17 Human Functional pEC50 = 7.2 7.2 -19 2
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 216 6 1 2 2.6 C(CCc1cnc[nH]1)OCc1ccccc1 10.1016/j.bmcl.2010.10.041
9974306 206932 None 0 Human Functional pEC50 = 7.2 7.2 - 1
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 336 8 3 2 3.4 S=C(NCCCCCc1c[nH]cn1)NCc1ccc(Cl)cc1 10.1016/j.bmcl.2010.10.041
CHEMBL72372 206932 None 0 Human Functional pEC50 = 7.2 7.2 - 1
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 336 8 3 2 3.4 S=C(NCCCCCc1c[nH]cn1)NCc1ccc(Cl)cc1 10.1016/j.bmcl.2010.10.041
10060212 206992 None 0 Human Functional pEC50 = 7.2 7.2 - 1
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 7 3 2 2.0 CCC/N=C(\S)NCCCCc1c[nH]cn1 10.1016/j.bmcl.2010.10.041
CHEMBL72769 206992 None 0 Human Functional pEC50 = 7.2 7.2 - 1
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 7 3 2 2.0 CCC/N=C(\S)NCCCCc1c[nH]cn1 10.1016/j.bmcl.2010.10.041
136192874 56499 None 0 Mouse Functional pEC50 = 7.2 7.2 1 3
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 2 2 4 2.7 CN1CCC(/C(=N/O)c2nc3cc(Cl)ccc3[nH]2)CC1 10.1016/j.bmcl.2010.10.041
CHEMBL1632414 56499 None 0 Mouse Functional pEC50 = 7.2 7.2 1 3
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 2 2 4 2.7 CN1CCC(/C(=N/O)c2nc3cc(Cl)ccc3[nH]2)CC1 10.1016/j.bmcl.2010.10.041
1236 2067 None 16 Human Functional pEC50 = 6.2 6.2 -549 3
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
1237 2067 None 16 Human Functional pEC50 = 6.2 6.2 -549 3
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
156615 2067 None 16 Human Functional pEC50 = 6.2 6.2 -549 3
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
CHEMBL268229 2067 None 16 Human Functional pEC50 = 6.2 6.2 -549 3
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
25129175 187485 None 0 Rat Functional pEC50 = 6.2 6.2 - 1
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium 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 COc1cnc(N)nc1N1CCN(C)CC1 10.1021/jm8005959
CHEMBL493477 187485 None 0 Rat Functional pEC50 = 6.2 6.2 - 1
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium 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 COc1cnc(N)nc1N1CCN(C)CC1 10.1021/jm8005959
25130914 187360 None 0 Human Functional pEC50 = 7.2 7.2 15 2
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 298 4 2 6 1.4 CN1CCN(c2cc(NCc3ccccc3)nc(N)n2)CC1 10.1021/jm8005959
CHEMBL492677 187360 None 0 Human Functional pEC50 = 7.2 7.2 15 2
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 298 4 2 6 1.4 CN1CCN(c2cc(NCc3ccccc3)nc(N)n2)CC1 10.1021/jm8005959
25130908 171954 None 1 Rat Functional pEC50 = 7.2 7.2 - 1
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium 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 Cc1cnc(N)nc1N1CCN(C)CC1 10.1021/jm8005959
CHEMBL446896 171954 None 1 Rat Functional pEC50 = 7.2 7.2 - 1
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium 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 Cc1cnc(N)nc1N1CCN(C)CC1 10.1021/jm8005959
24797775 187351 None 0 Rat Functional pEC50 = 7.2 7.2 - 1
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium 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 249 1 1 5 1.1 CN1CCN(c2cc(C(C)(C)C)nc(N)n2)CC1 10.1021/jm8005959
CHEMBL492631 187351 None 0 Rat Functional pEC50 = 7.2 7.2 - 1
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium 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 249 1 1 5 1.1 CN1CCN(c2cc(C(C)(C)C)nc(N)n2)CC1 10.1021/jm8005959
1204 1932 None 74 Mouse Functional pEC50 = 5.2 5.2 -151 11
Agonist activity at mouse H4R by [35S]-GTPgammaS-binding assayAgonist activity at mouse H4R by [35S]-GTPgammaS-binding assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.9b01342
1247 1932 None 74 Mouse Functional pEC50 = 5.2 5.2 -151 11
Agonist activity at mouse H4R by [35S]-GTPgammaS-binding assayAgonist activity at mouse H4R by [35S]-GTPgammaS-binding assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.9b01342
1375 1932 None 74 Mouse Functional pEC50 = 5.2 5.2 -151 11
Agonist activity at mouse H4R by [35S]-GTPgammaS-binding assayAgonist activity at mouse H4R by [35S]-GTPgammaS-binding assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.9b01342
774 1932 None 74 Mouse Functional pEC50 = 5.2 5.2 -151 11
Agonist activity at mouse H4R by [35S]-GTPgammaS-binding assayAgonist activity at mouse H4R by [35S]-GTPgammaS-binding assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.9b01342
774.0 1932 None 74 Mouse Functional pEC50 = 5.2 5.2 -151 11
Agonist activity at mouse H4R by [35S]-GTPgammaS-binding assayAgonist activity at mouse H4R by [35S]-GTPgammaS-binding assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.9b01342
CHEMBL90 1932 None 74 Mouse Functional pEC50 = 5.2 5.2 -151 11
Agonist activity at mouse H4R by [35S]-GTPgammaS-binding assayAgonist activity at mouse H4R by [35S]-GTPgammaS-binding assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.9b01342
DB05381 1932 None 74 Mouse Functional pEC50 = 5.2 5.2 -151 11
Agonist activity at mouse H4R by [35S]-GTPgammaS-binding assayAgonist activity at mouse H4R by [35S]-GTPgammaS-binding assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.9b01342
25130912 188847 None 0 Rat Functional pEC50 = 7.2 7.2 - 1
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium 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 262 2 1 6 0.4 CN1CCN(c2cc(N3CCCC3)nc(N)n2)CC1 10.1021/jm8005959
CHEMBL505061 188847 None 0 Rat Functional pEC50 = 7.2 7.2 - 1
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium 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 262 2 1 6 0.4 CN1CCN(c2cc(N3CCCC3)nc(N)n2)CC1 10.1021/jm8005959
1204 1932 None 74 Human Functional pEC50 = 8.1 8.1 -3 11
Agonist activity at human H4R by [35S]-GTPgammaS-binding assayAgonist activity at human H4R by [35S]-GTPgammaS-binding assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.9b01342
1247 1932 None 74 Human Functional pEC50 = 8.1 8.1 -3 11
Agonist activity at human H4R by [35S]-GTPgammaS-binding assayAgonist activity at human H4R by [35S]-GTPgammaS-binding assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.9b01342
1375 1932 None 74 Human Functional pEC50 = 8.1 8.1 -3 11
Agonist activity at human H4R by [35S]-GTPgammaS-binding assayAgonist activity at human H4R by [35S]-GTPgammaS-binding assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.9b01342
774 1932 None 74 Human Functional pEC50 = 8.1 8.1 -3 11
Agonist activity at human H4R by [35S]-GTPgammaS-binding assayAgonist activity at human H4R by [35S]-GTPgammaS-binding assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.9b01342
774.0 1932 None 74 Human Functional pEC50 = 8.1 8.1 -3 11
Agonist activity at human H4R by [35S]-GTPgammaS-binding assayAgonist activity at human H4R by [35S]-GTPgammaS-binding assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.9b01342
CHEMBL90 1932 None 74 Human Functional pEC50 = 8.1 8.1 -3 11
Agonist activity at human H4R by [35S]-GTPgammaS-binding assayAgonist activity at human H4R by [35S]-GTPgammaS-binding assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.9b01342
DB05381 1932 None 74 Human Functional pEC50 = 8.1 8.1 -3 11
Agonist activity at human H4R by [35S]-GTPgammaS-binding assayAgonist activity at human H4R by [35S]-GTPgammaS-binding assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.9b01342
25149521 179158 None 0 Human Functional pEC50 = 8.1 8.1 9 2
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 375 8 4 3 3.2 N=C(NCCCc1c[nH]cn1)NC(=O)CC(c1ccccc1)c1ccccc1 10.1016/j.bmcl.2010.10.041
CHEMBL471413 179158 None 0 Human Functional pEC50 = 8.1 8.1 9 2
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 375 8 4 3 3.2 N=C(NCCCc1c[nH]cn1)NC(=O)CC(c1ccccc1)c1ccccc1 10.1016/j.bmcl.2010.10.041
1204 1932 None 74 Human Functional pEC50 = 8.1 8.1 -3 11
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 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmcl.2015.12.035
1247 1932 None 74 Human Functional pEC50 = 8.1 8.1 -3 11
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 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmcl.2015.12.035
1375 1932 None 74 Human Functional pEC50 = 8.1 8.1 -3 11
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 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmcl.2015.12.035
774 1932 None 74 Human Functional pEC50 = 8.1 8.1 -3 11
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 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmcl.2015.12.035
774.0 1932 None 74 Human Functional pEC50 = 8.1 8.1 -3 11
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 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmcl.2015.12.035
CHEMBL90 1932 None 74 Human Functional pEC50 = 8.1 8.1 -3 11
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 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmcl.2015.12.035
DB05381 1932 None 74 Human Functional pEC50 = 8.1 8.1 -3 11
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 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmcl.2015.12.035
1267 3804 None 32 Human Functional pEC50 = 7.2 7.2 -17 5
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 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1016/j.bmc.2009.08.059
3035905 3804 None 32 Human Functional pEC50 = 7.2 7.2 -17 5
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 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1016/j.bmc.2009.08.059
CHEMBL260374 3804 None 32 Human Functional pEC50 = 7.2 7.2 -17 5
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 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1016/j.bmc.2009.08.059
1269 121 None 34 Human Functional pEC50 = 7.2 7.2 35 6
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 125 2 2 2 0.2 Cc1c(CCN)nc[nH]1 10.1021/jm900526h
37463 121 None 34 Human Functional pEC50 = 7.2 7.2 35 6
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 125 2 2 2 0.2 Cc1c(CCN)nc[nH]1 10.1021/jm900526h
CHEMBL275443 121 None 34 Human Functional pEC50 = 7.2 7.2 35 6
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 125 2 2 2 0.2 Cc1c(CCN)nc[nH]1 10.1021/jm900526h
1267 3804 None 32 Human Functional pEC50 = 7.2 7.2 -17 5
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 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1016/j.bmc.2009.08.059
3035905 3804 None 32 Human Functional pEC50 = 7.2 7.2 -17 5
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 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1016/j.bmc.2009.08.059
CHEMBL260374 3804 None 32 Human Functional pEC50 = 7.2 7.2 -17 5
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 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1016/j.bmc.2009.08.059
44482031 5644 None 0 Human Functional pEC50 = 6.2 6.2 - 1
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 234 6 3 3 0.8 CCN/C(=N\C#N)NCCCCc1c[nH]cn1 10.1021/jm900526h
CHEMBL1077756 5644 None 0 Human Functional pEC50 = 6.2 6.2 - 1
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 234 6 3 3 0.8 CCN/C(=N\C#N)NCCCCc1c[nH]cn1 10.1021/jm900526h
46890019 7314 None 0 Human Functional pEC50 = 6.2 6.2 - 1
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 394 6 1 4 3.8 Cc1cc(OCCCN2C3CN(C)CC32)ccc1-c1nc2c(C)c(F)ccc2[nH]1 10.1016/j.bmcl.2010.04.017
CHEMBL1086085 7314 None 0 Human Functional pEC50 = 6.2 6.2 - 1
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 394 6 1 4 3.8 Cc1cc(OCCCN2C3CN(C)CC32)ccc1-c1nc2c(C)c(F)ccc2[nH]1 10.1016/j.bmcl.2010.04.017
156015638 178377 None 0 Human Functional pEC50 = 7.1 7.1 - 1
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 415 10 1 2 5.5 Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCCCCc1c[nH]cn1 10.1021/acs.jmedchem.0c00160
CHEMBL4642520 178377 None 0 Human Functional pEC50 = 7.1 7.1 - 1
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 415 10 1 2 5.5 Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCCCCc1c[nH]cn1 10.1021/acs.jmedchem.0c00160
CHEMBL4650832 178377 None 0 Human Functional pEC50 = 7.1 7.1 - 1
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 415 10 1 2 5.5 Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCCCCc1c[nH]cn1 10.1021/acs.jmedchem.0c00160
1278 2150 None 56 Rat Functional pEC50 = 6.1 6.1 -1 4
Agonist activity at rat H4R by [35S]-GTPgammaS-binding assayAgonist activity at rat H4R by [35S]-GTPgammaS-binding assay
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/acs.jmedchem.9b01342
1279 2150 None 56 Rat Functional pEC50 = 6.1 6.1 -1 4
Agonist activity at rat H4R by [35S]-GTPgammaS-binding assayAgonist activity at rat H4R by [35S]-GTPgammaS-binding assay
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/acs.jmedchem.9b01342
4908365 2150 None 56 Rat Functional pEC50 = 6.1 6.1 -1 4
Agonist activity at rat H4R by [35S]-GTPgammaS-binding assayAgonist activity at rat H4R by [35S]-GTPgammaS-binding assay
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/acs.jmedchem.9b01342
CHEMBL129198 2150 None 56 Rat Functional pEC50 = 6.1 6.1 -1 4
Agonist activity at rat H4R by [35S]-GTPgammaS-binding assayAgonist activity at rat H4R by [35S]-GTPgammaS-binding assay
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/acs.jmedchem.9b01342
10978141 5152 None 0 Human Functional pEC50 = 6.1 6.1 -7 2
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
CHEMBL105803 5152 None 0 Human Functional pEC50 = 6.1 6.1 -7 2
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
58227127 117193 None 0 Human Functional pEC50 = 7.1 7.1 - 1
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 261 3 1 5 1.6 CN1CCN(c2ccnc(NC3CCCC3)n2)CC1 10.1016/j.bmcl.2014.12.027
CHEMBL3393543 117193 None 0 Human Functional pEC50 = 7.1 7.1 - 1
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 261 3 1 5 1.6 CN1CCN(c2ccnc(NC3CCCC3)n2)CC1 10.1016/j.bmcl.2014.12.027
44481489 5715 None 0 Human Functional pEC50 = 6.1 6.1 18 2
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(\NCCCc1ccccc1)NCCCc1c[nH]cn1 10.1021/jm900526h
CHEMBL1078210 5715 None 0 Human Functional pEC50 = 6.1 6.1 18 2
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(\NCCCc1ccccc1)NCCCc1c[nH]cn1 10.1021/jm900526h
10419556 5360 None 0 Human Functional pEC50 = 5.1 5.1 -9 2
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
CHEMBL106913 5360 None 0 Human Functional pEC50 = 5.1 5.1 -9 2
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
11086114 7396 None 0 Human Functional pEC50 = 5.1 5.1 - 1
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
CHEMBL108649 7396 None 0 Human Functional pEC50 = 5.1 5.1 - 1
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
10820930 5801 None 0 Human Functional pEC50 = 4.1 4.1 - 1
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
CHEMBL107877 5801 None 0 Human Functional pEC50 = 4.1 4.1 - 1
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
10106063 109327 None 11 Human Functional pEC50 = 7.1 7.1 40 2
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
CHEMBL321860 109327 None 11 Human Functional pEC50 = 7.1 7.1 40 2
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
10106063 109327 None 11 Human Functional pEC50 = 7.1 7.1 40 2
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-stimulated cAMP production incubated for 6 hrs by CRE/beta-galactosidase reporter gene assayAgonist activity at human histamine H4 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-stimulated cAMP production incubated for 6 hrs by CRE/beta-galactosidase reporter gene assay
ChEMBL 248 3 3 4 0.3 C/N=C(\NC#N)NC[C@H]1CC[C@H](c2c[nH]cn2)O1 10.1021/acs.jmedchem.6b00120
CHEMBL321860 109327 None 11 Human Functional pEC50 = 7.1 7.1 40 2
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-stimulated cAMP production incubated for 6 hrs by CRE/beta-galactosidase reporter gene assayAgonist activity at human histamine H4 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-stimulated cAMP production incubated for 6 hrs by CRE/beta-galactosidase reporter gene assay
ChEMBL 248 3 3 4 0.3 C/N=C(\NC#N)NC[C@H]1CC[C@H](c2c[nH]cn2)O1 10.1021/acs.jmedchem.6b00120
56954318 82109 None 0 Human Functional pEC50 = 7.1 7.1 2 2
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 444 13 6 4 0.1 N/C(=N\C(=O)CCCCC(=O)/N=C(\N)NCCCc1c[nH]cn1)NCCCc1c[nH]cn1 10.1021/jm201128q
CHEMBL2165640 82109 None 0 Human Functional pEC50 = 7.1 7.1 2 2
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 444 13 6 4 0.1 N/C(=N\C(=O)CCCCC(=O)/N=C(\N)NCCCc1c[nH]cn1)NCCCc1c[nH]cn1 10.1021/jm201128q
10106063 109327 None 11 Human Functional pEC50 = 7.1 7.1 40 2
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
CHEMBL321860 109327 None 11 Human Functional pEC50 = 7.1 7.1 40 2
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
10017000 206943 None 0 Human Functional pEC50 = 7.1 7.1 - 1
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 288 7 3 2 2.4 S=C(NCCCCc1c[nH]cn1)NCc1ccccc1 10.1016/j.bmcl.2010.10.041
CHEMBL72431 206943 None 0 Human Functional pEC50 = 7.1 7.1 - 1
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 288 7 3 2 2.4 S=C(NCCCCc1c[nH]cn1)NCc1ccccc1 10.1016/j.bmcl.2010.10.041
1204 1932 None 74 Human Functional pEC50 = 7.1 7.1 -3 11
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 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmcl.2010.10.041
1247 1932 None 74 Human Functional pEC50 = 7.1 7.1 -3 11
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 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmcl.2010.10.041
1375 1932 None 74 Human Functional pEC50 = 7.1 7.1 -3 11
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 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmcl.2010.10.041
774 1932 None 74 Human Functional pEC50 = 7.1 7.1 -3 11
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 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmcl.2010.10.041
774.0 1932 None 74 Human Functional pEC50 = 7.1 7.1 -3 11
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 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmcl.2010.10.041
CHEMBL90 1932 None 74 Human Functional pEC50 = 7.1 7.1 -3 11
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 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmcl.2010.10.041
DB05381 1932 None 74 Human Functional pEC50 = 7.1 7.1 -3 11
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 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmcl.2010.10.041
136192874 56499 None 0 Human Functional pEC50 = 7.1 7.1 -1 3
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 292 2 2 4 2.7 CN1CCC(/C(=N/O)c2nc3cc(Cl)ccc3[nH]2)CC1 10.1016/j.bmcl.2010.10.041
CHEMBL1632414 56499 None 0 Human Functional pEC50 = 7.1 7.1 -1 3
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 292 2 2 4 2.7 CN1CCC(/C(=N/O)c2nc3cc(Cl)ccc3[nH]2)CC1 10.1016/j.bmcl.2010.10.041
1267 3804 None 32 Human Functional pEC50 = 7.1 7.1 -17 5
Inverse agonist activity at human histamine H4 receptor expressed in HEK293 cells assessed by forskolin induced cAMP response element activation by luciferase reporter gene assayInverse agonist activity at human histamine H4 receptor expressed in HEK293 cells assessed by forskolin induced cAMP response element activation by luciferase reporter gene assay
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1021/jm1013488
3035905 3804 None 32 Human Functional pEC50 = 7.1 7.1 -17 5
Inverse agonist activity at human histamine H4 receptor expressed in HEK293 cells assessed by forskolin induced cAMP response element activation by luciferase reporter gene assayInverse agonist activity at human histamine H4 receptor expressed in HEK293 cells assessed by forskolin induced cAMP response element activation by luciferase reporter gene assay
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1021/jm1013488
CHEMBL260374 3804 None 32 Human Functional pEC50 = 7.1 7.1 -17 5
Inverse agonist activity at human histamine H4 receptor expressed in HEK293 cells assessed by forskolin induced cAMP response element activation by luciferase reporter gene assayInverse agonist activity at human histamine H4 receptor expressed in HEK293 cells assessed by forskolin induced cAMP response element activation by luciferase reporter gene assay
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1021/jm1013488
1239 2033 None 15 Human Functional pEC50 = 6.1 6.1 -1995 2
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 0.2 CNCCc1cnc[nH]1 10.1016/j.bmcl.2010.10.041
1240 2033 None 15 Human Functional pEC50 = 6.1 6.1 -1995 2
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 0.2 CNCCc1cnc[nH]1 10.1016/j.bmcl.2010.10.041
912 2033 None 15 Human Functional pEC50 = 6.1 6.1 -1995 2
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 0.2 CNCCc1cnc[nH]1 10.1016/j.bmcl.2010.10.041
CHEMBL268490 2033 None 15 Human Functional pEC50 = 6.1 6.1 -1995 2
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 0.2 CNCCc1cnc[nH]1 10.1016/j.bmcl.2010.10.041
10978141 5152 None 0 Human Functional pEC50 = 6.1 6.1 -7 2
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
CHEMBL105803 5152 None 0 Human Functional pEC50 = 6.1 6.1 -7 2
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
1278 2150 None 56 Mouse Functional pEC50 = 6.1 6.1 -1 4
Agonist activity at mouse H4R by [35S]-GTPgammaS-binding assayAgonist activity at mouse H4R by [35S]-GTPgammaS-binding assay
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/acs.jmedchem.9b01342
1279 2150 None 56 Mouse Functional pEC50 = 6.1 6.1 -1 4
Agonist activity at mouse H4R by [35S]-GTPgammaS-binding assayAgonist activity at mouse H4R by [35S]-GTPgammaS-binding assay
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/acs.jmedchem.9b01342
4908365 2150 None 56 Mouse Functional pEC50 = 6.1 6.1 -1 4
Agonist activity at mouse H4R by [35S]-GTPgammaS-binding assayAgonist activity at mouse H4R by [35S]-GTPgammaS-binding assay
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/acs.jmedchem.9b01342
CHEMBL129198 2150 None 56 Mouse Functional pEC50 = 6.1 6.1 -1 4
Agonist activity at mouse H4R by [35S]-GTPgammaS-binding assayAgonist activity at mouse H4R by [35S]-GTPgammaS-binding assay
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/acs.jmedchem.9b01342
42625303 180872 None 0 Mouse Functional pEC50 = 6.1 6.1 -501 6
Agonist activity at mouse H4R by [35S]-GTPgammaS-binding assayAgonist activity at mouse 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 180872 None 0 Mouse Functional pEC50 = 6.1 6.1 -501 6
Agonist activity at mouse H4R by [35S]-GTPgammaS-binding assayAgonist activity at mouse 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
10419556 5360 None 0 Human Functional pEC50 = 5.1 5.1 -9 2
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
CHEMBL106913 5360 None 0 Human Functional pEC50 = 5.1 5.1 -9 2
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
11086114 7396 None 0 Human Functional pEC50 = 5.1 5.1 - 1
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
CHEMBL108649 7396 None 0 Human Functional pEC50 = 5.1 5.1 - 1
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
155513612 176425 None 0 Mouse Functional pEC50 = 5.1 5.1 -14 3
Agonist activity at mouse H4R expressed in Sf9 cells by [35S]-GTPgammaS-binding assayAgonist activity at mouse H4R expressed in Sf9 cells by [35S]-GTPgammaS-binding assay
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 176425 None 0 Mouse Functional pEC50 = 5.1 5.1 -14 3
Agonist activity at mouse H4R expressed in Sf9 cells by [35S]-GTPgammaS-binding assayAgonist activity at mouse H4R expressed in Sf9 cells by [35S]-GTPgammaS-binding assay
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 176425 None 0 Mouse Functional pEC50 = 5.1 5.1 -14 3
Agonist activity at mouse H4R expressed in Sf9 cells by [35S]-GTPgammaS-binding assayAgonist activity at mouse H4R expressed in Sf9 cells by [35S]-GTPgammaS-binding assay
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 176425 None 0 Mouse Functional pEC50 = 5.1 5.1 -14 3
Agonist activity at mouse H4R expressed in Sf9 cells by [35S]-GTPgammaS-binding assayAgonist activity at mouse H4R expressed in Sf9 cells by [35S]-GTPgammaS-binding assay
ChEMBL 277 4 1 5 2.1 CN(C)[C@@H]1CCN(c2ccnc(NCC(C)(C)C)n2)C1 10.1021/acs.jmedchem.9b01342
25130230 172559 None 0 Rat Functional pEC50 = 5.1 5.1 -3 2
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium 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 1 7 -0.0 CN1CCN(c2cc(-n3ccnc3)nc(N)n2)CC1 10.1021/jm8005959
CHEMBL448085 172559 None 0 Rat Functional pEC50 = 5.1 5.1 -3 2
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium 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 1 7 -0.0 CN1CCN(c2cc(-n3ccnc3)nc(N)n2)CC1 10.1021/jm8005959
25133971 187455 None 1 Rat Functional pEC50 = 5.1 5.1 - 1
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium 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 249 1 1 5 1.1 CN1CCN(c2nc(N)cc(C(C)(C)C)n2)CC1 10.1021/jm8005959
CHEMBL493261 187455 None 1 Rat Functional pEC50 = 5.1 5.1 - 1
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium 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 249 1 1 5 1.1 CN1CCN(c2nc(N)cc(C(C)(C)C)n2)CC1 10.1021/jm8005959
25130229 188863 None 5 Rat Functional pEC50 = 5.1 5.1 - 1
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium 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 271 2 1 7 0.3 CN1CCN(c2cc(-c3cncnc3)nc(N)n2)CC1 10.1021/jm8005959
CHEMBL505346 188863 None 5 Rat Functional pEC50 = 5.1 5.1 - 1
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium 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 271 2 1 7 0.3 CN1CCN(c2cc(-c3cncnc3)nc(N)n2)CC1 10.1021/jm8005959
56954515 82096 None 0 Human Functional pEC50 = 8.1 8.1 -2 3
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 546 17 6 6 2.3 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)CCCCCCCCC(=O)/N=C(\N)NCCCc1c[nH]cn1 10.1021/jm201128q
CHEMBL2165628 82096 None 0 Human Functional pEC50 = 8.1 8.1 -2 3
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 546 17 6 6 2.3 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)CCCCCCCCC(=O)/N=C(\N)NCCCc1c[nH]cn1 10.1021/jm201128q
56954322 82111 None 0 Human Functional pEC50 = 8.1 8.1 -4 3
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 500 17 6 4 1.7 N/C(=N\C(=O)CCCCCCCCC(=O)/N=C(\N)NCCCc1c[nH]cn1)NCCCc1c[nH]cn1 10.1021/jm201128q
CHEMBL2165642 82111 None 0 Human Functional pEC50 = 8.1 8.1 -4 3
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 500 17 6 4 1.7 N/C(=N\C(=O)CCCCCCCCC(=O)/N=C(\N)NCCCc1c[nH]cn1)NCCCc1c[nH]cn1 10.1021/jm201128q
45257131 202364 None 0 Human Functional pEC50 = 8.1 8.1 - 1
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 312 4 2 6 1.7 Cc1ccccc1CNc1cc(N2CCN(C)CC2)nc(N)n1 10.1016/j.bmc.2009.08.059
CHEMBL594731 202364 None 0 Human Functional pEC50 = 8.1 8.1 - 1
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 312 4 2 6 1.7 Cc1ccccc1CNc1cc(N2CCN(C)CC2)nc(N)n1 10.1016/j.bmc.2009.08.059
11846298 139368 None 0 Human Functional pEC50 = 7.1 7.1 - 1
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)ccc3Oc3ccc(F)cc32)CC1 10.1021/jm051008s
CHEMBL379102 139368 None 0 Human Functional pEC50 = 7.1 7.1 - 1
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)ccc3Oc3ccc(F)cc32)CC1 10.1021/jm051008s
25129176 172864 None 0 Rat Functional pEC50 = 5.1 5.1 - 1
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium 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 269 2 1 5 1.5 CN1CCN(c2nc(N)ncc2-c2ccccc2)CC1 10.1021/jm8005959
CHEMBL451108 172864 None 0 Rat Functional pEC50 = 5.1 5.1 - 1
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium 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 269 2 1 5 1.5 CN1CCN(c2nc(N)ncc2-c2ccccc2)CC1 10.1021/jm8005959
58227388 117188 None 0 Human Functional pEC50 = 7.1 7.1 - 1
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 4 1 5 1.3 CC(C)CNc1nccc(N2CCN(C)CC2)n1 10.1016/j.bmcl.2014.12.027
CHEMBL3393538 117188 None 0 Human Functional pEC50 = 7.1 7.1 - 1
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 4 1 5 1.3 CC(C)CNc1nccc(N2CCN(C)CC2)n1 10.1016/j.bmcl.2014.12.027
1223 953 None 33 Mouse Functional pEC50 = 6.1 6.1 -812 4
Agonist activity at mouse H4R by [35S]-GTPgammaS-binding assayAgonist activity at mouse 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 953 None 33 Mouse Functional pEC50 = 6.1 6.1 -812 4
Agonist activity at mouse H4R by [35S]-GTPgammaS-binding assayAgonist activity at mouse 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 953 None 33 Mouse Functional pEC50 = 6.1 6.1 -812 4
Agonist activity at mouse H4R by [35S]-GTPgammaS-binding assayAgonist activity at mouse 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
10820929 108263 None 1 Human Functional pEC50 = 4.1 4.1 -30 2
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
CHEMBL319658 108263 None 1 Human Functional pEC50 = 4.1 4.1 -30 2
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
53233801 61565 None 0 Human Functional pEC50 = 7.1 7.1 - 1
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 264 4 2 6 0.9 CC(C)CNc1nc(N)cc(N2CCN(C)CC2)n1 10.1016/j.bmcl.2011.03.017
CHEMBL1770985 61565 None 0 Human Functional pEC50 = 7.1 7.1 - 1
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 264 4 2 6 0.9 CC(C)CNc1nc(N)cc(N2CCN(C)CC2)n1 10.1016/j.bmcl.2011.03.017
58227252 117194 None 0 Human Functional pEC50 = 7.1 7.1 - 1
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 261 4 2 5 1.6 CN[C@@H]1CCN(c2ccnc(NC3CCCC3)n2)C1 10.1016/j.bmcl.2014.12.027
CHEMBL3393544 117194 None 0 Human Functional pEC50 = 7.1 7.1 - 1
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 261 4 2 5 1.6 CN[C@@H]1CCN(c2ccnc(NC3CCCC3)n2)C1 10.1016/j.bmcl.2014.12.027
1204 1932 None 74 Mouse Functional pEC50 = 7.1 7.1 -151 11
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 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.0c00160
1204 1932 None 74 Mouse Functional pEC50 = 7.1 7.1 -151 11
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 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.9b01342
1247 1932 None 74 Mouse Functional pEC50 = 7.1 7.1 -151 11
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 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.0c00160
1247 1932 None 74 Mouse Functional pEC50 = 7.1 7.1 -151 11
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 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.9b01342
1375 1932 None 74 Mouse Functional pEC50 = 7.1 7.1 -151 11
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 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.0c00160
1375 1932 None 74 Mouse Functional pEC50 = 7.1 7.1 -151 11
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 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.9b01342
774 1932 None 74 Mouse Functional pEC50 = 7.1 7.1 -151 11
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 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.0c00160
774 1932 None 74 Mouse Functional pEC50 = 7.1 7.1 -151 11
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 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.9b01342
774.0 1932 None 74 Mouse Functional pEC50 = 7.1 7.1 -151 11
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 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.0c00160
774.0 1932 None 74 Mouse Functional pEC50 = 7.1 7.1 -151 11
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 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.9b01342
CHEMBL90 1932 None 74 Mouse Functional pEC50 = 7.1 7.1 -151 11
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 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.0c00160
CHEMBL90 1932 None 74 Mouse Functional pEC50 = 7.1 7.1 -151 11
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 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.9b01342
DB05381 1932 None 74 Mouse Functional pEC50 = 7.1 7.1 -151 11
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 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.0c00160
DB05381 1932 None 74 Mouse Functional pEC50 = 7.1 7.1 -151 11
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 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.9b01342
1274 4064 None 14 Mouse Functional pEC50 = 5.1 5.1 -199 4
Agonist activity at mouse H4R by [35S]-GTPgammaS-binding assayAgonist activity at mouse 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 4064 None 14 Mouse Functional pEC50 = 5.1 5.1 -199 4
Agonist activity at mouse H4R by [35S]-GTPgammaS-binding assayAgonist activity at mouse 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 4064 None 14 Mouse Functional pEC50 = 5.1 5.1 -199 4
Agonist activity at mouse H4R by [35S]-GTPgammaS-binding assayAgonist activity at mouse H4R by [35S]-GTPgammaS-binding assay
ChEMBL 161 3 4 3 -1.1 NC(=N)SCCN=C(N)N 10.1021/acs.jmedchem.9b01342
25130236 187807 None 0 Rat Functional pEC50 = 5.1 5.1 -1 2
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium 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 268 1 0 4 2.2 CN1CCN(c2cc(C(C)(C)C)nc(Cl)n2)CC1 10.1021/jm8005959
CHEMBL495265 187807 None 0 Rat Functional pEC50 = 5.1 5.1 -1 2
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium 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 268 1 0 4 2.2 CN1CCN(c2cc(C(C)(C)C)nc(Cl)n2)CC1 10.1021/jm8005959
1267 3804 None 32 Human Functional pEC50 = 7.1 7.1 -17 5
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 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1016/j.bmc.2009.08.059
3035905 3804 None 32 Human Functional pEC50 = 7.1 7.1 -17 5
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 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1016/j.bmc.2009.08.059
CHEMBL260374 3804 None 32 Human Functional pEC50 = 7.1 7.1 -17 5
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 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1016/j.bmc.2009.08.059
25129877 169563 None 0 Rat Functional pEC50 = 6.1 6.1 - 1
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium 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(-c3cccc(I)c3)nc(N)n2)CC1 10.1021/jm8005959
CHEMBL442865 169563 None 0 Rat Functional pEC50 = 6.1 6.1 - 1
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium 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(-c3cccc(I)c3)nc(N)n2)CC1 10.1021/jm8005959
44568847 187355 None 0 Rat Functional pEC50 = 5.1 5.1 - 1
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium 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 6 2.0 CN1CCN(c2cc(Sc3ccccc3)nc(N)n2)CC1 10.1021/jm8005959
CHEMBL492652 187355 None 0 Rat Functional pEC50 = 5.1 5.1 - 1
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium 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 6 2.0 CN1CCN(c2cc(Sc3ccccc3)nc(N)n2)CC1 10.1021/jm8005959
25101945 193215 None 0 Mouse Functional pEC50 = 8.0 8.0 1 2
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 2 2 5 1.6 CNC1CN(c2nc(N)nc3c2CCCc2ccccc2-3)C1 10.1021/jm800670r
CHEMBL522673 193215 None 0 Mouse Functional pEC50 = 8.0 8.0 1 2
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 2 2 5 1.6 CNC1CN(c2nc(N)nc3c2CCCc2ccccc2-3)C1 10.1021/jm800670r
25101945 193215 None 0 Rat Functional pEC50 = 8.0 8.0 -1 2
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 2 2 5 1.6 CNC1CN(c2nc(N)nc3c2CCCc2ccccc2-3)C1 10.1021/jm800670r
CHEMBL522673 193215 None 0 Rat Functional pEC50 = 8.0 8.0 -1 2
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 2 2 5 1.6 CNC1CN(c2nc(N)nc3c2CCCc2ccccc2-3)C1 10.1021/jm800670r
58227143 117191 None 0 Human Functional pEC50 = 7.0 7.0 - 1
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 1 5 1.4 CCCCNc1nccc(N2CCN(C)CC2)n1 10.1016/j.bmcl.2014.12.027
CHEMBL3393541 117191 None 0 Human Functional pEC50 = 7.0 7.0 - 1
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 1 5 1.4 CCCCNc1nccc(N2CCN(C)CC2)n1 10.1016/j.bmcl.2014.12.027
16061961 202135 None 0 Human Functional pEC50 = 7.0 7.0 - 1
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 316 4 2 6 1.6 CN1CCN(c2cc(NCc3ccc(F)cc3)nc(N)n2)CC1 10.1016/j.bmc.2009.08.059
CHEMBL593103 202135 None 0 Human Functional pEC50 = 7.0 7.0 - 1
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 316 4 2 6 1.6 CN1CCN(c2cc(NCc3ccc(F)cc3)nc(N)n2)CC1 10.1016/j.bmc.2009.08.059
112936251 137353 None 0 Human Functional pEC50 = 6.0 6.0 - 1
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 359 5 1 5 3.5 CN1CCN(c2cc(-c3ccccc3)nc(NCc3ccccc3)n2)CC1 10.1016/j.bmcl.2015.12.035
CHEMBL3752085 137353 None 0 Human Functional pEC50 = 6.0 6.0 - 1
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 359 5 1 5 3.5 CN1CCN(c2cc(-c3ccccc3)nc(NCc3ccccc3)n2)CC1 10.1016/j.bmcl.2015.12.035
58227163 176568 None 0 Rat Functional pEC50 = 7.0 7.0 -8 3
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 3 2 5 1.7 CC(C)(C)CNc1nccc(N2CCCNCC2)n1 10.1021/acs.jmedchem.9b01342
CHEMBL4518374 176568 None 0 Rat Functional pEC50 = 7.0 7.0 -8 3
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 3 2 5 1.7 CC(C)(C)CNc1nccc(N2CCCNCC2)n1 10.1021/acs.jmedchem.9b01342
CHEMBL4596491 176568 None 0 Rat Functional pEC50 = 7.0 7.0 -8 3
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 3 2 5 1.7 CC(C)(C)CNc1nccc(N2CCCNCC2)n1 10.1021/acs.jmedchem.9b01342
25131556 188979 None 5 Rat Functional pEC50 = 7.0 7.0 -3 2
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium 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 COc1ncccc1-c1cc(N2CCN(C)CC2)nc(N)n1 10.1021/jm8005959
CHEMBL507063 188979 None 5 Rat Functional pEC50 = 7.0 7.0 -3 2
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium 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 COc1ncccc1-c1cc(N2CCN(C)CC2)nc(N)n1 10.1021/jm8005959
25128830 187819 None 0 Rat Functional pEC50 = 6.0 6.0 - 1
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium 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 234 1 0 4 1.5 CN1CCN(c2cc(C(C)(C)C)ncn2)CC1 10.1021/jm8005959
CHEMBL495342 187819 None 0 Rat Functional pEC50 = 6.0 6.0 - 1
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium 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 234 1 0 4 1.5 CN1CCN(c2cc(C(C)(C)C)ncn2)CC1 10.1021/jm8005959
127035835 137372 None 0 Human Functional pEC50 = 6.0 6.0 - 1
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 385 4 1 5 3.6 CN1CCN(c2nc(NCc3ccccc3)nc3c2CCc2ccccc2-3)CC1 10.1016/j.bmcl.2015.12.035
CHEMBL3752270 137372 None 0 Human Functional pEC50 = 6.0 6.0 - 1
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 385 4 1 5 3.6 CN1CCN(c2nc(NCc3ccccc3)nc3c2CCc2ccccc2-3)CC1 10.1016/j.bmcl.2015.12.035
11983344 5679 None 2 Human Functional pEC50 = 6.0 6.0 - 1
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 220 5 3 3 0.4 CN/C(=N\C#N)NCCCCc1c[nH]cn1 10.1021/jm900526h
CHEMBL1077862 5679 None 2 Human Functional pEC50 = 6.0 6.0 - 1
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 220 5 3 3 0.4 CN/C(=N\C#N)NCCCCc1c[nH]cn1 10.1021/jm900526h
25128829 187440 None 0 Rat Functional pEC50 = 5.0 5.0 - 1
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium 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 265 5 1 5 1.7 CN(C)CCCN(C)c1cc(C(C)(C)C)nc(N)n1 10.1021/jm8005959
CHEMBL493100 187440 None 0 Rat Functional pEC50 = 5.0 5.0 - 1
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium 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 265 5 1 5 1.7 CN(C)CCCN(C)c1cc(C(C)(C)C)nc(N)n1 10.1021/jm8005959
24745335 295 None 13 Human Functional pIC50 = 9.2 9.2 - 1
Antagonist activity at H4R in human eosinophils assessed as inhibition of histamine-induced shape change by GAFS assayAntagonist activity at H4R in human eosinophils assessed as inhibition of histamine-induced shape change by GAFS assay
ChEMBL 262 5 3 6 0.7 CN[C@@H]1CCN(C1)c1cc(NCC2CC2)nc(n1)N 10.1016/j.bmcl.2011.07.125
8985 295 None 13 Human Functional pIC50 = 9.2 9.2 - 1
Antagonist activity at H4R in human eosinophils assessed as inhibition of histamine-induced shape change by GAFS assayAntagonist activity at H4R in human eosinophils assessed as inhibition of histamine-induced shape change by GAFS assay
ChEMBL 262 5 3 6 0.7 CN[C@@H]1CCN(C1)c1cc(NCC2CC2)nc(n1)N 10.1016/j.bmcl.2011.07.125
CHEMBL1915540 295 None 13 Human Functional pIC50 = 9.2 9.2 - 1
Antagonist activity at H4R in human eosinophils assessed as inhibition of histamine-induced shape change by GAFS assayAntagonist activity at H4R in human eosinophils assessed as inhibition of histamine-induced shape change by GAFS assay
ChEMBL 262 5 3 6 0.7 CN[C@@H]1CCN(C1)c1cc(NCC2CC2)nc(n1)N 10.1016/j.bmcl.2011.07.125
DB15027 295 None 13 Human Functional pIC50 = 9.2 9.2 - 1
Antagonist activity at H4R in human eosinophils assessed as inhibition of histamine-induced shape change by GAFS assayAntagonist activity at H4R in human eosinophils assessed as inhibition of histamine-induced shape change by GAFS assay
ChEMBL 262 5 3 6 0.7 CN[C@@H]1CCN(C1)c1cc(NCC2CC2)nc(n1)N 10.1016/j.bmcl.2011.07.125
24745335 295 None 13 Human Functional pIC50 = 8.9 8.9 - 1
Antagonist activity at H4R in human eosinophils assessed as inhibition of histamine-induced actin polymerisationAntagonist activity at H4R in human eosinophils assessed as inhibition of histamine-induced actin polymerisation
ChEMBL 262 5 3 6 0.7 CN[C@@H]1CCN(C1)c1cc(NCC2CC2)nc(n1)N 10.1016/j.bmcl.2011.07.125
8985 295 None 13 Human Functional pIC50 = 8.9 8.9 - 1
Antagonist activity at H4R in human eosinophils assessed as inhibition of histamine-induced actin polymerisationAntagonist activity at H4R in human eosinophils assessed as inhibition of histamine-induced actin polymerisation
ChEMBL 262 5 3 6 0.7 CN[C@@H]1CCN(C1)c1cc(NCC2CC2)nc(n1)N 10.1016/j.bmcl.2011.07.125
CHEMBL1915540 295 None 13 Human Functional pIC50 = 8.9 8.9 - 1
Antagonist activity at H4R in human eosinophils assessed as inhibition of histamine-induced actin polymerisationAntagonist activity at H4R in human eosinophils assessed as inhibition of histamine-induced actin polymerisation
ChEMBL 262 5 3 6 0.7 CN[C@@H]1CCN(C1)c1cc(NCC2CC2)nc(n1)N 10.1016/j.bmcl.2011.07.125
DB15027 295 None 13 Human Functional pIC50 = 8.9 8.9 - 1
Antagonist activity at H4R in human eosinophils assessed as inhibition of histamine-induced actin polymerisationAntagonist activity at H4R in human eosinophils assessed as inhibition of histamine-induced actin polymerisation
ChEMBL 262 5 3 6 0.7 CN[C@@H]1CCN(C1)c1cc(NCC2CC2)nc(n1)N 10.1016/j.bmcl.2011.07.125
156013896 178345 None 0 Human Functional pIC50 = 8.8 8.8 -3 3
Inverse agonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells assessed as reduction in histamine-induced inhibition of forskolin stimulated luciferase activity by luciferase reporter gene assayInverse agonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells assessed as reduction in histamine-induced inhibition of forskolin stimulated luciferase activity by luciferase reporter gene assay
ChEMBL 401 9 1 2 5.1 Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCCCc1c[nH]cn1 10.1021/acs.jmedchem.0c00160
CHEMBL4635634 178345 None 0 Human Functional pIC50 = 8.8 8.8 -3 3
Inverse agonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells assessed as reduction in histamine-induced inhibition of forskolin stimulated luciferase activity by luciferase reporter gene assayInverse agonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells assessed as reduction in histamine-induced inhibition of forskolin stimulated luciferase activity by luciferase reporter gene assay
ChEMBL 401 9 1 2 5.1 Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCCCc1c[nH]cn1 10.1021/acs.jmedchem.0c00160
CHEMBL4650570 178345 None 0 Human Functional pIC50 = 8.8 8.8 -3 3
Inverse agonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells assessed as reduction in histamine-induced inhibition of forskolin stimulated luciferase activity by luciferase reporter gene assayInverse agonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells assessed as reduction in histamine-induced inhibition of forskolin stimulated luciferase activity by luciferase reporter gene assay
ChEMBL 401 9 1 2 5.1 Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCCCc1c[nH]cn1 10.1021/acs.jmedchem.0c00160
44129134 201964 None 0 Human Functional pIC50 = 8 8.0 - 1
Inverse agonist activity at human histamine H4 receptor expressed in HEK293T cells by CRE-beta-galactosidase assayInverse agonist activity at human histamine H4 receptor expressed in HEK293T cells by CRE-beta-galactosidase assay
ChEMBL 384 5 2 7 0.7 CN1CCN(c2nc(NCCS(N)(=O)=O)c3cc(Cl)ccc3n2)CC1 10.1021/jm901379s
CHEMBL591969 201964 None 0 Human Functional pIC50 = 8 8.0 - 1
Inverse agonist activity at human histamine H4 receptor expressed in HEK293T cells by CRE-beta-galactosidase assayInverse agonist activity at human histamine H4 receptor expressed in HEK293T cells by CRE-beta-galactosidase assay
ChEMBL 384 5 2 7 0.7 CN1CCN(c2nc(NCCS(N)(=O)=O)c3cc(Cl)ccc3n2)CC1 10.1021/jm901379s
56835171 69762 None 0 Human Functional pIC50 = 7.0 7.0 - 1
Antagonist activity at human H4 receptor expressed in HEK293T cells assessed as inhibition of histamine-induced [35S]GTPgammaS bindingAntagonist activity at human H4 receptor expressed in HEK293T cells assessed as inhibition of histamine-induced [35S]GTPgammaS binding
ChEMBL 295 2 2 6 1.9 Nc1nc(N2CCNCC2)c2ccc(-c3ccco3)cc2n1 10.1016/j.bmcl.2011.10.104
CHEMBL1935574 69762 None 0 Human Functional pIC50 = 7.0 7.0 - 1
Antagonist activity at human H4 receptor expressed in HEK293T cells assessed as inhibition of histamine-induced [35S]GTPgammaS bindingAntagonist activity at human H4 receptor expressed in HEK293T cells assessed as inhibition of histamine-induced [35S]GTPgammaS binding
ChEMBL 295 2 2 6 1.9 Nc1nc(N2CCNCC2)c2ccc(-c3ccco3)cc2n1 10.1016/j.bmcl.2011.10.104
16082828 80291 None 0 Human Functional pIC50 = 7.0 7.0 -6 3
Antagonist activity at human H4 receptor expressed in 293-EBNA cells assessed as inhibition of histamine agonist activity by luciferase reporter gene assayAntagonist activity at human H4 receptor expressed in 293-EBNA cells assessed as inhibition of histamine agonist activity by luciferase reporter gene assay
ChEMBL 275 6 2 2 3.3 Clc1ccc(CNCC[C@@H]2C[C@H]2c2c[nH]cn2)cc1 10.1021/jm0603318
CHEMBL213886 80291 None 0 Human Functional pIC50 = 7.0 7.0 -6 3
Antagonist activity at human H4 receptor expressed in 293-EBNA cells assessed as inhibition of histamine agonist activity by luciferase reporter gene assayAntagonist activity at human H4 receptor expressed in 293-EBNA cells assessed as inhibition of histamine agonist activity by luciferase reporter gene assay
ChEMBL 275 6 2 2 3.3 Clc1ccc(CNCC[C@@H]2C[C@H]2c2c[nH]cn2)cc1 10.1021/jm0603318
71525678 89759 None 0 Human Functional pIC50 = 7.0 7.0 - 1
Antagonist activity at human histamine H4 receptor expressed in HEK cells assessed as inhibition of histamine-induced [35S]GTPgammaS bindingAntagonist activity at human histamine H4 receptor expressed in HEK cells assessed as inhibition of histamine-induced [35S]GTPgammaS binding
ChEMBL 258 3 2 6 0.6 CCc1cnc2c(N3CC(NC)C3)nc(N)nc2c1 10.1016/j.bmcl.2013.02.091
CHEMBL2376800 89759 None 0 Human Functional pIC50 = 7.0 7.0 - 1
Antagonist activity at human histamine H4 receptor expressed in HEK cells assessed as inhibition of histamine-induced [35S]GTPgammaS bindingAntagonist activity at human histamine H4 receptor expressed in HEK cells assessed as inhibition of histamine-induced [35S]GTPgammaS binding
ChEMBL 258 3 2 6 0.6 CCc1cnc2c(N3CC(NC)C3)nc(N)nc2c1 10.1016/j.bmcl.2013.02.091
71525679 89760 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Antagonist activity at human histamine H4 receptor expressed in HEK cells assessed as inhibition of histamine-induced [35S]GTPgammaS bindingAntagonist activity at human histamine H4 receptor expressed in HEK cells assessed as inhibition of histamine-induced [35S]GTPgammaS binding
ChEMBL 272 3 2 6 1.0 CCc1cnc2c(N3CC[C@@H](NC)C3)nc(N)nc2c1 10.1016/j.bmcl.2013.02.091
CHEMBL2376801 89760 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Antagonist activity at human histamine H4 receptor expressed in HEK cells assessed as inhibition of histamine-induced [35S]GTPgammaS bindingAntagonist activity at human histamine H4 receptor expressed in HEK cells assessed as inhibition of histamine-induced [35S]GTPgammaS binding
ChEMBL 272 3 2 6 1.0 CCc1cnc2c(N3CC[C@@H](NC)C3)nc(N)nc2c1 10.1016/j.bmcl.2013.02.091
1278 2150 None 56 Human Functional pIC50 = 7.9 7.9 1 4
Antagonist activity at recombinant human H4 receptor expressed in CHOK1 cells co-expressing Galpha16/aequorin assessed as inhibition of histamine-induced intracellular calcium flux preincubated for 30 mins followed by histamine addition and measured for 30 secs in presence of coelenterazine by luminescence assayAntagonist activity at recombinant human H4 receptor expressed in CHOK1 cells co-expressing Galpha16/aequorin assessed as inhibition of histamine-induced intracellular calcium flux preincubated for 30 mins followed by histamine addition and measured for 30 secs in presence of coelenterazine by luminescence assay
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1016/j.bmc.2019.02.020
1279 2150 None 56 Human Functional pIC50 = 7.9 7.9 1 4
Antagonist activity at recombinant human H4 receptor expressed in CHOK1 cells co-expressing Galpha16/aequorin assessed as inhibition of histamine-induced intracellular calcium flux preincubated for 30 mins followed by histamine addition and measured for 30 secs in presence of coelenterazine by luminescence assayAntagonist activity at recombinant human H4 receptor expressed in CHOK1 cells co-expressing Galpha16/aequorin assessed as inhibition of histamine-induced intracellular calcium flux preincubated for 30 mins followed by histamine addition and measured for 30 secs in presence of coelenterazine by luminescence assay
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1016/j.bmc.2019.02.020
4908365 2150 None 56 Human Functional pIC50 = 7.9 7.9 1 4
Antagonist activity at recombinant human H4 receptor expressed in CHOK1 cells co-expressing Galpha16/aequorin assessed as inhibition of histamine-induced intracellular calcium flux preincubated for 30 mins followed by histamine addition and measured for 30 secs in presence of coelenterazine by luminescence assayAntagonist activity at recombinant human H4 receptor expressed in CHOK1 cells co-expressing Galpha16/aequorin assessed as inhibition of histamine-induced intracellular calcium flux preincubated for 30 mins followed by histamine addition and measured for 30 secs in presence of coelenterazine by luminescence assay
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1016/j.bmc.2019.02.020
CHEMBL129198 2150 None 56 Human Functional pIC50 = 7.9 7.9 1 4
Antagonist activity at recombinant human H4 receptor expressed in CHOK1 cells co-expressing Galpha16/aequorin assessed as inhibition of histamine-induced intracellular calcium flux preincubated for 30 mins followed by histamine addition and measured for 30 secs in presence of coelenterazine by luminescence assayAntagonist activity at recombinant human H4 receptor expressed in CHOK1 cells co-expressing Galpha16/aequorin assessed as inhibition of histamine-induced intracellular calcium flux preincubated for 30 mins followed by histamine addition and measured for 30 secs in presence of coelenterazine by luminescence assay
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1016/j.bmc.2019.02.020
10446295 2132 None 34 Human Functional pIC50 = 6.9 6.9 11 2
Inhibition of mouse bone-marrow mast cell chemotaxis mediated by histamine H4 receptorInhibition of mouse bone-marrow mast cell chemotaxis mediated by histamine H4 receptor
ChEMBL 278 1 1 3 1.6 CN1CCN(CC1)C(=O)c1nc2c([nH]1)cc(cc2)Cl 10.1021/jm0502081
1277 2132 None 34 Human Functional pIC50 = 6.9 6.9 11 2
Inhibition of mouse bone-marrow mast cell chemotaxis mediated by histamine H4 receptorInhibition of mouse bone-marrow mast cell chemotaxis mediated by histamine H4 receptor
ChEMBL 278 1 1 3 1.6 CN1CCN(CC1)C(=O)c1nc2c([nH]1)cc(cc2)Cl 10.1021/jm0502081
CHEMBL185951 2132 None 34 Human Functional pIC50 = 6.9 6.9 11 2
Inhibition of mouse bone-marrow mast cell chemotaxis mediated by histamine H4 receptorInhibition of mouse bone-marrow mast cell chemotaxis mediated by histamine H4 receptor
ChEMBL 278 1 1 3 1.6 CN1CCN(CC1)C(=O)c1nc2c([nH]1)cc(cc2)Cl 10.1021/jm0502081
155563181 175407 None 0 Human Functional pIC50 = 5.9 5.9 - 1
Antagonist activity at human H4 receptor expressed in CHO-K1 cells co-expressing G protein alpha16 assessed as inhibition of histamine-induced calcium mobilization incubated for 16 hrs by aequorin-based functional assayAntagonist activity at human H4 receptor expressed in CHO-K1 cells co-expressing G protein alpha16 assessed as inhibition of histamine-induced calcium mobilization incubated for 16 hrs by aequorin-based functional assay
ChEMBL 498 12 1 7 5.1 CCOC(=O)C1=C(C)NC(C)=C(C(=O)OCC)C1c1ccc(OCCCCCN2CCCCC2)cc1 10.1021/acs.jmedchem.9b00937
CHEMBL4573309 175407 None 0 Human Functional pIC50 = 5.9 5.9 - 1
Antagonist activity at human H4 receptor expressed in CHO-K1 cells co-expressing G protein alpha16 assessed as inhibition of histamine-induced calcium mobilization incubated for 16 hrs by aequorin-based functional assayAntagonist activity at human H4 receptor expressed in CHO-K1 cells co-expressing G protein alpha16 assessed as inhibition of histamine-induced calcium mobilization incubated for 16 hrs by aequorin-based functional assay
ChEMBL 498 12 1 7 5.1 CCOC(=O)C1=C(C)NC(C)=C(C(=O)OCC)C1c1ccc(OCCCCCN2CCCCC2)cc1 10.1021/acs.jmedchem.9b00937
25147771 174342 None 0 Human Functional pIC50 = 6.8 6.8 - 1
Inverse agonist activity at human histamine H4 receptor expressed in HEK293T cells by CRE-beta-galactosidase assayInverse agonist activity at human histamine H4 receptor expressed in HEK293T cells by CRE-beta-galactosidase assay
ChEMBL 357 4 1 6 3.2 CN1CCN(c2nc(NCc3ccoc3)c3cc(Cl)ccc3n2)CC1 10.1021/jm800876b
CHEMBL454890 174342 None 0 Human Functional pIC50 = 6.8 6.8 - 1
Inverse agonist activity at human histamine H4 receptor expressed in HEK293T cells by CRE-beta-galactosidase assayInverse agonist activity at human histamine H4 receptor expressed in HEK293T cells by CRE-beta-galactosidase assay
ChEMBL 357 4 1 6 3.2 CN1CCN(c2nc(NCc3ccoc3)c3cc(Cl)ccc3n2)CC1 10.1021/jm800876b
16082833 80378 None 0 Human Functional pIC50 = 5.8 5.8 -40 2
Antagonist activity at human H4 receptor expressed in 293-EBNA cells assessed as inhibition of histamine agonist activity by luciferase reporter gene assayAntagonist activity at human H4 receptor expressed in 293-EBNA cells assessed as inhibition of histamine agonist activity by luciferase reporter gene assay
ChEMBL 247 6 2 2 3.1 c1nc([C@H]2C[C@@H]2CCNCC2CCCCC2)c[nH]1 10.1021/jm0603318
CHEMBL214312 80378 None 0 Human Functional pIC50 = 5.8 5.8 -40 2
Antagonist activity at human H4 receptor expressed in 293-EBNA cells assessed as inhibition of histamine agonist activity by luciferase reporter gene assayAntagonist activity at human H4 receptor expressed in 293-EBNA cells assessed as inhibition of histamine agonist activity by luciferase reporter gene assay
ChEMBL 247 6 2 2 3.1 c1nc([C@H]2C[C@@H]2CCNCC2CCCCC2)c[nH]1 10.1021/jm0603318
90645145 112241 None 0 Human Functional pIC50 = 5.8 5.8 - 1
Antagonist activity at human histamine H4 receptor expressed in gamma-irradiated recombinant CHO cells assessed as inhibition of forskolin/histamine-induced intracellular cAMP accumulation preincubated for 30 mins followed by Eu chelate-labeled cAMP/anti-cAMP mAb addition measured after 1 hr by TR-FRET immunoassayAntagonist activity at human histamine H4 receptor expressed in gamma-irradiated recombinant CHO cells assessed as inhibition of forskolin/histamine-induced intracellular cAMP accumulation preincubated for 30 mins followed by Eu chelate-labeled cAMP/anti-cAMP mAb addition measured after 1 hr by TR-FRET immunoassay
ChEMBL 348 2 1 6 1.6 CN1CCN(c2nc(N)nc(-c3ccc(Br)cc3)n2)CC1 10.1016/j.ejmech.2014.06.032
CHEMBL3290578 112241 None 0 Human Functional pIC50 = 5.8 5.8 - 1
Antagonist activity at human histamine H4 receptor expressed in gamma-irradiated recombinant CHO cells assessed as inhibition of forskolin/histamine-induced intracellular cAMP accumulation preincubated for 30 mins followed by Eu chelate-labeled cAMP/anti-cAMP mAb addition measured after 1 hr by TR-FRET immunoassayAntagonist activity at human histamine H4 receptor expressed in gamma-irradiated recombinant CHO cells assessed as inhibition of forskolin/histamine-induced intracellular cAMP accumulation preincubated for 30 mins followed by Eu chelate-labeled cAMP/anti-cAMP mAb addition measured after 1 hr by TR-FRET immunoassay
ChEMBL 348 2 1 6 1.6 CN1CCN(c2nc(N)nc(-c3ccc(Br)cc3)n2)CC1 10.1016/j.ejmech.2014.06.032
1267 3804 None 32 Human Functional pIC50 = 7.7 7.7 -17 5
Antagonist activity at human H4 receptor expressed in CHO-K1 cells co-expressing G protein alpha16 assessed as inhibition of histamine-induced calcium mobilization incubated for 16 hrs by aequorin-based functional assayAntagonist activity at human H4 receptor expressed in CHO-K1 cells co-expressing G protein alpha16 assessed as inhibition of histamine-induced calcium mobilization incubated for 16 hrs by aequorin-based functional assay
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1021/acs.jmedchem.9b00937
3035905 3804 None 32 Human Functional pIC50 = 7.7 7.7 -17 5
Antagonist activity at human H4 receptor expressed in CHO-K1 cells co-expressing G protein alpha16 assessed as inhibition of histamine-induced calcium mobilization incubated for 16 hrs by aequorin-based functional assayAntagonist activity at human H4 receptor expressed in CHO-K1 cells co-expressing G protein alpha16 assessed as inhibition of histamine-induced calcium mobilization incubated for 16 hrs by aequorin-based functional assay
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1021/acs.jmedchem.9b00937
CHEMBL260374 3804 None 32 Human Functional pIC50 = 7.7 7.7 -17 5
Antagonist activity at human H4 receptor expressed in CHO-K1 cells co-expressing G protein alpha16 assessed as inhibition of histamine-induced calcium mobilization incubated for 16 hrs by aequorin-based functional assayAntagonist activity at human H4 receptor expressed in CHO-K1 cells co-expressing G protein alpha16 assessed as inhibition of histamine-induced calcium mobilization incubated for 16 hrs by aequorin-based functional assay
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1021/acs.jmedchem.9b00937
1278 2150 None 56 Human Functional pIC50 = 6.7 6.7 1 4
Antagonist activity at H4R in human eosinophils assessed as inhibition of histamine-induced shape change by GAFS assayAntagonist activity at H4R in human eosinophils assessed as inhibition of histamine-induced shape change by GAFS assay
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1016/j.bmcl.2011.07.125
1279 2150 None 56 Human Functional pIC50 = 6.7 6.7 1 4
Antagonist activity at H4R in human eosinophils assessed as inhibition of histamine-induced shape change by GAFS assayAntagonist activity at H4R in human eosinophils assessed as inhibition of histamine-induced shape change by GAFS assay
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1016/j.bmcl.2011.07.125
4908365 2150 None 56 Human Functional pIC50 = 6.7 6.7 1 4
Antagonist activity at H4R in human eosinophils assessed as inhibition of histamine-induced shape change by GAFS assayAntagonist activity at H4R in human eosinophils assessed as inhibition of histamine-induced shape change by GAFS assay
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1016/j.bmcl.2011.07.125
CHEMBL129198 2150 None 56 Human Functional pIC50 = 6.7 6.7 1 4
Antagonist activity at H4R in human eosinophils assessed as inhibition of histamine-induced shape change by GAFS assayAntagonist activity at H4R in human eosinophils assessed as inhibition of histamine-induced shape change by GAFS assay
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1016/j.bmcl.2011.07.125
1278 2150 None 56 Human Functional pIC50 = 6.7 6.7 1 4
Antagonist actiivty at human H4R expressed in human U2OS cells assessed as inhibition of [35S]GTPgammaS binding after 30 mins by scintillation proximity assayAntagonist actiivty at human H4R expressed in human U2OS cells assessed as inhibition of [35S]GTPgammaS binding after 30 mins by scintillation proximity assay
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/jm401677g
1279 2150 None 56 Human Functional pIC50 = 6.7 6.7 1 4
Antagonist actiivty at human H4R expressed in human U2OS cells assessed as inhibition of [35S]GTPgammaS binding after 30 mins by scintillation proximity assayAntagonist actiivty at human H4R expressed in human U2OS cells assessed as inhibition of [35S]GTPgammaS binding after 30 mins by scintillation proximity assay
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/jm401677g
4908365 2150 None 56 Human Functional pIC50 = 6.7 6.7 1 4
Antagonist actiivty at human H4R expressed in human U2OS cells assessed as inhibition of [35S]GTPgammaS binding after 30 mins by scintillation proximity assayAntagonist actiivty at human H4R expressed in human U2OS cells assessed as inhibition of [35S]GTPgammaS binding after 30 mins by scintillation proximity assay
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/jm401677g
CHEMBL129198 2150 None 56 Human Functional pIC50 = 6.7 6.7 1 4
Antagonist actiivty at human H4R expressed in human U2OS cells assessed as inhibition of [35S]GTPgammaS binding after 30 mins by scintillation proximity assayAntagonist actiivty at human H4R expressed in human U2OS cells assessed as inhibition of [35S]GTPgammaS binding after 30 mins by scintillation proximity assay
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/jm401677g
3201696 15776 None 2 Human Functional pIC50 = 4.7 4.7 -22 2
Antagonist activity at human histamine H4 receptorAntagonist activity at human histamine H4 receptor
ChEMBL 348 5 0 6 2.1 CN1CCN(C(c2ccccc2)c2nnnn2Cc2ccccc2)CC1 10.1016/j.bmcl.2010.07.009
CHEMBL1222728 15776 None 2 Human Functional pIC50 = 4.7 4.7 -22 2
Antagonist activity at human histamine H4 receptorAntagonist activity at human histamine H4 receptor
ChEMBL 348 5 0 6 2.1 CN1CCN(C(c2ccccc2)c2nnnn2Cc2ccccc2)CC1 10.1016/j.bmcl.2010.07.009
1278 2150 None 56 Human Functional pIC50 = 6.7 6.7 1 4
Antagonist activity at H4R in human eosinophils assessed as inhibition of histamine-induced CD11b upregulationAntagonist activity at H4R in human eosinophils assessed as inhibition of histamine-induced CD11b upregulation
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1016/j.bmcl.2011.07.125
1279 2150 None 56 Human Functional pIC50 = 6.7 6.7 1 4
Antagonist activity at H4R in human eosinophils assessed as inhibition of histamine-induced CD11b upregulationAntagonist activity at H4R in human eosinophils assessed as inhibition of histamine-induced CD11b upregulation
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1016/j.bmcl.2011.07.125
4908365 2150 None 56 Human Functional pIC50 = 6.7 6.7 1 4
Antagonist activity at H4R in human eosinophils assessed as inhibition of histamine-induced CD11b upregulationAntagonist activity at H4R in human eosinophils assessed as inhibition of histamine-induced CD11b upregulation
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1016/j.bmcl.2011.07.125
CHEMBL129198 2150 None 56 Human Functional pIC50 = 6.7 6.7 1 4
Antagonist activity at H4R in human eosinophils assessed as inhibition of histamine-induced CD11b upregulationAntagonist activity at H4R in human eosinophils assessed as inhibition of histamine-induced CD11b upregulation
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1016/j.bmcl.2011.07.125
63868328 174355 None 1 Human Functional pIC50 = 6.6 6.6 - 1
Antagonist activity at recombinant human H4 receptor expressed in CHOK1 cells co-expressing Galpha16/aequorin assessed as inhibition of histamine-induced intracellular calcium flux preincubated for 30 mins followed by histamine addition and measured for 30 secs in presence of coelenterazine by luminescence assayAntagonist activity at recombinant human H4 receptor expressed in CHOK1 cells co-expressing Galpha16/aequorin assessed as inhibition of histamine-induced intracellular calcium flux preincubated for 30 mins followed by histamine addition and measured for 30 secs in presence of coelenterazine by luminescence assay
ChEMBL 236 3 1 6 0.2 CCCc1nc(N)nc(N2CCN(C)CC2)n1 10.1016/j.bmc.2019.02.020
CHEMBL4549015 174355 None 1 Human Functional pIC50 = 6.6 6.6 - 1
Antagonist activity at recombinant human H4 receptor expressed in CHOK1 cells co-expressing Galpha16/aequorin assessed as inhibition of histamine-induced intracellular calcium flux preincubated for 30 mins followed by histamine addition and measured for 30 secs in presence of coelenterazine by luminescence assayAntagonist activity at recombinant human H4 receptor expressed in CHOK1 cells co-expressing Galpha16/aequorin assessed as inhibition of histamine-induced intracellular calcium flux preincubated for 30 mins followed by histamine addition and measured for 30 secs in presence of coelenterazine by luminescence assay
ChEMBL 236 3 1 6 0.2 CCCc1nc(N)nc(N2CCN(C)CC2)n1 10.1016/j.bmc.2019.02.020
71548412 1909 None 22 Human Functional pIC50 = 7.6 7.6 14 2
Antagonist activity at recombinant human histamine H4 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine induced stimulation of [35S]-GTPgammaS binding by scintillation proximity assayAntagonist activity at recombinant human histamine H4 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine induced stimulation of [35S]-GTPgammaS binding by scintillation proximity assay
ChEMBL 334 2 1 8 0.2 CNC1CN(C1)c1nc2ncc(cc2n2c1nnn2)Br 10.1021/acs.jmedchem.7b01855
9879 1909 None 22 Human Functional pIC50 = 7.6 7.6 14 2
Antagonist activity at recombinant human histamine H4 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine induced stimulation of [35S]-GTPgammaS binding by scintillation proximity assayAntagonist activity at recombinant human histamine H4 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine induced stimulation of [35S]-GTPgammaS binding by scintillation proximity assay
ChEMBL 334 2 1 8 0.2 CNC1CN(C1)c1nc2ncc(cc2n2c1nnn2)Br 10.1021/acs.jmedchem.7b01855
CHEMBL4790724 1909 None 22 Human Functional pIC50 = 7.6 7.6 14 2
Antagonist activity at recombinant human histamine H4 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine induced stimulation of [35S]-GTPgammaS binding by scintillation proximity assayAntagonist activity at recombinant human histamine H4 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine induced stimulation of [35S]-GTPgammaS binding by scintillation proximity assay
ChEMBL 334 2 1 8 0.2 CNC1CN(C1)c1nc2ncc(cc2n2c1nnn2)Br 10.1021/acs.jmedchem.7b01855
16656871 7978 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Inverse agonist activity at human histamine H4 receptor assessed as inhibition of [35S]GTPgammaS binding after 15 mins by scintillation proximity assayInverse agonist activity at human histamine H4 receptor assessed as inhibition of [35S]GTPgammaS binding after 15 mins by scintillation proximity assay
ChEMBL 302 2 1 5 2.8 CN[C@H]1CCN(c2ncnc3c2oc2ccc(Cl)cc23)C1 10.1016/j.bmcl.2010.02.097
CHEMBL1090531 7978 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Inverse agonist activity at human histamine H4 receptor assessed as inhibition of [35S]GTPgammaS binding after 15 mins by scintillation proximity assayInverse agonist activity at human histamine H4 receptor assessed as inhibition of [35S]GTPgammaS binding after 15 mins by scintillation proximity assay
ChEMBL 302 2 1 5 2.8 CN[C@H]1CCN(c2ncnc3c2oc2ccc(Cl)cc23)C1 10.1016/j.bmcl.2010.02.097
16718567 8164 None 0 Human Functional pIC50 = 8.5 8.5 3311 2
Inverse agonist activity at human histamine H4 receptor assessed as inhibition of [35S]GTPgammaS binding after 15 mins by scintillation proximity assayInverse agonist activity at human histamine H4 receptor assessed as inhibition of [35S]GTPgammaS binding after 15 mins by scintillation proximity assay
ChEMBL 317 2 2 6 2.4 CN[C@@H]1CCN(c2nc(N)nc3c2oc2ccc(Cl)cc23)C1 10.1016/j.bmcl.2010.02.097
CHEMBL1091874 8164 None 0 Human Functional pIC50 = 8.5 8.5 3311 2
Inverse agonist activity at human histamine H4 receptor assessed as inhibition of [35S]GTPgammaS binding after 15 mins by scintillation proximity assayInverse agonist activity at human histamine H4 receptor assessed as inhibition of [35S]GTPgammaS binding after 15 mins by scintillation proximity assay
ChEMBL 317 2 2 6 2.4 CN[C@@H]1CCN(c2nc(N)nc3c2oc2ccc(Cl)cc23)C1 10.1016/j.bmcl.2010.02.097
1278 2150 None 56 Human Functional pIC50 = 7.5 7.5 1 4
Antagonist activity at H4R in human eosinophils assessed as inhibition of imetit-induced shape change by GAFS assayAntagonist activity at H4R in human eosinophils assessed as inhibition of imetit-induced shape change by GAFS assay
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1016/j.bmcl.2011.07.125
1279 2150 None 56 Human Functional pIC50 = 7.5 7.5 1 4
Antagonist activity at H4R in human eosinophils assessed as inhibition of imetit-induced shape change by GAFS assayAntagonist activity at H4R in human eosinophils assessed as inhibition of imetit-induced shape change by GAFS assay
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1016/j.bmcl.2011.07.125
4908365 2150 None 56 Human Functional pIC50 = 7.5 7.5 1 4
Antagonist activity at H4R in human eosinophils assessed as inhibition of imetit-induced shape change by GAFS assayAntagonist activity at H4R in human eosinophils assessed as inhibition of imetit-induced shape change by GAFS assay
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1016/j.bmcl.2011.07.125
CHEMBL129198 2150 None 56 Human Functional pIC50 = 7.5 7.5 1 4
Antagonist activity at H4R in human eosinophils assessed as inhibition of imetit-induced shape change by GAFS assayAntagonist activity at H4R in human eosinophils assessed as inhibition of imetit-induced shape change by GAFS assay
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1016/j.bmcl.2011.07.125
155540438 172644 None 0 Human Functional pIC50 = 7.5 7.5 - 1
Antagonist activity at recombinant human H4 receptor expressed in CHOK1 cells co-expressing Galpha16/aequorin assessed as inhibition of histamine-induced intracellular calcium flux preincubated for 30 mins followed by histamine addition and measured for 30 secs in presence of coelenterazine by luminescence assayAntagonist activity at recombinant human H4 receptor expressed in CHOK1 cells co-expressing Galpha16/aequorin assessed as inhibition of histamine-induced intracellular calcium flux preincubated for 30 mins followed by histamine addition and measured for 30 secs in presence of coelenterazine by luminescence assay
ChEMBL 290 3 1 6 1.3 CN1CCN(c2nc(N)nc(CC3CCCCC3)n2)CC1 10.1016/j.bmc.2019.02.020
CHEMBL4483783 172644 None 0 Human Functional pIC50 = 7.5 7.5 - 1
Antagonist activity at recombinant human H4 receptor expressed in CHOK1 cells co-expressing Galpha16/aequorin assessed as inhibition of histamine-induced intracellular calcium flux preincubated for 30 mins followed by histamine addition and measured for 30 secs in presence of coelenterazine by luminescence assayAntagonist activity at recombinant human H4 receptor expressed in CHOK1 cells co-expressing Galpha16/aequorin assessed as inhibition of histamine-induced intracellular calcium flux preincubated for 30 mins followed by histamine addition and measured for 30 secs in presence of coelenterazine by luminescence assay
ChEMBL 290 3 1 6 1.3 CN1CCN(c2nc(N)nc(CC3CCCCC3)n2)CC1 10.1016/j.bmc.2019.02.020
44129130 202012 None 0 Human Functional pIC50 = 7.5 7.5 - 1
Inverse agonist activity at human histamine H4 receptor expressed in HEK293T cells by CRE-beta-galactosidase assayInverse agonist activity at human histamine H4 receptor expressed in HEK293T cells by CRE-beta-galactosidase assay
ChEMBL 460 7 2 7 2.9 CN1CCN(c2nc(NCCS(=O)(=O)Nc3ccccc3)c3cc(Cl)ccc3n2)CC1 10.1021/jm901379s
CHEMBL592379 202012 None 0 Human Functional pIC50 = 7.5 7.5 - 1
Inverse agonist activity at human histamine H4 receptor expressed in HEK293T cells by CRE-beta-galactosidase assayInverse agonist activity at human histamine H4 receptor expressed in HEK293T cells by CRE-beta-galactosidase assay
ChEMBL 460 7 2 7 2.9 CN1CCN(c2nc(NCCS(=O)(=O)Nc3ccccc3)c3cc(Cl)ccc3n2)CC1 10.1021/jm901379s
11682208 8276 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Inverse agonist activity at human histamine H4 receptor assessed as inhibition of [35S]GTPgammaS binding after 15 mins by scintillation proximity assayInverse agonist activity at human histamine H4 receptor assessed as inhibition of [35S]GTPgammaS binding after 15 mins by scintillation proximity assay
ChEMBL 370 1 0 5 3.8 CN1CCN(c2nc(C(F)(F)F)nc3c2oc2ccc(Cl)cc23)CC1 10.1016/j.bmcl.2010.02.097
CHEMBL1092542 8276 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Inverse agonist activity at human histamine H4 receptor assessed as inhibition of [35S]GTPgammaS binding after 15 mins by scintillation proximity assayInverse agonist activity at human histamine H4 receptor assessed as inhibition of [35S]GTPgammaS binding after 15 mins by scintillation proximity assay
ChEMBL 370 1 0 5 3.8 CN1CCN(c2nc(C(F)(F)F)nc3c2oc2ccc(Cl)cc23)CC1 10.1016/j.bmcl.2010.02.097
25112105 8165 None 0 Human Functional pIC50 = 8.4 8.4 - 1
Inverse agonist activity at human histamine H4 receptor assessed as inhibition of [35S]GTPgammaS binding after 15 mins by scintillation proximity assayInverse agonist activity at human histamine H4 receptor assessed as inhibition of [35S]GTPgammaS binding after 15 mins by scintillation proximity assay
ChEMBL 317 2 2 6 2.4 CN[C@H]1CCN(c2nc(N)nc3c2oc2ccc(Cl)cc23)C1 10.1016/j.bmcl.2010.02.097
CHEMBL1091875 8165 None 0 Human Functional pIC50 = 8.4 8.4 - 1
Inverse agonist activity at human histamine H4 receptor assessed as inhibition of [35S]GTPgammaS binding after 15 mins by scintillation proximity assayInverse agonist activity at human histamine H4 receptor assessed as inhibition of [35S]GTPgammaS binding after 15 mins by scintillation proximity assay
ChEMBL 317 2 2 6 2.4 CN[C@H]1CCN(c2nc(N)nc3c2oc2ccc(Cl)cc23)C1 10.1016/j.bmcl.2010.02.097
24745335 295 None 13 Human Functional pIC50 = 8.3 8.3 - 1
Antagonist activity at H4R in human eosinophils assessed as inhibition of histamine-induced CD11b upregulationAntagonist activity at H4R in human eosinophils assessed as inhibition of histamine-induced CD11b upregulation
ChEMBL 262 5 3 6 0.7 CN[C@@H]1CCN(C1)c1cc(NCC2CC2)nc(n1)N 10.1016/j.bmcl.2011.07.125
8985 295 None 13 Human Functional pIC50 = 8.3 8.3 - 1
Antagonist activity at H4R in human eosinophils assessed as inhibition of histamine-induced CD11b upregulationAntagonist activity at H4R in human eosinophils assessed as inhibition of histamine-induced CD11b upregulation
ChEMBL 262 5 3 6 0.7 CN[C@@H]1CCN(C1)c1cc(NCC2CC2)nc(n1)N 10.1016/j.bmcl.2011.07.125
CHEMBL1915540 295 None 13 Human Functional pIC50 = 8.3 8.3 - 1
Antagonist activity at H4R in human eosinophils assessed as inhibition of histamine-induced CD11b upregulationAntagonist activity at H4R in human eosinophils assessed as inhibition of histamine-induced CD11b upregulation
ChEMBL 262 5 3 6 0.7 CN[C@@H]1CCN(C1)c1cc(NCC2CC2)nc(n1)N 10.1016/j.bmcl.2011.07.125
DB15027 295 None 13 Human Functional pIC50 = 8.3 8.3 - 1
Antagonist activity at H4R in human eosinophils assessed as inhibition of histamine-induced CD11b upregulationAntagonist activity at H4R in human eosinophils assessed as inhibition of histamine-induced CD11b upregulation
ChEMBL 262 5 3 6 0.7 CN[C@@H]1CCN(C1)c1cc(NCC2CC2)nc(n1)N 10.1016/j.bmcl.2011.07.125
1278 2150 None 56 Human Functional pIC50 = 7.4 7.4 1 4
Inhibition of mouse bone-marrow mast cell chemotaxis mediated by histamine H4 receptorInhibition of mouse bone-marrow mast cell chemotaxis mediated by histamine H4 receptor
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/jm0502081
1279 2150 None 56 Human Functional pIC50 = 7.4 7.4 1 4
Inhibition of mouse bone-marrow mast cell chemotaxis mediated by histamine H4 receptorInhibition of mouse bone-marrow mast cell chemotaxis mediated by histamine H4 receptor
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/jm0502081
4908365 2150 None 56 Human Functional pIC50 = 7.4 7.4 1 4
Inhibition of mouse bone-marrow mast cell chemotaxis mediated by histamine H4 receptorInhibition of mouse bone-marrow mast cell chemotaxis mediated by histamine H4 receptor
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/jm0502081
CHEMBL129198 2150 None 56 Human Functional pIC50 = 7.4 7.4 1 4
Inhibition of mouse bone-marrow mast cell chemotaxis mediated by histamine H4 receptorInhibition of mouse bone-marrow mast cell chemotaxis mediated by histamine H4 receptor
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/jm0502081
16656872 7914 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Inverse agonist activity at human histamine H4 receptor assessed as inhibition of [35S]GTPgammaS binding after 15 mins by scintillation proximity assayInverse agonist activity at human histamine H4 receptor assessed as inhibition of [35S]GTPgammaS binding after 15 mins by scintillation proximity assay
ChEMBL 302 2 1 5 2.8 CN[C@@H]1CCN(c2ncnc3c2oc2ccc(Cl)cc23)C1 10.1016/j.bmcl.2010.02.097
CHEMBL1090190 7914 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Inverse agonist activity at human histamine H4 receptor assessed as inhibition of [35S]GTPgammaS binding after 15 mins by scintillation proximity assayInverse agonist activity at human histamine H4 receptor assessed as inhibition of [35S]GTPgammaS binding after 15 mins by scintillation proximity assay
ChEMBL 302 2 1 5 2.8 CN[C@@H]1CCN(c2ncnc3c2oc2ccc(Cl)cc23)C1 10.1016/j.bmcl.2010.02.097
122193095 123981 None 0 Human Functional pIC50 = 6.4 6.4 - 1
Antagonist activity at human H4R expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by TR-FRET immunoassayAntagonist activity at human H4R expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by TR-FRET immunoassay
ChEMBL 330 3 1 6 2.0 CN1CCN(c2nc(N)nc(/C=C/c3cccc(Cl)c3)n2)CC1 10.1016/j.ejmech.2015.08.014
CHEMBL3628042 123981 None 0 Human Functional pIC50 = 6.4 6.4 - 1
Antagonist activity at human H4R expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by TR-FRET immunoassayAntagonist activity at human H4R expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by TR-FRET immunoassay
ChEMBL 330 3 1 6 2.0 CN1CCN(c2nc(N)nc(/C=C/c3cccc(Cl)c3)n2)CC1 10.1016/j.ejmech.2015.08.014
49841846 69760 None 0 Human Functional pIC50 = 7.3 7.3 - 1
Antagonist activity at human H4 receptor expressed in HEK293T cells assessed as inhibition of histamine-induced [35S]GTPgammaS bindingAntagonist activity at human H4 receptor expressed in HEK293T cells assessed as inhibition of histamine-induced [35S]GTPgammaS binding
ChEMBL 325 2 1 6 2.7 CN1CCN(c2nc(N)nc3cc(-c4ccsc4)ccc23)CC1 10.1016/j.bmcl.2011.10.104
CHEMBL1935572 69760 None 0 Human Functional pIC50 = 7.3 7.3 - 1
Antagonist activity at human H4 receptor expressed in HEK293T cells assessed as inhibition of histamine-induced [35S]GTPgammaS bindingAntagonist activity at human H4 receptor expressed in HEK293T cells assessed as inhibition of histamine-induced [35S]GTPgammaS binding
ChEMBL 325 2 1 6 2.7 CN1CCN(c2nc(N)nc3cc(-c4ccsc4)ccc23)CC1 10.1016/j.bmcl.2011.10.104
49841719 69759 None 0 Human Functional pIC50 = 7.3 7.3 - 1
Antagonist activity at human H4 receptor expressed in HEK293T cells assessed as inhibition of histamine-induced [35S]GTPgammaS bindingAntagonist activity at human H4 receptor expressed in HEK293T cells assessed as inhibition of histamine-induced [35S]GTPgammaS binding
ChEMBL 309 2 1 6 2.2 CN1CCN(c2nc(N)nc3cc(-c4ccoc4)ccc23)CC1 10.1016/j.bmcl.2011.10.104
CHEMBL1935571 69759 None 0 Human Functional pIC50 = 7.3 7.3 - 1
Antagonist activity at human H4 receptor expressed in HEK293T cells assessed as inhibition of histamine-induced [35S]GTPgammaS bindingAntagonist activity at human H4 receptor expressed in HEK293T cells assessed as inhibition of histamine-induced [35S]GTPgammaS binding
ChEMBL 309 2 1 6 2.2 CN1CCN(c2nc(N)nc3cc(-c4ccoc4)ccc23)CC1 10.1016/j.bmcl.2011.10.104
1278 2150 None 56 Human Functional pIC50 = 8.3 8.3 1 4
Antagonist activity at H4R in human eosinophils assessed as inhibition of histamine-induced actin polymerisationAntagonist activity at H4R in human eosinophils assessed as inhibition of histamine-induced actin polymerisation
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1016/j.bmcl.2011.07.125
1279 2150 None 56 Human Functional pIC50 = 8.3 8.3 1 4
Antagonist activity at H4R in human eosinophils assessed as inhibition of histamine-induced actin polymerisationAntagonist activity at H4R in human eosinophils assessed as inhibition of histamine-induced actin polymerisation
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1016/j.bmcl.2011.07.125
4908365 2150 None 56 Human Functional pIC50 = 8.3 8.3 1 4
Antagonist activity at H4R in human eosinophils assessed as inhibition of histamine-induced actin polymerisationAntagonist activity at H4R in human eosinophils assessed as inhibition of histamine-induced actin polymerisation
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1016/j.bmcl.2011.07.125
CHEMBL129198 2150 None 56 Human Functional pIC50 = 8.3 8.3 1 4
Antagonist activity at H4R in human eosinophils assessed as inhibition of histamine-induced actin polymerisationAntagonist activity at H4R in human eosinophils assessed as inhibition of histamine-induced actin polymerisation
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1016/j.bmcl.2011.07.125
90645147 112239 None 0 Human Functional pIC50 = 6.3 6.3 - 1
Antagonist activity at human histamine H4 receptor expressed in gamma-irradiated recombinant CHO cells assessed as inhibition of forskolin/histamine-induced intracellular cAMP accumulation preincubated for 30 mins followed by Eu chelate-labeled cAMP/anti-cAMP mAb addition measured after 1 hr by TR-FRET immunoassayAntagonist activity at human histamine H4 receptor expressed in gamma-irradiated recombinant CHO cells assessed as inhibition of forskolin/histamine-induced intracellular cAMP accumulation preincubated for 30 mins followed by Eu chelate-labeled cAMP/anti-cAMP mAb addition measured after 1 hr by TR-FRET immunoassay
ChEMBL 304 2 1 6 1.5 CN1CCN(c2nc(N)nc(-c3ccc(Cl)cc3)n2)CC1 10.1016/j.ejmech.2014.06.032
CHEMBL3290576 112239 None 0 Human Functional pIC50 = 6.3 6.3 - 1
Antagonist activity at human histamine H4 receptor expressed in gamma-irradiated recombinant CHO cells assessed as inhibition of forskolin/histamine-induced intracellular cAMP accumulation preincubated for 30 mins followed by Eu chelate-labeled cAMP/anti-cAMP mAb addition measured after 1 hr by TR-FRET immunoassayAntagonist activity at human histamine H4 receptor expressed in gamma-irradiated recombinant CHO cells assessed as inhibition of forskolin/histamine-induced intracellular cAMP accumulation preincubated for 30 mins followed by Eu chelate-labeled cAMP/anti-cAMP mAb addition measured after 1 hr by TR-FRET immunoassay
ChEMBL 304 2 1 6 1.5 CN1CCN(c2nc(N)nc(-c3ccc(Cl)cc3)n2)CC1 10.1016/j.ejmech.2014.06.032
24745335 295 None 13 Human Functional pIC50 = 7.3 7.3 - 1
Antagonist activity at human histamine H4 receptor expressed in HEK cells assessed as inhibition of histamine-induced [35S]GTPgammaS bindingAntagonist activity at human histamine H4 receptor expressed in HEK cells assessed as inhibition of histamine-induced [35S]GTPgammaS binding
ChEMBL 262 5 3 6 0.7 CN[C@@H]1CCN(C1)c1cc(NCC2CC2)nc(n1)N 10.1016/j.bmcl.2013.02.091
8985 295 None 13 Human Functional pIC50 = 7.3 7.3 - 1
Antagonist activity at human histamine H4 receptor expressed in HEK cells assessed as inhibition of histamine-induced [35S]GTPgammaS bindingAntagonist activity at human histamine H4 receptor expressed in HEK cells assessed as inhibition of histamine-induced [35S]GTPgammaS binding
ChEMBL 262 5 3 6 0.7 CN[C@@H]1CCN(C1)c1cc(NCC2CC2)nc(n1)N 10.1016/j.bmcl.2013.02.091
CHEMBL1915540 295 None 13 Human Functional pIC50 = 7.3 7.3 - 1
Antagonist activity at human histamine H4 receptor expressed in HEK cells assessed as inhibition of histamine-induced [35S]GTPgammaS bindingAntagonist activity at human histamine H4 receptor expressed in HEK cells assessed as inhibition of histamine-induced [35S]GTPgammaS binding
ChEMBL 262 5 3 6 0.7 CN[C@@H]1CCN(C1)c1cc(NCC2CC2)nc(n1)N 10.1016/j.bmcl.2013.02.091
DB15027 295 None 13 Human Functional pIC50 = 7.3 7.3 - 1
Antagonist activity at human histamine H4 receptor expressed in HEK cells assessed as inhibition of histamine-induced [35S]GTPgammaS bindingAntagonist activity at human histamine H4 receptor expressed in HEK cells assessed as inhibition of histamine-induced [35S]GTPgammaS binding
ChEMBL 262 5 3 6 0.7 CN[C@@H]1CCN(C1)c1cc(NCC2CC2)nc(n1)N 10.1016/j.bmcl.2013.02.091
10446295 2132 None 34 Human Functional pIC50 = 6.3 6.3 11 2
Inhibition of human eosinophil chemotaxis mediated by histamine H4 receptorInhibition of human eosinophil chemotaxis mediated by histamine H4 receptor
ChEMBL 278 1 1 3 1.6 CN1CCN(CC1)C(=O)c1nc2c([nH]1)cc(cc2)Cl 10.1021/jm0502081
1277 2132 None 34 Human Functional pIC50 = 6.3 6.3 11 2
Inhibition of human eosinophil chemotaxis mediated by histamine H4 receptorInhibition of human eosinophil chemotaxis mediated by histamine H4 receptor
ChEMBL 278 1 1 3 1.6 CN1CCN(CC1)C(=O)c1nc2c([nH]1)cc(cc2)Cl 10.1021/jm0502081
CHEMBL185951 2132 None 34 Human Functional pIC50 = 6.3 6.3 11 2
Inhibition of human eosinophil chemotaxis mediated by histamine H4 receptorInhibition of human eosinophil chemotaxis mediated by histamine H4 receptor
ChEMBL 278 1 1 3 1.6 CN1CCN(CC1)C(=O)c1nc2c([nH]1)cc(cc2)Cl 10.1021/jm0502081
122194625 124088 None 0 Human Functional pIC50 = 6.2 6.2 - 1
Antagonist activity at human H4R expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by TR-FRET immunoassayAntagonist activity at human H4R expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by TR-FRET immunoassay
ChEMBL 310 3 1 6 1.7 Cc1cccc(/C=C/c2nc(N)nc(N3CCN(C)CC3)n2)c1 10.1016/j.ejmech.2015.08.014
CHEMBL3629828 124088 None 0 Human Functional pIC50 = 6.2 6.2 - 1
Antagonist activity at human H4R expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by TR-FRET immunoassayAntagonist activity at human H4R expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by TR-FRET immunoassay
ChEMBL 310 3 1 6 1.7 Cc1cccc(/C=C/c2nc(N)nc(N3CCN(C)CC3)n2)c1 10.1016/j.ejmech.2015.08.014
1267 3804 None 32 Human Functional pIC50 = 6.2 6.2 -17 5
Antagonist activity at histamine H4 receptor expressed in HEK293 cells co-transfected with pCRE-Luc gene assessed as inhibition of forskolin/histamine-induced cAMP accumulation after 5 hrs by luciferase reporter gene assayAntagonist activity at histamine H4 receptor expressed in HEK293 cells co-transfected with pCRE-Luc gene assessed as inhibition of forskolin/histamine-induced cAMP accumulation after 5 hrs by luciferase reporter gene assay
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1016/j.bmc.2011.09.061
3035905 3804 None 32 Human Functional pIC50 = 6.2 6.2 -17 5
Antagonist activity at histamine H4 receptor expressed in HEK293 cells co-transfected with pCRE-Luc gene assessed as inhibition of forskolin/histamine-induced cAMP accumulation after 5 hrs by luciferase reporter gene assayAntagonist activity at histamine H4 receptor expressed in HEK293 cells co-transfected with pCRE-Luc gene assessed as inhibition of forskolin/histamine-induced cAMP accumulation after 5 hrs by luciferase reporter gene assay
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1016/j.bmc.2011.09.061
CHEMBL260374 3804 None 32 Human Functional pIC50 = 6.2 6.2 -17 5
Antagonist activity at histamine H4 receptor expressed in HEK293 cells co-transfected with pCRE-Luc gene assessed as inhibition of forskolin/histamine-induced cAMP accumulation after 5 hrs by luciferase reporter gene assayAntagonist activity at histamine H4 receptor expressed in HEK293 cells co-transfected with pCRE-Luc gene assessed as inhibition of forskolin/histamine-induced cAMP accumulation after 5 hrs by luciferase reporter gene assay
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1016/j.bmc.2011.09.061
1267 3804 None 32 Human Functional pIC50 = 6.2 6.2 -17 5
Antagonist activity at human H4 receptor expressed in 293-EBNA cells assessed as inhibition of histamine agonist activity by luciferase reporter gene assayAntagonist activity at human H4 receptor expressed in 293-EBNA cells assessed as inhibition of histamine agonist activity by luciferase reporter gene assay
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1021/jm0603318
3035905 3804 None 32 Human Functional pIC50 = 6.2 6.2 -17 5
Antagonist activity at human H4 receptor expressed in 293-EBNA cells assessed as inhibition of histamine agonist activity by luciferase reporter gene assayAntagonist activity at human H4 receptor expressed in 293-EBNA cells assessed as inhibition of histamine agonist activity by luciferase reporter gene assay
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1021/jm0603318
CHEMBL260374 3804 None 32 Human Functional pIC50 = 6.2 6.2 -17 5
Antagonist activity at human H4 receptor expressed in 293-EBNA cells assessed as inhibition of histamine agonist activity by luciferase reporter gene assayAntagonist activity at human H4 receptor expressed in 293-EBNA cells assessed as inhibition of histamine agonist activity by luciferase reporter gene assay
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1021/jm0603318
25147772 173513 None 9 Human Functional pIC50 = 7.2 7.2 - 1
Inverse agonist activity at human histamine H4 receptor expressed in HEK293T cells by CRE-beta-galactosidase assayInverse agonist activity at human histamine H4 receptor expressed in HEK293T cells by CRE-beta-galactosidase assay
ChEMBL 373 4 1 6 3.7 CN1CCN(c2nc(NCc3cccs3)c3cc(Cl)ccc3n2)CC1 10.1021/jm800876b
CHEMBL452847 173513 None 9 Human Functional pIC50 = 7.2 7.2 - 1
Inverse agonist activity at human histamine H4 receptor expressed in HEK293T cells by CRE-beta-galactosidase assayInverse agonist activity at human histamine H4 receptor expressed in HEK293T cells by CRE-beta-galactosidase assay
ChEMBL 373 4 1 6 3.7 CN1CCN(c2nc(NCc3cccs3)c3cc(Cl)ccc3n2)CC1 10.1021/jm800876b
71548412 1909 None 22 Mouse Functional pIC50 = 6.2 6.2 -14 2
Antagonist activity at recombinant mouse histamine H4 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine induced stimulation of [35S]-GTPgammaS binding by scintillation proximity assayAntagonist activity at recombinant mouse histamine H4 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine induced stimulation of [35S]-GTPgammaS binding by scintillation proximity assay
ChEMBL 334 2 1 8 0.2 CNC1CN(C1)c1nc2ncc(cc2n2c1nnn2)Br 10.1021/acs.jmedchem.7b01855
9879 1909 None 22 Mouse Functional pIC50 = 6.2 6.2 -14 2
Antagonist activity at recombinant mouse histamine H4 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine induced stimulation of [35S]-GTPgammaS binding by scintillation proximity assayAntagonist activity at recombinant mouse histamine H4 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine induced stimulation of [35S]-GTPgammaS binding by scintillation proximity assay
ChEMBL 334 2 1 8 0.2 CNC1CN(C1)c1nc2ncc(cc2n2c1nnn2)Br 10.1021/acs.jmedchem.7b01855
CHEMBL4790724 1909 None 22 Mouse Functional pIC50 = 6.2 6.2 -14 2
Antagonist activity at recombinant mouse histamine H4 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine induced stimulation of [35S]-GTPgammaS binding by scintillation proximity assayAntagonist activity at recombinant mouse histamine H4 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine induced stimulation of [35S]-GTPgammaS binding by scintillation proximity assay
ChEMBL 334 2 1 8 0.2 CNC1CN(C1)c1nc2ncc(cc2n2c1nnn2)Br 10.1021/acs.jmedchem.7b01855
11709443 8248 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Inverse agonist activity at human histamine H4 receptor assessed as inhibition of [35S]GTPgammaS binding after 15 mins by scintillation proximity assayInverse agonist activity at human histamine H4 receptor assessed as inhibition of [35S]GTPgammaS binding after 15 mins by scintillation proximity assay
ChEMBL 314 1 0 5 2.9 CN1C[C@@H]2C[C@H]1CN2c1ncnc2c1oc1ccc(Cl)cc12 10.1016/j.bmcl.2010.02.097
CHEMBL1092332 8248 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Inverse agonist activity at human histamine H4 receptor assessed as inhibition of [35S]GTPgammaS binding after 15 mins by scintillation proximity assayInverse agonist activity at human histamine H4 receptor assessed as inhibition of [35S]GTPgammaS binding after 15 mins by scintillation proximity assay
ChEMBL 314 1 0 5 2.9 CN1C[C@@H]2C[C@H]1CN2c1ncnc2c1oc1ccc(Cl)cc12 10.1016/j.bmcl.2010.02.097
71519674 89763 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity at human histamine H4 receptor expressed in HEK cells assessed as inhibition of histamine-induced [35S]GTPgammaS bindingAntagonist activity at human histamine H4 receptor expressed in HEK cells assessed as inhibition of histamine-induced [35S]GTPgammaS binding
ChEMBL 270 3 2 6 0.9 CNC1CN(c2nc(N)nc3cc(C4CC4)cnc23)C1 10.1016/j.bmcl.2013.02.091
CHEMBL2376804 89763 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity at human histamine H4 receptor expressed in HEK cells assessed as inhibition of histamine-induced [35S]GTPgammaS bindingAntagonist activity at human histamine H4 receptor expressed in HEK cells assessed as inhibition of histamine-induced [35S]GTPgammaS binding
ChEMBL 270 3 2 6 0.9 CNC1CN(c2nc(N)nc3cc(C4CC4)cnc23)C1 10.1016/j.bmcl.2013.02.091
16656874 8108 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Inverse agonist activity at human histamine H4 receptor assessed as inhibition of [35S]GTPgammaS binding after 15 mins by scintillation proximity assayInverse agonist activity at human histamine H4 receptor assessed as inhibition of [35S]GTPgammaS binding after 15 mins by scintillation proximity assay
ChEMBL 288 2 1 5 2.4 CNC1CN(c2ncnc3c2oc2ccc(Cl)cc23)C1 10.1016/j.bmcl.2010.02.097
CHEMBL1091569 8108 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Inverse agonist activity at human histamine H4 receptor assessed as inhibition of [35S]GTPgammaS binding after 15 mins by scintillation proximity assayInverse agonist activity at human histamine H4 receptor assessed as inhibition of [35S]GTPgammaS binding after 15 mins by scintillation proximity assay
ChEMBL 288 2 1 5 2.4 CNC1CN(c2ncnc3c2oc2ccc(Cl)cc23)C1 10.1016/j.bmcl.2010.02.097
49841845 69761 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Antagonist activity at human H4 receptor expressed in HEK293T cells assessed as inhibition of histamine-induced [35S]GTPgammaS bindingAntagonist activity at human H4 receptor expressed in HEK293T cells assessed as inhibition of histamine-induced [35S]GTPgammaS binding
ChEMBL 309 2 1 6 2.2 CN1CCN(c2nc(N)nc3cc(-c4ccco4)ccc23)CC1 10.1016/j.bmcl.2011.10.104
CHEMBL1935573 69761 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Antagonist activity at human H4 receptor expressed in HEK293T cells assessed as inhibition of histamine-induced [35S]GTPgammaS bindingAntagonist activity at human H4 receptor expressed in HEK293T cells assessed as inhibition of histamine-induced [35S]GTPgammaS binding
ChEMBL 309 2 1 6 2.2 CN1CCN(c2nc(N)nc3cc(-c4ccco4)ccc23)CC1 10.1016/j.bmcl.2011.10.104
156013896 178345 None 0 Mouse Functional pIC50 = 7.1 7.1 -38 3
Inverse agonist activity at mouse H4R expressed in HEK293-SF-mH4R-His6-CRE-Luc cells assessed as reduction in histamine-induced inhibition of forskolin stimulated luciferase activity by luciferase reporter gene assayInverse agonist activity at mouse H4R expressed in HEK293-SF-mH4R-His6-CRE-Luc cells assessed as reduction in histamine-induced inhibition of forskolin stimulated luciferase activity by luciferase reporter gene assay
ChEMBL 401 9 1 2 5.1 Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCCCc1c[nH]cn1 10.1021/acs.jmedchem.0c00160
CHEMBL4635634 178345 None 0 Mouse Functional pIC50 = 7.1 7.1 -38 3
Inverse agonist activity at mouse H4R expressed in HEK293-SF-mH4R-His6-CRE-Luc cells assessed as reduction in histamine-induced inhibition of forskolin stimulated luciferase activity by luciferase reporter gene assayInverse agonist activity at mouse H4R expressed in HEK293-SF-mH4R-His6-CRE-Luc cells assessed as reduction in histamine-induced inhibition of forskolin stimulated luciferase activity by luciferase reporter gene assay
ChEMBL 401 9 1 2 5.1 Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCCCc1c[nH]cn1 10.1021/acs.jmedchem.0c00160
CHEMBL4650570 178345 None 0 Mouse Functional pIC50 = 7.1 7.1 -38 3
Inverse agonist activity at mouse H4R expressed in HEK293-SF-mH4R-His6-CRE-Luc cells assessed as reduction in histamine-induced inhibition of forskolin stimulated luciferase activity by luciferase reporter gene assayInverse agonist activity at mouse H4R expressed in HEK293-SF-mH4R-His6-CRE-Luc cells assessed as reduction in histamine-induced inhibition of forskolin stimulated luciferase activity by luciferase reporter gene assay
ChEMBL 401 9 1 2 5.1 Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCCCc1c[nH]cn1 10.1021/acs.jmedchem.0c00160
1278 2150 None 56 Human Functional pIC50 = 7.1 7.1 1 4
Inhibition of human eosinophil chemotaxis mediated by histamine H4 receptorInhibition of human eosinophil chemotaxis mediated by histamine H4 receptor
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/jm0502081
1279 2150 None 56 Human Functional pIC50 = 7.1 7.1 1 4
Inhibition of human eosinophil chemotaxis mediated by histamine H4 receptorInhibition of human eosinophil chemotaxis mediated by histamine H4 receptor
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/jm0502081
4908365 2150 None 56 Human Functional pIC50 = 7.1 7.1 1 4
Inhibition of human eosinophil chemotaxis mediated by histamine H4 receptorInhibition of human eosinophil chemotaxis mediated by histamine H4 receptor
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/jm0502081
CHEMBL129198 2150 None 56 Human Functional pIC50 = 7.1 7.1 1 4
Inhibition of human eosinophil chemotaxis mediated by histamine H4 receptorInhibition of human eosinophil chemotaxis mediated by histamine H4 receptor
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/jm0502081
16082831 80377 None 0 Human Functional pIC50 = 6.1 6.1 -100 3
Antagonist activity at human H4 receptor expressed in 293-EBNA cells assessed as inhibition of histamine agonist activity by luciferase reporter gene assayAntagonist activity at human H4 receptor expressed in 293-EBNA cells assessed as inhibition of histamine agonist activity by luciferase reporter gene assay
ChEMBL 275 6 2 2 3.3 Clc1ccc(CNCC[C@H]2C[C@@H]2c2c[nH]cn2)cc1 10.1021/jm0603318
CHEMBL214311 80377 None 0 Human Functional pIC50 = 6.1 6.1 -100 3
Antagonist activity at human H4 receptor expressed in 293-EBNA cells assessed as inhibition of histamine agonist activity by luciferase reporter gene assayAntagonist activity at human H4 receptor expressed in 293-EBNA cells assessed as inhibition of histamine agonist activity by luciferase reporter gene assay
ChEMBL 275 6 2 2 3.3 Clc1ccc(CNCC[C@H]2C[C@@H]2c2c[nH]cn2)cc1 10.1021/jm0603318
71525681 89762 None 0 Human Functional pIC50 = 7.0 7.0 - 1
Antagonist activity at human histamine H4 receptor expressed in HEK cells assessed as inhibition of histamine-induced [35S]GTPgammaS bindingAntagonist activity at human histamine H4 receptor expressed in HEK cells assessed as inhibition of histamine-induced [35S]GTPgammaS binding
ChEMBL 298 3 2 6 1.7 CNC1CN(c2nc(N)nc3cc(C4CCCC4)cnc23)C1 10.1016/j.bmcl.2013.02.091
CHEMBL2376803 89762 None 0 Human Functional pIC50 = 7.0 7.0 - 1
Antagonist activity at human histamine H4 receptor expressed in HEK cells assessed as inhibition of histamine-induced [35S]GTPgammaS bindingAntagonist activity at human histamine H4 receptor expressed in HEK cells assessed as inhibition of histamine-induced [35S]GTPgammaS binding
ChEMBL 298 3 2 6 1.7 CNC1CN(c2nc(N)nc3cc(C4CCCC4)cnc23)C1 10.1016/j.bmcl.2013.02.091
1267 3804 None 32 Human Functional pIC50 = 6.0 6.0 -17 5
Antagonist activity at human H4 receptor expressed in HEK293T cells assessed as inhibition of histamine-induced [35S]GTPgammaS bindingAntagonist activity at human H4 receptor expressed in HEK293T cells assessed as inhibition of histamine-induced [35S]GTPgammaS binding
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1016/j.bmcl.2011.10.104
3035905 3804 None 32 Human Functional pIC50 = 6.0 6.0 -17 5
Antagonist activity at human H4 receptor expressed in HEK293T cells assessed as inhibition of histamine-induced [35S]GTPgammaS bindingAntagonist activity at human H4 receptor expressed in HEK293T cells assessed as inhibition of histamine-induced [35S]GTPgammaS binding
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1016/j.bmcl.2011.10.104
CHEMBL260374 3804 None 32 Human Functional pIC50 = 6.0 6.0 -17 5
Antagonist activity at human H4 receptor expressed in HEK293T cells assessed as inhibition of histamine-induced [35S]GTPgammaS bindingAntagonist activity at human H4 receptor expressed in HEK293T cells assessed as inhibition of histamine-induced [35S]GTPgammaS binding
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1016/j.bmcl.2011.10.104
58227148 117197 None 0 Human Functional pKd = 10.1 10.1 - 1
Antagonist activity at human recombinant histamine H4 receptor expressed in SK-N-MC cells assessed as inhibition of forskolin-stimulated cAMP-mediated reporter gene activityAntagonist activity at human recombinant histamine H4 receptor expressed in SK-N-MC cells assessed as inhibition of forskolin-stimulated cAMP-mediated reporter gene activity
ChEMBL 287 4 2 5 1.9 CN[C@@H]1CCN(c2ccnc(NC3CC4CCC3C4)n2)C1 10.1016/j.bmcl.2014.12.027
CHEMBL3393547 117197 None 0 Human Functional pKd = 10.1 10.1 - 1
Antagonist activity at human recombinant histamine H4 receptor expressed in SK-N-MC cells assessed as inhibition of forskolin-stimulated cAMP-mediated reporter gene activityAntagonist activity at human recombinant histamine H4 receptor expressed in SK-N-MC cells assessed as inhibition of forskolin-stimulated cAMP-mediated reporter gene activity
ChEMBL 287 4 2 5 1.9 CN[C@@H]1CCN(c2ccnc(NC3CC4CCC3C4)n2)C1 10.1016/j.bmcl.2014.12.027
59777258 110189 None 0 Human Functional pKd = 10 10.0 - 0
Antagonist activity at human histamine H4 receptor expressed in SK-N-MC cells assessed as reduction of histamine-induced inhibition of cAMP-mediated beta-galactosidase reporter gene activity treated 10 mins prior to histamine challenge by microplate reader analysisAntagonist activity at human histamine H4 receptor expressed in SK-N-MC cells assessed as reduction of histamine-induced inhibition of cAMP-mediated beta-galactosidase reporter gene activity treated 10 mins prior to histamine challenge by microplate reader analysis
ChEMBL 273 2 2 5 1.5 Nc1nc(C2CCCC2)cc(N2C[C@H]3CCN[C@H]3C2)n1 10.1021/jm401727m
CHEMBL3236561 110189 None 0 Human Functional pKd = 10 10.0 - 0
Antagonist activity at human histamine H4 receptor expressed in SK-N-MC cells assessed as reduction of histamine-induced inhibition of cAMP-mediated beta-galactosidase reporter gene activity treated 10 mins prior to histamine challenge by microplate reader analysisAntagonist activity at human histamine H4 receptor expressed in SK-N-MC cells assessed as reduction of histamine-induced inhibition of cAMP-mediated beta-galactosidase reporter gene activity treated 10 mins prior to histamine challenge by microplate reader analysis
ChEMBL 273 2 2 5 1.5 Nc1nc(C2CCCC2)cc(N2C[C@H]3CCN[C@H]3C2)n1 10.1021/jm401727m
24797604 110180 None 0 Human Functional pKd = 9.9 9.9 - 0
Antagonist activity at human histamine H4 receptor expressed in SK-N-MC cells assessed as reduction of histamine-induced inhibition of cAMP-mediated beta-galactosidase reporter gene activity treated 10 mins prior to histamine challenge by microplate reader analysisAntagonist activity at human histamine H4 receptor expressed in SK-N-MC cells assessed as reduction of histamine-induced inhibition of cAMP-mediated beta-galactosidase reporter gene activity treated 10 mins prior to histamine challenge by microplate reader analysis
ChEMBL 261 2 1 5 1.5 CN1CCN(c2cc(C3CCCC3)nc(N)n2)CC1 10.1021/jm401727m
CHEMBL3236552 110180 None 0 Human Functional pKd = 9.9 9.9 - 0
Antagonist activity at human histamine H4 receptor expressed in SK-N-MC cells assessed as reduction of histamine-induced inhibition of cAMP-mediated beta-galactosidase reporter gene activity treated 10 mins prior to histamine challenge by microplate reader analysisAntagonist activity at human histamine H4 receptor expressed in SK-N-MC cells assessed as reduction of histamine-induced inhibition of cAMP-mediated beta-galactosidase reporter gene activity treated 10 mins prior to histamine challenge by microplate reader analysis
ChEMBL 261 2 1 5 1.5 CN1CCN(c2cc(C3CCCC3)nc(N)n2)CC1 10.1021/jm401727m
24994542 110182 None 0 Human Functional pKd = 9.6 9.6 - 0
Antagonist activity at human histamine H4 receptor expressed in SK-N-MC cells assessed as reduction of histamine-induced inhibition of cAMP-mediated beta-galactosidase reporter gene activity treated 10 mins prior to histamine challenge by microplate reader analysisAntagonist activity at human histamine H4 receptor expressed in SK-N-MC cells assessed as reduction of histamine-induced inhibition of cAMP-mediated beta-galactosidase reporter gene activity treated 10 mins prior to histamine challenge by microplate reader analysis
ChEMBL 261 3 2 5 1.5 CN[C@@H]1CCN(c2cc(C3CCCC3)nc(N)n2)C1 10.1021/jm401727m
CHEMBL3236554 110182 None 0 Human Functional pKd = 9.6 9.6 - 0
Antagonist activity at human histamine H4 receptor expressed in SK-N-MC cells assessed as reduction of histamine-induced inhibition of cAMP-mediated beta-galactosidase reporter gene activity treated 10 mins prior to histamine challenge by microplate reader analysisAntagonist activity at human histamine H4 receptor expressed in SK-N-MC cells assessed as reduction of histamine-induced inhibition of cAMP-mediated beta-galactosidase reporter gene activity treated 10 mins prior to histamine challenge by microplate reader analysis
ChEMBL 261 3 2 5 1.5 CN[C@@H]1CCN(c2cc(C3CCCC3)nc(N)n2)C1 10.1021/jm401727m
24798144 110181 None 0 Human Functional pKd = 9.5 9.5 - 1
Antagonist activity at human histamine H4 receptor expressed in SK-N-MC cells assessed as reduction of histamine-induced inhibition of cAMP-mediated beta-galactosidase reporter gene activity treated 10 mins prior to histamine challenge by microplate reader analysisAntagonist activity at human histamine H4 receptor expressed in SK-N-MC cells assessed as reduction of histamine-induced inhibition of cAMP-mediated beta-galactosidase reporter gene activity treated 10 mins prior to histamine challenge by microplate reader analysis
ChEMBL 247 2 2 5 1.1 Nc1nc(C2CCCC2)cc(N2CCNCC2)n1 10.1021/jm401727m
CHEMBL3236553 110181 None 0 Human Functional pKd = 9.5 9.5 - 1
Antagonist activity at human histamine H4 receptor expressed in SK-N-MC cells assessed as reduction of histamine-induced inhibition of cAMP-mediated beta-galactosidase reporter gene activity treated 10 mins prior to histamine challenge by microplate reader analysisAntagonist activity at human histamine H4 receptor expressed in SK-N-MC cells assessed as reduction of histamine-induced inhibition of cAMP-mediated beta-galactosidase reporter gene activity treated 10 mins prior to histamine challenge by microplate reader analysis
ChEMBL 247 2 2 5 1.1 Nc1nc(C2CCCC2)cc(N2CCNCC2)n1 10.1021/jm401727m
53257796 110203 None 0 Human Functional pKd = 9.4 9.4 - 0
Antagonist activity at human histamine H4 receptor expressed in SK-N-MC cells assessed as reduction of histamine-induced inhibition of cAMP-mediated beta-galactosidase reporter gene activity treated 10 mins prior to histamine challenge by microplate reader analysisAntagonist activity at human histamine H4 receptor expressed in SK-N-MC cells assessed as reduction of histamine-induced inhibition of cAMP-mediated beta-galactosidase reporter gene activity treated 10 mins prior to histamine challenge by microplate reader analysis
ChEMBL 247 3 2 5 1.1 CN[C@@H]1CCN(c2cc(C3CCC3)nc(N)n2)C1 10.1021/jm401727m
CHEMBL3236575 110203 None 0 Human Functional pKd = 9.4 9.4 - 0
Antagonist activity at human histamine H4 receptor expressed in SK-N-MC cells assessed as reduction of histamine-induced inhibition of cAMP-mediated beta-galactosidase reporter gene activity treated 10 mins prior to histamine challenge by microplate reader analysisAntagonist activity at human histamine H4 receptor expressed in SK-N-MC cells assessed as reduction of histamine-induced inhibition of cAMP-mediated beta-galactosidase reporter gene activity treated 10 mins prior to histamine challenge by microplate reader analysis
ChEMBL 247 3 2 5 1.1 CN[C@@H]1CCN(c2cc(C3CCC3)nc(N)n2)C1 10.1021/jm401727m
54587790 61560 None 0 Human Functional pKd = 9.4 9.4 - 0
Antagonist activity at human histamine H4 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 6 hrsAntagonist activity at human histamine H4 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 6 hrs
ChEMBL 276 4 3 6 1.2 CN[C@@H]1CCN(c2cc(NC3CCCC3)nc(N)n2)C1 10.1016/j.bmcl.2011.03.017
CHEMBL1770980 61560 None 0 Human Functional pKd = 9.4 9.4 - 0
Antagonist activity at human histamine H4 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 6 hrsAntagonist activity at human histamine H4 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 6 hrs
ChEMBL 276 4 3 6 1.2 CN[C@@H]1CCN(c2cc(NC3CCCC3)nc(N)n2)C1 10.1016/j.bmcl.2011.03.017
24745337 61559 None 0 Human Functional pKd = 9.3 9.3 - 0
Antagonist activity at human histamine H4 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 6 hrsAntagonist activity at human histamine H4 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 6 hrs
ChEMBL 264 5 3 6 0.9 CN[C@@H]1CCN(c2cc(NCC(C)C)nc(N)n2)C1 10.1016/j.bmcl.2011.03.017
CHEMBL1770979 61559 None 0 Human Functional pKd = 9.3 9.3 - 0
Antagonist activity at human histamine H4 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 6 hrsAntagonist activity at human histamine H4 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 6 hrs
ChEMBL 264 5 3 6 0.9 CN[C@@H]1CCN(c2cc(NCC(C)C)nc(N)n2)C1 10.1016/j.bmcl.2011.03.017
59777338 110184 None 0 Human Functional pKd = 9.2 9.2 - 0
Antagonist activity at human histamine H4 receptor expressed in SK-N-MC cells assessed as reduction of histamine-induced inhibition of cAMP-mediated beta-galactosidase reporter gene activity treated 10 mins prior to histamine challenge by microplate reader analysisAntagonist activity at human histamine H4 receptor expressed in SK-N-MC cells assessed as reduction of histamine-induced inhibition of cAMP-mediated beta-galactosidase reporter gene activity treated 10 mins prior to histamine challenge by microplate reader analysis
ChEMBL 247 2 2 5 1.3 Nc1nc(C2CCCC2)cc(N2CC[C@@H](N)C2)n1 10.1021/jm401727m
CHEMBL3236556 110184 None 0 Human Functional pKd = 9.2 9.2 - 0
Antagonist activity at human histamine H4 receptor expressed in SK-N-MC cells assessed as reduction of histamine-induced inhibition of cAMP-mediated beta-galactosidase reporter gene activity treated 10 mins prior to histamine challenge by microplate reader analysisAntagonist activity at human histamine H4 receptor expressed in SK-N-MC cells assessed as reduction of histamine-induced inhibition of cAMP-mediated beta-galactosidase reporter gene activity treated 10 mins prior to histamine challenge by microplate reader analysis
ChEMBL 247 2 2 5 1.3 Nc1nc(C2CCCC2)cc(N2CC[C@@H](N)C2)n1 10.1021/jm401727m
44547268 117176 None 0 Human Functional pKd = 9.2 9.2 - 0
Antagonist activity at human recombinant histamine H4 receptor expressed in SK-N-MC cells assessed as inhibition of forskolin-stimulated cAMP-mediated reporter gene activityAntagonist activity at human recombinant histamine H4 receptor expressed in SK-N-MC cells assessed as inhibition of forskolin-stimulated cAMP-mediated reporter gene activity
ChEMBL 248 5 2 4 1.9 CN[C@@H]1CCN(c2ccnc(NCC(C)C)c2)C1 10.1016/j.bmcl.2014.12.027
CHEMBL3393526 117176 None 0 Human Functional pKd = 9.2 9.2 - 0
Antagonist activity at human recombinant histamine H4 receptor expressed in SK-N-MC cells assessed as inhibition of forskolin-stimulated cAMP-mediated reporter gene activityAntagonist activity at human recombinant histamine H4 receptor expressed in SK-N-MC cells assessed as inhibition of forskolin-stimulated cAMP-mediated reporter gene activity
ChEMBL 248 5 2 4 1.9 CN[C@@H]1CCN(c2ccnc(NCC(C)C)c2)C1 10.1016/j.bmcl.2014.12.027
58227340 117182 None 0 Human Functional pKd = 9 9.0 - 0
Antagonist activity at human recombinant histamine H4 receptor expressed in SK-N-MC cells assessed as inhibition of forskolin-stimulated cAMP-mediated reporter gene activityAntagonist activity at human recombinant histamine H4 receptor expressed in SK-N-MC cells assessed as inhibition of forskolin-stimulated cAMP-mediated reporter gene activity
ChEMBL 260 4 2 4 2.2 CN[C@@H]1CCN(c2ccnc(NC3CCCC3)c2)C1 10.1016/j.bmcl.2014.12.027
CHEMBL3393532 117182 None 0 Human Functional pKd = 9 9.0 - 0
Antagonist activity at human recombinant histamine H4 receptor expressed in SK-N-MC cells assessed as inhibition of forskolin-stimulated cAMP-mediated reporter gene activityAntagonist activity at human recombinant histamine H4 receptor expressed in SK-N-MC cells assessed as inhibition of forskolin-stimulated cAMP-mediated reporter gene activity
ChEMBL 260 4 2 4 2.2 CN[C@@H]1CCN(c2ccnc(NC3CCCC3)c2)C1 10.1016/j.bmcl.2014.12.027
58227200 117185 None 0 Human Functional pKd = 9 9.0 - 0
Antagonist activity at human recombinant histamine H4 receptor expressed in SK-N-MC cells assessed as inhibition of forskolin-stimulated cAMP-mediated reporter gene activityAntagonist activity at human recombinant histamine H4 receptor expressed in SK-N-MC cells assessed as inhibition of forskolin-stimulated cAMP-mediated reporter gene activity
ChEMBL 286 4 2 4 2.5 CN[C@H]1CCN(c2ccnc(NC3CC4CCC3C4)c2)C1 10.1016/j.bmcl.2014.12.027
CHEMBL3393535 117185 None 0 Human Functional pKd = 9 9.0 - 0
Antagonist activity at human recombinant histamine H4 receptor expressed in SK-N-MC cells assessed as inhibition of forskolin-stimulated cAMP-mediated reporter gene activityAntagonist activity at human recombinant histamine H4 receptor expressed in SK-N-MC cells assessed as inhibition of forskolin-stimulated cAMP-mediated reporter gene activity
ChEMBL 286 4 2 4 2.5 CN[C@H]1CCN(c2ccnc(NC3CC4CCC3C4)c2)C1 10.1016/j.bmcl.2014.12.027
54585781 61581 None 0 Human Functional pKd = 8.9 8.9 - 0
Antagonist activity at human histamine H4 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 6 hrsAntagonist activity at human histamine H4 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 6 hrs
ChEMBL 264 4 2 6 0.9 CC(C)CNc1cc(N2CCN(C)CC2)nc(N)n1 10.1016/j.bmcl.2011.03.017
CHEMBL1771000 61581 None 0 Human Functional pKd = 8.9 8.9 - 0
Antagonist activity at human histamine H4 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 6 hrsAntagonist activity at human histamine H4 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 6 hrs
ChEMBL 264 4 2 6 0.9 CC(C)CNc1cc(N2CCN(C)CC2)nc(N)n1 10.1016/j.bmcl.2011.03.017
54583873 61549 None 0 Human Functional pKd = 8.8 8.8 - 0
Antagonist activity at human histamine H4 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 6 hrsAntagonist activity at human histamine H4 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 6 hrs
ChEMBL 249 4 3 5 1.3 CN[C@@H]1CCN(c2cc(N)nc(NC(C)C)c2)C1 10.1016/j.bmcl.2011.03.017
CHEMBL1770969 61549 None 0 Human Functional pKd = 8.8 8.8 - 0
Antagonist activity at human histamine H4 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 6 hrsAntagonist activity at human histamine H4 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 6 hrs
ChEMBL 249 4 3 5 1.3 CN[C@@H]1CCN(c2cc(N)nc(NC(C)C)c2)C1 10.1016/j.bmcl.2011.03.017
54587787 61551 None 0 Human Functional pKd = 8.8 8.8 - 0
Antagonist activity at human histamine H4 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 6 hrsAntagonist activity at human histamine H4 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 6 hrs
ChEMBL 263 5 3 5 1.5 CN[C@@H]1CCN(c2cc(N)nc(NCC(C)C)c2)C1 10.1016/j.bmcl.2011.03.017
CHEMBL1770971 61551 None 0 Human Functional pKd = 8.8 8.8 - 0
Antagonist activity at human histamine H4 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 6 hrsAntagonist activity at human histamine H4 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 6 hrs
ChEMBL 263 5 3 5 1.5 CN[C@@H]1CCN(c2cc(N)nc(NCC(C)C)c2)C1 10.1016/j.bmcl.2011.03.017
54581940 61572 None 0 Human Functional pKd = 8.8 8.8 - 0
Antagonist activity at human histamine H4 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 6 hrsAntagonist activity at human histamine H4 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 6 hrs
ChEMBL 264 5 3 6 0.9 CN[C@@H]1CCN(c2cc(N)nc(NCC(C)C)n2)C1 10.1016/j.bmcl.2011.03.017
CHEMBL1770992 61572 None 0 Human Functional pKd = 8.8 8.8 - 0
Antagonist activity at human histamine H4 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 6 hrsAntagonist activity at human histamine H4 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 6 hrs
ChEMBL 264 5 3 6 0.9 CN[C@@H]1CCN(c2cc(N)nc(NCC(C)C)n2)C1 10.1016/j.bmcl.2011.03.017
25130912 188847 None 0 Human Functional pKd = 8.7 8.7 - 1
Antagonist activity at human histamine H4 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 6 hrsAntagonist activity at human histamine H4 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 6 hrs
ChEMBL 262 2 1 6 0.4 CN1CCN(c2cc(N3CCCC3)nc(N)n2)CC1 10.1016/j.bmcl.2011.03.017
CHEMBL505061 188847 None 0 Human Functional pKd = 8.7 8.7 - 1
Antagonist activity at human histamine H4 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 6 hrsAntagonist activity at human histamine H4 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 6 hrs
ChEMBL 262 2 1 6 0.4 CN1CCN(c2cc(N3CCCC3)nc(N)n2)CC1 10.1016/j.bmcl.2011.03.017
23653543 68070 None 0 Human Functional pKd = 8.7 8.7 - 0
Antagonist activity at recombinant human histamine H4 receptorAntagonist activity at recombinant human histamine H4 receptor
ChEMBL 317 1 1 6 2.4 CN1CCN(c2nc(N)nc3c2oc2ccc(Cl)cc23)CC1 10.1016/j.bmcl.2011.08.014
CHEMBL1914541 68070 None 0 Human Functional pKd = 8.7 8.7 - 0
Antagonist activity at recombinant human histamine H4 receptorAntagonist activity at recombinant human histamine H4 receptor
ChEMBL 317 1 1 6 2.4 CN1CCN(c2nc(N)nc3c2oc2ccc(Cl)cc23)CC1 10.1016/j.bmcl.2011.08.014
24994636 110193 None 0 Human Functional pKd = 8 8.0 - 0
Antagonist activity at human histamine H4 receptor expressed in SK-N-MC cells assessed as reduction of histamine-induced inhibition of cAMP-mediated beta-galactosidase reporter gene activity treated 10 mins prior to histamine challenge by microplate reader analysisAntagonist activity at human histamine H4 receptor expressed in SK-N-MC cells assessed as reduction of histamine-induced inhibition of cAMP-mediated beta-galactosidase reporter gene activity treated 10 mins prior to histamine challenge by microplate reader analysis
ChEMBL 277 3 3 6 0.5 CN[C@H]1CN(c2cc(C3CCCC3)nc(N)n2)C[C@@H]1O 10.1021/jm401727m
CHEMBL3236565 110193 None 0 Human Functional pKd = 8 8.0 - 0
Antagonist activity at human histamine H4 receptor expressed in SK-N-MC cells assessed as reduction of histamine-induced inhibition of cAMP-mediated beta-galactosidase reporter gene activity treated 10 mins prior to histamine challenge by microplate reader analysisAntagonist activity at human histamine H4 receptor expressed in SK-N-MC cells assessed as reduction of histamine-induced inhibition of cAMP-mediated beta-galactosidase reporter gene activity treated 10 mins prior to histamine challenge by microplate reader analysis
ChEMBL 277 3 3 6 0.5 CN[C@H]1CN(c2cc(C3CCCC3)nc(N)n2)C[C@@H]1O 10.1021/jm401727m
42624149 110196 None 0 Human Functional pKd = 8 8.0 - 0
Antagonist activity at human histamine H4 receptor expressed in SK-N-MC cells assessed as reduction of histamine-induced inhibition of cAMP-mediated beta-galactosidase reporter gene activity treated 10 mins prior to histamine challenge by microplate reader analysisAntagonist activity at human histamine H4 receptor expressed in SK-N-MC cells assessed as reduction of histamine-induced inhibition of cAMP-mediated beta-galactosidase reporter gene activity treated 10 mins prior to histamine challenge by microplate reader analysis
ChEMBL 221 3 2 5 0.4 CCc1cc(N2CC[C@@H](NC)C2)nc(N)n1 10.1021/jm401727m
CHEMBL3236568 110196 None 0 Human Functional pKd = 8 8.0 - 0
Antagonist activity at human histamine H4 receptor expressed in SK-N-MC cells assessed as reduction of histamine-induced inhibition of cAMP-mediated beta-galactosidase reporter gene activity treated 10 mins prior to histamine challenge by microplate reader analysisAntagonist activity at human histamine H4 receptor expressed in SK-N-MC cells assessed as reduction of histamine-induced inhibition of cAMP-mediated beta-galactosidase reporter gene activity treated 10 mins prior to histamine challenge by microplate reader analysis
ChEMBL 221 3 2 5 0.4 CCc1cc(N2CC[C@@H](NC)C2)nc(N)n1 10.1021/jm401727m
59777262 110200 None 0 Human Functional pKd = 8 8.0 - 0
Antagonist activity at human histamine H4 receptor expressed in SK-N-MC cells assessed as reduction of histamine-induced inhibition of cAMP-mediated beta-galactosidase reporter gene activity treated 10 mins prior to histamine challenge by microplate reader analysisAntagonist activity at human histamine H4 receptor expressed in SK-N-MC cells assessed as reduction of histamine-induced inhibition of cAMP-mediated beta-galactosidase reporter gene activity treated 10 mins prior to histamine challenge by microplate reader analysis
ChEMBL 283 4 2 5 1.4 CN[C@@H]1CCN(c2cc(Cc3ccccc3)nc(N)n2)C1 10.1021/jm401727m
CHEMBL3236572 110200 None 0 Human Functional pKd = 8 8.0 - 0
Antagonist activity at human histamine H4 receptor expressed in SK-N-MC cells assessed as reduction of histamine-induced inhibition of cAMP-mediated beta-galactosidase reporter gene activity treated 10 mins prior to histamine challenge by microplate reader analysisAntagonist activity at human histamine H4 receptor expressed in SK-N-MC cells assessed as reduction of histamine-induced inhibition of cAMP-mediated beta-galactosidase reporter gene activity treated 10 mins prior to histamine challenge by microplate reader analysis
ChEMBL 283 4 2 5 1.4 CN[C@@H]1CCN(c2cc(Cc3ccccc3)nc(N)n2)C1 10.1021/jm401727m
54584824 61557 None 0 Human Functional pKd = 8 8.0 - 0
Antagonist activity at human histamine H4 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 6 hrsAntagonist activity at human histamine H4 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 6 hrs
ChEMBL 250 4 3 6 0.7 CN[C@@H]1CCN(c2cc(NC(C)C)nc(N)n2)C1 10.1016/j.bmcl.2011.03.017
CHEMBL1770977 61557 None 0 Human Functional pKd = 8 8.0 - 0
Antagonist activity at human histamine H4 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 6 hrsAntagonist activity at human histamine H4 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 6 hrs
ChEMBL 250 4 3 6 0.7 CN[C@@H]1CCN(c2cc(NC(C)C)nc(N)n2)C1 10.1016/j.bmcl.2011.03.017
58227337 117203 None 0 Human Functional pKd = 8 8.0 - 0
Antagonist activity at human recombinant histamine H4 receptor expressed in SK-N-MC cells assessed as inhibition of forskolin-stimulated cAMP-mediated reporter gene activityAntagonist activity at human recombinant histamine H4 receptor expressed in SK-N-MC cells assessed as inhibition of forskolin-stimulated cAMP-mediated reporter gene activity
ChEMBL 261 4 2 5 1.6 CN[C@@H]1CCN(c2cnnc(NC3CCCC3)c2)C1 10.1016/j.bmcl.2014.12.027
CHEMBL3393553 117203 None 0 Human Functional pKd = 8 8.0 - 0
Antagonist activity at human recombinant histamine H4 receptor expressed in SK-N-MC cells assessed as inhibition of forskolin-stimulated cAMP-mediated reporter gene activityAntagonist activity at human recombinant histamine H4 receptor expressed in SK-N-MC cells assessed as inhibition of forskolin-stimulated cAMP-mediated reporter gene activity
ChEMBL 261 4 2 5 1.6 CN[C@@H]1CCN(c2cnnc(NC3CCCC3)c2)C1 10.1016/j.bmcl.2014.12.027
58227259 117206 None 0 Human Functional pKd = 8 8.0 - 1
Antagonist activity at human recombinant histamine H4 receptor expressed in SK-N-MC cells assessed as inhibition of forskolin-stimulated cAMP-mediated reporter gene activityAntagonist activity at human recombinant histamine H4 receptor expressed in SK-N-MC cells assessed as inhibition of forskolin-stimulated cAMP-mediated reporter gene activity
ChEMBL 287 4 2 5 1.9 CN[C@@H]1CCN(c2cnnc(NC3CC4CCC3C4)c2)C1 10.1016/j.bmcl.2014.12.027
CHEMBL3393556 117206 None 0 Human Functional pKd = 8 8.0 - 1
Antagonist activity at human recombinant histamine H4 receptor expressed in SK-N-MC cells assessed as inhibition of forskolin-stimulated cAMP-mediated reporter gene activityAntagonist activity at human recombinant histamine H4 receptor expressed in SK-N-MC cells assessed as inhibition of forskolin-stimulated cAMP-mediated reporter gene activity
ChEMBL 287 4 2 5 1.9 CN[C@@H]1CCN(c2cnnc(NC3CC4CCC3C4)c2)C1 10.1016/j.bmcl.2014.12.027
24798144 110181 None 0 Mouse Functional pKd = 8 8.0 - 1
Antagonist activity at mouse histamine H4 receptor expressed in SK-N-MC cells assessed as reduction of histamine-induced inhibition of cAMP-mediated beta-galactosidase reporter gene activity treated 10 mins prior to histamine challenge by microplate reader analysisAntagonist activity at mouse histamine H4 receptor expressed in SK-N-MC cells assessed as reduction of histamine-induced inhibition of cAMP-mediated beta-galactosidase reporter gene activity treated 10 mins prior to histamine challenge by microplate reader analysis
ChEMBL 247 2 2 5 1.1 Nc1nc(C2CCCC2)cc(N2CCNCC2)n1 10.1021/jm401727m
CHEMBL3236553 110181 None 0 Mouse Functional pKd = 8 8.0 - 1
Antagonist activity at mouse histamine H4 receptor expressed in SK-N-MC cells assessed as reduction of histamine-induced inhibition of cAMP-mediated beta-galactosidase reporter gene activity treated 10 mins prior to histamine challenge by microplate reader analysisAntagonist activity at mouse histamine H4 receptor expressed in SK-N-MC cells assessed as reduction of histamine-induced inhibition of cAMP-mediated beta-galactosidase reporter gene activity treated 10 mins prior to histamine challenge by microplate reader analysis
ChEMBL 247 2 2 5 1.1 Nc1nc(C2CCCC2)cc(N2CCNCC2)n1 10.1021/jm401727m
24826766 68123 None 0 Human Functional pKd = 8 8.0 - 0
Antagonist activity at recombinant human histamine H4 receptorAntagonist activity at recombinant human histamine H4 receptor
ChEMBL 317 2 2 6 2.4 CNC1CCN(c2nc(N)nc3c2oc2ccc(Cl)cc23)C1 10.1016/j.bmcl.2011.08.014
CHEMBL1914750 68123 None 0 Human Functional pKd = 8 8.0 - 0
Antagonist activity at recombinant human histamine H4 receptorAntagonist activity at recombinant human histamine H4 receptor
ChEMBL 317 2 2 6 2.4 CNC1CCN(c2nc(N)nc3c2oc2ccc(Cl)cc23)C1 10.1016/j.bmcl.2011.08.014
9944571 117081 None 0 Human Functional pKd = 8 8.0 - 0
Antagonistic activity at human histamine H4 receptor in SK-N-MC cells by inhibition of forskolin-stimulated cAMP-mediated reporter gene activityAntagonistic activity at human histamine H4 receptor in SK-N-MC cells by inhibition of forskolin-stimulated cAMP-mediated reporter gene activity
ChEMBL 311 1 1 2 2.9 CN1CCN(C(=O)c2cc3cc(Cl)cc(Cl)c3[nH]2)CC1 10.1021/jm0502081
CHEMBL338937 117081 None 0 Human Functional pKd = 8 8.0 - 0
Antagonistic activity at human histamine H4 receptor in SK-N-MC cells by inhibition of forskolin-stimulated cAMP-mediated reporter gene activityAntagonistic activity at human histamine H4 receptor in SK-N-MC cells by inhibition of forskolin-stimulated cAMP-mediated reporter gene activity
ChEMBL 311 1 1 2 2.9 CN1CCN(C(=O)c2cc3cc(Cl)cc(Cl)c3[nH]2)CC1 10.1021/jm0502081
24994634 2142 None 30 Human Functional pKd = 7.9 7.9 - 1
Antagonist activity at human histamine H4 receptor expressed in SK-N-MC cells assessed as reduction of histamine-induced inhibition of cAMP-mediated beta-galactosidase reporter gene activity treated 10 mins prior to histamine challenge by microplate reader analysisAntagonist activity at human histamine H4 receptor expressed in SK-N-MC cells assessed as reduction of histamine-induced inhibition of cAMP-mediated beta-galactosidase reporter gene activity treated 10 mins prior to histamine challenge by microplate reader analysis
ChEMBL 221 2 2 5 0.7 N[C@@H]1CCN(C1)c1cc(nc(n1)N)C(C)C 10.1021/jm401727m
8984 2142 None 30 Human Functional pKd = 7.9 7.9 - 1
Antagonist activity at human histamine H4 receptor expressed in SK-N-MC cells assessed as reduction of histamine-induced inhibition of cAMP-mediated beta-galactosidase reporter gene activity treated 10 mins prior to histamine challenge by microplate reader analysisAntagonist activity at human histamine H4 receptor expressed in SK-N-MC cells assessed as reduction of histamine-induced inhibition of cAMP-mediated beta-galactosidase reporter gene activity treated 10 mins prior to histamine challenge by microplate reader analysis
ChEMBL 221 2 2 5 0.7 N[C@@H]1CCN(C1)c1cc(nc(n1)N)C(C)C 10.1021/jm401727m
CHEMBL3236549 2142 None 30 Human Functional pKd = 7.9 7.9 - 1
Antagonist activity at human histamine H4 receptor expressed in SK-N-MC cells assessed as reduction of histamine-induced inhibition of cAMP-mediated beta-galactosidase reporter gene activity treated 10 mins prior to histamine challenge by microplate reader analysisAntagonist activity at human histamine H4 receptor expressed in SK-N-MC cells assessed as reduction of histamine-induced inhibition of cAMP-mediated beta-galactosidase reporter gene activity treated 10 mins prior to histamine challenge by microplate reader analysis
ChEMBL 221 2 2 5 0.7 N[C@@H]1CCN(C1)c1cc(nc(n1)N)C(C)C 10.1021/jm401727m
53258370 110197 None 0 Human Functional pKd = 7.9 7.9 - 0
Antagonist activity at human histamine H4 receptor expressed in SK-N-MC cells assessed as reduction of histamine-induced inhibition of cAMP-mediated beta-galactosidase reporter gene activity treated 10 mins prior to histamine challenge by microplate reader analysisAntagonist activity at human histamine H4 receptor expressed in SK-N-MC cells assessed as reduction of histamine-induced inhibition of cAMP-mediated beta-galactosidase reporter gene activity treated 10 mins prior to histamine challenge by microplate reader analysis
ChEMBL 207 2 2 5 0.2 CCc1cc(N2CC[C@@H](N)C2)nc(N)n1 10.1021/jm401727m
CHEMBL3236569 110197 None 0 Human Functional pKd = 7.9 7.9 - 0
Antagonist activity at human histamine H4 receptor expressed in SK-N-MC cells assessed as reduction of histamine-induced inhibition of cAMP-mediated beta-galactosidase reporter gene activity treated 10 mins prior to histamine challenge by microplate reader analysisAntagonist activity at human histamine H4 receptor expressed in SK-N-MC cells assessed as reduction of histamine-induced inhibition of cAMP-mediated beta-galactosidase reporter gene activity treated 10 mins prior to histamine challenge by microplate reader analysis
ChEMBL 207 2 2 5 0.2 CCc1cc(N2CC[C@@H](N)C2)nc(N)n1 10.1021/jm401727m
24994635 110198 None 0 Human Functional pKd = 7.9 7.9 - 0
Antagonist activity at human histamine H4 receptor expressed in SK-N-MC cells assessed as reduction of histamine-induced inhibition of cAMP-mediated beta-galactosidase reporter gene activity treated 10 mins prior to histamine challenge by microplate reader analysisAntagonist activity at human histamine H4 receptor expressed in SK-N-MC cells assessed as reduction of histamine-induced inhibition of cAMP-mediated beta-galactosidase reporter gene activity treated 10 mins prior to histamine challenge by microplate reader analysis
ChEMBL 235 3 2 5 1.0 CN[C@@H]1CCN(c2cc(C(C)C)nc(N)n2)C1 10.1021/jm401727m
CHEMBL3236570 110198 None 0 Human Functional pKd = 7.9 7.9 - 0
Antagonist activity at human histamine H4 receptor expressed in SK-N-MC cells assessed as reduction of histamine-induced inhibition of cAMP-mediated beta-galactosidase reporter gene activity treated 10 mins prior to histamine challenge by microplate reader analysisAntagonist activity at human histamine H4 receptor expressed in SK-N-MC cells assessed as reduction of histamine-induced inhibition of cAMP-mediated beta-galactosidase reporter gene activity treated 10 mins prior to histamine challenge by microplate reader analysis
ChEMBL 235 3 2 5 1.0 CN[C@@H]1CCN(c2cc(C(C)C)nc(N)n2)C1 10.1021/jm401727m
54582865 61539 None 0 Human Functional pKd = 7.9 7.9 - 0
Antagonist activity at human histamine H4 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 6 hrsAntagonist activity at human histamine H4 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 6 hrs
ChEMBL 276 4 3 6 1.2 CN[C@@H]1CCN(c2cc(N)nc(NC3CCCC3)n2)C1 10.1016/j.bmcl.2011.03.017
CHEMBL1770959 61539 None 0 Human Functional pKd = 7.9 7.9 - 0
Antagonist activity at human histamine H4 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 6 hrsAntagonist activity at human histamine H4 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 6 hrs
ChEMBL 276 4 3 6 1.2 CN[C@@H]1CCN(c2cc(N)nc(NC3CCCC3)n2)C1 10.1016/j.bmcl.2011.03.017
54584825 61570 None 0 Human Functional pKd = 7.9 7.9 - 0
Antagonist activity at human histamine H4 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 6 hrsAntagonist activity at human histamine H4 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 6 hrs
ChEMBL 250 4 3 6 0.7 CN[C@@H]1CCN(c2cc(N)nc(NC(C)C)n2)C1 10.1016/j.bmcl.2011.03.017
CHEMBL1770990 61570 None 0 Human Functional pKd = 7.9 7.9 - 0
Antagonist activity at human histamine H4 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 6 hrsAntagonist activity at human histamine H4 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 6 hrs
ChEMBL 250 4 3 6 0.7 CN[C@@H]1CCN(c2cc(N)nc(NC(C)C)n2)C1 10.1016/j.bmcl.2011.03.017
11587279 125118 None 3 Human Functional pKd = 7.9 7.9 - 0
Antagonistic activity at human histamine H4 receptor in SK-N-MC cells by inhibition of forskolin-stimulated cAMP-mediated reporter gene activityAntagonistic activity at human histamine H4 receptor in SK-N-MC cells by inhibition of forskolin-stimulated cAMP-mediated reporter gene activity
ChEMBL 283 1 1 3 2.3 CN1CCN(C(=O)c2cc3cc(Cl)sc3[nH]2)CC1 10.1021/jm0502081
CHEMBL364400 125118 None 3 Human Functional pKd = 7.9 7.9 - 0
Antagonistic activity at human histamine H4 receptor in SK-N-MC cells by inhibition of forskolin-stimulated cAMP-mediated reporter gene activityAntagonistic activity at human histamine H4 receptor in SK-N-MC cells by inhibition of forskolin-stimulated cAMP-mediated reporter gene activity
ChEMBL 283 1 1 3 2.3 CN1CCN(C(=O)c2cc3cc(Cl)sc3[nH]2)CC1 10.1021/jm0502081
46890627 6591 None 0 Human Functional pKd = 7.9 7.9 - 0
Intrinsic activity at human histamine H4 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-induced cAMP responsive element-beta-galactosidase activity after 6 hrs by colorimetric cAMP assayIntrinsic activity at human histamine H4 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-induced cAMP responsive element-beta-galactosidase activity after 6 hrs by colorimetric cAMP assay
ChEMBL 408 6 2 4 4.0 Cc1cc(OCCCN2CC3CCNC3C2)ccc1-c1nc2c(C)c(F)ccc2[nH]1 10.1016/j.bmcl.2010.04.017
CHEMBL1083098 6591 None 0 Human Functional pKd = 7.9 7.9 - 0
Intrinsic activity at human histamine H4 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-induced cAMP responsive element-beta-galactosidase activity after 6 hrs by colorimetric cAMP assayIntrinsic activity at human histamine H4 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-induced cAMP responsive element-beta-galactosidase activity after 6 hrs by colorimetric cAMP assay
ChEMBL 408 6 2 4 4.0 Cc1cc(OCCCN2CC3CCNC3C2)ccc1-c1nc2c(C)c(F)ccc2[nH]1 10.1016/j.bmcl.2010.04.017
66740470 109854 None 0 Human Functional pKd = 6.9 6.9 - 0
Antagonist activity at human histamine H4 receptor expressed in SK-N-MC cells assessed as reduction of histamine-induced inhibition of cAMP-mediated beta-galactosidase reporter gene activity treated 10 mins prior to histamine challenge by microplate reader analysisAntagonist activity at human histamine H4 receptor expressed in SK-N-MC cells assessed as reduction of histamine-induced inhibition of cAMP-mediated beta-galactosidase reporter gene activity treated 10 mins prior to histamine challenge by microplate reader analysis
ChEMBL 289 2 2 6 0.9 Nc1nc(C2CCCC2)cc(N2C[C@H]3NCCO[C@@H]3C2)n1 10.1021/jm401727m
CHEMBL3233048 109854 None 0 Human Functional pKd = 6.9 6.9 - 0
Antagonist activity at human histamine H4 receptor expressed in SK-N-MC cells assessed as reduction of histamine-induced inhibition of cAMP-mediated beta-galactosidase reporter gene activity treated 10 mins prior to histamine challenge by microplate reader analysisAntagonist activity at human histamine H4 receptor expressed in SK-N-MC cells assessed as reduction of histamine-induced inhibition of cAMP-mediated beta-galactosidase reporter gene activity treated 10 mins prior to histamine challenge by microplate reader analysis
ChEMBL 289 2 2 6 0.9 Nc1nc(C2CCCC2)cc(N2C[C@H]3NCCO[C@@H]3C2)n1 10.1021/jm401727m
11687917 14971 None 0 Human Functional pKd = 6.9 6.9 - 0
Antagonistic activity at human histamine H4 receptor in SK-N-MC cells by inhibition of forskolin-stimulated cAMP-mediated reporter gene activityAntagonistic activity at human histamine H4 receptor in SK-N-MC cells by inhibition of forskolin-stimulated cAMP-mediated reporter gene activity
ChEMBL 292 1 1 3 1.9 Cc1cc(Cl)c2nc(C(=O)N3CCN(C)CC3)[nH]c2c1 10.1021/jm0502081
CHEMBL120854 14971 None 0 Human Functional pKd = 6.9 6.9 - 0
Antagonistic activity at human histamine H4 receptor in SK-N-MC cells by inhibition of forskolin-stimulated cAMP-mediated reporter gene activityAntagonistic activity at human histamine H4 receptor in SK-N-MC cells by inhibition of forskolin-stimulated cAMP-mediated reporter gene activity
ChEMBL 292 1 1 3 1.9 Cc1cc(Cl)c2nc(C(=O)N3CCN(C)CC3)[nH]c2c1 10.1021/jm0502081
9966927 18882 None 3 Human Functional pKd = 6.9 6.9 - 0
Antagonistic activity at human histamine H4 receptor in SK-N-MC cells by inhibition of forskolin-stimulated cAMP-mediated reporter gene activityAntagonistic activity at human histamine H4 receptor in SK-N-MC cells by inhibition of forskolin-stimulated cAMP-mediated reporter gene activity
ChEMBL 321 1 1 2 2.3 CN1CCN(C(=O)c2cc3cccc(Br)c3[nH]2)CC1 10.1021/jm0502081
CHEMBL128252 18882 None 3 Human Functional pKd = 6.9 6.9 - 0
Antagonistic activity at human histamine H4 receptor in SK-N-MC cells by inhibition of forskolin-stimulated cAMP-mediated reporter gene activityAntagonistic activity at human histamine H4 receptor in SK-N-MC cells by inhibition of forskolin-stimulated cAMP-mediated reporter gene activity
ChEMBL 321 1 1 2 2.3 CN1CCN(C(=O)c2cc3cccc(Br)c3[nH]2)CC1 10.1021/jm0502081
54581938 61552 None 0 Human Functional pKd = 7.8 7.8 - 0
Antagonist activity at human histamine H4 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 6 hrsAntagonist activity at human histamine H4 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 6 hrs
ChEMBL 261 3 2 5 1.1 CN[C@@H]1CCN(c2cc(N)nc(N3CCCC3)c2)C1 10.1016/j.bmcl.2011.03.017
CHEMBL1770972 61552 None 0 Human Functional pKd = 7.8 7.8 - 0
Antagonist activity at human histamine H4 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 6 hrsAntagonist activity at human histamine H4 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 6 hrs
ChEMBL 261 3 2 5 1.1 CN[C@@H]1CCN(c2cc(N)nc(N3CCCC3)c2)C1 10.1016/j.bmcl.2011.03.017
67087450 117200 None 0 Human Functional pKd = 7.8 7.8 - 1
Antagonist activity at human recombinant histamine H4 receptor expressed in SK-N-MC cells assessed as inhibition of forskolin-stimulated cAMP-mediated reporter gene activityAntagonist activity at human recombinant histamine H4 receptor expressed in SK-N-MC cells assessed as inhibition of forskolin-stimulated cAMP-mediated reporter gene activity
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 117200 None 0 Human Functional pKd = 7.8 7.8 - 1
Antagonist activity at human recombinant histamine H4 receptor expressed in SK-N-MC cells assessed as inhibition of forskolin-stimulated cAMP-mediated reporter gene activityAntagonist activity at human recombinant histamine H4 receptor expressed in SK-N-MC cells assessed as inhibition of forskolin-stimulated cAMP-mediated reporter gene activity
ChEMBL 249 5 2 5 1.3 CN[C@@H]1CCN(c2cnnc(NCC(C)C)c2)C1 10.1016/j.bmcl.2014.12.027
11594278 14696 None 0 Human Functional pKd = 7.8 7.8 - 0
Antagonistic activity at human histamine H4 receptor in SK-N-MC cells by inhibition of forskolin-stimulated cAMP-mediated reporter gene activityAntagonistic activity at human histamine H4 receptor in SK-N-MC cells by inhibition of forskolin-stimulated cAMP-mediated reporter gene activity
ChEMBL 276 1 1 3 1.4 Cc1c(F)ccc2[nH]c(C(=O)N3CCN(C)CC3)nc12 10.1021/jm0502081
CHEMBL120591 14696 None 0 Human Functional pKd = 7.8 7.8 - 0
Antagonistic activity at human histamine H4 receptor in SK-N-MC cells by inhibition of forskolin-stimulated cAMP-mediated reporter gene activityAntagonistic activity at human histamine H4 receptor in SK-N-MC cells by inhibition of forskolin-stimulated cAMP-mediated reporter gene activity
ChEMBL 276 1 1 3 1.4 Cc1c(F)ccc2[nH]c(C(=O)N3CCN(C)CC3)nc12 10.1021/jm0502081
9923162 18947 None 5 Human Functional pKd = 7.8 7.8 - 1
Antagonistic activity at human histamine H4 receptor in SK-N-MC cells by inhibition of forskolin-stimulated cAMP-mediated reporter gene activityAntagonistic activity at human histamine H4 receptor in SK-N-MC cells by inhibition of forskolin-stimulated cAMP-mediated reporter gene activity
ChEMBL 321 1 1 2 2.3 CN1CCN(C(=O)c2cc3cc(Br)ccc3[nH]2)CC1 10.1021/jm0502081
CHEMBL128613 18947 None 5 Human Functional pKd = 7.8 7.8 - 1
Antagonistic activity at human histamine H4 receptor in SK-N-MC cells by inhibition of forskolin-stimulated cAMP-mediated reporter gene activityAntagonistic activity at human histamine H4 receptor in SK-N-MC cells by inhibition of forskolin-stimulated cAMP-mediated reporter gene activity
ChEMBL 321 1 1 2 2.3 CN1CCN(C(=O)c2cc3cc(Br)ccc3[nH]2)CC1 10.1021/jm0502081
11120826 18925 None 0 Human Functional pKd = 6.8 6.8 - 0
Antagonistic activity at human histamine H4 receptor in SK-N-MC cells by inhibition of forskolin-stimulated cAMP-mediated reporter gene activityAntagonistic activity at human histamine H4 receptor in SK-N-MC cells by inhibition of forskolin-stimulated cAMP-mediated reporter gene activity
ChEMBL 321 1 1 2 2.3 CN1CCN(C(=O)c2cc3c(Br)cccc3[nH]2)CC1 10.1021/jm0502081
CHEMBL128505 18925 None 0 Human Functional pKd = 6.8 6.8 - 0
Antagonistic activity at human histamine H4 receptor in SK-N-MC cells by inhibition of forskolin-stimulated cAMP-mediated reporter gene activityAntagonistic activity at human histamine H4 receptor in SK-N-MC cells by inhibition of forskolin-stimulated cAMP-mediated reporter gene activity
ChEMBL 321 1 1 2 2.3 CN1CCN(C(=O)c2cc3c(Br)cccc3[nH]2)CC1 10.1021/jm0502081
46890677 7293 None 0 Human Functional pKd = 6.8 6.8 - 0
Intrinsic activity at human histamine H4 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-induced cAMP responsive element-beta-galactosidase activity after 6 hrs by colorimetric cAMP assayIntrinsic activity at human histamine H4 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-induced cAMP responsive element-beta-galactosidase activity after 6 hrs by colorimetric cAMP assay
ChEMBL 394 6 1 4 3.8 Cc1cc(OCCCN2CC3C(C2)N3C)ccc1-c1nc2c(C)c(F)ccc2[nH]1 10.1016/j.bmcl.2010.04.017
CHEMBL1086038 7293 None 0 Human Functional pKd = 6.8 6.8 - 0
Intrinsic activity at human histamine H4 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-induced cAMP responsive element-beta-galactosidase activity after 6 hrs by colorimetric cAMP assayIntrinsic activity at human histamine H4 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-induced cAMP responsive element-beta-galactosidase activity after 6 hrs by colorimetric cAMP assay
ChEMBL 394 6 1 4 3.8 Cc1cc(OCCCN2CC3C(C2)N3C)ccc1-c1nc2c(C)c(F)ccc2[nH]1 10.1016/j.bmcl.2010.04.017
46890166 7318 None 0 Mouse Functional pKd = 4.8 4.8 -3 4
Antagonist activity at mouse histamine H4 receptor in SK-N-MC cells assessed as inhibition of forskolin-stimulated cAMP release preincubated for 10 mins before forskolin challengeAntagonist activity at mouse histamine H4 receptor in SK-N-MC cells assessed as inhibition of 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 7318 None 0 Mouse Functional pKd = 4.8 4.8 -3 4
Antagonist activity at mouse histamine H4 receptor in SK-N-MC cells assessed as inhibition of forskolin-stimulated cAMP release preincubated for 10 mins before forskolin challengeAntagonist activity at mouse histamine H4 receptor in SK-N-MC cells assessed as inhibition of 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
66740898 110190 None 0 Human Functional pKd = 7.7 7.7 - 0
Antagonist activity at human histamine H4 receptor expressed in SK-N-MC cells assessed as reduction of histamine-induced inhibition of cAMP-mediated beta-galactosidase reporter gene activity treated 10 mins prior to histamine challenge by microplate reader analysisAntagonist activity at human histamine H4 receptor expressed in SK-N-MC cells assessed as reduction of histamine-induced inhibition of cAMP-mediated beta-galactosidase reporter gene activity treated 10 mins prior to histamine challenge by microplate reader analysis
ChEMBL 287 2 1 5 1.7 CN1C[C@H]2CN(c3cc(C4CCCC4)nc(N)n3)C[C@H]2C1 10.1021/jm401727m
CHEMBL3236562 110190 None 0 Human Functional pKd = 7.7 7.7 - 0
Antagonist activity at human histamine H4 receptor expressed in SK-N-MC cells assessed as reduction of histamine-induced inhibition of cAMP-mediated beta-galactosidase reporter gene activity treated 10 mins prior to histamine challenge by microplate reader analysisAntagonist activity at human histamine H4 receptor expressed in SK-N-MC cells assessed as reduction of histamine-induced inhibition of cAMP-mediated beta-galactosidase reporter gene activity treated 10 mins prior to histamine challenge by microplate reader analysis
ChEMBL 287 2 1 5 1.7 CN1C[C@H]2CN(c3cc(C4CCCC4)nc(N)n3)C[C@H]2C1 10.1021/jm401727m
10468601 198047 None 0 Human Functional pKd = 7.7 7.7 - 0
Antagonist activity at human histamine H4 receptor expressed in human SK-N-MC cells assessed as inhibition of 2-[3-(imidazol-4-yl)-propyl]-1-(4-iodo-benzyl)-isothiourea dihydrobromide-induced intrinsic activityAntagonist activity at human histamine H4 receptor expressed in human SK-N-MC cells assessed as inhibition of 2-[3-(imidazol-4-yl)-propyl]-1-(4-iodo-benzyl)-isothiourea dihydrobromide-induced intrinsic activity
ChEMBL 274 6 3 3 2.8 N=C(NCc1ccccc1)SCCCc1c[nH]cn1 10.1016/j.bmc.2009.04.007
CHEMBL1202324 198047 None 0 Human Functional pKd = 7.7 7.7 - 0
Antagonist activity at human histamine H4 receptor expressed in human SK-N-MC cells assessed as inhibition of 2-[3-(imidazol-4-yl)-propyl]-1-(4-iodo-benzyl)-isothiourea dihydrobromide-induced intrinsic activityAntagonist activity at human histamine H4 receptor expressed in human SK-N-MC cells assessed as inhibition of 2-[3-(imidazol-4-yl)-propyl]-1-(4-iodo-benzyl)-isothiourea dihydrobromide-induced intrinsic activity
ChEMBL 274 6 3 3 2.8 N=C(NCc1ccccc1)SCCCc1c[nH]cn1 10.1016/j.bmc.2009.04.007
CHEMBL555434 198047 None 0 Human Functional pKd = 7.7 7.7 - 0
Antagonist activity at human histamine H4 receptor expressed in human SK-N-MC cells assessed as inhibition of 2-[3-(imidazol-4-yl)-propyl]-1-(4-iodo-benzyl)-isothiourea dihydrobromide-induced intrinsic activityAntagonist activity at human histamine H4 receptor expressed in human SK-N-MC cells assessed as inhibition of 2-[3-(imidazol-4-yl)-propyl]-1-(4-iodo-benzyl)-isothiourea dihydrobromide-induced intrinsic activity
ChEMBL 274 6 3 3 2.8 N=C(NCc1ccccc1)SCCCc1c[nH]cn1 10.1016/j.bmc.2009.04.007
53233904 61545 None 0 Human Functional pKd = 7.7 7.7 - 0
Antagonist activity at human histamine H4 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 6 hrsAntagonist activity at human histamine H4 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 6 hrs
ChEMBL 261 2 1 5 1.0 CN1CCN(c2cc(N)nc(N3CCCC3)c2)CC1 10.1016/j.bmcl.2011.03.017
CHEMBL1770965 61545 None 0 Human Functional pKd = 7.7 7.7 - 0
Antagonist activity at human histamine H4 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 6 hrsAntagonist activity at human histamine H4 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 6 hrs
ChEMBL 261 2 1 5 1.0 CN1CCN(c2cc(N)nc(N3CCCC3)c2)CC1 10.1016/j.bmcl.2011.03.017
10446295 2132 None 34 Human Functional pKd = 7.7 7.7 11 2
Antagonistic activity at human histamine H4 receptor in SK-N-MC cells by inhibition of forskolin-stimulated cAMP-mediated reporter gene activityAntagonistic activity at human histamine H4 receptor in SK-N-MC cells by inhibition of forskolin-stimulated cAMP-mediated reporter gene activity
ChEMBL 278 1 1 3 1.6 CN1CCN(CC1)C(=O)c1nc2c([nH]1)cc(cc2)Cl 10.1021/jm0502081
1277 2132 None 34 Human Functional pKd = 7.7 7.7 11 2
Antagonistic activity at human histamine H4 receptor in SK-N-MC cells by inhibition of forskolin-stimulated cAMP-mediated reporter gene activityAntagonistic activity at human histamine H4 receptor in SK-N-MC cells by inhibition of forskolin-stimulated cAMP-mediated reporter gene activity
ChEMBL 278 1 1 3 1.6 CN1CCN(CC1)C(=O)c1nc2c([nH]1)cc(cc2)Cl 10.1021/jm0502081
CHEMBL185951 2132 None 34 Human Functional pKd = 7.7 7.7 11 2
Antagonistic activity at human histamine H4 receptor in SK-N-MC cells by inhibition of forskolin-stimulated cAMP-mediated reporter gene activityAntagonistic activity at human histamine H4 receptor in SK-N-MC cells by inhibition of forskolin-stimulated cAMP-mediated reporter gene activity
ChEMBL 278 1 1 3 1.6 CN1CCN(CC1)C(=O)c1nc2c([nH]1)cc(cc2)Cl 10.1021/jm0502081
4242975 18849 None 6 Human Functional pKd = 7.7 7.7 - 0
Antagonistic activity at human histamine H4 receptor in SK-N-MC cells by inhibition of forskolin-stimulated cAMP-mediated reporter gene activityAntagonistic activity at human histamine H4 receptor in SK-N-MC cells by inhibition of forskolin-stimulated cAMP-mediated reporter gene activity
ChEMBL 257 1 1 2 1.9 Cc1ccc2[nH]c(C(=O)N3CCN(C)CC3)cc2c1 10.1021/jm0502081
CHEMBL128088 18849 None 6 Human Functional pKd = 7.7 7.7 - 0
Antagonistic activity at human histamine H4 receptor in SK-N-MC cells by inhibition of forskolin-stimulated cAMP-mediated reporter gene activityAntagonistic activity at human histamine H4 receptor in SK-N-MC cells by inhibition of forskolin-stimulated cAMP-mediated reporter gene activity
ChEMBL 257 1 1 2 1.9 Cc1ccc2[nH]c(C(=O)N3CCN(C)CC3)cc2c1 10.1021/jm0502081
9900313 19431 None 0 Human Functional pKd = 7.7 7.7 - 0
Antagonistic activity at human histamine H4 receptor in SK-N-MC cells by inhibition of forskolin-stimulated cAMP-mediated reporter gene activityAntagonistic activity at human histamine H4 receptor in SK-N-MC cells by inhibition of forskolin-stimulated cAMP-mediated reporter gene activity
ChEMBL 279 1 1 2 1.8 CN1CCN(C(=O)c2cc3cc(F)cc(F)c3[nH]2)CC1 10.1021/jm0502081
CHEMBL129444 19431 None 0 Human Functional pKd = 7.7 7.7 - 0
Antagonistic activity at human histamine H4 receptor in SK-N-MC cells by inhibition of forskolin-stimulated cAMP-mediated reporter gene activityAntagonistic activity at human histamine H4 receptor in SK-N-MC cells by inhibition of forskolin-stimulated cAMP-mediated reporter gene activity
ChEMBL 279 1 1 2 1.8 CN1CCN(C(=O)c2cc3cc(F)cc(F)c3[nH]2)CC1 10.1021/jm0502081
9839217 72544 None 0 Human Functional pKd = 7.7 7.7 - 0
Antagonistic activity at human histamine H4 receptor in SK-N-MC cells by inhibition of forskolin-stimulated cAMP-mediated reporter gene activityAntagonistic activity at human histamine H4 receptor in SK-N-MC cells by inhibition of forskolin-stimulated cAMP-mediated reporter gene activity
ChEMBL 297 1 1 3 2.6 Cc1c(Cl)sc2cc(C(=O)N3CCN(C)CC3)[nH]c12 10.1021/jm0502081
CHEMBL199062 72544 None 0 Human Functional pKd = 7.7 7.7 - 0
Antagonistic activity at human histamine H4 receptor in SK-N-MC cells by inhibition of forskolin-stimulated cAMP-mediated reporter gene activityAntagonistic activity at human histamine H4 receptor in SK-N-MC cells by inhibition of forskolin-stimulated cAMP-mediated reporter gene activity
ChEMBL 297 1 1 3 2.6 Cc1c(Cl)sc2cc(C(=O)N3CCN(C)CC3)[nH]c12 10.1021/jm0502081
11565330 97273 None 0 Human Functional pKd = 7.7 7.7 - 0
Antagonistic activity at human histamine H4 receptor in SK-N-MC cells by inhibition of forskolin-stimulated cAMP-mediated reporter gene activityAntagonistic activity at human histamine H4 receptor in SK-N-MC cells by inhibition of forskolin-stimulated cAMP-mediated reporter gene activity
ChEMBL 275 1 1 2 2.0 Cc1c(F)ccc2[nH]c(C(=O)N3CCN(C)CC3)cc12 10.1021/jm0502081
CHEMBL268525 97273 None 0 Human Functional pKd = 7.7 7.7 - 0
Antagonistic activity at human histamine H4 receptor in SK-N-MC cells by inhibition of forskolin-stimulated cAMP-mediated reporter gene activityAntagonistic activity at human histamine H4 receptor in SK-N-MC cells by inhibition of forskolin-stimulated cAMP-mediated reporter gene activity
ChEMBL 275 1 1 2 2.0 Cc1c(F)ccc2[nH]c(C(=O)N3CCN(C)CC3)cc12 10.1021/jm0502081
4906599 168765 None 7 Human Functional pKd = 7.7 7.7 - 0
Antagonistic activity at human histamine H4 receptor in SK-N-MC cells by inhibition of forskolin-stimulated cAMP-mediated reporter gene activityAntagonistic activity at human histamine H4 receptor in SK-N-MC cells by inhibition of forskolin-stimulated cAMP-mediated reporter gene activity
ChEMBL 261 1 1 2 1.7 CN1CCN(C(=O)c2cc3cc(F)ccc3[nH]2)CC1 10.1021/jm0502081
CHEMBL436381 168765 None 7 Human Functional pKd = 7.7 7.7 - 0
Antagonistic activity at human histamine H4 receptor in SK-N-MC cells by inhibition of forskolin-stimulated cAMP-mediated reporter gene activityAntagonistic activity at human histamine H4 receptor in SK-N-MC cells by inhibition of forskolin-stimulated cAMP-mediated reporter gene activity
ChEMBL 261 1 1 2 1.7 CN1CCN(C(=O)c2cc3cc(F)ccc3[nH]2)CC1 10.1021/jm0502081
24996854 110192 None 0 Human Functional pKd = 8.6 8.6 - 0
Antagonist activity at human histamine H4 receptor expressed in SK-N-MC cells assessed as reduction of histamine-induced inhibition of cAMP-mediated beta-galactosidase reporter gene activity treated 10 mins prior to histamine challenge by microplate reader analysisAntagonist activity at human histamine H4 receptor expressed in SK-N-MC cells assessed as reduction of histamine-induced inhibition of cAMP-mediated beta-galactosidase reporter gene activity treated 10 mins prior to histamine challenge by microplate reader analysis
ChEMBL 287 2 2 5 2.0 Nc1nc(C2CCCC2)cc(N2CCC3(CCCN3)C2)n1 10.1021/jm401727m
CHEMBL3236564 110192 None 0 Human Functional pKd = 8.6 8.6 - 0
Antagonist activity at human histamine H4 receptor expressed in SK-N-MC cells assessed as reduction of histamine-induced inhibition of cAMP-mediated beta-galactosidase reporter gene activity treated 10 mins prior to histamine challenge by microplate reader analysisAntagonist activity at human histamine H4 receptor expressed in SK-N-MC cells assessed as reduction of histamine-induced inhibition of cAMP-mediated beta-galactosidase reporter gene activity treated 10 mins prior to histamine challenge by microplate reader analysis
ChEMBL 287 2 2 5 2.0 Nc1nc(C2CCCC2)cc(N2CCC3(CCCN3)C2)n1 10.1021/jm401727m
42624150 110205 None 0 Human Functional pKd = 8.6 8.6 - 0
Antagonist activity at human histamine H4 receptor expressed in SK-N-MC cells assessed as reduction of histamine-induced inhibition of cAMP-mediated beta-galactosidase reporter gene activity treated 10 mins prior to histamine challenge by microplate reader analysisAntagonist activity at human histamine H4 receptor expressed in SK-N-MC cells assessed as reduction of histamine-induced inhibition of cAMP-mediated beta-galactosidase reporter gene activity treated 10 mins prior to histamine challenge by microplate reader analysis
ChEMBL 249 2 2 5 1.2 CN[C@@H]1CCN(c2cc(C(C)(C)C)nc(N)n2)C1 10.1021/jm401727m
CHEMBL3236577 110205 None 0 Human Functional pKd = 8.6 8.6 - 0
Antagonist activity at human histamine H4 receptor expressed in SK-N-MC cells assessed as reduction of histamine-induced inhibition of cAMP-mediated beta-galactosidase reporter gene activity treated 10 mins prior to histamine challenge by microplate reader analysisAntagonist activity at human histamine H4 receptor expressed in SK-N-MC cells assessed as reduction of histamine-induced inhibition of cAMP-mediated beta-galactosidase reporter gene activity treated 10 mins prior to histamine challenge by microplate reader analysis
ChEMBL 249 2 2 5 1.2 CN[C@@H]1CCN(c2cc(C(C)(C)C)nc(N)n2)C1 10.1021/jm401727m
24797956 110186 None 1 Human Functional pKd = 7.6 7.6 - 1
Antagonist activity at human histamine H4 receptor expressed in SK-N-MC cells assessed as reduction of histamine-induced inhibition of cAMP-mediated beta-galactosidase reporter gene activity treated 10 mins prior to histamine challenge by microplate reader analysisAntagonist activity at human histamine H4 receptor expressed in SK-N-MC cells assessed as reduction of histamine-induced inhibition of cAMP-mediated beta-galactosidase reporter gene activity treated 10 mins prior to histamine challenge by microplate reader analysis
ChEMBL 233 2 2 5 0.9 Nc1nc(C2CCCC2)cc(N2CC(N)C2)n1 10.1021/jm401727m
CHEMBL3236558 110186 None 1 Human Functional pKd = 7.6 7.6 - 1
Antagonist activity at human histamine H4 receptor expressed in SK-N-MC cells assessed as reduction of histamine-induced inhibition of cAMP-mediated beta-galactosidase reporter gene activity treated 10 mins prior to histamine challenge by microplate reader analysisAntagonist activity at human histamine H4 receptor expressed in SK-N-MC cells assessed as reduction of histamine-induced inhibition of cAMP-mediated beta-galactosidase reporter gene activity treated 10 mins prior to histamine challenge by microplate reader analysis
ChEMBL 233 2 2 5 0.9 Nc1nc(C2CCCC2)cc(N2CC(N)C2)n1 10.1021/jm401727m
24992735 110211 None 0 Human Functional pKd = 7.6 7.6 - 0
Antagonist activity at human histamine H4 receptor expressed in SK-N-MC cells assessed as reduction of histamine-induced inhibition of cAMP-mediated beta-galactosidase reporter gene activity treated 10 mins prior to histamine challenge by microplate reader analysisAntagonist activity at human histamine H4 receptor expressed in SK-N-MC cells assessed as reduction of histamine-induced inhibition of cAMP-mediated beta-galactosidase reporter gene activity treated 10 mins prior to histamine challenge by microplate reader analysis
ChEMBL 247 2 2 5 0.7 CN[C@@H]1CCN(c2nc(N)nc3c2CCCC3)C1 10.1021/jm401727m
CHEMBL3236582 110211 None 0 Human Functional pKd = 7.6 7.6 - 0
Antagonist activity at human histamine H4 receptor expressed in SK-N-MC cells assessed as reduction of histamine-induced inhibition of cAMP-mediated beta-galactosidase reporter gene activity treated 10 mins prior to histamine challenge by microplate reader analysisAntagonist activity at human histamine H4 receptor expressed in SK-N-MC cells assessed as reduction of histamine-induced inhibition of cAMP-mediated beta-galactosidase reporter gene activity treated 10 mins prior to histamine challenge by microplate reader analysis
ChEMBL 247 2 2 5 0.7 CN[C@@H]1CCN(c2nc(N)nc3c2CCCC3)C1 10.1021/jm401727m
10244243 141400 None 0 Human Functional pKd = 7.6 7.6 - 0
Antagonistic activity at human histamine H4 receptor in SK-N-MC cells by inhibition of forskolin-stimulated cAMP-mediated reporter gene activityAntagonistic activity at human histamine H4 receptor in SK-N-MC cells by inhibition of forskolin-stimulated cAMP-mediated reporter gene activity
ChEMBL 258 1 1 3 1.3 Cc1cccc2[nH]c(C(=O)N3CCN(C)CC3)nc12 10.1021/jm0502081
CHEMBL383384 141400 None 0 Human Functional pKd = 7.6 7.6 - 0
Antagonistic activity at human histamine H4 receptor in SK-N-MC cells by inhibition of forskolin-stimulated cAMP-mediated reporter gene activityAntagonistic activity at human histamine H4 receptor in SK-N-MC cells by inhibition of forskolin-stimulated cAMP-mediated reporter gene activity
ChEMBL 258 1 1 3 1.3 Cc1cccc2[nH]c(C(=O)N3CCN(C)CC3)nc12 10.1021/jm0502081
46890592 6394 None 0 Human Functional pKd = 7.6 7.6 - 2
Intrinsic activity at human histamine H4 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-induced cAMP responsive element-beta-galactosidase activity after 6 hrs by colorimetric cAMP assayIntrinsic activity at human histamine H4 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-induced cAMP responsive element-beta-galactosidase activity after 6 hrs by colorimetric cAMP assay
ChEMBL 422 6 2 4 4.4 Cc1cc(OCCCN2C[C@H]3CCCN[C@H]3C2)ccc1-c1nc2c(C)c(F)ccc2[nH]1 10.1016/j.bmcl.2010.04.017
CHEMBL1082296 6394 None 0 Human Functional pKd = 7.6 7.6 - 2
Intrinsic activity at human histamine H4 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-induced cAMP responsive element-beta-galactosidase activity after 6 hrs by colorimetric cAMP assayIntrinsic activity at human histamine H4 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-induced cAMP responsive element-beta-galactosidase activity after 6 hrs by colorimetric cAMP assay
ChEMBL 422 6 2 4 4.4 Cc1cc(OCCCN2C[C@H]3CCCN[C@H]3C2)ccc1-c1nc2c(C)c(F)ccc2[nH]1 10.1016/j.bmcl.2010.04.017
44547127 115982 None 0 Human Functional pKd = 8.5 8.5 - 1
Antagonist activity at human recombinant histamine H4 receptor expressed in SK-N-MC cells assessed as inhibition of forskolin-stimulated cAMP-mediated reporter gene activityAntagonist activity at human recombinant histamine H4 receptor expressed in SK-N-MC cells assessed as inhibition of forskolin-stimulated cAMP-mediated reporter gene activity
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 115982 None 0 Human Functional pKd = 8.5 8.5 - 1
Antagonist activity at human recombinant histamine H4 receptor expressed in SK-N-MC cells assessed as inhibition of forskolin-stimulated cAMP-mediated reporter gene activityAntagonist activity at human recombinant histamine H4 receptor expressed in SK-N-MC cells assessed as inhibition of forskolin-stimulated cAMP-mediated reporter gene activity
ChEMBL 234 4 2 4 1.7 CN[C@@H]1CCN(c2ccnc(NC(C)C)c2)C1 10.1016/j.bmcl.2014.12.027
24992077 110199 None 0 Human Functional pKd = 8.4 8.4 - 0
Antagonist activity at human histamine H4 receptor expressed in SK-N-MC cells assessed as reduction of histamine-induced inhibition of cAMP-mediated beta-galactosidase reporter gene activity treated 10 mins prior to histamine challenge by microplate reader analysisAntagonist activity at human histamine H4 receptor expressed in SK-N-MC cells assessed as reduction of histamine-induced inhibition of cAMP-mediated beta-galactosidase reporter gene activity treated 10 mins prior to histamine challenge by microplate reader analysis
ChEMBL 249 5 2 5 1.2 CCCCc1cc(N2CC[C@@H](NC)C2)nc(N)n1 10.1021/jm401727m
CHEMBL3236571 110199 None 0 Human Functional pKd = 8.4 8.4 - 0
Antagonist activity at human histamine H4 receptor expressed in SK-N-MC cells assessed as reduction of histamine-induced inhibition of cAMP-mediated beta-galactosidase reporter gene activity treated 10 mins prior to histamine challenge by microplate reader analysisAntagonist activity at human histamine H4 receptor expressed in SK-N-MC cells assessed as reduction of histamine-induced inhibition of cAMP-mediated beta-galactosidase reporter gene activity treated 10 mins prior to histamine challenge by microplate reader analysis
ChEMBL 249 5 2 5 1.2 CCCCc1cc(N2CC[C@@H](NC)C2)nc(N)n1 10.1021/jm401727m
10934567 19265 None 0 Human Functional pKd = 7.5 7.5 - 0
Antagonistic activity at human histamine H4 receptor in SK-N-MC cells by inhibition of forskolin-stimulated cAMP-mediated reporter gene activityAntagonistic activity at human histamine H4 receptor in SK-N-MC cells by inhibition of forskolin-stimulated cAMP-mediated reporter gene activity
ChEMBL 271 1 1 2 2.2 Cc1cc(C)c2[nH]c(C(=O)N3CCN(C)CC3)cc2c1 10.1021/jm0502081
CHEMBL129026 19265 None 0 Human Functional pKd = 7.5 7.5 - 0
Antagonistic activity at human histamine H4 receptor in SK-N-MC cells by inhibition of forskolin-stimulated cAMP-mediated reporter gene activityAntagonistic activity at human histamine H4 receptor in SK-N-MC cells by inhibition of forskolin-stimulated cAMP-mediated reporter gene activity
ChEMBL 271 1 1 2 2.2 Cc1cc(C)c2[nH]c(C(=O)N3CCN(C)CC3)cc2c1 10.1021/jm0502081
11630326 72596 None 0 Human Functional pKd = 7.5 7.5 - 0
Antagonistic activity at human histamine H4 receptor in SK-N-MC cells by inhibition of forskolin-stimulated cAMP-mediated reporter gene activityAntagonistic activity at human histamine H4 receptor in SK-N-MC cells by inhibition of forskolin-stimulated cAMP-mediated reporter gene activity
ChEMBL 263 1 1 3 1.9 Cc1csc2cc(C(=O)N3CCN(C)CC3)[nH]c12 10.1021/jm0502081
CHEMBL199231 72596 None 0 Human Functional pKd = 7.5 7.5 - 0
Antagonistic activity at human histamine H4 receptor in SK-N-MC cells by inhibition of forskolin-stimulated cAMP-mediated reporter gene activityAntagonistic activity at human histamine H4 receptor in SK-N-MC cells by inhibition of forskolin-stimulated cAMP-mediated reporter gene activity
ChEMBL 263 1 1 3 1.9 Cc1csc2cc(C(=O)N3CCN(C)CC3)[nH]c12 10.1021/jm0502081
44547567 117183 None 0 Human Functional pKd = 7.4 7.4 - 0
Antagonist activity at human recombinant histamine H4 receptor expressed in SK-N-MC cells assessed as inhibition of forskolin-stimulated cAMP-mediated reporter gene activityAntagonist activity at human recombinant histamine H4 receptor expressed in SK-N-MC cells assessed as inhibition of forskolin-stimulated cAMP-mediated reporter gene activity
ChEMBL 260 4 2 4 2.2 CN[C@H]1CCN(c2ccnc(NC3CCCC3)c2)C1 10.1016/j.bmcl.2014.12.027
CHEMBL3393533 117183 None 0 Human Functional pKd = 7.4 7.4 - 0
Antagonist activity at human recombinant histamine H4 receptor expressed in SK-N-MC cells assessed as inhibition of forskolin-stimulated cAMP-mediated reporter gene activityAntagonist activity at human recombinant histamine H4 receptor expressed in SK-N-MC cells assessed as inhibition of forskolin-stimulated cAMP-mediated reporter gene activity
ChEMBL 260 4 2 4 2.2 CN[C@H]1CCN(c2ccnc(NC3CCCC3)c2)C1 10.1016/j.bmcl.2014.12.027
4060730 19386 None 35 Human Functional pKd = 7.4 7.4 - 0
Antagonistic activity at human histamine H4 receptor in SK-N-MC cells by inhibition of forskolin-stimulated cAMP-mediated reporter gene activityAntagonistic activity at human histamine H4 receptor in SK-N-MC cells by inhibition of forskolin-stimulated cAMP-mediated reporter gene activity
ChEMBL 243 1 1 2 1.6 CN1CCN(C(=O)c2cc3ccccc3[nH]2)CC1 10.1021/jm0502081
CHEMBL129199 19386 None 35 Human Functional pKd = 7.4 7.4 - 0
Antagonistic activity at human histamine H4 receptor in SK-N-MC cells by inhibition of forskolin-stimulated cAMP-mediated reporter gene activityAntagonistic activity at human histamine H4 receptor in SK-N-MC cells by inhibition of forskolin-stimulated cAMP-mediated reporter gene activity
ChEMBL 243 1 1 2 1.6 CN1CCN(C(=O)c2cc3ccccc3[nH]2)CC1 10.1021/jm0502081
53378711 110206 None 0 Human Functional pKd = 8.3 8.3 - 0
Antagonist activity at human histamine H4 receptor expressed in SK-N-MC cells assessed as reduction of histamine-induced inhibition of cAMP-mediated beta-galactosidase reporter gene activity treated 10 mins prior to histamine challenge by microplate reader analysisAntagonist activity at human histamine H4 receptor expressed in SK-N-MC cells assessed as reduction of histamine-induced inhibition of cAMP-mediated beta-galactosidase reporter gene activity treated 10 mins prior to histamine challenge by microplate reader analysis
ChEMBL 235 1 2 5 0.9 CC(C)(C)c1cc(N2CC[C@@H](N)C2)nc(N)n1 10.1021/jm401727m
CHEMBL3236578 110206 None 0 Human Functional pKd = 8.3 8.3 - 0
Antagonist activity at human histamine H4 receptor expressed in SK-N-MC cells assessed as reduction of histamine-induced inhibition of cAMP-mediated beta-galactosidase reporter gene activity treated 10 mins prior to histamine challenge by microplate reader analysisAntagonist activity at human histamine H4 receptor expressed in SK-N-MC cells assessed as reduction of histamine-induced inhibition of cAMP-mediated beta-galactosidase reporter gene activity treated 10 mins prior to histamine challenge by microplate reader analysis
ChEMBL 235 1 2 5 0.9 CC(C)(C)c1cc(N2CC[C@@H](N)C2)nc(N)n1 10.1021/jm401727m
24994634 2142 None 30 Mouse Functional pKd = 8.3 8.3 - 1
Antagonist activity at mouse histamine H4 receptor expressed in SK-N-MC cells assessed as reduction of histamine-induced inhibition of cAMP-mediated beta-galactosidase reporter gene activity treated 10 mins prior to histamine challenge by microplate reader analysisAntagonist activity at mouse histamine H4 receptor expressed in SK-N-MC cells assessed as reduction of histamine-induced inhibition of cAMP-mediated beta-galactosidase reporter gene activity treated 10 mins prior to histamine challenge by microplate reader analysis
ChEMBL 221 2 2 5 0.7 N[C@@H]1CCN(C1)c1cc(nc(n1)N)C(C)C 10.1021/jm401727m
8984 2142 None 30 Mouse Functional pKd = 8.3 8.3 - 1
Antagonist activity at mouse histamine H4 receptor expressed in SK-N-MC cells assessed as reduction of histamine-induced inhibition of cAMP-mediated beta-galactosidase reporter gene activity treated 10 mins prior to histamine challenge by microplate reader analysisAntagonist activity at mouse histamine H4 receptor expressed in SK-N-MC cells assessed as reduction of histamine-induced inhibition of cAMP-mediated beta-galactosidase reporter gene activity treated 10 mins prior to histamine challenge by microplate reader analysis
ChEMBL 221 2 2 5 0.7 N[C@@H]1CCN(C1)c1cc(nc(n1)N)C(C)C 10.1021/jm401727m
CHEMBL3236549 2142 None 30 Mouse Functional pKd = 8.3 8.3 - 1
Antagonist activity at mouse histamine H4 receptor expressed in SK-N-MC cells assessed as reduction of histamine-induced inhibition of cAMP-mediated beta-galactosidase reporter gene activity treated 10 mins prior to histamine challenge by microplate reader analysisAntagonist activity at mouse histamine H4 receptor expressed in SK-N-MC cells assessed as reduction of histamine-induced inhibition of cAMP-mediated beta-galactosidase reporter gene activity treated 10 mins prior to histamine challenge by microplate reader analysis
ChEMBL 221 2 2 5 0.7 N[C@@H]1CCN(C1)c1cc(nc(n1)N)C(C)C 10.1021/jm401727m
54753437 68205 None 0 Human Functional pKd = 8.3 8.3 - 0
Antagonist activity at recombinant human histamine H4 receptorAntagonist activity at recombinant human histamine H4 receptor
ChEMBL 318 2 2 7 1.8 CN[C@@H]1CCN(c2nc(N)nc3c2oc2ncc(Cl)cc23)C1 10.1016/j.bmcl.2011.08.014
CHEMBL1915048 68205 None 0 Human Functional pKd = 8.3 8.3 - 0
Antagonist activity at recombinant human histamine H4 receptorAntagonist activity at recombinant human histamine H4 receptor
ChEMBL 318 2 2 7 1.8 CN[C@@H]1CCN(c2nc(N)nc3c2oc2ncc(Cl)cc23)C1 10.1016/j.bmcl.2011.08.014
42624149 110196 None 0 Mouse Functional pKd = 7.3 7.3 - 0
Antagonist activity at mouse histamine H4 receptor expressed in SK-N-MC cells assessed as reduction of histamine-induced inhibition of cAMP-mediated beta-galactosidase reporter gene activity treated 10 mins prior to histamine challenge by microplate reader analysisAntagonist activity at mouse histamine H4 receptor expressed in SK-N-MC cells assessed as reduction of histamine-induced inhibition of cAMP-mediated beta-galactosidase reporter gene activity treated 10 mins prior to histamine challenge by microplate reader analysis
ChEMBL 221 3 2 5 0.4 CCc1cc(N2CC[C@@H](NC)C2)nc(N)n1 10.1021/jm401727m
CHEMBL3236568 110196 None 0 Mouse Functional pKd = 7.3 7.3 - 0
Antagonist activity at mouse histamine H4 receptor expressed in SK-N-MC cells assessed as reduction of histamine-induced inhibition of cAMP-mediated beta-galactosidase reporter gene activity treated 10 mins prior to histamine challenge by microplate reader analysisAntagonist activity at mouse histamine H4 receptor expressed in SK-N-MC cells assessed as reduction of histamine-induced inhibition of cAMP-mediated beta-galactosidase reporter gene activity treated 10 mins prior to histamine challenge by microplate reader analysis
ChEMBL 221 3 2 5 0.4 CCc1cc(N2CC[C@@H](NC)C2)nc(N)n1 10.1021/jm401727m
46890590 7026 None 0 Mouse Functional pKd = 7.3 7.3 - 0
Antagonist activity at mouse histamine H4 receptor in SK-N-MC cells assessed as inhibition of forskolin-stimulated cAMP release preincubated for 10 mins before forskolin challengeAntagonist activity at mouse histamine H4 receptor in SK-N-MC cells assessed as inhibition of forskolin-stimulated cAMP release preincubated for 10 mins before forskolin challenge
ChEMBL 422 6 2 4 4.4 Cc1cc(OCCCN2CC3CCCNC3C2)ccc1-c1nc2c(C)c(F)ccc2[nH]1 10.1016/j.bmcl.2010.04.017
CHEMBL1084810 7026 None 0 Mouse Functional pKd = 7.3 7.3 - 0
Antagonist activity at mouse histamine H4 receptor in SK-N-MC cells assessed as inhibition of forskolin-stimulated cAMP release preincubated for 10 mins before forskolin challengeAntagonist activity at mouse histamine H4 receptor in SK-N-MC cells assessed as inhibition of forskolin-stimulated cAMP release preincubated for 10 mins before forskolin challenge
ChEMBL 422 6 2 4 4.4 Cc1cc(OCCCN2CC3CCCNC3C2)ccc1-c1nc2c(C)c(F)ccc2[nH]1 10.1016/j.bmcl.2010.04.017
11572877 67101 None 0 Human Functional pKd = 7.3 7.3 - 0
Antagonistic activity at human histamine H4 receptor in SK-N-MC cells by inhibition of forskolin-stimulated cAMP-mediated reporter gene activityAntagonistic activity at human histamine H4 receptor in SK-N-MC cells by inhibition of forskolin-stimulated cAMP-mediated reporter gene activity
ChEMBL 291 1 1 2 2.5 Cc1cc(Cl)c2[nH]c(C(=O)N3CCN(C)CC3)cc2c1 10.1021/jm0502081
CHEMBL187285 67101 None 0 Human Functional pKd = 7.3 7.3 - 0
Antagonistic activity at human histamine H4 receptor in SK-N-MC cells by inhibition of forskolin-stimulated cAMP-mediated reporter gene activityAntagonistic activity at human histamine H4 receptor in SK-N-MC cells by inhibition of forskolin-stimulated cAMP-mediated reporter gene activity
ChEMBL 291 1 1 2 2.5 Cc1cc(Cl)c2[nH]c(C(=O)N3CCN(C)CC3)cc2c1 10.1021/jm0502081
9992865 114491 None 0 Human Functional pKd = 7.3 7.3 - 0
Antagonistic activity at human histamine H4 receptor in SK-N-MC cells by inhibition of forskolin-stimulated cAMP-mediated reporter gene activityAntagonistic activity at human histamine H4 receptor in SK-N-MC cells by inhibition of forskolin-stimulated cAMP-mediated reporter gene activity
ChEMBL 262 1 1 3 1.1 CN1CCN(C(=O)c2nc3cc(F)ccc3[nH]2)CC1 10.1021/jm0502081
CHEMBL333220 114491 None 0 Human Functional pKd = 7.3 7.3 - 0
Antagonistic activity at human histamine H4 receptor in SK-N-MC cells by inhibition of forskolin-stimulated cAMP-mediated reporter gene activityAntagonistic activity at human histamine H4 receptor in SK-N-MC cells by inhibition of forskolin-stimulated cAMP-mediated reporter gene activity
ChEMBL 262 1 1 3 1.1 CN1CCN(C(=O)c2nc3cc(F)ccc3[nH]2)CC1 10.1021/jm0502081
11601630 132885 None 0 Human Functional pKd = 7.3 7.3 - 0
Antagonistic activity at human histamine H4 receptor in SK-N-MC cells by inhibition of forskolin-stimulated cAMP-mediated reporter gene activityAntagonistic activity at human histamine H4 receptor in SK-N-MC cells by inhibition of forskolin-stimulated cAMP-mediated reporter gene activity
ChEMBL 283 1 1 3 2.3 CN1CCN(C(=O)c2cc3sc(Cl)cc3[nH]2)CC1 10.1021/jm0502081
CHEMBL370135 132885 None 0 Human Functional pKd = 7.3 7.3 - 0
Antagonistic activity at human histamine H4 receptor in SK-N-MC cells by inhibition of forskolin-stimulated cAMP-mediated reporter gene activityAntagonistic activity at human histamine H4 receptor in SK-N-MC cells by inhibition of forskolin-stimulated cAMP-mediated reporter gene activity
ChEMBL 283 1 1 3 2.3 CN1CCN(C(=O)c2cc3sc(Cl)cc3[nH]2)CC1 10.1021/jm0502081
46890546 6517 None 0 Human Functional pKd = 7.3 7.3 - 1
Intrinsic activity at human histamine H4 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-induced cAMP responsive element-beta-galactosidase activity after 6 hrs by colorimetric cAMP assayIntrinsic activity at human histamine H4 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-induced cAMP responsive element-beta-galactosidase activity after 6 hrs by colorimetric cAMP assay
ChEMBL 382 6 2 4 3.8 Cc1cc(OCCCN2CCC(N)C2)ccc1-c1nc2c(C)c(F)ccc2[nH]1 10.1016/j.bmcl.2010.04.017
CHEMBL1082771 6517 None 0 Human Functional pKd = 7.3 7.3 - 1
Intrinsic activity at human histamine H4 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-induced cAMP responsive element-beta-galactosidase activity after 6 hrs by colorimetric cAMP assayIntrinsic activity at human histamine H4 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-induced cAMP responsive element-beta-galactosidase activity after 6 hrs by colorimetric cAMP assay
ChEMBL 382 6 2 4 3.8 Cc1cc(OCCCN2CCC(N)C2)ccc1-c1nc2c(C)c(F)ccc2[nH]1 10.1016/j.bmcl.2010.04.017
46890590 7026 None 0 Human Functional pKd = 7.3 7.3 - 0
Intrinsic activity at human histamine H4 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-induced cAMP responsive element-beta-galactosidase activity after 6 hrs by colorimetric cAMP assayIntrinsic activity at human histamine H4 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-induced cAMP responsive element-beta-galactosidase activity after 6 hrs by colorimetric cAMP assay
ChEMBL 422 6 2 4 4.4 Cc1cc(OCCCN2CC3CCCNC3C2)ccc1-c1nc2c(C)c(F)ccc2[nH]1 10.1016/j.bmcl.2010.04.017
CHEMBL1084810 7026 None 0 Human Functional pKd = 7.3 7.3 - 0
Intrinsic activity at human histamine H4 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-induced cAMP responsive element-beta-galactosidase activity after 6 hrs by colorimetric cAMP assayIntrinsic activity at human histamine H4 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-induced cAMP responsive element-beta-galactosidase activity after 6 hrs by colorimetric cAMP assay
ChEMBL 422 6 2 4 4.4 Cc1cc(OCCCN2CC3CCCNC3C2)ccc1-c1nc2c(C)c(F)ccc2[nH]1 10.1016/j.bmcl.2010.04.017
2063135 8380 None 6 Human Functional pKd = 8.2 8.2 - 1
Antagonist activity at recombinant human histamine H4 receptorAntagonist activity at recombinant human histamine H4 receptor
ChEMBL 302 1 0 5 2.8 CN1CCN(c2ncnc3c2oc2ccc(Cl)cc23)CC1 10.1016/j.bmcl.2011.08.014
CHEMBL1093180 8380 None 6 Human Functional pKd = 8.2 8.2 - 1
Antagonist activity at recombinant human histamine H4 receptorAntagonist activity at recombinant human histamine H4 receptor
ChEMBL 302 1 0 5 2.8 CN1CCN(c2ncnc3c2oc2ccc(Cl)cc23)CC1 10.1016/j.bmcl.2011.08.014
11066922 19430 None 0 Human Functional pKd = 8.2 8.2 - 0
Antagonistic activity at human histamine H4 receptor in SK-N-MC cells by inhibition of forskolin-stimulated cAMP-mediated reporter gene activityAntagonistic activity at human histamine H4 receptor in SK-N-MC cells by inhibition of forskolin-stimulated cAMP-mediated reporter gene activity
ChEMBL 311 1 1 2 2.9 CN1CCN(C(=O)c2cc3c(Cl)c(Cl)ccc3[nH]2)CC1 10.1021/jm0502081
CHEMBL129436 19430 None 0 Human Functional pKd = 8.2 8.2 - 0
Antagonistic activity at human histamine H4 receptor in SK-N-MC cells by inhibition of forskolin-stimulated cAMP-mediated reporter gene activityAntagonistic activity at human histamine H4 receptor in SK-N-MC cells by inhibition of forskolin-stimulated cAMP-mediated reporter gene activity
ChEMBL 311 1 1 2 2.9 CN1CCN(C(=O)c2cc3c(Cl)c(Cl)ccc3[nH]2)CC1 10.1021/jm0502081
24994634 2142 None 30 Rat Functional pKd = 7.2 7.2 - 1
Antagonist activity at rat histamine H4 receptor expressed in SK-N-MC cells assessed as reduction of histamine-induced inhibition of cAMP-mediated beta-galactosidase reporter gene activity treated 10 mins prior to histamine challenge by microplate reader analysisAntagonist activity at rat histamine H4 receptor expressed in SK-N-MC cells assessed as reduction of histamine-induced inhibition of cAMP-mediated beta-galactosidase reporter gene activity treated 10 mins prior to histamine challenge by microplate reader analysis
ChEMBL 221 2 2 5 0.7 N[C@@H]1CCN(C1)c1cc(nc(n1)N)C(C)C 10.1021/jm401727m
8984 2142 None 30 Rat Functional pKd = 7.2 7.2 - 1
Antagonist activity at rat histamine H4 receptor expressed in SK-N-MC cells assessed as reduction of histamine-induced inhibition of cAMP-mediated beta-galactosidase reporter gene activity treated 10 mins prior to histamine challenge by microplate reader analysisAntagonist activity at rat histamine H4 receptor expressed in SK-N-MC cells assessed as reduction of histamine-induced inhibition of cAMP-mediated beta-galactosidase reporter gene activity treated 10 mins prior to histamine challenge by microplate reader analysis
ChEMBL 221 2 2 5 0.7 N[C@@H]1CCN(C1)c1cc(nc(n1)N)C(C)C 10.1021/jm401727m
CHEMBL3236549 2142 None 30 Rat Functional pKd = 7.2 7.2 - 1
Antagonist activity at rat histamine H4 receptor expressed in SK-N-MC cells assessed as reduction of histamine-induced inhibition of cAMP-mediated beta-galactosidase reporter gene activity treated 10 mins prior to histamine challenge by microplate reader analysisAntagonist activity at rat histamine H4 receptor expressed in SK-N-MC cells assessed as reduction of histamine-induced inhibition of cAMP-mediated beta-galactosidase reporter gene activity treated 10 mins prior to histamine challenge by microplate reader analysis
ChEMBL 221 2 2 5 0.7 N[C@@H]1CCN(C1)c1cc(nc(n1)N)C(C)C 10.1021/jm401727m
10083188 141021 None 2 Human Functional pKd = 7.2 7.2 - 0
Antagonistic activity at human histamine H4 receptor in SK-N-MC cells by inhibition of forskolin-stimulated cAMP-mediated reporter gene activityAntagonistic activity at human histamine H4 receptor in SK-N-MC cells by inhibition of forskolin-stimulated cAMP-mediated reporter gene activity
ChEMBL 244 1 1 3 1.0 CN1CCN(C(=O)c2nc3ccccc3[nH]2)CC1 10.1021/jm0502081
CHEMBL382276 141021 None 2 Human Functional pKd = 7.2 7.2 - 0
Antagonistic activity at human histamine H4 receptor in SK-N-MC cells by inhibition of forskolin-stimulated cAMP-mediated reporter gene activityAntagonistic activity at human histamine H4 receptor in SK-N-MC cells by inhibition of forskolin-stimulated cAMP-mediated reporter gene activity
ChEMBL 244 1 1 3 1.0 CN1CCN(C(=O)c2nc3ccccc3[nH]2)CC1 10.1021/jm0502081
46890019 7314 None 0 Human Functional pKd = 7.2 7.2 - 1
Intrinsic activity at human histamine H4 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-induced cAMP responsive element-beta-galactosidase activity after 6 hrs by colorimetric cAMP assayIntrinsic activity at human histamine H4 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-induced cAMP responsive element-beta-galactosidase activity after 6 hrs by colorimetric cAMP assay
ChEMBL 394 6 1 4 3.8 Cc1cc(OCCCN2C3CN(C)CC32)ccc1-c1nc2c(C)c(F)ccc2[nH]1 10.1016/j.bmcl.2010.04.017
CHEMBL1086085 7314 None 0 Human Functional pKd = 7.2 7.2 - 1
Intrinsic activity at human histamine H4 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-induced cAMP responsive element-beta-galactosidase activity after 6 hrs by colorimetric cAMP assayIntrinsic activity at human histamine H4 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-induced cAMP responsive element-beta-galactosidase activity after 6 hrs by colorimetric cAMP assay
ChEMBL 394 6 1 4 3.8 Cc1cc(OCCCN2C3CN(C)CC32)ccc1-c1nc2c(C)c(F)ccc2[nH]1 10.1016/j.bmcl.2010.04.017
1278 2150 None 56 Human Functional pKd = 8.1 8.1 1 4
Decrease in the forskolin stimulatedcAMP levels was determined using SK-N-MC cells stably transfected with the human H4 receptorDecrease in the forskolin stimulatedcAMP levels was determined using SK-N-MC cells stably transfected with the human H4 receptor
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/jm0341047
1279 2150 None 56 Human Functional pKd = 8.1 8.1 1 4
Decrease in the forskolin stimulatedcAMP levels was determined using SK-N-MC cells stably transfected with the human H4 receptorDecrease in the forskolin stimulatedcAMP levels was determined using SK-N-MC cells stably transfected with the human H4 receptor
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/jm0341047
4908365 2150 None 56 Human Functional pKd = 8.1 8.1 1 4
Decrease in the forskolin stimulatedcAMP levels was determined using SK-N-MC cells stably transfected with the human H4 receptorDecrease in the forskolin stimulatedcAMP levels was determined using SK-N-MC cells stably transfected with the human H4 receptor
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/jm0341047
CHEMBL129198 2150 None 56 Human Functional pKd = 8.1 8.1 1 4
Decrease in the forskolin stimulatedcAMP levels was determined using SK-N-MC cells stably transfected with the human H4 receptorDecrease in the forskolin stimulatedcAMP levels was determined using SK-N-MC cells stably transfected with the human H4 receptor
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/jm0341047
10967174 19449 None 1 Human Functional pKd = 8.1 8.1 - 0
Decrease in the forskolin stimulatedcAMP levels was determined using SK-N-MC cells stably transfected with the human H4 receptorDecrease in the forskolin stimulatedcAMP levels was determined using SK-N-MC cells stably transfected with the human H4 receptor
ChEMBL 258 1 2 3 1.1 CN1CCN(C(=O)c2cc3cccc(N)c3[nH]2)CC1 10.1021/jm0341047
CHEMBL129540 19449 None 1 Human Functional pKd = 8.1 8.1 - 0
Decrease in the forskolin stimulatedcAMP levels was determined using SK-N-MC cells stably transfected with the human H4 receptorDecrease in the forskolin stimulatedcAMP levels was determined using SK-N-MC cells stably transfected with the human H4 receptor
ChEMBL 258 1 2 3 1.1 CN1CCN(C(=O)c2cc3cccc(N)c3[nH]2)CC1 10.1021/jm0341047
42624148 110202 None 0 Human Functional pKd = 8.1 8.1 - 0
Antagonist activity at human histamine H4 receptor expressed in SK-N-MC cells assessed as reduction of histamine-induced inhibition of cAMP-mediated beta-galactosidase reporter gene activity treated 10 mins prior to histamine challenge by microplate reader analysisAntagonist activity at human histamine H4 receptor expressed in SK-N-MC cells assessed as reduction of histamine-induced inhibition of cAMP-mediated beta-galactosidase reporter gene activity treated 10 mins prior to histamine challenge by microplate reader analysis
ChEMBL 233 3 2 5 0.7 CN[C@@H]1CCN(c2cc(C3CC3)nc(N)n2)C1 10.1021/jm401727m
CHEMBL3236574 110202 None 0 Human Functional pKd = 8.1 8.1 - 0
Antagonist activity at human histamine H4 receptor expressed in SK-N-MC cells assessed as reduction of histamine-induced inhibition of cAMP-mediated beta-galactosidase reporter gene activity treated 10 mins prior to histamine challenge by microplate reader analysisAntagonist activity at human histamine H4 receptor expressed in SK-N-MC cells assessed as reduction of histamine-induced inhibition of cAMP-mediated beta-galactosidase reporter gene activity treated 10 mins prior to histamine challenge by microplate reader analysis
ChEMBL 233 3 2 5 0.7 CN[C@@H]1CCN(c2cc(C3CC3)nc(N)n2)C1 10.1021/jm401727m
54583875 61575 None 0 Human Functional pKd = 8.1 8.1 - 0
Antagonist activity at human histamine H4 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 6 hrsAntagonist activity at human histamine H4 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 6 hrs
ChEMBL 262 3 2 6 0.5 CN[C@@H]1CCN(c2cc(N3CCCC3)nc(N)n2)C1 10.1016/j.bmcl.2011.03.017
CHEMBL1770995 61575 None 0 Human Functional pKd = 8.1 8.1 - 0
Antagonist activity at human histamine H4 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 6 hrsAntagonist activity at human histamine H4 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 6 hrs
ChEMBL 262 3 2 6 0.5 CN[C@@H]1CCN(c2cc(N3CCCC3)nc(N)n2)C1 10.1016/j.bmcl.2011.03.017
58227179 117198 None 0 Human Functional pKd = 8.1 8.1 - 0
Antagonist activity at human recombinant histamine H4 receptor expressed in SK-N-MC cells assessed as inhibition of forskolin-stimulated cAMP-mediated reporter gene activityAntagonist activity at human recombinant histamine H4 receptor expressed in SK-N-MC cells assessed as inhibition of forskolin-stimulated cAMP-mediated reporter gene activity
ChEMBL 287 4 2 5 1.9 CN[C@H]1CCN(c2ccnc(NC3CC4CCC3C4)n2)C1 10.1016/j.bmcl.2014.12.027
CHEMBL3393548 117198 None 0 Human Functional pKd = 8.1 8.1 - 0
Antagonist activity at human recombinant histamine H4 receptor expressed in SK-N-MC cells assessed as inhibition of forskolin-stimulated cAMP-mediated reporter gene activityAntagonist activity at human recombinant histamine H4 receptor expressed in SK-N-MC cells assessed as inhibition of forskolin-stimulated cAMP-mediated reporter gene activity
ChEMBL 287 4 2 5 1.9 CN[C@H]1CCN(c2ccnc(NC3CC4CCC3C4)n2)C1 10.1016/j.bmcl.2014.12.027
58227086 117207 None 0 Human Functional pKd = 8.1 8.1 - 0
Antagonist activity at human recombinant histamine H4 receptor expressed in SK-N-MC cells assessed as inhibition of forskolin-stimulated cAMP-mediated reporter gene activityAntagonist activity at human recombinant histamine H4 receptor expressed in SK-N-MC cells assessed as inhibition of forskolin-stimulated cAMP-mediated reporter gene activity
ChEMBL 287 4 2 5 1.9 CN[C@H]1CCN(c2cnnc(NC3CC4CCC3C4)c2)C1 10.1016/j.bmcl.2014.12.027
CHEMBL3393557 117207 None 0 Human Functional pKd = 8.1 8.1 - 0
Antagonist activity at human recombinant histamine H4 receptor expressed in SK-N-MC cells assessed as inhibition of forskolin-stimulated cAMP-mediated reporter gene activityAntagonist activity at human recombinant histamine H4 receptor expressed in SK-N-MC cells assessed as inhibition of forskolin-stimulated cAMP-mediated reporter gene activity
ChEMBL 287 4 2 5 1.9 CN[C@H]1CCN(c2cnnc(NC3CC4CCC3C4)c2)C1 10.1016/j.bmcl.2014.12.027
1278 2150 None 56 Human Functional pKd = 8.1 8.1 1 4
Antagonistic activity at human histamine H4 receptor in SK-N-MC cells by inhibition of forskolin-stimulated cAMP-mediated reporter gene activityAntagonistic activity at human histamine H4 receptor in SK-N-MC cells by inhibition of forskolin-stimulated cAMP-mediated reporter gene activity
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/jm0502081
1279 2150 None 56 Human Functional pKd = 8.1 8.1 1 4
Antagonistic activity at human histamine H4 receptor in SK-N-MC cells by inhibition of forskolin-stimulated cAMP-mediated reporter gene activityAntagonistic activity at human histamine H4 receptor in SK-N-MC cells by inhibition of forskolin-stimulated cAMP-mediated reporter gene activity
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/jm0502081
4908365 2150 None 56 Human Functional pKd = 8.1 8.1 1 4
Antagonistic activity at human histamine H4 receptor in SK-N-MC cells by inhibition of forskolin-stimulated cAMP-mediated reporter gene activityAntagonistic activity at human histamine H4 receptor in SK-N-MC cells by inhibition of forskolin-stimulated cAMP-mediated reporter gene activity
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/jm0502081
CHEMBL129198 2150 None 56 Human Functional pKd = 8.1 8.1 1 4
Antagonistic activity at human histamine H4 receptor in SK-N-MC cells by inhibition of forskolin-stimulated cAMP-mediated reporter gene activityAntagonistic activity at human histamine H4 receptor in SK-N-MC cells by inhibition of forskolin-stimulated cAMP-mediated reporter gene activity
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/jm0502081
10967174 19449 None 1 Human Functional pKd = 8.1 8.1 - 0
Antagonistic activity at human histamine H4 receptor in SK-N-MC cells by inhibition of forskolin-stimulated cAMP-mediated reporter gene activityAntagonistic activity at human histamine H4 receptor in SK-N-MC cells by inhibition of forskolin-stimulated cAMP-mediated reporter gene activity
ChEMBL 258 1 2 3 1.1 CN1CCN(C(=O)c2cc3cccc(N)c3[nH]2)CC1 10.1021/jm0502081
CHEMBL129540 19449 None 1 Human Functional pKd = 8.1 8.1 - 0
Antagonistic activity at human histamine H4 receptor in SK-N-MC cells by inhibition of forskolin-stimulated cAMP-mediated reporter gene activityAntagonistic activity at human histamine H4 receptor in SK-N-MC cells by inhibition of forskolin-stimulated cAMP-mediated reporter gene activity
ChEMBL 258 1 2 3 1.1 CN1CCN(C(=O)c2cc3cccc(N)c3[nH]2)CC1 10.1021/jm0502081
10988959 118172 None 1 Human Functional pKd = 8.1 8.1 - 0
Antagonistic activity at human histamine H4 receptor in SK-N-MC cells by inhibition of forskolin-stimulated cAMP-mediated reporter gene activityAntagonistic activity at human histamine H4 receptor in SK-N-MC cells by inhibition of forskolin-stimulated cAMP-mediated reporter gene activity
ChEMBL 258 1 2 3 1.1 CN1CCN(C(=O)c2cc3cc(N)ccc3[nH]2)CC1 10.1021/jm0502081
CHEMBL340740 118172 None 1 Human Functional pKd = 8.1 8.1 - 0
Antagonistic activity at human histamine H4 receptor in SK-N-MC cells by inhibition of forskolin-stimulated cAMP-mediated reporter gene activityAntagonistic activity at human histamine H4 receptor in SK-N-MC cells by inhibition of forskolin-stimulated cAMP-mediated reporter gene activity
ChEMBL 258 1 2 3 1.1 CN1CCN(C(=O)c2cc3cc(N)ccc3[nH]2)CC1 10.1021/jm0502081
10923241 19172 None 0 Human Functional pKd = 7.1 7.1 - 0
Antagonistic activity at human histamine H4 receptor in SK-N-MC cells by inhibition of forskolin-stimulated cAMP-mediated reporter gene activityAntagonistic activity at human histamine H4 receptor in SK-N-MC cells by inhibition of forskolin-stimulated cAMP-mediated reporter gene activity
ChEMBL 259 1 2 3 1.3 CN1CCN(C(=O)c2cc3cc(O)ccc3[nH]2)CC1 10.1021/jm0502081
CHEMBL128958 19172 None 0 Human Functional pKd = 7.1 7.1 - 0
Antagonistic activity at human histamine H4 receptor in SK-N-MC cells by inhibition of forskolin-stimulated cAMP-mediated reporter gene activityAntagonistic activity at human histamine H4 receptor in SK-N-MC cells by inhibition of forskolin-stimulated cAMP-mediated reporter gene activity
ChEMBL 259 1 2 3 1.3 CN1CCN(C(=O)c2cc3cc(O)ccc3[nH]2)CC1 10.1021/jm0502081
9878733 116908 None 0 Human Functional pKd = 7.1 7.1 - 0
Antagonistic activity at human histamine H4 receptor in SK-N-MC cells by inhibition of forskolin-stimulated cAMP-mediated reporter gene activityAntagonistic activity at human histamine H4 receptor in SK-N-MC cells by inhibition of forskolin-stimulated cAMP-mediated reporter gene activity
ChEMBL 277 1 1 2 2.2 CN1CCN(C(=O)c2cc3cccc(Cl)c3[nH]2)CC1 10.1021/jm0502081
CHEMBL338051 116908 None 0 Human Functional pKd = 7.1 7.1 - 0
Antagonistic activity at human histamine H4 receptor in SK-N-MC cells by inhibition of forskolin-stimulated cAMP-mediated reporter gene activityAntagonistic activity at human histamine H4 receptor in SK-N-MC cells by inhibition of forskolin-stimulated cAMP-mediated reporter gene activity
ChEMBL 277 1 1 2 2.2 CN1CCN(C(=O)c2cc3cccc(Cl)c3[nH]2)CC1 10.1021/jm0502081
11623296 117087 None 0 Human Functional pKd = 7.1 7.1 - 0
Antagonistic activity at human histamine H4 receptor in SK-N-MC cells by inhibition of forskolin-stimulated cAMP-mediated reporter gene activityAntagonistic activity at human histamine H4 receptor in SK-N-MC cells by inhibition of forskolin-stimulated cAMP-mediated reporter gene activity
ChEMBL 280 1 1 3 1.2 CN1CCN(C(=O)c2nc3c(F)c(F)ccc3[nH]2)CC1 10.1021/jm0502081
CHEMBL338972 117087 None 0 Human Functional pKd = 7.1 7.1 - 0
Antagonistic activity at human histamine H4 receptor in SK-N-MC cells by inhibition of forskolin-stimulated cAMP-mediated reporter gene activityAntagonistic activity at human histamine H4 receptor in SK-N-MC cells by inhibition of forskolin-stimulated cAMP-mediated reporter gene activity
ChEMBL 280 1 1 3 1.2 CN1CCN(C(=O)c2nc3c(F)c(F)ccc3[nH]2)CC1 10.1021/jm0502081
16202258 68240 None 0 Human Functional pKi = 10.5 10.5 - 0
Antagonist activity at full length human H4R expressed in HEK293 cells assessed as reversal of forskolin-induced cAMP production by CRE-beta-lactamase reporter gene assayAntagonist activity at full length human H4R expressed in HEK293 cells assessed as reversal of forskolin-induced cAMP production by CRE-beta-lactamase reporter gene assay
ChEMBL 264 4 3 6 0.9 CNC1CN(c2cc(NCC(C)(C)C)nc(N)n2)C1 10.1016/j.bmcl.2011.07.125
CHEMBL1915536 68240 None 0 Human Functional pKi = 10.5 10.5 - 0
Antagonist activity at full length human H4R expressed in HEK293 cells assessed as reversal of forskolin-induced cAMP production by CRE-beta-lactamase reporter gene assayAntagonist activity at full length human H4R expressed in HEK293 cells assessed as reversal of forskolin-induced cAMP production by CRE-beta-lactamase reporter gene assay
ChEMBL 264 4 3 6 0.9 CNC1CN(c2cc(NCC(C)(C)C)nc(N)n2)C1 10.1016/j.bmcl.2011.07.125
24745506 68241 None 0 Human Functional pKi = 8.8 8.8 - 0
Antagonist activity at full length human H4R expressed in HEK293 cells assessed as reversal of forskolin-induced cAMP production by CRE-beta-lactamase reporter gene assayAntagonist activity at full length human H4R expressed in HEK293 cells assessed as reversal of forskolin-induced cAMP production by CRE-beta-lactamase reporter gene assay
ChEMBL 278 5 3 6 1.3 CNC1CN(c2cc(NCCC(C)(C)C)nc(N)n2)C1 10.1016/j.bmcl.2011.07.125
CHEMBL1915537 68241 None 0 Human Functional pKi = 8.8 8.8 - 0
Antagonist activity at full length human H4R expressed in HEK293 cells assessed as reversal of forskolin-induced cAMP production by CRE-beta-lactamase reporter gene assayAntagonist activity at full length human H4R expressed in HEK293 cells assessed as reversal of forskolin-induced cAMP production by CRE-beta-lactamase reporter gene assay
ChEMBL 278 5 3 6 1.3 CNC1CN(c2cc(NCCC(C)(C)C)nc(N)n2)C1 10.1016/j.bmcl.2011.07.125
24745335 295 None 13 Human Functional pKi = 8.8 8.8 - 1
Antagonist activity at full length human H4R expressed in HEK293 cells assessed as reversal of forskolin-induced cAMP production by CRE-beta-lactamase reporter gene assayAntagonist activity at full length human H4R expressed in HEK293 cells assessed as reversal of forskolin-induced cAMP production by CRE-beta-lactamase reporter gene assay
ChEMBL 262 5 3 6 0.7 CN[C@@H]1CCN(C1)c1cc(NCC2CC2)nc(n1)N 10.1016/j.bmcl.2011.07.125
8985 295 None 13 Human Functional pKi = 8.8 8.8 - 1
Antagonist activity at full length human H4R expressed in HEK293 cells assessed as reversal of forskolin-induced cAMP production by CRE-beta-lactamase reporter gene assayAntagonist activity at full length human H4R expressed in HEK293 cells assessed as reversal of forskolin-induced cAMP production by CRE-beta-lactamase reporter gene assay
ChEMBL 262 5 3 6 0.7 CN[C@@H]1CCN(C1)c1cc(NCC2CC2)nc(n1)N 10.1016/j.bmcl.2011.07.125
CHEMBL1915540 295 None 13 Human Functional pKi = 8.8 8.8 - 1
Antagonist activity at full length human H4R expressed in HEK293 cells assessed as reversal of forskolin-induced cAMP production by CRE-beta-lactamase reporter gene assayAntagonist activity at full length human H4R expressed in HEK293 cells assessed as reversal of forskolin-induced cAMP production by CRE-beta-lactamase reporter gene assay
ChEMBL 262 5 3 6 0.7 CN[C@@H]1CCN(C1)c1cc(NCC2CC2)nc(n1)N 10.1016/j.bmcl.2011.07.125
DB15027 295 None 13 Human Functional pKi = 8.8 8.8 - 1
Antagonist activity at full length human H4R expressed in HEK293 cells assessed as reversal of forskolin-induced cAMP production by CRE-beta-lactamase reporter gene assayAntagonist activity at full length human H4R expressed in HEK293 cells assessed as reversal of forskolin-induced cAMP production by CRE-beta-lactamase reporter gene assay
ChEMBL 262 5 3 6 0.7 CN[C@@H]1CCN(C1)c1cc(NCC2CC2)nc(n1)N 10.1016/j.bmcl.2011.07.125
44187557 197955 None 0 Human Functional pKi = 8.8 8.8 - 0
Agonistic activity at histamine H4 receptorAgonistic activity at histamine H4 receptor
ChEMBL 342 6 3 3 4.1 N=C(NCc1ccc(Cl)c(Cl)c1)SCCCc1c[nH]cn1 10.1021/jm1013488
CHEMBL1202332 197955 None 0 Human Functional pKi = 8.8 8.8 - 0
Agonistic activity at histamine H4 receptorAgonistic activity at histamine H4 receptor
ChEMBL 342 6 3 3 4.1 N=C(NCc1ccc(Cl)c(Cl)c1)SCCCc1c[nH]cn1 10.1021/jm1013488
CHEMBL553423 197955 None 0 Human Functional pKi = 8.8 8.8 - 0
Agonistic activity at histamine H4 receptorAgonistic activity at histamine H4 receptor
ChEMBL 342 6 3 3 4.1 N=C(NCc1ccc(Cl)c(Cl)c1)SCCCc1c[nH]cn1 10.1021/jm1013488
135525668 68234 None 0 Human Functional pKi = 8 8.0 - 0
Antagonist activity at full length human H4R expressed in HEK293 cells assessed as reversal of forskolin-induced cAMP production by CRE-beta-lactamase reporter gene assayAntagonist activity at full length human H4R expressed in HEK293 cells assessed as reversal of forskolin-induced cAMP production by CRE-beta-lactamase reporter gene assay
ChEMBL 305 1 2 3 1.7 CN1C[C@H]2CN(C(=N)c3nc4cc(F)c(F)cc4[nH]3)C[C@H]2C1 10.1016/j.bmcl.2011.07.125
CHEMBL1915348 68234 None 0 Human Functional pKi = 8 8.0 - 0
Antagonist activity at full length human H4R expressed in HEK293 cells assessed as reversal of forskolin-induced cAMP production by CRE-beta-lactamase reporter gene assayAntagonist activity at full length human H4R expressed in HEK293 cells assessed as reversal of forskolin-induced cAMP production by CRE-beta-lactamase reporter gene assay
ChEMBL 305 1 2 3 1.7 CN1C[C@H]2CN(C(=N)c3nc4cc(F)c(F)cc4[nH]3)C[C@H]2C1 10.1016/j.bmcl.2011.07.125
136042270 69937 None 0 Human Functional pKi = 7.9 7.9 - 0
Antagonist activity at human histamine H4 receptor expressed in HEK293 cells assessed as rev inhibition of forskolin-stimulated cAMP accumulation by CRE-betalactamase reporter gene assayAntagonist activity at human histamine H4 receptor expressed in HEK293 cells assessed as rev inhibition of forskolin-stimulated cAMP accumulation by CRE-betalactamase reporter gene assay
ChEMBL 269 1 2 3 1.4 CN1C[C@H]2CN(C(=N)c3nc4ccccc4[nH]3)C[C@H]2C1 10.1016/j.bmcl.2011.11.098
CHEMBL1938979 69937 None 0 Human Functional pKi = 7.9 7.9 - 0
Antagonist activity at human histamine H4 receptor expressed in HEK293 cells assessed as rev inhibition of forskolin-stimulated cAMP accumulation by CRE-betalactamase reporter gene assayAntagonist activity at human histamine H4 receptor expressed in HEK293 cells assessed as rev inhibition of forskolin-stimulated cAMP accumulation by CRE-betalactamase reporter gene assay
ChEMBL 269 1 2 3 1.4 CN1C[C@H]2CN(C(=N)c3nc4ccccc4[nH]3)C[C@H]2C1 10.1016/j.bmcl.2011.11.098
24745507 68242 None 0 Human Functional pKi = 7.9 7.9 - 0
Antagonist activity at full length human H4R expressed in HEK293 cells assessed as reversal of forskolin-induced cAMP production by CRE-beta-lactamase reporter gene assayAntagonist activity at full length human H4R expressed in HEK293 cells assessed as reversal of forskolin-induced cAMP production by CRE-beta-lactamase reporter gene assay
ChEMBL 302 5 3 6 1.2 CNC1CN(c2cc(NCc3cccc(F)c3)nc(N)n2)C1 10.1016/j.bmcl.2011.07.125
CHEMBL1915538 68242 None 0 Human Functional pKi = 7.9 7.9 - 0
Antagonist activity at full length human H4R expressed in HEK293 cells assessed as reversal of forskolin-induced cAMP production by CRE-beta-lactamase reporter gene assayAntagonist activity at full length human H4R expressed in HEK293 cells assessed as reversal of forskolin-induced cAMP production by CRE-beta-lactamase reporter gene assay
ChEMBL 302 5 3 6 1.2 CNC1CN(c2cc(NCc3cccc(F)c3)nc(N)n2)C1 10.1016/j.bmcl.2011.07.125
57401167 69891 None 0 Human Functional pKi = 6.9 6.9 - 0
Antagonist activity at human histamine H4 receptor expressed in HEK293 cells assessed as rev inhibition of forskolin-stimulated cAMP accumulation by CRE-betalactamase reporter gene assayAntagonist activity at human histamine H4 receptor expressed in HEK293 cells assessed as rev inhibition of forskolin-stimulated cAMP accumulation by CRE-betalactamase reporter gene assay
ChEMBL 306 1 1 3 1.5 CN1C[C@H]2CN(C(=O)c3nc4c(F)c(F)ccc4[nH]3)C[C@H]2C1 10.1016/j.bmcl.2011.11.098
CHEMBL1938846 69891 None 0 Human Functional pKi = 6.9 6.9 - 0
Antagonist activity at human histamine H4 receptor expressed in HEK293 cells assessed as rev inhibition of forskolin-stimulated cAMP accumulation by CRE-betalactamase reporter gene assayAntagonist activity at human histamine H4 receptor expressed in HEK293 cells assessed as rev inhibition of forskolin-stimulated cAMP accumulation by CRE-betalactamase reporter gene assay
ChEMBL 306 1 1 3 1.5 CN1C[C@H]2CN(C(=O)c3nc4c(F)c(F)ccc4[nH]3)C[C@H]2C1 10.1016/j.bmcl.2011.11.098
57400778 68232 None 0 Human Functional pKi = 6.8 6.8 - 0
Antagonist activity at human histamine H4 receptor expressed in HEK293 cells assessed as rev inhibition of forskolin-stimulated cAMP accumulation by CRE-betalactamase reporter gene assayAntagonist activity at human histamine H4 receptor expressed in HEK293 cells assessed as rev inhibition of forskolin-stimulated cAMP accumulation by CRE-betalactamase reporter gene assay
ChEMBL 288 1 1 3 1.3 CN1C[C@H]2CN(C(=O)c3nc4cc(F)ccc4[nH]3)C[C@H]2C1 10.1016/j.bmcl.2011.11.098
CHEMBL1915346 68232 None 0 Human Functional pKi = 6.8 6.8 - 0
Antagonist activity at human histamine H4 receptor expressed in HEK293 cells assessed as rev inhibition of forskolin-stimulated cAMP accumulation by CRE-betalactamase reporter gene assayAntagonist activity at human histamine H4 receptor expressed in HEK293 cells assessed as rev inhibition of forskolin-stimulated cAMP accumulation by CRE-betalactamase reporter gene assay
ChEMBL 288 1 1 3 1.3 CN1C[C@H]2CN(C(=O)c3nc4cc(F)ccc4[nH]3)C[C@H]2C1 10.1016/j.bmcl.2011.11.098
135525668 68234 None 0 Human Functional pKi = 7.8 7.8 - 0
Antagonist activity at human histamine H4 receptor expressed in HEK293 cells assessed as rev inhibition of forskolin-stimulated cAMP accumulation by CRE-betalactamase reporter gene assayAntagonist activity at human histamine H4 receptor expressed in HEK293 cells assessed as rev inhibition of forskolin-stimulated cAMP accumulation by CRE-betalactamase reporter gene assay
ChEMBL 305 1 2 3 1.7 CN1C[C@H]2CN(C(=N)c3nc4cc(F)c(F)cc4[nH]3)C[C@H]2C1 10.1016/j.bmcl.2011.11.098
CHEMBL1915348 68234 None 0 Human Functional pKi = 7.8 7.8 - 0
Antagonist activity at human histamine H4 receptor expressed in HEK293 cells assessed as rev inhibition of forskolin-stimulated cAMP accumulation by CRE-betalactamase reporter gene assayAntagonist activity at human histamine H4 receptor expressed in HEK293 cells assessed as rev inhibition of forskolin-stimulated cAMP accumulation by CRE-betalactamase reporter gene assay
ChEMBL 305 1 2 3 1.7 CN1C[C@H]2CN(C(=N)c3nc4cc(F)c(F)cc4[nH]3)C[C@H]2C1 10.1016/j.bmcl.2011.11.098
57391926 69924 None 0 Human Functional pKi = 6.7 6.7 - 0
Antagonist activity at human histamine H4 receptor expressed in HEK293 cells assessed as rev inhibition of forskolin-stimulated cAMP accumulation by CRE-betalactamase reporter gene assayAntagonist activity at human histamine H4 receptor expressed in HEK293 cells assessed as rev inhibition of forskolin-stimulated cAMP accumulation by CRE-betalactamase reporter gene assay
ChEMBL 270 1 1 3 1.2 CN1C[C@H]2CN(C(=O)c3nc4ccccc4[nH]3)C[C@H]2C1 10.1016/j.bmcl.2011.11.098
CHEMBL1938967 69924 None 0 Human Functional pKi = 6.7 6.7 - 0
Antagonist activity at human histamine H4 receptor expressed in HEK293 cells assessed as rev inhibition of forskolin-stimulated cAMP accumulation by CRE-betalactamase reporter gene assayAntagonist activity at human histamine H4 receptor expressed in HEK293 cells assessed as rev inhibition of forskolin-stimulated cAMP accumulation by CRE-betalactamase reporter gene assay
ChEMBL 270 1 1 3 1.2 CN1C[C@H]2CN(C(=O)c3nc4ccccc4[nH]3)C[C@H]2C1 10.1016/j.bmcl.2011.11.098
136042269 69936 None 0 Human Functional pKi = 7.7 7.7 - 0
Antagonist activity at human histamine H4 receptor expressed in HEK293 cells assessed as rev inhibition of forskolin-stimulated cAMP accumulation by CRE-betalactamase reporter gene assayAntagonist activity at human histamine H4 receptor expressed in HEK293 cells assessed as rev inhibition of forskolin-stimulated cAMP accumulation by CRE-betalactamase reporter gene assay
ChEMBL 323 1 2 3 1.8 CN1C[C@H]2CN(C(=N)c3nc4c(F)c(F)c(F)cc4[nH]3)C[C@H]2C1 10.1016/j.bmcl.2011.11.098
CHEMBL1938978 69936 None 0 Human Functional pKi = 7.7 7.7 - 0
Antagonist activity at human histamine H4 receptor expressed in HEK293 cells assessed as rev inhibition of forskolin-stimulated cAMP accumulation by CRE-betalactamase reporter gene assayAntagonist activity at human histamine H4 receptor expressed in HEK293 cells assessed as rev inhibition of forskolin-stimulated cAMP accumulation by CRE-betalactamase reporter gene assay
ChEMBL 323 1 2 3 1.8 CN1C[C@H]2CN(C(=N)c3nc4c(F)c(F)c(F)cc4[nH]3)C[C@H]2C1 10.1016/j.bmcl.2011.11.098
57402929 69889 None 0 Human Functional pKi = 6.7 6.7 - 0
Antagonist activity at human histamine H4 receptor expressed in HEK293 cells assessed as rev inhibition of forskolin-stimulated cAMP accumulation by CRE-betalactamase reporter gene assayAntagonist activity at human histamine H4 receptor expressed in HEK293 cells assessed as rev inhibition of forskolin-stimulated cAMP accumulation by CRE-betalactamase reporter gene assay
ChEMBL 304 1 1 3 1.9 CN1C[C@H]2CN(C(=O)c3nc4cc(Cl)ccc4[nH]3)C[C@H]2C1 10.1016/j.bmcl.2011.11.098
CHEMBL1938844 69889 None 0 Human Functional pKi = 6.7 6.7 - 0
Antagonist activity at human histamine H4 receptor expressed in HEK293 cells assessed as rev inhibition of forskolin-stimulated cAMP accumulation by CRE-betalactamase reporter gene assayAntagonist activity at human histamine H4 receptor expressed in HEK293 cells assessed as rev inhibition of forskolin-stimulated cAMP accumulation by CRE-betalactamase reporter gene assay
ChEMBL 304 1 1 3 1.9 CN1C[C@H]2CN(C(=O)c3nc4cc(Cl)ccc4[nH]3)C[C@H]2C1 10.1016/j.bmcl.2011.11.098
57395538 68233 None 0 Human Functional pKi = 6.6 6.6 - 0
Antagonist activity at human histamine H4 receptor expressed in HEK293 cells assessed as rev inhibition of forskolin-stimulated cAMP accumulation by CRE-betalactamase reporter gene assayAntagonist activity at human histamine H4 receptor expressed in HEK293 cells assessed as rev inhibition of forskolin-stimulated cAMP accumulation by CRE-betalactamase reporter gene assay
ChEMBL 306 1 1 3 1.5 CN1C[C@H]2CN(C(=O)c3nc4cc(F)c(F)cc4[nH]3)C[C@H]2C1 10.1016/j.bmcl.2011.11.098
CHEMBL1915347 68233 None 0 Human Functional pKi = 6.6 6.6 - 0
Antagonist activity at human histamine H4 receptor expressed in HEK293 cells assessed as rev inhibition of forskolin-stimulated cAMP accumulation by CRE-betalactamase reporter gene assayAntagonist activity at human histamine H4 receptor expressed in HEK293 cells assessed as rev inhibition of forskolin-stimulated cAMP accumulation by CRE-betalactamase reporter gene assay
ChEMBL 306 1 1 3 1.5 CN1C[C@H]2CN(C(=O)c3nc4cc(F)c(F)cc4[nH]3)C[C@H]2C1 10.1016/j.bmcl.2011.11.098
136042267 69934 None 0 Human Functional pKi = 7.6 7.6 - 0
Antagonist activity at human histamine H4 receptor expressed in HEK293 cells assessed as rev inhibition of forskolin-stimulated cAMP accumulation by CRE-betalactamase reporter gene assayAntagonist activity at human histamine H4 receptor expressed in HEK293 cells assessed as rev inhibition of forskolin-stimulated cAMP accumulation by CRE-betalactamase reporter gene assay
ChEMBL 305 1 2 3 1.7 CN1C[C@H]2CN(C(=N)c3nc4c(F)c(F)ccc4[nH]3)C[C@H]2C1 10.1016/j.bmcl.2011.11.098
CHEMBL1938976 69934 None 0 Human Functional pKi = 7.6 7.6 - 0
Antagonist activity at human histamine H4 receptor expressed in HEK293 cells assessed as rev inhibition of forskolin-stimulated cAMP accumulation by CRE-betalactamase reporter gene assayAntagonist activity at human histamine H4 receptor expressed in HEK293 cells assessed as rev inhibition of forskolin-stimulated cAMP accumulation by CRE-betalactamase reporter gene assay
ChEMBL 305 1 2 3 1.7 CN1C[C@H]2CN(C(=N)c3nc4c(F)c(F)ccc4[nH]3)C[C@H]2C1 10.1016/j.bmcl.2011.11.098
57400777 68231 None 0 Human Functional pKi = 7.6 7.6 - 0
Antagonist activity at full length human H4R expressed in HEK293 cells assessed as reversal of forskolin-induced cAMP production by CRE-beta-lactamase reporter gene assayAntagonist activity at full length human H4R expressed in HEK293 cells assessed as reversal of forskolin-induced cAMP production by CRE-beta-lactamase reporter gene assay
ChEMBL 303 1 1 2 2.5 CN1C[C@H]2CN(C(=O)c3cc4cc(Cl)ccc4[nH]3)C[C@H]2C1 10.1016/j.bmcl.2011.07.125
CHEMBL1915345 68231 None 0 Human Functional pKi = 7.6 7.6 - 0
Antagonist activity at full length human H4R expressed in HEK293 cells assessed as reversal of forskolin-induced cAMP production by CRE-beta-lactamase reporter gene assayAntagonist activity at full length human H4R expressed in HEK293 cells assessed as reversal of forskolin-induced cAMP production by CRE-beta-lactamase reporter gene assay
ChEMBL 303 1 1 2 2.5 CN1C[C@H]2CN(C(=O)c3cc4cc(Cl)ccc4[nH]3)C[C@H]2C1 10.1016/j.bmcl.2011.07.125
57400777 68231 None 0 Human Functional pKi = 7.6 7.6 - 0
Antagonist activity at human histamine H4 receptor expressed in HEK293 cells assessed as rev inhibition of forskolin-stimulated cAMP accumulation by CRE-betalactamase reporter gene assayAntagonist activity at human histamine H4 receptor expressed in HEK293 cells assessed as rev inhibition of forskolin-stimulated cAMP accumulation by CRE-betalactamase reporter gene assay
ChEMBL 303 1 1 2 2.5 CN1C[C@H]2CN(C(=O)c3cc4cc(Cl)ccc4[nH]3)C[C@H]2C1 10.1016/j.bmcl.2011.11.098
CHEMBL1915345 68231 None 0 Human Functional pKi = 7.6 7.6 - 0
Antagonist activity at human histamine H4 receptor expressed in HEK293 cells assessed as rev inhibition of forskolin-stimulated cAMP accumulation by CRE-betalactamase reporter gene assayAntagonist activity at human histamine H4 receptor expressed in HEK293 cells assessed as rev inhibition of forskolin-stimulated cAMP accumulation by CRE-betalactamase reporter gene assay
ChEMBL 303 1 1 2 2.5 CN1C[C@H]2CN(C(=O)c3cc4cc(Cl)ccc4[nH]3)C[C@H]2C1 10.1016/j.bmcl.2011.11.098
49841846 69760 None 0 Human Functional pKi = 8.5 8.5 - 1
Antagonist activity at human H4 receptor expressed in HEK293T cells assessed as inhibition of histamine-induced [35S]GTPgammaS bindingAntagonist activity at human H4 receptor expressed in HEK293T cells assessed as inhibition of histamine-induced [35S]GTPgammaS binding
ChEMBL 325 2 1 6 2.7 CN1CCN(c2nc(N)nc3cc(-c4ccsc4)ccc23)CC1 10.1016/j.bmcl.2011.10.104
CHEMBL1935572 69760 None 0 Human Functional pKi = 8.5 8.5 - 1
Antagonist activity at human H4 receptor expressed in HEK293T cells assessed as inhibition of histamine-induced [35S]GTPgammaS bindingAntagonist activity at human H4 receptor expressed in HEK293T cells assessed as inhibition of histamine-induced [35S]GTPgammaS binding
ChEMBL 325 2 1 6 2.7 CN1CCN(c2nc(N)nc3cc(-c4ccsc4)ccc23)CC1 10.1016/j.bmcl.2011.10.104
11688307 69925 None 0 Human Functional pKi = 5.5 5.5 - 0
Antagonist activity at human histamine H4 receptor expressed in HEK293 cells assessed as rev inhibition of forskolin-stimulated cAMP accumulation by CRE-betalactamase reporter gene assayAntagonist activity at human histamine H4 receptor expressed in HEK293 cells assessed as rev inhibition of forskolin-stimulated cAMP accumulation by CRE-betalactamase reporter gene assay
ChEMBL 318 2 1 3 2.2 CCN1C[C@H]2CN(C(=O)c3nc4cc(Cl)ccc4[nH]3)C[C@H]2C1 10.1016/j.bmcl.2011.11.098
CHEMBL1938968 69925 None 0 Human Functional pKi = 5.5 5.5 - 0
Antagonist activity at human histamine H4 receptor expressed in HEK293 cells assessed as rev inhibition of forskolin-stimulated cAMP accumulation by CRE-betalactamase reporter gene assayAntagonist activity at human histamine H4 receptor expressed in HEK293 cells assessed as rev inhibition of forskolin-stimulated cAMP accumulation by CRE-betalactamase reporter gene assay
ChEMBL 318 2 1 3 2.2 CCN1C[C@H]2CN(C(=O)c3nc4cc(Cl)ccc4[nH]3)C[C@H]2C1 10.1016/j.bmcl.2011.11.098
54754351 68239 None 0 Human Functional pKi = 7.4 7.4 - 0
Antagonist activity at human histamine H4 receptor by functional assayAntagonist activity at human histamine H4 receptor by functional assay
ChEMBL 277 4 1 5 2.1 CN1CCN(c2cc(NCCC(C)(C)C)ncn2)CC1 10.1016/j.bmcl.2011.07.114
CHEMBL1915535 68239 None 0 Human Functional pKi = 7.4 7.4 - 0
Antagonist activity at human histamine H4 receptor by functional assayAntagonist activity at human histamine H4 receptor by functional assay
ChEMBL 277 4 1 5 2.1 CN1CCN(c2cc(NCCC(C)(C)C)ncn2)CC1 10.1016/j.bmcl.2011.07.114
57400778 68232 None 0 Human Functional pKi = 7.4 7.4 - 0
Antagonist activity at full length human H4R expressed in HEK293 cells assessed as reversal of forskolin-induced cAMP production by CRE-beta-lactamase reporter gene assayAntagonist activity at full length human H4R expressed in HEK293 cells assessed as reversal of forskolin-induced cAMP production by CRE-beta-lactamase reporter gene assay
ChEMBL 288 1 1 3 1.3 CN1C[C@H]2CN(C(=O)c3nc4cc(F)ccc4[nH]3)C[C@H]2C1 10.1016/j.bmcl.2011.07.125
CHEMBL1915346 68232 None 0 Human Functional pKi = 7.4 7.4 - 0
Antagonist activity at full length human H4R expressed in HEK293 cells assessed as reversal of forskolin-induced cAMP production by CRE-beta-lactamase reporter gene assayAntagonist activity at full length human H4R expressed in HEK293 cells assessed as reversal of forskolin-induced cAMP production by CRE-beta-lactamase reporter gene assay
ChEMBL 288 1 1 3 1.3 CN1C[C@H]2CN(C(=O)c3nc4cc(F)ccc4[nH]3)C[C@H]2C1 10.1016/j.bmcl.2011.07.125
10446295 2132 None 34 Human Functional pKi = 7.4 7.4 11 2
Antagonist activity at human histamine H4 receptor by functional assayAntagonist activity at human histamine H4 receptor by functional assay
ChEMBL 278 1 1 3 1.6 CN1CCN(CC1)C(=O)c1nc2c([nH]1)cc(cc2)Cl 10.1016/j.bmcl.2011.07.114
1277 2132 None 34 Human Functional pKi = 7.4 7.4 11 2
Antagonist activity at human histamine H4 receptor by functional assayAntagonist activity at human histamine H4 receptor by functional assay
ChEMBL 278 1 1 3 1.6 CN1CCN(CC1)C(=O)c1nc2c([nH]1)cc(cc2)Cl 10.1016/j.bmcl.2011.07.114
CHEMBL185951 2132 None 34 Human Functional pKi = 7.4 7.4 11 2
Antagonist activity at human histamine H4 receptor by functional assayAntagonist activity at human histamine H4 receptor by functional assay
ChEMBL 278 1 1 3 1.6 CN1CCN(CC1)C(=O)c1nc2c([nH]1)cc(cc2)Cl 10.1016/j.bmcl.2011.07.114
10446295 2132 None 34 Human Functional pKi = 7.4 7.4 11 2
Antagonist activity at human histamine H4 receptor expressed in HEK293 cells assessed as rev inhibition of forskolin-stimulated cAMP accumulation by CRE-betalactamase reporter gene assayAntagonist activity at human histamine H4 receptor expressed in HEK293 cells assessed as rev inhibition of forskolin-stimulated cAMP accumulation by CRE-betalactamase reporter gene assay
ChEMBL 278 1 1 3 1.6 CN1CCN(CC1)C(=O)c1nc2c([nH]1)cc(cc2)Cl 10.1016/j.bmcl.2011.11.098
1277 2132 None 34 Human Functional pKi = 7.4 7.4 11 2
Antagonist activity at human histamine H4 receptor expressed in HEK293 cells assessed as rev inhibition of forskolin-stimulated cAMP accumulation by CRE-betalactamase reporter gene assayAntagonist activity at human histamine H4 receptor expressed in HEK293 cells assessed as rev inhibition of forskolin-stimulated cAMP accumulation by CRE-betalactamase reporter gene assay
ChEMBL 278 1 1 3 1.6 CN1CCN(CC1)C(=O)c1nc2c([nH]1)cc(cc2)Cl 10.1016/j.bmcl.2011.11.098
CHEMBL185951 2132 None 34 Human Functional pKi = 7.4 7.4 11 2
Antagonist activity at human histamine H4 receptor expressed in HEK293 cells assessed as rev inhibition of forskolin-stimulated cAMP accumulation by CRE-betalactamase reporter gene assayAntagonist activity at human histamine H4 receptor expressed in HEK293 cells assessed as rev inhibition of forskolin-stimulated cAMP accumulation by CRE-betalactamase reporter gene assay
ChEMBL 278 1 1 3 1.6 CN1CCN(CC1)C(=O)c1nc2c([nH]1)cc(cc2)Cl 10.1016/j.bmcl.2011.11.098
49841719 69759 None 0 Human Functional pKi = 8.4 8.4 - 1
Antagonist activity at human H4 receptor expressed in HEK293T cells assessed as inhibition of histamine-induced [35S]GTPgammaS bindingAntagonist activity at human H4 receptor expressed in HEK293T cells assessed as inhibition of histamine-induced [35S]GTPgammaS binding
ChEMBL 309 2 1 6 2.2 CN1CCN(c2nc(N)nc3cc(-c4ccoc4)ccc23)CC1 10.1016/j.bmcl.2011.10.104
CHEMBL1935571 69759 None 0 Human Functional pKi = 8.4 8.4 - 1
Antagonist activity at human H4 receptor expressed in HEK293T cells assessed as inhibition of histamine-induced [35S]GTPgammaS bindingAntagonist activity at human H4 receptor expressed in HEK293T cells assessed as inhibition of histamine-induced [35S]GTPgammaS binding
ChEMBL 309 2 1 6 2.2 CN1CCN(c2nc(N)nc3cc(-c4ccoc4)ccc23)CC1 10.1016/j.bmcl.2011.10.104
57391927 69926 None 0 Human Functional pKi = 5.4 5.4 - 0
Antagonist activity at human histamine H4 receptor expressed in HEK293 cells assessed as rev inhibition of forskolin-stimulated cAMP accumulation by CRE-betalactamase reporter gene assayAntagonist activity at human histamine H4 receptor expressed in HEK293 cells assessed as rev inhibition of forskolin-stimulated cAMP accumulation by CRE-betalactamase reporter gene assay
ChEMBL 332 2 1 3 2.6 CC(C)N1C[C@H]2CN(C(=O)c3nc4cc(Cl)ccc4[nH]3)C[C@H]2C1 10.1016/j.bmcl.2011.11.098
CHEMBL1938969 69926 None 0 Human Functional pKi = 5.4 5.4 - 0
Antagonist activity at human histamine H4 receptor expressed in HEK293 cells assessed as rev inhibition of forskolin-stimulated cAMP accumulation by CRE-betalactamase reporter gene assayAntagonist activity at human histamine H4 receptor expressed in HEK293 cells assessed as rev inhibition of forskolin-stimulated cAMP accumulation by CRE-betalactamase reporter gene assay
ChEMBL 332 2 1 3 2.6 CC(C)N1C[C@H]2CN(C(=O)c3nc4cc(Cl)ccc4[nH]3)C[C@H]2C1 10.1016/j.bmcl.2011.11.098
1278 2150 None 56 Human Functional pKi = 7.3 7.3 1 4
Antagonist activity at human histamine H4 receptor expressed in HEK293 cells assessed as rev inhibition of forskolin-stimulated cAMP accumulation by CRE-betalactamase reporter gene assayAntagonist activity at human histamine H4 receptor expressed in HEK293 cells assessed as rev inhibition of forskolin-stimulated cAMP accumulation by CRE-betalactamase reporter gene assay
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1016/j.bmcl.2011.11.098
1279 2150 None 56 Human Functional pKi = 7.3 7.3 1 4
Antagonist activity at human histamine H4 receptor expressed in HEK293 cells assessed as rev inhibition of forskolin-stimulated cAMP accumulation by CRE-betalactamase reporter gene assayAntagonist activity at human histamine H4 receptor expressed in HEK293 cells assessed as rev inhibition of forskolin-stimulated cAMP accumulation by CRE-betalactamase reporter gene assay
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1016/j.bmcl.2011.11.098
4908365 2150 None 56 Human Functional pKi = 7.3 7.3 1 4
Antagonist activity at human histamine H4 receptor expressed in HEK293 cells assessed as rev inhibition of forskolin-stimulated cAMP accumulation by CRE-betalactamase reporter gene assayAntagonist activity at human histamine H4 receptor expressed in HEK293 cells assessed as rev inhibition of forskolin-stimulated cAMP accumulation by CRE-betalactamase reporter gene assay
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1016/j.bmcl.2011.11.098
CHEMBL129198 2150 None 56 Human Functional pKi = 7.3 7.3 1 4
Antagonist activity at human histamine H4 receptor expressed in HEK293 cells assessed as rev inhibition of forskolin-stimulated cAMP accumulation by CRE-betalactamase reporter gene assayAntagonist activity at human histamine H4 receptor expressed in HEK293 cells assessed as rev inhibition of forskolin-stimulated cAMP accumulation by CRE-betalactamase reporter gene assay
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1016/j.bmcl.2011.11.098
49841845 69761 None 0 Human Functional pKi = 8.3 8.3 - 1
Antagonist activity at human H4 receptor expressed in HEK293T cells assessed as inhibition of histamine-induced [35S]GTPgammaS bindingAntagonist activity at human H4 receptor expressed in HEK293T cells assessed as inhibition of histamine-induced [35S]GTPgammaS binding
ChEMBL 309 2 1 6 2.2 CN1CCN(c2nc(N)nc3cc(-c4ccco4)ccc23)CC1 10.1016/j.bmcl.2011.10.104
CHEMBL1935573 69761 None 0 Human Functional pKi = 8.3 8.3 - 1
Antagonist activity at human H4 receptor expressed in HEK293T cells assessed as inhibition of histamine-induced [35S]GTPgammaS bindingAntagonist activity at human H4 receptor expressed in HEK293T cells assessed as inhibition of histamine-induced [35S]GTPgammaS binding
ChEMBL 309 2 1 6 2.2 CN1CCN(c2nc(N)nc3cc(-c4ccco4)ccc23)CC1 10.1016/j.bmcl.2011.10.104
57395538 68233 None 0 Human Functional pKi = 7.3 7.3 - 0
Antagonist activity at full length human H4R expressed in HEK293 cells assessed as reversal of forskolin-induced cAMP production by CRE-beta-lactamase reporter gene assayAntagonist activity at full length human H4R expressed in HEK293 cells assessed as reversal of forskolin-induced cAMP production by CRE-beta-lactamase reporter gene assay
ChEMBL 306 1 1 3 1.5 CN1C[C@H]2CN(C(=O)c3nc4cc(F)c(F)cc4[nH]3)C[C@H]2C1 10.1016/j.bmcl.2011.07.125
CHEMBL1915347 68233 None 0 Human Functional pKi = 7.3 7.3 - 0
Antagonist activity at full length human H4R expressed in HEK293 cells assessed as reversal of forskolin-induced cAMP production by CRE-beta-lactamase reporter gene assayAntagonist activity at full length human H4R expressed in HEK293 cells assessed as reversal of forskolin-induced cAMP production by CRE-beta-lactamase reporter gene assay
ChEMBL 306 1 1 3 1.5 CN1C[C@H]2CN(C(=O)c3nc4cc(F)c(F)cc4[nH]3)C[C@H]2C1 10.1016/j.bmcl.2011.07.125
136042265 69932 None 0 Human Functional pKi = 7.3 7.3 - 0
Antagonist activity at human histamine H4 receptor expressed in HEK293 cells assessed as rev inhibition of forskolin-stimulated cAMP accumulation by CRE-betalactamase reporter gene assayAntagonist activity at human histamine H4 receptor expressed in HEK293 cells assessed as rev inhibition of forskolin-stimulated cAMP accumulation by CRE-betalactamase reporter gene assay
ChEMBL 303 1 2 3 2.0 CN1C[C@H]2CN(C(=N)c3nc4cc(Cl)ccc4[nH]3)C[C@H]2C1 10.1016/j.bmcl.2011.11.098
CHEMBL1938974 69932 None 0 Human Functional pKi = 7.3 7.3 - 0
Antagonist activity at human histamine H4 receptor expressed in HEK293 cells assessed as rev inhibition of forskolin-stimulated cAMP accumulation by CRE-betalactamase reporter gene assayAntagonist activity at human histamine H4 receptor expressed in HEK293 cells assessed as rev inhibition of forskolin-stimulated cAMP accumulation by CRE-betalactamase reporter gene assay
ChEMBL 303 1 2 3 2.0 CN1C[C@H]2CN(C(=N)c3nc4cc(Cl)ccc4[nH]3)C[C@H]2C1 10.1016/j.bmcl.2011.11.098
57395620 68238 None 0 Human Functional pKi = 6.2 6.2 - 0
Antagonist activity at full length human H4R expressed in HEK293 cells assessed as reversal of forskolin-induced cAMP production by CRE-beta-lactamase reporter gene assayAntagonist activity at full length human H4R expressed in HEK293 cells assessed as reversal of forskolin-induced cAMP production by CRE-beta-lactamase reporter gene assay
ChEMBL 263 5 3 5 2.1 CC(C)(C)CCNc1cc(N[C@H]2CCNC2)ncn1 10.1016/j.bmcl.2011.07.125
CHEMBL1915534 68238 None 0 Human Functional pKi = 6.2 6.2 - 0
Antagonist activity at full length human H4R expressed in HEK293 cells assessed as reversal of forskolin-induced cAMP production by CRE-beta-lactamase reporter gene assayAntagonist activity at full length human H4R expressed in HEK293 cells assessed as reversal of forskolin-induced cAMP production by CRE-beta-lactamase reporter gene assay
ChEMBL 263 5 3 5 2.1 CC(C)(C)CCNc1cc(N[C@H]2CCNC2)ncn1 10.1016/j.bmcl.2011.07.125
57395620 68238 None 0 Human Functional pKi = 6.2 6.2 - 0
Antagonist activity at human histamine H4 receptor by functional assayAntagonist activity at human histamine H4 receptor by functional assay
ChEMBL 263 5 3 5 2.1 CC(C)(C)CCNc1cc(N[C@H]2CCNC2)ncn1 10.1016/j.bmcl.2011.07.114
CHEMBL1915534 68238 None 0 Human Functional pKi = 6.2 6.2 - 0
Antagonist activity at human histamine H4 receptor by functional assayAntagonist activity at human histamine H4 receptor by functional assay
ChEMBL 263 5 3 5 2.1 CC(C)(C)CCNc1cc(N[C@H]2CCNC2)ncn1 10.1016/j.bmcl.2011.07.114
1278 2150 None 56 Human Functional pKi = 8.2 8.2 1 4
Antagonist activity at full length human H4R expressed in HEK293 cells assessed as reversal of forskolin-induced cAMP production by CRE-beta-lactamase reporter gene assayAntagonist activity at full length human H4R expressed in HEK293 cells assessed as reversal of forskolin-induced cAMP production by CRE-beta-lactamase reporter gene assay
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1016/j.bmcl.2011.07.125
1279 2150 None 56 Human Functional pKi = 8.2 8.2 1 4
Antagonist activity at full length human H4R expressed in HEK293 cells assessed as reversal of forskolin-induced cAMP production by CRE-beta-lactamase reporter gene assayAntagonist activity at full length human H4R expressed in HEK293 cells assessed as reversal of forskolin-induced cAMP production by CRE-beta-lactamase reporter gene assay
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1016/j.bmcl.2011.07.125
4908365 2150 None 56 Human Functional pKi = 8.2 8.2 1 4
Antagonist activity at full length human H4R expressed in HEK293 cells assessed as reversal of forskolin-induced cAMP production by CRE-beta-lactamase reporter gene assayAntagonist activity at full length human H4R expressed in HEK293 cells assessed as reversal of forskolin-induced cAMP production by CRE-beta-lactamase reporter gene assay
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1016/j.bmcl.2011.07.125
CHEMBL129198 2150 None 56 Human Functional pKi = 8.2 8.2 1 4
Antagonist activity at full length human H4R expressed in HEK293 cells assessed as reversal of forskolin-induced cAMP production by CRE-beta-lactamase reporter gene assayAntagonist activity at full length human H4R expressed in HEK293 cells assessed as reversal of forskolin-induced cAMP production by CRE-beta-lactamase reporter gene assay
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1016/j.bmcl.2011.07.125
1278 2150 None 56 Human Functional pKi = 8.2 8.2 1 4
Antagonist activity at human histamine H4 receptor by functional assayAntagonist activity at human histamine H4 receptor by functional assay
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1016/j.bmcl.2011.07.114
1279 2150 None 56 Human Functional pKi = 8.2 8.2 1 4
Antagonist activity at human histamine H4 receptor by functional assayAntagonist activity at human histamine H4 receptor by functional assay
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1016/j.bmcl.2011.07.114
4908365 2150 None 56 Human Functional pKi = 8.2 8.2 1 4
Antagonist activity at human histamine H4 receptor by functional assayAntagonist activity at human histamine H4 receptor by functional assay
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1016/j.bmcl.2011.07.114
CHEMBL129198 2150 None 56 Human Functional pKi = 8.2 8.2 1 4
Antagonist activity at human histamine H4 receptor by functional assayAntagonist activity at human histamine H4 receptor by functional assay
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1016/j.bmcl.2011.07.114
1278 2150 None 56 Human Functional pKi = 8.2 8.2 1 4
Antagonist activity at human histamine H4 receptor expressed in HEK293 cells assessed as rev inhibition of forskolin-stimulated cAMP accumulation by CRE-betalactamase reporter gene assayAntagonist activity at human histamine H4 receptor expressed in HEK293 cells assessed as rev inhibition of forskolin-stimulated cAMP accumulation by CRE-betalactamase reporter gene assay
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1016/j.bmcl.2011.11.098
1279 2150 None 56 Human Functional pKi = 8.2 8.2 1 4
Antagonist activity at human histamine H4 receptor expressed in HEK293 cells assessed as rev inhibition of forskolin-stimulated cAMP accumulation by CRE-betalactamase reporter gene assayAntagonist activity at human histamine H4 receptor expressed in HEK293 cells assessed as rev inhibition of forskolin-stimulated cAMP accumulation by CRE-betalactamase reporter gene assay
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1016/j.bmcl.2011.11.098
4908365 2150 None 56 Human Functional pKi = 8.2 8.2 1 4
Antagonist activity at human histamine H4 receptor expressed in HEK293 cells assessed as rev inhibition of forskolin-stimulated cAMP accumulation by CRE-betalactamase reporter gene assayAntagonist activity at human histamine H4 receptor expressed in HEK293 cells assessed as rev inhibition of forskolin-stimulated cAMP accumulation by CRE-betalactamase reporter gene assay
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1016/j.bmcl.2011.11.098
CHEMBL129198 2150 None 56 Human Functional pKi = 8.2 8.2 1 4
Antagonist activity at human histamine H4 receptor expressed in HEK293 cells assessed as rev inhibition of forskolin-stimulated cAMP accumulation by CRE-betalactamase reporter gene assayAntagonist activity at human histamine H4 receptor expressed in HEK293 cells assessed as rev inhibition of forskolin-stimulated cAMP accumulation by CRE-betalactamase reporter gene assay
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1016/j.bmcl.2011.11.098
1267 3804 None 32 Human Functional pKi = 7.2 7.2 -17 5
Antagonist activity at human H4 receptor expressed in HEK293T cells assessed as inhibition of histamine-induced [35S]GTPgammaS bindingAntagonist activity at human H4 receptor expressed in HEK293T cells assessed as inhibition of histamine-induced [35S]GTPgammaS binding
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1016/j.bmcl.2011.10.104
3035905 3804 None 32 Human Functional pKi = 7.2 7.2 -17 5
Antagonist activity at human H4 receptor expressed in HEK293T cells assessed as inhibition of histamine-induced [35S]GTPgammaS bindingAntagonist activity at human H4 receptor expressed in HEK293T cells assessed as inhibition of histamine-induced [35S]GTPgammaS binding
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1016/j.bmcl.2011.10.104
CHEMBL260374 3804 None 32 Human Functional pKi = 7.2 7.2 -17 5
Antagonist activity at human H4 receptor expressed in HEK293T cells assessed as inhibition of histamine-induced [35S]GTPgammaS bindingAntagonist activity at human H4 receptor expressed in HEK293T cells assessed as inhibition of histamine-induced [35S]GTPgammaS binding
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1016/j.bmcl.2011.10.104
56835171 69762 None 0 Human Functional pKi = 8.2 8.2 - 1
Antagonist activity at human H4 receptor expressed in HEK293T cells assessed as inhibition of histamine-induced [35S]GTPgammaS bindingAntagonist activity at human H4 receptor expressed in HEK293T cells assessed as inhibition of histamine-induced [35S]GTPgammaS binding
ChEMBL 295 2 2 6 1.9 Nc1nc(N2CCNCC2)c2ccc(-c3ccco3)cc2n1 10.1016/j.bmcl.2011.10.104
CHEMBL1935574 69762 None 0 Human Functional pKi = 8.2 8.2 - 1
Antagonist activity at human H4 receptor expressed in HEK293T cells assessed as inhibition of histamine-induced [35S]GTPgammaS bindingAntagonist activity at human H4 receptor expressed in HEK293T cells assessed as inhibition of histamine-induced [35S]GTPgammaS binding
ChEMBL 295 2 2 6 1.9 Nc1nc(N2CCNCC2)c2ccc(-c3ccco3)cc2n1 10.1016/j.bmcl.2011.10.104
57390145 69928 None 0 Human Functional pKi = 5.1 5.1 - 0
Antagonist activity at human histamine H4 receptor expressed in HEK293 cells assessed as rev inhibition of forskolin-stimulated cAMP accumulation by CRE-betalactamase reporter gene assayAntagonist activity at human histamine H4 receptor expressed in HEK293 cells assessed as rev inhibition of forskolin-stimulated cAMP accumulation by CRE-betalactamase reporter gene assay
ChEMBL 290 1 2 3 1.5 O=C(c1nc2cc(Cl)ccc2[nH]1)N1C[C@@H]2CNC[C@@H]2C1 10.1016/j.bmcl.2011.11.098
CHEMBL1938970 69928 None 0 Human Functional pKi = 5.1 5.1 - 0
Antagonist activity at human histamine H4 receptor expressed in HEK293 cells assessed as rev inhibition of forskolin-stimulated cAMP accumulation by CRE-betalactamase reporter gene assayAntagonist activity at human histamine H4 receptor expressed in HEK293 cells assessed as rev inhibition of forskolin-stimulated cAMP accumulation by CRE-betalactamase reporter gene assay
ChEMBL 290 1 2 3 1.5 O=C(c1nc2cc(Cl)ccc2[nH]1)N1C[C@@H]2CNC[C@@H]2C1 10.1016/j.bmcl.2011.11.098
136042268 69935 None 0 Human Functional pKi = 8.0 8.0 - 0
Antagonist activity at human histamine H4 receptor expressed in HEK293 cells assessed as rev inhibition of forskolin-stimulated cAMP accumulation by CRE-betalactamase reporter gene assayAntagonist activity at human histamine H4 receptor expressed in HEK293 cells assessed as rev inhibition of forskolin-stimulated cAMP accumulation by CRE-betalactamase reporter gene assay
ChEMBL 287 1 2 3 1.5 CN1C[C@H]2CN(C(=N)c3nc4cc(F)ccc4[nH]3)C[C@H]2C1 10.1016/j.bmcl.2011.11.098
CHEMBL1938977 69935 None 0 Human Functional pKi = 8.0 8.0 - 0
Antagonist activity at human histamine H4 receptor expressed in HEK293 cells assessed as rev inhibition of forskolin-stimulated cAMP accumulation by CRE-betalactamase reporter gene assayAntagonist activity at human histamine H4 receptor expressed in HEK293 cells assessed as rev inhibition of forskolin-stimulated cAMP accumulation by CRE-betalactamase reporter gene assay
ChEMBL 287 1 2 3 1.5 CN1C[C@H]2CN(C(=N)c3nc4cc(F)ccc4[nH]3)C[C@H]2C1 10.1016/j.bmcl.2011.11.098
136042266 69933 None 0 Human Functional pKi = 8.0 8.0 - 0
Antagonist activity at human histamine H4 receptor expressed in HEK293 cells assessed as rev inhibition of forskolin-stimulated cAMP accumulation by CRE-betalactamase reporter gene assayAntagonist activity at human histamine H4 receptor expressed in HEK293 cells assessed as rev inhibition of forskolin-stimulated cAMP accumulation by CRE-betalactamase reporter gene assay
ChEMBL 301 1 2 3 1.8 Cc1c(F)ccc2[nH]c(C(=N)N3C[C@@H]4CN(C)C[C@@H]4C3)nc12 10.1016/j.bmcl.2011.11.098
CHEMBL1938975 69933 None 0 Human Functional pKi = 8.0 8.0 - 0
Antagonist activity at human histamine H4 receptor expressed in HEK293 cells assessed as rev inhibition of forskolin-stimulated cAMP accumulation by CRE-betalactamase reporter gene assayAntagonist activity at human histamine H4 receptor expressed in HEK293 cells assessed as rev inhibition of forskolin-stimulated cAMP accumulation by CRE-betalactamase reporter gene assay
ChEMBL 301 1 2 3 1.8 Cc1c(F)ccc2[nH]c(C(=N)N3C[C@@H]4CN(C)C[C@@H]4C3)nc12 10.1016/j.bmcl.2011.11.098
54754351 68239 None 0 Human Functional pKi = 7.0 7.0 - 0
Antagonist activity at full length human H4R expressed in HEK293 cells assessed as reversal of forskolin-induced cAMP production by CRE-beta-lactamase reporter gene assayAntagonist activity at full length human H4R expressed in HEK293 cells assessed as reversal of forskolin-induced cAMP production by CRE-beta-lactamase reporter gene assay
ChEMBL 277 4 1 5 2.1 CN1CCN(c2cc(NCCC(C)(C)C)ncn2)CC1 10.1016/j.bmcl.2011.07.125
CHEMBL1915535 68239 None 0 Human Functional pKi = 7.0 7.0 - 0
Antagonist activity at full length human H4R expressed in HEK293 cells assessed as reversal of forskolin-induced cAMP production by CRE-beta-lactamase reporter gene assayAntagonist activity at full length human H4R expressed in HEK293 cells assessed as reversal of forskolin-induced cAMP production by CRE-beta-lactamase reporter gene assay
ChEMBL 277 4 1 5 2.1 CN1CCN(c2cc(NCCC(C)(C)C)ncn2)CC1 10.1016/j.bmcl.2011.07.125
56950378 69890 None 0 Human Functional pKi = 7.0 7.0 - 0
Antagonist activity at human histamine H4 receptor expressed in HEK293 cells assessed as rev inhibition of forskolin-stimulated cAMP accumulation by CRE-betalactamase reporter gene assayAntagonist activity at human histamine H4 receptor expressed in HEK293 cells assessed as rev inhibition of forskolin-stimulated cAMP accumulation by CRE-betalactamase reporter gene assay
ChEMBL 302 1 1 3 1.6 Cc1c(F)ccc2[nH]c(C(=O)N3C[C@@H]4CN(C)C[C@@H]4C3)nc12 10.1016/j.bmcl.2011.11.098
CHEMBL1938845 69890 None 0 Human Functional pKi = 7.0 7.0 - 0
Antagonist activity at human histamine H4 receptor expressed in HEK293 cells assessed as rev inhibition of forskolin-stimulated cAMP accumulation by CRE-betalactamase reporter gene assayAntagonist activity at human histamine H4 receptor expressed in HEK293 cells assessed as rev inhibition of forskolin-stimulated cAMP accumulation by CRE-betalactamase reporter gene assay
ChEMBL 302 1 1 3 1.6 Cc1c(F)ccc2[nH]c(C(=O)N3C[C@@H]4CN(C)C[C@@H]4C3)nc12 10.1016/j.bmcl.2011.11.098
135 2532 None 33 Human Functional pEC50 = 8.2 8.2 -2 33
NoneNone
Drug Central 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
1796 2532 None 33 Human Functional pEC50 = 8.2 8.2 -2 33
NoneNone
Drug Central 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
4184 2532 None 33 Human Functional pEC50 = 8.2 8.2 -2 33
NoneNone
Drug Central 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
4184.0 2532 None 33 Human Functional pEC50 = 8.2 8.2 -2 33
NoneNone
Drug Central 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
CHEMBL6437 2532 None 33 Human Functional pEC50 = 8.2 8.2 -2 33
NoneNone
Drug Central 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
DB06148 2532 None 33 Human Functional pEC50 = 8.2 8.2 -2 33
NoneNone
Drug Central 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
1225 1471 None 18 Human Functional pEC50 = 8.2 8.2 -3 11
NoneNone
Drug Central 279 3 0 2 4.0 CN(CC/C=C\1/c2ccccc2OCc2c1cccc2)C None
3958 1471 None 18 Human Functional pEC50 = 8.2 8.2 -3 11
NoneNone
Drug Central 279 3 0 2 4.0 CN(CC/C=C\1/c2ccccc2OCc2c1cccc2)C None
667477 1471 None 18 Human Functional pEC50 = 8.2 8.2 -3 11
NoneNone
Drug Central 279 3 0 2 4.0 CN(CC/C=C\1/c2ccccc2OCc2c1cccc2)C None
667477.0 1471 None 18 Human Functional pEC50 = 8.2 8.2 -3 11
NoneNone
Drug Central 279 3 0 2 4.0 CN(CC/C=C\1/c2ccccc2OCc2c1cccc2)C None
CHEMBL860 1471 None 18 Human Functional pEC50 = 8.2 8.2 -3 11
NoneNone
Drug Central 279 3 0 2 4.0 CN(CC/C=C\1/c2ccccc2OCc2c1cccc2)C None
DB01142 1471 None 18 Human Functional pEC50 = 8.2 8.2 -3 11
NoneNone
Drug Central 279 3 0 2 4.0 CN(CC/C=C\1/c2ccccc2OCc2c1cccc2)C None
5344 173577 None 67 Human Functional pIC50 = 8.3 8.3 60 6
NoneNone
Drug Central 267 3 2 5 1.7 Cc1noc(NS(=O)(=O)c2ccc(N)cc2)c1C None
CHEMBL453 173577 None 67 Human Functional pIC50 = 8.3 8.3 60 6
NoneNone
Drug Central 267 3 2 5 1.7 Cc1noc(NS(=O)(=O)c2ccc(N)cc2)c1C None
1272 831 None 0 Human Functional pIC50 None 8.1 8.1 - 1
UnclassifiedUnclassified
Guide to Pharmacology None None None None 15265943


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Ligands (move mouse cursor over ligand name to see structure) Receptor Activity Chemical information
Sel. page Common
name		 GPCRdb
ID		 Reference
ligand		 Vendors

 Species

 Assay
Type		 Activity
Type		 Activity
Relation		 Activity
Value		 p-value
(-log)		 Fold
selectivity		 Tested
GPCRs		 Assay
Description		 Source

 Mol
weight		 Rot
Bonds		 H don

 H acc

 LogP

 Smiles

 DOI
51354301 58909 None 0 Human Binding pEC50 = 6 6.0 -10 2
Agonist activity at histamine H4 receptor (unknown origin) expressed in human U2OS cells increase in beta-arrestin2 recruitment after 2 hrs by luminescence assayAgonist activity at histamine H4 receptor (unknown origin) expressed in human U2OS cells increase in beta-arrestin2 recruitment after 2 hrs by luminescence assay
ChEMBL 259 5 1 4 2.4 c1nc(CCn2cc(CC3CCCCC3)nn2)c[nH]1 10.1021/acs.jmedchem.8b00435
CHEMBL1688969 58909 None 0 Human Binding pEC50 = 6 6.0 -10 2
Agonist activity at histamine H4 receptor (unknown origin) expressed in human U2OS cells increase in beta-arrestin2 recruitment after 2 hrs by luminescence assayAgonist activity at histamine H4 receptor (unknown origin) expressed in human U2OS cells increase in beta-arrestin2 recruitment after 2 hrs by luminescence assay
ChEMBL 259 5 1 4 2.4 c1nc(CCn2cc(CC3CCCCC3)nn2)c[nH]1 10.1021/acs.jmedchem.8b00435
70692530 75718 None 0 Human Binding pEC50 = 6 6.0 - 1
Agonist activity at histamine H4 receptor (unknown origin) expressed in human U2OS cells increase in beta-arrestin2 recruitment after 2 hrs by luminescence assayAgonist activity at histamine H4 receptor (unknown origin) expressed in human U2OS cells increase in beta-arrestin2 recruitment after 2 hrs by luminescence assay
ChEMBL 322 2 1 4 2.1 CN1CCN(C(=O)c2cc3cc(Cl)cc([N+](=O)[O-])c3[nH]2)CC1 10.1021/acs.jmedchem.8b00435
CHEMBL2047474 75718 None 0 Human Binding pEC50 = 6 6.0 - 1
Agonist activity at histamine H4 receptor (unknown origin) expressed in human U2OS cells increase in beta-arrestin2 recruitment after 2 hrs by luminescence assayAgonist activity at histamine H4 receptor (unknown origin) expressed in human U2OS cells increase in beta-arrestin2 recruitment after 2 hrs by luminescence assay
ChEMBL 322 2 1 4 2.1 CN1CCN(C(=O)c2cc3cc(Cl)cc([N+](=O)[O-])c3[nH]2)CC1 10.1021/acs.jmedchem.8b00435
90667434 109545 None 0 Human Binding pEC50 = 6 6.0 - 1
Agonist activity at human recombinant histamine H4 receptor-RGS19 fusion protein expressed in Sf9 cells coexpressing Galphai2,Gbeta1gamma2 preincubated for 2 mins before [gamma32P]GTP addition measured after 20 mins by steady-state GTPase activity assayAgonist activity at human recombinant histamine H4 receptor-RGS19 fusion protein expressed in Sf9 cells coexpressing Galphai2,Gbeta1gamma2 preincubated for 2 mins before [gamma32P]GTP addition measured after 20 mins by steady-state GTPase activity assay
ChEMBL 313 7 2 3 1.9 CC(CC(=O)/N=C(\N)NCCCn1ccnc1)c1ccccc1 10.1039/C3MD00245D
CHEMBL3220892 109545 None 0 Human Binding pEC50 = 6 6.0 - 1
Agonist activity at human recombinant histamine H4 receptor-RGS19 fusion protein expressed in Sf9 cells coexpressing Galphai2,Gbeta1gamma2 preincubated for 2 mins before [gamma32P]GTP addition measured after 20 mins by steady-state GTPase activity assayAgonist activity at human recombinant histamine H4 receptor-RGS19 fusion protein expressed in Sf9 cells coexpressing Galphai2,Gbeta1gamma2 preincubated for 2 mins before [gamma32P]GTP addition measured after 20 mins by steady-state GTPase activity assay
ChEMBL 313 7 2 3 1.9 CC(CC(=O)/N=C(\N)NCCCn1ccnc1)c1ccccc1 10.1039/C3MD00245D
44367568 45755 None 3 Human Binding pEC50 = 6.0 6.0 - 1
Inhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H4 receptorInhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H4 receptor
ChEMBL 151 2 2 2 0.6 c1nc(C[C@@H]2CCNC2)c[nH]1 10.1021/jm030905y
CHEMBL153051 45755 None 3 Human Binding pEC50 = 6.0 6.0 - 1
Inhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H4 receptorInhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H4 receptor
ChEMBL 151 2 2 2 0.6 c1nc(C[C@@H]2CCNC2)c[nH]1 10.1021/jm030905y
9877454 208071 None 2 Human Binding pEC50 = 5.0 5.0 -4 2
Inhibition of the cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H4 receptorInhibition of the cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H4 receptor
ChEMBL 159 2 1 2 1.4 c1ccc(Cc2c[nH]cn2)nc1 10.1021/jm049932u
CHEMBL81644 208071 None 2 Human Binding pEC50 = 5.0 5.0 -4 2
Inhibition of the cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H4 receptorInhibition of the cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H4 receptor
ChEMBL 159 2 1 2 1.4 c1ccc(Cc2c[nH]cn2)nc1 10.1021/jm049932u
155512725 176346 None 0 Mouse Binding pEC50 = 6.0 6.0 - 2
Agonist activity at mouse H4R expressed in HEK293T-beta-arr2-mH4R cells by beta-arrestin2 recruitment assayAgonist activity at mouse H4R expressed in HEK293T-beta-arr2-mH4R cells by beta-arrestin2 recruitment assay
ChEMBL 237 6 3 5 1.7 CC(C)(C)CNc1nccc(NCCCN)n1 10.1021/acs.jmedchem.9b01342
CHEMBL4437371 176346 None 0 Mouse Binding pEC50 = 6.0 6.0 - 2
Agonist activity at mouse H4R expressed in HEK293T-beta-arr2-mH4R cells by beta-arrestin2 recruitment assayAgonist activity at mouse H4R expressed in HEK293T-beta-arr2-mH4R cells by beta-arrestin2 recruitment assay
ChEMBL 237 6 3 5 1.7 CC(C)(C)CNc1nccc(NCCCN)n1 10.1021/acs.jmedchem.9b01342
CHEMBL4594753 176346 None 0 Mouse Binding pEC50 = 6.0 6.0 - 2
Agonist activity at mouse H4R expressed in HEK293T-beta-arr2-mH4R cells by beta-arrestin2 recruitment assayAgonist activity at mouse H4R expressed in HEK293T-beta-arr2-mH4R cells by beta-arrestin2 recruitment assay
ChEMBL 237 6 3 5 1.7 CC(C)(C)CNc1nccc(NCCCN)n1 10.1021/acs.jmedchem.9b01342
1267 3804 None 32 Human Binding pEC50 = 7.0 7.0 -33 27
Agonist activity at human H4 receptor expressed in insect Sf9 cells co-expressing RGS19 fusion protein and Gialpha2, Gbeta1gamma2 assessed as gamma[32P]GTP binding by liquid scintillation countingAgonist activity at human H4 receptor expressed in insect Sf9 cells co-expressing RGS19 fusion protein and Gialpha2, Gbeta1gamma2 assessed as gamma[32P]GTP binding by liquid scintillation counting
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1021/jm9000693
3035905 3804 None 32 Human Binding pEC50 = 7.0 7.0 -33 27
Agonist activity at human H4 receptor expressed in insect Sf9 cells co-expressing RGS19 fusion protein and Gialpha2, Gbeta1gamma2 assessed as gamma[32P]GTP binding by liquid scintillation countingAgonist activity at human H4 receptor expressed in insect Sf9 cells co-expressing RGS19 fusion protein and Gialpha2, Gbeta1gamma2 assessed as gamma[32P]GTP binding by liquid scintillation counting
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1021/jm9000693
CHEMBL260374 3804 None 32 Human Binding pEC50 = 7.0 7.0 -33 27
Agonist activity at human H4 receptor expressed in insect Sf9 cells co-expressing RGS19 fusion protein and Gialpha2, Gbeta1gamma2 assessed as gamma[32P]GTP binding by liquid scintillation countingAgonist activity at human H4 receptor expressed in insect Sf9 cells co-expressing RGS19 fusion protein and Gialpha2, Gbeta1gamma2 assessed as gamma[32P]GTP binding by liquid scintillation counting
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1021/jm9000693
9793791 46032 None 3 Human Binding pEC50 = 6.0 6.0 - 1
Inhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H4 receptorInhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H4 receptor
ChEMBL 137 2 2 2 0.5 NCC1CC1c1c[nH]cn1 10.1021/jm030905y
CHEMBL153284 46032 None 3 Human Binding pEC50 = 6.0 6.0 - 1
Inhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H4 receptorInhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H4 receptor
ChEMBL 137 2 2 2 0.5 NCC1CC1c1c[nH]cn1 10.1021/jm030905y
155524115 176652 None 0 Mouse Binding pEC50 = 7.9 7.9 1 3
Agonist activity at mouse H4R expressed in HEK293T-beta-arr2-mH4R cells by beta-arrestin2 recruitment assayAgonist activity at mouse H4R expressed in HEK293T-beta-arr2-mH4R cells by beta-arrestin2 recruitment assay
ChEMBL 286 3 2 5 2.2 CC(C)(C)CNc1nccc(N2CCc3nc[nH]c3C2)n1 10.1021/acs.jmedchem.9b01342
CHEMBL4454158 176652 None 0 Mouse Binding pEC50 = 7.9 7.9 1 3
Agonist activity at mouse H4R expressed in HEK293T-beta-arr2-mH4R cells by beta-arrestin2 recruitment assayAgonist activity at mouse H4R expressed in HEK293T-beta-arr2-mH4R cells by beta-arrestin2 recruitment assay
ChEMBL 286 3 2 5 2.2 CC(C)(C)CNc1nccc(N2CCc3nc[nH]c3C2)n1 10.1021/acs.jmedchem.9b01342
CHEMBL4597218 176652 None 0 Mouse Binding pEC50 = 7.9 7.9 1 3
Agonist activity at mouse H4R expressed in HEK293T-beta-arr2-mH4R cells by beta-arrestin2 recruitment assayAgonist activity at mouse H4R expressed in HEK293T-beta-arr2-mH4R cells by beta-arrestin2 recruitment assay
ChEMBL 286 3 2 5 2.2 CC(C)(C)CNc1nccc(N2CCc3nc[nH]c3C2)n1 10.1021/acs.jmedchem.9b01342
1204 1932 None 74 Human Binding pEC50 = 7.9 7.9 -3 24
Activity at human recombinant histamine H4 receptor-RGS4 fusion protein expressed in Sf9 cells coexpressing Galphai2 and G-beta-1-gamma-2 by steady-state GTPase activity assayActivity at human recombinant histamine H4 receptor-RGS4 fusion protein expressed in Sf9 cells coexpressing Galphai2 and G-beta-1-gamma-2 by steady-state GTPase activity assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm800841w
1247 1932 None 74 Human Binding pEC50 = 7.9 7.9 -3 24
Activity at human recombinant histamine H4 receptor-RGS4 fusion protein expressed in Sf9 cells coexpressing Galphai2 and G-beta-1-gamma-2 by steady-state GTPase activity assayActivity at human recombinant histamine H4 receptor-RGS4 fusion protein expressed in Sf9 cells coexpressing Galphai2 and G-beta-1-gamma-2 by steady-state GTPase activity assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm800841w
1375 1932 None 74 Human Binding pEC50 = 7.9 7.9 -3 24
Activity at human recombinant histamine H4 receptor-RGS4 fusion protein expressed in Sf9 cells coexpressing Galphai2 and G-beta-1-gamma-2 by steady-state GTPase activity assayActivity at human recombinant histamine H4 receptor-RGS4 fusion protein expressed in Sf9 cells coexpressing Galphai2 and G-beta-1-gamma-2 by steady-state GTPase activity assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm800841w
774 1932 None 74 Human Binding pEC50 = 7.9 7.9 -3 24
Activity at human recombinant histamine H4 receptor-RGS4 fusion protein expressed in Sf9 cells coexpressing Galphai2 and G-beta-1-gamma-2 by steady-state GTPase activity assayActivity at human recombinant histamine H4 receptor-RGS4 fusion protein expressed in Sf9 cells coexpressing Galphai2 and G-beta-1-gamma-2 by steady-state GTPase activity assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm800841w
774.0 1932 None 74 Human Binding pEC50 = 7.9 7.9 -3 24
Activity at human recombinant histamine H4 receptor-RGS4 fusion protein expressed in Sf9 cells coexpressing Galphai2 and G-beta-1-gamma-2 by steady-state GTPase activity assayActivity at human recombinant histamine H4 receptor-RGS4 fusion protein expressed in Sf9 cells coexpressing Galphai2 and G-beta-1-gamma-2 by steady-state GTPase activity assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm800841w
CHEMBL90 1932 None 74 Human Binding pEC50 = 7.9 7.9 -3 24
Activity at human recombinant histamine H4 receptor-RGS4 fusion protein expressed in Sf9 cells coexpressing Galphai2 and G-beta-1-gamma-2 by steady-state GTPase activity assayActivity at human recombinant histamine H4 receptor-RGS4 fusion protein expressed in Sf9 cells coexpressing Galphai2 and G-beta-1-gamma-2 by steady-state GTPase activity assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm800841w
DB05381 1932 None 74 Human Binding pEC50 = 7.9 7.9 -3 24
Activity at human recombinant histamine H4 receptor-RGS4 fusion protein expressed in Sf9 cells coexpressing Galphai2 and G-beta-1-gamma-2 by steady-state GTPase activity assayActivity at human recombinant histamine H4 receptor-RGS4 fusion protein expressed in Sf9 cells coexpressing Galphai2 and G-beta-1-gamma-2 by steady-state GTPase activity assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm800841w
1236 2067 None 16 Human Binding pEC50 = 6.0 6.0 -208 7
Inhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H4 receptorInhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H4 receptor
ChEMBL 125 2 2 2 0.3 C[C@H](Cc1cnc[nH]1)N 10.1021/jm030905y
1237 2067 None 16 Human Binding pEC50 = 6.0 6.0 -208 7
Inhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H4 receptorInhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H4 receptor
ChEMBL 125 2 2 2 0.3 C[C@H](Cc1cnc[nH]1)N 10.1021/jm030905y
156615 2067 None 16 Human Binding pEC50 = 6.0 6.0 -208 7
Inhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H4 receptorInhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H4 receptor
ChEMBL 125 2 2 2 0.3 C[C@H](Cc1cnc[nH]1)N 10.1021/jm030905y
CHEMBL268229 2067 None 16 Human Binding pEC50 = 6.0 6.0 -208 7
Inhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H4 receptorInhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H4 receptor
ChEMBL 125 2 2 2 0.3 C[C@H](Cc1cnc[nH]1)N 10.1021/jm030905y
46890592 6394 None 0 Mouse Binding pEC50 = 5.9 5.9 - 1
Displacement of [3H]histamine from mouse recombinant histamine H4 receptorDisplacement of [3H]histamine from mouse recombinant histamine H4 receptor
ChEMBL 422 6 2 4 4.4 Cc1cc(OCCCN2C[C@H]3CCCN[C@H]3C2)ccc1-c1nc2c(C)c(F)ccc2[nH]1 10.1016/j.bmcl.2010.04.017
CHEMBL1082296 6394 None 0 Mouse Binding pEC50 = 5.9 5.9 - 1
Displacement of [3H]histamine from mouse recombinant histamine H4 receptorDisplacement of [3H]histamine from mouse recombinant histamine H4 receptor
ChEMBL 422 6 2 4 4.4 Cc1cc(OCCCN2C[C@H]3CCCN[C@H]3C2)ccc1-c1nc2c(C)c(F)ccc2[nH]1 10.1016/j.bmcl.2010.04.017
46890166 7318 None 0 Mouse Binding pEC50 = 7.9 7.9 -4786 2
Displacement of [3H]histamine from mouse recombinant histamine H4 receptorDisplacement of [3H]histamine from mouse recombinant histamine H4 receptor
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 7318 None 0 Mouse Binding pEC50 = 7.9 7.9 -4786 2
Displacement of [3H]histamine from mouse recombinant histamine H4 receptorDisplacement of [3H]histamine from mouse recombinant histamine H4 receptor
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
1204 1932 None 74 Human Binding pEC50 = 7.9 7.9 -3 24
Agonist activity at human H4 receptor expressed in insect Sf9 cells co-expressing RGS19 fusion protein and Gialpha2, Gbeta1gamma2 assessed as gamma[32P]GTP binding by liquid scintillation countingAgonist activity at human H4 receptor expressed in insect Sf9 cells co-expressing RGS19 fusion protein and Gialpha2, Gbeta1gamma2 assessed as gamma[32P]GTP binding by liquid scintillation counting
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm9000693
1247 1932 None 74 Human Binding pEC50 = 7.9 7.9 -3 24
Agonist activity at human H4 receptor expressed in insect Sf9 cells co-expressing RGS19 fusion protein and Gialpha2, Gbeta1gamma2 assessed as gamma[32P]GTP binding by liquid scintillation countingAgonist activity at human H4 receptor expressed in insect Sf9 cells co-expressing RGS19 fusion protein and Gialpha2, Gbeta1gamma2 assessed as gamma[32P]GTP binding by liquid scintillation counting
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm9000693
1375 1932 None 74 Human Binding pEC50 = 7.9 7.9 -3 24
Agonist activity at human H4 receptor expressed in insect Sf9 cells co-expressing RGS19 fusion protein and Gialpha2, Gbeta1gamma2 assessed as gamma[32P]GTP binding by liquid scintillation countingAgonist activity at human H4 receptor expressed in insect Sf9 cells co-expressing RGS19 fusion protein and Gialpha2, Gbeta1gamma2 assessed as gamma[32P]GTP binding by liquid scintillation counting
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm9000693
774 1932 None 74 Human Binding pEC50 = 7.9 7.9 -3 24
Agonist activity at human H4 receptor expressed in insect Sf9 cells co-expressing RGS19 fusion protein and Gialpha2, Gbeta1gamma2 assessed as gamma[32P]GTP binding by liquid scintillation countingAgonist activity at human H4 receptor expressed in insect Sf9 cells co-expressing RGS19 fusion protein and Gialpha2, Gbeta1gamma2 assessed as gamma[32P]GTP binding by liquid scintillation counting
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm9000693
774.0 1932 None 74 Human Binding pEC50 = 7.9 7.9 -3 24
Agonist activity at human H4 receptor expressed in insect Sf9 cells co-expressing RGS19 fusion protein and Gialpha2, Gbeta1gamma2 assessed as gamma[32P]GTP binding by liquid scintillation countingAgonist activity at human H4 receptor expressed in insect Sf9 cells co-expressing RGS19 fusion protein and Gialpha2, Gbeta1gamma2 assessed as gamma[32P]GTP binding by liquid scintillation counting
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm9000693
CHEMBL90 1932 None 74 Human Binding pEC50 = 7.9 7.9 -3 24
Agonist activity at human H4 receptor expressed in insect Sf9 cells co-expressing RGS19 fusion protein and Gialpha2, Gbeta1gamma2 assessed as gamma[32P]GTP binding by liquid scintillation countingAgonist activity at human H4 receptor expressed in insect Sf9 cells co-expressing RGS19 fusion protein and Gialpha2, Gbeta1gamma2 assessed as gamma[32P]GTP binding by liquid scintillation counting
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm9000693
DB05381 1932 None 74 Human Binding pEC50 = 7.9 7.9 -3 24
Agonist activity at human H4 receptor expressed in insect Sf9 cells co-expressing RGS19 fusion protein and Gialpha2, Gbeta1gamma2 assessed as gamma[32P]GTP binding by liquid scintillation countingAgonist activity at human H4 receptor expressed in insect Sf9 cells co-expressing RGS19 fusion protein and Gialpha2, Gbeta1gamma2 assessed as gamma[32P]GTP binding by liquid scintillation counting
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm9000693
1204 1932 None 74 Human Binding pEC50 = 7.9 7.9 -3 24
Agonist activity at human recombinant histamine H4 receptor-RGS19 fusion protein expressed in Sf9 cells coexpressing Galphai2,Gbeta1gamma2 preincubated for 2 mins before [gamma32P]GTP addition measured after 20 mins by steady-state GTPase activity assayAgonist activity at human recombinant histamine H4 receptor-RGS19 fusion protein expressed in Sf9 cells coexpressing Galphai2,Gbeta1gamma2 preincubated for 2 mins before [gamma32P]GTP addition measured after 20 mins by steady-state GTPase activity assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1039/C3MD00245D
1247 1932 None 74 Human Binding pEC50 = 7.9 7.9 -3 24
Agonist activity at human recombinant histamine H4 receptor-RGS19 fusion protein expressed in Sf9 cells coexpressing Galphai2,Gbeta1gamma2 preincubated for 2 mins before [gamma32P]GTP addition measured after 20 mins by steady-state GTPase activity assayAgonist activity at human recombinant histamine H4 receptor-RGS19 fusion protein expressed in Sf9 cells coexpressing Galphai2,Gbeta1gamma2 preincubated for 2 mins before [gamma32P]GTP addition measured after 20 mins by steady-state GTPase activity assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1039/C3MD00245D
1375 1932 None 74 Human Binding pEC50 = 7.9 7.9 -3 24
Agonist activity at human recombinant histamine H4 receptor-RGS19 fusion protein expressed in Sf9 cells coexpressing Galphai2,Gbeta1gamma2 preincubated for 2 mins before [gamma32P]GTP addition measured after 20 mins by steady-state GTPase activity assayAgonist activity at human recombinant histamine H4 receptor-RGS19 fusion protein expressed in Sf9 cells coexpressing Galphai2,Gbeta1gamma2 preincubated for 2 mins before [gamma32P]GTP addition measured after 20 mins by steady-state GTPase activity assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1039/C3MD00245D
774 1932 None 74 Human Binding pEC50 = 7.9 7.9 -3 24
Agonist activity at human recombinant histamine H4 receptor-RGS19 fusion protein expressed in Sf9 cells coexpressing Galphai2,Gbeta1gamma2 preincubated for 2 mins before [gamma32P]GTP addition measured after 20 mins by steady-state GTPase activity assayAgonist activity at human recombinant histamine H4 receptor-RGS19 fusion protein expressed in Sf9 cells coexpressing Galphai2,Gbeta1gamma2 preincubated for 2 mins before [gamma32P]GTP addition measured after 20 mins by steady-state GTPase activity assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1039/C3MD00245D
774.0 1932 None 74 Human Binding pEC50 = 7.9 7.9 -3 24
Agonist activity at human recombinant histamine H4 receptor-RGS19 fusion protein expressed in Sf9 cells coexpressing Galphai2,Gbeta1gamma2 preincubated for 2 mins before [gamma32P]GTP addition measured after 20 mins by steady-state GTPase activity assayAgonist activity at human recombinant histamine H4 receptor-RGS19 fusion protein expressed in Sf9 cells coexpressing Galphai2,Gbeta1gamma2 preincubated for 2 mins before [gamma32P]GTP addition measured after 20 mins by steady-state GTPase activity assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1039/C3MD00245D
CHEMBL90 1932 None 74 Human Binding pEC50 = 7.9 7.9 -3 24
Agonist activity at human recombinant histamine H4 receptor-RGS19 fusion protein expressed in Sf9 cells coexpressing Galphai2,Gbeta1gamma2 preincubated for 2 mins before [gamma32P]GTP addition measured after 20 mins by steady-state GTPase activity assayAgonist activity at human recombinant histamine H4 receptor-RGS19 fusion protein expressed in Sf9 cells coexpressing Galphai2,Gbeta1gamma2 preincubated for 2 mins before [gamma32P]GTP addition measured after 20 mins by steady-state GTPase activity assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1039/C3MD00245D
DB05381 1932 None 74 Human Binding pEC50 = 7.9 7.9 -3 24
Agonist activity at human recombinant histamine H4 receptor-RGS19 fusion protein expressed in Sf9 cells coexpressing Galphai2,Gbeta1gamma2 preincubated for 2 mins before [gamma32P]GTP addition measured after 20 mins by steady-state GTPase activity assayAgonist activity at human recombinant histamine H4 receptor-RGS19 fusion protein expressed in Sf9 cells coexpressing Galphai2,Gbeta1gamma2 preincubated for 2 mins before [gamma32P]GTP addition measured after 20 mins by steady-state GTPase activity assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1039/C3MD00245D
1278 2150 None 56 Human Binding pEC50 = 7.9 7.9 -3 8
Agonist activity at histamine H4 receptor (unknown origin) assessed as increase in beta-arrestin recruitmentAgonist activity at histamine H4 receptor (unknown origin) assessed as increase in beta-arrestin recruitment
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/acs.jmedchem.8b00435
1279 2150 None 56 Human Binding pEC50 = 7.9 7.9 -3 8
Agonist activity at histamine H4 receptor (unknown origin) assessed as increase in beta-arrestin recruitmentAgonist activity at histamine H4 receptor (unknown origin) assessed as increase in beta-arrestin recruitment
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/acs.jmedchem.8b00435
4908365 2150 None 56 Human Binding pEC50 = 7.9 7.9 -3 8
Agonist activity at histamine H4 receptor (unknown origin) assessed as increase in beta-arrestin recruitmentAgonist activity at histamine H4 receptor (unknown origin) assessed as increase in beta-arrestin recruitment
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/acs.jmedchem.8b00435
CHEMBL129198 2150 None 56 Human Binding pEC50 = 7.9 7.9 -3 8
Agonist activity at histamine H4 receptor (unknown origin) assessed as increase in beta-arrestin recruitmentAgonist activity at histamine H4 receptor (unknown origin) assessed as increase in beta-arrestin recruitment
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/acs.jmedchem.8b00435
155524115 176652 None 0 Mouse Binding pEC50 = 7.9 7.9 1 3
Agonist activity at mouse recombinant H4R expressed in HEK293T cells by beta-arrestin recruitment assayAgonist activity at mouse recombinant H4R expressed in HEK293T cells by beta-arrestin recruitment assay
ChEMBL 286 3 2 5 2.2 CC(C)(C)CNc1nccc(N2CCc3nc[nH]c3C2)n1 10.1021/acs.jmedchem.0c00160
CHEMBL4454158 176652 None 0 Mouse Binding pEC50 = 7.9 7.9 1 3
Agonist activity at mouse recombinant H4R expressed in HEK293T cells by beta-arrestin recruitment assayAgonist activity at mouse recombinant H4R expressed in HEK293T cells by beta-arrestin recruitment assay
ChEMBL 286 3 2 5 2.2 CC(C)(C)CNc1nccc(N2CCc3nc[nH]c3C2)n1 10.1021/acs.jmedchem.0c00160
CHEMBL4597218 176652 None 0 Mouse Binding pEC50 = 7.9 7.9 1 3
Agonist activity at mouse recombinant H4R expressed in HEK293T cells by beta-arrestin recruitment assayAgonist activity at mouse recombinant H4R expressed in HEK293T cells by beta-arrestin recruitment assay
ChEMBL 286 3 2 5 2.2 CC(C)(C)CNc1nccc(N2CCc3nc[nH]c3C2)n1 10.1021/acs.jmedchem.0c00160
11344458 207656 None 0 Human Binding pEC50 = 5.9 5.9 -14 2
Inhibition of the cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H4 receptorInhibition of the cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H4 receptor
ChEMBL 187 4 1 2 2.0 c1cncc(CCCc2c[nH]cn2)c1 10.1021/jm049932u
CHEMBL78497 207656 None 0 Human Binding pEC50 = 5.9 5.9 -14 2
Inhibition of the cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H4 receptorInhibition of the cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H4 receptor
ChEMBL 187 4 1 2 2.0 c1cncc(CCCc2c[nH]cn2)c1 10.1021/jm049932u
1204 1932 None 74 Human Binding pEC50 = 7.9 7.9 -3 24
Agonist activity at human SF-His6-tagged histamine H4 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated response incubated for 5 hrs by luciferase reporter gene assayAgonist activity at human SF-His6-tagged histamine H4 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated response incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.6b00120
1247 1932 None 74 Human Binding pEC50 = 7.9 7.9 -3 24
Agonist activity at human SF-His6-tagged histamine H4 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated response incubated for 5 hrs by luciferase reporter gene assayAgonist activity at human SF-His6-tagged histamine H4 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated response incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.6b00120
1375 1932 None 74 Human Binding pEC50 = 7.9 7.9 -3 24
Agonist activity at human SF-His6-tagged histamine H4 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated response incubated for 5 hrs by luciferase reporter gene assayAgonist activity at human SF-His6-tagged histamine H4 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated response incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.6b00120
774 1932 None 74 Human Binding pEC50 = 7.9 7.9 -3 24
Agonist activity at human SF-His6-tagged histamine H4 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated response incubated for 5 hrs by luciferase reporter gene assayAgonist activity at human SF-His6-tagged histamine H4 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated response incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.6b00120
774.0 1932 None 74 Human Binding pEC50 = 7.9 7.9 -3 24
Agonist activity at human SF-His6-tagged histamine H4 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated response incubated for 5 hrs by luciferase reporter gene assayAgonist activity at human SF-His6-tagged histamine H4 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated response incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.6b00120
CHEMBL90 1932 None 74 Human Binding pEC50 = 7.9 7.9 -3 24
Agonist activity at human SF-His6-tagged histamine H4 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated response incubated for 5 hrs by luciferase reporter gene assayAgonist activity at human SF-His6-tagged histamine H4 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated response incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.6b00120
DB05381 1932 None 74 Human Binding pEC50 = 7.9 7.9 -3 24
Agonist activity at human SF-His6-tagged histamine H4 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated response incubated for 5 hrs by luciferase reporter gene assayAgonist activity at human SF-His6-tagged histamine H4 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated response incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.6b00120
24797956 110186 None 1 Human Binding pEC50 = 5.9 5.9 - 1
Agonist activity at human H4 receptorAgonist activity at human H4 receptor
ChEMBL 233 2 2 5 0.9 Nc1nc(C2CCCC2)cc(N2CC(N)C2)n1 10.1021/jm401727m
CHEMBL3236558 110186 None 1 Human Binding pEC50 = 5.9 5.9 - 1
Agonist activity at human H4 receptorAgonist activity at human H4 receptor
ChEMBL 233 2 2 5 0.9 Nc1nc(C2CCCC2)cc(N2CC(N)C2)n1 10.1021/jm401727m
58227373 176613 None 0 Mouse Binding pEC50 = 6.9 6.9 - 2
Agonist activity at mouse H4R expressed in HEK293T-beta-arr2-mH4R cells by beta-arrestin2 recruitment assayAgonist activity at mouse H4R expressed in HEK293T-beta-arr2-mH4R cells by beta-arrestin2 recruitment assay
ChEMBL 249 3 2 5 1.5 CC(C)(C)CNc1nccc(N2CC[C@@H](N)C2)n1 10.1021/acs.jmedchem.9b01342
CHEMBL4455324 176613 None 0 Mouse Binding pEC50 = 6.9 6.9 - 2
Agonist activity at mouse H4R expressed in HEK293T-beta-arr2-mH4R cells by beta-arrestin2 recruitment assayAgonist activity at mouse H4R expressed in HEK293T-beta-arr2-mH4R cells by beta-arrestin2 recruitment assay
ChEMBL 249 3 2 5 1.5 CC(C)(C)CNc1nccc(N2CC[C@@H](N)C2)n1 10.1021/acs.jmedchem.9b01342
CHEMBL4596881 176613 None 0 Mouse Binding pEC50 = 6.9 6.9 - 2
Agonist activity at mouse H4R expressed in HEK293T-beta-arr2-mH4R cells by beta-arrestin2 recruitment assayAgonist activity at mouse H4R expressed in HEK293T-beta-arr2-mH4R cells by beta-arrestin2 recruitment assay
ChEMBL 249 3 2 5 1.5 CC(C)(C)CNc1nccc(N2CC[C@@H](N)C2)n1 10.1021/acs.jmedchem.9b01342
155552061 176583 None 0 Human Binding pEC50 = 6.9 6.9 38 2
Agonist activity at human H4R expressed in HEK293T-beta-arr2-hH4R cells by beta-arrestin2 recruitment assayAgonist activity at human H4R expressed in HEK293T-beta-arr2-hH4R cells by beta-arrestin2 recruitment assay
ChEMBL 277 3 1 5 2.1 CN1CCCN(c2ccnc(NCC(C)(C)C)n2)CC1 10.1021/acs.jmedchem.9b01342
CHEMBL4543119 176583 None 0 Human Binding pEC50 = 6.9 6.9 38 2
Agonist activity at human H4R expressed in HEK293T-beta-arr2-hH4R cells by beta-arrestin2 recruitment assayAgonist activity at human H4R expressed in HEK293T-beta-arr2-hH4R cells by beta-arrestin2 recruitment assay
ChEMBL 277 3 1 5 2.1 CN1CCCN(c2ccnc(NCC(C)(C)C)n2)CC1 10.1021/acs.jmedchem.9b01342
CHEMBL4596606 176583 None 0 Human Binding pEC50 = 6.9 6.9 38 2
Agonist activity at human H4R expressed in HEK293T-beta-arr2-hH4R cells by beta-arrestin2 recruitment assayAgonist activity at human H4R expressed in HEK293T-beta-arr2-hH4R cells by beta-arrestin2 recruitment assay
ChEMBL 277 3 1 5 2.1 CN1CCCN(c2ccnc(NCC(C)(C)C)n2)CC1 10.1021/acs.jmedchem.9b01342
46887115 8513 None 0 Human Binding pEC50 = 5.9 5.9 - 0
Activity at human recombinant GAIP-fused histamine H4 receptor expressed in Sf9 cells coexpressing Galphai, Gbeta1gamma2 by steady-state GTPase activity assayActivity at human recombinant GAIP-fused histamine H4 receptor expressed in Sf9 cells coexpressing Galphai, Gbeta1gamma2 by steady-state GTPase activity assay
ChEMBL 365 7 4 5 3.2 Cc1nc(N)sc1CCCNC(=N)NC(=O)C[C@H](C)C1CCCCC1 10.1016/j.bmcl.2010.03.082
CHEMBL1094144 8513 None 0 Human Binding pEC50 = 5.9 5.9 - 0
Activity at human recombinant GAIP-fused histamine H4 receptor expressed in Sf9 cells coexpressing Galphai, Gbeta1gamma2 by steady-state GTPase activity assayActivity at human recombinant GAIP-fused histamine H4 receptor expressed in Sf9 cells coexpressing Galphai, Gbeta1gamma2 by steady-state GTPase activity assay
ChEMBL 365 7 4 5 3.2 Cc1nc(N)sc1CCCNC(=N)NC(=O)C[C@H](C)C1CCCCC1 10.1016/j.bmcl.2010.03.082
58227373 176613 None 0 Human Binding pEC50 = 7.8 7.8 1 2
Agonist activity at human H4R expressed in HEK293T-beta-arr2-hH4R cells by beta-arrestin2 recruitment assayAgonist activity at human H4R expressed in HEK293T-beta-arr2-hH4R cells by beta-arrestin2 recruitment assay
ChEMBL 249 3 2 5 1.5 CC(C)(C)CNc1nccc(N2CC[C@@H](N)C2)n1 10.1021/acs.jmedchem.9b01342
CHEMBL4455324 176613 None 0 Human Binding pEC50 = 7.8 7.8 1 2
Agonist activity at human H4R expressed in HEK293T-beta-arr2-hH4R cells by beta-arrestin2 recruitment assayAgonist activity at human H4R expressed in HEK293T-beta-arr2-hH4R cells by beta-arrestin2 recruitment assay
ChEMBL 249 3 2 5 1.5 CC(C)(C)CNc1nccc(N2CC[C@@H](N)C2)n1 10.1021/acs.jmedchem.9b01342
CHEMBL4596881 176613 None 0 Human Binding pEC50 = 7.8 7.8 1 2
Agonist activity at human H4R expressed in HEK293T-beta-arr2-hH4R cells by beta-arrestin2 recruitment assayAgonist activity at human H4R expressed in HEK293T-beta-arr2-hH4R cells by beta-arrestin2 recruitment assay
ChEMBL 249 3 2 5 1.5 CC(C)(C)CNc1nccc(N2CC[C@@H](N)C2)n1 10.1021/acs.jmedchem.9b01342
155517880 176772 None 0 Rat Binding pEC50 = 6.8 6.8 - 2
Agonist activity at rat H4R expressed in HEK293T-beta-arr2-rH4R cells by beta-arrestin2 recruitment assayAgonist activity at rat H4R expressed in HEK293T-beta-arr2-rH4R cells by beta-arrestin2 recruitment assay
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 176772 None 0 Rat Binding pEC50 = 6.8 6.8 - 2
Agonist activity at rat H4R expressed in HEK293T-beta-arr2-rH4R cells by beta-arrestin2 recruitment assayAgonist activity at rat H4R expressed in HEK293T-beta-arr2-rH4R cells by beta-arrestin2 recruitment assay
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 176772 None 0 Rat Binding pEC50 = 6.8 6.8 - 2
Agonist activity at rat H4R expressed in HEK293T-beta-arr2-rH4R cells by beta-arrestin2 recruitment assayAgonist activity at rat H4R expressed in HEK293T-beta-arr2-rH4R cells by beta-arrestin2 recruitment assay
ChEMBL 291 4 4 5 1.0 CC(C)(C)CNc1nccc(N2CC[C@@H](NC(=N)N)C2)n1 10.1021/acs.jmedchem.9b01342
25149335 184331 None 0 Human Binding pEC50 = 7.8 7.8 - 1
Agonist activity at human H4 receptor expressed in insect Sf9 cells co-expressing RGS19 fusion protein and Gialpha2, Gbeta1gamma2 assessed as gamma[32P]GTP binding by liquid scintillation countingAgonist activity at human H4 receptor expressed in insect Sf9 cells co-expressing RGS19 fusion protein and Gialpha2, Gbeta1gamma2 assessed as gamma[32P]GTP binding by liquid scintillation counting
ChEMBL 313 7 3 2 2.0 CC(CC(=O)/N=C(\N)NCCCc1c[nH]cn1)c1ccccc1 10.1021/jm9000693
CHEMBL483406 184331 None 0 Human Binding pEC50 = 7.8 7.8 - 1
Agonist activity at human H4 receptor expressed in insect Sf9 cells co-expressing RGS19 fusion protein and Gialpha2, Gbeta1gamma2 assessed as gamma[32P]GTP binding by liquid scintillation countingAgonist activity at human H4 receptor expressed in insect Sf9 cells co-expressing RGS19 fusion protein and Gialpha2, Gbeta1gamma2 assessed as gamma[32P]GTP binding by liquid scintillation counting
ChEMBL 313 7 3 2 2.0 CC(CC(=O)/N=C(\N)NCCCc1c[nH]cn1)c1ccccc1 10.1021/jm9000693
25149335 184331 None 0 Human Binding pEC50 = 7.8 7.8 - 1
Agonist activity at human recombinant histamine H4 receptor-RGS19 fusion protein expressed in Sf9 cells coexpressing Galphai2,Gbeta1gamma2 preincubated for 2 mins before [gamma32P]GTP addition measured after 20 mins by steady-state GTPase activity assayAgonist activity at human recombinant histamine H4 receptor-RGS19 fusion protein expressed in Sf9 cells coexpressing Galphai2,Gbeta1gamma2 preincubated for 2 mins before [gamma32P]GTP addition measured after 20 mins by steady-state GTPase activity assay
ChEMBL 313 7 3 2 2.0 CC(CC(=O)/N=C(\N)NCCCc1c[nH]cn1)c1ccccc1 10.1039/C3MD00245D
CHEMBL483406 184331 None 0 Human Binding pEC50 = 7.8 7.8 - 1
Agonist activity at human recombinant histamine H4 receptor-RGS19 fusion protein expressed in Sf9 cells coexpressing Galphai2,Gbeta1gamma2 preincubated for 2 mins before [gamma32P]GTP addition measured after 20 mins by steady-state GTPase activity assayAgonist activity at human recombinant histamine H4 receptor-RGS19 fusion protein expressed in Sf9 cells coexpressing Galphai2,Gbeta1gamma2 preincubated for 2 mins before [gamma32P]GTP addition measured after 20 mins by steady-state GTPase activity assay
ChEMBL 313 7 3 2 2.0 CC(CC(=O)/N=C(\N)NCCCc1c[nH]cn1)c1ccccc1 10.1039/C3MD00245D
25149335 184331 None 0 Human Binding pEC50 = 7.8 7.8 - 1
Activity at human recombinant histamine H4 receptor-RGS4 fusion protein expressed in Sf9 cells coexpressing Galphai2 and G-beta-1-gamma-2 by steady-state GTPase activity assayActivity at human recombinant histamine H4 receptor-RGS4 fusion protein expressed in Sf9 cells coexpressing Galphai2 and G-beta-1-gamma-2 by steady-state GTPase activity assay
ChEMBL 313 7 3 2 2.0 CC(CC(=O)/N=C(\N)NCCCc1c[nH]cn1)c1ccccc1 10.1021/jm800841w
CHEMBL483406 184331 None 0 Human Binding pEC50 = 7.8 7.8 - 1
Activity at human recombinant histamine H4 receptor-RGS4 fusion protein expressed in Sf9 cells coexpressing Galphai2 and G-beta-1-gamma-2 by steady-state GTPase activity assayActivity at human recombinant histamine H4 receptor-RGS4 fusion protein expressed in Sf9 cells coexpressing Galphai2 and G-beta-1-gamma-2 by steady-state GTPase activity assay
ChEMBL 313 7 3 2 2.0 CC(CC(=O)/N=C(\N)NCCCc1c[nH]cn1)c1ccccc1 10.1021/jm800841w
45267230 198938 None 0 Human Binding pEC50 = 7.8 7.8 -1 2
Agonist activity at histamine H4 receptor (unknown origin) expressed in human U2OS cells increase in beta-arrestin2 recruitment after 2 hrs by luminescence assayAgonist activity at histamine H4 receptor (unknown origin) expressed in human U2OS cells increase in beta-arrestin2 recruitment after 2 hrs by luminescence assay
ChEMBL 308 6 3 3 3.5 N=C(NCc1ccccc1Cl)SCCCc1c[nH]cn1 10.1021/acs.jmedchem.8b00435
CHEMBL1202318 198938 None 0 Human Binding pEC50 = 7.8 7.8 -1 2
Agonist activity at histamine H4 receptor (unknown origin) expressed in human U2OS cells increase in beta-arrestin2 recruitment after 2 hrs by luminescence assayAgonist activity at histamine H4 receptor (unknown origin) expressed in human U2OS cells increase in beta-arrestin2 recruitment after 2 hrs by luminescence assay
ChEMBL 308 6 3 3 3.5 N=C(NCc1ccccc1Cl)SCCCc1c[nH]cn1 10.1021/acs.jmedchem.8b00435
CHEMBL563342 198938 None 0 Human Binding pEC50 = 7.8 7.8 -1 2
Agonist activity at histamine H4 receptor (unknown origin) expressed in human U2OS cells increase in beta-arrestin2 recruitment after 2 hrs by luminescence assayAgonist activity at histamine H4 receptor (unknown origin) expressed in human U2OS cells increase in beta-arrestin2 recruitment after 2 hrs by luminescence assay
ChEMBL 308 6 3 3 3.5 N=C(NCc1ccccc1Cl)SCCCc1c[nH]cn1 10.1021/acs.jmedchem.8b00435
42625223 180031 None 0 Human Binding pEC50 = 6.8 6.8 - 1
Agonist activity at human H4 receptor expressed in insect Sf9 cells co-expressing RGS19 fusion protein and Gialpha2, Gbeta1gamma2 assessed as gamma[32P]GTP binding by liquid scintillation countingAgonist activity at human H4 receptor expressed in insect Sf9 cells co-expressing RGS19 fusion protein and Gialpha2, Gbeta1gamma2 assessed as gamma[32P]GTP binding by liquid scintillation counting
ChEMBL 395 8 4 3 1.4 CN(CCC(=O)/N=C(\N)NCCCc1c[nH]cn1)C(=O)c1cc2ccccc2[nH]1 10.1021/jm9000693
CHEMBL474617 180031 None 0 Human Binding pEC50 = 6.8 6.8 - 1
Agonist activity at human H4 receptor expressed in insect Sf9 cells co-expressing RGS19 fusion protein and Gialpha2, Gbeta1gamma2 assessed as gamma[32P]GTP binding by liquid scintillation countingAgonist activity at human H4 receptor expressed in insect Sf9 cells co-expressing RGS19 fusion protein and Gialpha2, Gbeta1gamma2 assessed as gamma[32P]GTP binding by liquid scintillation counting
ChEMBL 395 8 4 3 1.4 CN(CCC(=O)/N=C(\N)NCCCc1c[nH]cn1)C(=O)c1cc2ccccc2[nH]1 10.1021/jm9000693
11240759 105269 None 1 Human Binding pEC50 = 5.8 5.8 -190 2
Inhibition of the cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H4 receptorInhibition of the cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H4 receptor
ChEMBL 173 3 1 2 1.6 c1cc(CCc2c[nH]cn2)ccn1 10.1021/jm049932u
CHEMBL311473 105269 None 1 Human Binding pEC50 = 5.8 5.8 -190 2
Inhibition of the cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H4 receptorInhibition of the cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H4 receptor
ChEMBL 173 3 1 2 1.6 c1cc(CCc2c[nH]cn2)ccn1 10.1021/jm049932u
9812843 207702 None 1 Human Binding pEC50 = 4.8 4.8 -4 2
Inhibition of the cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H4 receptorInhibition of the cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H4 receptor
ChEMBL 159 2 1 2 1.4 c1cncc(Cc2c[nH]cn2)c1 10.1021/jm049932u
CHEMBL78838 207702 None 1 Human Binding pEC50 = 4.8 4.8 -4 2
Inhibition of the cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H4 receptorInhibition of the cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H4 receptor
ChEMBL 159 2 1 2 1.4 c1cncc(Cc2c[nH]cn2)c1 10.1021/jm049932u
11469514 104223 None 0 Human Binding pEC50 = 5.8 5.8 -64 2
Inhibition of the cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H4 receptorInhibition of the cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H4 receptor
ChEMBL 187 4 1 2 2.0 c1cc(CCCc2c[nH]cn2)ccn1 10.1021/jm049932u
CHEMBL309654 104223 None 0 Human Binding pEC50 = 5.8 5.8 -64 2
Inhibition of the cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H4 receptorInhibition of the cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H4 receptor
ChEMBL 187 4 1 2 2.0 c1cc(CCCc2c[nH]cn2)ccn1 10.1021/jm049932u
155524115 176652 None 0 Rat Binding pEC50 = 7.8 7.8 - 3
Agonist activity at rat H4R expressed in HEK293T-beta-arr2-rH4R cells by beta-arrestin2 recruitment assayAgonist activity at rat H4R expressed in HEK293T-beta-arr2-rH4R cells by beta-arrestin2 recruitment assay
ChEMBL 286 3 2 5 2.2 CC(C)(C)CNc1nccc(N2CCc3nc[nH]c3C2)n1 10.1021/acs.jmedchem.9b01342
CHEMBL4454158 176652 None 0 Rat Binding pEC50 = 7.8 7.8 - 3
Agonist activity at rat H4R expressed in HEK293T-beta-arr2-rH4R cells by beta-arrestin2 recruitment assayAgonist activity at rat H4R expressed in HEK293T-beta-arr2-rH4R cells by beta-arrestin2 recruitment assay
ChEMBL 286 3 2 5 2.2 CC(C)(C)CNc1nccc(N2CCc3nc[nH]c3C2)n1 10.1021/acs.jmedchem.9b01342
CHEMBL4597218 176652 None 0 Rat Binding pEC50 = 7.8 7.8 - 3
Agonist activity at rat H4R expressed in HEK293T-beta-arr2-rH4R cells by beta-arrestin2 recruitment assayAgonist activity at rat H4R expressed in HEK293T-beta-arr2-rH4R cells by beta-arrestin2 recruitment assay
ChEMBL 286 3 2 5 2.2 CC(C)(C)CNc1nccc(N2CCc3nc[nH]c3C2)n1 10.1021/acs.jmedchem.9b01342
127052293 140325 None 3 Mouse Binding pEC50 = 6.8 6.8 - 4
Agonist activity at mouse SF-His6-tagged histamine H4 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated response incubated for 5 hrs by luciferase reporter gene assayAgonist activity at mouse SF-His6-tagged histamine H4 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated response incubated for 5 hrs by luciferase reporter gene assay
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 140325 None 3 Mouse Binding pEC50 = 6.8 6.8 - 4
Agonist activity at mouse SF-His6-tagged histamine H4 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated response incubated for 5 hrs by luciferase reporter gene assayAgonist activity at mouse SF-His6-tagged histamine H4 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated response incubated for 5 hrs by luciferase reporter gene assay
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
155513612 176425 None 0 Human Binding pEC50 = 7.7 7.7 1 4
Agonist activity at human H4R expressed in HEK293T-beta-arr2-hH4R cells by beta-arrestin2 recruitment assayAgonist activity at human H4R expressed in HEK293T-beta-arr2-hH4R cells by beta-arrestin2 recruitment assay
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 176425 None 0 Human Binding pEC50 = 7.7 7.7 1 4
Agonist activity at human H4R expressed in HEK293T-beta-arr2-hH4R cells by beta-arrestin2 recruitment assayAgonist activity at human H4R expressed in HEK293T-beta-arr2-hH4R cells by beta-arrestin2 recruitment assay
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 176425 None 0 Human Binding pEC50 = 7.7 7.7 1 4
Agonist activity at human H4R expressed in HEK293T-beta-arr2-hH4R cells by beta-arrestin2 recruitment assayAgonist activity at human H4R expressed in HEK293T-beta-arr2-hH4R cells by beta-arrestin2 recruitment assay
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 176425 None 0 Human Binding pEC50 = 7.7 7.7 1 4
Agonist activity at human H4R expressed in HEK293T-beta-arr2-hH4R cells by beta-arrestin2 recruitment assayAgonist activity at human H4R expressed in HEK293T-beta-arr2-hH4R cells by beta-arrestin2 recruitment assay
ChEMBL 277 4 1 5 2.1 CN(C)[C@@H]1CCN(c2ccnc(NCC(C)(C)C)n2)C1 10.1021/acs.jmedchem.9b01342
42626109 179874 None 0 Human Binding pEC50 = 7.7 7.7 - 1
Agonist activity at human H4 receptor expressed in insect Sf9 cells co-expressing RGS19 fusion protein and Gialpha2, Gbeta1gamma2 assessed as gamma[32P]GTP binding by liquid scintillation countingAgonist activity at human H4 receptor expressed in insect Sf9 cells co-expressing RGS19 fusion protein and Gialpha2, Gbeta1gamma2 assessed as gamma[32P]GTP binding by liquid scintillation counting
ChEMBL 324 6 4 2 1.5 N/C(=N\C(=O)Cc1c[nH]c2ccccc12)NCCCc1c[nH]cn1 10.1021/jm9000693
CHEMBL474447 179874 None 0 Human Binding pEC50 = 7.7 7.7 - 1
Agonist activity at human H4 receptor expressed in insect Sf9 cells co-expressing RGS19 fusion protein and Gialpha2, Gbeta1gamma2 assessed as gamma[32P]GTP binding by liquid scintillation countingAgonist activity at human H4 receptor expressed in insect Sf9 cells co-expressing RGS19 fusion protein and Gialpha2, Gbeta1gamma2 assessed as gamma[32P]GTP binding by liquid scintillation counting
ChEMBL 324 6 4 2 1.5 N/C(=N\C(=O)Cc1c[nH]c2ccccc12)NCCCc1c[nH]cn1 10.1021/jm9000693
155512725 176346 None 0 Rat Binding pEC50 = 6.7 6.7 - 2
Agonist activity at rat H4R expressed in HEK293T-beta-arr2-rH4R cells by beta-arrestin2 recruitment assayAgonist activity at rat H4R expressed in HEK293T-beta-arr2-rH4R cells by beta-arrestin2 recruitment assay
ChEMBL 237 6 3 5 1.7 CC(C)(C)CNc1nccc(NCCCN)n1 10.1021/acs.jmedchem.9b01342
CHEMBL4437371 176346 None 0 Rat Binding pEC50 = 6.7 6.7 - 2
Agonist activity at rat H4R expressed in HEK293T-beta-arr2-rH4R cells by beta-arrestin2 recruitment assayAgonist activity at rat H4R expressed in HEK293T-beta-arr2-rH4R cells by beta-arrestin2 recruitment assay
ChEMBL 237 6 3 5 1.7 CC(C)(C)CNc1nccc(NCCCN)n1 10.1021/acs.jmedchem.9b01342
CHEMBL4594753 176346 None 0 Rat Binding pEC50 = 6.7 6.7 - 2
Agonist activity at rat H4R expressed in HEK293T-beta-arr2-rH4R cells by beta-arrestin2 recruitment assayAgonist activity at rat H4R expressed in HEK293T-beta-arr2-rH4R cells by beta-arrestin2 recruitment assay
ChEMBL 237 6 3 5 1.7 CC(C)(C)CNc1nccc(NCCCN)n1 10.1021/acs.jmedchem.9b01342
42625386 178458 None 0 Human Binding pEC50 = 8.6 8.6 - 1
Agonist activity at human H4 receptor expressed in insect Sf9 cells co-expressing RGS19 fusion protein and Gialpha2, Gbeta1gamma2 assessed as gamma[32P]GTP binding by liquid scintillation countingAgonist activity at human H4 receptor expressed in insect Sf9 cells co-expressing RGS19 fusion protein and Gialpha2, Gbeta1gamma2 assessed as gamma[32P]GTP binding by liquid scintillation counting
ChEMBL 237 6 3 2 0.6 CCCC(=O)/N=C(\N)NCCCc1c[nH]cn1 10.1021/jm9000693
CHEMBL465170 178458 None 0 Human Binding pEC50 = 8.6 8.6 - 1
Agonist activity at human H4 receptor expressed in insect Sf9 cells co-expressing RGS19 fusion protein and Gialpha2, Gbeta1gamma2 assessed as gamma[32P]GTP binding by liquid scintillation countingAgonist activity at human H4 receptor expressed in insect Sf9 cells co-expressing RGS19 fusion protein and Gialpha2, Gbeta1gamma2 assessed as gamma[32P]GTP binding by liquid scintillation counting
ChEMBL 237 6 3 2 0.6 CCCC(=O)/N=C(\N)NCCCc1c[nH]cn1 10.1021/jm9000693
46830167 8763 None 0 Human Binding pEC50 = 8.6 8.6 - 0
Activity at human recombinant GAIP-fused histamine H4 receptor expressed in Sf9 cells coexpressing Galphai, Gbeta1gamma2 by steady-state GTPase activity assayActivity at human recombinant GAIP-fused histamine H4 receptor expressed in Sf9 cells coexpressing Galphai, Gbeta1gamma2 by steady-state GTPase activity assay
ChEMBL 313 7 4 3 2.2 C[C@@H](CC(=O)NC(=N)NCCCc1c[nH]cn1)c1ccccc1 10.1016/j.bmcl.2010.03.082
CHEMBL1096429 8763 None 0 Human Binding pEC50 = 8.6 8.6 - 0
Activity at human recombinant GAIP-fused histamine H4 receptor expressed in Sf9 cells coexpressing Galphai, Gbeta1gamma2 by steady-state GTPase activity assayActivity at human recombinant GAIP-fused histamine H4 receptor expressed in Sf9 cells coexpressing Galphai, Gbeta1gamma2 by steady-state GTPase activity assay
ChEMBL 313 7 4 3 2.2 C[C@@H](CC(=O)NC(=N)NCCCc1c[nH]cn1)c1ccccc1 10.1016/j.bmcl.2010.03.082
11171320 45942 None 2 Human Binding pEC50 = 5.7 5.7 - 1
Inhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H4 receptorInhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H4 receptor
ChEMBL 179 3 2 2 1.3 c1nc(CCC2CCCNC2)c[nH]1 10.1021/jm030905y
CHEMBL153207 45942 None 2 Human Binding pEC50 = 5.7 5.7 - 1
Inhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H4 receptorInhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H4 receptor
ChEMBL 179 3 2 2 1.3 c1nc(CCC2CCCNC2)c[nH]1 10.1021/jm030905y
170389 209439 None 25 Human Binding pEC50 = 6.7 6.7 1 3
Inhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H4 receptorInhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H4 receptor
ChEMBL 125 3 2 2 0.3 NCCCc1c[nH]cn1 10.1021/jm030905y
CHEMBL4634086 209439 None 25 Human Binding pEC50 = 6.7 6.7 1 3
Inhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H4 receptorInhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H4 receptor
ChEMBL 125 3 2 2 0.3 NCCCc1c[nH]cn1 10.1021/jm030905y
CHEMBL91353 209439 None 25 Human Binding pEC50 = 6.7 6.7 1 3
Inhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H4 receptorInhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H4 receptor
ChEMBL 125 3 2 2 0.3 NCCCc1c[nH]cn1 10.1021/jm030905y
46887041 8762 None 1 Human Binding pEC50 = 7.6 7.6 - 0
Activity at human recombinant GAIP-fused histamine H4 receptor expressed in Sf9 cells coexpressing Galphai, Gbeta1gamma2 by steady-state GTPase activity assayActivity at human recombinant GAIP-fused histamine H4 receptor expressed in Sf9 cells coexpressing Galphai, Gbeta1gamma2 by steady-state GTPase activity assay
ChEMBL 313 7 4 3 2.2 C[C@H](CC(=O)NC(=N)NCCCc1c[nH]cn1)c1ccccc1 10.1016/j.bmcl.2010.03.082
CHEMBL1096428 8762 None 1 Human Binding pEC50 = 7.6 7.6 - 0
Activity at human recombinant GAIP-fused histamine H4 receptor expressed in Sf9 cells coexpressing Galphai, Gbeta1gamma2 by steady-state GTPase activity assayActivity at human recombinant GAIP-fused histamine H4 receptor expressed in Sf9 cells coexpressing Galphai, Gbeta1gamma2 by steady-state GTPase activity assay
ChEMBL 313 7 4 3 2.2 C[C@H](CC(=O)NC(=N)NCCCc1c[nH]cn1)c1ccccc1 10.1016/j.bmcl.2010.03.082
155517880 176772 None 0 Mouse Binding pEC50 = 6.6 6.6 - 2
Agonist activity at mouse H4R expressed in HEK293T-beta-arr2-mH4R cells by beta-arrestin2 recruitment assayAgonist activity at mouse H4R expressed in HEK293T-beta-arr2-mH4R cells by beta-arrestin2 recruitment assay
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 176772 None 0 Mouse Binding pEC50 = 6.6 6.6 - 2
Agonist activity at mouse H4R expressed in HEK293T-beta-arr2-mH4R cells by beta-arrestin2 recruitment assayAgonist activity at mouse H4R expressed in HEK293T-beta-arr2-mH4R cells by beta-arrestin2 recruitment assay
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 176772 None 0 Mouse Binding pEC50 = 6.6 6.6 - 2
Agonist activity at mouse H4R expressed in HEK293T-beta-arr2-mH4R cells by beta-arrestin2 recruitment assayAgonist activity at mouse H4R expressed in HEK293T-beta-arr2-mH4R cells by beta-arrestin2 recruitment assay
ChEMBL 291 4 4 5 1.0 CC(C)(C)CNc1nccc(N2CC[C@@H](NC(=N)N)C2)n1 10.1021/acs.jmedchem.9b01342
1204 1932 None 74 Mouse Binding pEC50 = 5.6 5.6 -15 24
Agonist activity at mouse H4R expressed in HEK293 cells co-expressing ELucC/ELucN-beta-arrestin2 assessed as induction of beta-arrestin recruitment by luciferase reporter gene assayAgonist activity at mouse H4R expressed in HEK293 cells co-expressing ELucC/ELucN-beta-arrestin2 assessed as induction of beta-arrestin recruitment by luciferase reporter gene assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.0c00160
1247 1932 None 74 Mouse Binding pEC50 = 5.6 5.6 -15 24
Agonist activity at mouse H4R expressed in HEK293 cells co-expressing ELucC/ELucN-beta-arrestin2 assessed as induction of beta-arrestin recruitment by luciferase reporter gene assayAgonist activity at mouse H4R expressed in HEK293 cells co-expressing ELucC/ELucN-beta-arrestin2 assessed as induction of beta-arrestin recruitment by luciferase reporter gene assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.0c00160
1375 1932 None 74 Mouse Binding pEC50 = 5.6 5.6 -15 24
Agonist activity at mouse H4R expressed in HEK293 cells co-expressing ELucC/ELucN-beta-arrestin2 assessed as induction of beta-arrestin recruitment by luciferase reporter gene assayAgonist activity at mouse H4R expressed in HEK293 cells co-expressing ELucC/ELucN-beta-arrestin2 assessed as induction of beta-arrestin recruitment by luciferase reporter gene assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.0c00160
774 1932 None 74 Mouse Binding pEC50 = 5.6 5.6 -15 24
Agonist activity at mouse H4R expressed in HEK293 cells co-expressing ELucC/ELucN-beta-arrestin2 assessed as induction of beta-arrestin recruitment by luciferase reporter gene assayAgonist activity at mouse H4R expressed in HEK293 cells co-expressing ELucC/ELucN-beta-arrestin2 assessed as induction of beta-arrestin recruitment by luciferase reporter gene assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.0c00160
774.0 1932 None 74 Mouse Binding pEC50 = 5.6 5.6 -15 24
Agonist activity at mouse H4R expressed in HEK293 cells co-expressing ELucC/ELucN-beta-arrestin2 assessed as induction of beta-arrestin recruitment by luciferase reporter gene assayAgonist activity at mouse H4R expressed in HEK293 cells co-expressing ELucC/ELucN-beta-arrestin2 assessed as induction of beta-arrestin recruitment by luciferase reporter gene assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.0c00160
CHEMBL90 1932 None 74 Mouse Binding pEC50 = 5.6 5.6 -15 24
Agonist activity at mouse H4R expressed in HEK293 cells co-expressing ELucC/ELucN-beta-arrestin2 assessed as induction of beta-arrestin recruitment by luciferase reporter gene assayAgonist activity at mouse H4R expressed in HEK293 cells co-expressing ELucC/ELucN-beta-arrestin2 assessed as induction of beta-arrestin recruitment by luciferase reporter gene assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.0c00160
DB05381 1932 None 74 Mouse Binding pEC50 = 5.6 5.6 -15 24
Agonist activity at mouse H4R expressed in HEK293 cells co-expressing ELucC/ELucN-beta-arrestin2 assessed as induction of beta-arrestin recruitment by luciferase reporter gene assayAgonist activity at mouse H4R expressed in HEK293 cells co-expressing ELucC/ELucN-beta-arrestin2 assessed as induction of beta-arrestin recruitment by luciferase reporter gene assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.0c00160
1204 1932 None 74 Mouse Binding pEC50 = 5.6 5.6 -15 24
Agonist activity at mouse H4R expressed in HEK293T-beta-arr2-mH4R cells by beta-arrestin2 recruitment assayAgonist activity at mouse H4R expressed in HEK293T-beta-arr2-mH4R cells by beta-arrestin2 recruitment assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.9b01342
1247 1932 None 74 Mouse Binding pEC50 = 5.6 5.6 -15 24
Agonist activity at mouse H4R expressed in HEK293T-beta-arr2-mH4R cells by beta-arrestin2 recruitment assayAgonist activity at mouse H4R expressed in HEK293T-beta-arr2-mH4R cells by beta-arrestin2 recruitment assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.9b01342
1375 1932 None 74 Mouse Binding pEC50 = 5.6 5.6 -15 24
Agonist activity at mouse H4R expressed in HEK293T-beta-arr2-mH4R cells by beta-arrestin2 recruitment assayAgonist activity at mouse H4R expressed in HEK293T-beta-arr2-mH4R cells by beta-arrestin2 recruitment assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.9b01342
774 1932 None 74 Mouse Binding pEC50 = 5.6 5.6 -15 24
Agonist activity at mouse H4R expressed in HEK293T-beta-arr2-mH4R cells by beta-arrestin2 recruitment assayAgonist activity at mouse H4R expressed in HEK293T-beta-arr2-mH4R cells by beta-arrestin2 recruitment assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.9b01342
774.0 1932 None 74 Mouse Binding pEC50 = 5.6 5.6 -15 24
Agonist activity at mouse H4R expressed in HEK293T-beta-arr2-mH4R cells by beta-arrestin2 recruitment assayAgonist activity at mouse H4R expressed in HEK293T-beta-arr2-mH4R cells by beta-arrestin2 recruitment assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.9b01342
CHEMBL90 1932 None 74 Mouse Binding pEC50 = 5.6 5.6 -15 24
Agonist activity at mouse H4R expressed in HEK293T-beta-arr2-mH4R cells by beta-arrestin2 recruitment assayAgonist activity at mouse H4R expressed in HEK293T-beta-arr2-mH4R cells by beta-arrestin2 recruitment assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.9b01342
DB05381 1932 None 74 Mouse Binding pEC50 = 5.6 5.6 -15 24
Agonist activity at mouse H4R expressed in HEK293T-beta-arr2-mH4R cells by beta-arrestin2 recruitment assayAgonist activity at mouse H4R expressed in HEK293T-beta-arr2-mH4R cells by beta-arrestin2 recruitment assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.9b01342
127052293 140325 None 3 Human Binding pEC50 = 7.6 7.6 34 4
Agonist activity at human SF-His6-tagged histamine H4 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated response incubated for 5 hrs by luciferase reporter gene assayAgonist activity at human SF-His6-tagged histamine H4 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated response incubated for 5 hrs by luciferase reporter gene assay
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 140325 None 3 Human Binding pEC50 = 7.6 7.6 34 4
Agonist activity at human SF-His6-tagged histamine H4 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated response incubated for 5 hrs by luciferase reporter gene assayAgonist activity at human SF-His6-tagged histamine H4 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated response incubated for 5 hrs by luciferase reporter gene assay
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
11301441 96207 None 12 Human Binding pEC50 = 7.6 7.6 - 1
Agonist activity at histamine H4 receptor (unknown origin) expressed in human U2OS cells increase in beta-arrestin2 recruitment after 2 hrs by luminescence assayAgonist activity at histamine H4 receptor (unknown origin) expressed in human U2OS cells increase in beta-arrestin2 recruitment after 2 hrs by luminescence assay
ChEMBL 312 1 1 4 2.0 CN1CCN(c2nc3cc(Cl)c(Cl)cc3[nH]c2=O)CC1 10.1021/acs.jmedchem.8b00435
CHEMBL260549 96207 None 12 Human Binding pEC50 = 7.6 7.6 - 1
Agonist activity at histamine H4 receptor (unknown origin) expressed in human U2OS cells increase in beta-arrestin2 recruitment after 2 hrs by luminescence assayAgonist activity at histamine H4 receptor (unknown origin) expressed in human U2OS cells increase in beta-arrestin2 recruitment after 2 hrs by luminescence assay
ChEMBL 312 1 1 4 2.0 CN1CCN(c2nc3cc(Cl)c(Cl)cc3[nH]c2=O)CC1 10.1021/acs.jmedchem.8b00435
1278 2150 None 56 Human Binding pEC50 = 7.6 7.6 -3 8
Agonist activity at human H4R expressed in human U2OS cells assessed as recruitment of beta-arrestin after 2 hrs by PathHunter beta-galactosidase enzyme fragment complementation assayAgonist activity at human H4R expressed in human U2OS cells assessed as recruitment of beta-arrestin after 2 hrs by PathHunter beta-galactosidase enzyme fragment complementation assay
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/jm401677g
1279 2150 None 56 Human Binding pEC50 = 7.6 7.6 -3 8
Agonist activity at human H4R expressed in human U2OS cells assessed as recruitment of beta-arrestin after 2 hrs by PathHunter beta-galactosidase enzyme fragment complementation assayAgonist activity at human H4R expressed in human U2OS cells assessed as recruitment of beta-arrestin after 2 hrs by PathHunter beta-galactosidase enzyme fragment complementation assay
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/jm401677g
4908365 2150 None 56 Human Binding pEC50 = 7.6 7.6 -3 8
Agonist activity at human H4R expressed in human U2OS cells assessed as recruitment of beta-arrestin after 2 hrs by PathHunter beta-galactosidase enzyme fragment complementation assayAgonist activity at human H4R expressed in human U2OS cells assessed as recruitment of beta-arrestin after 2 hrs by PathHunter beta-galactosidase enzyme fragment complementation assay
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/jm401677g
CHEMBL129198 2150 None 56 Human Binding pEC50 = 7.6 7.6 -3 8
Agonist activity at human H4R expressed in human U2OS cells assessed as recruitment of beta-arrestin after 2 hrs by PathHunter beta-galactosidase enzyme fragment complementation assayAgonist activity at human H4R expressed in human U2OS cells assessed as recruitment of beta-arrestin after 2 hrs by PathHunter beta-galactosidase enzyme fragment complementation assay
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/jm401677g
58227401 176556 None 0 Mouse Binding pEC50 = 7.6 7.6 - 2
Agonist activity at mouse H4R expressed in HEK293T-beta-arr2-mH4R cells by beta-arrestin2 recruitment assayAgonist activity at mouse H4R expressed in HEK293T-beta-arr2-mH4R cells by beta-arrestin2 recruitment assay
ChEMBL 263 4 2 5 1.7 CN[C@@H]1CCN(c2ccnc(NCC(C)(C)C)n2)C1 10.1021/acs.jmedchem.9b01342
CHEMBL4443126 176556 None 0 Mouse Binding pEC50 = 7.6 7.6 - 2
Agonist activity at mouse H4R expressed in HEK293T-beta-arr2-mH4R cells by beta-arrestin2 recruitment assayAgonist activity at mouse H4R expressed in HEK293T-beta-arr2-mH4R cells by beta-arrestin2 recruitment assay
ChEMBL 263 4 2 5 1.7 CN[C@@H]1CCN(c2ccnc(NCC(C)(C)C)n2)C1 10.1021/acs.jmedchem.9b01342
CHEMBL4596409 176556 None 0 Mouse Binding pEC50 = 7.6 7.6 - 2
Agonist activity at mouse H4R expressed in HEK293T-beta-arr2-mH4R cells by beta-arrestin2 recruitment assayAgonist activity at mouse H4R expressed in HEK293T-beta-arr2-mH4R cells by beta-arrestin2 recruitment assay
ChEMBL 263 4 2 5 1.7 CN[C@@H]1CCN(c2ccnc(NCC(C)(C)C)n2)C1 10.1021/acs.jmedchem.9b01342
155513612 176425 None 0 Rat Binding pEC50 = 7.6 7.6 -2 4
Agonist activity at rat H4R expressed in HEK293T-beta-arr2-rH4R cells by beta-arrestin2 recruitment assayAgonist activity at rat H4R expressed in HEK293T-beta-arr2-rH4R cells by beta-arrestin2 recruitment assay
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 176425 None 0 Rat Binding pEC50 = 7.6 7.6 -2 4
Agonist activity at rat H4R expressed in HEK293T-beta-arr2-rH4R cells by beta-arrestin2 recruitment assayAgonist activity at rat H4R expressed in HEK293T-beta-arr2-rH4R cells by beta-arrestin2 recruitment assay
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 176425 None 0 Rat Binding pEC50 = 7.6 7.6 -2 4
Agonist activity at rat H4R expressed in HEK293T-beta-arr2-rH4R cells by beta-arrestin2 recruitment assayAgonist activity at rat H4R expressed in HEK293T-beta-arr2-rH4R cells by beta-arrestin2 recruitment assay
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 176425 None 0 Rat Binding pEC50 = 7.6 7.6 -2 4
Agonist activity at rat H4R expressed in HEK293T-beta-arr2-rH4R cells by beta-arrestin2 recruitment assayAgonist activity at rat H4R expressed in HEK293T-beta-arr2-rH4R cells by beta-arrestin2 recruitment assay
ChEMBL 277 4 1 5 2.1 CN(C)[C@@H]1CCN(c2ccnc(NCC(C)(C)C)n2)C1 10.1021/acs.jmedchem.9b01342
42625222 179876 None 0 Human Binding pEC50 = 7.6 7.6 - 0
Agonist activity at human H4 receptor expressed in insect Sf9 cells co-expressing RGS19 fusion protein and Gialpha2, Gbeta1gamma2 assessed as gamma[32P]GTP binding by liquid scintillation countingAgonist activity at human H4 receptor expressed in insect Sf9 cells co-expressing RGS19 fusion protein and Gialpha2, Gbeta1gamma2 assessed as gamma[32P]GTP binding by liquid scintillation counting
ChEMBL 367 7 5 3 0.7 N/C(=N\C(=O)CNC(=O)c1cc2ccccc2[nH]1)NCCCc1c[nH]cn1 10.1021/jm9000693
CHEMBL474449 179876 None 0 Human Binding pEC50 = 7.6 7.6 - 0
Agonist activity at human H4 receptor expressed in insect Sf9 cells co-expressing RGS19 fusion protein and Gialpha2, Gbeta1gamma2 assessed as gamma[32P]GTP binding by liquid scintillation countingAgonist activity at human H4 receptor expressed in insect Sf9 cells co-expressing RGS19 fusion protein and Gialpha2, Gbeta1gamma2 assessed as gamma[32P]GTP binding by liquid scintillation counting
ChEMBL 367 7 5 3 0.7 N/C(=N\C(=O)CNC(=O)c1cc2ccccc2[nH]1)NCCCc1c[nH]cn1 10.1021/jm9000693
1267 3804 None 32 Mouse Binding pEC50 = 7.6 7.6 -21 27
Antagonist activity at mouse H4R expressed in HEK293 cells co-expressing ELucC/ELucN-beta-arrestin2 assessed as inhibition of histamine-induced beta-arrestin recruitment preincubated for 15 mins followed by histamine addition by luciferase reporter gene assayAntagonist activity at mouse H4R expressed in HEK293 cells co-expressing ELucC/ELucN-beta-arrestin2 assessed as inhibition of histamine-induced beta-arrestin recruitment preincubated for 15 mins followed by histamine addition by luciferase reporter gene assay
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1021/acs.jmedchem.0c00160
3035905 3804 None 32 Mouse Binding pEC50 = 7.6 7.6 -21 27
Antagonist activity at mouse H4R expressed in HEK293 cells co-expressing ELucC/ELucN-beta-arrestin2 assessed as inhibition of histamine-induced beta-arrestin recruitment preincubated for 15 mins followed by histamine addition by luciferase reporter gene assayAntagonist activity at mouse H4R expressed in HEK293 cells co-expressing ELucC/ELucN-beta-arrestin2 assessed as inhibition of histamine-induced beta-arrestin recruitment preincubated for 15 mins followed by histamine addition by luciferase reporter gene assay
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1021/acs.jmedchem.0c00160
CHEMBL260374 3804 None 32 Mouse Binding pEC50 = 7.6 7.6 -21 27
Antagonist activity at mouse H4R expressed in HEK293 cells co-expressing ELucC/ELucN-beta-arrestin2 assessed as inhibition of histamine-induced beta-arrestin recruitment preincubated for 15 mins followed by histamine addition by luciferase reporter gene assayAntagonist activity at mouse H4R expressed in HEK293 cells co-expressing ELucC/ELucN-beta-arrestin2 assessed as inhibition of histamine-induced beta-arrestin recruitment preincubated for 15 mins followed by histamine addition by luciferase reporter gene assay
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1021/acs.jmedchem.0c00160
90667228 109525 None 0 Human Binding pEC50 = 5.5 5.5 - 0
Agonist activity at human recombinant histamine H4 receptor-RGS19 fusion protein expressed in Sf9 cells coexpressing Galphai2,Gbeta1gamma2 preincubated for 2 mins before [gamma32P]GTP addition measured after 20 mins by steady-state GTPase activity assayAgonist activity at human recombinant histamine H4 receptor-RGS19 fusion protein expressed in Sf9 cells coexpressing Galphai2,Gbeta1gamma2 preincubated for 2 mins before [gamma32P]GTP addition measured after 20 mins by steady-state GTPase activity assay
ChEMBL 313 7 3 2 2.0 CC(CC(=O)/N=C(\N)NCCCc1ncc[nH]1)c1ccccc1 10.1039/C3MD00245D
CHEMBL3220629 109525 None 0 Human Binding pEC50 = 5.5 5.5 - 0
Agonist activity at human recombinant histamine H4 receptor-RGS19 fusion protein expressed in Sf9 cells coexpressing Galphai2,Gbeta1gamma2 preincubated for 2 mins before [gamma32P]GTP addition measured after 20 mins by steady-state GTPase activity assayAgonist activity at human recombinant histamine H4 receptor-RGS19 fusion protein expressed in Sf9 cells coexpressing Galphai2,Gbeta1gamma2 preincubated for 2 mins before [gamma32P]GTP addition measured after 20 mins by steady-state GTPase activity assay
ChEMBL 313 7 3 2 2.0 CC(CC(=O)/N=C(\N)NCCCc1ncc[nH]1)c1ccccc1 10.1039/C3MD00245D
58227401 176556 None 0 Rat Binding pEC50 = 7.5 7.5 - 2
Agonist activity at rat H4R expressed in HEK293T-beta-arr2-rH4R cells by beta-arrestin2 recruitment assayAgonist activity at rat H4R expressed in HEK293T-beta-arr2-rH4R cells by beta-arrestin2 recruitment assay
ChEMBL 263 4 2 5 1.7 CN[C@@H]1CCN(c2ccnc(NCC(C)(C)C)n2)C1 10.1021/acs.jmedchem.9b01342
CHEMBL4443126 176556 None 0 Rat Binding pEC50 = 7.5 7.5 - 2
Agonist activity at rat H4R expressed in HEK293T-beta-arr2-rH4R cells by beta-arrestin2 recruitment assayAgonist activity at rat H4R expressed in HEK293T-beta-arr2-rH4R cells by beta-arrestin2 recruitment assay
ChEMBL 263 4 2 5 1.7 CN[C@@H]1CCN(c2ccnc(NCC(C)(C)C)n2)C1 10.1021/acs.jmedchem.9b01342
CHEMBL4596409 176556 None 0 Rat Binding pEC50 = 7.5 7.5 - 2
Agonist activity at rat H4R expressed in HEK293T-beta-arr2-rH4R cells by beta-arrestin2 recruitment assayAgonist activity at rat H4R expressed in HEK293T-beta-arr2-rH4R cells by beta-arrestin2 recruitment assay
ChEMBL 263 4 2 5 1.7 CN[C@@H]1CCN(c2ccnc(NCC(C)(C)C)n2)C1 10.1021/acs.jmedchem.9b01342
42625303 180872 None 0 Human Binding pEC50 = 8.5 8.5 - 1
Agonist activity at human H4 receptor expressed in insect Sf9 cells co-expressing RGS19 fusion protein and Gialpha2, Gbeta1gamma2 assessed as gamma[32P]GTP binding by liquid scintillation countingAgonist activity at human H4 receptor expressed in insect Sf9 cells co-expressing RGS19 fusion protein and Gialpha2, Gbeta1gamma2 assessed as gamma[32P]GTP binding by liquid scintillation counting
ChEMBL 223 5 3 2 0.2 CCC(=O)/N=C(\N)NCCCc1c[nH]cn1 10.1021/jm9000693
CHEMBL475621 180872 None 0 Human Binding pEC50 = 8.5 8.5 - 1
Agonist activity at human H4 receptor expressed in insect Sf9 cells co-expressing RGS19 fusion protein and Gialpha2, Gbeta1gamma2 assessed as gamma[32P]GTP binding by liquid scintillation countingAgonist activity at human H4 receptor expressed in insect Sf9 cells co-expressing RGS19 fusion protein and Gialpha2, Gbeta1gamma2 assessed as gamma[32P]GTP binding by liquid scintillation counting
ChEMBL 223 5 3 2 0.2 CCC(=O)/N=C(\N)NCCCc1c[nH]cn1 10.1021/jm9000693
42625304 179206 None 0 Human Binding pEC50 = 8.4 8.4 - 1
Agonist activity at human H4 receptor expressed in insect Sf9 cells co-expressing RGS19 fusion protein and Gialpha2, Gbeta1gamma2 assessed as gamma[32P]GTP binding by liquid scintillation countingAgonist activity at human H4 receptor expressed in insect Sf9 cells co-expressing RGS19 fusion protein and Gialpha2, Gbeta1gamma2 assessed as gamma[32P]GTP binding by liquid scintillation counting
ChEMBL 237 5 3 2 0.4 CC(C)C(=O)/N=C(\N)NCCCc1c[nH]cn1 10.1021/jm9000693
CHEMBL471724 179206 None 0 Human Binding pEC50 = 8.4 8.4 - 1
Agonist activity at human H4 receptor expressed in insect Sf9 cells co-expressing RGS19 fusion protein and Gialpha2, Gbeta1gamma2 assessed as gamma[32P]GTP binding by liquid scintillation countingAgonist activity at human H4 receptor expressed in insect Sf9 cells co-expressing RGS19 fusion protein and Gialpha2, Gbeta1gamma2 assessed as gamma[32P]GTP binding by liquid scintillation counting
ChEMBL 237 5 3 2 0.4 CC(C)C(=O)/N=C(\N)NCCCc1c[nH]cn1 10.1021/jm9000693
11286909 207742 None 0 Human Binding pEC50 = 5.5 5.5 -1 2
Inhibition of the cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H4 receptorInhibition of the cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H4 receptor
ChEMBL 187 4 1 2 2.0 c1ccc(CCCc2c[nH]cn2)nc1 10.1021/jm049932u
CHEMBL79126 207742 None 0 Human Binding pEC50 = 5.5 5.5 -1 2
Inhibition of the cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H4 receptorInhibition of the cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H4 receptor
ChEMBL 187 4 1 2 2.0 c1ccc(CCCc2c[nH]cn2)nc1 10.1021/jm049932u
9964223 208145 None 6 Human Binding pEC50 = 4.5 4.5 -36 2
Inhibition of the cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H4 receptorInhibition of the cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H4 receptor
ChEMBL 173 3 1 2 1.6 c1cncc(CCc2c[nH]cn2)c1 10.1021/jm049932u
CHEMBL82244 208145 None 6 Human Binding pEC50 = 4.5 4.5 -36 2
Inhibition of the cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H4 receptorInhibition of the cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H4 receptor
ChEMBL 173 3 1 2 1.6 c1cncc(CCc2c[nH]cn2)c1 10.1021/jm049932u
42626111 189803 None 0 Human Binding pEC50 = 7.5 7.5 - 0
Agonist activity at human H4 receptor expressed in insect Sf9 cells co-expressing RGS19 fusion protein and Gialpha2, Gbeta1gamma2 assessed as gamma[32P]GTP binding by liquid scintillation countingAgonist activity at human H4 receptor expressed in insect Sf9 cells co-expressing RGS19 fusion protein and Gialpha2, Gbeta1gamma2 assessed as gamma[32P]GTP binding by liquid scintillation counting
ChEMBL 381 8 5 3 1.1 N/C(=N\C(=O)CCNC(=O)c1cc2ccccc2[nH]1)NCCCc1c[nH]cn1 10.1021/jm9000693
CHEMBL515428 189803 None 0 Human Binding pEC50 = 7.5 7.5 - 0
Agonist activity at human H4 receptor expressed in insect Sf9 cells co-expressing RGS19 fusion protein and Gialpha2, Gbeta1gamma2 assessed as gamma[32P]GTP binding by liquid scintillation countingAgonist activity at human H4 receptor expressed in insect Sf9 cells co-expressing RGS19 fusion protein and Gialpha2, Gbeta1gamma2 assessed as gamma[32P]GTP binding by liquid scintillation counting
ChEMBL 381 8 5 3 1.1 N/C(=N\C(=O)CCNC(=O)c1cc2ccccc2[nH]1)NCCCc1c[nH]cn1 10.1021/jm9000693
1204 1932 None 74 Human Binding pEC50 = 7.5 7.5 -3 24
Agonist activity at human H4R expressed in HEK293 cells co-expressing ELucC/ELucN-beta-arrestin2 assessed as induction of beta-arrestin recruitment by luciferase reporter gene assayAgonist activity at human H4R expressed in HEK293 cells co-expressing ELucC/ELucN-beta-arrestin2 assessed as induction of beta-arrestin recruitment by luciferase reporter gene assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.0c00160
1247 1932 None 74 Human Binding pEC50 = 7.5 7.5 -3 24
Agonist activity at human H4R expressed in HEK293 cells co-expressing ELucC/ELucN-beta-arrestin2 assessed as induction of beta-arrestin recruitment by luciferase reporter gene assayAgonist activity at human H4R expressed in HEK293 cells co-expressing ELucC/ELucN-beta-arrestin2 assessed as induction of beta-arrestin recruitment by luciferase reporter gene assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.0c00160
1375 1932 None 74 Human Binding pEC50 = 7.5 7.5 -3 24
Agonist activity at human H4R expressed in HEK293 cells co-expressing ELucC/ELucN-beta-arrestin2 assessed as induction of beta-arrestin recruitment by luciferase reporter gene assayAgonist activity at human H4R expressed in HEK293 cells co-expressing ELucC/ELucN-beta-arrestin2 assessed as induction of beta-arrestin recruitment by luciferase reporter gene assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.0c00160
774 1932 None 74 Human Binding pEC50 = 7.5 7.5 -3 24
Agonist activity at human H4R expressed in HEK293 cells co-expressing ELucC/ELucN-beta-arrestin2 assessed as induction of beta-arrestin recruitment by luciferase reporter gene assayAgonist activity at human H4R expressed in HEK293 cells co-expressing ELucC/ELucN-beta-arrestin2 assessed as induction of beta-arrestin recruitment by luciferase reporter gene assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.0c00160
774.0 1932 None 74 Human Binding pEC50 = 7.5 7.5 -3 24
Agonist activity at human H4R expressed in HEK293 cells co-expressing ELucC/ELucN-beta-arrestin2 assessed as induction of beta-arrestin recruitment by luciferase reporter gene assayAgonist activity at human H4R expressed in HEK293 cells co-expressing ELucC/ELucN-beta-arrestin2 assessed as induction of beta-arrestin recruitment by luciferase reporter gene assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.0c00160
CHEMBL90 1932 None 74 Human Binding pEC50 = 7.5 7.5 -3 24
Agonist activity at human H4R expressed in HEK293 cells co-expressing ELucC/ELucN-beta-arrestin2 assessed as induction of beta-arrestin recruitment by luciferase reporter gene assayAgonist activity at human H4R expressed in HEK293 cells co-expressing ELucC/ELucN-beta-arrestin2 assessed as induction of beta-arrestin recruitment by luciferase reporter gene assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.0c00160
DB05381 1932 None 74 Human Binding pEC50 = 7.5 7.5 -3 24
Agonist activity at human H4R expressed in HEK293 cells co-expressing ELucC/ELucN-beta-arrestin2 assessed as induction of beta-arrestin recruitment by luciferase reporter gene assayAgonist activity at human H4R expressed in HEK293 cells co-expressing ELucC/ELucN-beta-arrestin2 assessed as induction of beta-arrestin recruitment by luciferase reporter gene assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.0c00160
1204 1932 None 74 Human Binding pEC50 = 7.5 7.5 -3 24
Agonist activity at human H4R expressed in HEK293T-beta-arr2-hH4R cells by beta-arrestin2 recruitment assayAgonist activity at human H4R expressed in HEK293T-beta-arr2-hH4R cells by beta-arrestin2 recruitment assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.9b01342
1247 1932 None 74 Human Binding pEC50 = 7.5 7.5 -3 24
Agonist activity at human H4R expressed in HEK293T-beta-arr2-hH4R cells by beta-arrestin2 recruitment assayAgonist activity at human H4R expressed in HEK293T-beta-arr2-hH4R cells by beta-arrestin2 recruitment assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.9b01342
1375 1932 None 74 Human Binding pEC50 = 7.5 7.5 -3 24
Agonist activity at human H4R expressed in HEK293T-beta-arr2-hH4R cells by beta-arrestin2 recruitment assayAgonist activity at human H4R expressed in HEK293T-beta-arr2-hH4R cells by beta-arrestin2 recruitment assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.9b01342
774 1932 None 74 Human Binding pEC50 = 7.5 7.5 -3 24
Agonist activity at human H4R expressed in HEK293T-beta-arr2-hH4R cells by beta-arrestin2 recruitment assayAgonist activity at human H4R expressed in HEK293T-beta-arr2-hH4R cells by beta-arrestin2 recruitment assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.9b01342
774.0 1932 None 74 Human Binding pEC50 = 7.5 7.5 -3 24
Agonist activity at human H4R expressed in HEK293T-beta-arr2-hH4R cells by beta-arrestin2 recruitment assayAgonist activity at human H4R expressed in HEK293T-beta-arr2-hH4R cells by beta-arrestin2 recruitment assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.9b01342
CHEMBL90 1932 None 74 Human Binding pEC50 = 7.5 7.5 -3 24
Agonist activity at human H4R expressed in HEK293T-beta-arr2-hH4R cells by beta-arrestin2 recruitment assayAgonist activity at human H4R expressed in HEK293T-beta-arr2-hH4R cells by beta-arrestin2 recruitment assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.9b01342
DB05381 1932 None 74 Human Binding pEC50 = 7.5 7.5 -3 24
Agonist activity at human H4R expressed in HEK293T-beta-arr2-hH4R cells by beta-arrestin2 recruitment assayAgonist activity at human H4R expressed in HEK293T-beta-arr2-hH4R cells by beta-arrestin2 recruitment assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.9b01342
58227373 176613 None 0 Rat Binding pEC50 = 7.5 7.5 - 2
Agonist activity at rat H4R expressed in HEK293T-beta-arr2-rH4R cells by beta-arrestin2 recruitment assayAgonist activity at rat H4R expressed in HEK293T-beta-arr2-rH4R cells by beta-arrestin2 recruitment assay
ChEMBL 249 3 2 5 1.5 CC(C)(C)CNc1nccc(N2CC[C@@H](N)C2)n1 10.1021/acs.jmedchem.9b01342
CHEMBL4455324 176613 None 0 Rat Binding pEC50 = 7.5 7.5 - 2
Agonist activity at rat H4R expressed in HEK293T-beta-arr2-rH4R cells by beta-arrestin2 recruitment assayAgonist activity at rat H4R expressed in HEK293T-beta-arr2-rH4R cells by beta-arrestin2 recruitment assay
ChEMBL 249 3 2 5 1.5 CC(C)(C)CNc1nccc(N2CC[C@@H](N)C2)n1 10.1021/acs.jmedchem.9b01342
CHEMBL4596881 176613 None 0 Rat Binding pEC50 = 7.5 7.5 - 2
Agonist activity at rat H4R expressed in HEK293T-beta-arr2-rH4R cells by beta-arrestin2 recruitment assayAgonist activity at rat H4R expressed in HEK293T-beta-arr2-rH4R cells by beta-arrestin2 recruitment assay
ChEMBL 249 3 2 5 1.5 CC(C)(C)CNc1nccc(N2CC[C@@H](N)C2)n1 10.1021/acs.jmedchem.9b01342
155552061 176583 None 0 Rat Binding pEC50 = 6.5 6.5 - 2
Agonist activity at rat H4R expressed in HEK293T-beta-arr2-rH4R cells by beta-arrestin2 recruitment assayAgonist activity at rat H4R expressed in HEK293T-beta-arr2-rH4R cells by beta-arrestin2 recruitment assay
ChEMBL 277 3 1 5 2.1 CN1CCCN(c2ccnc(NCC(C)(C)C)n2)CC1 10.1021/acs.jmedchem.9b01342
CHEMBL4543119 176583 None 0 Rat Binding pEC50 = 6.5 6.5 - 2
Agonist activity at rat H4R expressed in HEK293T-beta-arr2-rH4R cells by beta-arrestin2 recruitment assayAgonist activity at rat H4R expressed in HEK293T-beta-arr2-rH4R cells by beta-arrestin2 recruitment assay
ChEMBL 277 3 1 5 2.1 CN1CCCN(c2ccnc(NCC(C)(C)C)n2)CC1 10.1021/acs.jmedchem.9b01342
CHEMBL4596606 176583 None 0 Rat Binding pEC50 = 6.5 6.5 - 2
Agonist activity at rat H4R expressed in HEK293T-beta-arr2-rH4R cells by beta-arrestin2 recruitment assayAgonist activity at rat H4R expressed in HEK293T-beta-arr2-rH4R cells by beta-arrestin2 recruitment assay
ChEMBL 277 3 1 5 2.1 CN1CCCN(c2ccnc(NCC(C)(C)C)n2)CC1 10.1021/acs.jmedchem.9b01342
58227163 176568 None 0 Mouse Binding pEC50 = 6.5 6.5 - 2
Agonist activity at mouse H4R expressed in HEK293T-beta-arr2-mH4R cells by beta-arrestin2 recruitment assayAgonist activity at mouse H4R expressed in HEK293T-beta-arr2-mH4R cells by beta-arrestin2 recruitment assay
ChEMBL 263 3 2 5 1.7 CC(C)(C)CNc1nccc(N2CCCNCC2)n1 10.1021/acs.jmedchem.9b01342
CHEMBL4518374 176568 None 0 Mouse Binding pEC50 = 6.5 6.5 - 2
Agonist activity at mouse H4R expressed in HEK293T-beta-arr2-mH4R cells by beta-arrestin2 recruitment assayAgonist activity at mouse H4R expressed in HEK293T-beta-arr2-mH4R cells by beta-arrestin2 recruitment assay
ChEMBL 263 3 2 5 1.7 CC(C)(C)CNc1nccc(N2CCCNCC2)n1 10.1021/acs.jmedchem.9b01342
CHEMBL4596491 176568 None 0 Mouse Binding pEC50 = 6.5 6.5 - 2
Agonist activity at mouse H4R expressed in HEK293T-beta-arr2-mH4R cells by beta-arrestin2 recruitment assayAgonist activity at mouse H4R expressed in HEK293T-beta-arr2-mH4R cells by beta-arrestin2 recruitment assay
ChEMBL 263 3 2 5 1.7 CC(C)(C)CNc1nccc(N2CCCNCC2)n1 10.1021/acs.jmedchem.9b01342
127050776 140334 None 0 Mouse Binding pEC50 = 5.4 5.4 - 2
Agonist activity at mouse SF-His6-tagged histamine H4 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated response incubated for 5 hrs by luciferase reporter gene assayAgonist activity at mouse SF-His6-tagged histamine H4 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated response incubated for 5 hrs by luciferase reporter gene assay
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 140334 None 0 Mouse Binding pEC50 = 5.4 5.4 - 2
Agonist activity at mouse SF-His6-tagged histamine H4 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated response incubated for 5 hrs by luciferase reporter gene assayAgonist activity at mouse SF-His6-tagged histamine H4 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated response incubated for 5 hrs by luciferase reporter gene assay
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
1204 1932 None 74 Rat Binding pEC50 = 5.4 5.4 -12 24
Agonist activity at rat H4R expressed in HEK293T-beta-arr2-rH4R cells by beta-arrestin2 recruitment assayAgonist activity at rat H4R expressed in HEK293T-beta-arr2-rH4R cells by beta-arrestin2 recruitment assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.9b01342
1247 1932 None 74 Rat Binding pEC50 = 5.4 5.4 -12 24
Agonist activity at rat H4R expressed in HEK293T-beta-arr2-rH4R cells by beta-arrestin2 recruitment assayAgonist activity at rat H4R expressed in HEK293T-beta-arr2-rH4R cells by beta-arrestin2 recruitment assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.9b01342
1375 1932 None 74 Rat Binding pEC50 = 5.4 5.4 -12 24
Agonist activity at rat H4R expressed in HEK293T-beta-arr2-rH4R cells by beta-arrestin2 recruitment assayAgonist activity at rat H4R expressed in HEK293T-beta-arr2-rH4R cells by beta-arrestin2 recruitment assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.9b01342
774 1932 None 74 Rat Binding pEC50 = 5.4 5.4 -12 24
Agonist activity at rat H4R expressed in HEK293T-beta-arr2-rH4R cells by beta-arrestin2 recruitment assayAgonist activity at rat H4R expressed in HEK293T-beta-arr2-rH4R cells by beta-arrestin2 recruitment assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.9b01342
774.0 1932 None 74 Rat Binding pEC50 = 5.4 5.4 -12 24
Agonist activity at rat H4R expressed in HEK293T-beta-arr2-rH4R cells by beta-arrestin2 recruitment assayAgonist activity at rat H4R expressed in HEK293T-beta-arr2-rH4R cells by beta-arrestin2 recruitment assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.9b01342
CHEMBL90 1932 None 74 Rat Binding pEC50 = 5.4 5.4 -12 24
Agonist activity at rat H4R expressed in HEK293T-beta-arr2-rH4R cells by beta-arrestin2 recruitment assayAgonist activity at rat H4R expressed in HEK293T-beta-arr2-rH4R cells by beta-arrestin2 recruitment assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.9b01342
DB05381 1932 None 74 Rat Binding pEC50 = 5.4 5.4 -12 24
Agonist activity at rat H4R expressed in HEK293T-beta-arr2-rH4R cells by beta-arrestin2 recruitment assayAgonist activity at rat H4R expressed in HEK293T-beta-arr2-rH4R cells by beta-arrestin2 recruitment assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.9b01342
45269820 197805 None 0 Human Binding pEC50 = 7.4 7.4 -1 2
Agonist activity at histamine H4 receptor (unknown origin) expressed in human U2OS cells increase in beta-arrestin2 recruitment after 2 hrs by luminescence assayAgonist activity at histamine H4 receptor (unknown origin) expressed in human U2OS cells increase in beta-arrestin2 recruitment after 2 hrs by luminescence assay
ChEMBL 308 6 3 3 3.5 N=C(NCc1cccc(Cl)c1)SCCCc1c[nH]cn1 10.1021/acs.jmedchem.8b00435
CHEMBL1202326 197805 None 0 Human Binding pEC50 = 7.4 7.4 -1 2
Agonist activity at histamine H4 receptor (unknown origin) expressed in human U2OS cells increase in beta-arrestin2 recruitment after 2 hrs by luminescence assayAgonist activity at histamine H4 receptor (unknown origin) expressed in human U2OS cells increase in beta-arrestin2 recruitment after 2 hrs by luminescence assay
ChEMBL 308 6 3 3 3.5 N=C(NCc1cccc(Cl)c1)SCCCc1c[nH]cn1 10.1021/acs.jmedchem.8b00435
CHEMBL551790 197805 None 0 Human Binding pEC50 = 7.4 7.4 -1 2
Agonist activity at histamine H4 receptor (unknown origin) expressed in human U2OS cells increase in beta-arrestin2 recruitment after 2 hrs by luminescence assayAgonist activity at histamine H4 receptor (unknown origin) expressed in human U2OS cells increase in beta-arrestin2 recruitment after 2 hrs by luminescence assay
ChEMBL 308 6 3 3 3.5 N=C(NCc1cccc(Cl)c1)SCCCc1c[nH]cn1 10.1021/acs.jmedchem.8b00435
155512725 176346 None 0 Human Binding pEC50 = 7.4 7.4 154 2
Agonist activity at human H4R expressed in HEK293T-beta-arr2-hH4R cells by beta-arrestin2 recruitment assayAgonist activity at human H4R expressed in HEK293T-beta-arr2-hH4R cells by beta-arrestin2 recruitment assay
ChEMBL 237 6 3 5 1.7 CC(C)(C)CNc1nccc(NCCCN)n1 10.1021/acs.jmedchem.9b01342
CHEMBL4437371 176346 None 0 Human Binding pEC50 = 7.4 7.4 154 2
Agonist activity at human H4R expressed in HEK293T-beta-arr2-hH4R cells by beta-arrestin2 recruitment assayAgonist activity at human H4R expressed in HEK293T-beta-arr2-hH4R cells by beta-arrestin2 recruitment assay
ChEMBL 237 6 3 5 1.7 CC(C)(C)CNc1nccc(NCCCN)n1 10.1021/acs.jmedchem.9b01342
CHEMBL4594753 176346 None 0 Human Binding pEC50 = 7.4 7.4 154 2
Agonist activity at human H4R expressed in HEK293T-beta-arr2-hH4R cells by beta-arrestin2 recruitment assayAgonist activity at human H4R expressed in HEK293T-beta-arr2-hH4R cells by beta-arrestin2 recruitment assay
ChEMBL 237 6 3 5 1.7 CC(C)(C)CNc1nccc(NCCCN)n1 10.1021/acs.jmedchem.9b01342
16078981 44087 None 7 Human Binding pEC50 = 5.4 5.4 - 1
Inhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H4 receptorInhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H4 receptor
ChEMBL 165 2 2 2 1.0 c1nc(CC2CCCNC2)c[nH]1 10.1021/jm030905y
CHEMBL151467 44087 None 7 Human Binding pEC50 = 5.4 5.4 - 1
Inhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H4 receptorInhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H4 receptor
ChEMBL 165 2 2 2 1.0 c1nc(CC2CCCNC2)c[nH]1 10.1021/jm030905y
155524115 176652 None 0 Human Binding pEC50 = 8.4 8.4 -2 3
Agonist activity at human H4R expressed in HEK293T-beta-arr2-hH4R cells by beta-arrestin2 recruitment assayAgonist activity at human H4R expressed in HEK293T-beta-arr2-hH4R cells by beta-arrestin2 recruitment assay
ChEMBL 286 3 2 5 2.2 CC(C)(C)CNc1nccc(N2CCc3nc[nH]c3C2)n1 10.1021/acs.jmedchem.9b01342
CHEMBL4454158 176652 None 0 Human Binding pEC50 = 8.4 8.4 -2 3
Agonist activity at human H4R expressed in HEK293T-beta-arr2-hH4R cells by beta-arrestin2 recruitment assayAgonist activity at human H4R expressed in HEK293T-beta-arr2-hH4R cells by beta-arrestin2 recruitment assay
ChEMBL 286 3 2 5 2.2 CC(C)(C)CNc1nccc(N2CCc3nc[nH]c3C2)n1 10.1021/acs.jmedchem.9b01342
CHEMBL4597218 176652 None 0 Human Binding pEC50 = 8.4 8.4 -2 3
Agonist activity at human H4R expressed in HEK293T-beta-arr2-hH4R cells by beta-arrestin2 recruitment assayAgonist activity at human H4R expressed in HEK293T-beta-arr2-hH4R cells by beta-arrestin2 recruitment assay
ChEMBL 286 3 2 5 2.2 CC(C)(C)CNc1nccc(N2CCc3nc[nH]c3C2)n1 10.1021/acs.jmedchem.9b01342
46887043 8765 None 0 Human Binding pEC50 = 8.3 8.3 - 0
Activity at human recombinant GAIP-fused histamine H4 receptor expressed in Sf9 cells coexpressing Galphai, Gbeta1gamma2 by steady-state GTPase activity assayActivity at human recombinant GAIP-fused histamine H4 receptor expressed in Sf9 cells coexpressing Galphai, Gbeta1gamma2 by steady-state GTPase activity assay
ChEMBL 319 7 4 3 2.6 C[C@@H](CC(=O)NC(=N)NCCCc1c[nH]cn1)C1CCCCC1 10.1016/j.bmcl.2010.03.082
CHEMBL1096431 8765 None 0 Human Binding pEC50 = 8.3 8.3 - 0
Activity at human recombinant GAIP-fused histamine H4 receptor expressed in Sf9 cells coexpressing Galphai, Gbeta1gamma2 by steady-state GTPase activity assayActivity at human recombinant GAIP-fused histamine H4 receptor expressed in Sf9 cells coexpressing Galphai, Gbeta1gamma2 by steady-state GTPase activity assay
ChEMBL 319 7 4 3 2.6 C[C@@H](CC(=O)NC(=N)NCCCc1c[nH]cn1)C1CCCCC1 10.1016/j.bmcl.2010.03.082
42625384 169876 None 0 Human Binding pEC50 = 8.3 8.3 - 1
Agonist activity at human H4 receptor expressed in insect Sf9 cells co-expressing RGS19 fusion protein and Gialpha2, Gbeta1gamma2 assessed as gamma[32P]GTP binding by liquid scintillation countingAgonist activity at human H4 receptor expressed in insect Sf9 cells co-expressing RGS19 fusion protein and Gialpha2, Gbeta1gamma2 assessed as gamma[32P]GTP binding by liquid scintillation counting
ChEMBL 209 4 3 2 -0.2 CC(=O)/N=C(\N)NCCCc1c[nH]cn1 10.1021/jm9000693
CHEMBL443896 169876 None 0 Human Binding pEC50 = 8.3 8.3 - 1
Agonist activity at human H4 receptor expressed in insect Sf9 cells co-expressing RGS19 fusion protein and Gialpha2, Gbeta1gamma2 assessed as gamma[32P]GTP binding by liquid scintillation countingAgonist activity at human H4 receptor expressed in insect Sf9 cells co-expressing RGS19 fusion protein and Gialpha2, Gbeta1gamma2 assessed as gamma[32P]GTP binding by liquid scintillation counting
ChEMBL 209 4 3 2 -0.2 CC(=O)/N=C(\N)NCCCc1c[nH]cn1 10.1021/jm9000693
44367567 169304 None 2 Human Binding pEC50 = 6.4 6.4 - 1
Inhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H4 receptorInhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H4 receptor
ChEMBL 151 2 2 2 0.6 c1nc(C[C@H]2CCNC2)c[nH]1 10.1021/jm030905y
CHEMBL440730 169304 None 2 Human Binding pEC50 = 6.4 6.4 - 1
Inhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H4 receptorInhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H4 receptor
ChEMBL 151 2 2 2 0.6 c1nc(C[C@H]2CCNC2)c[nH]1 10.1021/jm030905y
58227163 176568 None 0 Human Binding pEC50 = 7.4 7.4 40 2
Agonist activity at human H4R expressed in HEK293T-beta-arr2-hH4R cells by beta-arrestin2 recruitment assayAgonist activity at human H4R expressed in HEK293T-beta-arr2-hH4R cells by beta-arrestin2 recruitment assay
ChEMBL 263 3 2 5 1.7 CC(C)(C)CNc1nccc(N2CCCNCC2)n1 10.1021/acs.jmedchem.9b01342
CHEMBL4518374 176568 None 0 Human Binding pEC50 = 7.4 7.4 40 2
Agonist activity at human H4R expressed in HEK293T-beta-arr2-hH4R cells by beta-arrestin2 recruitment assayAgonist activity at human H4R expressed in HEK293T-beta-arr2-hH4R cells by beta-arrestin2 recruitment assay
ChEMBL 263 3 2 5 1.7 CC(C)(C)CNc1nccc(N2CCCNCC2)n1 10.1021/acs.jmedchem.9b01342
CHEMBL4596491 176568 None 0 Human Binding pEC50 = 7.4 7.4 40 2
Agonist activity at human H4R expressed in HEK293T-beta-arr2-hH4R cells by beta-arrestin2 recruitment assayAgonist activity at human H4R expressed in HEK293T-beta-arr2-hH4R cells by beta-arrestin2 recruitment assay
ChEMBL 263 3 2 5 1.7 CC(C)(C)CNc1nccc(N2CCCNCC2)n1 10.1021/acs.jmedchem.9b01342
155513612 176425 None 0 Mouse Binding pEC50 = 7.3 7.3 -1 4
Agonist activity at mouse recombinant H4R expressed in HEK293T cells by beta-arrestin recruitment assayAgonist activity at mouse recombinant H4R expressed in HEK293T cells by beta-arrestin recruitment assay
ChEMBL 277 4 1 5 2.1 CN(C)[C@@H]1CCN(c2ccnc(NCC(C)(C)C)n2)C1 10.1021/acs.jmedchem.0c00160
CHEMBL4439142 176425 None 0 Mouse Binding pEC50 = 7.3 7.3 -1 4
Agonist activity at mouse recombinant H4R expressed in HEK293T cells by beta-arrestin recruitment assayAgonist activity at mouse recombinant H4R expressed in HEK293T cells by beta-arrestin recruitment assay
ChEMBL 277 4 1 5 2.1 CN(C)[C@@H]1CCN(c2ccnc(NCC(C)(C)C)n2)C1 10.1021/acs.jmedchem.0c00160
CHEMBL4515149 176425 None 0 Mouse Binding pEC50 = 7.3 7.3 -1 4
Agonist activity at mouse recombinant H4R expressed in HEK293T cells by beta-arrestin recruitment assayAgonist activity at mouse recombinant H4R expressed in HEK293T cells by beta-arrestin recruitment assay
ChEMBL 277 4 1 5 2.1 CN(C)[C@@H]1CCN(c2ccnc(NCC(C)(C)C)n2)C1 10.1021/acs.jmedchem.0c00160
CHEMBL4595327 176425 None 0 Mouse Binding pEC50 = 7.3 7.3 -1 4
Agonist activity at mouse recombinant H4R expressed in HEK293T cells by beta-arrestin recruitment assayAgonist activity at mouse recombinant H4R expressed in HEK293T cells by beta-arrestin recruitment assay
ChEMBL 277 4 1 5 2.1 CN(C)[C@@H]1CCN(c2ccnc(NCC(C)(C)C)n2)C1 10.1021/acs.jmedchem.0c00160
156013896 178345 None 0 Mouse Binding pEC50 = 7.3 7.3 -22 4
Antagonist activity at mouse H4R expressed in HEK293 cells co-expressing ELucC/ELucN-beta-arrestin2 assessed as inhibition of histamine-induced beta-arrestin recruitment preincubated for 15 mins followed by histamine addition by luciferase reporter gene assayAntagonist activity at mouse H4R expressed in HEK293 cells co-expressing ELucC/ELucN-beta-arrestin2 assessed as inhibition of histamine-induced beta-arrestin recruitment preincubated for 15 mins followed by histamine addition by luciferase reporter gene assay
ChEMBL 401 9 1 2 5.1 Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCCCc1c[nH]cn1 10.1021/acs.jmedchem.0c00160
CHEMBL4635634 178345 None 0 Mouse Binding pEC50 = 7.3 7.3 -22 4
Antagonist activity at mouse H4R expressed in HEK293 cells co-expressing ELucC/ELucN-beta-arrestin2 assessed as inhibition of histamine-induced beta-arrestin recruitment preincubated for 15 mins followed by histamine addition by luciferase reporter gene assayAntagonist activity at mouse H4R expressed in HEK293 cells co-expressing ELucC/ELucN-beta-arrestin2 assessed as inhibition of histamine-induced beta-arrestin recruitment preincubated for 15 mins followed by histamine addition by luciferase reporter gene assay
ChEMBL 401 9 1 2 5.1 Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCCCc1c[nH]cn1 10.1021/acs.jmedchem.0c00160
CHEMBL4650570 178345 None 0 Mouse Binding pEC50 = 7.3 7.3 -22 4
Antagonist activity at mouse H4R expressed in HEK293 cells co-expressing ELucC/ELucN-beta-arrestin2 assessed as inhibition of histamine-induced beta-arrestin recruitment preincubated for 15 mins followed by histamine addition by luciferase reporter gene assayAntagonist activity at mouse H4R expressed in HEK293 cells co-expressing ELucC/ELucN-beta-arrestin2 assessed as inhibition of histamine-induced beta-arrestin recruitment preincubated for 15 mins followed by histamine addition by luciferase reporter gene assay
ChEMBL 401 9 1 2 5.1 Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCCCc1c[nH]cn1 10.1021/acs.jmedchem.0c00160
127049855 140315 None 0 Human Binding pEC50 = 6.3 6.3 -1 4
Agonist activity at human SF-His6-tagged histamine H4 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated response incubated for 5 hrs by luciferase reporter gene assayAgonist activity at human SF-His6-tagged histamine H4 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated response incubated for 5 hrs by luciferase reporter gene assay
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
CHEMBL3805220 140315 None 0 Human Binding pEC50 = 6.3 6.3 -1 4
Agonist activity at human SF-His6-tagged histamine H4 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated response incubated for 5 hrs by luciferase reporter gene assayAgonist activity at human SF-His6-tagged histamine H4 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated response incubated for 5 hrs by luciferase reporter gene assay
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
11957573 2010 None 25 Human Binding pEC50 = 7.3 7.3 -38 7
Inhibition of human Histamine H4 receptorInhibition of human Histamine H4 receptor
ChEMBL 170 3 3 3 0.6 NC(=N)SCCc1cnc[nH]1 10.1021/jm020415q
1250 2010 None 25 Human Binding pEC50 = 7.3 7.3 -38 7
Inhibition of human Histamine H4 receptorInhibition of human Histamine H4 receptor
ChEMBL 170 3 3 3 0.6 NC(=N)SCCc1cnc[nH]1 10.1021/jm020415q
3692 2010 None 25 Human Binding pEC50 = 7.3 7.3 -38 7
Inhibition of human Histamine H4 receptorInhibition of human Histamine H4 receptor
ChEMBL 170 3 3 3 0.6 NC(=N)SCCc1cnc[nH]1 10.1021/jm020415q
CHEMBL19439 2010 None 25 Human Binding pEC50 = 7.3 7.3 -38 7
Inhibition of human Histamine H4 receptorInhibition of human Histamine H4 receptor
ChEMBL 170 3 3 3 0.6 NC(=N)SCCc1cnc[nH]1 10.1021/jm020415q
155513612 176425 None 0 Mouse Binding pEC50 = 7.3 7.3 -1 4
Agonist activity at mouse H4R expressed in HEK293T-beta-arr2-mH4R cells by beta-arrestin2 recruitment assayAgonist activity at mouse H4R expressed in HEK293T-beta-arr2-mH4R cells by beta-arrestin2 recruitment assay
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 176425 None 0 Mouse Binding pEC50 = 7.3 7.3 -1 4
Agonist activity at mouse H4R expressed in HEK293T-beta-arr2-mH4R cells by beta-arrestin2 recruitment assayAgonist activity at mouse H4R expressed in HEK293T-beta-arr2-mH4R cells by beta-arrestin2 recruitment assay
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 176425 None 0 Mouse Binding pEC50 = 7.3 7.3 -1 4
Agonist activity at mouse H4R expressed in HEK293T-beta-arr2-mH4R cells by beta-arrestin2 recruitment assayAgonist activity at mouse H4R expressed in HEK293T-beta-arr2-mH4R cells by beta-arrestin2 recruitment assay
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 176425 None 0 Mouse Binding pEC50 = 7.3 7.3 -1 4
Agonist activity at mouse H4R expressed in HEK293T-beta-arr2-mH4R cells by beta-arrestin2 recruitment assayAgonist activity at mouse H4R expressed in HEK293T-beta-arr2-mH4R cells by beta-arrestin2 recruitment assay
ChEMBL 277 4 1 5 2.1 CN(C)[C@@H]1CCN(c2ccnc(NCC(C)(C)C)n2)C1 10.1021/acs.jmedchem.9b01342
127051301 140287 None 0 Mouse Binding pEC50 = 6.3 6.3 - 2
Agonist activity at mouse SF-His6-tagged histamine H4 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated response incubated for 5 hrs by luciferase reporter gene assayAgonist activity at mouse SF-His6-tagged histamine H4 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated response incubated for 5 hrs by luciferase reporter gene assay
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 140287 None 0 Mouse Binding pEC50 = 6.3 6.3 - 2
Agonist activity at mouse SF-His6-tagged histamine H4 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated response incubated for 5 hrs by luciferase reporter gene assayAgonist activity at mouse SF-His6-tagged histamine H4 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated response incubated for 5 hrs by luciferase reporter gene assay
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
1204 1932 None 74 Human Binding pEC50 = 7.3 7.3 -3 24
Inhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H4 receptorInhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H4 receptor
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm030905y
1247 1932 None 74 Human Binding pEC50 = 7.3 7.3 -3 24
Inhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H4 receptorInhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H4 receptor
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm030905y
1375 1932 None 74 Human Binding pEC50 = 7.3 7.3 -3 24
Inhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H4 receptorInhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H4 receptor
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm030905y
774 1932 None 74 Human Binding pEC50 = 7.3 7.3 -3 24
Inhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H4 receptorInhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H4 receptor
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm030905y
774.0 1932 None 74 Human Binding pEC50 = 7.3 7.3 -3 24
Inhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H4 receptorInhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H4 receptor
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm030905y
CHEMBL90 1932 None 74 Human Binding pEC50 = 7.3 7.3 -3 24
Inhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H4 receptorInhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H4 receptor
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm030905y
DB05381 1932 None 74 Human Binding pEC50 = 7.3 7.3 -3 24
Inhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H4 receptorInhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H4 receptor
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm030905y
46235428 6606 None 0 Mouse Binding pEC50 = 6.3 6.3 - 1
Displacement of [3H]histamine from mouse recombinant histamine H4 receptorDisplacement of [3H]histamine from mouse recombinant histamine H4 receptor
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 6606 None 0 Mouse Binding pEC50 = 6.3 6.3 - 1
Displacement of [3H]histamine from mouse recombinant histamine H4 receptorDisplacement of [3H]histamine from mouse recombinant histamine H4 receptor
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
1251 2014 None 28 Human Binding pEC50 = 7.3 7.3 -100 5
Inhibition of the cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H4 receptorInhibition of the cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H4 receptor
ChEMBL 165 2 2 2 1.0 N1CCC(CC1)Cc1[nH]cnc1 10.1021/jm049932u
3035842 2014 None 28 Human Binding pEC50 = 7.3 7.3 -100 5
Inhibition of the cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H4 receptorInhibition of the cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H4 receptor
ChEMBL 165 2 2 2 1.0 N1CCC(CC1)Cc1[nH]cnc1 10.1021/jm049932u
CHEMBL18661 2014 None 28 Human Binding pEC50 = 7.3 7.3 -100 5
Inhibition of the cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H4 receptorInhibition of the cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H4 receptor
ChEMBL 165 2 2 2 1.0 N1CCC(CC1)Cc1[nH]cnc1 10.1021/jm049932u
1251 2014 None 28 Human Binding pEC50 = 7.3 7.3 -100 5
Inhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H4 receptorInhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H4 receptor
ChEMBL 165 2 2 2 1.0 N1CCC(CC1)Cc1[nH]cnc1 10.1021/jm030905y
3035842 2014 None 28 Human Binding pEC50 = 7.3 7.3 -100 5
Inhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H4 receptorInhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H4 receptor
ChEMBL 165 2 2 2 1.0 N1CCC(CC1)Cc1[nH]cnc1 10.1021/jm030905y
CHEMBL18661 2014 None 28 Human Binding pEC50 = 7.3 7.3 -100 5
Inhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H4 receptorInhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H4 receptor
ChEMBL 165 2 2 2 1.0 N1CCC(CC1)Cc1[nH]cnc1 10.1021/jm030905y
11206058 104471 None 4 Human Binding pEC50 = 4.2 4.2 -10 2
Inhibition of the cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H4 receptorInhibition of the cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H4 receptor
ChEMBL 173 3 1 2 1.6 c1ccc(CCc2c[nH]cn2)nc1 10.1021/jm049932u
CHEMBL310360 104471 None 4 Human Binding pEC50 = 4.2 4.2 -10 2
Inhibition of the cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H4 receptorInhibition of the cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H4 receptor
ChEMBL 173 3 1 2 1.6 c1ccc(CCc2c[nH]cn2)nc1 10.1021/jm049932u
127049855 140315 None 0 Mouse Binding pEC50 = 6.2 6.2 - 4
Agonist activity at mouse SF-His6-tagged histamine H4 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated response incubated for 5 hrs by luciferase reporter gene assayAgonist activity at mouse SF-His6-tagged histamine H4 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated response incubated for 5 hrs by luciferase reporter gene assay
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
CHEMBL3805220 140315 None 0 Mouse Binding pEC50 = 6.2 6.2 - 4
Agonist activity at mouse SF-His6-tagged histamine H4 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated response incubated for 5 hrs by luciferase reporter gene assayAgonist activity at mouse SF-His6-tagged histamine H4 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated response incubated for 5 hrs by luciferase reporter gene assay
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
25149708 188543 None 0 Human Binding pEC50 = 8.2 8.2 - 0
Activity at human recombinant histamine H4 receptor-RGS4 fusion protein expressed in Sf9 cells coexpressing Galphai2 and G-beta-1-gamma-2 by steady-state GTPase activity assayActivity at human recombinant histamine H4 receptor-RGS4 fusion protein expressed in Sf9 cells coexpressing Galphai2 and G-beta-1-gamma-2 by steady-state GTPase activity assay
ChEMBL 319 7 4 4 2.2 CC(CC(=O)NC(=N)NCCCc1c[nH]cn1)c1cccs1 10.1021/jm800841w
CHEMBL502339 188543 None 0 Human Binding pEC50 = 8.2 8.2 - 0
Activity at human recombinant histamine H4 receptor-RGS4 fusion protein expressed in Sf9 cells coexpressing Galphai2 and G-beta-1-gamma-2 by steady-state GTPase activity assayActivity at human recombinant histamine H4 receptor-RGS4 fusion protein expressed in Sf9 cells coexpressing Galphai2 and G-beta-1-gamma-2 by steady-state GTPase activity assay
ChEMBL 319 7 4 4 2.2 CC(CC(=O)NC(=N)NCCCc1c[nH]cn1)c1cccs1 10.1021/jm800841w
58227401 176556 None 0 Human Binding pEC50 = 8.2 8.2 7 2
Agonist activity at human H4R expressed in HEK293T-beta-arr2-hH4R cells by beta-arrestin2 recruitment assayAgonist activity at human H4R expressed in HEK293T-beta-arr2-hH4R cells by beta-arrestin2 recruitment assay
ChEMBL 263 4 2 5 1.7 CN[C@@H]1CCN(c2ccnc(NCC(C)(C)C)n2)C1 10.1021/acs.jmedchem.9b01342
CHEMBL4443126 176556 None 0 Human Binding pEC50 = 8.2 8.2 7 2
Agonist activity at human H4R expressed in HEK293T-beta-arr2-hH4R cells by beta-arrestin2 recruitment assayAgonist activity at human H4R expressed in HEK293T-beta-arr2-hH4R cells by beta-arrestin2 recruitment assay
ChEMBL 263 4 2 5 1.7 CN[C@@H]1CCN(c2ccnc(NCC(C)(C)C)n2)C1 10.1021/acs.jmedchem.9b01342
CHEMBL4596409 176556 None 0 Human Binding pEC50 = 8.2 8.2 7 2
Agonist activity at human H4R expressed in HEK293T-beta-arr2-hH4R cells by beta-arrestin2 recruitment assayAgonist activity at human H4R expressed in HEK293T-beta-arr2-hH4R cells by beta-arrestin2 recruitment assay
ChEMBL 263 4 2 5 1.7 CN[C@@H]1CCN(c2ccnc(NCC(C)(C)C)n2)C1 10.1021/acs.jmedchem.9b01342
46887079 8511 None 0 Human Binding pEC50 = 5.2 5.2 - 0
Activity at human recombinant GAIP-fused histamine H4 receptor expressed in Sf9 cells coexpressing Galphai, Gbeta1gamma2 by steady-state GTPase activity assayActivity at human recombinant GAIP-fused histamine H4 receptor expressed in Sf9 cells coexpressing Galphai, Gbeta1gamma2 by steady-state GTPase activity assay
ChEMBL 365 7 4 5 3.2 Cc1nc(N)sc1CCCNC(=N)NC(=O)CC(C)C1CCCCC1 10.1016/j.bmcl.2010.03.082
CHEMBL1094142 8511 None 0 Human Binding pEC50 = 5.2 5.2 - 0
Activity at human recombinant GAIP-fused histamine H4 receptor expressed in Sf9 cells coexpressing Galphai, Gbeta1gamma2 by steady-state GTPase activity assayActivity at human recombinant GAIP-fused histamine H4 receptor expressed in Sf9 cells coexpressing Galphai, Gbeta1gamma2 by steady-state GTPase activity assay
ChEMBL 365 7 4 5 3.2 Cc1nc(N)sc1CCCNC(=N)NC(=O)CC(C)C1CCCCC1 10.1016/j.bmcl.2010.03.082
127051301 140287 None 0 Human Binding pEC50 = 7.2 7.2 5 2
Agonist activity at human SF-His6-tagged histamine H4 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated response incubated for 5 hrs by luciferase reporter gene assayAgonist activity at human SF-His6-tagged histamine H4 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated response incubated for 5 hrs by luciferase reporter gene assay
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 140287 None 0 Human Binding pEC50 = 7.2 7.2 5 2
Agonist activity at human SF-His6-tagged histamine H4 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated response incubated for 5 hrs by luciferase reporter gene assayAgonist activity at human SF-His6-tagged histamine H4 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated response incubated for 5 hrs by luciferase reporter gene assay
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
25130914 187360 None 0 Human Binding pEC50 = 7.2 7.2 - 1
Agonist activity at histamine H4 receptor (unknown origin) expressed in human U2OS cells increase in beta-arrestin2 recruitment after 2 hrs by luminescence assayAgonist activity at histamine H4 receptor (unknown origin) expressed in human U2OS cells increase in beta-arrestin2 recruitment after 2 hrs by luminescence assay
ChEMBL 298 4 2 6 1.4 CN1CCN(c2cc(NCc3ccccc3)nc(N)n2)CC1 10.1021/acs.jmedchem.8b00435
CHEMBL492677 187360 None 0 Human Binding pEC50 = 7.2 7.2 - 1
Agonist activity at histamine H4 receptor (unknown origin) expressed in human U2OS cells increase in beta-arrestin2 recruitment after 2 hrs by luminescence assayAgonist activity at histamine H4 receptor (unknown origin) expressed in human U2OS cells increase in beta-arrestin2 recruitment after 2 hrs by luminescence assay
ChEMBL 298 4 2 6 1.4 CN1CCN(c2cc(NCc3ccccc3)nc(N)n2)CC1 10.1021/acs.jmedchem.8b00435
156015638 178377 None 0 Human Binding pEC50 = 7.2 7.2 -58 4
Agonist activity at human H4R expressed in HEK293 cells co-expressing ELucC/ELucN-beta-arrestin2 assessed as induction of beta-arrestin recruitment by luciferase reporter gene assayAgonist activity at human H4R expressed in HEK293 cells co-expressing ELucC/ELucN-beta-arrestin2 assessed as induction of beta-arrestin recruitment by luciferase reporter gene assay
ChEMBL 415 10 1 2 5.5 Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCCCCc1c[nH]cn1 10.1021/acs.jmedchem.0c00160
CHEMBL4642520 178377 None 0 Human Binding pEC50 = 7.2 7.2 -58 4
Agonist activity at human H4R expressed in HEK293 cells co-expressing ELucC/ELucN-beta-arrestin2 assessed as induction of beta-arrestin recruitment by luciferase reporter gene assayAgonist activity at human H4R expressed in HEK293 cells co-expressing ELucC/ELucN-beta-arrestin2 assessed as induction of beta-arrestin recruitment by luciferase reporter gene assay
ChEMBL 415 10 1 2 5.5 Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCCCCc1c[nH]cn1 10.1021/acs.jmedchem.0c00160
CHEMBL4650832 178377 None 0 Human Binding pEC50 = 7.2 7.2 -58 4
Agonist activity at human H4R expressed in HEK293 cells co-expressing ELucC/ELucN-beta-arrestin2 assessed as induction of beta-arrestin recruitment by luciferase reporter gene assayAgonist activity at human H4R expressed in HEK293 cells co-expressing ELucC/ELucN-beta-arrestin2 assessed as induction of beta-arrestin recruitment by luciferase reporter gene assay
ChEMBL 415 10 1 2 5.5 Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCCCCc1c[nH]cn1 10.1021/acs.jmedchem.0c00160
58227163 176568 None 0 Rat Binding pEC50 = 6.2 6.2 - 2
Agonist activity at rat H4R expressed in HEK293T-beta-arr2-rH4R cells by beta-arrestin2 recruitment assayAgonist activity at rat H4R expressed in HEK293T-beta-arr2-rH4R cells by beta-arrestin2 recruitment assay
ChEMBL 263 3 2 5 1.7 CC(C)(C)CNc1nccc(N2CCCNCC2)n1 10.1021/acs.jmedchem.9b01342
CHEMBL4518374 176568 None 0 Rat Binding pEC50 = 6.2 6.2 - 2
Agonist activity at rat H4R expressed in HEK293T-beta-arr2-rH4R cells by beta-arrestin2 recruitment assayAgonist activity at rat H4R expressed in HEK293T-beta-arr2-rH4R cells by beta-arrestin2 recruitment assay
ChEMBL 263 3 2 5 1.7 CC(C)(C)CNc1nccc(N2CCCNCC2)n1 10.1021/acs.jmedchem.9b01342
CHEMBL4596491 176568 None 0 Rat Binding pEC50 = 6.2 6.2 - 2
Agonist activity at rat H4R expressed in HEK293T-beta-arr2-rH4R cells by beta-arrestin2 recruitment assayAgonist activity at rat H4R expressed in HEK293T-beta-arr2-rH4R cells by beta-arrestin2 recruitment assay
ChEMBL 263 3 2 5 1.7 CC(C)(C)CNc1nccc(N2CCCNCC2)n1 10.1021/acs.jmedchem.9b01342
25149613 179306 None 0 Human Binding pEC50 = 7.2 7.2 - 1
Activity at human recombinant histamine H4 receptor-RGS4 fusion protein expressed in Sf9 cells coexpressing Galphai2 and G-beta-1-gamma-2 by steady-state GTPase activity assayActivity at human recombinant histamine H4 receptor-RGS4 fusion protein expressed in Sf9 cells coexpressing Galphai2 and G-beta-1-gamma-2 by steady-state GTPase activity assay
ChEMBL 382 8 4 5 2.7 N=C(NCCCc1c[nH]cn1)NC(=O)CC(c1ccccc1)c1nccs1 10.1021/jm800841w
CHEMBL472441 179306 None 0 Human Binding pEC50 = 7.2 7.2 - 1
Activity at human recombinant histamine H4 receptor-RGS4 fusion protein expressed in Sf9 cells coexpressing Galphai2 and G-beta-1-gamma-2 by steady-state GTPase activity assayActivity at human recombinant histamine H4 receptor-RGS4 fusion protein expressed in Sf9 cells coexpressing Galphai2 and G-beta-1-gamma-2 by steady-state GTPase activity assay
ChEMBL 382 8 4 5 2.7 N=C(NCCCc1c[nH]cn1)NC(=O)CC(c1ccccc1)c1nccs1 10.1021/jm800841w
136773074 157457 None 0 Human Binding pEC50 = 5.2 5.2 - 1
Agonist activity at human H4 receptor expressed in CHO cell membranes co-expressing Galphai2 by GTPgamma[35S] binding assayAgonist activity at human H4 receptor expressed in CHO cell membranes co-expressing Galphai2 by GTPgamma[35S] binding assay
ChEMBL 335 6 2 4 3.6 COc1ccc(/C(=N/[C@H](C)Cc2cnc[nH]2)c2ccccc2)c(O)c1 10.1016/j.ejmech.2016.09.074
CHEMBL4077914 157457 None 0 Human Binding pEC50 = 5.2 5.2 - 1
Agonist activity at human H4 receptor expressed in CHO cell membranes co-expressing Galphai2 by GTPgamma[35S] binding assayAgonist activity at human H4 receptor expressed in CHO cell membranes co-expressing Galphai2 by GTPgamma[35S] binding assay
ChEMBL 335 6 2 4 3.6 COc1ccc(/C(=N/[C@H](C)Cc2cnc[nH]2)c2ccccc2)c(O)c1 10.1016/j.ejmech.2016.09.074
42625221 189697 None 0 Human Binding pEC50 = 8.2 8.2 - 1
Agonist activity at human H4 receptor expressed in insect Sf9 cells co-expressing RGS19 fusion protein and Gialpha2, Gbeta1gamma2 assessed as gamma[32P]GTP binding by liquid scintillation countingAgonist activity at human H4 receptor expressed in insect Sf9 cells co-expressing RGS19 fusion protein and Gialpha2, Gbeta1gamma2 assessed as gamma[32P]GTP binding by liquid scintillation counting
ChEMBL 338 7 4 2 1.9 N/C(=N\C(=O)CCc1c[nH]c2ccccc12)NCCCc1c[nH]cn1 10.1021/jm9000693
CHEMBL514641 189697 None 0 Human Binding pEC50 = 8.2 8.2 - 1
Agonist activity at human H4 receptor expressed in insect Sf9 cells co-expressing RGS19 fusion protein and Gialpha2, Gbeta1gamma2 assessed as gamma[32P]GTP binding by liquid scintillation countingAgonist activity at human H4 receptor expressed in insect Sf9 cells co-expressing RGS19 fusion protein and Gialpha2, Gbeta1gamma2 assessed as gamma[32P]GTP binding by liquid scintillation counting
ChEMBL 338 7 4 2 1.9 N/C(=N\C(=O)CCc1c[nH]c2ccccc12)NCCCc1c[nH]cn1 10.1021/jm9000693
24798144 110181 None 0 Mouse Binding pEC50 = 8.1 8.1 -19 3
Partial agonist activity at mouse histamine H4 receptorPartial agonist activity at mouse histamine H4 receptor
ChEMBL 247 2 2 5 1.1 Nc1nc(C2CCCC2)cc(N2CCNCC2)n1 10.1021/jm401727m
CHEMBL3236553 110181 None 0 Mouse Binding pEC50 = 8.1 8.1 -19 3
Partial agonist activity at mouse histamine H4 receptorPartial agonist activity at mouse histamine H4 receptor
ChEMBL 247 2 2 5 1.1 Nc1nc(C2CCCC2)cc(N2CCNCC2)n1 10.1021/jm401727m
10374457 28903 None 2 Human Binding pEC50 = 5.2 5.2 - 2
Inhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H4 receptorInhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H4 receptor
ChEMBL 123 1 2 2 0.2 N[C@H]1C[C@@H]1c1c[nH]cn1 10.1021/jm030905y
CHEMBL13795 28903 None 2 Human Binding pEC50 = 5.2 5.2 - 2
Inhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H4 receptorInhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H4 receptor
ChEMBL 123 1 2 2 0.2 N[C@H]1C[C@@H]1c1c[nH]cn1 10.1021/jm030905y
11819221 45774 None 2 Human Binding pEC50 = 6.1 6.1 - 1
Inhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H4 receptorInhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H4 receptor
ChEMBL 151 2 2 2 0.6 c1nc(CC2CCNC2)c[nH]1 10.1021/jm030905y
CHEMBL153061 45774 None 2 Human Binding pEC50 = 6.1 6.1 - 1
Inhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H4 receptorInhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H4 receptor
ChEMBL 151 2 2 2 0.6 c1nc(CC2CCNC2)c[nH]1 10.1021/jm030905y
1204 1932 None 74 Human Binding pEC50 = 7.1 7.1 -3 24
Inhibition of human Histamine H4 receptorInhibition of human Histamine H4 receptor
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm020415q
1247 1932 None 74 Human Binding pEC50 = 7.1 7.1 -3 24
Inhibition of human Histamine H4 receptorInhibition of human Histamine H4 receptor
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm020415q
1375 1932 None 74 Human Binding pEC50 = 7.1 7.1 -3 24
Inhibition of human Histamine H4 receptorInhibition of human Histamine H4 receptor
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm020415q
774 1932 None 74 Human Binding pEC50 = 7.1 7.1 -3 24
Inhibition of human Histamine H4 receptorInhibition of human Histamine H4 receptor
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm020415q
774.0 1932 None 74 Human Binding pEC50 = 7.1 7.1 -3 24
Inhibition of human Histamine H4 receptorInhibition of human Histamine H4 receptor
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm020415q
CHEMBL90 1932 None 74 Human Binding pEC50 = 7.1 7.1 -3 24
Inhibition of human Histamine H4 receptorInhibition of human Histamine H4 receptor
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm020415q
DB05381 1932 None 74 Human Binding pEC50 = 7.1 7.1 -3 24
Inhibition of human Histamine H4 receptorInhibition of human Histamine H4 receptor
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm020415q
90667229 109526 None 0 Human Binding pEC50 = 6.1 6.1 - 0
Agonist activity at human recombinant histamine H4 receptor-RGS19 fusion protein expressed in Sf9 cells coexpressing Galphai2,Gbeta1gamma2 preincubated for 2 mins before [gamma32P]GTP addition measured after 20 mins by steady-state GTPase activity assayAgonist activity at human recombinant histamine H4 receptor-RGS19 fusion protein expressed in Sf9 cells coexpressing Galphai2,Gbeta1gamma2 preincubated for 2 mins before [gamma32P]GTP addition measured after 20 mins by steady-state GTPase activity assay
ChEMBL 319 7 3 3 2.0 CC(CC(=O)/N=C(\N)NCCCc1ncc[nH]1)c1cccs1 10.1039/C3MD00245D
CHEMBL3220630 109526 None 0 Human Binding pEC50 = 6.1 6.1 - 0
Agonist activity at human recombinant histamine H4 receptor-RGS19 fusion protein expressed in Sf9 cells coexpressing Galphai2,Gbeta1gamma2 preincubated for 2 mins before [gamma32P]GTP addition measured after 20 mins by steady-state GTPase activity assayAgonist activity at human recombinant histamine H4 receptor-RGS19 fusion protein expressed in Sf9 cells coexpressing Galphai2,Gbeta1gamma2 preincubated for 2 mins before [gamma32P]GTP addition measured after 20 mins by steady-state GTPase activity assay
ChEMBL 319 7 3 3 2.0 CC(CC(=O)/N=C(\N)NCCCc1ncc[nH]1)c1cccs1 10.1039/C3MD00245D
11546127 95537 None 1 Human Binding pEC50 = 5.1 5.1 - 1
Agonist activity at human H4 receptor expressed in CHO cell membranes co-expressing Galphai2 by GTPgamma[35S] binding assayAgonist activity at human H4 receptor expressed in CHO cell membranes co-expressing Galphai2 by GTPgamma[35S] binding assay
ChEMBL 414 7 2 5 3.3 COc1ccc2c(c1)c(CC(=O)NCCCO)c(C)n2C(=O)c1ccc(Cl)cc1 10.1016/j.ejmech.2016.09.074
CHEMBL25725 95537 None 1 Human Binding pEC50 = 5.1 5.1 - 1
Agonist activity at human H4 receptor expressed in CHO cell membranes co-expressing Galphai2 by GTPgamma[35S] binding assayAgonist activity at human H4 receptor expressed in CHO cell membranes co-expressing Galphai2 by GTPgamma[35S] binding assay
ChEMBL 414 7 2 5 3.3 COc1ccc2c(c1)c(CC(=O)NCCCO)c(C)n2C(=O)c1ccc(Cl)cc1 10.1016/j.ejmech.2016.09.074
182527 110631 None 3 Human Binding pEC50 = 8.1 8.1 - 0
Agonist activity at human H4 receptor expressed in insect Sf9 cells co-expressing RGS19 fusion protein and Gialpha2, Gbeta1gamma2 assessed as gamma[32P]GTP binding by liquid scintillation countingAgonist activity at human H4 receptor expressed in insect Sf9 cells co-expressing RGS19 fusion protein and Gialpha2, Gbeta1gamma2 assessed as gamma[32P]GTP binding by liquid scintillation counting
ChEMBL 167 4 4 2 -0.2 N=C(N)NCCCc1c[nH]cn1 10.1021/jm9000693
CHEMBL325327 110631 None 3 Human Binding pEC50 = 8.1 8.1 - 0
Agonist activity at human H4 receptor expressed in insect Sf9 cells co-expressing RGS19 fusion protein and Gialpha2, Gbeta1gamma2 assessed as gamma[32P]GTP binding by liquid scintillation countingAgonist activity at human H4 receptor expressed in insect Sf9 cells co-expressing RGS19 fusion protein and Gialpha2, Gbeta1gamma2 assessed as gamma[32P]GTP binding by liquid scintillation counting
ChEMBL 167 4 4 2 -0.2 N=C(N)NCCCc1c[nH]cn1 10.1021/jm9000693
46887042 8764 None 0 Human Binding pEC50 = 8.1 8.1 - 0
Activity at human recombinant GAIP-fused histamine H4 receptor expressed in Sf9 cells coexpressing Galphai, Gbeta1gamma2 by steady-state GTPase activity assayActivity at human recombinant GAIP-fused histamine H4 receptor expressed in Sf9 cells coexpressing Galphai, Gbeta1gamma2 by steady-state GTPase activity assay
ChEMBL 319 7 4 3 2.6 C[C@H](CC(=O)NC(=N)NCCCc1c[nH]cn1)C1CCCCC1 10.1016/j.bmcl.2010.03.082
CHEMBL1096430 8764 None 0 Human Binding pEC50 = 8.1 8.1 - 0
Activity at human recombinant GAIP-fused histamine H4 receptor expressed in Sf9 cells coexpressing Galphai, Gbeta1gamma2 by steady-state GTPase activity assayActivity at human recombinant GAIP-fused histamine H4 receptor expressed in Sf9 cells coexpressing Galphai, Gbeta1gamma2 by steady-state GTPase activity assay
ChEMBL 319 7 4 3 2.6 C[C@H](CC(=O)NC(=N)NCCCc1c[nH]cn1)C1CCCCC1 10.1016/j.bmcl.2010.03.082
25149521 179158 None 0 Human Binding pEC50 = 8.1 8.1 - 1
Activity at human recombinant histamine H4 receptor-RGS4 fusion protein expressed in Sf9 cells coexpressing Galphai2 and G-beta-1-gamma-2 by steady-state GTPase activity assayActivity at human recombinant histamine H4 receptor-RGS4 fusion protein expressed in Sf9 cells coexpressing Galphai2 and G-beta-1-gamma-2 by steady-state GTPase activity assay
ChEMBL 375 8 4 3 3.2 N=C(NCCCc1c[nH]cn1)NC(=O)CC(c1ccccc1)c1ccccc1 10.1021/jm800841w
CHEMBL471413 179158 None 0 Human Binding pEC50 = 8.1 8.1 - 1
Activity at human recombinant histamine H4 receptor-RGS4 fusion protein expressed in Sf9 cells coexpressing Galphai2 and G-beta-1-gamma-2 by steady-state GTPase activity assayActivity at human recombinant histamine H4 receptor-RGS4 fusion protein expressed in Sf9 cells coexpressing Galphai2 and G-beta-1-gamma-2 by steady-state GTPase activity assay
ChEMBL 375 8 4 3 3.2 N=C(NCCCc1c[nH]cn1)NC(=O)CC(c1ccccc1)c1ccccc1 10.1021/jm800841w
155552061 176583 None 0 Mouse Binding pEC50 = 6.1 6.1 - 2
Agonist activity at mouse H4R expressed in HEK293T-beta-arr2-mH4R cells by beta-arrestin2 recruitment assayAgonist activity at mouse H4R expressed in HEK293T-beta-arr2-mH4R cells by beta-arrestin2 recruitment assay
ChEMBL 277 3 1 5 2.1 CN1CCCN(c2ccnc(NCC(C)(C)C)n2)CC1 10.1021/acs.jmedchem.9b01342
CHEMBL4543119 176583 None 0 Mouse Binding pEC50 = 6.1 6.1 - 2
Agonist activity at mouse H4R expressed in HEK293T-beta-arr2-mH4R cells by beta-arrestin2 recruitment assayAgonist activity at mouse H4R expressed in HEK293T-beta-arr2-mH4R cells by beta-arrestin2 recruitment assay
ChEMBL 277 3 1 5 2.1 CN1CCCN(c2ccnc(NCC(C)(C)C)n2)CC1 10.1021/acs.jmedchem.9b01342
CHEMBL4596606 176583 None 0 Mouse Binding pEC50 = 6.1 6.1 - 2
Agonist activity at mouse H4R expressed in HEK293T-beta-arr2-mH4R cells by beta-arrestin2 recruitment assayAgonist activity at mouse H4R expressed in HEK293T-beta-arr2-mH4R cells by beta-arrestin2 recruitment assay
ChEMBL 277 3 1 5 2.1 CN1CCCN(c2ccnc(NCC(C)(C)C)n2)CC1 10.1021/acs.jmedchem.9b01342
155517880 176772 None 0 Human Binding pEC50 = 7.1 7.1 16 2
Agonist activity at human H4R expressed in HEK293T-beta-arr2-hH4R cells by beta-arrestin2 recruitment assayAgonist activity at human H4R expressed in HEK293T-beta-arr2-hH4R cells by beta-arrestin2 recruitment assay
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 176772 None 0 Human Binding pEC50 = 7.1 7.1 16 2
Agonist activity at human H4R expressed in HEK293T-beta-arr2-hH4R cells by beta-arrestin2 recruitment assayAgonist activity at human H4R expressed in HEK293T-beta-arr2-hH4R cells by beta-arrestin2 recruitment assay
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 176772 None 0 Human Binding pEC50 = 7.1 7.1 16 2
Agonist activity at human H4R expressed in HEK293T-beta-arr2-hH4R cells by beta-arrestin2 recruitment assayAgonist activity at human H4R expressed in HEK293T-beta-arr2-hH4R cells by beta-arrestin2 recruitment assay
ChEMBL 291 4 4 5 1.0 CC(C)(C)CNc1nccc(N2CC[C@@H](NC(=N)N)C2)n1 10.1021/acs.jmedchem.9b01342
1249 2009 None 10 Human Binding pEC50 = 7.1 7.1 -3 3
Inhibition of the cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H4 receptorInhibition of the cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H4 receptor
ChEMBL 139 4 2 2 0.7 NCCCCc1cnc[nH]1 10.1021/jm049932u
13499360 2009 None 10 Human Binding pEC50 = 7.1 7.1 -3 3
Inhibition of the cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H4 receptorInhibition of the cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H4 receptor
ChEMBL 139 4 2 2 0.7 NCCCCc1cnc[nH]1 10.1021/jm049932u
CHEMBL90019 2009 None 10 Human Binding pEC50 = 7.1 7.1 -3 3
Inhibition of the cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H4 receptorInhibition of the cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H4 receptor
ChEMBL 139 4 2 2 0.7 NCCCCc1cnc[nH]1 10.1021/jm049932u
1249 2009 None 10 Human Binding pEC50 = 7.1 7.1 -3 3
Inhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H4 receptorInhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H4 receptor
ChEMBL 139 4 2 2 0.7 NCCCCc1cnc[nH]1 10.1021/jm030905y
13499360 2009 None 10 Human Binding pEC50 = 7.1 7.1 -3 3
Inhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H4 receptorInhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H4 receptor
ChEMBL 139 4 2 2 0.7 NCCCCc1cnc[nH]1 10.1021/jm030905y
CHEMBL90019 2009 None 10 Human Binding pEC50 = 7.1 7.1 -3 3
Inhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H4 receptorInhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H4 receptor
ChEMBL 139 4 2 2 0.7 NCCCCc1cnc[nH]1 10.1021/jm030905y
1204 1932 None 74 Human Binding pEC50 = 8.0 8.0 -3 24
Activity at human recombinant GAIP-fused histamine H4 receptor expressed in Sf9 cells coexpressing Galphai, Gbeta1gamma2 by steady-state GTPase activity assayActivity at human recombinant GAIP-fused histamine H4 receptor expressed in Sf9 cells coexpressing Galphai, Gbeta1gamma2 by steady-state GTPase activity assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmcl.2010.03.082
1247 1932 None 74 Human Binding pEC50 = 8.0 8.0 -3 24
Activity at human recombinant GAIP-fused histamine H4 receptor expressed in Sf9 cells coexpressing Galphai, Gbeta1gamma2 by steady-state GTPase activity assayActivity at human recombinant GAIP-fused histamine H4 receptor expressed in Sf9 cells coexpressing Galphai, Gbeta1gamma2 by steady-state GTPase activity assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmcl.2010.03.082
1375 1932 None 74 Human Binding pEC50 = 8.0 8.0 -3 24
Activity at human recombinant GAIP-fused histamine H4 receptor expressed in Sf9 cells coexpressing Galphai, Gbeta1gamma2 by steady-state GTPase activity assayActivity at human recombinant GAIP-fused histamine H4 receptor expressed in Sf9 cells coexpressing Galphai, Gbeta1gamma2 by steady-state GTPase activity assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmcl.2010.03.082
774 1932 None 74 Human Binding pEC50 = 8.0 8.0 -3 24
Activity at human recombinant GAIP-fused histamine H4 receptor expressed in Sf9 cells coexpressing Galphai, Gbeta1gamma2 by steady-state GTPase activity assayActivity at human recombinant GAIP-fused histamine H4 receptor expressed in Sf9 cells coexpressing Galphai, Gbeta1gamma2 by steady-state GTPase activity assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmcl.2010.03.082
774.0 1932 None 74 Human Binding pEC50 = 8.0 8.0 -3 24
Activity at human recombinant GAIP-fused histamine H4 receptor expressed in Sf9 cells coexpressing Galphai, Gbeta1gamma2 by steady-state GTPase activity assayActivity at human recombinant GAIP-fused histamine H4 receptor expressed in Sf9 cells coexpressing Galphai, Gbeta1gamma2 by steady-state GTPase activity assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmcl.2010.03.082
CHEMBL90 1932 None 74 Human Binding pEC50 = 8.0 8.0 -3 24
Activity at human recombinant GAIP-fused histamine H4 receptor expressed in Sf9 cells coexpressing Galphai, Gbeta1gamma2 by steady-state GTPase activity assayActivity at human recombinant GAIP-fused histamine H4 receptor expressed in Sf9 cells coexpressing Galphai, Gbeta1gamma2 by steady-state GTPase activity assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmcl.2010.03.082
DB05381 1932 None 74 Human Binding pEC50 = 8.0 8.0 -3 24
Activity at human recombinant GAIP-fused histamine H4 receptor expressed in Sf9 cells coexpressing Galphai, Gbeta1gamma2 by steady-state GTPase activity assayActivity at human recombinant GAIP-fused histamine H4 receptor expressed in Sf9 cells coexpressing Galphai, Gbeta1gamma2 by steady-state GTPase activity assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmcl.2010.03.082
4024 2015 None 18 Human Binding pEC50 = 6.0 6.0 -301 2
Inhibition of the cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H4 receptorInhibition of the cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H4 receptor
ChEMBL 159 2 1 2 1.4 n1ccc(cc1)Cc1c[nH]cn1 10.1021/jm049932u
9989505 2015 None 18 Human Binding pEC50 = 6.0 6.0 -301 2
Inhibition of the cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H4 receptorInhibition of the cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H4 receptor
ChEMBL 159 2 1 2 1.4 n1ccc(cc1)Cc1c[nH]cn1 10.1021/jm049932u
CHEMBL82298 2015 None 18 Human Binding pEC50 = 6.0 6.0 -301 2
Inhibition of the cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H4 receptorInhibition of the cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H4 receptor
ChEMBL 159 2 1 2 1.4 n1ccc(cc1)Cc1c[nH]cn1 10.1021/jm049932u
1204 1932 None 74 Mouse Binding pEC50 = 7.0 7.0 -15 24
Agonist activity at mouse SF-His6-tagged histamine H4 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated response incubated for 5 hrs by luciferase reporter gene assayAgonist activity at mouse SF-His6-tagged histamine H4 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated response incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.6b00120
1247 1932 None 74 Mouse Binding pEC50 = 7.0 7.0 -15 24
Agonist activity at mouse SF-His6-tagged histamine H4 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated response incubated for 5 hrs by luciferase reporter gene assayAgonist activity at mouse SF-His6-tagged histamine H4 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated response incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.6b00120
1375 1932 None 74 Mouse Binding pEC50 = 7.0 7.0 -15 24
Agonist activity at mouse SF-His6-tagged histamine H4 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated response incubated for 5 hrs by luciferase reporter gene assayAgonist activity at mouse SF-His6-tagged histamine H4 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated response incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.6b00120
774 1932 None 74 Mouse Binding pEC50 = 7.0 7.0 -15 24
Agonist activity at mouse SF-His6-tagged histamine H4 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated response incubated for 5 hrs by luciferase reporter gene assayAgonist activity at mouse SF-His6-tagged histamine H4 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated response incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.6b00120
774.0 1932 None 74 Mouse Binding pEC50 = 7.0 7.0 -15 24
Agonist activity at mouse SF-His6-tagged histamine H4 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated response incubated for 5 hrs by luciferase reporter gene assayAgonist activity at mouse SF-His6-tagged histamine H4 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated response incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.6b00120
CHEMBL90 1932 None 74 Mouse Binding pEC50 = 7.0 7.0 -15 24
Agonist activity at mouse SF-His6-tagged histamine H4 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated response incubated for 5 hrs by luciferase reporter gene assayAgonist activity at mouse SF-His6-tagged histamine H4 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated response incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.6b00120
DB05381 1932 None 74 Mouse Binding pEC50 = 7.0 7.0 -15 24
Agonist activity at mouse SF-His6-tagged histamine H4 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated response incubated for 5 hrs by luciferase reporter gene assayAgonist activity at mouse SF-His6-tagged histamine H4 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated response incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.6b00120
16718567 8164 None 0 Human Binding pIC50 = 9 9.0 - 1
Displacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assayDisplacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assay
ChEMBL 317 2 2 6 2.4 CN[C@@H]1CCN(c2nc(N)nc3c2oc2ccc(Cl)cc23)C1 10.1016/j.bmcl.2010.02.097
CHEMBL1091874 8164 None 0 Human Binding pIC50 = 9 9.0 - 1
Displacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assayDisplacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assay
ChEMBL 317 2 2 6 2.4 CN[C@@H]1CCN(c2nc(N)nc3c2oc2ccc(Cl)cc23)C1 10.1016/j.bmcl.2010.02.097
46885297 8417 None 0 Human Binding pIC50 = 6 6.0 - 0
Displacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assayDisplacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assay
ChEMBL 318 1 1 6 2.5 CN1CCN(c2nc(O)nc3c2oc2ccc(Cl)cc23)CC1 10.1016/j.bmcl.2010.02.097
CHEMBL1093438 8417 None 0 Human Binding pIC50 = 6 6.0 - 0
Displacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assayDisplacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assay
ChEMBL 318 1 1 6 2.5 CN1CCN(c2nc(O)nc3c2oc2ccc(Cl)cc23)CC1 10.1016/j.bmcl.2010.02.097
17747460 61349 None 13 Human Binding pIC50 = 5 5.0 - 4
Binding affinity to human histamine H4 receptorBinding affinity to human histamine H4 receptor
ChEMBL 640 14 0 6 7.8 O=c1c2ccccc2c(Cc2ccc(Cl)cc2)nn1C[C@H]1CCCN1CCCCc1ccc(OCCCN2CCCCCC2)cc1 10.1021/jm1013874
CHEMBL1767164 61349 None 13 Human Binding pIC50 = 5 5.0 - 4
Binding affinity to human histamine H4 receptorBinding affinity to human histamine H4 receptor
ChEMBL 640 14 0 6 7.8 O=c1c2ccccc2c(Cc2ccc(Cl)cc2)nn1C[C@H]1CCCN1CCCCc1ccc(OCCCN2CCCCCC2)cc1 10.1021/jm1013874
46884945 8247 None 0 Human Binding pIC50 = 5 5.0 - 0
Displacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assayDisplacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assay
ChEMBL 330 1 0 5 3.6 CC1CN(c2ncnc3c2oc2ccc(Cl)cc23)CC(C)N1C 10.1016/j.bmcl.2010.02.097
CHEMBL1092331 8247 None 0 Human Binding pIC50 = 5 5.0 - 0
Displacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assayDisplacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assay
ChEMBL 330 1 0 5 3.6 CC1CN(c2ncnc3c2oc2ccc(Cl)cc23)CC(C)N1C 10.1016/j.bmcl.2010.02.097
71547931 183217 None 0 Human Binding pIC50 = 6.0 6.0 - 0
Displacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting methodDisplacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting method
ChEMBL 289 2 1 7 0.7 CNC1CN(c2nc3ncc(Cl)cc3c3ncnn23)C1 10.1021/acs.jmedchem.7b01855
CHEMBL4794724 183217 None 0 Human Binding pIC50 = 6.0 6.0 - 0
Displacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting methodDisplacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting method
ChEMBL 289 2 1 7 0.7 CNC1CN(c2nc3ncc(Cl)cc3c3ncnn23)C1 10.1021/acs.jmedchem.7b01855
11335478 161059 None 0 Human Binding pIC50 = 6.0 6.0 - 0
Histamine H-4 Receptor Binding Assay: Histamine H-4 Receptor Binding AssayHistamine H-4 Receptor Binding Assay: Histamine H-4 Receptor Binding Assay
ChEMBL 297 0 2 3 3.5 O[C@@H]1Cc2ccccc2C(=C2CCNCC2)c2ccsc21 nan
CHEMBL4115693 161059 None 0 Human Binding pIC50 = 6.0 6.0 - 0
Histamine H-4 Receptor Binding Assay: Histamine H-4 Receptor Binding AssayHistamine H-4 Receptor Binding Assay: Histamine H-4 Receptor Binding Assay
ChEMBL 297 0 2 3 3.5 O[C@@H]1Cc2ccccc2C(=C2CCNCC2)c2ccsc21 nan
1224 1432 None 51 Human Binding pIC50 = 5.0 5.0 -194 13
Histamine H-4 Receptor Binding Assay: Histamine H-4 Receptor Binding AssayHistamine H-4 Receptor Binding Assay: Histamine H-4 Receptor Binding Assay
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C nan
3100 1432 None 51 Human Binding pIC50 = 5.0 5.0 -194 13
Histamine H-4 Receptor Binding Assay: Histamine H-4 Receptor Binding AssayHistamine H-4 Receptor Binding Assay: Histamine H-4 Receptor Binding Assay
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C nan
3100.0 1432 None 51 Human Binding pIC50 = 5.0 5.0 -194 13
Histamine H-4 Receptor Binding Assay: Histamine H-4 Receptor Binding AssayHistamine H-4 Receptor Binding Assay: Histamine H-4 Receptor Binding Assay
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C nan
8980 1432 None 51 Human Binding pIC50 = 5.0 5.0 -194 13
Histamine H-4 Receptor Binding Assay: Histamine H-4 Receptor Binding AssayHistamine H-4 Receptor Binding Assay: Histamine H-4 Receptor Binding Assay
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C nan
916 1432 None 51 Human Binding pIC50 = 5.0 5.0 -194 13
Histamine H-4 Receptor Binding Assay: Histamine H-4 Receptor Binding AssayHistamine H-4 Receptor Binding Assay: Histamine H-4 Receptor Binding Assay
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C nan
CHEMBL657 1432 None 51 Human Binding pIC50 = 5.0 5.0 -194 13
Histamine H-4 Receptor Binding Assay: Histamine H-4 Receptor Binding AssayHistamine H-4 Receptor Binding Assay: Histamine H-4 Receptor Binding Assay
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C nan
DB01075 1432 None 51 Human Binding pIC50 = 5.0 5.0 -194 13
Histamine H-4 Receptor Binding Assay: Histamine H-4 Receptor Binding AssayHistamine H-4 Receptor Binding Assay: Histamine H-4 Receptor Binding Assay
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C nan
11709443 8248 None 0 Human Binding pIC50 = 7.0 7.0 - 0
Displacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assayDisplacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assay
ChEMBL 314 1 0 5 2.9 CN1C[C@@H]2C[C@H]1CN2c1ncnc2c1oc1ccc(Cl)cc12 10.1016/j.bmcl.2010.02.097
CHEMBL1092332 8248 None 0 Human Binding pIC50 = 7.0 7.0 - 0
Displacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assayDisplacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assay
ChEMBL 314 1 0 5 2.9 CN1C[C@@H]2C[C@H]1CN2c1ncnc2c1oc1ccc(Cl)cc12 10.1016/j.bmcl.2010.02.097
71548405 182265 None 0 Human Binding pIC50 = 5.9 5.9 - 0
Displacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting methodDisplacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting method
ChEMBL 303 2 0 7 1.1 CN(C)C1CN(c2nc3ncc(Cl)cc3n3cnnc23)C1 10.1021/acs.jmedchem.7b01855
CHEMBL4782441 182265 None 0 Human Binding pIC50 = 5.9 5.9 - 0
Displacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting methodDisplacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting method
ChEMBL 303 2 0 7 1.1 CN(C)C1CN(c2nc3ncc(Cl)cc3n3cnnc23)C1 10.1021/acs.jmedchem.7b01855
46884998 7979 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Displacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assayDisplacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assay
ChEMBL 288 1 1 5 2.6 NC1CCN(c2ncnc3c2oc2ccc(Cl)cc23)C1 10.1016/j.bmcl.2010.02.097
CHEMBL1090532 7979 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Displacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assayDisplacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assay
ChEMBL 288 1 1 5 2.6 NC1CCN(c2ncnc3c2oc2ccc(Cl)cc23)C1 10.1016/j.bmcl.2010.02.097
25112105 8165 None 0 Human Binding pIC50 = 7.9 7.9 - 1
Displacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assayDisplacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assay
ChEMBL 317 2 2 6 2.4 CN[C@H]1CCN(c2nc(N)nc3c2oc2ccc(Cl)cc23)C1 10.1016/j.bmcl.2010.02.097
CHEMBL1091875 8165 None 0 Human Binding pIC50 = 7.9 7.9 - 1
Displacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assayDisplacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assay
ChEMBL 317 2 2 6 2.4 CN[C@H]1CCN(c2nc(N)nc3c2oc2ccc(Cl)cc23)C1 10.1016/j.bmcl.2010.02.097
71547681 183051 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Displacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting methodDisplacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting method
ChEMBL 289 1 1 7 0.7 Clc1cnc2nc(N3CCNCC3)c3nncn3c2c1 10.1021/acs.jmedchem.7b01855
CHEMBL4792733 183051 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Displacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting methodDisplacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting method
ChEMBL 289 1 1 7 0.7 Clc1cnc2nc(N3CCNCC3)c3nncn3c2c1 10.1021/acs.jmedchem.7b01855
46885128 7972 None 0 Human Binding pIC50 = 5.9 5.9 - 0
Displacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assayDisplacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assay
ChEMBL 316 2 1 5 3.2 CNC1(C)CCN(c2ncnc3c2oc2ccc(Cl)cc23)C1 10.1016/j.bmcl.2010.02.097
CHEMBL1090519 7972 None 0 Human Binding pIC50 = 5.9 5.9 - 0
Displacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assayDisplacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assay
ChEMBL 316 2 1 5 3.2 CNC1(C)CCN(c2ncnc3c2oc2ccc(Cl)cc23)C1 10.1016/j.bmcl.2010.02.097
46885129 7973 None 0 Human Binding pIC50 = 5.9 5.9 - 0
Displacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assayDisplacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assay
ChEMBL 328 1 1 5 3.2 Clc1ccc2oc3c(N4CC5CCCNC5C4)ncnc3c2c1 10.1016/j.bmcl.2010.02.097
CHEMBL1090520 7973 None 0 Human Binding pIC50 = 5.9 5.9 - 0
Displacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assayDisplacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assay
ChEMBL 328 1 1 5 3.2 Clc1ccc2oc3c(N4CC5CCCNC5C4)ncnc3c2c1 10.1016/j.bmcl.2010.02.097
46885241 8277 None 0 Human Binding pIC50 = 4.9 4.9 - 0
Displacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assayDisplacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assay
ChEMBL 370 2 1 5 3.8 CN[C@@H]1CCN(c2nc(C(F)(F)F)nc3c2oc2ccc(Cl)cc23)C1 10.1016/j.bmcl.2010.02.097
CHEMBL1092543 8277 None 0 Human Binding pIC50 = 4.9 4.9 - 0
Displacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assayDisplacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assay
ChEMBL 370 2 1 5 3.8 CN[C@@H]1CCN(c2nc(C(F)(F)F)nc3c2oc2ccc(Cl)cc23)C1 10.1016/j.bmcl.2010.02.097
156013896 178345 None 0 Human Binding pIC50 = 7.8 7.8 -7 4
Inverse agonist activity at human H4R expressed in HEK293 cells co-expressing ELucC/ELucN-beta-arrestin2 assessed as inhibition of histamine-induced beta-arrestin recruitment by luciferase reporter gene assayInverse agonist activity at human H4R expressed in HEK293 cells co-expressing ELucC/ELucN-beta-arrestin2 assessed as inhibition of histamine-induced beta-arrestin recruitment by luciferase reporter gene assay
ChEMBL 401 9 1 2 5.1 Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCCCc1c[nH]cn1 10.1021/acs.jmedchem.0c00160
CHEMBL4635634 178345 None 0 Human Binding pIC50 = 7.8 7.8 -7 4
Inverse agonist activity at human H4R expressed in HEK293 cells co-expressing ELucC/ELucN-beta-arrestin2 assessed as inhibition of histamine-induced beta-arrestin recruitment by luciferase reporter gene assayInverse agonist activity at human H4R expressed in HEK293 cells co-expressing ELucC/ELucN-beta-arrestin2 assessed as inhibition of histamine-induced beta-arrestin recruitment by luciferase reporter gene assay
ChEMBL 401 9 1 2 5.1 Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCCCc1c[nH]cn1 10.1021/acs.jmedchem.0c00160
CHEMBL4650570 178345 None 0 Human Binding pIC50 = 7.8 7.8 -7 4
Inverse agonist activity at human H4R expressed in HEK293 cells co-expressing ELucC/ELucN-beta-arrestin2 assessed as inhibition of histamine-induced beta-arrestin recruitment by luciferase reporter gene assayInverse agonist activity at human H4R expressed in HEK293 cells co-expressing ELucC/ELucN-beta-arrestin2 assessed as inhibition of histamine-induced beta-arrestin recruitment by luciferase reporter gene assay
ChEMBL 401 9 1 2 5.1 Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCCCc1c[nH]cn1 10.1021/acs.jmedchem.0c00160
16656869 8106 None 1 Human Binding pIC50 = 5.8 5.8 - 0
Displacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assayDisplacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assay
ChEMBL 316 2 1 5 3.1 CNC1CCN(c2nc(C)nc3c2oc2ccc(Cl)cc23)C1 10.1016/j.bmcl.2010.02.097
CHEMBL1091559 8106 None 1 Human Binding pIC50 = 5.8 5.8 - 0
Displacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assayDisplacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assay
ChEMBL 316 2 1 5 3.1 CNC1CCN(c2nc(C)nc3c2oc2ccc(Cl)cc23)C1 10.1016/j.bmcl.2010.02.097
124087 1389 None 72 Human Binding pIC50 = 4.8 4.8 -5888 15
Histamine H-4 Receptor Binding Assay: Histamine H-4 Receptor Binding AssayHistamine H-4 Receptor Binding Assay: Histamine H-4 Receptor Binding Assay
ChEMBL 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 nan
124087.0 1389 None 72 Human Binding pIC50 = 4.8 4.8 -5888 15
Histamine H-4 Receptor Binding Assay: Histamine H-4 Receptor Binding AssayHistamine H-4 Receptor Binding Assay: Histamine H-4 Receptor Binding Assay
ChEMBL 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 nan
7157 1389 None 72 Human Binding pIC50 = 4.8 4.8 -5888 15
Histamine H-4 Receptor Binding Assay: Histamine H-4 Receptor Binding AssayHistamine H-4 Receptor Binding Assay: Histamine H-4 Receptor Binding Assay
ChEMBL 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 nan
814 1389 None 72 Human Binding pIC50 = 4.8 4.8 -5888 15
Histamine H-4 Receptor Binding Assay: Histamine H-4 Receptor Binding AssayHistamine H-4 Receptor Binding Assay: Histamine H-4 Receptor Binding Assay
ChEMBL 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 nan
CHEMBL1172 1389 None 72 Human Binding pIC50 = 4.8 4.8 -5888 15
Histamine H-4 Receptor Binding Assay: Histamine H-4 Receptor Binding AssayHistamine H-4 Receptor Binding Assay: Histamine H-4 Receptor Binding Assay
ChEMBL 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 nan
DB00967 1389 None 72 Human Binding pIC50 = 4.8 4.8 -5888 15
Histamine H-4 Receptor Binding Assay: Histamine H-4 Receptor Binding AssayHistamine H-4 Receptor Binding Assay: Histamine H-4 Receptor Binding Assay
ChEMBL 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 nan
11566111 8348 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Displacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assayDisplacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assay
ChEMBL 328 1 0 5 3.3 CN1CC2CCC1CN2c1ncnc2c1oc1ccc(Cl)cc12 10.1016/j.bmcl.2010.02.097
CHEMBL1092933 8348 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Displacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assayDisplacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assay
ChEMBL 328 1 0 5 3.3 CN1CC2CCC1CN2c1ncnc2c1oc1ccc(Cl)cc12 10.1016/j.bmcl.2010.02.097
71547932 182873 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Displacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting methodDisplacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting method
ChEMBL 303 1 0 7 1.1 CN1CCN(c2nc3ncc(Cl)cc3c3ncnn23)CC1 10.1021/acs.jmedchem.7b01855
CHEMBL4790239 182873 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Displacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting methodDisplacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting method
ChEMBL 303 1 0 7 1.1 CN1CCN(c2nc3ncc(Cl)cc3c3ncnn23)CC1 10.1021/acs.jmedchem.7b01855
13680692 183540 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Displacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting methodDisplacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting method
ChEMBL 313 2 0 8 0.9 CN1CCN(c2nc3ccc([N+](=O)[O-])cc3n3cnnc23)CC1 10.1021/acs.jmedchem.7b01855
CHEMBL4798729 183540 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Displacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting methodDisplacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting method
ChEMBL 313 2 0 8 0.9 CN1CCN(c2nc3ccc([N+](=O)[O-])cc3n3cnnc23)CC1 10.1021/acs.jmedchem.7b01855
46885239 8196 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Displacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assayDisplacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assay
ChEMBL 302 2 1 5 2.8 CN[C@@H]1CCN(c2ncnc3c2oc2cc(Cl)ccc23)C1 10.1016/j.bmcl.2010.02.097
CHEMBL1092064 8196 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Displacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assayDisplacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assay
ChEMBL 302 2 1 5 2.8 CN[C@@H]1CCN(c2ncnc3c2oc2cc(Cl)ccc23)C1 10.1016/j.bmcl.2010.02.097
71547762 182825 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Displacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting methodDisplacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting method
ChEMBL 337 1 0 7 1.7 CN1CCN(c2nc3nc(Cl)c(Cl)cc3n3cnnc23)CC1 10.1021/acs.jmedchem.7b01855
CHEMBL4789645 182825 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Displacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting methodDisplacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting method
ChEMBL 337 1 0 7 1.7 CN1CCN(c2nc3nc(Cl)c(Cl)cc3n3cnnc23)CC1 10.1021/acs.jmedchem.7b01855
2063135 8380 None 6 Human Binding pIC50 = 7.7 7.7 - 1
Displacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assayDisplacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assay
ChEMBL 302 1 0 5 2.8 CN1CCN(c2ncnc3c2oc2ccc(Cl)cc23)CC1 10.1016/j.bmcl.2010.02.097
CHEMBL1093180 8380 None 6 Human Binding pIC50 = 7.7 7.7 - 1
Displacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assayDisplacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assay
ChEMBL 302 1 0 5 2.8 CN1CCN(c2ncnc3c2oc2ccc(Cl)cc23)CC1 10.1016/j.bmcl.2010.02.097
11695388 8246 None 0 Human Binding pIC50 = 5.7 5.7 - 0
Displacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assayDisplacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assay
ChEMBL 316 1 0 5 3.2 CC1CN(c2ncnc3c2oc2ccc(Cl)cc23)CCN1C 10.1016/j.bmcl.2010.02.097
CHEMBL1092330 8246 None 0 Human Binding pIC50 = 5.7 5.7 - 0
Displacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assayDisplacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assay
ChEMBL 316 1 0 5 3.2 CC1CN(c2ncnc3c2oc2ccc(Cl)cc23)CCN1C 10.1016/j.bmcl.2010.02.097
9904236 14081 None 23 Human Binding pIC50 = 5.7 5.7 - 1
Histamine H-4 Receptor Binding Assay: Histamine H-4 Receptor Binding AssayHistamine H-4 Receptor Binding Assay: Histamine H-4 Receptor Binding Assay
ChEMBL 295 0 1 3 3.7 O=C1Cc2ccccc2C(=C2CCNCC2)c2ccsc21 nan
CHEMBL1197564 14081 None 23 Human Binding pIC50 = 5.7 5.7 - 1
Histamine H-4 Receptor Binding Assay: Histamine H-4 Receptor Binding AssayHistamine H-4 Receptor Binding Assay: Histamine H-4 Receptor Binding Assay
ChEMBL 295 0 1 3 3.7 O=C1Cc2ccccc2C(=C2CCNCC2)c2ccsc21 nan
46884997 7722 None 0 Human Binding pIC50 = 4.7 4.7 - 0
Displacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assayDisplacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assay
ChEMBL 316 2 0 5 3.2 CN(C)C1CCN(c2ncnc3c2oc2ccc(Cl)cc23)C1 10.1016/j.bmcl.2010.02.097
CHEMBL1088888 7722 None 0 Human Binding pIC50 = 4.7 4.7 - 0
Displacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assayDisplacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assay
ChEMBL 316 2 0 5 3.2 CN(C)C1CCN(c2ncnc3c2oc2ccc(Cl)cc23)C1 10.1016/j.bmcl.2010.02.097
1530 2182 None 36 Human Binding pIC50 = 4.7 4.7 -21379 24
Histamine H-4 Receptor Binding Assay: Histamine H-4 Receptor Binding AssayHistamine H-4 Receptor Binding Assay: Histamine H-4 Receptor Binding Assay
ChEMBL 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 nan
3827 2182 None 36 Human Binding pIC50 = 4.7 4.7 -21379 24
Histamine H-4 Receptor Binding Assay: Histamine H-4 Receptor Binding AssayHistamine H-4 Receptor Binding Assay: Histamine H-4 Receptor Binding Assay
ChEMBL 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 nan
3827.0 2182 None 36 Human Binding pIC50 = 4.7 4.7 -21379 24
Histamine H-4 Receptor Binding Assay: Histamine H-4 Receptor Binding AssayHistamine H-4 Receptor Binding Assay: Histamine H-4 Receptor Binding Assay
ChEMBL 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 nan
7206 2182 None 36 Human Binding pIC50 = 4.7 4.7 -21379 24
Histamine H-4 Receptor Binding Assay: Histamine H-4 Receptor Binding AssayHistamine H-4 Receptor Binding Assay: Histamine H-4 Receptor Binding Assay
ChEMBL 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 nan
CHEMBL534 2182 None 36 Human Binding pIC50 = 4.7 4.7 -21379 24
Histamine H-4 Receptor Binding Assay: Histamine H-4 Receptor Binding AssayHistamine H-4 Receptor Binding Assay: Histamine H-4 Receptor Binding Assay
ChEMBL 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 nan
DB00920 2182 None 36 Human Binding pIC50 = 4.7 4.7 -21379 24
Histamine H-4 Receptor Binding Assay: Histamine H-4 Receptor Binding AssayHistamine H-4 Receptor Binding Assay: Histamine H-4 Receptor Binding Assay
ChEMBL 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 nan
20889070 181978 None 5 Human Binding pIC50 = 7.7 7.7 - 0
Displacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting methodDisplacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting method
ChEMBL 302 1 0 6 1.7 CN1CCN(c2nc3ccc(Cl)cc3n3cnnc23)CC1 10.1021/acs.jmedchem.7b01855
CHEMBL4778864 181978 None 5 Human Binding pIC50 = 7.7 7.7 - 0
Displacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting methodDisplacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting method
ChEMBL 302 1 0 6 1.7 CN1CCN(c2nc3ccc(Cl)cc3n3cnnc23)CC1 10.1021/acs.jmedchem.7b01855
820836 102996 None 5 Human Binding pIC50 = 5.6 5.6 - 0
Displacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting methodDisplacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting method
ChEMBL 268 1 0 6 1.0 CN1CCN(c2nc3ccccc3n3cnnc23)CC1 10.1021/acs.jmedchem.7b01855
CHEMBL306316 102996 None 5 Human Binding pIC50 = 5.6 5.6 - 0
Displacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting methodDisplacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting method
ChEMBL 268 1 0 6 1.0 CN1CCN(c2nc3ccccc3n3cnnc23)CC1 10.1021/acs.jmedchem.7b01855
121237834 147447 None 0 Human Binding pIC50 = 5.6 5.6 - 0
Histamine H-4 Receptor Binding Assay: Histamine H-4 Receptor Binding AssayHistamine H-4 Receptor Binding Assay: Histamine H-4 Receptor Binding Assay
ChEMBL 297 0 2 3 3.5 O[C@H]1Cc2ccccc2C(=C2CCNCC2)c2ccsc21 nan
CHEMBL3929465 147447 None 0 Human Binding pIC50 = 5.6 5.6 - 0
Histamine H-4 Receptor Binding Assay: Histamine H-4 Receptor Binding AssayHistamine H-4 Receptor Binding Assay: Histamine H-4 Receptor Binding Assay
ChEMBL 297 0 2 3 3.5 O[C@H]1Cc2ccccc2C(=C2CCNCC2)c2ccsc21 nan
46884996 7999 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Displacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assayDisplacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assay
ChEMBL 328 1 0 5 3.3 Clc1ccc2oc3c(N4CCN5CCCC5C4)ncnc3c2c1 10.1016/j.bmcl.2010.02.097
CHEMBL1090655 7999 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Displacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assayDisplacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assay
ChEMBL 328 1 0 5 3.3 Clc1ccc2oc3c(N4CCN5CCCC5C4)ncnc3c2c1 10.1016/j.bmcl.2010.02.097
71548223 181966 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Displacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting methodDisplacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting method
ChEMBL 401 3 0 8 2.0 CN1CCN(c2nc3nc(OCC(F)(F)F)c(Cl)cc3n3cnnc23)CC1 10.1021/acs.jmedchem.7b01855
CHEMBL4778712 181966 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Displacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting methodDisplacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting method
ChEMBL 401 3 0 8 2.0 CN1CCN(c2nc3nc(OCC(F)(F)F)c(Cl)cc3n3cnnc23)CC1 10.1021/acs.jmedchem.7b01855
71547685 183096 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Displacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting methodDisplacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting method
ChEMBL 294 1 0 8 0.3 CN1CCN(c2nc3ncc(C#N)cc3n3cnnc23)CC1 10.1021/acs.jmedchem.7b01855
CHEMBL4793425 183096 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Displacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting methodDisplacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting method
ChEMBL 294 1 0 8 0.3 CN1CCN(c2nc3ncc(C#N)cc3n3cnnc23)CC1 10.1021/acs.jmedchem.7b01855
71548412 1909 None 22 Human Binding pIC50 = 7.6 7.6 - 0
Displacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting methodDisplacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting method
ChEMBL 334 2 1 8 0.2 CNC1CN(C1)c1nc2ncc(cc2n2c1nnn2)Br 10.1021/acs.jmedchem.7b01855
9879 1909 None 22 Human Binding pIC50 = 7.6 7.6 - 0
Displacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting methodDisplacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting method
ChEMBL 334 2 1 8 0.2 CNC1CN(C1)c1nc2ncc(cc2n2c1nnn2)Br 10.1021/acs.jmedchem.7b01855
CHEMBL4790724 1909 None 22 Human Binding pIC50 = 7.6 7.6 - 0
Displacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting methodDisplacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting method
ChEMBL 334 2 1 8 0.2 CNC1CN(C1)c1nc2ncc(cc2n2c1nnn2)Br 10.1021/acs.jmedchem.7b01855
71547764 182459 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Displacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting methodDisplacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting method
ChEMBL 328 1 0 8 0.9 CN1CCN(c2nc3nc(C#N)c(Cl)cc3n3cnnc23)CC1 10.1021/acs.jmedchem.7b01855
CHEMBL4784683 182459 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Displacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting methodDisplacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting method
ChEMBL 328 1 0 8 0.9 CN1CCN(c2nc3nc(C#N)c(Cl)cc3n3cnnc23)CC1 10.1021/acs.jmedchem.7b01855
71548498 182346 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Displacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting methodDisplacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting method
ChEMBL 348 1 0 8 0.6 CN1CCN(c2nc3ncc(Br)cc3n3nnnc23)CC1 10.1021/acs.jmedchem.7b01855
CHEMBL4783487 182346 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Displacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting methodDisplacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting method
ChEMBL 348 1 0 8 0.6 CN1CCN(c2nc3ncc(Br)cc3n3nnnc23)CC1 10.1021/acs.jmedchem.7b01855
71548031 183014 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Displacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting methodDisplacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting method
ChEMBL 337 1 0 7 1.4 CN1CCN(c2nc3ncc(C(F)(F)F)cc3n3cnnc23)CC1 10.1021/acs.jmedchem.7b01855
CHEMBL4792352 183014 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Displacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting methodDisplacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting method
ChEMBL 337 1 0 7 1.4 CN1CCN(c2nc3ncc(C(F)(F)F)cc3n3cnnc23)CC1 10.1021/acs.jmedchem.7b01855
16656871 7978 None 0 Human Binding pIC50 = 6.5 6.5 - 0
Displacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assayDisplacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assay
ChEMBL 302 2 1 5 2.8 CN[C@H]1CCN(c2ncnc3c2oc2ccc(Cl)cc23)C1 10.1016/j.bmcl.2010.02.097
CHEMBL1090531 7978 None 0 Human Binding pIC50 = 6.5 6.5 - 0
Displacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assayDisplacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assay
ChEMBL 302 2 1 5 2.8 CN[C@H]1CCN(c2ncnc3c2oc2ccc(Cl)cc23)C1 10.1016/j.bmcl.2010.02.097
1278 2150 None 56 Human Binding pIC50 = 7.5 7.5 -3 8
Displacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting methodDisplacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting method
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/acs.jmedchem.7b01855
1279 2150 None 56 Human Binding pIC50 = 7.5 7.5 -3 8
Displacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting methodDisplacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting method
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/acs.jmedchem.7b01855
4908365 2150 None 56 Human Binding pIC50 = 7.5 7.5 -3 8
Displacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting methodDisplacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting method
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/acs.jmedchem.7b01855
CHEMBL129198 2150 None 56 Human Binding pIC50 = 7.5 7.5 -3 8
Displacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting methodDisplacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting method
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/acs.jmedchem.7b01855
71548412 1909 None 22 Mouse Binding pIC50 = 6.5 6.5 - 0
Displacement of [3H]-histamine from recombinant mouse histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting methodDisplacement of [3H]-histamine from recombinant mouse histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting method
ChEMBL 334 2 1 8 0.2 CNC1CN(C1)c1nc2ncc(cc2n2c1nnn2)Br 10.1021/acs.jmedchem.7b01855
9879 1909 None 22 Mouse Binding pIC50 = 6.5 6.5 - 0
Displacement of [3H]-histamine from recombinant mouse histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting methodDisplacement of [3H]-histamine from recombinant mouse histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting method
ChEMBL 334 2 1 8 0.2 CNC1CN(C1)c1nc2ncc(cc2n2c1nnn2)Br 10.1021/acs.jmedchem.7b01855
CHEMBL4790724 1909 None 22 Mouse Binding pIC50 = 6.5 6.5 - 0
Displacement of [3H]-histamine from recombinant mouse histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting methodDisplacement of [3H]-histamine from recombinant mouse histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting method
ChEMBL 334 2 1 8 0.2 CNC1CN(C1)c1nc2ncc(cc2n2c1nnn2)Br 10.1021/acs.jmedchem.7b01855
71548319 183344 None 0 Human Binding pIC50 = 5.5 5.5 - 0
Displacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting methodDisplacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting method
ChEMBL 317 1 0 7 1.5 CN1CCCN(c2nc3ncc(Cl)cc3n3cnnc23)CC1 10.1021/acs.jmedchem.7b01855
CHEMBL4796300 183344 None 0 Human Binding pIC50 = 5.5 5.5 - 0
Displacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting methodDisplacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting method
ChEMBL 317 1 0 7 1.5 CN1CCCN(c2nc3ncc(Cl)cc3n3cnnc23)CC1 10.1021/acs.jmedchem.7b01855
46885178 7715 None 0 Human Binding pIC50 = 7.5 7.5 - 0
Displacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assayDisplacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assay
ChEMBL 336 2 1 5 3.2 CN[C@@H]1CCN(c2ncnc3c2oc2ccc(C(F)(F)F)cc23)C1 10.1016/j.bmcl.2010.02.097
CHEMBL1088859 7715 None 0 Human Binding pIC50 = 7.5 7.5 - 0
Displacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assayDisplacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assay
ChEMBL 336 2 1 5 3.2 CN[C@@H]1CCN(c2ncnc3c2oc2ccc(C(F)(F)F)cc23)C1 10.1016/j.bmcl.2010.02.097
71548224 182634 None 0 Human Binding pIC50 = 6.5 6.5 - 0
Displacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting methodDisplacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting method
ChEMBL 361 1 0 7 1.5 Cc1c(Br)cnc2nc(N3CCN(C)CC3)c3nncn3c12 10.1021/acs.jmedchem.7b01855
CHEMBL4787243 182634 None 0 Human Binding pIC50 = 6.5 6.5 - 0
Displacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting methodDisplacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting method
ChEMBL 361 1 0 7 1.5 Cc1c(Br)cnc2nc(N3CCN(C)CC3)c3nncn3c12 10.1021/acs.jmedchem.7b01855
71547599 182174 None 0 Human Binding pIC50 = 5.5 5.5 - 0
Displacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting methodDisplacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting method
ChEMBL 269 1 0 7 0.4 CN1CCN(c2nc3ncccc3n3cnnc23)CC1 10.1021/acs.jmedchem.7b01855
CHEMBL4781409 182174 None 0 Human Binding pIC50 = 5.5 5.5 - 0
Displacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting methodDisplacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting method
ChEMBL 269 1 0 7 0.4 CN1CCN(c2nc3ncccc3n3cnnc23)CC1 10.1021/acs.jmedchem.7b01855
71547680 182933 None 0 Human Binding pIC50 = 5.5 5.5 - 0
Displacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting methodDisplacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting method
ChEMBL 269 1 0 7 0.4 CN1CCN(c2nc3cccnc3n3cnnc23)CC1 10.1021/acs.jmedchem.7b01855
CHEMBL4791152 182933 None 0 Human Binding pIC50 = 5.5 5.5 - 0
Displacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting methodDisplacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting method
ChEMBL 269 1 0 7 0.4 CN1CCN(c2nc3cccnc3n3cnnc23)CC1 10.1021/acs.jmedchem.7b01855
11709905 8373 None 0 Human Binding pIC50 = 6.5 6.5 - 0
Displacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assayDisplacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assay
ChEMBL 342 2 0 5 3.7 CN1CCN(c2nc(C3CC3)nc3c2oc2ccc(Cl)cc23)CC1 10.1016/j.bmcl.2010.02.097
CHEMBL1093138 8373 None 0 Human Binding pIC50 = 6.5 6.5 - 0
Displacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assayDisplacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assay
ChEMBL 342 2 0 5 3.7 CN1CCN(c2nc(C3CC3)nc3c2oc2ccc(Cl)cc23)CC1 10.1016/j.bmcl.2010.02.097
16656872 7914 None 0 Human Binding pIC50 = 7.5 7.5 - 0
Displacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assayDisplacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assay
ChEMBL 302 2 1 5 2.8 CN[C@@H]1CCN(c2ncnc3c2oc2ccc(Cl)cc23)C1 10.1016/j.bmcl.2010.02.097
CHEMBL1090190 7914 None 0 Human Binding pIC50 = 7.5 7.5 - 0
Displacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assayDisplacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assay
ChEMBL 302 2 1 5 2.8 CN[C@@H]1CCN(c2ncnc3c2oc2ccc(Cl)cc23)C1 10.1016/j.bmcl.2010.02.097
71548027 181956 None 0 Human Binding pIC50 = 7.5 7.5 - 0
Displacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting methodDisplacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting method
ChEMBL 395 1 0 7 1.0 CN1CCN(c2nc3ncc(I)cc3n3cnnc23)CC1 10.1021/acs.jmedchem.7b01855
CHEMBL4778591 181956 None 0 Human Binding pIC50 = 7.5 7.5 - 0
Displacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting methodDisplacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting method
ChEMBL 395 1 0 7 1.0 CN1CCN(c2nc3ncc(I)cc3n3cnnc23)CC1 10.1021/acs.jmedchem.7b01855
3934857 8105 None 27 Human Binding pIC50 = 7.4 7.4 - 0
Displacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assayDisplacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assay
ChEMBL 316 1 0 5 3.1 Cc1nc(N2CCN(C)CC2)c2oc3ccc(Cl)cc3c2n1 10.1016/j.bmcl.2010.02.097
CHEMBL1091558 8105 None 27 Human Binding pIC50 = 7.4 7.4 - 0
Displacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assayDisplacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assay
ChEMBL 316 1 0 5 3.1 Cc1nc(N2CCN(C)CC2)c2oc3ccc(Cl)cc3c2n1 10.1016/j.bmcl.2010.02.097
71547282 183179 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Displacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting methodDisplacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting method
ChEMBL 317 1 0 7 1.5 C[C@H]1CN(c2nc3ncc(Cl)cc3n3cnnc23)CCN1C 10.1021/acs.jmedchem.7b01855
CHEMBL4794336 183179 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Displacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting methodDisplacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting method
ChEMBL 317 1 0 7 1.5 C[C@H]1CN(c2nc3ncc(Cl)cc3n3cnnc23)CCN1C 10.1021/acs.jmedchem.7b01855
1278 2150 None 56 Mouse Binding pIC50 = 7.4 7.4 -4 8
Inhibition of histamine H4 receptor-mediated chemotaxis in mouse bone marrow cellsInhibition of histamine H4 receptor-mediated chemotaxis in mouse bone marrow cells
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1016/j.ejmech.2012.06.016
1279 2150 None 56 Mouse Binding pIC50 = 7.4 7.4 -4 8
Inhibition of histamine H4 receptor-mediated chemotaxis in mouse bone marrow cellsInhibition of histamine H4 receptor-mediated chemotaxis in mouse bone marrow cells
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1016/j.ejmech.2012.06.016
4908365 2150 None 56 Mouse Binding pIC50 = 7.4 7.4 -4 8
Inhibition of histamine H4 receptor-mediated chemotaxis in mouse bone marrow cellsInhibition of histamine H4 receptor-mediated chemotaxis in mouse bone marrow cells
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1016/j.ejmech.2012.06.016
CHEMBL129198 2150 None 56 Mouse Binding pIC50 = 7.4 7.4 -4 8
Inhibition of histamine H4 receptor-mediated chemotaxis in mouse bone marrow cellsInhibition of histamine H4 receptor-mediated chemotaxis in mouse bone marrow cells
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1016/j.ejmech.2012.06.016
89477685 183680 None 0 Human Binding pIC50 = 5.4 5.4 - 0
Displacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting methodDisplacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting method
ChEMBL 303 2 1 7 1.1 CN[C@@H]1CCN(c2nc3ncc(Cl)cc3n3cnnc23)C1 10.1021/acs.jmedchem.7b01855
CHEMBL4800462 183680 None 0 Human Binding pIC50 = 5.4 5.4 - 0
Displacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting methodDisplacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting method
ChEMBL 303 2 1 7 1.1 CN[C@@H]1CCN(c2nc3ncc(Cl)cc3n3cnnc23)C1 10.1021/acs.jmedchem.7b01855
89477651 183554 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Displacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting methodDisplacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting method
ChEMBL 315 1 0 7 1.2 CN1C[C@@H]2C[C@H]1CN2c1nc2ncc(Cl)cc2n2cnnc12 10.1021/acs.jmedchem.7b01855
CHEMBL4798915 183554 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Displacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting methodDisplacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting method
ChEMBL 315 1 0 7 1.2 CN1C[C@@H]2C[C@H]1CN2c1nc2ncc(Cl)cc2n2cnnc12 10.1021/acs.jmedchem.7b01855
11638468 8349 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Displacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assayDisplacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assay
ChEMBL 328 1 0 5 3.3 CN1C2CCC1CN(c1ncnc3c1oc1ccc(Cl)cc13)C2 10.1016/j.bmcl.2010.02.097
CHEMBL1092934 8349 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Displacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assayDisplacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assay
ChEMBL 328 1 0 5 3.3 CN1C2CCC1CN(c1ncnc3c1oc1ccc(Cl)cc13)C2 10.1016/j.bmcl.2010.02.097
71547281 183393 None 0 Human Binding pIC50 = 5.3 5.3 - 0
Displacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting methodDisplacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting method
ChEMBL 317 2 0 7 1.5 CN(C)[C@@H]1CCN(c2nc3ncc(Cl)cc3n3cnnc23)C1 10.1021/acs.jmedchem.7b01855
CHEMBL4796842 183393 None 0 Human Binding pIC50 = 5.3 5.3 - 0
Displacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting methodDisplacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting method
ChEMBL 317 2 0 7 1.5 CN(C)[C@@H]1CCN(c2nc3ncc(Cl)cc3n3cnnc23)C1 10.1021/acs.jmedchem.7b01855
1267 3804 None 32 Human Binding pIC50 = 6.3 6.3 -33 27
Inverse agonist activity at human H4R expressed in HEK293 cells co-expressing ELucC/ELucN-beta-arrestin2 assessed as inhibition of histamine-induced beta-arrestin recruitment by luciferase reporter gene assayInverse agonist activity at human H4R expressed in HEK293 cells co-expressing ELucC/ELucN-beta-arrestin2 assessed as inhibition of histamine-induced beta-arrestin recruitment by luciferase reporter gene assay
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1021/acs.jmedchem.0c00160
3035905 3804 None 32 Human Binding pIC50 = 6.3 6.3 -33 27
Inverse agonist activity at human H4R expressed in HEK293 cells co-expressing ELucC/ELucN-beta-arrestin2 assessed as inhibition of histamine-induced beta-arrestin recruitment by luciferase reporter gene assayInverse agonist activity at human H4R expressed in HEK293 cells co-expressing ELucC/ELucN-beta-arrestin2 assessed as inhibition of histamine-induced beta-arrestin recruitment by luciferase reporter gene assay
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1021/acs.jmedchem.0c00160
CHEMBL260374 3804 None 32 Human Binding pIC50 = 6.3 6.3 -33 27
Inverse agonist activity at human H4R expressed in HEK293 cells co-expressing ELucC/ELucN-beta-arrestin2 assessed as inhibition of histamine-induced beta-arrestin recruitment by luciferase reporter gene assayInverse agonist activity at human H4R expressed in HEK293 cells co-expressing ELucC/ELucN-beta-arrestin2 assessed as inhibition of histamine-induced beta-arrestin recruitment by luciferase reporter gene assay
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1021/acs.jmedchem.0c00160
89477709 182800 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Displacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting methodDisplacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting method
ChEMBL 301 1 1 7 0.9 Clc1cnc2nc(N3C[C@@H]4C[C@H]3CN4)c3nncn3c2c1 10.1021/acs.jmedchem.7b01855
CHEMBL4789385 182800 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Displacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting methodDisplacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting method
ChEMBL 301 1 1 7 0.9 Clc1cnc2nc(N3C[C@@H]4C[C@H]3CN4)c3nncn3c2c1 10.1021/acs.jmedchem.7b01855
71547597 183237 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Displacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting methodDisplacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting method
ChEMBL 283 1 0 7 0.7 Cc1cnc2nc(N3CCN(C)CC3)c3nncn3c2c1 10.1021/acs.jmedchem.7b01855
CHEMBL4795091 183237 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Displacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting methodDisplacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting method
ChEMBL 283 1 0 7 0.7 Cc1cnc2nc(N3CCN(C)CC3)c3nncn3c2c1 10.1021/acs.jmedchem.7b01855
71547848 183143 None 0 Human Binding pIC50 = 7.3 7.3 - 0
Displacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting methodDisplacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting method
ChEMBL 329 1 0 7 1.6 Clc1cnc2nc(N3CCN4CCCC4C3)c3nncn3c2c1 10.1021/acs.jmedchem.7b01855
CHEMBL4793974 183143 None 0 Human Binding pIC50 = 7.3 7.3 - 0
Displacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting methodDisplacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting method
ChEMBL 329 1 0 7 1.6 Clc1cnc2nc(N3CCN4CCCC4C3)c3nncn3c2c1 10.1021/acs.jmedchem.7b01855
71547765 182594 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Displacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting methodDisplacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting method
ChEMBL 347 3 0 8 1.5 CCOc1nc2nc(N3CCN(C)CC3)c3nncn3c2cc1Cl 10.1021/acs.jmedchem.7b01855
CHEMBL4786816 182594 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Displacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting methodDisplacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting method
ChEMBL 347 3 0 8 1.5 CCOc1nc2nc(N3CCN(C)CC3)c3nncn3c2cc1Cl 10.1021/acs.jmedchem.7b01855
71547682 182308 None 0 Human Binding pIC50 = 5.3 5.3 - 0
Displacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting methodDisplacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting method
ChEMBL 275 1 1 7 0.5 NC1CN(c2nc3ncc(Cl)cc3n3cnnc23)C1 10.1021/acs.jmedchem.7b01855
CHEMBL4782945 182308 None 0 Human Binding pIC50 = 5.3 5.3 - 0
Displacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting methodDisplacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting method
ChEMBL 275 1 1 7 0.5 NC1CN(c2nc3ncc(Cl)cc3n3cnnc23)C1 10.1021/acs.jmedchem.7b01855
89477439 182182 None 0 Human Binding pIC50 = 7.3 7.3 - 0
Displacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting methodDisplacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting method
ChEMBL 290 2 1 8 0.1 CNC1CN(c2nc3ncc(Cl)cc3n3nnnc23)C1 10.1021/acs.jmedchem.7b01855
CHEMBL4781484 182182 None 0 Human Binding pIC50 = 7.3 7.3 - 0
Displacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting methodDisplacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting method
ChEMBL 290 2 1 8 0.1 CNC1CN(c2nc3ncc(Cl)cc3n3nnnc23)C1 10.1021/acs.jmedchem.7b01855
58475282 181758 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Displacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting methodDisplacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting method
ChEMBL 282 1 0 6 1.3 Cc1ccc2nc(N3CCN(C)CC3)c3nncn3c2c1 10.1021/acs.jmedchem.7b01855
CHEMBL4776004 181758 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Displacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting methodDisplacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting method
ChEMBL 282 1 0 6 1.3 Cc1ccc2nc(N3CCN(C)CC3)c3nncn3c2c1 10.1021/acs.jmedchem.7b01855
71548411 182685 None 0 Human Binding pIC50 = 7.2 7.2 - 0
Displacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting methodDisplacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting method
ChEMBL 304 1 0 8 0.5 CN1CCN(c2nc3ncc(Cl)cc3n3nnnc23)CC1 10.1021/acs.jmedchem.7b01855
CHEMBL4787983 182685 None 0 Human Binding pIC50 = 7.2 7.2 - 0
Displacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting methodDisplacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting method
ChEMBL 304 1 0 8 0.5 CN1CCN(c2nc3ncc(Cl)cc3n3nnnc23)CC1 10.1021/acs.jmedchem.7b01855
53380276 182910 None 0 Human Binding pIC50 = 5.2 5.2 - 0
Displacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting methodDisplacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting method
ChEMBL 301 1 0 5 2.3 CN1CCN(c2cc3ccc(Cl)cc3n3cnnc23)CC1 10.1021/acs.jmedchem.7b01855
CHEMBL4790726 182910 None 0 Human Binding pIC50 = 5.2 5.2 - 0
Displacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting methodDisplacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting method
ChEMBL 301 1 0 5 2.3 CN1CCN(c2cc3ccc(Cl)cc3n3cnnc23)CC1 10.1021/acs.jmedchem.7b01855
46885181 8339 None 0 Human Binding pIC50 = 5.2 5.2 - 0
Displacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assayDisplacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assay
ChEMBL 293 2 1 6 2.0 CNC1CCN(c2ncnc3c2oc2ccc(C#N)cc23)C1 10.1016/j.bmcl.2010.02.097
CHEMBL1092880 8339 None 0 Human Binding pIC50 = 5.2 5.2 - 0
Displacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assayDisplacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assay
ChEMBL 293 2 1 6 2.0 CNC1CCN(c2ncnc3c2oc2ccc(C#N)cc23)C1 10.1016/j.bmcl.2010.02.097
89477539 182816 None 0 Human Binding pIC50 = 5.2 5.2 - 0
Displacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting methodDisplacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting method
ChEMBL 289 1 1 7 0.9 N[C@@H]1CCN(c2nc3ncc(Cl)cc3n3cnnc23)C1 10.1021/acs.jmedchem.7b01855
CHEMBL4789543 182816 None 0 Human Binding pIC50 = 5.2 5.2 - 0
Displacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting methodDisplacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting method
ChEMBL 289 1 1 7 0.9 N[C@@H]1CCN(c2nc3ncc(Cl)cc3n3cnnc23)C1 10.1021/acs.jmedchem.7b01855
71515465 182250 None 0 Human Binding pIC50 = 7.2 7.2 - 0
Displacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting methodDisplacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting method
ChEMBL 289 2 1 7 0.7 CNC1CN(c2nc3ncc(Cl)cc3n3cnnc23)C1 10.1021/acs.jmedchem.7b01855
CHEMBL4782303 182250 None 0 Human Binding pIC50 = 7.2 7.2 - 0
Displacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting methodDisplacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting method
ChEMBL 289 2 1 7 0.7 CNC1CN(c2nc3ncc(Cl)cc3n3cnnc23)C1 10.1021/acs.jmedchem.7b01855
71547683 181910 None 0 Human Binding pIC50 = 7.2 7.2 - 0
Displacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting methodDisplacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting method
ChEMBL 347 1 0 7 1.2 CN1CCN(c2nc3ncc(Br)cc3n3cnnc23)CC1 10.1021/acs.jmedchem.7b01855
CHEMBL4778068 181910 None 0 Human Binding pIC50 = 7.2 7.2 - 0
Displacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting methodDisplacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting method
ChEMBL 347 1 0 7 1.2 CN1CCN(c2nc3ncc(Br)cc3n3cnnc23)CC1 10.1021/acs.jmedchem.7b01855
CHEMBL5087167 217564 None 0 Mouse Binding pIC50 = 5.2 5.2 - 2
mBMMC chemotaxismBMMC chemotaxis
ChEMBL None None None Cn1cc2c(-c3c(-c4ccc(F)cn4)nn4c3COC(C)(C)C4)ccnc2n1 10.6019/CHEMBL5058645
89477445 182156 None 0 Human Binding pIC50 = 6.1 6.1 - 0
Displacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting methodDisplacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting method
ChEMBL 303 1 1 7 1.1 C[C@H]1CN(c2nc3ncc(Cl)cc3n3cnnc23)CCN1 10.1021/acs.jmedchem.7b01855
CHEMBL4781143 182156 None 0 Human Binding pIC50 = 6.1 6.1 - 0
Displacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting methodDisplacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting method
ChEMBL 303 1 1 7 1.1 C[C@H]1CN(c2nc3ncc(Cl)cc3n3cnnc23)CCN1 10.1021/acs.jmedchem.7b01855
71547678 183446 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Displacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting methodDisplacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting method
ChEMBL 303 1 0 7 1.1 CN1CCN(c2nc3ncc(Cl)cc3n3cnnc23)CC1 10.1021/acs.jmedchem.7b01855
CHEMBL4797517 183446 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Displacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting methodDisplacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting method
ChEMBL 303 1 0 7 1.1 CN1CCN(c2nc3ncc(Cl)cc3n3cnnc23)CC1 10.1021/acs.jmedchem.7b01855
24994634 2142 None 30 Mouse Binding pIC50 = 8.1 8.1 2 7
mBMMC chemotaxismBMMC chemotaxis
ChEMBL 221 2 2 5 0.7 N[C@@H]1CCN(C1)c1cc(nc(n1)N)C(C)C 10.6019/CHEMBL5058644
8984 2142 None 30 Mouse Binding pIC50 = 8.1 8.1 2 7
mBMMC chemotaxismBMMC chemotaxis
ChEMBL 221 2 2 5 0.7 N[C@@H]1CCN(C1)c1cc(nc(n1)N)C(C)C 10.6019/CHEMBL5058644
CHEMBL3236549 2142 None 30 Mouse Binding pIC50 = 8.1 8.1 2 7
mBMMC chemotaxismBMMC chemotaxis
ChEMBL 221 2 2 5 0.7 N[C@@H]1CCN(C1)c1cc(nc(n1)N)C(C)C 10.6019/CHEMBL5058644
11682208 8276 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Displacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assayDisplacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assay
ChEMBL 370 1 0 5 3.8 CN1CCN(c2nc(C(F)(F)F)nc3c2oc2ccc(Cl)cc23)CC1 10.1016/j.bmcl.2010.02.097
CHEMBL1092542 8276 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Displacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assayDisplacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assay
ChEMBL 370 1 0 5 3.8 CN1CCN(c2nc(C(F)(F)F)nc3c2oc2ccc(Cl)cc23)CC1 10.1016/j.bmcl.2010.02.097
46885177 8131 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Displacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assayDisplacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assay
ChEMBL 282 2 1 5 2.5 CN[C@@H]1CCN(c2ncnc3c2oc2ccc(C)cc23)C1 10.1016/j.bmcl.2010.02.097
CHEMBL1091729 8131 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Displacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assayDisplacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assay
ChEMBL 282 2 1 5 2.5 CN[C@@H]1CCN(c2ncnc3c2oc2ccc(C)cc23)C1 10.1016/j.bmcl.2010.02.097
1278 2150 None 56 Human Binding pIC50 = 7.1 7.1 -3 8
Inhibition of histamine H4 receptor-mediated chemotaxis in human eosinophilsInhibition of histamine H4 receptor-mediated chemotaxis in human eosinophils
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1016/j.ejmech.2012.06.016
1279 2150 None 56 Human Binding pIC50 = 7.1 7.1 -3 8
Inhibition of histamine H4 receptor-mediated chemotaxis in human eosinophilsInhibition of histamine H4 receptor-mediated chemotaxis in human eosinophils
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1016/j.ejmech.2012.06.016
4908365 2150 None 56 Human Binding pIC50 = 7.1 7.1 -3 8
Inhibition of histamine H4 receptor-mediated chemotaxis in human eosinophilsInhibition of histamine H4 receptor-mediated chemotaxis in human eosinophils
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1016/j.ejmech.2012.06.016
CHEMBL129198 2150 None 56 Human Binding pIC50 = 7.1 7.1 -3 8
Inhibition of histamine H4 receptor-mediated chemotaxis in human eosinophilsInhibition of histamine H4 receptor-mediated chemotaxis in human eosinophils
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1016/j.ejmech.2012.06.016
16656874 8108 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Displacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assayDisplacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assay
ChEMBL 288 2 1 5 2.4 CNC1CN(c2ncnc3c2oc2ccc(Cl)cc23)C1 10.1016/j.bmcl.2010.02.097
CHEMBL1091569 8108 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Displacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assayDisplacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assay
ChEMBL 288 2 1 5 2.4 CNC1CN(c2ncnc3c2oc2ccc(Cl)cc23)C1 10.1016/j.bmcl.2010.02.097
46885298 8418 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Displacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assayDisplacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assay
ChEMBL 332 2 0 6 2.8 COc1nc(N2CCN(C)CC2)c2oc3ccc(Cl)cc3c2n1 10.1016/j.bmcl.2010.02.097
CHEMBL1093439 8418 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Displacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assayDisplacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assay
ChEMBL 332 2 0 6 2.8 COc1nc(N2CCN(C)CC2)c2oc3ccc(Cl)cc3c2n1 10.1016/j.bmcl.2010.02.097
16656870 7723 None 0 Human Binding pIC50 = 7.0 7.0 - 0
Displacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assayDisplacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assay
ChEMBL 302 2 1 5 2.8 CNC1CCN(c2ncnc3c2oc2ccc(Cl)cc23)C1 10.1016/j.bmcl.2010.02.097
CHEMBL1088889 7723 None 0 Human Binding pIC50 = 7.0 7.0 - 0
Displacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assayDisplacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assay
ChEMBL 302 2 1 5 2.8 CNC1CCN(c2ncnc3c2oc2ccc(Cl)cc23)C1 10.1016/j.bmcl.2010.02.097
1278 2150 None 56 Human Binding pKd = 8 8.0 -3 8
pA2 value against histamine h4 receptorpA2 value against histamine h4 receptor
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1016/j.bmcl.2004.08.035
1279 2150 None 56 Human Binding pKd = 8 8.0 -3 8
pA2 value against histamine h4 receptorpA2 value against histamine h4 receptor
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1016/j.bmcl.2004.08.035
4908365 2150 None 56 Human Binding pKd = 8 8.0 -3 8
pA2 value against histamine h4 receptorpA2 value against histamine h4 receptor
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1016/j.bmcl.2004.08.035
CHEMBL129198 2150 None 56 Human Binding pKd = 8 8.0 -3 8
pA2 value against histamine h4 receptorpA2 value against histamine h4 receptor
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1016/j.bmcl.2004.08.035
71525681 89762 None 0 Human Binding pKd = 8.0 8.0 2 6
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells by competitive kinetic analysisDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells by competitive kinetic analysis
ChEMBL 298 3 2 6 1.7 CNC1CN(c2nc(N)nc3cc(C4CCCC4)cnc23)C1 10.1016/j.bmcl.2013.02.091
CHEMBL2376803 89762 None 0 Human Binding pKd = 8.0 8.0 2 6
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells by competitive kinetic analysisDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells by competitive kinetic analysis
ChEMBL 298 3 2 6 1.7 CNC1CN(c2nc(N)nc3cc(C4CCCC4)cnc23)C1 10.1016/j.bmcl.2013.02.091
11846300 80297 None 3 Human Binding pKd = 8.0 8.0 -2 4
Displacement of [3H]histamine from human histamine H4 receptor transfected in SK-N-MC cellsDisplacement of [3H]histamine from human histamine H4 receptor transfected in SK-N-MC cells
ChEMBL 327 0 0 4 3.8 CN1CCN(C2=Nc3ccc(Cl)cc3Oc3ccccc32)CC1 10.1021/jm051008s
CHEMBL213912 80297 None 3 Human Binding pKd = 8.0 8.0 -2 4
Displacement of [3H]histamine from human histamine H4 receptor transfected in SK-N-MC cellsDisplacement of [3H]histamine from human histamine H4 receptor transfected in SK-N-MC cells
ChEMBL 327 0 0 4 3.8 CN1CCN(C2=Nc3ccc(Cl)cc3Oc3ccccc32)CC1 10.1021/jm051008s
156013896 178345 None 0 Human Binding pKd = 8.0 8.0 -7 4
Binding affinity to human recombinant NLuc/GPCR-fused H4R expressed in HEK293T cells assessed as dissociation constant measured after 30 mins in presence of thioperamide by furimazine substrate based BRET assayBinding affinity to human recombinant NLuc/GPCR-fused H4R expressed in HEK293T cells assessed as dissociation constant measured after 30 mins in presence of thioperamide by furimazine substrate based BRET assay
ChEMBL 401 9 1 2 5.1 Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCCCc1c[nH]cn1 10.1021/acs.jmedchem.0c00160
CHEMBL4635634 178345 None 0 Human Binding pKd = 8.0 8.0 -7 4
Binding affinity to human recombinant NLuc/GPCR-fused H4R expressed in HEK293T cells assessed as dissociation constant measured after 30 mins in presence of thioperamide by furimazine substrate based BRET assayBinding affinity to human recombinant NLuc/GPCR-fused H4R expressed in HEK293T cells assessed as dissociation constant measured after 30 mins in presence of thioperamide by furimazine substrate based BRET assay
ChEMBL 401 9 1 2 5.1 Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCCCc1c[nH]cn1 10.1021/acs.jmedchem.0c00160
CHEMBL4650570 178345 None 0 Human Binding pKd = 8.0 8.0 -7 4
Binding affinity to human recombinant NLuc/GPCR-fused H4R expressed in HEK293T cells assessed as dissociation constant measured after 30 mins in presence of thioperamide by furimazine substrate based BRET assayBinding affinity to human recombinant NLuc/GPCR-fused H4R expressed in HEK293T cells assessed as dissociation constant measured after 30 mins in presence of thioperamide by furimazine substrate based BRET assay
ChEMBL 401 9 1 2 5.1 Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCCCc1c[nH]cn1 10.1021/acs.jmedchem.0c00160
135398737 958 None 57 Human Binding pKd = 7.9 7.9 -57 91
Displacement of [3H]histamine from human histamine H4 receptor transfected in SK-N-MC cellsDisplacement of [3H]histamine from human histamine H4 receptor transfected in SK-N-MC cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm051008s
135398737.0 958 None 57 Human Binding pKd = 7.9 7.9 -57 91
Displacement of [3H]histamine from human histamine H4 receptor transfected in SK-N-MC cellsDisplacement of [3H]histamine from human histamine H4 receptor transfected in SK-N-MC cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm051008s
38 958 None 57 Human Binding pKd = 7.9 7.9 -57 91
Displacement of [3H]histamine from human histamine H4 receptor transfected in SK-N-MC cellsDisplacement of [3H]histamine from human histamine H4 receptor transfected in SK-N-MC cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm051008s
722 958 None 57 Human Binding pKd = 7.9 7.9 -57 91
Displacement of [3H]histamine from human histamine H4 receptor transfected in SK-N-MC cellsDisplacement of [3H]histamine from human histamine H4 receptor transfected in SK-N-MC cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm051008s
CHEMBL42 958 None 57 Human Binding pKd = 7.9 7.9 -57 91
Displacement of [3H]histamine from human histamine H4 receptor transfected in SK-N-MC cellsDisplacement of [3H]histamine from human histamine H4 receptor transfected in SK-N-MC cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm051008s
DB00363 958 None 57 Human Binding pKd = 7.9 7.9 -57 91
Displacement of [3H]histamine from human histamine H4 receptor transfected in SK-N-MC cellsDisplacement of [3H]histamine from human histamine H4 receptor transfected in SK-N-MC cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm051008s
24994634 2142 None 30 Human Binding pKd = 7.9 7.9 -2 7
Cell based cAMP Assays (pA2)Cell based cAMP Assays (pA2)
ChEMBL 221 2 2 5 0.7 N[C@@H]1CCN(C1)c1cc(nc(n1)N)C(C)C 10.6019/CHEMBL5058644
8984 2142 None 30 Human Binding pKd = 7.9 7.9 -2 7
Cell based cAMP Assays (pA2)Cell based cAMP Assays (pA2)
ChEMBL 221 2 2 5 0.7 N[C@@H]1CCN(C1)c1cc(nc(n1)N)C(C)C 10.6019/CHEMBL5058644
CHEMBL3236549 2142 None 30 Human Binding pKd = 7.9 7.9 -2 7
Cell based cAMP Assays (pA2)Cell based cAMP Assays (pA2)
ChEMBL 221 2 2 5 0.7 N[C@@H]1CCN(C1)c1cc(nc(n1)N)C(C)C 10.6019/CHEMBL5058644
11846300 80297 None 3 Human Binding pKd = 7.9 7.9 -2 4
Displacement of [3H]histamine from human histamine H4 receptor transfected in SK-N-MC cells at 10 nMDisplacement of [3H]histamine from human histamine H4 receptor transfected in SK-N-MC cells at 10 nM
ChEMBL 327 0 0 4 3.8 CN1CCN(C2=Nc3ccc(Cl)cc3Oc3ccccc32)CC1 10.1021/jm051008s
CHEMBL213912 80297 None 3 Human Binding pKd = 7.9 7.9 -2 4
Displacement of [3H]histamine from human histamine H4 receptor transfected in SK-N-MC cells at 10 nMDisplacement of [3H]histamine from human histamine H4 receptor transfected in SK-N-MC cells at 10 nM
ChEMBL 327 0 0 4 3.8 CN1CCN(C2=Nc3ccc(Cl)cc3Oc3ccccc32)CC1 10.1021/jm051008s
71519674 89763 None 0 Human Binding pKd = 7.9 7.9 1 5
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells by competitive kinetic analysisDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells by competitive kinetic analysis
ChEMBL 270 3 2 6 0.9 CNC1CN(c2nc(N)nc3cc(C4CC4)cnc23)C1 10.1016/j.bmcl.2013.02.091
CHEMBL2376804 89763 None 0 Human Binding pKd = 7.9 7.9 1 5
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells by competitive kinetic analysisDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells by competitive kinetic analysis
ChEMBL 270 3 2 6 0.9 CNC1CN(c2nc(N)nc3cc(C4CC4)cnc23)C1 10.1016/j.bmcl.2013.02.091
1204 1932 None 74 Rat Binding pKd = 6.9 6.9 -12 24
Binding affinity to rat H4RBinding affinity to rat H4R
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.9b01342
1247 1932 None 74 Rat Binding pKd = 6.9 6.9 -12 24
Binding affinity to rat H4RBinding affinity to rat H4R
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.9b01342
1375 1932 None 74 Rat Binding pKd = 6.9 6.9 -12 24
Binding affinity to rat H4RBinding affinity to rat H4R
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.9b01342
774 1932 None 74 Rat Binding pKd = 6.9 6.9 -12 24
Binding affinity to rat H4RBinding affinity to rat H4R
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.9b01342
774.0 1932 None 74 Rat Binding pKd = 6.9 6.9 -12 24
Binding affinity to rat H4RBinding affinity to rat H4R
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.9b01342
CHEMBL90 1932 None 74 Rat Binding pKd = 6.9 6.9 -12 24
Binding affinity to rat H4RBinding affinity to rat H4R
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.9b01342
DB05381 1932 None 74 Rat Binding pKd = 6.9 6.9 -12 24
Binding affinity to rat H4RBinding affinity to rat H4R
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.9b01342
135398737 958 None 57 Human Binding pKd = 7.8 7.8 -57 91
Displacement of [3H]Histamine from human histamine H4 receptor transfected in SK-N-MC cells at 100 nMDisplacement of [3H]Histamine from human histamine H4 receptor transfected in SK-N-MC cells at 100 nM
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm051008s
135398737.0 958 None 57 Human Binding pKd = 7.8 7.8 -57 91
Displacement of [3H]Histamine from human histamine H4 receptor transfected in SK-N-MC cells at 100 nMDisplacement of [3H]Histamine from human histamine H4 receptor transfected in SK-N-MC cells at 100 nM
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm051008s
38 958 None 57 Human Binding pKd = 7.8 7.8 -57 91
Displacement of [3H]Histamine from human histamine H4 receptor transfected in SK-N-MC cells at 100 nMDisplacement of [3H]Histamine from human histamine H4 receptor transfected in SK-N-MC cells at 100 nM
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm051008s
722 958 None 57 Human Binding pKd = 7.8 7.8 -57 91
Displacement of [3H]Histamine from human histamine H4 receptor transfected in SK-N-MC cells at 100 nMDisplacement of [3H]Histamine from human histamine H4 receptor transfected in SK-N-MC cells at 100 nM
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm051008s
CHEMBL42 958 None 57 Human Binding pKd = 7.8 7.8 -57 91
Displacement of [3H]Histamine from human histamine H4 receptor transfected in SK-N-MC cells at 100 nMDisplacement of [3H]Histamine from human histamine H4 receptor transfected in SK-N-MC cells at 100 nM
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm051008s
DB00363 958 None 57 Human Binding pKd = 7.8 7.8 -57 91
Displacement of [3H]Histamine from human histamine H4 receptor transfected in SK-N-MC cells at 100 nMDisplacement of [3H]Histamine from human histamine H4 receptor transfected in SK-N-MC cells at 100 nM
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm051008s
155513612 176425 None 0 Mouse Binding pKd = 7.8 7.8 -1 4
Binding affinity to mouse H4R expressed in HEK293T-SF-His6-CRE-Luc cells by saturation binding studyBinding affinity to mouse H4R expressed in HEK293T-SF-His6-CRE-Luc cells by saturation binding study
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 176425 None 0 Mouse Binding pKd = 7.8 7.8 -1 4
Binding affinity to mouse H4R expressed in HEK293T-SF-His6-CRE-Luc cells by saturation binding studyBinding affinity to mouse H4R expressed in HEK293T-SF-His6-CRE-Luc cells by saturation binding study
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 176425 None 0 Mouse Binding pKd = 7.8 7.8 -1 4
Binding affinity to mouse H4R expressed in HEK293T-SF-His6-CRE-Luc cells by saturation binding studyBinding affinity to mouse H4R expressed in HEK293T-SF-His6-CRE-Luc cells by saturation binding study
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 176425 None 0 Mouse Binding pKd = 7.8 7.8 -1 4
Binding affinity to mouse H4R expressed in HEK293T-SF-His6-CRE-Luc cells by saturation binding studyBinding affinity to mouse H4R expressed in HEK293T-SF-His6-CRE-Luc cells by saturation binding study
ChEMBL 277 4 1 5 2.1 CN(C)[C@@H]1CCN(c2ccnc(NCC(C)(C)C)n2)C1 10.1021/acs.jmedchem.9b01342
156015638 178377 None 0 Mouse Binding pKd = 6.8 6.8 -158 4
Binding affinity to mouse recombinant NLuc/GPCR-fused H4R expressed in HEK293T cells measured after 30 mins by furimazine substrate based BRET assayBinding affinity to mouse recombinant NLuc/GPCR-fused H4R expressed in HEK293T cells measured after 30 mins by furimazine substrate based BRET assay
ChEMBL 415 10 1 2 5.5 Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCCCCc1c[nH]cn1 10.1021/acs.jmedchem.0c00160
CHEMBL4642520 178377 None 0 Mouse Binding pKd = 6.8 6.8 -158 4
Binding affinity to mouse recombinant NLuc/GPCR-fused H4R expressed in HEK293T cells measured after 30 mins by furimazine substrate based BRET assayBinding affinity to mouse recombinant NLuc/GPCR-fused H4R expressed in HEK293T cells measured after 30 mins by furimazine substrate based BRET assay
ChEMBL 415 10 1 2 5.5 Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCCCCc1c[nH]cn1 10.1021/acs.jmedchem.0c00160
CHEMBL4650832 178377 None 0 Mouse Binding pKd = 6.8 6.8 -158 4
Binding affinity to mouse recombinant NLuc/GPCR-fused H4R expressed in HEK293T cells measured after 30 mins by furimazine substrate based BRET assayBinding affinity to mouse recombinant NLuc/GPCR-fused H4R expressed in HEK293T cells measured after 30 mins by furimazine substrate based BRET assay
ChEMBL 415 10 1 2 5.5 Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCCCCc1c[nH]cn1 10.1021/acs.jmedchem.0c00160
1204 1932 None 74 Human Binding pKd = 7.8 7.8 -3 24
Displacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.1c00692
1247 1932 None 74 Human Binding pKd = 7.8 7.8 -3 24
Displacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.1c00692
1375 1932 None 74 Human Binding pKd = 7.8 7.8 -3 24
Displacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.1c00692
774 1932 None 74 Human Binding pKd = 7.8 7.8 -3 24
Displacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.1c00692
774.0 1932 None 74 Human Binding pKd = 7.8 7.8 -3 24
Displacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.1c00692
CHEMBL90 1932 None 74 Human Binding pKd = 7.8 7.8 -3 24
Displacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.1c00692
DB05381 1932 None 74 Human Binding pKd = 7.8 7.8 -3 24
Displacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.1c00692
119570 3159 None 58 Human Binding pKd = 7.8 7.8 -301 40
Displacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1021/acs.jmedchem.1c00692
119570.0 3159 None 58 Human Binding pKd = 7.8 7.8 -301 40
Displacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1021/acs.jmedchem.1c00692
2233 3159 None 58 Human Binding pKd = 7.8 7.8 -301 40
Displacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1021/acs.jmedchem.1c00692
953 3159 None 58 Human Binding pKd = 7.8 7.8 -301 40
Displacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1021/acs.jmedchem.1c00692
CHEMBL301265 3159 None 58 Human Binding pKd = 7.8 7.8 -301 40
Displacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1021/acs.jmedchem.1c00692
DB00413 3159 None 58 Human Binding pKd = 7.8 7.8 -301 40
Displacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1021/acs.jmedchem.1c00692
168268716 192871 None 0 Human Binding pKd = 7.8 7.8 -3 4
Displacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis
ChEMBL 372 3 4 4 3.5 Cc1nc(N)sc1-c1ccc(N/C(N)=N/C(=O)NC2CCCCC2)cc1 10.1021/acs.jmedchem.1c00692
CHEMBL5170276 192871 None 0 Human Binding pKd = 7.8 7.8 -3 4
Displacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis
ChEMBL 372 3 4 4 3.5 Cc1nc(N)sc1-c1ccc(N/C(N)=N/C(=O)NC2CCCCC2)cc1 10.1021/acs.jmedchem.1c00692
CHEMBL5221176 192871 None 0 Human Binding pKd = 7.8 7.8 -3 4
Displacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis
ChEMBL 372 3 4 4 3.5 Cc1nc(N)sc1-c1ccc(N/C(N)=N/C(=O)NC2CCCCC2)cc1 10.1021/acs.jmedchem.1c00692
168268680 192875 None 0 Human Binding pKd = 7.8 7.8 -2 4
Displacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis
ChEMBL 662 11 8 8 4.8 Cc1nc(N)sc1-c1ccc(N/C(N)=N/C(=O)NCCCCCCNC(=O)/N=C(\N)Nc2ccc(-c3sc(N)nc3C)cc2)cc1 10.1021/acs.jmedchem.1c00692
CHEMBL5172675 192875 None 0 Human Binding pKd = 7.8 7.8 -2 4
Displacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis
ChEMBL 662 11 8 8 4.8 Cc1nc(N)sc1-c1ccc(N/C(N)=N/C(=O)NCCCCCCNC(=O)/N=C(\N)Nc2ccc(-c3sc(N)nc3C)cc2)cc1 10.1021/acs.jmedchem.1c00692
CHEMBL5221210 192875 None 0 Human Binding pKd = 7.8 7.8 -2 4
Displacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis
ChEMBL 662 11 8 8 4.8 Cc1nc(N)sc1-c1ccc(N/C(N)=N/C(=O)NCCCCCCNC(=O)/N=C(\N)Nc2ccc(-c3sc(N)nc3C)cc2)cc1 10.1021/acs.jmedchem.1c00692
168268827 192888 None 0 Human Binding pKd = 7.8 7.8 -6 4
Displacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis
ChEMBL 450 8 4 4 4.8 Cc1nc(N)sc1-c1cccc(N/C(N)=N/C(=O)NCC(C)CCCc2ccccc2)c1 10.1021/acs.jmedchem.1c00692
CHEMBL5179906 192888 None 0 Human Binding pKd = 7.8 7.8 -6 4
Displacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis
ChEMBL 450 8 4 4 4.8 Cc1nc(N)sc1-c1cccc(N/C(N)=N/C(=O)NCC(C)CCCc2ccccc2)c1 10.1021/acs.jmedchem.1c00692
CHEMBL5221314 192888 None 0 Human Binding pKd = 7.8 7.8 -6 4
Displacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis
ChEMBL 450 8 4 4 4.8 Cc1nc(N)sc1-c1cccc(N/C(N)=N/C(=O)NCC(C)CCCc2ccccc2)c1 10.1021/acs.jmedchem.1c00692
168268853 192894 None 0 Human Binding pKd = 7.8 7.8 -83 6
Displacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis
ChEMBL 389 8 4 5 1.9 Cc1ccc(CC(C)CNC(=O)/N=C(\N)NCCCc2nnc(N)s2)cc1 10.1021/acs.jmedchem.1c00692
CHEMBL5180504 192894 None 0 Human Binding pKd = 7.8 7.8 -83 6
Displacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis
ChEMBL 389 8 4 5 1.9 Cc1ccc(CC(C)CNC(=O)/N=C(\N)NCCCc2nnc(N)s2)cc1 10.1021/acs.jmedchem.1c00692
CHEMBL5221353 192894 None 0 Human Binding pKd = 7.8 7.8 -83 6
Displacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis
ChEMBL 389 8 4 5 1.9 Cc1ccc(CC(C)CNC(=O)/N=C(\N)NCCCc2nnc(N)s2)cc1 10.1021/acs.jmedchem.1c00692
168273471 192910 None 0 Human Binding pKd = 7.8 7.8 -50 4
Displacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis
ChEMBL 596 17 8 10 0.7 N/C(=N\C(=O)NCCCCCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5173079 192910 None 0 Human Binding pKd = 7.8 7.8 -50 4
Displacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis
ChEMBL 596 17 8 10 0.7 N/C(=N\C(=O)NCCCCCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5221433 192910 None 0 Human Binding pKd = 7.8 7.8 -50 4
Displacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis
ChEMBL 596 17 8 10 0.7 N/C(=N\C(=O)NCCCCCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
168273549 192912 None 0 Human Binding pKd = 7.8 7.8 -5 4
Displacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis
ChEMBL 436 6 4 4 4.3 Cc1ccc(CC(C)CNC(=O)/N=C(\N)Nc2ccc(-c3sc(N)nc3C)cc2)cc1 10.1021/acs.jmedchem.1c00692
CHEMBL5174342 192912 None 0 Human Binding pKd = 7.8 7.8 -5 4
Displacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis
ChEMBL 436 6 4 4 4.3 Cc1ccc(CC(C)CNC(=O)/N=C(\N)Nc2ccc(-c3sc(N)nc3C)cc2)cc1 10.1021/acs.jmedchem.1c00692
CHEMBL5221438 192912 None 0 Human Binding pKd = 7.8 7.8 -5 4
Displacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis
ChEMBL 436 6 4 4 4.3 Cc1ccc(CC(C)CNC(=O)/N=C(\N)Nc2ccc(-c3sc(N)nc3C)cc2)cc1 10.1021/acs.jmedchem.1c00692
168273640 192914 None 0 Human Binding pKd = 7.8 7.8 -12 6
Displacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis
ChEMBL 568 15 8 10 -0.1 N/C(=N\C(=O)NCCCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5176229 192914 None 0 Human Binding pKd = 7.8 7.8 -12 6
Displacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis
ChEMBL 568 15 8 10 -0.1 N/C(=N\C(=O)NCCCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5221444 192914 None 0 Human Binding pKd = 7.8 7.8 -12 6
Displacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis
ChEMBL 568 15 8 10 -0.1 N/C(=N\C(=O)NCCCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
168273745 192917 None 0 Human Binding pKd = 7.8 7.8 -11 6
Displacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis
ChEMBL 332 6 4 4 1.5 N/C(=N\C(=O)NCc1ccccc1)NCCCc1cnc(N)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5178472 192917 None 0 Human Binding pKd = 7.8 7.8 -11 6
Displacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis
ChEMBL 332 6 4 4 1.5 N/C(=N\C(=O)NCc1ccccc1)NCCCc1cnc(N)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5221451 192917 None 0 Human Binding pKd = 7.8 7.8 -11 6
Displacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis
ChEMBL 332 6 4 4 1.5 N/C(=N\C(=O)NCc1ccccc1)NCCCc1cnc(N)s1 10.1021/acs.jmedchem.1c00692
168274129 192918 None 0 Human Binding pKd = 7.8 7.8 -5 4
Displacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis
ChEMBL 370 12 5 6 1.0 NCCCCCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5176780 192918 None 0 Human Binding pKd = 7.8 7.8 -5 4
Displacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis
ChEMBL 370 12 5 6 1.0 NCCCCCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5221468 192918 None 0 Human Binding pKd = 7.8 7.8 -5 4
Displacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis
ChEMBL 370 12 5 6 1.0 NCCCCCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
168275750 192935 None 0 Human Binding pKd = 7.8 7.8 -5 4
Displacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis
ChEMBL 332 6 3 4 1.6 Cc1nnc(CCCN/C(N)=N/C(=O)NCc2ccccc2)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5175558 192935 None 0 Human Binding pKd = 7.8 7.8 -5 4
Displacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis
ChEMBL 332 6 3 4 1.6 Cc1nnc(CCCN/C(N)=N/C(=O)NCc2ccccc2)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5221581 192935 None 0 Human Binding pKd = 7.8 7.8 -5 4
Displacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis
ChEMBL 332 6 3 4 1.6 Cc1nnc(CCCN/C(N)=N/C(=O)NCc2ccccc2)s1 10.1021/acs.jmedchem.1c00692
168276867 192944 None 0 Human Binding pKd = 7.8 7.8 -4 4
Displacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis
ChEMBL 662 11 8 8 4.8 Cc1nc(N)sc1-c1cccc(N/C(N)=N/C(=O)NCCCCCCNC(=O)/N=C(\N)Nc2cccc(-c3sc(N)nc3C)c2)c1 10.1021/acs.jmedchem.1c00692
CHEMBL5174278 192944 None 0 Human Binding pKd = 7.8 7.8 -4 4
Displacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis
ChEMBL 662 11 8 8 4.8 Cc1nc(N)sc1-c1cccc(N/C(N)=N/C(=O)NCCCCCCNC(=O)/N=C(\N)Nc2cccc(-c3sc(N)nc3C)c2)c1 10.1021/acs.jmedchem.1c00692
CHEMBL5221653 192944 None 0 Human Binding pKd = 7.8 7.8 -4 4
Displacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis
ChEMBL 662 11 8 8 4.8 Cc1nc(N)sc1-c1cccc(N/C(N)=N/C(=O)NCCCCCCNC(=O)/N=C(\N)Nc2cccc(-c3sc(N)nc3C)c2)c1 10.1021/acs.jmedchem.1c00692
168277996 192955 None 0 Human Binding pKd = 7.8 7.8 -5 4
Displacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis
ChEMBL 380 4 4 4 3.3 Cc1nc(N)sc1-c1cccc(N/C(N)=N/C(=O)NCc2ccccc2)c1 10.1021/acs.jmedchem.1c00692
CHEMBL5173373 192955 None 0 Human Binding pKd = 7.8 7.8 -5 4
Displacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis
ChEMBL 380 4 4 4 3.3 Cc1nc(N)sc1-c1cccc(N/C(N)=N/C(=O)NCc2ccccc2)c1 10.1021/acs.jmedchem.1c00692
CHEMBL5221736 192955 None 0 Human Binding pKd = 7.8 7.8 -5 4
Displacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis
ChEMBL 380 4 4 4 3.3 Cc1nc(N)sc1-c1cccc(N/C(N)=N/C(=O)NCc2ccccc2)c1 10.1021/acs.jmedchem.1c00692
168278471 192957 None 0 Human Binding pKd = 7.8 7.8 -17 6
Displacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis
ChEMBL 312 8 4 4 1.5 CCCCCNC(=O)/N=C(\N)NCCCc1cnc(N)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5183205 192957 None 0 Human Binding pKd = 7.8 7.8 -17 6
Displacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis
ChEMBL 312 8 4 4 1.5 CCCCCNC(=O)/N=C(\N)NCCCc1cnc(N)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5221757 192957 None 0 Human Binding pKd = 7.8 7.8 -17 6
Displacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis
ChEMBL 312 8 4 4 1.5 CCCCCNC(=O)/N=C(\N)NCCCc1cnc(N)s1 10.1021/acs.jmedchem.1c00692
168278543 192960 None 0 Human Binding pKd = 7.8 7.8 -4 4
Displacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis
ChEMBL 358 4 4 4 1.6 N/C(=N\C(=O)NCc1ccccc1)NCC1CCc2nc(N)sc2C1 10.1021/acs.jmedchem.1c00692
CHEMBL5184846 192960 None 0 Human Binding pKd = 7.8 7.8 -4 4
Displacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis
ChEMBL 358 4 4 4 1.6 N/C(=N\C(=O)NCc1ccccc1)NCC1CCc2nc(N)sc2C1 10.1021/acs.jmedchem.1c00692
CHEMBL5221764 192960 None 0 Human Binding pKd = 7.8 7.8 -4 4
Displacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis
ChEMBL 358 4 4 4 1.6 N/C(=N\C(=O)NCc1ccccc1)NCC1CCc2nc(N)sc2C1 10.1021/acs.jmedchem.1c00692
168280339 192974 None 0 Human Binding pKd = 7.8 7.8 -3 4
Displacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis
ChEMBL 372 8 3 5 1.1 C[C@@H](NC(=O)/N=C(\N)NCCCn1cc(CN(C)C)nn1)c1ccccc1 10.1021/acs.jmedchem.1c00692
CHEMBL5188592 192974 None 0 Human Binding pKd = 7.8 7.8 -3 4
Displacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis
ChEMBL 372 8 3 5 1.1 C[C@@H](NC(=O)/N=C(\N)NCCCn1cc(CN(C)C)nn1)c1ccccc1 10.1021/acs.jmedchem.1c00692
CHEMBL5221885 192974 None 0 Human Binding pKd = 7.8 7.8 -3 4
Displacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis
ChEMBL 372 8 3 5 1.1 C[C@@H](NC(=O)/N=C(\N)NCCCn1cc(CN(C)C)nn1)c1ccccc1 10.1021/acs.jmedchem.1c00692
168281536 192990 None 0 Human Binding pKd = 7.8 7.8 2 4
Displacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis
ChEMBL 369 12 4 5 1.7 Cc1nnc(CCCN/C(N)=N/C(=O)NCCCCCCCCN)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5189006 192990 None 0 Human Binding pKd = 7.8 7.8 2 4
Displacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis
ChEMBL 369 12 4 5 1.7 Cc1nnc(CCCN/C(N)=N/C(=O)NCCCCCCCCN)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5221966 192990 None 0 Human Binding pKd = 7.8 7.8 2 4
Displacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis
ChEMBL 369 12 4 5 1.7 Cc1nnc(CCCN/C(N)=N/C(=O)NCCCCCCCCN)s1 10.1021/acs.jmedchem.1c00692
168281746 192991 None 0 Human Binding pKd = 7.8 7.8 -1071 6
Displacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis
ChEMBL 365 6 4 5 1.6 CC(NC(=O)/N=C(\N)NCCCc1nnc(N)s1)c1cccc(F)c1 10.1021/acs.jmedchem.1c00692
CHEMBL5184911 192991 None 0 Human Binding pKd = 7.8 7.8 -1071 6
Displacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis
ChEMBL 365 6 4 5 1.6 CC(NC(=O)/N=C(\N)NCCCc1nnc(N)s1)c1cccc(F)c1 10.1021/acs.jmedchem.1c00692
CHEMBL5221974 192991 None 0 Human Binding pKd = 7.8 7.8 -1071 6
Displacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis
ChEMBL 365 6 4 5 1.6 CC(NC(=O)/N=C(\N)NCCCc1nnc(N)s1)c1cccc(F)c1 10.1021/acs.jmedchem.1c00692
168283097 193002 None 0 Human Binding pKd = 7.8 7.8 -5 4
Displacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis
ChEMBL 311 9 4 5 0.8 CCCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)o1 10.1021/acs.jmedchem.1c00692
CHEMBL5186770 193002 None 0 Human Binding pKd = 7.8 7.8 -5 4
Displacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis
ChEMBL 311 9 4 5 0.8 CCCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)o1 10.1021/acs.jmedchem.1c00692
CHEMBL5222043 193002 None 0 Human Binding pKd = 7.8 7.8 -5 4
Displacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis
ChEMBL 311 9 4 5 0.8 CCCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)o1 10.1021/acs.jmedchem.1c00692
168283321 193004 None 0 Human Binding pKd = 7.8 7.8 -6 4
Displacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis
ChEMBL 364 7 4 4 2.3 Cc1nc(N)oc1CCCN/C(N)=N/C(=O)NCC(C)C1CCCCC1 10.1021/acs.jmedchem.1c00692
CHEMBL5183015 193004 None 0 Human Binding pKd = 7.8 7.8 -6 4
Displacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis
ChEMBL 364 7 4 4 2.3 Cc1nc(N)oc1CCCN/C(N)=N/C(=O)NCC(C)C1CCCCC1 10.1021/acs.jmedchem.1c00692
CHEMBL5222057 193004 None 0 Human Binding pKd = 7.8 7.8 -6 4
Displacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis
ChEMBL 364 7 4 4 2.3 Cc1nc(N)oc1CCCN/C(N)=N/C(=O)NCC(C)C1CCCCC1 10.1021/acs.jmedchem.1c00692
168283536 193009 None 0 Human Binding pKd = 7.8 7.8 -5 4
Displacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis
ChEMBL 312 8 3 4 1.6 CCCCCNC(=O)/N=C(/N)NCCCc1nnc(C)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5187758 193009 None 0 Human Binding pKd = 7.8 7.8 -5 4
Displacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis
ChEMBL 312 8 3 4 1.6 CCCCCNC(=O)/N=C(/N)NCCCc1nnc(C)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5222074 193009 None 0 Human Binding pKd = 7.8 7.8 -5 4
Displacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis
ChEMBL 312 8 3 4 1.6 CCCCCNC(=O)/N=C(/N)NCCCc1nnc(C)s1 10.1021/acs.jmedchem.1c00692
168284289 193015 None 0 Human Binding pKd = 7.8 7.8 -7 4
Displacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis
ChEMBL 428 8 4 4 3.1 CC(CCCc1ccccc1)CNC(=O)/N=C(\N)NCC1CCc2nc(N)sc2C1 10.1021/acs.jmedchem.1c00692
CHEMBL5194860 193015 None 0 Human Binding pKd = 7.8 7.8 -7 4
Displacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis
ChEMBL 428 8 4 4 3.1 CC(CCCc1ccccc1)CNC(=O)/N=C(\N)NCC1CCc2nc(N)sc2C1 10.1021/acs.jmedchem.1c00692
CHEMBL5222123 193015 None 0 Human Binding pKd = 7.8 7.8 -7 4
Displacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis
ChEMBL 428 8 4 4 3.1 CC(CCCc1ccccc1)CNC(=O)/N=C(\N)NCC1CCc2nc(N)sc2C1 10.1021/acs.jmedchem.1c00692
168284480 193019 None 0 Human Binding pKd = 7.8 7.8 -5 4
Displacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis
ChEMBL 330 6 4 4 1.3 Cc1nc(N)oc1CCCN/C(N)=N/C(=O)NCc1ccccc1 10.1021/acs.jmedchem.1c00692
CHEMBL5197548 193019 None 0 Human Binding pKd = 7.8 7.8 -5 4
Displacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis
ChEMBL 330 6 4 4 1.3 Cc1nc(N)oc1CCCN/C(N)=N/C(=O)NCc1ccccc1 10.1021/acs.jmedchem.1c00692
CHEMBL5222137 193019 None 0 Human Binding pKd = 7.8 7.8 -5 4
Displacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis
ChEMBL 330 6 4 4 1.3 Cc1nc(N)oc1CCCN/C(N)=N/C(=O)NCc1ccccc1 10.1021/acs.jmedchem.1c00692
168286141 193033 None 0 Human Binding pKd = 7.8 7.8 -5 4
Displacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis
ChEMBL 450 8 4 4 4.8 Cc1nc(N)sc1-c1ccc(N/C(N)=N/C(=O)NCC(C)CCCc2ccccc2)cc1 10.1021/acs.jmedchem.1c00692
CHEMBL5192993 193033 None 0 Human Binding pKd = 7.8 7.8 -5 4
Displacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis
ChEMBL 450 8 4 4 4.8 Cc1nc(N)sc1-c1ccc(N/C(N)=N/C(=O)NCC(C)CCCc2ccccc2)cc1 10.1021/acs.jmedchem.1c00692
CHEMBL5222231 193033 None 0 Human Binding pKd = 7.8 7.8 -5 4
Displacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis
ChEMBL 450 8 4 4 4.8 Cc1nc(N)sc1-c1ccc(N/C(N)=N/C(=O)NCC(C)CCCc2ccccc2)cc1 10.1021/acs.jmedchem.1c00692
168286426 193035 None 0 Human Binding pKd = 7.8 7.8 -109 6
Displacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis
ChEMBL 403 10 4 5 2.3 CC(CCCc1ccccc1)CNC(=O)/N=C(\N)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5198795 193035 None 0 Human Binding pKd = 7.8 7.8 -109 6
Displacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis
ChEMBL 403 10 4 5 2.3 CC(CCCc1ccccc1)CNC(=O)/N=C(\N)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5222241 193035 None 0 Human Binding pKd = 7.8 7.8 -109 6
Displacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis
ChEMBL 403 10 4 5 2.3 CC(CCCc1ccccc1)CNC(=O)/N=C(\N)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
168290235 193077 None 0 Human Binding pKd = 7.8 7.8 -1071 20
Displacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis
ChEMBL 315 6 4 3 1.1 C[C@@H](NC(=O)/N=C(\N)NCCCc1ncn[nH]1)c1ccccc1 10.1021/acs.jmedchem.1c00692
CHEMBL5201074 193077 None 0 Human Binding pKd = 7.8 7.8 -1071 20
Displacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis
ChEMBL 315 6 4 3 1.1 C[C@@H](NC(=O)/N=C(\N)NCCCc1ncn[nH]1)c1ccccc1 10.1021/acs.jmedchem.1c00692
CHEMBL5222491 193077 None 0 Human Binding pKd = 7.8 7.8 -1071 20
Displacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis
ChEMBL 315 6 4 3 1.1 C[C@@H](NC(=O)/N=C(\N)NCCCc1ncn[nH]1)c1ccccc1 10.1021/acs.jmedchem.1c00692
168290815 193082 None 0 Human Binding pKd = 7.8 7.8 -1071 6
Displacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis
ChEMBL 327 9 4 5 1.2 CCCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5200771 193082 None 0 Human Binding pKd = 7.8 7.8 -1071 6
Displacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis
ChEMBL 327 9 4 5 1.2 CCCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5222529 193082 None 0 Human Binding pKd = 7.8 7.8 -1071 6
Displacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis
ChEMBL 327 9 4 5 1.2 CCCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
168291233 193088 None 0 Human Binding pKd = 7.8 7.8 5 4
Displacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis
ChEMBL 373 8 4 5 1.4 Cc1ccc(CC(C)CNC(=O)/N=C(\N)NCCCc2nnc(N)o2)cc1 10.1021/acs.jmedchem.1c00692
CHEMBL5200106 193088 None 0 Human Binding pKd = 7.8 7.8 5 4
Displacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis
ChEMBL 373 8 4 5 1.4 Cc1ccc(CC(C)CNC(=O)/N=C(\N)NCCCc2nnc(N)o2)cc1 10.1021/acs.jmedchem.1c00692
CHEMBL5222556 193088 None 0 Human Binding pKd = 7.8 7.8 5 4
Displacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis
ChEMBL 373 8 4 5 1.4 Cc1ccc(CC(C)CNC(=O)/N=C(\N)NCCCc2nnc(N)o2)cc1 10.1021/acs.jmedchem.1c00692
168292954 193106 None 0 Human Binding pKd = 7.8 7.8 -112 6
Displacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis
ChEMBL 388 8 4 4 2.5 Cc1ccc(CC(C)CNC(=O)/N=C(\N)NCCCc2cnc(N)s2)cc1 10.1021/acs.jmedchem.1c00692
CHEMBL5202592 193106 None 0 Human Binding pKd = 7.8 7.8 -112 6
Displacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis
ChEMBL 388 8 4 4 2.5 Cc1ccc(CC(C)CNC(=O)/N=C(\N)NCCCc2cnc(N)s2)cc1 10.1021/acs.jmedchem.1c00692
CHEMBL5222660 193106 None 0 Human Binding pKd = 7.8 7.8 -112 6
Displacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis
ChEMBL 388 8 4 4 2.5 Cc1ccc(CC(C)CNC(=O)/N=C(\N)NCCCc2cnc(N)s2)cc1 10.1021/acs.jmedchem.1c00692
168294161 193115 None 0 Human Binding pKd = 7.8 7.8 -7 4
Displacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis
ChEMBL 360 6 4 4 3.3 CCCCCNC(=O)/N=C(\N)Nc1cccc(-c2sc(N)nc2C)c1 10.1021/acs.jmedchem.1c00692
CHEMBL5204739 193115 None 0 Human Binding pKd = 7.8 7.8 -7 4
Displacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis
ChEMBL 360 6 4 4 3.3 CCCCCNC(=O)/N=C(\N)Nc1cccc(-c2sc(N)nc2C)c1 10.1021/acs.jmedchem.1c00692
CHEMBL5222742 193115 None 0 Human Binding pKd = 7.8 7.8 -7 4
Displacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis
ChEMBL 360 6 4 4 3.3 CCCCCNC(=O)/N=C(\N)Nc1cccc(-c2sc(N)nc2C)c1 10.1021/acs.jmedchem.1c00692
168294445 193119 None 0 Human Binding pKd = 7.8 7.8 -8 4
Displacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis
ChEMBL 414 6 4 4 2.6 Cc1ccc(CC(C)CNC(=O)/N=C(\N)NCC2CCc3nc(N)sc3C2)cc1 10.1021/acs.jmedchem.1c00692
CHEMBL5208113 193119 None 0 Human Binding pKd = 7.8 7.8 -8 4
Displacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis
ChEMBL 414 6 4 4 2.6 Cc1ccc(CC(C)CNC(=O)/N=C(\N)NCC2CCc3nc(N)sc3C2)cc1 10.1021/acs.jmedchem.1c00692
CHEMBL5222768 193119 None 0 Human Binding pKd = 7.8 7.8 -8 4
Displacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis
ChEMBL 414 6 4 4 2.6 Cc1ccc(CC(C)CNC(=O)/N=C(\N)NCC2CCc3nc(N)sc3C2)cc1 10.1021/acs.jmedchem.1c00692
168294166 193123 None 0 Human Binding pKd = 7.8 7.8 -4 4
Displacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis
ChEMBL 360 6 4 4 3.3 CCCCCNC(=O)/N=C(\N)Nc1ccc(-c2sc(N)nc2C)cc1 10.1021/acs.jmedchem.1c00692
CHEMBL5209081 193123 None 0 Human Binding pKd = 7.8 7.8 -4 4
Displacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis
ChEMBL 360 6 4 4 3.3 CCCCCNC(=O)/N=C(\N)Nc1ccc(-c2sc(N)nc2C)cc1 10.1021/acs.jmedchem.1c00692
CHEMBL5222775 193123 None 0 Human Binding pKd = 7.8 7.8 -4 4
Displacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis
ChEMBL 360 6 4 4 3.3 CCCCCNC(=O)/N=C(\N)Nc1ccc(-c2sc(N)nc2C)cc1 10.1021/acs.jmedchem.1c00692
168294449 193127 None 0 Human Binding pKd = 7.8 7.8 -181 6
Displacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis
ChEMBL 367 7 4 5 1.9 CC(CNC(=O)/N=C(\N)NCCCc1nnc(N)s1)C1CCCCC1 10.1021/acs.jmedchem.1c00692
CHEMBL5204599 193127 None 0 Human Binding pKd = 7.8 7.8 -181 6
Displacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis
ChEMBL 367 7 4 5 1.9 CC(CNC(=O)/N=C(\N)NCCCc1nnc(N)s1)C1CCCCC1 10.1021/acs.jmedchem.1c00692
CHEMBL5222793 193127 None 0 Human Binding pKd = 7.8 7.8 -181 6
Displacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis
ChEMBL 367 7 4 5 1.9 CC(CNC(=O)/N=C(\N)NCCCc1nnc(N)s1)C1CCCCC1 10.1021/acs.jmedchem.1c00692
168294767 193128 None 0 Human Binding pKd = 7.8 7.8 -301 20
Displacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis
ChEMBL 313 8 4 5 0.9 CCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5207281 193128 None 0 Human Binding pKd = 7.8 7.8 -301 20
Displacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis
ChEMBL 313 8 4 5 0.9 CCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5222802 193128 None 0 Human Binding pKd = 7.8 7.8 -301 20
Displacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis
ChEMBL 313 8 4 5 0.9 CCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
168294770 193129 None 0 Human Binding pKd = 7.8 7.8 -6 4
Displacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis
ChEMBL 436 6 4 4 4.3 Cc1ccc(CC(C)CNC(=O)/N=C(\N)Nc2cccc(-c3sc(N)nc3C)c2)cc1 10.1021/acs.jmedchem.1c00692
CHEMBL5208327 193129 None 0 Human Binding pKd = 7.8 7.8 -6 4
Displacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis
ChEMBL 436 6 4 4 4.3 Cc1ccc(CC(C)CNC(=O)/N=C(\N)Nc2cccc(-c3sc(N)nc3C)c2)cc1 10.1021/acs.jmedchem.1c00692
CHEMBL5222806 193129 None 0 Human Binding pKd = 7.8 7.8 -6 4
Displacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis
ChEMBL 436 6 4 4 4.3 Cc1ccc(CC(C)CNC(=O)/N=C(\N)Nc2cccc(-c3sc(N)nc3C)c2)cc1 10.1021/acs.jmedchem.1c00692
168294776 193135 None 0 Human Binding pKd = 7.8 7.8 7 4
Displacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis
ChEMBL 366 7 3 4 2.6 Cc1nnc(CCCN/C(N)=N/C(=O)NCC(C)C2CCCCC2)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5209479 193135 None 0 Human Binding pKd = 7.8 7.8 7 4
Displacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis
ChEMBL 366 7 3 4 2.6 Cc1nnc(CCCN/C(N)=N/C(=O)NCC(C)C2CCCCC2)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5222831 193135 None 0 Human Binding pKd = 7.8 7.8 7 4
Displacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis
ChEMBL 366 7 3 4 2.6 Cc1nnc(CCCN/C(N)=N/C(=O)NCC(C)C2CCCCC2)s1 10.1021/acs.jmedchem.1c00692
168295528 193140 None 0 Human Binding pKd = 7.8 7.8 -301 20
Displacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis
ChEMBL 333 6 4 5 0.9 N/C(=N\C(=O)NCc1ccccc1)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5206565 193140 None 0 Human Binding pKd = 7.8 7.8 -301 20
Displacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis
ChEMBL 333 6 4 5 0.9 N/C(=N\C(=O)NCc1ccccc1)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5222872 193140 None 0 Human Binding pKd = 7.8 7.8 -301 20
Displacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis
ChEMBL 333 6 4 5 0.9 N/C(=N\C(=O)NCc1ccccc1)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
168294178 193144 None 0 Human Binding pKd = 7.8 7.8 -5 4
Displacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis
ChEMBL 414 5 4 4 4.4 Cc1nc(N)sc1-c1ccc(N/C(N)=N/C(=O)NCC(C)C2CCCCC2)cc1 10.1021/acs.jmedchem.1c00692
CHEMBL5205197 193144 None 0 Human Binding pKd = 7.8 7.8 -5 4
Displacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis
ChEMBL 414 5 4 4 4.4 Cc1nc(N)sc1-c1ccc(N/C(N)=N/C(=O)NCC(C)C2CCCCC2)cc1 10.1021/acs.jmedchem.1c00692
CHEMBL5222887 193144 None 0 Human Binding pKd = 7.8 7.8 -5 4
Displacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis
ChEMBL 414 5 4 4 4.4 Cc1nc(N)sc1-c1ccc(N/C(N)=N/C(=O)NCC(C)C2CCCCC2)cc1 10.1021/acs.jmedchem.1c00692
168295541 193149 None 0 Human Binding pKd = 7.8 7.8 -1071 6
Displacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis
ChEMBL 347 6 4 5 1.4 C[C@@H](NC(=O)/N=C(\N)NCCCc1nnc(N)s1)c1ccccc1 10.1021/acs.jmedchem.1c00692
CHEMBL5208845 193149 None 0 Human Binding pKd = 7.8 7.8 -1071 6
Displacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis
ChEMBL 347 6 4 5 1.4 C[C@@H](NC(=O)/N=C(\N)NCCCc1nnc(N)s1)c1ccccc1 10.1021/acs.jmedchem.1c00692
CHEMBL5222926 193149 None 0 Human Binding pKd = 7.8 7.8 -1071 6
Displacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis
ChEMBL 347 6 4 5 1.4 C[C@@H](NC(=O)/N=C(\N)NCCCc1nnc(N)s1)c1ccccc1 10.1021/acs.jmedchem.1c00692
168295543 193150 None 0 Human Binding pKd = 7.8 7.8 -8 4
Displacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis
ChEMBL 380 4 4 4 3.3 Cc1nc(N)sc1-c1ccc(N/C(N)=N/C(=O)NCc2ccccc2)cc1 10.1021/acs.jmedchem.1c00692
CHEMBL5209021 193150 None 0 Human Binding pKd = 7.8 7.8 -8 4
Displacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis
ChEMBL 380 4 4 4 3.3 Cc1nc(N)sc1-c1ccc(N/C(N)=N/C(=O)NCc2ccccc2)cc1 10.1021/acs.jmedchem.1c00692
CHEMBL5222929 193150 None 0 Human Binding pKd = 7.8 7.8 -8 4
Displacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis
ChEMBL 380 4 4 4 3.3 Cc1nc(N)sc1-c1ccc(N/C(N)=N/C(=O)NCc2ccccc2)cc1 10.1021/acs.jmedchem.1c00692
168295803 193154 None 0 Human Binding pKd = 7.8 7.8 -6 4
Displacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis
ChEMBL 338 6 4 4 1.6 CCCCCNC(=O)/N=C(\N)NCC1CCc2nc(N)sc2C1 10.1021/acs.jmedchem.1c00692
CHEMBL5207206 193154 None 0 Human Binding pKd = 7.8 7.8 -6 4
Displacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis
ChEMBL 338 6 4 4 1.6 CCCCCNC(=O)/N=C(\N)NCC1CCc2nc(N)sc2C1 10.1021/acs.jmedchem.1c00692
CHEMBL5222937 193154 None 0 Human Binding pKd = 7.8 7.8 -6 4
Displacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis
ChEMBL 338 6 4 4 1.6 CCCCCNC(=O)/N=C(\N)NCC1CCc2nc(N)sc2C1 10.1021/acs.jmedchem.1c00692
168294182 193157 None 0 Human Binding pKd = 7.8 7.8 -5 4
Displacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis
ChEMBL 314 6 4 2 1.7 C[C@@H](NC(=O)/N=C(\N)NCCCc1c[nH]cn1)c1ccccc1 10.1021/acs.jmedchem.1c00692
CHEMBL5208722 193157 None 0 Human Binding pKd = 7.8 7.8 -5 4
Displacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis
ChEMBL 314 6 4 2 1.7 C[C@@H](NC(=O)/N=C(\N)NCCCc1c[nH]cn1)c1ccccc1 10.1021/acs.jmedchem.1c00692
CHEMBL5222960 193157 None 0 Human Binding pKd = 7.8 7.8 -5 4
Displacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis
ChEMBL 314 6 4 2 1.7 C[C@@H](NC(=O)/N=C(\N)NCCCc1c[nH]cn1)c1ccccc1 10.1021/acs.jmedchem.1c00692
156013896 178345 None 0 Human Binding pKd = 7.8 7.8 -7 4
Binding affinity to human recombinant NLuc/GPCR-fused H4R expressed in HEK293T cells measured after 30 mins by furimazine substrate based BRET assayBinding affinity to human recombinant NLuc/GPCR-fused H4R expressed in HEK293T cells measured after 30 mins by furimazine substrate based BRET assay
ChEMBL 401 9 1 2 5.1 Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCCCc1c[nH]cn1 10.1021/acs.jmedchem.0c00160
CHEMBL4635634 178345 None 0 Human Binding pKd = 7.8 7.8 -7 4
Binding affinity to human recombinant NLuc/GPCR-fused H4R expressed in HEK293T cells measured after 30 mins by furimazine substrate based BRET assayBinding affinity to human recombinant NLuc/GPCR-fused H4R expressed in HEK293T cells measured after 30 mins by furimazine substrate based BRET assay
ChEMBL 401 9 1 2 5.1 Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCCCc1c[nH]cn1 10.1021/acs.jmedchem.0c00160
CHEMBL4650570 178345 None 0 Human Binding pKd = 7.8 7.8 -7 4
Binding affinity to human recombinant NLuc/GPCR-fused H4R expressed in HEK293T cells measured after 30 mins by furimazine substrate based BRET assayBinding affinity to human recombinant NLuc/GPCR-fused H4R expressed in HEK293T cells measured after 30 mins by furimazine substrate based BRET assay
ChEMBL 401 9 1 2 5.1 Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCCCc1c[nH]cn1 10.1021/acs.jmedchem.0c00160
156015638 178377 None 0 Mouse Binding pKd = 6.8 6.8 -158 4
Binding affinity to mouse recombinant NLuc/GPCR-fused H4R expressed in HEK293T cells measured after 30 mins by furimazine substrate based BRET assayBinding affinity to mouse recombinant NLuc/GPCR-fused H4R expressed in HEK293T cells measured after 30 mins by furimazine substrate based BRET assay
ChEMBL 415 10 1 2 5.5 Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCCCCc1c[nH]cn1 10.1021/acs.jmedchem.0c00160
CHEMBL4642520 178377 None 0 Mouse Binding pKd = 6.8 6.8 -158 4
Binding affinity to mouse recombinant NLuc/GPCR-fused H4R expressed in HEK293T cells measured after 30 mins by furimazine substrate based BRET assayBinding affinity to mouse recombinant NLuc/GPCR-fused H4R expressed in HEK293T cells measured after 30 mins by furimazine substrate based BRET assay
ChEMBL 415 10 1 2 5.5 Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCCCCc1c[nH]cn1 10.1021/acs.jmedchem.0c00160
CHEMBL4650832 178377 None 0 Mouse Binding pKd = 6.8 6.8 -158 4
Binding affinity to mouse recombinant NLuc/GPCR-fused H4R expressed in HEK293T cells measured after 30 mins by furimazine substrate based BRET assayBinding affinity to mouse recombinant NLuc/GPCR-fused H4R expressed in HEK293T cells measured after 30 mins by furimazine substrate based BRET assay
ChEMBL 415 10 1 2 5.5 Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCCCCc1c[nH]cn1 10.1021/acs.jmedchem.0c00160
155513612 176425 None 0 Mouse Binding pKd = 7.8 7.8 -1 4
Binding affinity to mouse H4R expressed in HEK293T-SF-His6-CRE-Luc cells assessed as equilibrium dissociation constant by saturation binding studyBinding affinity to mouse H4R expressed in HEK293T-SF-His6-CRE-Luc cells assessed as equilibrium dissociation constant by saturation binding study
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 176425 None 0 Mouse Binding pKd = 7.8 7.8 -1 4
Binding affinity to mouse H4R expressed in HEK293T-SF-His6-CRE-Luc cells assessed as equilibrium dissociation constant by saturation binding studyBinding affinity to mouse H4R expressed in HEK293T-SF-His6-CRE-Luc cells assessed as equilibrium dissociation constant by saturation binding study
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 176425 None 0 Mouse Binding pKd = 7.8 7.8 -1 4
Binding affinity to mouse H4R expressed in HEK293T-SF-His6-CRE-Luc cells assessed as equilibrium dissociation constant by saturation binding studyBinding affinity to mouse H4R expressed in HEK293T-SF-His6-CRE-Luc cells assessed as equilibrium dissociation constant by saturation binding study
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 176425 None 0 Mouse Binding pKd = 7.8 7.8 -1 4
Binding affinity to mouse H4R expressed in HEK293T-SF-His6-CRE-Luc cells assessed as equilibrium dissociation constant by saturation binding studyBinding affinity to mouse H4R expressed in HEK293T-SF-His6-CRE-Luc cells assessed as equilibrium dissociation constant by saturation binding study
ChEMBL 277 4 1 5 2.1 CN(C)[C@@H]1CCN(c2ccnc(NCC(C)(C)C)n2)C1 10.1021/acs.jmedchem.9b01342
156013896 178345 None 0 Human Binding pKd = 7.8 7.8 -7 4
Binding affinity to human recombinant NLuc/GPCR-fused H4R expressed in HEK293T cells measured after 30 mins by furimazine substrate based BRET assayBinding affinity to human recombinant NLuc/GPCR-fused H4R expressed in HEK293T cells measured after 30 mins by furimazine substrate based BRET assay
ChEMBL 401 9 1 2 5.1 Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCCCc1c[nH]cn1 10.1021/acs.jmedchem.0c00160
CHEMBL4635634 178345 None 0 Human Binding pKd = 7.8 7.8 -7 4
Binding affinity to human recombinant NLuc/GPCR-fused H4R expressed in HEK293T cells measured after 30 mins by furimazine substrate based BRET assayBinding affinity to human recombinant NLuc/GPCR-fused H4R expressed in HEK293T cells measured after 30 mins by furimazine substrate based BRET assay
ChEMBL 401 9 1 2 5.1 Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCCCc1c[nH]cn1 10.1021/acs.jmedchem.0c00160
CHEMBL4650570 178345 None 0 Human Binding pKd = 7.8 7.8 -7 4
Binding affinity to human recombinant NLuc/GPCR-fused H4R expressed in HEK293T cells measured after 30 mins by furimazine substrate based BRET assayBinding affinity to human recombinant NLuc/GPCR-fused H4R expressed in HEK293T cells measured after 30 mins by furimazine substrate based BRET assay
ChEMBL 401 9 1 2 5.1 Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCCCc1c[nH]cn1 10.1021/acs.jmedchem.0c00160
135398737 958 None 57 Human Binding pKd = 7.7 7.7 -57 91
Displacement of [3H]histamine from human histamine H4 receptor transfected in SK-N-MC cells at 300 nMDisplacement of [3H]histamine from human histamine H4 receptor transfected in SK-N-MC cells at 300 nM
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm051008s
135398737.0 958 None 57 Human Binding pKd = 7.7 7.7 -57 91
Displacement of [3H]histamine from human histamine H4 receptor transfected in SK-N-MC cells at 300 nMDisplacement of [3H]histamine from human histamine H4 receptor transfected in SK-N-MC cells at 300 nM
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm051008s
38 958 None 57 Human Binding pKd = 7.7 7.7 -57 91
Displacement of [3H]histamine from human histamine H4 receptor transfected in SK-N-MC cells at 300 nMDisplacement of [3H]histamine from human histamine H4 receptor transfected in SK-N-MC cells at 300 nM
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm051008s
722 958 None 57 Human Binding pKd = 7.7 7.7 -57 91
Displacement of [3H]histamine from human histamine H4 receptor transfected in SK-N-MC cells at 300 nMDisplacement of [3H]histamine from human histamine H4 receptor transfected in SK-N-MC cells at 300 nM
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm051008s
CHEMBL42 958 None 57 Human Binding pKd = 7.7 7.7 -57 91
Displacement of [3H]histamine from human histamine H4 receptor transfected in SK-N-MC cells at 300 nMDisplacement of [3H]histamine from human histamine H4 receptor transfected in SK-N-MC cells at 300 nM
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm051008s
DB00363 958 None 57 Human Binding pKd = 7.7 7.7 -57 91
Displacement of [3H]histamine from human histamine H4 receptor transfected in SK-N-MC cells at 300 nMDisplacement of [3H]histamine from human histamine H4 receptor transfected in SK-N-MC cells at 300 nM
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm051008s
71525679 89760 None 0 Human Binding pKd = 7.7 7.7 6 6
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells by competitive kinetic analysisDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells by competitive kinetic analysis
ChEMBL 272 3 2 6 1.0 CCc1cnc2c(N3CC[C@@H](NC)C3)nc(N)nc2c1 10.1016/j.bmcl.2013.02.091
CHEMBL2376801 89760 None 0 Human Binding pKd = 7.7 7.7 6 6
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells by competitive kinetic analysisDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells by competitive kinetic analysis
ChEMBL 272 3 2 6 1.0 CCc1cnc2c(N3CC[C@@H](NC)C3)nc(N)nc2c1 10.1016/j.bmcl.2013.02.091
155513612 176425 None 0 Rat Binding pKd = 7.7 7.7 -2 4
Binding affinity to rat H4R expressed in HEK293T-SF-His6-CRE-Luc cells assessed as equilibrium dissociation constant by saturation binding studyBinding affinity to rat H4R expressed in HEK293T-SF-His6-CRE-Luc cells assessed as equilibrium dissociation constant by saturation binding study
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 176425 None 0 Rat Binding pKd = 7.7 7.7 -2 4
Binding affinity to rat H4R expressed in HEK293T-SF-His6-CRE-Luc cells assessed as equilibrium dissociation constant by saturation binding studyBinding affinity to rat H4R expressed in HEK293T-SF-His6-CRE-Luc cells assessed as equilibrium dissociation constant by saturation binding study
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 176425 None 0 Rat Binding pKd = 7.7 7.7 -2 4
Binding affinity to rat H4R expressed in HEK293T-SF-His6-CRE-Luc cells assessed as equilibrium dissociation constant by saturation binding studyBinding affinity to rat H4R expressed in HEK293T-SF-His6-CRE-Luc cells assessed as equilibrium dissociation constant by saturation binding study
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 176425 None 0 Rat Binding pKd = 7.7 7.7 -2 4
Binding affinity to rat H4R expressed in HEK293T-SF-His6-CRE-Luc cells assessed as equilibrium dissociation constant by saturation binding studyBinding affinity to rat H4R expressed in HEK293T-SF-His6-CRE-Luc cells assessed as equilibrium dissociation constant by saturation binding study
ChEMBL 277 4 1 5 2.1 CN(C)[C@@H]1CCN(c2ccnc(NCC(C)(C)C)n2)C1 10.1021/acs.jmedchem.9b01342
155513612 176425 None 0 Rat Binding pKd = 7.7 7.7 -2 4
Binding affinity to rat H4R expressed in HEK293T-SF-His6-CRE-Luc cells by saturation binding studyBinding affinity to rat H4R expressed in HEK293T-SF-His6-CRE-Luc cells by saturation binding study
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 176425 None 0 Rat Binding pKd = 7.7 7.7 -2 4
Binding affinity to rat H4R expressed in HEK293T-SF-His6-CRE-Luc cells by saturation binding studyBinding affinity to rat H4R expressed in HEK293T-SF-His6-CRE-Luc cells by saturation binding study
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 176425 None 0 Rat Binding pKd = 7.7 7.7 -2 4
Binding affinity to rat H4R expressed in HEK293T-SF-His6-CRE-Luc cells by saturation binding studyBinding affinity to rat H4R expressed in HEK293T-SF-His6-CRE-Luc cells by saturation binding study
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 176425 None 0 Rat Binding pKd = 7.7 7.7 -2 4
Binding affinity to rat H4R expressed in HEK293T-SF-His6-CRE-Luc cells by saturation binding studyBinding affinity to rat H4R expressed in HEK293T-SF-His6-CRE-Luc cells by saturation binding study
ChEMBL 277 4 1 5 2.1 CN(C)[C@@H]1CCN(c2ccnc(NCC(C)(C)C)n2)C1 10.1021/acs.jmedchem.9b01342
11846300 80297 None 3 Human Binding pKd = 7.7 7.7 -2 4
Displacement of [3H]histamine from human histamine H4 receptor transfected in SK-N-MC cells at 30 nMDisplacement of [3H]histamine from human histamine H4 receptor transfected in SK-N-MC cells at 30 nM
ChEMBL 327 0 0 4 3.8 CN1CCN(C2=Nc3ccc(Cl)cc3Oc3ccccc32)CC1 10.1021/jm051008s
CHEMBL213912 80297 None 3 Human Binding pKd = 7.7 7.7 -2 4
Displacement of [3H]histamine from human histamine H4 receptor transfected in SK-N-MC cells at 30 nMDisplacement of [3H]histamine from human histamine H4 receptor transfected in SK-N-MC cells at 30 nM
ChEMBL 327 0 0 4 3.8 CN1CCN(C2=Nc3ccc(Cl)cc3Oc3ccccc32)CC1 10.1021/jm051008s
24745335 295 None 13 Human Binding pKd = 7.6 7.6 4 5
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells by competitive kinetic analysisDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells by competitive kinetic analysis
ChEMBL 262 5 3 6 0.7 CN[C@@H]1CCN(C1)c1cc(NCC2CC2)nc(n1)N 10.1016/j.bmcl.2013.02.091
8985 295 None 13 Human Binding pKd = 7.6 7.6 4 5
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells by competitive kinetic analysisDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells by competitive kinetic analysis
ChEMBL 262 5 3 6 0.7 CN[C@@H]1CCN(C1)c1cc(NCC2CC2)nc(n1)N 10.1016/j.bmcl.2013.02.091
CHEMBL1915540 295 None 13 Human Binding pKd = 7.6 7.6 4 5
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells by competitive kinetic analysisDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells by competitive kinetic analysis
ChEMBL 262 5 3 6 0.7 CN[C@@H]1CCN(C1)c1cc(NCC2CC2)nc(n1)N 10.1016/j.bmcl.2013.02.091
DB15027 295 None 13 Human Binding pKd = 7.6 7.6 4 5
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells by competitive kinetic analysisDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells by competitive kinetic analysis
ChEMBL 262 5 3 6 0.7 CN[C@@H]1CCN(C1)c1cc(NCC2CC2)nc(n1)N 10.1016/j.bmcl.2013.02.091
1278 2150 None 56 Human Binding pKd = 8.4 8.4 -3 8
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells by competitive kinetic analysisDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells by competitive kinetic analysis
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1016/j.bmcl.2013.02.091
1279 2150 None 56 Human Binding pKd = 8.4 8.4 -3 8
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells by competitive kinetic analysisDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells by competitive kinetic analysis
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1016/j.bmcl.2013.02.091
4908365 2150 None 56 Human Binding pKd = 8.4 8.4 -3 8
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells by competitive kinetic analysisDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells by competitive kinetic analysis
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1016/j.bmcl.2013.02.091
CHEMBL129198 2150 None 56 Human Binding pKd = 8.4 8.4 -3 8
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells by competitive kinetic analysisDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells by competitive kinetic analysis
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1016/j.bmcl.2013.02.091
1223 953 None 33 Human Binding pKd = 7.5 7.5 -60 11
Binding affinity to NLuc-tagged human H4R expressed in HEK293T cell homogenates using NanoGlo as substrate preincubated for 2 hrs followed by substrate addition measured after 5 min by NanoBRET saturation binding assayBinding affinity to NLuc-tagged human H4R expressed in HEK293T cell homogenates using NanoGlo as substrate preincubated for 2 hrs followed by substrate addition measured after 5 min by NanoBRET saturation binding assay
ChEMBL 308 6 2 3 3.2 Clc1ccc(cc1)CN=C(SCCCc1cnc[nH]1)N 10.1021/acs.jmedchem.2c00125
2790 953 None 33 Human Binding pKd = 7.5 7.5 -60 11
Binding affinity to NLuc-tagged human H4R expressed in HEK293T cell homogenates using NanoGlo as substrate preincubated for 2 hrs followed by substrate addition measured after 5 min by NanoBRET saturation binding assayBinding affinity to NLuc-tagged human H4R expressed in HEK293T cell homogenates using NanoGlo as substrate preincubated for 2 hrs followed by substrate addition measured after 5 min by NanoBRET saturation binding assay
ChEMBL 308 6 2 3 3.2 Clc1ccc(cc1)CN=C(SCCCc1cnc[nH]1)N 10.1021/acs.jmedchem.2c00125
CHEMBL14690 953 None 33 Human Binding pKd = 7.5 7.5 -60 11
Binding affinity to NLuc-tagged human H4R expressed in HEK293T cell homogenates using NanoGlo as substrate preincubated for 2 hrs followed by substrate addition measured after 5 min by NanoBRET saturation binding assayBinding affinity to NLuc-tagged human H4R expressed in HEK293T cell homogenates using NanoGlo as substrate preincubated for 2 hrs followed by substrate addition measured after 5 min by NanoBRET saturation binding assay
ChEMBL 308 6 2 3 3.2 Clc1ccc(cc1)CN=C(SCCCc1cnc[nH]1)N 10.1021/acs.jmedchem.2c00125
1223 953 None 33 Human Binding pKd = 7.5 7.5 -60 11
Binding affinity to NLuc-tagged human H4R expressed in HEK293T cell homogenates using NanoGlo as substrate preincubated for 2 hrs followed by substrate addition measured after 5 min by NanoBRET saturation binding assayBinding affinity to NLuc-tagged human H4R expressed in HEK293T cell homogenates using NanoGlo as substrate preincubated for 2 hrs followed by substrate addition measured after 5 min by NanoBRET saturation binding assay
ChEMBL 308 6 2 3 3.2 Clc1ccc(cc1)CN=C(SCCCc1cnc[nH]1)N 10.1021/acs.jmedchem.2c00125
2790 953 None 33 Human Binding pKd = 7.5 7.5 -60 11
Binding affinity to NLuc-tagged human H4R expressed in HEK293T cell homogenates using NanoGlo as substrate preincubated for 2 hrs followed by substrate addition measured after 5 min by NanoBRET saturation binding assayBinding affinity to NLuc-tagged human H4R expressed in HEK293T cell homogenates using NanoGlo as substrate preincubated for 2 hrs followed by substrate addition measured after 5 min by NanoBRET saturation binding assay
ChEMBL 308 6 2 3 3.2 Clc1ccc(cc1)CN=C(SCCCc1cnc[nH]1)N 10.1021/acs.jmedchem.2c00125
CHEMBL14690 953 None 33 Human Binding pKd = 7.5 7.5 -60 11
Binding affinity to NLuc-tagged human H4R expressed in HEK293T cell homogenates using NanoGlo as substrate preincubated for 2 hrs followed by substrate addition measured after 5 min by NanoBRET saturation binding assayBinding affinity to NLuc-tagged human H4R expressed in HEK293T cell homogenates using NanoGlo as substrate preincubated for 2 hrs followed by substrate addition measured after 5 min by NanoBRET saturation binding assay
ChEMBL 308 6 2 3 3.2 Clc1ccc(cc1)CN=C(SCCCc1cnc[nH]1)N 10.1021/acs.jmedchem.2c00125
156013896 178345 None 0 Mouse Binding pKd = 7.5 7.5 -22 4
Binding affinity to mouse recombinant NLuc/GPCR-fused H4R expressed in HEK293T cells assessed as dissociation constant measured after 30 mins in presence of thioperamide by furimazine substrate based BRET assayBinding affinity to mouse recombinant NLuc/GPCR-fused H4R expressed in HEK293T cells assessed as dissociation constant measured after 30 mins in presence of thioperamide by furimazine substrate based BRET assay
ChEMBL 401 9 1 2 5.1 Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCCCc1c[nH]cn1 10.1021/acs.jmedchem.0c00160
CHEMBL4635634 178345 None 0 Mouse Binding pKd = 7.5 7.5 -22 4
Binding affinity to mouse recombinant NLuc/GPCR-fused H4R expressed in HEK293T cells assessed as dissociation constant measured after 30 mins in presence of thioperamide by furimazine substrate based BRET assayBinding affinity to mouse recombinant NLuc/GPCR-fused H4R expressed in HEK293T cells assessed as dissociation constant measured after 30 mins in presence of thioperamide by furimazine substrate based BRET assay
ChEMBL 401 9 1 2 5.1 Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCCCc1c[nH]cn1 10.1021/acs.jmedchem.0c00160
CHEMBL4650570 178345 None 0 Mouse Binding pKd = 7.5 7.5 -22 4
Binding affinity to mouse recombinant NLuc/GPCR-fused H4R expressed in HEK293T cells assessed as dissociation constant measured after 30 mins in presence of thioperamide by furimazine substrate based BRET assayBinding affinity to mouse recombinant NLuc/GPCR-fused H4R expressed in HEK293T cells assessed as dissociation constant measured after 30 mins in presence of thioperamide by furimazine substrate based BRET assay
ChEMBL 401 9 1 2 5.1 Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCCCc1c[nH]cn1 10.1021/acs.jmedchem.0c00160
155513612 176425 None 0 Mouse Binding pKd = 7.5 7.5 -1 4
Binding affinity to mouse H4R expressed in HEK293T-SF-His6-CRE-Luc cells assessed as kinetically derived dissociation constant by saturation binding studyBinding affinity to mouse H4R expressed in HEK293T-SF-His6-CRE-Luc cells assessed as kinetically derived dissociation constant by saturation binding study
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 176425 None 0 Mouse Binding pKd = 7.5 7.5 -1 4
Binding affinity to mouse H4R expressed in HEK293T-SF-His6-CRE-Luc cells assessed as kinetically derived dissociation constant by saturation binding studyBinding affinity to mouse H4R expressed in HEK293T-SF-His6-CRE-Luc cells assessed as kinetically derived dissociation constant by saturation binding study
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 176425 None 0 Mouse Binding pKd = 7.5 7.5 -1 4
Binding affinity to mouse H4R expressed in HEK293T-SF-His6-CRE-Luc cells assessed as kinetically derived dissociation constant by saturation binding studyBinding affinity to mouse H4R expressed in HEK293T-SF-His6-CRE-Luc cells assessed as kinetically derived dissociation constant by saturation binding study
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 176425 None 0 Mouse Binding pKd = 7.5 7.5 -1 4
Binding affinity to mouse H4R expressed in HEK293T-SF-His6-CRE-Luc cells assessed as kinetically derived dissociation constant by saturation binding studyBinding affinity to mouse H4R expressed in HEK293T-SF-His6-CRE-Luc cells assessed as kinetically derived dissociation constant by saturation binding study
ChEMBL 277 4 1 5 2.1 CN(C)[C@@H]1CCN(c2ccnc(NCC(C)(C)C)n2)C1 10.1021/acs.jmedchem.9b01342
155513612 176425 None 0 Mouse Binding pKd = 7.5 7.5 -1 4
Binding affinity to mouse H4R expressed in HEK293T-SF-His6-CRE-Luc cells by kinetic binding studyBinding affinity to mouse H4R expressed in HEK293T-SF-His6-CRE-Luc cells by kinetic binding study
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 176425 None 0 Mouse Binding pKd = 7.5 7.5 -1 4
Binding affinity to mouse H4R expressed in HEK293T-SF-His6-CRE-Luc cells by kinetic binding studyBinding affinity to mouse H4R expressed in HEK293T-SF-His6-CRE-Luc cells by kinetic binding study
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 176425 None 0 Mouse Binding pKd = 7.5 7.5 -1 4
Binding affinity to mouse H4R expressed in HEK293T-SF-His6-CRE-Luc cells by kinetic binding studyBinding affinity to mouse H4R expressed in HEK293T-SF-His6-CRE-Luc cells by kinetic binding study
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 176425 None 0 Mouse Binding pKd = 7.5 7.5 -1 4
Binding affinity to mouse H4R expressed in HEK293T-SF-His6-CRE-Luc cells by kinetic binding studyBinding affinity to mouse H4R expressed in HEK293T-SF-His6-CRE-Luc cells by kinetic binding study
ChEMBL 277 4 1 5 2.1 CN(C)[C@@H]1CCN(c2ccnc(NCC(C)(C)C)n2)C1 10.1021/acs.jmedchem.9b01342
155513612 176425 None 0 Rat Binding pKd = 7.5 7.5 -2 4
Binding affinity to rat H4R expressed in HEK293T-SF-His6-CRE-Luc cells assessed as kinetically derived dissociation constant by saturation binding studyBinding affinity to rat H4R expressed in HEK293T-SF-His6-CRE-Luc cells assessed as kinetically derived dissociation constant by saturation binding study
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 176425 None 0 Rat Binding pKd = 7.5 7.5 -2 4
Binding affinity to rat H4R expressed in HEK293T-SF-His6-CRE-Luc cells assessed as kinetically derived dissociation constant by saturation binding studyBinding affinity to rat H4R expressed in HEK293T-SF-His6-CRE-Luc cells assessed as kinetically derived dissociation constant by saturation binding study
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 176425 None 0 Rat Binding pKd = 7.5 7.5 -2 4
Binding affinity to rat H4R expressed in HEK293T-SF-His6-CRE-Luc cells assessed as kinetically derived dissociation constant by saturation binding studyBinding affinity to rat H4R expressed in HEK293T-SF-His6-CRE-Luc cells assessed as kinetically derived dissociation constant by saturation binding study
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 176425 None 0 Rat Binding pKd = 7.5 7.5 -2 4
Binding affinity to rat H4R expressed in HEK293T-SF-His6-CRE-Luc cells assessed as kinetically derived dissociation constant by saturation binding studyBinding affinity to rat H4R expressed in HEK293T-SF-His6-CRE-Luc cells assessed as kinetically derived dissociation constant by saturation binding study
ChEMBL 277 4 1 5 2.1 CN(C)[C@@H]1CCN(c2ccnc(NCC(C)(C)C)n2)C1 10.1021/acs.jmedchem.9b01342
155513612 176425 None 0 Rat Binding pKd = 7.5 7.5 -2 4
Binding affinity to rat H4R expressed in HEK293T-SF-His6-CRE-Luc cells by kinetic binding studyBinding affinity to rat H4R expressed in HEK293T-SF-His6-CRE-Luc cells by kinetic binding study
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 176425 None 0 Rat Binding pKd = 7.5 7.5 -2 4
Binding affinity to rat H4R expressed in HEK293T-SF-His6-CRE-Luc cells by kinetic binding studyBinding affinity to rat H4R expressed in HEK293T-SF-His6-CRE-Luc cells by kinetic binding study
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 176425 None 0 Rat Binding pKd = 7.5 7.5 -2 4
Binding affinity to rat H4R expressed in HEK293T-SF-His6-CRE-Luc cells by kinetic binding studyBinding affinity to rat H4R expressed in HEK293T-SF-His6-CRE-Luc cells by kinetic binding study
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 176425 None 0 Rat Binding pKd = 7.5 7.5 -2 4
Binding affinity to rat H4R expressed in HEK293T-SF-His6-CRE-Luc cells by kinetic binding studyBinding affinity to rat H4R expressed in HEK293T-SF-His6-CRE-Luc cells by kinetic binding study
ChEMBL 277 4 1 5 2.1 CN(C)[C@@H]1CCN(c2ccnc(NCC(C)(C)C)n2)C1 10.1021/acs.jmedchem.9b01342
155513612 176425 None 0 Human Binding pKd = 7.4 7.4 1 4
Binding affinity to human H4R expressed in HEK293T-SF-His6-CRE-Luc cells by saturation binding studyBinding affinity to human H4R expressed in HEK293T-SF-His6-CRE-Luc cells by saturation binding study
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 176425 None 0 Human Binding pKd = 7.4 7.4 1 4
Binding affinity to human H4R expressed in HEK293T-SF-His6-CRE-Luc cells by saturation binding studyBinding affinity to human H4R expressed in HEK293T-SF-His6-CRE-Luc cells by saturation binding study
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 176425 None 0 Human Binding pKd = 7.4 7.4 1 4
Binding affinity to human H4R expressed in HEK293T-SF-His6-CRE-Luc cells by saturation binding studyBinding affinity to human H4R expressed in HEK293T-SF-His6-CRE-Luc cells by saturation binding study
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 176425 None 0 Human Binding pKd = 7.4 7.4 1 4
Binding affinity to human H4R expressed in HEK293T-SF-His6-CRE-Luc cells by saturation binding studyBinding affinity to human H4R expressed in HEK293T-SF-His6-CRE-Luc cells by saturation binding study
ChEMBL 277 4 1 5 2.1 CN(C)[C@@H]1CCN(c2ccnc(NCC(C)(C)C)n2)C1 10.1021/acs.jmedchem.9b01342
156013896 178345 None 0 Human Binding pKd = 7.4 7.4 -7 4
Binding affinity to recombinant human N- terminal NLuc-tagged H4R expressed in HEK293T cells by flow cytometryBinding affinity to recombinant human N- terminal NLuc-tagged H4R expressed in HEK293T cells by flow cytometry
ChEMBL 401 9 1 2 5.1 Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCCCc1c[nH]cn1 10.1021/acs.jmedchem.0c00160
CHEMBL4635634 178345 None 0 Human Binding pKd = 7.4 7.4 -7 4
Binding affinity to recombinant human N- terminal NLuc-tagged H4R expressed in HEK293T cells by flow cytometryBinding affinity to recombinant human N- terminal NLuc-tagged H4R expressed in HEK293T cells by flow cytometry
ChEMBL 401 9 1 2 5.1 Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCCCc1c[nH]cn1 10.1021/acs.jmedchem.0c00160
CHEMBL4650570 178345 None 0 Human Binding pKd = 7.4 7.4 -7 4
Binding affinity to recombinant human N- terminal NLuc-tagged H4R expressed in HEK293T cells by flow cytometryBinding affinity to recombinant human N- terminal NLuc-tagged H4R expressed in HEK293T cells by flow cytometry
ChEMBL 401 9 1 2 5.1 Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCCCc1c[nH]cn1 10.1021/acs.jmedchem.0c00160
56835171 69762 None 0 Human Binding pKd = 7.4 7.4 1 9
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells by competitive kinetic analysisDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells by competitive kinetic analysis
ChEMBL 295 2 2 6 1.9 Nc1nc(N2CCNCC2)c2ccc(-c3ccco3)cc2n1 10.1016/j.bmcl.2013.02.091
CHEMBL1935574 69762 None 0 Human Binding pKd = 7.4 7.4 1 9
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells by competitive kinetic analysisDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells by competitive kinetic analysis
ChEMBL 295 2 2 6 1.9 Nc1nc(N2CCNCC2)c2ccc(-c3ccco3)cc2n1 10.1016/j.bmcl.2013.02.091
155513612 176425 None 0 Human Binding pKd = 7.4 7.4 1 4
Binding affinity to human H4R expressed in HEK293T-SF-His6-CRE-Luc cells assessed as equilibrium dissociation constant by saturation binding studyBinding affinity to human H4R expressed in HEK293T-SF-His6-CRE-Luc cells assessed as equilibrium dissociation constant by saturation binding study
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 176425 None 0 Human Binding pKd = 7.4 7.4 1 4
Binding affinity to human H4R expressed in HEK293T-SF-His6-CRE-Luc cells assessed as equilibrium dissociation constant by saturation binding studyBinding affinity to human H4R expressed in HEK293T-SF-His6-CRE-Luc cells assessed as equilibrium dissociation constant by saturation binding study
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 176425 None 0 Human Binding pKd = 7.4 7.4 1 4
Binding affinity to human H4R expressed in HEK293T-SF-His6-CRE-Luc cells assessed as equilibrium dissociation constant by saturation binding studyBinding affinity to human H4R expressed in HEK293T-SF-His6-CRE-Luc cells assessed as equilibrium dissociation constant by saturation binding study
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 176425 None 0 Human Binding pKd = 7.4 7.4 1 4
Binding affinity to human H4R expressed in HEK293T-SF-His6-CRE-Luc cells assessed as equilibrium dissociation constant by saturation binding studyBinding affinity to human H4R expressed in HEK293T-SF-His6-CRE-Luc cells assessed as equilibrium dissociation constant by saturation binding study
ChEMBL 277 4 1 5 2.1 CN(C)[C@@H]1CCN(c2ccnc(NCC(C)(C)C)n2)C1 10.1021/acs.jmedchem.9b01342
156013896 178345 None 0 Human Binding pKd = 7.4 7.4 -7 4
Binding affinity to recombinant human N- terminal NLuc-tagged H4R expressed in HEK293T cells by flow cytometryBinding affinity to recombinant human N- terminal NLuc-tagged H4R expressed in HEK293T cells by flow cytometry
ChEMBL 401 9 1 2 5.1 Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCCCc1c[nH]cn1 10.1021/acs.jmedchem.0c00160
CHEMBL4635634 178345 None 0 Human Binding pKd = 7.4 7.4 -7 4
Binding affinity to recombinant human N- terminal NLuc-tagged H4R expressed in HEK293T cells by flow cytometryBinding affinity to recombinant human N- terminal NLuc-tagged H4R expressed in HEK293T cells by flow cytometry
ChEMBL 401 9 1 2 5.1 Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCCCc1c[nH]cn1 10.1021/acs.jmedchem.0c00160
CHEMBL4650570 178345 None 0 Human Binding pKd = 7.4 7.4 -7 4
Binding affinity to recombinant human N- terminal NLuc-tagged H4R expressed in HEK293T cells by flow cytometryBinding affinity to recombinant human N- terminal NLuc-tagged H4R expressed in HEK293T cells by flow cytometry
ChEMBL 401 9 1 2 5.1 Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCCCc1c[nH]cn1 10.1021/acs.jmedchem.0c00160
1204 1932 None 74 Mouse Binding pKd = 7.4 7.4 -15 24
Binding affinity to mouse H4RBinding affinity to mouse H4R
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.9b01342
1247 1932 None 74 Mouse Binding pKd = 7.4 7.4 -15 24
Binding affinity to mouse H4RBinding affinity to mouse H4R
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.9b01342
1375 1932 None 74 Mouse Binding pKd = 7.4 7.4 -15 24
Binding affinity to mouse H4RBinding affinity to mouse H4R
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.9b01342
774 1932 None 74 Mouse Binding pKd = 7.4 7.4 -15 24
Binding affinity to mouse H4RBinding affinity to mouse H4R
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.9b01342
774.0 1932 None 74 Mouse Binding pKd = 7.4 7.4 -15 24
Binding affinity to mouse H4RBinding affinity to mouse H4R
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.9b01342
CHEMBL90 1932 None 74 Mouse Binding pKd = 7.4 7.4 -15 24
Binding affinity to mouse H4RBinding affinity to mouse H4R
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.9b01342
DB05381 1932 None 74 Mouse Binding pKd = 7.4 7.4 -15 24
Binding affinity to mouse H4RBinding affinity to mouse H4R
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.9b01342
156013896 178345 None 0 Mouse Binding pKd = 7.3 7.3 -22 4
Binding affinity to mouse recombinant NLuc/GPCR-fused H4R expressed in HEK293T cells assessed as dissociation constant measured after 30 mins in presence of thioperamide by furimazine substrate based BRET assayBinding affinity to mouse recombinant NLuc/GPCR-fused H4R expressed in HEK293T cells assessed as dissociation constant measured after 30 mins in presence of thioperamide by furimazine substrate based BRET assay
ChEMBL 401 9 1 2 5.1 Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCCCc1c[nH]cn1 10.1021/acs.jmedchem.0c00160
CHEMBL4635634 178345 None 0 Mouse Binding pKd = 7.3 7.3 -22 4
Binding affinity to mouse recombinant NLuc/GPCR-fused H4R expressed in HEK293T cells assessed as dissociation constant measured after 30 mins in presence of thioperamide by furimazine substrate based BRET assayBinding affinity to mouse recombinant NLuc/GPCR-fused H4R expressed in HEK293T cells assessed as dissociation constant measured after 30 mins in presence of thioperamide by furimazine substrate based BRET assay
ChEMBL 401 9 1 2 5.1 Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCCCc1c[nH]cn1 10.1021/acs.jmedchem.0c00160
CHEMBL4650570 178345 None 0 Mouse Binding pKd = 7.3 7.3 -22 4
Binding affinity to mouse recombinant NLuc/GPCR-fused H4R expressed in HEK293T cells assessed as dissociation constant measured after 30 mins in presence of thioperamide by furimazine substrate based BRET assayBinding affinity to mouse recombinant NLuc/GPCR-fused H4R expressed in HEK293T cells assessed as dissociation constant measured after 30 mins in presence of thioperamide by furimazine substrate based BRET assay
ChEMBL 401 9 1 2 5.1 Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCCCc1c[nH]cn1 10.1021/acs.jmedchem.0c00160
1204 1932 None 74 Human Binding pKd = 8.3 8.3 -3 24
Binding affinity to human H4RBinding affinity to human H4R
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.9b01342
1247 1932 None 74 Human Binding pKd = 8.3 8.3 -3 24
Binding affinity to human H4RBinding affinity to human H4R
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.9b01342
1375 1932 None 74 Human Binding pKd = 8.3 8.3 -3 24
Binding affinity to human H4RBinding affinity to human H4R
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.9b01342
774 1932 None 74 Human Binding pKd = 8.3 8.3 -3 24
Binding affinity to human H4RBinding affinity to human H4R
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.9b01342
774.0 1932 None 74 Human Binding pKd = 8.3 8.3 -3 24
Binding affinity to human H4RBinding affinity to human H4R
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.9b01342
CHEMBL90 1932 None 74 Human Binding pKd = 8.3 8.3 -3 24
Binding affinity to human H4RBinding affinity to human H4R
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.9b01342
DB05381 1932 None 74 Human Binding pKd = 8.3 8.3 -3 24
Binding affinity to human H4RBinding affinity to human H4R
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.9b01342
156013896 178345 None 0 Mouse Binding pKd = 7.3 7.3 -22 4
Binding affinity to recombinant mouse N- terminal NLuc-tagged H4R expressed in HEK293T cells by flow cytometryBinding affinity to recombinant mouse N- terminal NLuc-tagged H4R expressed in HEK293T cells by flow cytometry
ChEMBL 401 9 1 2 5.1 Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCCCc1c[nH]cn1 10.1021/acs.jmedchem.0c00160
CHEMBL4635634 178345 None 0 Mouse Binding pKd = 7.3 7.3 -22 4
Binding affinity to recombinant mouse N- terminal NLuc-tagged H4R expressed in HEK293T cells by flow cytometryBinding affinity to recombinant mouse N- terminal NLuc-tagged H4R expressed in HEK293T cells by flow cytometry
ChEMBL 401 9 1 2 5.1 Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCCCc1c[nH]cn1 10.1021/acs.jmedchem.0c00160
CHEMBL4650570 178345 None 0 Mouse Binding pKd = 7.3 7.3 -22 4
Binding affinity to recombinant mouse N- terminal NLuc-tagged H4R expressed in HEK293T cells by flow cytometryBinding affinity to recombinant mouse N- terminal NLuc-tagged H4R expressed in HEK293T cells by flow cytometry
ChEMBL 401 9 1 2 5.1 Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCCCc1c[nH]cn1 10.1021/acs.jmedchem.0c00160
155513612 176425 None 0 Human Binding pKd = 7.2 7.2 1 4
Binding affinity to human H4R expressed in HEK293T-SF-His6-CRE-Luc cells assessed as kinetically derived dissociation constant by saturation binding studyBinding affinity to human H4R expressed in HEK293T-SF-His6-CRE-Luc cells assessed as kinetically derived dissociation constant by saturation binding study
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 176425 None 0 Human Binding pKd = 7.2 7.2 1 4
Binding affinity to human H4R expressed in HEK293T-SF-His6-CRE-Luc cells assessed as kinetically derived dissociation constant by saturation binding studyBinding affinity to human H4R expressed in HEK293T-SF-His6-CRE-Luc cells assessed as kinetically derived dissociation constant by saturation binding study
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 176425 None 0 Human Binding pKd = 7.2 7.2 1 4
Binding affinity to human H4R expressed in HEK293T-SF-His6-CRE-Luc cells assessed as kinetically derived dissociation constant by saturation binding studyBinding affinity to human H4R expressed in HEK293T-SF-His6-CRE-Luc cells assessed as kinetically derived dissociation constant by saturation binding study
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 176425 None 0 Human Binding pKd = 7.2 7.2 1 4
Binding affinity to human H4R expressed in HEK293T-SF-His6-CRE-Luc cells assessed as kinetically derived dissociation constant by saturation binding studyBinding affinity to human H4R expressed in HEK293T-SF-His6-CRE-Luc cells assessed as kinetically derived dissociation constant by saturation binding study
ChEMBL 277 4 1 5 2.1 CN(C)[C@@H]1CCN(c2ccnc(NCC(C)(C)C)n2)C1 10.1021/acs.jmedchem.9b01342
155513612 176425 None 0 Human Binding pKd = 7.2 7.2 1 4
Binding affinity to human H4R expressed in HEK293T-SF-His6-CRE-Luc cells by kinetic binding studyBinding affinity to human H4R expressed in HEK293T-SF-His6-CRE-Luc cells by kinetic binding study
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 176425 None 0 Human Binding pKd = 7.2 7.2 1 4
Binding affinity to human H4R expressed in HEK293T-SF-His6-CRE-Luc cells by kinetic binding studyBinding affinity to human H4R expressed in HEK293T-SF-His6-CRE-Luc cells by kinetic binding study
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 176425 None 0 Human Binding pKd = 7.2 7.2 1 4
Binding affinity to human H4R expressed in HEK293T-SF-His6-CRE-Luc cells by kinetic binding studyBinding affinity to human H4R expressed in HEK293T-SF-His6-CRE-Luc cells by kinetic binding study
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 176425 None 0 Human Binding pKd = 7.2 7.2 1 4
Binding affinity to human H4R expressed in HEK293T-SF-His6-CRE-Luc cells by kinetic binding studyBinding affinity to human H4R expressed in HEK293T-SF-His6-CRE-Luc cells by kinetic binding study
ChEMBL 277 4 1 5 2.1 CN(C)[C@@H]1CCN(c2ccnc(NCC(C)(C)C)n2)C1 10.1021/acs.jmedchem.9b01342
156013896 178345 None 0 Mouse Binding pKd = 7.2 7.2 -22 4
Binding affinity to mouse recombinant NLuc/GPCR-fused H4R expressed in HEK293T cells measured after 30 mins by furimazine substrate based BRET assayBinding affinity to mouse recombinant NLuc/GPCR-fused H4R expressed in HEK293T cells measured after 30 mins by furimazine substrate based BRET assay
ChEMBL 401 9 1 2 5.1 Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCCCc1c[nH]cn1 10.1021/acs.jmedchem.0c00160
CHEMBL4635634 178345 None 0 Mouse Binding pKd = 7.2 7.2 -22 4
Binding affinity to mouse recombinant NLuc/GPCR-fused H4R expressed in HEK293T cells measured after 30 mins by furimazine substrate based BRET assayBinding affinity to mouse recombinant NLuc/GPCR-fused H4R expressed in HEK293T cells measured after 30 mins by furimazine substrate based BRET assay
ChEMBL 401 9 1 2 5.1 Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCCCc1c[nH]cn1 10.1021/acs.jmedchem.0c00160
CHEMBL4650570 178345 None 0 Mouse Binding pKd = 7.2 7.2 -22 4
Binding affinity to mouse recombinant NLuc/GPCR-fused H4R expressed in HEK293T cells measured after 30 mins by furimazine substrate based BRET assayBinding affinity to mouse recombinant NLuc/GPCR-fused H4R expressed in HEK293T cells measured after 30 mins by furimazine substrate based BRET assay
ChEMBL 401 9 1 2 5.1 Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCCCc1c[nH]cn1 10.1021/acs.jmedchem.0c00160
156013896 178345 None 0 Mouse Binding pKd = 7.2 7.2 -22 4
Binding affinity to recombinant mouse N- terminal NLuc-tagged H4R expressed in HEK293T cells by flow cytometryBinding affinity to recombinant mouse N- terminal NLuc-tagged H4R expressed in HEK293T cells by flow cytometry
ChEMBL 401 9 1 2 5.1 Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCCCc1c[nH]cn1 10.1021/acs.jmedchem.0c00160
CHEMBL4635634 178345 None 0 Mouse Binding pKd = 7.2 7.2 -22 4
Binding affinity to recombinant mouse N- terminal NLuc-tagged H4R expressed in HEK293T cells by flow cytometryBinding affinity to recombinant mouse N- terminal NLuc-tagged H4R expressed in HEK293T cells by flow cytometry
ChEMBL 401 9 1 2 5.1 Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCCCc1c[nH]cn1 10.1021/acs.jmedchem.0c00160
CHEMBL4650570 178345 None 0 Mouse Binding pKd = 7.2 7.2 -22 4
Binding affinity to recombinant mouse N- terminal NLuc-tagged H4R expressed in HEK293T cells by flow cytometryBinding affinity to recombinant mouse N- terminal NLuc-tagged H4R expressed in HEK293T cells by flow cytometry
ChEMBL 401 9 1 2 5.1 Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCCCc1c[nH]cn1 10.1021/acs.jmedchem.0c00160
156013896 178345 None 0 Mouse Binding pKd = 7.2 7.2 -22 4
Binding affinity to mouse recombinant NLuc/GPCR-fused H4R expressed in HEK293T cells measured after 30 mins by furimazine substrate based BRET assayBinding affinity to mouse recombinant NLuc/GPCR-fused H4R expressed in HEK293T cells measured after 30 mins by furimazine substrate based BRET assay
ChEMBL 401 9 1 2 5.1 Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCCCc1c[nH]cn1 10.1021/acs.jmedchem.0c00160
CHEMBL4635634 178345 None 0 Mouse Binding pKd = 7.2 7.2 -22 4
Binding affinity to mouse recombinant NLuc/GPCR-fused H4R expressed in HEK293T cells measured after 30 mins by furimazine substrate based BRET assayBinding affinity to mouse recombinant NLuc/GPCR-fused H4R expressed in HEK293T cells measured after 30 mins by furimazine substrate based BRET assay
ChEMBL 401 9 1 2 5.1 Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCCCc1c[nH]cn1 10.1021/acs.jmedchem.0c00160
CHEMBL4650570 178345 None 0 Mouse Binding pKd = 7.2 7.2 -22 4
Binding affinity to mouse recombinant NLuc/GPCR-fused H4R expressed in HEK293T cells measured after 30 mins by furimazine substrate based BRET assayBinding affinity to mouse recombinant NLuc/GPCR-fused H4R expressed in HEK293T cells measured after 30 mins by furimazine substrate based BRET assay
ChEMBL 401 9 1 2 5.1 Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCCCc1c[nH]cn1 10.1021/acs.jmedchem.0c00160
135398737 958 None 57 Human Binding pKd = 7.2 7.2 -57 91
Displacement of [3H]histamine from human histamine H4 receptor transfected in SK-N-MC cells at 1 uMDisplacement of [3H]histamine from human histamine H4 receptor transfected in SK-N-MC cells at 1 uM
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm051008s
135398737.0 958 None 57 Human Binding pKd = 7.2 7.2 -57 91
Displacement of [3H]histamine from human histamine H4 receptor transfected in SK-N-MC cells at 1 uMDisplacement of [3H]histamine from human histamine H4 receptor transfected in SK-N-MC cells at 1 uM
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm051008s
38 958 None 57 Human Binding pKd = 7.2 7.2 -57 91
Displacement of [3H]histamine from human histamine H4 receptor transfected in SK-N-MC cells at 1 uMDisplacement of [3H]histamine from human histamine H4 receptor transfected in SK-N-MC cells at 1 uM
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm051008s
722 958 None 57 Human Binding pKd = 7.2 7.2 -57 91
Displacement of [3H]histamine from human histamine H4 receptor transfected in SK-N-MC cells at 1 uMDisplacement of [3H]histamine from human histamine H4 receptor transfected in SK-N-MC cells at 1 uM
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm051008s
CHEMBL42 958 None 57 Human Binding pKd = 7.2 7.2 -57 91
Displacement of [3H]histamine from human histamine H4 receptor transfected in SK-N-MC cells at 1 uMDisplacement of [3H]histamine from human histamine H4 receptor transfected in SK-N-MC cells at 1 uM
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm051008s
DB00363 958 None 57 Human Binding pKd = 7.2 7.2 -57 91
Displacement of [3H]histamine from human histamine H4 receptor transfected in SK-N-MC cells at 1 uMDisplacement of [3H]histamine from human histamine H4 receptor transfected in SK-N-MC cells at 1 uM
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm051008s
11846300 80297 None 3 Human Binding pKd = 7.1 7.1 -2 4
Displacement of [3H]Histamine from human histamine H4 receptor transfected in SK-N-MC cells at 100 nMDisplacement of [3H]Histamine from human histamine H4 receptor transfected in SK-N-MC cells at 100 nM
ChEMBL 327 0 0 4 3.8 CN1CCN(C2=Nc3ccc(Cl)cc3Oc3ccccc32)CC1 10.1021/jm051008s
CHEMBL213912 80297 None 3 Human Binding pKd = 7.1 7.1 -2 4
Displacement of [3H]Histamine from human histamine H4 receptor transfected in SK-N-MC cells at 100 nMDisplacement of [3H]Histamine from human histamine H4 receptor transfected in SK-N-MC cells at 100 nM
ChEMBL 327 0 0 4 3.8 CN1CCN(C2=Nc3ccc(Cl)cc3Oc3ccccc32)CC1 10.1021/jm051008s
156015638 178377 None 0 Human Binding pKd = 7.1 7.1 -58 4
Binding affinity to human recombinant NLuc/GPCR-fused H4R expressed in HEK293T cells measured after 30 mins by furimazine substrate based BRET assayBinding affinity to human recombinant NLuc/GPCR-fused H4R expressed in HEK293T cells measured after 30 mins by furimazine substrate based BRET assay
ChEMBL 415 10 1 2 5.5 Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCCCCc1c[nH]cn1 10.1021/acs.jmedchem.0c00160
CHEMBL4642520 178377 None 0 Human Binding pKd = 7.1 7.1 -58 4
Binding affinity to human recombinant NLuc/GPCR-fused H4R expressed in HEK293T cells measured after 30 mins by furimazine substrate based BRET assayBinding affinity to human recombinant NLuc/GPCR-fused H4R expressed in HEK293T cells measured after 30 mins by furimazine substrate based BRET assay
ChEMBL 415 10 1 2 5.5 Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCCCCc1c[nH]cn1 10.1021/acs.jmedchem.0c00160
CHEMBL4650832 178377 None 0 Human Binding pKd = 7.1 7.1 -58 4
Binding affinity to human recombinant NLuc/GPCR-fused H4R expressed in HEK293T cells measured after 30 mins by furimazine substrate based BRET assayBinding affinity to human recombinant NLuc/GPCR-fused H4R expressed in HEK293T cells measured after 30 mins by furimazine substrate based BRET assay
ChEMBL 415 10 1 2 5.5 Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCCCCc1c[nH]cn1 10.1021/acs.jmedchem.0c00160
156015638 178377 None 0 Human Binding pKd = 7.1 7.1 -58 4
Binding affinity to human recombinant NLuc/GPCR-fused H4R expressed in HEK293T cells measured after 30 mins by furimazine substrate based BRET assayBinding affinity to human recombinant NLuc/GPCR-fused H4R expressed in HEK293T cells measured after 30 mins by furimazine substrate based BRET assay
ChEMBL 415 10 1 2 5.5 Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCCCCc1c[nH]cn1 10.1021/acs.jmedchem.0c00160
CHEMBL4642520 178377 None 0 Human Binding pKd = 7.1 7.1 -58 4
Binding affinity to human recombinant NLuc/GPCR-fused H4R expressed in HEK293T cells measured after 30 mins by furimazine substrate based BRET assayBinding affinity to human recombinant NLuc/GPCR-fused H4R expressed in HEK293T cells measured after 30 mins by furimazine substrate based BRET assay
ChEMBL 415 10 1 2 5.5 Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCCCCc1c[nH]cn1 10.1021/acs.jmedchem.0c00160
CHEMBL4650832 178377 None 0 Human Binding pKd = 7.1 7.1 -58 4
Binding affinity to human recombinant NLuc/GPCR-fused H4R expressed in HEK293T cells measured after 30 mins by furimazine substrate based BRET assayBinding affinity to human recombinant NLuc/GPCR-fused H4R expressed in HEK293T cells measured after 30 mins by furimazine substrate based BRET assay
ChEMBL 415 10 1 2 5.5 Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCCCCc1c[nH]cn1 10.1021/acs.jmedchem.0c00160
71525678 89759 None 0 Human Binding pKd = 8.1 8.1 5 6
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells by competitive kinetic analysisDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells by competitive kinetic analysis
ChEMBL 258 3 2 6 0.6 CCc1cnc2c(N3CC(NC)C3)nc(N)nc2c1 10.1016/j.bmcl.2013.02.091
CHEMBL2376800 89759 None 0 Human Binding pKd = 8.1 8.1 5 6
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells by competitive kinetic analysisDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells by competitive kinetic analysis
ChEMBL 258 3 2 6 0.6 CCc1cnc2c(N3CC(NC)C3)nc(N)nc2c1 10.1016/j.bmcl.2013.02.091
156013896 178345 None 0 Human Binding pKd = 8.0 8.0 -7 4
Binding affinity to human recombinant NLuc/GPCR-fused H4R expressed in HEK293T cells assessed as dissociation constant measured after 30 mins in presence of thioperamide by furimazine substrate based BRET assayBinding affinity to human recombinant NLuc/GPCR-fused H4R expressed in HEK293T cells assessed as dissociation constant measured after 30 mins in presence of thioperamide by furimazine substrate based BRET assay
ChEMBL 401 9 1 2 5.1 Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCCCc1c[nH]cn1 10.1021/acs.jmedchem.0c00160
CHEMBL4635634 178345 None 0 Human Binding pKd = 8.0 8.0 -7 4
Binding affinity to human recombinant NLuc/GPCR-fused H4R expressed in HEK293T cells assessed as dissociation constant measured after 30 mins in presence of thioperamide by furimazine substrate based BRET assayBinding affinity to human recombinant NLuc/GPCR-fused H4R expressed in HEK293T cells assessed as dissociation constant measured after 30 mins in presence of thioperamide by furimazine substrate based BRET assay
ChEMBL 401 9 1 2 5.1 Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCCCc1c[nH]cn1 10.1021/acs.jmedchem.0c00160
CHEMBL4650570 178345 None 0 Human Binding pKd = 8.0 8.0 -7 4
Binding affinity to human recombinant NLuc/GPCR-fused H4R expressed in HEK293T cells assessed as dissociation constant measured after 30 mins in presence of thioperamide by furimazine substrate based BRET assayBinding affinity to human recombinant NLuc/GPCR-fused H4R expressed in HEK293T cells assessed as dissociation constant measured after 30 mins in presence of thioperamide by furimazine substrate based BRET assay
ChEMBL 401 9 1 2 5.1 Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCCCc1c[nH]cn1 10.1021/acs.jmedchem.0c00160
54587788 61555 None 0 Human Binding pKi = 10.4 10.4 - 1
Displacement of [3H]histamine from human histamine H4 receptorDisplacement of [3H]histamine from human histamine H4 receptor
ChEMBL 277 4 3 5 1.9 CN[C@@H]1CCN(c2cc(N)nc(NCC(C)(C)C)c2)C1 10.1016/j.bmcl.2011.03.017
CHEMBL1770975 61555 None 0 Human Binding pKi = 10.4 10.4 - 1
Displacement of [3H]histamine from human histamine H4 receptorDisplacement of [3H]histamine from human histamine H4 receptor
ChEMBL 277 4 3 5 1.9 CN[C@@H]1CCN(c2cc(N)nc(NCC(C)(C)C)c2)C1 10.1016/j.bmcl.2011.03.017
23653543 68070 None 0 Human Binding pKi = 10 10.0 - 1
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 317 1 1 6 2.4 CN1CCN(c2nc(N)nc3c2oc2ccc(Cl)cc23)CC1 10.1016/j.bmcl.2011.08.014
CHEMBL1914541 68070 None 0 Human Binding pKi = 10 10.0 - 1
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 317 1 1 6 2.4 CN1CCN(c2nc(N)nc3c2oc2ccc(Cl)cc23)CC1 10.1016/j.bmcl.2011.08.014
54587787 61551 None 0 Human Binding pKi = 9.7 9.7 - 1
Displacement of [3H]histamine from human histamine H4 receptorDisplacement of [3H]histamine from human histamine H4 receptor
ChEMBL 263 5 3 5 1.5 CN[C@@H]1CCN(c2cc(N)nc(NCC(C)C)c2)C1 10.1016/j.bmcl.2011.03.017
CHEMBL1770971 61551 None 0 Human Binding pKi = 9.7 9.7 - 1
Displacement of [3H]histamine from human histamine H4 receptorDisplacement of [3H]histamine from human histamine H4 receptor
ChEMBL 263 5 3 5 1.5 CN[C@@H]1CCN(c2cc(N)nc(NCC(C)C)c2)C1 10.1016/j.bmcl.2011.03.017
46235428 6606 None 0 Human Binding pKi = 9.7 9.7 - 1
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
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 6606 None 0 Human Binding pKi = 9.7 9.7 - 1
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
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
54586763 61548 None 0 Human Binding pKi = 9.5 9.5 - 1
Displacement of [3H]histamine from human histamine H4 receptorDisplacement of [3H]histamine from human histamine H4 receptor
ChEMBL 277 3 2 5 1.9 CN1CCN(c2cc(N)nc(NCC(C)(C)C)c2)CC1 10.1016/j.bmcl.2011.03.017
CHEMBL1770968 61548 None 0 Human Binding pKi = 9.5 9.5 - 1
Displacement of [3H]histamine from human histamine H4 receptorDisplacement of [3H]histamine from human histamine H4 receptor
ChEMBL 277 3 2 5 1.9 CN1CCN(c2cc(N)nc(NCC(C)(C)C)c2)CC1 10.1016/j.bmcl.2011.03.017
24826169 68062 None 0 Human Binding pKi = 9.5 9.5 - 1
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 333 1 1 6 2.8 CN1CCN(c2nc(N)nc3c2sc2ccc(Cl)cc23)CC1 10.1016/j.bmcl.2011.08.014
CHEMBL1914462 68062 None 0 Human Binding pKi = 9.5 9.5 - 1
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 333 1 1 6 2.8 CN1CCN(c2nc(N)nc3c2sc2ccc(Cl)cc23)CC1 10.1016/j.bmcl.2011.08.014
16718567 8164 None 0 Human Binding pKi = 9.4 9.4 - 1
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 317 2 2 6 2.4 CN[C@@H]1CCN(c2nc(N)nc3c2oc2ccc(Cl)cc23)C1 10.1016/j.bmcl.2011.08.014
CHEMBL1091874 8164 None 0 Human Binding pKi = 9.4 9.4 - 1
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 317 2 2 6 2.4 CN[C@@H]1CCN(c2nc(N)nc3c2oc2ccc(Cl)cc23)C1 10.1016/j.bmcl.2011.08.014
24737950 68153 None 0 Human Binding pKi = 9.2 9.2 - 1
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 361 2 2 6 2.5 CN[C@@H]1CCN(c2nc(N)nc3c2oc2ccc(Br)cc23)C1 10.1016/j.bmcl.2011.08.014
CHEMBL1914781 68153 None 0 Human Binding pKi = 9.2 9.2 - 1
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 361 2 2 6 2.5 CN[C@@H]1CCN(c2nc(N)nc3c2oc2ccc(Br)cc23)C1 10.1016/j.bmcl.2011.08.014
58227148 117197 None 0 Human Binding pKi = 9.1 9.1 - 1
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 287 4 2 5 1.9 CN[C@@H]1CCN(c2ccnc(NC3CC4CCC3C4)n2)C1 10.1016/j.bmcl.2014.12.027
CHEMBL3393547 117197 None 0 Human Binding pKi = 9.1 9.1 - 1
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 287 4 2 5 1.9 CN[C@@H]1CCN(c2ccnc(NC3CC4CCC3C4)n2)C1 10.1016/j.bmcl.2014.12.027
57399746 68128 None 0 Human Binding pKi = 9.1 9.1 - 1
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 351 1 1 6 2.7 CN1CCN(c2nc(N)nc3c2oc2ccc(C(F)(F)F)cc23)CC1 10.1016/j.bmcl.2011.08.014
CHEMBL1914755 68128 None 0 Human Binding pKi = 9.1 9.1 - 1
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 351 1 1 6 2.7 CN1CCN(c2nc(N)nc3c2oc2ccc(C(F)(F)F)cc23)CC1 10.1016/j.bmcl.2011.08.014
54580885 61553 None 0 Human Binding pKi = 9.1 9.1 - 1
Displacement of [3H]histamine from human histamine H4 receptorDisplacement of [3H]histamine from human histamine H4 receptor
ChEMBL 275 4 3 5 1.8 CN[C@@H]1CCN(c2cc(N)nc(NC3CCCC3)c2)C1 10.1016/j.bmcl.2011.03.017
CHEMBL1770973 61553 None 0 Human Binding pKi = 9.1 9.1 - 1
Displacement of [3H]histamine from human histamine H4 receptorDisplacement of [3H]histamine from human histamine H4 receptor
ChEMBL 275 4 3 5 1.8 CN[C@@H]1CCN(c2cc(N)nc(NC3CCCC3)c2)C1 10.1016/j.bmcl.2011.03.017
24826766 68123 None 0 Human Binding pKi = 9.1 9.1 - 1
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 317 2 2 6 2.4 CNC1CCN(c2nc(N)nc3c2oc2ccc(Cl)cc23)C1 10.1016/j.bmcl.2011.08.014
CHEMBL1914750 68123 None 0 Human Binding pKi = 9.1 9.1 - 1
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 317 2 2 6 2.4 CNC1CCN(c2nc(N)nc3c2oc2ccc(Cl)cc23)C1 10.1016/j.bmcl.2011.08.014
59777338 110184 None 0 Human Binding pKi = 9.0 9.0 - 1
Displacement of [3H]histamine from human recombinant histamine H4 receptor expressed in SK-N-MC cells after 45 mins by competition binding analysisDisplacement of [3H]histamine from human recombinant histamine H4 receptor expressed in SK-N-MC cells after 45 mins by competition binding analysis
ChEMBL 247 2 2 5 1.3 Nc1nc(C2CCCC2)cc(N2CC[C@@H](N)C2)n1 10.1021/jm401727m
CHEMBL3236556 110184 None 0 Human Binding pKi = 9.0 9.0 - 1
Displacement of [3H]histamine from human recombinant histamine H4 receptor expressed in SK-N-MC cells after 45 mins by competition binding analysisDisplacement of [3H]histamine from human recombinant histamine H4 receptor expressed in SK-N-MC cells after 45 mins by competition binding analysis
ChEMBL 247 2 2 5 1.3 Nc1nc(C2CCCC2)cc(N2CC[C@@H](N)C2)n1 10.1021/jm401727m
1204 1932 None 74 Human Binding pKi = 9 9.0 -3 24
Displacement of [3H]-Histamine from human histamine 4 receptor transfected in HEK293T cells incubated for 16 hrs by liquid scintillation counter analysisDisplacement of [3H]-Histamine from human histamine 4 receptor transfected in HEK293T cells incubated for 16 hrs by liquid scintillation counter analysis
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmc.2020.115924
1247 1932 None 74 Human Binding pKi = 9 9.0 -3 24
Displacement of [3H]-Histamine from human histamine 4 receptor transfected in HEK293T cells incubated for 16 hrs by liquid scintillation counter analysisDisplacement of [3H]-Histamine from human histamine 4 receptor transfected in HEK293T cells incubated for 16 hrs by liquid scintillation counter analysis
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmc.2020.115924
1375 1932 None 74 Human Binding pKi = 9 9.0 -3 24
Displacement of [3H]-Histamine from human histamine 4 receptor transfected in HEK293T cells incubated for 16 hrs by liquid scintillation counter analysisDisplacement of [3H]-Histamine from human histamine 4 receptor transfected in HEK293T cells incubated for 16 hrs by liquid scintillation counter analysis
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmc.2020.115924
774 1932 None 74 Human Binding pKi = 9 9.0 -3 24
Displacement of [3H]-Histamine from human histamine 4 receptor transfected in HEK293T cells incubated for 16 hrs by liquid scintillation counter analysisDisplacement of [3H]-Histamine from human histamine 4 receptor transfected in HEK293T cells incubated for 16 hrs by liquid scintillation counter analysis
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmc.2020.115924
774.0 1932 None 74 Human Binding pKi = 9 9.0 -3 24
Displacement of [3H]-Histamine from human histamine 4 receptor transfected in HEK293T cells incubated for 16 hrs by liquid scintillation counter analysisDisplacement of [3H]-Histamine from human histamine 4 receptor transfected in HEK293T cells incubated for 16 hrs by liquid scintillation counter analysis
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmc.2020.115924
CHEMBL90 1932 None 74 Human Binding pKi = 9 9.0 -3 24
Displacement of [3H]-Histamine from human histamine 4 receptor transfected in HEK293T cells incubated for 16 hrs by liquid scintillation counter analysisDisplacement of [3H]-Histamine from human histamine 4 receptor transfected in HEK293T cells incubated for 16 hrs by liquid scintillation counter analysis
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmc.2020.115924
DB05381 1932 None 74 Human Binding pKi = 9 9.0 -3 24
Displacement of [3H]-Histamine from human histamine 4 receptor transfected in HEK293T cells incubated for 16 hrs by liquid scintillation counter analysisDisplacement of [3H]-Histamine from human histamine 4 receptor transfected in HEK293T cells incubated for 16 hrs by liquid scintillation counter analysis
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmc.2020.115924
1223 953 None 33 Human Binding pKi = 9 9.0 -60 11
Displacement of [3H]histamine from human H4 receptor Q7.42L mutant expressed in HEK293 cells after 1 to 1.5 hrs by scintillation countingDisplacement of [3H]histamine from human H4 receptor Q7.42L mutant expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting
ChEMBL 308 6 2 3 3.2 Clc1ccc(cc1)CN=C(SCCCc1cnc[nH]1)N 10.1021/jm201042n
2790 953 None 33 Human Binding pKi = 9 9.0 -60 11
Displacement of [3H]histamine from human H4 receptor Q7.42L mutant expressed in HEK293 cells after 1 to 1.5 hrs by scintillation countingDisplacement of [3H]histamine from human H4 receptor Q7.42L mutant expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting
ChEMBL 308 6 2 3 3.2 Clc1ccc(cc1)CN=C(SCCCc1cnc[nH]1)N 10.1021/jm201042n
CHEMBL14690 953 None 33 Human Binding pKi = 9 9.0 -60 11
Displacement of [3H]histamine from human H4 receptor Q7.42L mutant expressed in HEK293 cells after 1 to 1.5 hrs by scintillation countingDisplacement of [3H]histamine from human H4 receptor Q7.42L mutant expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting
ChEMBL 308 6 2 3 3.2 Clc1ccc(cc1)CN=C(SCCCc1cnc[nH]1)N 10.1021/jm201042n
54581940 61572 None 0 Human Binding pKi = 9 9.0 - 1
Displacement of [3H]histamine from human histamine H4 receptorDisplacement of [3H]histamine from human histamine H4 receptor
ChEMBL 264 5 3 6 0.9 CN[C@@H]1CCN(c2cc(N)nc(NCC(C)C)n2)C1 10.1016/j.bmcl.2011.03.017
CHEMBL1770992 61572 None 0 Human Binding pKi = 9 9.0 - 1
Displacement of [3H]histamine from human histamine H4 receptorDisplacement of [3H]histamine from human histamine H4 receptor
ChEMBL 264 5 3 6 0.9 CN[C@@H]1CCN(c2cc(N)nc(NCC(C)C)n2)C1 10.1016/j.bmcl.2011.03.017
24797598 61582 None 0 Human Binding pKi = 9 9.0 - 1
Displacement of [3H]histamine from human histamine H4 receptorDisplacement of [3H]histamine from human histamine H4 receptor
ChEMBL 276 3 2 6 1.2 CN1CCN(c2cc(NC3CCCC3)nc(N)n2)CC1 10.1016/j.bmcl.2011.03.017
CHEMBL1771001 61582 None 0 Human Binding pKi = 9 9.0 - 1
Displacement of [3H]histamine from human histamine H4 receptorDisplacement of [3H]histamine from human histamine H4 receptor
ChEMBL 276 3 2 6 1.2 CN1CCN(c2cc(NC3CCCC3)nc(N)n2)CC1 10.1016/j.bmcl.2011.03.017
11224088 136544 None 0 Human Binding pKi = 9 9.0 - 1
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 426 6 1 4 4.9 Cc1cc(C)c2nc(-c3ccc(OCCCN4CCCN(C)CC4)cc3Cl)[nH]c2c1 10.1021/jm800876b
CHEMBL373579 136544 None 0 Human Binding pKi = 9 9.0 - 1
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 426 6 1 4 4.9 Cc1cc(C)c2nc(-c3ccc(OCCCN4CCCN(C)CC4)cc3Cl)[nH]c2c1 10.1021/jm800876b
24798144 110181 None 0 Human Binding pKi = 9 9.0 19 3
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 247 2 2 5 1.1 Nc1nc(C2CCCC2)cc(N2CCNCC2)n1 10.1016/j.bmcl.2014.10.013
CHEMBL3236553 110181 None 0 Human Binding pKi = 9 9.0 19 3
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 247 2 2 5 1.1 Nc1nc(C2CCCC2)cc(N2CCNCC2)n1 10.1016/j.bmcl.2014.10.013
58227342 117184 None 0 Human Binding pKi = 9 9.0 - 1
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 286 4 2 4 2.5 CN[C@@H]1CCN(c2ccnc(NC3CC4CCC3C4)c2)C1 10.1016/j.bmcl.2014.12.027
CHEMBL3393534 117184 None 0 Human Binding pKi = 9 9.0 - 1
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 286 4 2 4 2.5 CN[C@@H]1CCN(c2ccnc(NC3CC4CCC3C4)c2)C1 10.1016/j.bmcl.2014.12.027
11224088 136544 None 0 Human Binding pKi = 9 9.0 - 1
Displacement of [3H]histamine from human recombinant histamine H4 receptor expressed in SK-N-MC cellsDisplacement of [3H]histamine from human recombinant histamine H4 receptor expressed in SK-N-MC cells
ChEMBL 426 6 1 4 4.9 Cc1cc(C)c2nc(-c3ccc(OCCCN4CCCN(C)CC4)cc3Cl)[nH]c2c1 10.1016/j.bmcl.2006.08.117
CHEMBL373579 136544 None 0 Human Binding pKi = 9 9.0 - 1
Displacement of [3H]histamine from human recombinant histamine H4 receptor expressed in SK-N-MC cellsDisplacement of [3H]histamine from human recombinant histamine H4 receptor expressed in SK-N-MC cells
ChEMBL 426 6 1 4 4.9 Cc1cc(C)c2nc(-c3ccc(OCCCN4CCCN(C)CC4)cc3Cl)[nH]c2c1 10.1016/j.bmcl.2006.08.117
24825998 68133 None 0 Human Binding pKi = 9 9.0 - 1
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 377 1 1 6 2.9 CN1CCN(c2nc(N)nc3c2sc2ccc(Br)cc23)CC1 10.1016/j.bmcl.2011.08.014
CHEMBL1914760 68133 None 0 Human Binding pKi = 9 9.0 - 1
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 377 1 1 6 2.9 CN1CCN(c2nc(N)nc3c2sc2ccc(Br)cc23)CC1 10.1016/j.bmcl.2011.08.014
57396301 68155 None 0 Human Binding pKi = 9 9.0 - 1
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 351 2 2 6 2.8 CN[C@@H]1CCN(c2nc(N)nc3c2oc2ccc(C(F)(F)F)cc23)C1 10.1016/j.bmcl.2011.08.014
CHEMBL1914783 68155 None 0 Human Binding pKi = 9 9.0 - 1
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 351 2 2 6 2.8 CN[C@@H]1CCN(c2nc(N)nc3c2oc2ccc(C(F)(F)F)cc23)C1 10.1016/j.bmcl.2011.08.014
127050310 140922 None 0 Human Binding pKi = 9 9.0 - 1
Inhibition of histamine H4 receptor (unknown origin)Inhibition of histamine H4 receptor (unknown origin)
ChEMBL 347 3 2 6 2.9 CN[C@H]1CCN(c2nc(N)nc3c2oc2ccc(C(C)(F)F)cc23)C1 10.1039/C6MD00108D
CHEMBL3819260 140922 None 0 Human Binding pKi = 9 9.0 - 1
Inhibition of histamine H4 receptor (unknown origin)Inhibition of histamine H4 receptor (unknown origin)
ChEMBL 347 3 2 6 2.9 CN[C@H]1CCN(c2nc(N)nc3c2oc2ccc(C(C)(F)F)cc23)C1 10.1039/C6MD00108D
46222048 8986 None 0 Human Binding pKi = 9.0 9.0 -4 13
Displacement of [3H]histamine from human histamine H4 receptor expressed in CHO-K1 cells after 1 hr by liquid scintillation countingDisplacement of [3H]histamine from human histamine H4 receptor expressed in CHO-K1 cells after 1 hr by liquid scintillation counting
ChEMBL 260 4 1 2 4.0 CC(C)(C)c1ccc(SCCc2c[nH]cn2)cc1 10.1016/j.bmc.2010.04.052
CHEMBL1098230 8986 None 0 Human Binding pKi = 9.0 9.0 -4 13
Displacement of [3H]histamine from human histamine H4 receptor expressed in CHO-K1 cells after 1 hr by liquid scintillation countingDisplacement of [3H]histamine from human histamine H4 receptor expressed in CHO-K1 cells after 1 hr by liquid scintillation counting
ChEMBL 260 4 1 2 4.0 CC(C)(C)c1ccc(SCCc2c[nH]cn2)cc1 10.1016/j.bmc.2010.04.052
24994542 110182 None 0 Human Binding pKi = 9.0 9.0 - 1
Displacement of [3H]histamine from human recombinant histamine H4 receptor expressed in SK-N-MC cells after 45 mins by competition binding analysisDisplacement of [3H]histamine from human recombinant histamine H4 receptor expressed in SK-N-MC cells after 45 mins by competition binding analysis
ChEMBL 261 3 2 5 1.5 CN[C@@H]1CCN(c2cc(C3CCCC3)nc(N)n2)C1 10.1021/jm401727m
CHEMBL3236554 110182 None 0 Human Binding pKi = 9.0 9.0 - 1
Displacement of [3H]histamine from human recombinant histamine H4 receptor expressed in SK-N-MC cells after 45 mins by competition binding analysisDisplacement of [3H]histamine from human recombinant histamine H4 receptor expressed in SK-N-MC cells after 45 mins by competition binding analysis
ChEMBL 261 3 2 5 1.5 CN[C@@H]1CCN(c2cc(C3CCCC3)nc(N)n2)C1 10.1021/jm401727m
24948752 68069 None 0 Human Binding pKi = 9.0 9.0 - 1
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 317 1 2 6 2.4 Nc1nc(N2CCCNCC2)c2oc3ccc(Cl)cc3c2n1 10.1016/j.bmcl.2011.08.014
CHEMBL1914540 68069 None 0 Human Binding pKi = 9.0 9.0 - 1
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 317 1 2 6 2.4 Nc1nc(N2CCCNCC2)c2oc3ccc(Cl)cc3c2n1 10.1016/j.bmcl.2011.08.014
24825727 68071 None 0 Human Binding pKi = 9.0 9.0 - 1
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 303 1 2 6 2.0 Nc1nc(N2CCNCC2)c2oc3ccc(Cl)cc3c2n1 10.1016/j.bmcl.2011.08.014
CHEMBL1914542 68071 None 0 Human Binding pKi = 9.0 9.0 - 1
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 303 1 2 6 2.0 Nc1nc(N2CCNCC2)c2oc3ccc(Cl)cc3c2n1 10.1016/j.bmcl.2011.08.014
46222048 8986 None 0 Human Binding pKi = 9.0 9.0 -4 13
Inhibition of human recombinant histamine H4 receptor expressed in CHO cellsInhibition of human recombinant histamine H4 receptor expressed in CHO cells
ChEMBL 260 4 1 2 4.0 CC(C)(C)c1ccc(SCCc2c[nH]cn2)cc1 10.1021/jm901890s
CHEMBL1098230 8986 None 0 Human Binding pKi = 9.0 9.0 -4 13
Inhibition of human recombinant histamine H4 receptor expressed in CHO cellsInhibition of human recombinant histamine H4 receptor expressed in CHO cells
ChEMBL 260 4 1 2 4.0 CC(C)(C)c1ccc(SCCc2c[nH]cn2)cc1 10.1021/jm901890s
155524115 176652 None 0 Human Binding pKi = 8.9 8.9 -2 3
Inhibition of UR-DEBa242 binding to human recombinant NLuc/GPCR-fused H4R expressed in HEK293T cells measured after 30 mins by furimazine substrate based BRET assayInhibition of UR-DEBa242 binding to human recombinant NLuc/GPCR-fused H4R expressed in HEK293T cells measured after 30 mins by furimazine substrate based BRET assay
ChEMBL 286 3 2 5 2.2 CC(C)(C)CNc1nccc(N2CCc3nc[nH]c3C2)n1 10.1021/acs.jmedchem.0c00160
CHEMBL4454158 176652 None 0 Human Binding pKi = 8.9 8.9 -2 3
Inhibition of UR-DEBa242 binding to human recombinant NLuc/GPCR-fused H4R expressed in HEK293T cells measured after 30 mins by furimazine substrate based BRET assayInhibition of UR-DEBa242 binding to human recombinant NLuc/GPCR-fused H4R expressed in HEK293T cells measured after 30 mins by furimazine substrate based BRET assay
ChEMBL 286 3 2 5 2.2 CC(C)(C)CNc1nccc(N2CCc3nc[nH]c3C2)n1 10.1021/acs.jmedchem.0c00160
CHEMBL4597218 176652 None 0 Human Binding pKi = 8.9 8.9 -2 3
Inhibition of UR-DEBa242 binding to human recombinant NLuc/GPCR-fused H4R expressed in HEK293T cells measured after 30 mins by furimazine substrate based BRET assayInhibition of UR-DEBa242 binding to human recombinant NLuc/GPCR-fused H4R expressed in HEK293T cells measured after 30 mins by furimazine substrate based BRET assay
ChEMBL 286 3 2 5 2.2 CC(C)(C)CNc1nccc(N2CCc3nc[nH]c3C2)n1 10.1021/acs.jmedchem.0c00160
24798144 110181 None 0 Human Binding pKi = 8.9 8.9 19 3
Displacement of [3H]histamine from human recombinant histamine H4 receptor expressed in SK-N-MC cells after 45 mins by competition binding analysisDisplacement of [3H]histamine from human recombinant histamine H4 receptor expressed in SK-N-MC cells after 45 mins by competition binding analysis
ChEMBL 247 2 2 5 1.1 Nc1nc(C2CCCC2)cc(N2CCNCC2)n1 10.1021/jm401727m
CHEMBL3236553 110181 None 0 Human Binding pKi = 8.9 8.9 19 3
Displacement of [3H]histamine from human recombinant histamine H4 receptor expressed in SK-N-MC cells after 45 mins by competition binding analysisDisplacement of [3H]histamine from human recombinant histamine H4 receptor expressed in SK-N-MC cells after 45 mins by competition binding analysis
ChEMBL 247 2 2 5 1.1 Nc1nc(C2CCCC2)cc(N2CCNCC2)n1 10.1021/jm401727m
155524115 176652 None 0 Mouse Binding pKi = 8.9 8.9 1 3
Inhibition of UR-DEBa242 binding to mouse recombinant NLuc/GPCR-fused H4R expressed in HEK293T cells measured after 30 mins by furimazine substrate based BRET assayInhibition of UR-DEBa242 binding to mouse recombinant NLuc/GPCR-fused H4R expressed in HEK293T cells measured after 30 mins by furimazine substrate based BRET assay
ChEMBL 286 3 2 5 2.2 CC(C)(C)CNc1nccc(N2CCc3nc[nH]c3C2)n1 10.1021/acs.jmedchem.0c00160
CHEMBL4454158 176652 None 0 Mouse Binding pKi = 8.9 8.9 1 3
Inhibition of UR-DEBa242 binding to mouse recombinant NLuc/GPCR-fused H4R expressed in HEK293T cells measured after 30 mins by furimazine substrate based BRET assayInhibition of UR-DEBa242 binding to mouse recombinant NLuc/GPCR-fused H4R expressed in HEK293T cells measured after 30 mins by furimazine substrate based BRET assay
ChEMBL 286 3 2 5 2.2 CC(C)(C)CNc1nccc(N2CCc3nc[nH]c3C2)n1 10.1021/acs.jmedchem.0c00160
CHEMBL4597218 176652 None 0 Mouse Binding pKi = 8.9 8.9 1 3
Inhibition of UR-DEBa242 binding to mouse recombinant NLuc/GPCR-fused H4R expressed in HEK293T cells measured after 30 mins by furimazine substrate based BRET assayInhibition of UR-DEBa242 binding to mouse recombinant NLuc/GPCR-fused H4R expressed in HEK293T cells measured after 30 mins by furimazine substrate based BRET assay
ChEMBL 286 3 2 5 2.2 CC(C)(C)CNc1nccc(N2CCc3nc[nH]c3C2)n1 10.1021/acs.jmedchem.0c00160
24797604 110180 None 0 Human Binding pKi = 8.9 8.9 - 1
Displacement of [3H]histamine from human recombinant histamine H4 receptor expressed in SK-N-MC cells after 45 mins by competition binding analysisDisplacement of [3H]histamine from human recombinant histamine H4 receptor expressed in SK-N-MC cells after 45 mins by competition binding analysis
ChEMBL 261 2 1 5 1.5 CN1CCN(c2cc(C3CCCC3)nc(N)n2)CC1 10.1021/jm401727m
CHEMBL3236552 110180 None 0 Human Binding pKi = 8.9 8.9 - 1
Displacement of [3H]histamine from human recombinant histamine H4 receptor expressed in SK-N-MC cells after 45 mins by competition binding analysisDisplacement of [3H]histamine from human recombinant histamine H4 receptor expressed in SK-N-MC cells after 45 mins by competition binding analysis
ChEMBL 261 2 1 5 1.5 CN1CCN(c2cc(C3CCCC3)nc(N)n2)CC1 10.1021/jm401727m
44231618 5892 None 0 Rat Binding pKi = 8.8 8.8 1 4
Displacement of [3H]-histamine from rat histamine H4 receptor after 1 hr by liquid scintillation countingDisplacement of [3H]-histamine from rat histamine H4 receptor after 1 hr by liquid scintillation counting
ChEMBL 287 2 2 5 1.6 CNC1CN(c2nc(N)nc3c2CCCC32CCCC2)C1 10.1016/j.bmcl.2010.01.131
CHEMBL1079516 5892 None 0 Rat Binding pKi = 8.8 8.8 1 4
Displacement of [3H]-histamine from rat histamine H4 receptor after 1 hr by liquid scintillation countingDisplacement of [3H]-histamine from rat histamine H4 receptor after 1 hr by liquid scintillation counting
ChEMBL 287 2 2 5 1.6 CNC1CN(c2nc(N)nc3c2CCCC32CCCC2)C1 10.1016/j.bmcl.2010.01.131
25128824 193287 None 0 Rat Binding pKi = 8.8 8.8 3 2
Displacement of [3H]histamine from rat histamine H4 receptor expressed in HEK293 cellsDisplacement of [3H]histamine from rat histamine H4 receptor expressed in HEK293 cells
ChEMBL 313 1 2 5 1.8 Nc1nc2c(c(N3CCNCC3)n1)CCCc1ccc(F)cc1-2 10.1021/jm800670r
CHEMBL523225 193287 None 0 Rat Binding pKi = 8.8 8.8 3 2
Displacement of [3H]histamine from rat histamine H4 receptor expressed in HEK293 cellsDisplacement of [3H]histamine from rat histamine H4 receptor expressed in HEK293 cells
ChEMBL 313 1 2 5 1.8 Nc1nc2c(c(N3CCNCC3)n1)CCCc1ccc(F)cc1-2 10.1021/jm800670r
24992077 110199 None 0 Human Binding pKi = 8.8 8.8 - 1
Displacement of [3H]histamine from human recombinant histamine H4 receptor expressed in SK-N-MC cells after 45 mins by competition binding analysisDisplacement of [3H]histamine from human recombinant histamine H4 receptor expressed in SK-N-MC cells after 45 mins by competition binding analysis
ChEMBL 249 5 2 5 1.2 CCCCc1cc(N2CC[C@@H](NC)C2)nc(N)n1 10.1021/jm401727m
CHEMBL3236571 110199 None 0 Human Binding pKi = 8.8 8.8 - 1
Displacement of [3H]histamine from human recombinant histamine H4 receptor expressed in SK-N-MC cells after 45 mins by competition binding analysisDisplacement of [3H]histamine from human recombinant histamine H4 receptor expressed in SK-N-MC cells after 45 mins by competition binding analysis
ChEMBL 249 5 2 5 1.2 CCCCc1cc(N2CC[C@@H](NC)C2)nc(N)n1 10.1021/jm401727m
44231618 5892 None 0 Human Binding pKi = 8.8 8.8 -1 4
Displacement of [3H]-histamine from human histamine H4 receptor expressed in HEK293 cells after 1 hr by liquid scintillation countingDisplacement of [3H]-histamine from human histamine H4 receptor expressed in HEK293 cells after 1 hr by liquid scintillation counting
ChEMBL 287 2 2 5 1.6 CNC1CN(c2nc(N)nc3c2CCCC32CCCC2)C1 10.1016/j.bmcl.2010.01.131
CHEMBL1079516 5892 None 0 Human Binding pKi = 8.8 8.8 -1 4
Displacement of [3H]-histamine from human histamine H4 receptor expressed in HEK293 cells after 1 hr by liquid scintillation countingDisplacement of [3H]-histamine from human histamine H4 receptor expressed in HEK293 cells after 1 hr by liquid scintillation counting
ChEMBL 287 2 2 5 1.6 CNC1CN(c2nc(N)nc3c2CCCC32CCCC2)C1 10.1016/j.bmcl.2010.01.131
44129130 202012 None 0 Rat Binding pKi = 8.8 8.8 2 2
Binding affinity to rat histamine H4 receptorBinding affinity to rat histamine H4 receptor
ChEMBL 460 7 2 7 2.9 CN1CCN(c2nc(NCCS(=O)(=O)Nc3ccccc3)c3cc(Cl)ccc3n2)CC1 10.1021/jm901379s
CHEMBL592379 202012 None 0 Rat Binding pKi = 8.8 8.8 2 2
Binding affinity to rat histamine H4 receptorBinding affinity to rat histamine H4 receptor
ChEMBL 460 7 2 7 2.9 CN1CCN(c2nc(NCCS(=O)(=O)Nc3ccccc3)c3cc(Cl)ccc3n2)CC1 10.1021/jm901379s
1223 953 None 33 Human Binding pKi = 8.8 8.8 -60 11
Displacement of [3H]histamine from human H4 receptor T6.55M mutant expressed in HEK293 cells after 1 to 1.5 hrs by scintillation countingDisplacement of [3H]histamine from human H4 receptor T6.55M mutant expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting
ChEMBL 308 6 2 3 3.2 Clc1ccc(cc1)CN=C(SCCCc1cnc[nH]1)N 10.1021/jm201042n
2790 953 None 33 Human Binding pKi = 8.8 8.8 -60 11
Displacement of [3H]histamine from human H4 receptor T6.55M mutant expressed in HEK293 cells after 1 to 1.5 hrs by scintillation countingDisplacement of [3H]histamine from human H4 receptor T6.55M mutant expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting
ChEMBL 308 6 2 3 3.2 Clc1ccc(cc1)CN=C(SCCCc1cnc[nH]1)N 10.1021/jm201042n
CHEMBL14690 953 None 33 Human Binding pKi = 8.8 8.8 -60 11
Displacement of [3H]histamine from human H4 receptor T6.55M mutant expressed in HEK293 cells after 1 to 1.5 hrs by scintillation countingDisplacement of [3H]histamine from human H4 receptor T6.55M mutant expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting
ChEMBL 308 6 2 3 3.2 Clc1ccc(cc1)CN=C(SCCCc1cnc[nH]1)N 10.1021/jm201042n
44187557 197955 None 0 Human Binding pKi = 8.8 8.8 3 2
Displacement of [3H]histamine from human histamine H4 receptor expressed in human SK-N-MC cells by liquid scintillation countingDisplacement of [3H]histamine from human histamine H4 receptor expressed in human SK-N-MC cells by liquid scintillation counting
ChEMBL 342 6 3 3 4.1 N=C(NCc1ccc(Cl)c(Cl)c1)SCCCc1c[nH]cn1 10.1016/j.bmc.2009.04.007
CHEMBL1202332 197955 None 0 Human Binding pKi = 8.8 8.8 3 2
Displacement of [3H]histamine from human histamine H4 receptor expressed in human SK-N-MC cells by liquid scintillation countingDisplacement of [3H]histamine from human histamine H4 receptor expressed in human SK-N-MC cells by liquid scintillation counting
ChEMBL 342 6 3 3 4.1 N=C(NCc1ccc(Cl)c(Cl)c1)SCCCc1c[nH]cn1 10.1016/j.bmc.2009.04.007
CHEMBL553423 197955 None 0 Human Binding pKi = 8.8 8.8 3 2
Displacement of [3H]histamine from human histamine H4 receptor expressed in human SK-N-MC cells by liquid scintillation countingDisplacement of [3H]histamine from human histamine H4 receptor expressed in human SK-N-MC cells by liquid scintillation counting
ChEMBL 342 6 3 3 4.1 N=C(NCc1ccc(Cl)c(Cl)c1)SCCCc1c[nH]cn1 10.1016/j.bmc.2009.04.007
1204 1932 None 74 Human Binding pKi = 8.8 8.8 -3 24
Binding affinity to histamine H4 receptor (unknown origin)Binding affinity to histamine H4 receptor (unknown origin)
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmcl.2016.09.049
1247 1932 None 74 Human Binding pKi = 8.8 8.8 -3 24
Binding affinity to histamine H4 receptor (unknown origin)Binding affinity to histamine H4 receptor (unknown origin)
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmcl.2016.09.049
1375 1932 None 74 Human Binding pKi = 8.8 8.8 -3 24
Binding affinity to histamine H4 receptor (unknown origin)Binding affinity to histamine H4 receptor (unknown origin)
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmcl.2016.09.049
774 1932 None 74 Human Binding pKi = 8.8 8.8 -3 24
Binding affinity to histamine H4 receptor (unknown origin)Binding affinity to histamine H4 receptor (unknown origin)
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmcl.2016.09.049
774.0 1932 None 74 Human Binding pKi = 8.8 8.8 -3 24
Binding affinity to histamine H4 receptor (unknown origin)Binding affinity to histamine H4 receptor (unknown origin)
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmcl.2016.09.049
CHEMBL90 1932 None 74 Human Binding pKi = 8.8 8.8 -3 24
Binding affinity to histamine H4 receptor (unknown origin)Binding affinity to histamine H4 receptor (unknown origin)
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmcl.2016.09.049
DB05381 1932 None 74 Human Binding pKi = 8.8 8.8 -3 24
Binding affinity to histamine H4 receptor (unknown origin)Binding affinity to histamine H4 receptor (unknown origin)
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmcl.2016.09.049
11957573 2010 None 25 Human Binding pKi = 8.8 8.8 -38 7
Displacement of [3H]histamine from human full-length histamine H4 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]histamine from human full-length histamine H4 receptor expressed in HEK293 cells after 60 mins
ChEMBL 170 3 3 3 0.6 NC(=N)SCCc1cnc[nH]1 10.1016/j.bmc.2011.03.046
1250 2010 None 25 Human Binding pKi = 8.8 8.8 -38 7
Displacement of [3H]histamine from human full-length histamine H4 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]histamine from human full-length histamine H4 receptor expressed in HEK293 cells after 60 mins
ChEMBL 170 3 3 3 0.6 NC(=N)SCCc1cnc[nH]1 10.1016/j.bmc.2011.03.046
3692 2010 None 25 Human Binding pKi = 8.8 8.8 -38 7
Displacement of [3H]histamine from human full-length histamine H4 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]histamine from human full-length histamine H4 receptor expressed in HEK293 cells after 60 mins
ChEMBL 170 3 3 3 0.6 NC(=N)SCCc1cnc[nH]1 10.1016/j.bmc.2011.03.046
CHEMBL19439 2010 None 25 Human Binding pKi = 8.8 8.8 -38 7
Displacement of [3H]histamine from human full-length histamine H4 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]histamine from human full-length histamine H4 receptor expressed in HEK293 cells after 60 mins
ChEMBL 170 3 3 3 0.6 NC(=N)SCCc1cnc[nH]1 10.1016/j.bmc.2011.03.046
16202258 68240 None 0 Human Binding pKi = 8.8 8.8 - 1
Displacement of [3H]-histamine from full length human H4R expressed in HEK293 cellsDisplacement of [3H]-histamine from full length human H4R expressed in HEK293 cells
ChEMBL 264 4 3 6 0.9 CNC1CN(c2cc(NCC(C)(C)C)nc(N)n2)C1 10.1016/j.bmcl.2011.07.125
CHEMBL1915536 68240 None 0 Human Binding pKi = 8.8 8.8 - 1
Displacement of [3H]-histamine from full length human H4R expressed in HEK293 cellsDisplacement of [3H]-histamine from full length human H4R expressed in HEK293 cells
ChEMBL 264 4 3 6 0.9 CNC1CN(c2cc(NCC(C)(C)C)nc(N)n2)C1 10.1016/j.bmcl.2011.07.125
66740859 110207 None 0 Human Binding pKi = 8.8 8.8 - 1
Displacement of [3H]histamine from human recombinant histamine H4 receptor expressed in SK-N-MC cells after 45 mins by competition binding analysisDisplacement of [3H]histamine from human recombinant histamine H4 receptor expressed in SK-N-MC cells after 45 mins by competition binding analysis
ChEMBL 327 3 2 5 2.3 CN[C@@H]1CCN(c2cc(C34CC5CC(CC(C5)C3)C4)nc(N)n2)C1 10.1021/jm401727m
CHEMBL3236579 110207 None 0 Human Binding pKi = 8.8 8.8 - 1
Displacement of [3H]histamine from human recombinant histamine H4 receptor expressed in SK-N-MC cells after 45 mins by competition binding analysisDisplacement of [3H]histamine from human recombinant histamine H4 receptor expressed in SK-N-MC cells after 45 mins by competition binding analysis
ChEMBL 327 3 2 5 2.3 CN[C@@H]1CCN(c2cc(C34CC5CC(CC(C5)C3)C4)nc(N)n2)C1 10.1021/jm401727m
24798232 110188 None 0 Human Binding pKi = 8.7 8.7 - 1
Displacement of [3H]histamine from human recombinant histamine H4 receptor expressed in SK-N-MC cells after 45 mins by competition binding analysisDisplacement of [3H]histamine from human recombinant histamine H4 receptor expressed in SK-N-MC cells after 45 mins by competition binding analysis
ChEMBL 287 2 2 5 1.9 Nc1nc(C2CCCC2)cc(N2C[C@H]3CCCN[C@H]3C2)n1 10.1021/jm401727m
CHEMBL3236560 110188 None 0 Human Binding pKi = 8.7 8.7 - 1
Displacement of [3H]histamine from human recombinant histamine H4 receptor expressed in SK-N-MC cells after 45 mins by competition binding analysisDisplacement of [3H]histamine from human recombinant histamine H4 receptor expressed in SK-N-MC cells after 45 mins by competition binding analysis
ChEMBL 287 2 2 5 1.9 Nc1nc(C2CCCC2)cc(N2C[C@H]3CCCN[C@H]3C2)n1 10.1021/jm401727m
44231735 7787 None 0 Human Binding pKi = 8.7 8.7 1 4
Displacement of [3H]-histamine from human histamine H4 receptor expressed in HEK293 cells after 1 hr by liquid scintillation countingDisplacement of [3H]-histamine from human histamine H4 receptor expressed in HEK293 cells after 1 hr by liquid scintillation counting
ChEMBL 301 2 2 5 2.0 CN[C@@H]1CCN(c2nc(N)nc3c2CCCC32CCCC2)C1 10.1016/j.bmcl.2010.01.131
CHEMBL1089390 7787 None 0 Human Binding pKi = 8.7 8.7 1 4
Displacement of [3H]-histamine from human histamine H4 receptor expressed in HEK293 cells after 1 hr by liquid scintillation countingDisplacement of [3H]-histamine from human histamine H4 receptor expressed in HEK293 cells after 1 hr by liquid scintillation counting
ChEMBL 301 2 2 5 2.0 CN[C@@H]1CCN(c2nc(N)nc3c2CCCC32CCCC2)C1 10.1016/j.bmcl.2010.01.131
25129527 187520 None 0 Human Binding pKi = 8.7 8.7 - 1
Displacement of [3H]histamine from wild type human histamine H4 receptor transfected in HEK293T cells after 1.5 hrs by liquid scintillation counting analysisDisplacement of [3H]histamine from wild type human histamine H4 receptor transfected in HEK293T cells after 1.5 hrs by liquid scintillation counting analysis
ChEMBL 303 2 1 5 2.1 CN1CCN(c2cc(-c3ccc(Cl)cc3)nc(N)n2)CC1 10.1039/C2MD20212C
CHEMBL493720 187520 None 0 Human Binding pKi = 8.7 8.7 - 1
Displacement of [3H]histamine from wild type human histamine H4 receptor transfected in HEK293T cells after 1.5 hrs by liquid scintillation counting analysisDisplacement of [3H]histamine from wild type human histamine H4 receptor transfected in HEK293T cells after 1.5 hrs by liquid scintillation counting analysis
ChEMBL 303 2 1 5 2.1 CN1CCN(c2cc(-c3ccc(Cl)cc3)nc(N)n2)CC1 10.1039/C2MD20212C
25217643 112233 None 0 Human Binding pKi = 8 8.0 - 1
Binding affinity to histamine H4 receptor (unknown origin) assessed as inhibition constantBinding affinity to histamine H4 receptor (unknown origin) assessed as inhibition constant
ChEMBL 289 2 0 5 1.9 CN1CCN(c2ncnc(-c3ccc(Cl)cc3)n2)CC1 10.1016/j.ejmech.2023.115151
CHEMBL3290570 112233 None 0 Human Binding pKi = 8 8.0 - 1
Binding affinity to histamine H4 receptor (unknown origin) assessed as inhibition constantBinding affinity to histamine H4 receptor (unknown origin) assessed as inhibition constant
ChEMBL 289 2 0 5 1.9 CN1CCN(c2ncnc(-c3ccc(Cl)cc3)n2)CC1 10.1016/j.ejmech.2023.115151
135525668 68234 None 0 Human Binding pKi = 8 8.0 263 2
Displacement of [3H]-histamine from full length human H4R expressed in HEK293 cellsDisplacement of [3H]-histamine from full length human H4R expressed in HEK293 cells
ChEMBL 305 1 2 3 1.7 CN1C[C@H]2CN(C(=N)c3nc4cc(F)c(F)cc4[nH]3)C[C@H]2C1 10.1016/j.bmcl.2011.07.125
CHEMBL1915348 68234 None 0 Human Binding pKi = 8 8.0 263 2
Displacement of [3H]-histamine from full length human H4R expressed in HEK293 cellsDisplacement of [3H]-histamine from full length human H4R expressed in HEK293 cells
ChEMBL 305 1 2 3 1.7 CN1C[C@H]2CN(C(=N)c3nc4cc(F)c(F)cc4[nH]3)C[C@H]2C1 10.1016/j.bmcl.2011.07.125
25217643 112233 None 0 Human Binding pKi = 8 8.0 - 1
Displacement of [3H]-histamine from human histamine H4 receptor after 45 mins by scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor after 45 mins by scintillation counting analysis
ChEMBL 289 2 0 5 1.9 CN1CCN(c2ncnc(-c3ccc(Cl)cc3)n2)CC1 10.1016/j.ejmech.2014.06.032
CHEMBL3290570 112233 None 0 Human Binding pKi = 8 8.0 - 1
Displacement of [3H]-histamine from human histamine H4 receptor after 45 mins by scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor after 45 mins by scintillation counting analysis
ChEMBL 289 2 0 5 1.9 CN1CCN(c2ncnc(-c3ccc(Cl)cc3)n2)CC1 10.1016/j.ejmech.2014.06.032
1249 2009 None 10 Human Binding pKi = 8 8.0 -3 3
Displacement of [3H]-histamine from human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2Displacement of [3H]-histamine from human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2
ChEMBL 139 4 2 2 0.7 NCCCCc1cnc[nH]1 10.1016/j.bmcl.2010.10.041
13499360 2009 None 10 Human Binding pKi = 8 8.0 -3 3
Displacement of [3H]-histamine from human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2Displacement of [3H]-histamine from human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2
ChEMBL 139 4 2 2 0.7 NCCCCc1cnc[nH]1 10.1016/j.bmcl.2010.10.041
CHEMBL90019 2009 None 10 Human Binding pKi = 8 8.0 -3 3
Displacement of [3H]-histamine from human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2Displacement of [3H]-histamine from human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2
ChEMBL 139 4 2 2 0.7 NCCCCc1cnc[nH]1 10.1016/j.bmcl.2010.10.041
10176414 4063 None 15 Human Binding pKi = 8 8.0 -3 3
Displacement of [3H]-histamine from human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2Displacement of [3H]-histamine from human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2
ChEMBL 184 4 3 3 1.0 NC(=N)SCCCc1cnc[nH]1 10.1016/j.bmcl.2010.10.041
1246 4063 None 15 Human Binding pKi = 8 8.0 -3 3
Displacement of [3H]-histamine from human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2Displacement of [3H]-histamine from human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2
ChEMBL 184 4 3 3 1.0 NC(=N)SCCCc1cnc[nH]1 10.1016/j.bmcl.2010.10.041
CHEMBL281576 4063 None 15 Human Binding pKi = 8 8.0 -3 3
Displacement of [3H]-histamine from human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2Displacement of [3H]-histamine from human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2
ChEMBL 184 4 3 3 1.0 NC(=N)SCCCc1cnc[nH]1 10.1016/j.bmcl.2010.10.041
10060212 206992 None 0 Human Binding pKi = 8 8.0 5 2
Displacement of [3H]-histamine from human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2Displacement of [3H]-histamine from human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2
ChEMBL 240 7 3 2 2.0 CCC/N=C(\S)NCCCCc1c[nH]cn1 10.1016/j.bmcl.2010.10.041
CHEMBL72769 206992 None 0 Human Binding pKi = 8 8.0 5 2
Displacement of [3H]-histamine from human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2Displacement of [3H]-histamine from human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2
ChEMBL 240 7 3 2 2.0 CCC/N=C(\S)NCCCCc1c[nH]cn1 10.1016/j.bmcl.2010.10.041
71681807 89680 None 0 Human Binding pKi = 8 8.0 - 1
Displacement of [3H]histamine displacement from human histamine H4 receptor expressed in SK-NM-C cells after 60 minsDisplacement of [3H]histamine displacement from human histamine H4 receptor expressed in SK-NM-C cells after 60 mins
ChEMBL 330 8 3 8 1.6 CC(C)CCc1cc(N(C)CCNc2ccnc(N)n2)nc(N)n1 10.1021/jm301886t
CHEMBL2375668 89680 None 0 Human Binding pKi = 8 8.0 - 1
Displacement of [3H]histamine displacement from human histamine H4 receptor expressed in SK-NM-C cells after 60 minsDisplacement of [3H]histamine displacement from human histamine H4 receptor expressed in SK-NM-C cells after 60 mins
ChEMBL 330 8 3 8 1.6 CC(C)CCc1cc(N(C)CCNc2ccnc(N)n2)nc(N)n1 10.1021/jm301886t
71681804 89705 None 0 Human Binding pKi = 8 8.0 - 1
Displacement of [3H]histamine displacement from human histamine H4 receptor expressed in SK-NM-C cells after 60 minsDisplacement of [3H]histamine displacement from human histamine H4 receptor expressed in SK-NM-C cells after 60 mins
ChEMBL 336 6 3 8 1.6 CN(CCNc1ccnc(N)n1)c1cc(-c2ccccc2)nc(N)n1 10.1021/jm301886t
CHEMBL2375770 89705 None 0 Human Binding pKi = 8 8.0 - 1
Displacement of [3H]histamine displacement from human histamine H4 receptor expressed in SK-NM-C cells after 60 minsDisplacement of [3H]histamine displacement from human histamine H4 receptor expressed in SK-NM-C cells after 60 mins
ChEMBL 336 6 3 8 1.6 CN(CCNc1ccnc(N)n1)c1cc(-c2ccccc2)nc(N)n1 10.1021/jm301886t
1223 953 None 33 Human Binding pKi = 8 8.0 -60 11
Displacement of [3H]histamine from human H4 receptor V3.40A mutant expressed in HEK293 cells after 1 to 1.5 hrs by scintillation countingDisplacement of [3H]histamine from human H4 receptor V3.40A mutant expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting
ChEMBL 308 6 2 3 3.2 Clc1ccc(cc1)CN=C(SCCCc1cnc[nH]1)N 10.1021/jm201042n
2790 953 None 33 Human Binding pKi = 8 8.0 -60 11
Displacement of [3H]histamine from human H4 receptor V3.40A mutant expressed in HEK293 cells after 1 to 1.5 hrs by scintillation countingDisplacement of [3H]histamine from human H4 receptor V3.40A mutant expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting
ChEMBL 308 6 2 3 3.2 Clc1ccc(cc1)CN=C(SCCCc1cnc[nH]1)N 10.1021/jm201042n
CHEMBL14690 953 None 33 Human Binding pKi = 8 8.0 -60 11
Displacement of [3H]histamine from human H4 receptor V3.40A mutant expressed in HEK293 cells after 1 to 1.5 hrs by scintillation countingDisplacement of [3H]histamine from human H4 receptor V3.40A mutant expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting
ChEMBL 308 6 2 3 3.2 Clc1ccc(cc1)CN=C(SCCCc1cnc[nH]1)N 10.1021/jm201042n
1223 953 None 33 Human Binding pKi = 8 8.0 -60 11
Displacement of [3H]histamine from human H4 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation countingDisplacement of [3H]histamine from human H4 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting
ChEMBL 308 6 2 3 3.2 Clc1ccc(cc1)CN=C(SCCCc1cnc[nH]1)N 10.1021/jm201042n
2790 953 None 33 Human Binding pKi = 8 8.0 -60 11
Displacement of [3H]histamine from human H4 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation countingDisplacement of [3H]histamine from human H4 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting
ChEMBL 308 6 2 3 3.2 Clc1ccc(cc1)CN=C(SCCCc1cnc[nH]1)N 10.1021/jm201042n
CHEMBL14690 953 None 33 Human Binding pKi = 8 8.0 -60 11
Displacement of [3H]histamine from human H4 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation countingDisplacement of [3H]histamine from human H4 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting
ChEMBL 308 6 2 3 3.2 Clc1ccc(cc1)CN=C(SCCCc1cnc[nH]1)N 10.1021/jm201042n
1249 2009 None 10 Human Binding pKi = 8 8.0 -3 3
Displacement of [3H]histamine from human H4 receptor expressed in SK-N-MC cellsDisplacement of [3H]histamine from human H4 receptor expressed in SK-N-MC cells
ChEMBL 139 4 2 2 0.7 NCCCCc1cnc[nH]1 10.1021/jm0504353
13499360 2009 None 10 Human Binding pKi = 8 8.0 -3 3
Displacement of [3H]histamine from human H4 receptor expressed in SK-N-MC cellsDisplacement of [3H]histamine from human H4 receptor expressed in SK-N-MC cells
ChEMBL 139 4 2 2 0.7 NCCCCc1cnc[nH]1 10.1021/jm0504353
CHEMBL90019 2009 None 10 Human Binding pKi = 8 8.0 -3 3
Displacement of [3H]histamine from human H4 receptor expressed in SK-N-MC cellsDisplacement of [3H]histamine from human H4 receptor expressed in SK-N-MC cells
ChEMBL 139 4 2 2 0.7 NCCCCc1cnc[nH]1 10.1021/jm0504353
53233802 61567 None 0 Human Binding pKi = 8 8.0 - 1
Displacement of [3H]histamine from human histamine H4 receptorDisplacement of [3H]histamine from human histamine H4 receptor
ChEMBL 276 3 2 6 1.2 CN1CCN(c2cc(N)nc(NC3CCCC3)n2)CC1 10.1016/j.bmcl.2011.03.017
CHEMBL1770987 61567 None 0 Human Binding pKi = 8 8.0 - 1
Displacement of [3H]histamine from human histamine H4 receptorDisplacement of [3H]histamine from human histamine H4 receptor
ChEMBL 276 3 2 6 1.2 CN1CCN(c2cc(N)nc(NC3CCCC3)n2)CC1 10.1016/j.bmcl.2011.03.017
70692529 75710 None 0 Human Binding pKi = 8 8.0 - 1
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 303 2 1 2 2.7 O=C(c1cc2cc(Cl)ccc2[nH]1)N1CC(N2CCCC2)C1 10.1016/j.ejmech.2012.06.016
CHEMBL2047466 75710 None 0 Human Binding pKi = 8 8.0 - 1
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 303 2 1 2 2.7 O=C(c1cc2cc(Cl)ccc2[nH]1)N1CC(N2CCCC2)C1 10.1016/j.ejmech.2012.06.016
46228994 201885 None 0 Human Binding pKi = 8 8.0 - 1
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells
ChEMBL 466 6 1 7 2.7 CC1CCCCN1S(=O)(=O)CCNc1nc(N2CCN(C)CC2)nc2ccc(Cl)cc12 10.1021/jm901379s
CHEMBL591249 201885 None 0 Human Binding pKi = 8 8.0 - 1
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells
ChEMBL 466 6 1 7 2.7 CC1CCCCN1S(=O)(=O)CCNc1nc(N2CCN(C)CC2)nc2ccc(Cl)cc12 10.1021/jm901379s
1223 953 None 33 Human Binding pKi = 8 8.0 -60 11
Displacement of [3H]histamine from human histamine H4 receptor expressed in human SK-N-MC cells by liquid scintillation countingDisplacement of [3H]histamine from human histamine H4 receptor expressed in human SK-N-MC cells by liquid scintillation counting
ChEMBL 308 6 2 3 3.2 Clc1ccc(cc1)CN=C(SCCCc1cnc[nH]1)N 10.1016/j.bmc.2009.04.007
2790 953 None 33 Human Binding pKi = 8 8.0 -60 11
Displacement of [3H]histamine from human histamine H4 receptor expressed in human SK-N-MC cells by liquid scintillation countingDisplacement of [3H]histamine from human histamine H4 receptor expressed in human SK-N-MC cells by liquid scintillation counting
ChEMBL 308 6 2 3 3.2 Clc1ccc(cc1)CN=C(SCCCc1cnc[nH]1)N 10.1016/j.bmc.2009.04.007
CHEMBL14690 953 None 33 Human Binding pKi = 8 8.0 -60 11
Displacement of [3H]histamine from human histamine H4 receptor expressed in human SK-N-MC cells by liquid scintillation countingDisplacement of [3H]histamine from human histamine H4 receptor expressed in human SK-N-MC cells by liquid scintillation counting
ChEMBL 308 6 2 3 3.2 Clc1ccc(cc1)CN=C(SCCCc1cnc[nH]1)N 10.1016/j.bmc.2009.04.007
45268092 198470 None 0 Human Binding pKi = 8 8.0 -3 2
Displacement of [3H]histamine from human histamine H4 receptor expressed in human SK-N-MC cells by liquid scintillation countingDisplacement of [3H]histamine from human histamine H4 receptor expressed in human SK-N-MC cells by liquid scintillation counting
ChEMBL 352 6 3 3 3.6 N=C(NCc1ccc(Br)cc1)SCCCc1c[nH]cn1 10.1016/j.bmc.2009.04.007
CHEMBL1743881 198470 None 0 Human Binding pKi = 8 8.0 -3 2
Displacement of [3H]histamine from human histamine H4 receptor expressed in human SK-N-MC cells by liquid scintillation countingDisplacement of [3H]histamine from human histamine H4 receptor expressed in human SK-N-MC cells by liquid scintillation counting
ChEMBL 352 6 3 3 3.6 N=C(NCc1ccc(Br)cc1)SCCCc1c[nH]cn1 10.1016/j.bmc.2009.04.007
CHEMBL560111 198470 None 0 Human Binding pKi = 8 8.0 -3 2
Displacement of [3H]histamine from human histamine H4 receptor expressed in human SK-N-MC cells by liquid scintillation countingDisplacement of [3H]histamine from human histamine H4 receptor expressed in human SK-N-MC cells by liquid scintillation counting
ChEMBL 352 6 3 3 3.6 N=C(NCc1ccc(Br)cc1)SCCCc1c[nH]cn1 10.1016/j.bmc.2009.04.007
45268093 198471 None 0 Human Binding pKi = 8 8.0 -3 2
Displacement of [3H]histamine from human histamine H4 receptor expressed in human SK-N-MC cells by liquid scintillation countingDisplacement of [3H]histamine from human histamine H4 receptor expressed in human SK-N-MC cells by liquid scintillation counting
ChEMBL 400 6 3 3 3.4 N=C(NCc1ccc(I)cc1)SCCCc1c[nH]cn1 10.1016/j.bmc.2009.04.007
CHEMBL1202321 198471 None 0 Human Binding pKi = 8 8.0 -3 2
Displacement of [3H]histamine from human histamine H4 receptor expressed in human SK-N-MC cells by liquid scintillation countingDisplacement of [3H]histamine from human histamine H4 receptor expressed in human SK-N-MC cells by liquid scintillation counting
ChEMBL 400 6 3 3 3.4 N=C(NCc1ccc(I)cc1)SCCCc1c[nH]cn1 10.1016/j.bmc.2009.04.007
CHEMBL560112 198471 None 0 Human Binding pKi = 8 8.0 -3 2
Displacement of [3H]histamine from human histamine H4 receptor expressed in human SK-N-MC cells by liquid scintillation countingDisplacement of [3H]histamine from human histamine H4 receptor expressed in human SK-N-MC cells by liquid scintillation counting
ChEMBL 400 6 3 3 3.4 N=C(NCc1ccc(I)cc1)SCCCc1c[nH]cn1 10.1016/j.bmc.2009.04.007
45267230 198938 None 0 Human Binding pKi = 8 8.0 -1 2
Displacement of [3H]histamine from human histamine H4 receptor expressed in human SK-N-MC cells by liquid scintillation countingDisplacement of [3H]histamine from human histamine H4 receptor expressed in human SK-N-MC cells by liquid scintillation counting
ChEMBL 308 6 3 3 3.5 N=C(NCc1ccccc1Cl)SCCCc1c[nH]cn1 10.1016/j.bmc.2009.04.007
CHEMBL1202318 198938 None 0 Human Binding pKi = 8 8.0 -1 2
Displacement of [3H]histamine from human histamine H4 receptor expressed in human SK-N-MC cells by liquid scintillation countingDisplacement of [3H]histamine from human histamine H4 receptor expressed in human SK-N-MC cells by liquid scintillation counting
ChEMBL 308 6 3 3 3.5 N=C(NCc1ccccc1Cl)SCCCc1c[nH]cn1 10.1016/j.bmc.2009.04.007
CHEMBL563342 198938 None 0 Human Binding pKi = 8 8.0 -1 2
Displacement of [3H]histamine from human histamine H4 receptor expressed in human SK-N-MC cells by liquid scintillation countingDisplacement of [3H]histamine from human histamine H4 receptor expressed in human SK-N-MC cells by liquid scintillation counting
ChEMBL 308 6 3 3 3.5 N=C(NCc1ccccc1Cl)SCCCc1c[nH]cn1 10.1016/j.bmc.2009.04.007
24737954 68151 None 0 Human Binding pKi = 8 8.0 - 1
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 301 2 2 6 1.9 CN[C@@H]1CCN(c2nc(N)nc3c2oc2cccc(F)c23)C1 10.1016/j.bmcl.2011.08.014
CHEMBL1914778 68151 None 0 Human Binding pKi = 8 8.0 - 1
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 301 2 2 6 1.9 CN[C@@H]1CCN(c2nc(N)nc3c2oc2cccc(F)c23)C1 10.1016/j.bmcl.2011.08.014
24826522 68158 None 0 Human Binding pKi = 8 8.0 - 1
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 351 2 2 6 3.1 CN[C@@H]1CCN(c2nc(N)nc3c2oc2ccc(Cl)c(Cl)c23)C1 10.1016/j.bmcl.2011.08.014
CHEMBL1914786 68158 None 0 Human Binding pKi = 8 8.0 - 1
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 351 2 2 6 3.1 CN[C@@H]1CCN(c2nc(N)nc3c2oc2ccc(Cl)c(Cl)c23)C1 10.1016/j.bmcl.2011.08.014
24826168 68161 None 0 Human Binding pKi = 8 8.0 - 1
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 333 2 2 6 2.9 CN[C@@H]1CCN(c2nc(N)nc3c2sc2ccc(Cl)cc23)C1 10.1016/j.bmcl.2011.08.014
CHEMBL1914789 68161 None 0 Human Binding pKi = 8 8.0 - 1
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 333 2 2 6 2.9 CN[C@@H]1CCN(c2nc(N)nc3c2sc2ccc(Cl)cc23)C1 10.1016/j.bmcl.2011.08.014
24745335 295 None 13 Human Binding pKi = 8.0 8.0 4 5
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 262 5 3 6 0.7 CN[C@@H]1CCN(C1)c1cc(NCC2CC2)nc(n1)N 10.1016/j.bmcl.2013.02.091
8985 295 None 13 Human Binding pKi = 8.0 8.0 4 5
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 262 5 3 6 0.7 CN[C@@H]1CCN(C1)c1cc(NCC2CC2)nc(n1)N 10.1016/j.bmcl.2013.02.091
CHEMBL1915540 295 None 13 Human Binding pKi = 8.0 8.0 4 5
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 262 5 3 6 0.7 CN[C@@H]1CCN(C1)c1cc(NCC2CC2)nc(n1)N 10.1016/j.bmcl.2013.02.091
DB15027 295 None 13 Human Binding pKi = 8.0 8.0 4 5
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 262 5 3 6 0.7 CN[C@@H]1CCN(C1)c1cc(NCC2CC2)nc(n1)N 10.1016/j.bmcl.2013.02.091
71525680 89765 None 0 Human Binding pKi = 8.0 8.0 97 2
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 284 3 2 6 1.3 CN[C@@H]1CCN(c2nc(N)nc3cc(C4CC4)cnc23)C1 10.1016/j.bmcl.2013.02.091
CHEMBL2376806 89765 None 0 Human Binding pKi = 8.0 8.0 97 2
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 284 3 2 6 1.3 CN[C@@H]1CCN(c2nc(N)nc3cc(C4CC4)cnc23)C1 10.1016/j.bmcl.2013.02.091
71525678 89759 None 0 Human Binding pKi = 8.0 8.0 5 6
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 258 3 2 6 0.6 CCc1cnc2c(N3CC(NC)C3)nc(N)nc2c1 10.1016/j.bmcl.2013.02.091
CHEMBL2376800 89759 None 0 Human Binding pKi = 8.0 8.0 5 6
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 258 3 2 6 0.6 CCc1cnc2c(N3CC(NC)C3)nc(N)nc2c1 10.1016/j.bmcl.2013.02.091
25101945 193215 None 0 Human Binding pKi = 8.0 8.0 -3 2
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells
ChEMBL 295 2 2 5 1.6 CNC1CN(c2nc(N)nc3c2CCCc2ccccc2-3)C1 10.1021/jm800670r
CHEMBL522673 193215 None 0 Human Binding pKi = 8.0 8.0 -3 2
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells
ChEMBL 295 2 2 5 1.6 CNC1CN(c2nc(N)nc3c2CCCc2ccccc2-3)C1 10.1021/jm800670r
136192886 56496 None 0 Mouse Binding pKi = 7 7.0 -1 4
Binding affinity to mouse histamine H4 receptor expressed in human SK-N-MC cells by radioligand displacement assayBinding affinity to mouse histamine H4 receptor expressed in human SK-N-MC cells by radioligand displacement assay
ChEMBL 257 2 2 3 2.7 CN1CCC(/C(=N/O)c2cc3ccccc3[nH]2)CC1 10.1016/j.bmcl.2010.10.041
CHEMBL1632411 56496 None 0 Mouse Binding pKi = 7 7.0 -1 4
Binding affinity to mouse histamine H4 receptor expressed in human SK-N-MC cells by radioligand displacement assayBinding affinity to mouse histamine H4 receptor expressed in human SK-N-MC cells by radioligand displacement assay
ChEMBL 257 2 2 3 2.7 CN1CCC(/C(=N/O)c2cc3ccccc3[nH]2)CC1 10.1016/j.bmcl.2010.10.041
44129134 201964 None 0 Rat Binding pKi = 7 7.0 -22 2
Binding affinity to rat histamine H4 receptorBinding affinity to rat histamine H4 receptor
ChEMBL 384 5 2 7 0.7 CN1CCN(c2nc(NCCS(N)(=O)=O)c3cc(Cl)ccc3n2)CC1 10.1021/jm901379s
CHEMBL591969 201964 None 0 Rat Binding pKi = 7 7.0 -22 2
Binding affinity to rat histamine H4 receptorBinding affinity to rat histamine H4 receptor
ChEMBL 384 5 2 7 0.7 CN1CCN(c2nc(NCCS(N)(=O)=O)c3cc(Cl)ccc3n2)CC1 10.1021/jm901379s
11694543 75826 None 2 Human Binding pKi = 7 7.0 -3 2
Displacement of [3H]histamine from human H4 receptor expressed in SK-N-MC cellsDisplacement of [3H]histamine from human H4 receptor expressed in SK-N-MC cells
ChEMBL 167 6 2 2 1.3 CCNCCCCc1c[nH]cn1 10.1021/jm0504353
CHEMBL204843 75826 None 2 Human Binding pKi = 7 7.0 -3 2
Displacement of [3H]histamine from human H4 receptor expressed in SK-N-MC cellsDisplacement of [3H]histamine from human H4 receptor expressed in SK-N-MC cells
ChEMBL 167 6 2 2 1.3 CCNCCCCc1c[nH]cn1 10.1021/jm0504353
11521414 141384 None 0 Human Binding pKi = 7 7.0 -3 2
Displacement of [3H]histamine from human H4 receptor expressed in SK-N-MC cellsDisplacement of [3H]histamine from human H4 receptor expressed in SK-N-MC cells
ChEMBL 221 6 2 2 2.7 c1nc(CCCCNC2CCCCC2)c[nH]1 10.1021/jm0504353
CHEMBL383324 141384 None 0 Human Binding pKi = 7 7.0 -3 2
Displacement of [3H]histamine from human H4 receptor expressed in SK-N-MC cellsDisplacement of [3H]histamine from human H4 receptor expressed in SK-N-MC cells
ChEMBL 221 6 2 2 2.7 c1nc(CCCCNC2CCCCC2)c[nH]1 10.1021/jm0504353
9812843 207702 None 1 Human Binding pKi = 7 7.0 -4 2
Displacement of [3H]histamine from human H4R receptor expressed in HEK293 cells at 10 uM after 1.5 hrs by liquid scintillation countingDisplacement of [3H]histamine from human H4R receptor expressed in HEK293 cells at 10 uM after 1.5 hrs by liquid scintillation counting
ChEMBL 159 2 1 2 1.4 c1cncc(Cc2c[nH]cn2)c1 10.1016/j.bmcl.2011.06.123
CHEMBL78838 207702 None 1 Human Binding pKi = 7 7.0 -4 2
Displacement of [3H]histamine from human H4R receptor expressed in HEK293 cells at 10 uM after 1.5 hrs by liquid scintillation countingDisplacement of [3H]histamine from human H4R receptor expressed in HEK293 cells at 10 uM after 1.5 hrs by liquid scintillation counting
ChEMBL 159 2 1 2 1.4 c1cncc(Cc2c[nH]cn2)c1 10.1016/j.bmcl.2011.06.123
53233904 61545 None 0 Human Binding pKi = 7 7.0 - 1
Displacement of [3H]histamine from human histamine H4 receptorDisplacement of [3H]histamine from human histamine H4 receptor
ChEMBL 261 2 1 5 1.0 CN1CCN(c2cc(N)nc(N3CCCC3)c2)CC1 10.1016/j.bmcl.2011.03.017
CHEMBL1770965 61545 None 0 Human Binding pKi = 7 7.0 - 1
Displacement of [3H]histamine from human histamine H4 receptorDisplacement of [3H]histamine from human histamine H4 receptor
ChEMBL 261 2 1 5 1.0 CN1CCN(c2cc(N)nc(N3CCCC3)c2)CC1 10.1016/j.bmcl.2011.03.017
39732699 75707 None 1 Human Binding pKi = 7 7.0 - 1
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 247 1 2 2 1.4 O=C(c1cc2cccc(F)c2[nH]1)N1CCNCC1 10.1016/j.ejmech.2012.06.016
CHEMBL2047463 75707 None 1 Human Binding pKi = 7 7.0 - 1
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 247 1 2 2 1.4 O=C(c1cc2cccc(F)c2[nH]1)N1CCNCC1 10.1016/j.ejmech.2012.06.016
70696623 75715 None 0 Human Binding pKi = 7 7.0 - 1
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 281 2 2 2 2.0 CNC1CN(C(=O)c2cc3cc(Cl)cc(F)c3[nH]2)C1 10.1016/j.ejmech.2012.06.016
CHEMBL2047471 75715 None 0 Human Binding pKi = 7 7.0 - 1
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 281 2 2 2 2.0 CNC1CN(C(=O)c2cc3cc(Cl)cc(F)c3[nH]2)C1 10.1016/j.ejmech.2012.06.016
51354298 58904 None 0 Human Binding pKi = 7 7.0 1 2
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells after 60 mins by liquid scintillation countingDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells after 60 mins by liquid scintillation counting
ChEMBL 233 4 1 4 1.9 CC(C)(C)c1cn(CCCc2c[nH]cn2)nn1 10.1021/jm1013488
CHEMBL1688944 58904 None 0 Human Binding pKi = 7 7.0 1 2
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells after 60 mins by liquid scintillation countingDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells after 60 mins by liquid scintillation counting
ChEMBL 233 4 1 4 1.9 CC(C)(C)c1cn(CCCc2c[nH]cn2)nn1 10.1021/jm1013488
45267237 198658 None 0 Human Binding pKi = 7 7.0 -7 2
Displacement of [3H]histamine from human histamine H4 receptor expressed in human SK-N-MC cells by liquid scintillation countingDisplacement of [3H]histamine from human histamine H4 receptor expressed in human SK-N-MC cells by liquid scintillation counting
ChEMBL 302 7 3 3 3.2 Cc1ccc(CCNC(=N)SCCCc2c[nH]cn2)cc1 10.1016/j.bmc.2009.04.007
CHEMBL1202320 198658 None 0 Human Binding pKi = 7 7.0 -7 2
Displacement of [3H]histamine from human histamine H4 receptor expressed in human SK-N-MC cells by liquid scintillation countingDisplacement of [3H]histamine from human histamine H4 receptor expressed in human SK-N-MC cells by liquid scintillation counting
ChEMBL 302 7 3 3 3.2 Cc1ccc(CCNC(=N)SCCCc2c[nH]cn2)cc1 10.1016/j.bmc.2009.04.007
CHEMBL561451 198658 None 0 Human Binding pKi = 7 7.0 -7 2
Displacement of [3H]histamine from human histamine H4 receptor expressed in human SK-N-MC cells by liquid scintillation countingDisplacement of [3H]histamine from human histamine H4 receptor expressed in human SK-N-MC cells by liquid scintillation counting
ChEMBL 302 7 3 3 3.2 Cc1ccc(CCNC(=N)SCCCc2c[nH]cn2)cc1 10.1016/j.bmc.2009.04.007
53378933 110201 None 0 Human Binding pKi = 7 7.0 - 1
Displacement of [3H]histamine from human recombinant histamine H4 receptor expressed in SK-N-MC cells after 45 mins by competition binding analysisDisplacement of [3H]histamine from human recombinant histamine H4 receptor expressed in SK-N-MC cells after 45 mins by competition binding analysis
ChEMBL 269 3 2 5 1.2 Nc1nc(Cc2ccccc2)cc(N2CC[C@@H](N)C2)n1 10.1021/jm401727m
CHEMBL3236573 110201 None 0 Human Binding pKi = 7 7.0 - 1
Displacement of [3H]histamine from human recombinant histamine H4 receptor expressed in SK-N-MC cells after 45 mins by competition binding analysisDisplacement of [3H]histamine from human recombinant histamine H4 receptor expressed in SK-N-MC cells after 45 mins by competition binding analysis
ChEMBL 269 3 2 5 1.2 Nc1nc(Cc2ccccc2)cc(N2CC[C@@H](N)C2)n1 10.1021/jm401727m
11087453 75671 None 0 Human Binding pKi = 7 7.0 - 1
Displacement of [3H]histamine from wild type human histamine H4 receptor transfected in HEK293T cells after 1.5 hrs by liquid scintillation counting analysisDisplacement of [3H]histamine from wild type human histamine H4 receptor transfected in HEK293T cells after 1.5 hrs by liquid scintillation counting analysis
ChEMBL 288 2 1 4 1.5 CN1CCN(C(=O)c2cc3cc([N+](=O)[O-])ccc3[nH]2)CC1 10.1039/C2MD20212C
CHEMBL2047270 75671 None 0 Human Binding pKi = 7 7.0 - 1
Displacement of [3H]histamine from wild type human histamine H4 receptor transfected in HEK293T cells after 1.5 hrs by liquid scintillation counting analysisDisplacement of [3H]histamine from wild type human histamine H4 receptor transfected in HEK293T cells after 1.5 hrs by liquid scintillation counting analysis
ChEMBL 288 2 1 4 1.5 CN1CCN(C(=O)c2cc3cc([N+](=O)[O-])ccc3[nH]2)CC1 10.1039/C2MD20212C
44395335 67083 None 0 Human Binding pKi = 6 6.0 25 2
Binding affinity towards human histamine H4 receptor was determined by [3H]Na-methylhistamine binding to SK-N-MC cell membranesBinding affinity towards human histamine H4 receptor was determined by [3H]Na-methylhistamine binding to SK-N-MC cell membranes
ChEMBL 266 4 2 3 1.5 CN(C)CCNC(=O)c1nc2cc(Cl)ccc2[nH]1 10.1016/j.bmcl.2004.08.035
CHEMBL187210 67083 None 0 Human Binding pKi = 6 6.0 25 2
Binding affinity towards human histamine H4 receptor was determined by [3H]Na-methylhistamine binding to SK-N-MC cell membranesBinding affinity towards human histamine H4 receptor was determined by [3H]Na-methylhistamine binding to SK-N-MC cell membranes
ChEMBL 266 4 2 3 1.5 CN(C)CCNC(=O)c1nc2cc(Cl)ccc2[nH]1 10.1016/j.bmcl.2004.08.035
10978141 5152 None 0 Human Binding pKi = 6 6.0 -4 2
Displacement of [3H]-histamine from human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2Displacement of [3H]-histamine from human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2
ChEMBL 258 5 1 3 2.8 c1ccc(COC[C@H]2CC[C@H](c3c[nH]cn3)O2)cc1 10.1016/j.bmcl.2010.10.041
CHEMBL105803 5152 None 0 Human Binding pKi = 6 6.0 -4 2
Displacement of [3H]-histamine from human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2Displacement of [3H]-histamine from human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2
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
71681477 89692 None 0 Human Binding pKi = 6 6.0 - 1
Displacement of [3H]histamine displacement from human histamine H4 receptor expressed in SK-NM-C cells after 60 minsDisplacement of [3H]histamine displacement from human histamine H4 receptor expressed in SK-NM-C cells after 60 mins
ChEMBL 398 7 4 8 3.3 Nc1nc(NCCNc2cc(-c3ccccc3)nc(N)n2)cc(-c2ccccc2)n1 10.1021/jm301886t
CHEMBL2375758 89692 None 0 Human Binding pKi = 6 6.0 - 1
Displacement of [3H]histamine displacement from human histamine H4 receptor expressed in SK-NM-C cells after 60 minsDisplacement of [3H]histamine displacement from human histamine H4 receptor expressed in SK-NM-C cells after 60 mins
ChEMBL 398 7 4 8 3.3 Nc1nc(NCCNc2cc(-c3ccccc3)nc(N)n2)cc(-c2ccccc2)n1 10.1021/jm301886t
71681802 89703 None 0 Human Binding pKi = 6 6.0 - 1
Displacement of [3H]histamine displacement from human histamine H4 receptor expressed in SK-NM-C cells after 60 minsDisplacement of [3H]histamine displacement from human histamine H4 receptor expressed in SK-NM-C cells after 60 mins
ChEMBL 302 8 4 8 1.4 CC(C)CNc1cc(NCCNc2ccnc(N)n2)ncn1 10.1021/jm301886t
CHEMBL2375769 89703 None 0 Human Binding pKi = 6 6.0 - 1
Displacement of [3H]histamine displacement from human histamine H4 receptor expressed in SK-NM-C cells after 60 minsDisplacement of [3H]histamine displacement from human histamine H4 receptor expressed in SK-NM-C cells after 60 mins
ChEMBL 302 8 4 8 1.4 CC(C)CNc1cc(NCCNc2ccnc(N)n2)ncn1 10.1021/jm301886t
206876 18952 None 4 Human Binding pKi = 6 6.0 - 1
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 273 2 1 3 1.6 COc1ccc2[nH]c(C(=O)N3CCN(C)CC3)cc2c1 10.1016/j.ejmech.2012.06.016
CHEMBL128637 18952 None 4 Human Binding pKi = 6 6.0 - 1
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 273 2 1 3 1.6 COc1ccc2[nH]c(C(=O)N3CCN(C)CC3)cc2c1 10.1016/j.ejmech.2012.06.016
66572107 75666 None 0 Human Binding pKi = 6 6.0 - 1
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 273 2 1 3 1.6 COc1cccc2[nH]c(C(=O)N3CCN(C)CC3)cc12 10.1016/j.ejmech.2012.06.016
CHEMBL2047265 75666 None 0 Human Binding pKi = 6 6.0 - 1
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 273 2 1 3 1.6 COc1cccc2[nH]c(C(=O)N3CCN(C)CC3)cc12 10.1016/j.ejmech.2012.06.016
66572115 75686 None 0 Human Binding pKi = 6 6.0 - 1
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 311 1 1 2 2.6 CN1CCN(C(=O)c2cc3cccc(C(F)(F)F)c3[nH]2)CC1 10.1016/j.ejmech.2012.06.016
CHEMBL2047442 75686 None 0 Human Binding pKi = 6 6.0 - 1
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 311 1 1 2 2.6 CN1CCN(C(=O)c2cc3cccc(C(F)(F)F)c3[nH]2)CC1 10.1016/j.ejmech.2012.06.016
11469514 104223 None 0 Human Binding pKi = 6 6.0 -64 2
Displacement of [3H]histamine from human histamine H4 receptor expressed in SK-N-MC cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in SK-N-MC cells
ChEMBL 187 4 1 2 2.0 c1cc(CCCc2c[nH]cn2)ccn1 10.1021/jm049932u
CHEMBL309654 104223 None 0 Human Binding pKi = 6 6.0 -64 2
Displacement of [3H]histamine from human histamine H4 receptor expressed in SK-N-MC cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in SK-N-MC cells
ChEMBL 187 4 1 2 2.0 c1cc(CCCc2c[nH]cn2)ccn1 10.1021/jm049932u
46890591 7027 None 0 Human Binding pKi = 6 6.0 - 1
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 436 6 1 4 4.8 Cc1cc(OCCCN2CC3CCCN(C)C3C2)ccc1-c1nc2c(C)c(F)ccc2[nH]1 10.1016/j.bmcl.2010.04.017
CHEMBL1084811 7027 None 0 Human Binding pKi = 6 6.0 - 1
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 436 6 1 4 4.8 Cc1cc(OCCCN2CC3CCCN(C)C3C2)ccc1-c1nc2c(C)c(F)ccc2[nH]1 10.1016/j.bmcl.2010.04.017
44275807 99024 None 0 Human Binding pKi = 5 5.0 -9120 10
Binding affinity towards human histaminergic (H4) receptorBinding affinity towards human histaminergic (H4) receptor
ChEMBL 422 7 0 4 4.5 C[C@H]1CC[C@H](C)N1CCCOc1ccc(-c2ccc(C(=O)N3CCOCC3)cc2)cc1 10.1016/s0960-894x(03)00118-5
CHEMBL27979 99024 None 0 Human Binding pKi = 5 5.0 -9120 10
Binding affinity towards human histaminergic (H4) receptorBinding affinity towards human histaminergic (H4) receptor
ChEMBL 422 7 0 4 4.5 C[C@H]1CC[C@H](C)N1CCCOc1ccc(-c2ccc(C(=O)N3CCOCC3)cc2)cc1 10.1016/s0960-894x(03)00118-5
4242418 117496 None 7 Human Binding pKi = 5 5.0 - 1
Displacement of [3H]- histamine from the recombinant human histamine H4 receptorDisplacement of [3H]- histamine from the recombinant human histamine H4 receptor
ChEMBL 229 2 1 2 1.9 CN1CCN(Cc2cc3ccccc3[nH]2)CC1 10.1021/jm0341047
CHEMBL339826 117496 None 7 Human Binding pKi = 5 5.0 - 1
Displacement of [3H]- histamine from the recombinant human histamine H4 receptorDisplacement of [3H]- histamine from the recombinant human histamine H4 receptor
ChEMBL 229 2 1 2 1.9 CN1CCN(Cc2cc3ccccc3[nH]2)CC1 10.1021/jm0341047
71681978 89687 None 0 Human Binding pKi = 5 5.0 - 1
Displacement of [3H]histamine displacement from human histamine H4 receptor expressed in SK-NM-C cells after 60 minsDisplacement of [3H]histamine displacement from human histamine H4 receptor expressed in SK-NM-C cells after 60 mins
ChEMBL 310 5 3 5 1.7 CN(CCNc1ccnc(N)n1)C(=O)c1cc2ccccc2[nH]1 10.1021/jm301886t
CHEMBL2375753 89687 None 0 Human Binding pKi = 5 5.0 - 1
Displacement of [3H]histamine displacement from human histamine H4 receptor expressed in SK-NM-C cells after 60 minsDisplacement of [3H]histamine displacement from human histamine H4 receptor expressed in SK-NM-C cells after 60 mins
ChEMBL 310 5 3 5 1.7 CN(CCNc1ccnc(N)n1)C(=O)c1cc2ccccc2[nH]1 10.1021/jm301886t
58227158 117199 None 0 Human Binding pKi = 5 5.0 - 1
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 249 4 1 5 1.3 CC(C)CNc1cc(N2CCN(C)CC2)cnn1 10.1016/j.bmcl.2014.12.027
CHEMBL3393549 117199 None 0 Human Binding pKi = 5 5.0 - 1
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 249 4 1 5 1.3 CC(C)CNc1cc(N2CCN(C)CC2)cnn1 10.1016/j.bmcl.2014.12.027
72901200 119841 None 26 Human Binding pKi = 5 5.0 -6918 33
GPCRScan assay: inhibition of H4GPCRScan assay: inhibition of H4
ChEMBL 322 7 2 4 3.8 Cc1ccc2nc(CNCCCOc3ccccc3)cc(O)c2c1 10.6019/CHEMBL4507309
CHEMBL3480577 119841 None 26 Human Binding pKi = 5 5.0 -6918 33
GPCRScan assay: inhibition of H4GPCRScan assay: inhibition of H4
ChEMBL 322 7 2 4 3.8 Cc1ccc2nc(CNCCCOc3ccccc3)cc(O)c2c1 10.6019/CHEMBL4507309
CHEMBL4552554 216471 None 0 Human Binding pKi = 5 5.0 -1 2
GPCRScan assay: inhibition of H4GPCRScan assay: inhibition of H4
ChEMBL None None None O=C(c1ccc(F)cc1)N1CC(COc2ccc(Br)cc2)(C(=O)O)C1 10.6019/CHEMBL4507298
57391926 69924 None 0 Human Binding pKi = 7.0 7.0 - 1
Displacement of [3H]histamine from human recombinant histamine H4 receptor expressed in CHO cells coexpressing Ga15 by radioligand filtration binding assayDisplacement of [3H]histamine from human recombinant histamine H4 receptor expressed in CHO cells coexpressing Ga15 by radioligand filtration binding assay
ChEMBL 270 1 1 3 1.2 CN1C[C@H]2CN(C(=O)c3nc4ccccc4[nH]3)C[C@H]2C1 10.1016/j.bmcl.2011.11.098
CHEMBL1938967 69924 None 0 Human Binding pKi = 7.0 7.0 - 1
Displacement of [3H]histamine from human recombinant histamine H4 receptor expressed in CHO cells coexpressing Ga15 by radioligand filtration binding assayDisplacement of [3H]histamine from human recombinant histamine H4 receptor expressed in CHO cells coexpressing Ga15 by radioligand filtration binding assay
ChEMBL 270 1 1 3 1.2 CN1C[C@H]2CN(C(=O)c3nc4ccccc4[nH]3)C[C@H]2C1 10.1016/j.bmcl.2011.11.098
11846300 80297 None 3 Human Binding pKi = 7.0 7.0 -2 4
Displacement of [3H]histamine from human histamine 4 receptor expressed in Sf9 cell membranes by liquid scintillation countingDisplacement of [3H]histamine from human histamine 4 receptor expressed in Sf9 cell membranes by liquid scintillation counting
ChEMBL 327 0 0 4 3.8 CN1CCN(C2=Nc3ccc(Cl)cc3Oc3ccccc32)CC1 10.1016/j.bmcl.2015.12.035
CHEMBL213912 80297 None 3 Human Binding pKi = 7.0 7.0 -2 4
Displacement of [3H]histamine from human histamine 4 receptor expressed in Sf9 cell membranes by liquid scintillation countingDisplacement of [3H]histamine from human histamine 4 receptor expressed in Sf9 cell membranes by liquid scintillation counting
ChEMBL 327 0 0 4 3.8 CN1CCN(C2=Nc3ccc(Cl)cc3Oc3ccccc32)CC1 10.1016/j.bmcl.2015.12.035
24854583 96175 None 0 Human Binding pKi = 5.0 5.0 - 1
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells
ChEMBL 304 2 0 4 3.0 CN1CCN(c2nc3ccccc3nc2-c2ccccc2)CC1 10.1021/jm7014217
CHEMBL260372 96175 None 0 Human Binding pKi = 5.0 5.0 - 1
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells
ChEMBL 304 2 0 4 3.0 CN1CCN(c2nc3ccccc3nc2-c2ccccc2)CC1 10.1021/jm7014217
16082860 138698 None 0 Human Binding pKi = 7.0 7.0 -7 2
Displacement of [3H]histamine form human H4 receptorDisplacement of [3H]histamine form human H4 receptor
ChEMBL 275 6 2 2 3.3 Clc1ccc(CNCC[C@H]2C[C@H]2c2c[nH]cn2)cc1 10.1021/jm0603318
CHEMBL377572 138698 None 0 Human Binding pKi = 7.0 7.0 -7 2
Displacement of [3H]histamine form human H4 receptorDisplacement of [3H]histamine form human H4 receptor
ChEMBL 275 6 2 2 3.3 Clc1ccc(CNCC[C@H]2C[C@H]2c2c[nH]cn2)cc1 10.1021/jm0603318
57391032 68122 None 0 Human Binding pKi = 7.0 7.0 - 1
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 315 1 2 6 2.2 Nc1nc(N2C[C@H]3C[C@@H]2CN3)c2oc3ccc(Cl)cc3c2n1 10.1016/j.bmcl.2011.08.014
CHEMBL1914749 68122 None 0 Human Binding pKi = 7.0 7.0 - 1
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 315 1 2 6 2.2 Nc1nc(N2C[C@H]3C[C@@H]2CN3)c2oc3ccc(Cl)cc3c2n1 10.1016/j.bmcl.2011.08.014
25179297 173935 None 0 Human Binding pKi = 7.0 7.0 - 1
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 374 4 1 7 3.1 CN1CCN(c2nc(NCc3nccs3)c3cc(Cl)ccc3n2)CC1 10.1021/jm800876b
CHEMBL453877 173935 None 0 Human Binding pKi = 7.0 7.0 - 1
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 374 4 1 7 3.1 CN1CCN(c2nc(NCc3nccs3)c3cc(Cl)ccc3n2)CC1 10.1021/jm800876b
24759518 179415 None 0 Human Binding pKi = 7.0 7.0 - 1
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 277 1 1 5 1.6 CN1CCN(c2nc(N)c3cc(Cl)ccc3n2)CC1 10.1021/jm800876b
CHEMBL473302 179415 None 0 Human Binding pKi = 7.0 7.0 - 1
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 277 1 1 5 1.6 CN1CCN(c2nc(N)c3cc(Cl)ccc3n2)CC1 10.1021/jm800876b
25178342 186892 None 0 Human Binding pKi = 7.0 7.0 - 1
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 385 4 1 5 3.8 CN1CCN(c2nc(NCc3ccc(F)cc3)c3cc(Cl)ccc3n2)CC1 10.1021/jm800876b
CHEMBL489070 186892 None 0 Human Binding pKi = 7.0 7.0 - 1
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 385 4 1 5 3.8 CN1CCN(c2nc(NCc3ccc(F)cc3)c3cc(Cl)ccc3n2)CC1 10.1021/jm800876b
25179297 173935 None 0 Human Binding pKi = 7.0 7.0 - 1
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells
ChEMBL 374 4 1 7 3.1 CN1CCN(c2nc(NCc3nccs3)c3cc(Cl)ccc3n2)CC1 10.1021/jm901379s
CHEMBL453877 173935 None 0 Human Binding pKi = 7.0 7.0 - 1
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells
ChEMBL 374 4 1 7 3.1 CN1CCN(c2nc(NCc3nccs3)c3cc(Cl)ccc3n2)CC1 10.1021/jm901379s
25178342 186892 None 0 Human Binding pKi = 7.0 7.0 - 1
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells
ChEMBL 385 4 1 5 3.8 CN1CCN(c2nc(NCc3ccc(F)cc3)c3cc(Cl)ccc3n2)CC1 10.1021/jm901379s
CHEMBL489070 186892 None 0 Human Binding pKi = 7.0 7.0 - 1
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells
ChEMBL 385 4 1 5 3.8 CN1CCN(c2nc(NCc3ccc(F)cc3)c3cc(Cl)ccc3n2)CC1 10.1021/jm901379s
71518535 86521 None 0 Human Binding pKi = 5.0 5.0 - 1
Displacement of [3H]Histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai/o and Gbeta1gammaDisplacement of [3H]Histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai/o and Gbeta1gamma
ChEMBL 354 3 1 5 2.6 CN1CCN(c2nc(N(C)C)nc3[nH]c(-c4ccc(F)cc4)cc23)CC1 10.1016/j.bmcl.2012.10.139
CHEMBL2314763 86521 None 0 Human Binding pKi = 5.0 5.0 - 1
Displacement of [3H]Histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai/o and Gbeta1gammaDisplacement of [3H]Histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai/o and Gbeta1gamma
ChEMBL 354 3 1 5 2.6 CN1CCN(c2nc(N(C)C)nc3[nH]c(-c4ccc(F)cc4)cc23)CC1 10.1016/j.bmcl.2012.10.139
10978141 5152 None 0 Human Binding pKi = 6.0 6.0 -4 2
Histamine H4 receptor competition binding using [3H]Na-methylhistamineHistamine H4 receptor competition binding using [3H]Na-methylhistamine
ChEMBL 258 5 1 3 2.8 c1ccc(COC[C@H]2CC[C@H](c3c[nH]cn3)O2)cc1 10.1021/jm0300025
CHEMBL105803 5152 None 0 Human Binding pKi = 6.0 6.0 -4 2
Histamine H4 receptor competition binding using [3H]Na-methylhistamineHistamine H4 receptor competition binding using [3H]Na-methylhistamine
ChEMBL 258 5 1 3 2.8 c1ccc(COC[C@H]2CC[C@H](c3c[nH]cn3)O2)cc1 10.1021/jm0300025
57393730 67906 None 0 Human Binding pKi = 5.0 5.0 -2754 3
Displacement of [3H]histamine from human H4R expressed in Sf9 cells co-expressing RGS19, Galphai2 and Gbeta1gamma2 after 60 mins by liquid scintillation countingDisplacement of [3H]histamine from human H4R expressed in Sf9 cells co-expressing RGS19, Galphai2 and Gbeta1gamma2 after 60 mins by liquid scintillation counting
ChEMBL 579 8 2 6 5.0 O=C(c1cc2ccccc2[nH]1)N1CCN(CCN2CCC(Nc3nc4ccccc4n3Cc3ccc(F)cc3)CC2)CC1 10.1016/j.bmcl.2011.09.001
CHEMBL1910386 67906 None 0 Human Binding pKi = 5.0 5.0 -2754 3
Displacement of [3H]histamine from human H4R expressed in Sf9 cells co-expressing RGS19, Galphai2 and Gbeta1gamma2 after 60 mins by liquid scintillation countingDisplacement of [3H]histamine from human H4R expressed in Sf9 cells co-expressing RGS19, Galphai2 and Gbeta1gamma2 after 60 mins by liquid scintillation counting
ChEMBL 579 8 2 6 5.0 O=C(c1cc2ccccc2[nH]1)N1CCN(CCN2CCC(Nc3nc4ccccc4n3Cc3ccc(F)cc3)CC2)CC1 10.1016/j.bmcl.2011.09.001
24826681 68141 None 0 Human Binding pKi = 6.0 6.0 - 1
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 303 1 2 6 2.0 Nc1nc(N2CCNCC2)c2oc3cccc(Cl)c3c2n1 10.1016/j.bmcl.2011.08.014
CHEMBL1914768 68141 None 0 Human Binding pKi = 6.0 6.0 - 1
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 303 1 2 6 2.0 Nc1nc(N2CCNCC2)c2oc3cccc(Cl)c3c2n1 10.1016/j.bmcl.2011.08.014
127049855 140315 None 0 Human Binding pKi = 6.0 6.0 -1 4
Displacement of [3H]UR-PI294 from human histamine H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 60 mins by liquid scintillation counting methodDisplacement of [3H]UR-PI294 from human histamine H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 60 mins by liquid scintillation counting method
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
CHEMBL3805220 140315 None 0 Human Binding pKi = 6.0 6.0 -1 4
Displacement of [3H]UR-PI294 from human histamine H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 60 mins by liquid scintillation counting methodDisplacement of [3H]UR-PI294 from human histamine H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 60 mins by liquid scintillation counting method
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
57391869 63140 None 0 Human Binding pKi = 6.0 6.0 -19 3
Displacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 subunit after 60 mins by liquid scintillation countingDisplacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 subunit after 60 mins by liquid scintillation counting
ChEMBL 223 6 2 3 1.6 CC=CCNC(=O)OCCCc1c[nH]cn1 10.1016/j.bmc.2011.03.046
CHEMBL1774589 63140 None 0 Human Binding pKi = 6.0 6.0 -19 3
Displacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 subunit after 60 mins by liquid scintillation countingDisplacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 subunit after 60 mins by liquid scintillation counting
ChEMBL 223 6 2 3 1.6 CC=CCNC(=O)OCCCc1c[nH]cn1 10.1016/j.bmc.2011.03.046
CHEMBL1789349 63140 None 0 Human Binding pKi = 6.0 6.0 -19 3
Displacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 subunit after 60 mins by liquid scintillation countingDisplacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 subunit after 60 mins by liquid scintillation counting
ChEMBL 223 6 2 3 1.6 CC=CCNC(=O)OCCCc1c[nH]cn1 10.1016/j.bmc.2011.03.046
90645163 112253 None 0 Human Binding pKi = 5.0 5.0 - 1
Displacement of [3H]-histamine from human histamine H4 receptor expressed in insect Sf9 cell membrane co-expressing Galphai2/Gbeta1gamma2 subunits after 60 mins by liquid scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor expressed in insect Sf9 cell membrane co-expressing Galphai2/Gbeta1gamma2 subunits after 60 mins by liquid scintillation counting analysis
ChEMBL 298 2 1 6 1.5 Cc1cc(C)cc(-c2nc(N)nc(N3CCN(C)CC3)n2)c1 10.1016/j.ejmech.2014.06.032
CHEMBL3290590 112253 None 0 Human Binding pKi = 5.0 5.0 - 1
Displacement of [3H]-histamine from human histamine H4 receptor expressed in insect Sf9 cell membrane co-expressing Galphai2/Gbeta1gamma2 subunits after 60 mins by liquid scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor expressed in insect Sf9 cell membrane co-expressing Galphai2/Gbeta1gamma2 subunits after 60 mins by liquid scintillation counting analysis
ChEMBL 298 2 1 6 1.5 Cc1cc(C)cc(-c2nc(N)nc(N3CCN(C)CC3)n2)c1 10.1016/j.ejmech.2014.06.032
10656971 16428 None 2 Human Binding pKi = 6.0 6.0 - 1
Displacement of [3H]histamine from human histamine H4 receptor expressed in CHO cells after 90 mins by scintillation counting techniqueDisplacement of [3H]histamine from human histamine H4 receptor expressed in CHO cells after 90 mins by scintillation counting technique
ChEMBL 228 1 0 4 1.4 CN1CCN(c2cnc3ccccc3n2)CC1 10.1016/j.bmcl.2011.07.114
CHEMBL123137 16428 None 2 Human Binding pKi = 6.0 6.0 - 1
Displacement of [3H]histamine from human histamine H4 receptor expressed in CHO cells after 90 mins by scintillation counting techniqueDisplacement of [3H]histamine from human histamine H4 receptor expressed in CHO cells after 90 mins by scintillation counting technique
ChEMBL 228 1 0 4 1.4 CN1CCN(c2cnc3ccccc3n2)CC1 10.1016/j.bmcl.2011.07.114
121238070 166582 None 0 Human Binding pKi = 5.0 5.0 - 1
Displacement of [3H]histamine from human H4R expressed in Sf9 cell membranes co-expressed with G protein Gai2 and Gb1gamma2 incubated for 60 mins by liquid scintillation counting methodDisplacement of [3H]histamine from human H4R expressed in Sf9 cell membranes co-expressed with G protein Gai2 and Gb1gamma2 incubated for 60 mins by liquid scintillation counting method
ChEMBL 334 4 1 7 1.4 CN1CCN(c2nc(N)nc(COc3ccc(Cl)cc3)n2)CC1 10.1016/j.ejmech.2017.09.035
CHEMBL4278404 166582 None 0 Human Binding pKi = 5.0 5.0 - 1
Displacement of [3H]histamine from human H4R expressed in Sf9 cell membranes co-expressed with G protein Gai2 and Gb1gamma2 incubated for 60 mins by liquid scintillation counting methodDisplacement of [3H]histamine from human H4R expressed in Sf9 cell membranes co-expressed with G protein Gai2 and Gb1gamma2 incubated for 60 mins by liquid scintillation counting method
ChEMBL 334 4 1 7 1.4 CN1CCN(c2nc(N)nc(COc3ccc(Cl)cc3)n2)CC1 10.1016/j.ejmech.2017.09.035
25178555 174343 None 0 Human Binding pKi = 7.0 7.0 - 1
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 374 4 1 7 3.1 CN1CCN(c2nc(NCc3cncs3)c3cc(Cl)ccc3n2)CC1 10.1021/jm800876b
CHEMBL454891 174343 None 0 Human Binding pKi = 7.0 7.0 - 1
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 374 4 1 7 3.1 CN1CCN(c2nc(NCc3cncs3)c3cc(Cl)ccc3n2)CC1 10.1021/jm800876b
25178555 174343 None 0 Human Binding pKi = 7.0 7.0 - 1
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells
ChEMBL 374 4 1 7 3.1 CN1CCN(c2nc(NCc3cncs3)c3cc(Cl)ccc3n2)CC1 10.1021/jm901379s
CHEMBL454891 174343 None 0 Human Binding pKi = 7.0 7.0 - 1
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells
ChEMBL 374 4 1 7 3.1 CN1CCN(c2nc(NCc3cncs3)c3cc(Cl)ccc3n2)CC1 10.1021/jm901379s
155540201 173011 None 0 Human Binding pKi = 6.0 6.0 -67 5
Displacement of [3H]-Nalpha-Methylhistamine from human recombinant histamine H4 receptor expressed in CHO cell membranes after 1 hrs by liquid scintillation counting analysisDisplacement of [3H]-Nalpha-Methylhistamine from human recombinant histamine H4 receptor expressed in CHO cell membranes after 1 hrs by liquid scintillation counting analysis
ChEMBL 513 16 2 4 5.5 N=C(N)N(CCCCN1CCN(CCCCCCCOc2ccccc2)CC1)Cc1ccc(Cl)cc1 10.1039/C8MD00527C
CHEMBL4516173 173011 None 0 Human Binding pKi = 6.0 6.0 -67 5
Displacement of [3H]-Nalpha-Methylhistamine from human recombinant histamine H4 receptor expressed in CHO cell membranes after 1 hrs by liquid scintillation counting analysisDisplacement of [3H]-Nalpha-Methylhistamine from human recombinant histamine H4 receptor expressed in CHO cell membranes after 1 hrs by liquid scintillation counting analysis
ChEMBL 513 16 2 4 5.5 N=C(N)N(CCCCN1CCN(CCCCCCCOc2ccccc2)CC1)Cc1ccc(Cl)cc1 10.1039/C8MD00527C
1278 2150 None 56 Guinea pig Binding pKi = 6.0 6.0 -281 8
Displacement of [3H]-histamine from guinea pig H4R expressed in HEK293T cellsDisplacement of [3H]-histamine from guinea pig H4R expressed in HEK293T cells
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1016/j.bmcl.2011.07.125
1279 2150 None 56 Guinea pig Binding pKi = 6.0 6.0 -281 8
Displacement of [3H]-histamine from guinea pig H4R expressed in HEK293T cellsDisplacement of [3H]-histamine from guinea pig H4R expressed in HEK293T cells
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1016/j.bmcl.2011.07.125
4908365 2150 None 56 Guinea pig Binding pKi = 6.0 6.0 -281 8
Displacement of [3H]-histamine from guinea pig H4R expressed in HEK293T cellsDisplacement of [3H]-histamine from guinea pig H4R expressed in HEK293T cells
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1016/j.bmcl.2011.07.125
CHEMBL129198 2150 None 56 Guinea pig Binding pKi = 6.0 6.0 -281 8
Displacement of [3H]-histamine from guinea pig H4R expressed in HEK293T cellsDisplacement of [3H]-histamine from guinea pig H4R expressed in HEK293T cells
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1016/j.bmcl.2011.07.125
832283 12402 None 4 Human Binding pKi = 6.0 6.0 - 1
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 333 4 1 5 3.0 CN1CCN(c2nc(NCc3ccccc3)c3ccccc3n2)CC1 10.1021/jm800876b
CHEMBL118572 12402 None 4 Human Binding pKi = 6.0 6.0 - 1
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 333 4 1 5 3.0 CN1CCN(c2nc(NCc3ccccc3)c3ccccc3n2)CC1 10.1021/jm800876b
832283 12402 None 4 Human Binding pKi = 6.0 6.0 - 1
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells
ChEMBL 333 4 1 5 3.0 CN1CCN(c2nc(NCc3ccccc3)c3ccccc3n2)CC1 10.1021/jm901379s
CHEMBL118572 12402 None 4 Human Binding pKi = 6.0 6.0 - 1
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells
ChEMBL 333 4 1 5 3.0 CN1CCN(c2nc(NCc3ccccc3)c3ccccc3n2)CC1 10.1021/jm901379s
10269628 138803 None 0 Human Binding pKi = 6.0 6.0 - 1
Displacement of [3H]histamine from human histamine H4 receptor transfected in SK-N-MC cellsDisplacement of [3H]histamine from human histamine H4 receptor transfected in SK-N-MC cells
ChEMBL 355 1 0 4 4.6 CC(C)N1CCN(C2=Nc3cc(Cl)ccc3Oc3ccccc32)CC1 10.1021/jm051008s
CHEMBL377985 138803 None 0 Human Binding pKi = 6.0 6.0 - 1
Displacement of [3H]histamine from human histamine H4 receptor transfected in SK-N-MC cellsDisplacement of [3H]histamine from human histamine H4 receptor transfected in SK-N-MC cells
ChEMBL 355 1 0 4 4.6 CC(C)N1CCN(C2=Nc3cc(Cl)ccc3Oc3ccccc32)CC1 10.1021/jm051008s
54582866 61568 None 0 Human Binding pKi = 6.0 6.0 - 1
Displacement of [3H]histamine from human histamine H4 receptorDisplacement of [3H]histamine from human histamine H4 receptor
ChEMBL 298 4 2 6 1.4 CN1CCN(c2cc(N)nc(NCc3ccccc3)n2)CC1 10.1016/j.bmcl.2011.03.017
CHEMBL1770988 61568 None 0 Human Binding pKi = 6.0 6.0 - 1
Displacement of [3H]histamine from human histamine H4 receptorDisplacement of [3H]histamine from human histamine H4 receptor
ChEMBL 298 4 2 6 1.4 CN1CCN(c2cc(N)nc(NCc3ccccc3)n2)CC1 10.1016/j.bmcl.2011.03.017
25133970 187694 None 1 Human Binding pKi = 6.0 6.0 - 1
Displacement of [3H]-histamine from recombinant human H4 receptor expressed in Sf9 cell membranes co-expressing Galphai2/Gbeta1gamma2Displacement of [3H]-histamine from recombinant human H4 receptor expressed in Sf9 cell membranes co-expressing Galphai2/Gbeta1gamma2
ChEMBL 250 1 1 6 0.5 CN1CCN(c2nc(N)nc(C(C)(C)C)n2)CC1 10.1016/j.bmc.2019.02.020
CHEMBL494679 187694 None 1 Human Binding pKi = 6.0 6.0 - 1
Displacement of [3H]-histamine from recombinant human H4 receptor expressed in Sf9 cell membranes co-expressing Galphai2/Gbeta1gamma2Displacement of [3H]-histamine from recombinant human H4 receptor expressed in Sf9 cell membranes co-expressing Galphai2/Gbeta1gamma2
ChEMBL 250 1 1 6 0.5 CN1CCN(c2nc(N)nc(C(C)(C)C)n2)CC1 10.1016/j.bmc.2019.02.020
49841962 69750 None 0 Human Binding pKi = 7.0 7.0 - 1
Displacement of [3H]histamine from human H4 receptor expressed in HEK cell membranesDisplacement of [3H]histamine from human H4 receptor expressed in HEK cell membranes
ChEMBL 309 2 1 6 2.2 CN1CCN(c2nc(N)nc3c(-c4ccoc4)cccc23)CC1 10.1016/j.bmcl.2011.10.104
CHEMBL1935562 69750 None 0 Human Binding pKi = 7.0 7.0 - 1
Displacement of [3H]histamine from human H4 receptor expressed in HEK cell membranesDisplacement of [3H]histamine from human H4 receptor expressed in HEK cell membranes
ChEMBL 309 2 1 6 2.2 CN1CCN(c2nc(N)nc3c(-c4ccoc4)cccc23)CC1 10.1016/j.bmcl.2011.10.104
44547568 117180 None 0 Human Binding pKi = 7.0 7.0 - 1
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 248 6 2 4 2.1 CCCCNc1cc(N2CC[C@H](NC)C2)ccn1 10.1016/j.bmcl.2014.12.027
CHEMBL3393530 117180 None 0 Human Binding pKi = 7.0 7.0 - 1
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 248 6 2 4 2.1 CCCCNc1cc(N2CC[C@H](NC)C2)ccn1 10.1016/j.bmcl.2014.12.027
13731320 158742 None 0 Human Binding pKi = 6.0 6.0 - 1
Antagonist activity at human H4 receptor expressed in CHO cells co-expressing Galphai2 assessed as inhibition of imetit-induced GTPgamma[35S] binding after 30 mins by microbeta scintillation counting methodAntagonist activity at human H4 receptor expressed in CHO cells co-expressing Galphai2 assessed as inhibition of imetit-induced GTPgamma[35S] binding after 30 mins by microbeta scintillation counting method
ChEMBL 320 2 2 2 4.0 O=C(Nc1cccc2ccccc12)N1CCC(c2c[nH]cn2)CC1 10.1016/j.ejmech.2016.09.074
CHEMBL4092578 158742 None 0 Human Binding pKi = 6.0 6.0 - 1
Antagonist activity at human H4 receptor expressed in CHO cells co-expressing Galphai2 assessed as inhibition of imetit-induced GTPgamma[35S] binding after 30 mins by microbeta scintillation counting methodAntagonist activity at human H4 receptor expressed in CHO cells co-expressing Galphai2 assessed as inhibition of imetit-induced GTPgamma[35S] binding after 30 mins by microbeta scintillation counting method
ChEMBL 320 2 2 2 4.0 O=C(Nc1cccc2ccccc12)N1CCC(c2c[nH]cn2)CC1 10.1016/j.ejmech.2016.09.074
127035837 137504 None 0 Human Binding pKi = 5.0 5.0 -5 2
Displacement of [3H]histamine from human histamine 4 receptor expressed in Sf9 cell membranes by liquid scintillation countingDisplacement of [3H]histamine from human histamine 4 receptor expressed in Sf9 cell membranes by liquid scintillation counting
ChEMBL 403 4 1 5 3.7 CN1CCN(c2nc(NCc3ccc(F)cc3)nc3c2CCc2ccccc2-3)CC1 10.1016/j.bmcl.2015.12.035
CHEMBL3753334 137504 None 0 Human Binding pKi = 5.0 5.0 -5 2
Displacement of [3H]histamine from human histamine 4 receptor expressed in Sf9 cell membranes by liquid scintillation countingDisplacement of [3H]histamine from human histamine 4 receptor expressed in Sf9 cell membranes by liquid scintillation counting
ChEMBL 403 4 1 5 3.7 CN1CCN(c2nc(NCc3ccc(F)cc3)nc3c2CCc2ccccc2-3)CC1 10.1016/j.bmcl.2015.12.035
21842421 112234 None 1 Human Binding pKi = 6.0 6.0 - 1
Displacement of [3H]-histamine from human histamine H4 receptor expressed in insect Sf9 cell membrane co-expressing Galphai2/Gbeta1gamma2 subunits after 60 mins by liquid scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor expressed in insect Sf9 cell membrane co-expressing Galphai2/Gbeta1gamma2 subunits after 60 mins by liquid scintillation counting analysis
ChEMBL 270 2 1 6 0.9 CN1CCN(c2nc(N)nc(-c3ccccc3)n2)CC1 10.1016/j.ejmech.2014.06.032
CHEMBL3290571 112234 None 1 Human Binding pKi = 6.0 6.0 - 1
Displacement of [3H]-histamine from human histamine H4 receptor expressed in insect Sf9 cell membrane co-expressing Galphai2/Gbeta1gamma2 subunits after 60 mins by liquid scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor expressed in insect Sf9 cell membrane co-expressing Galphai2/Gbeta1gamma2 subunits after 60 mins by liquid scintillation counting analysis
ChEMBL 270 2 1 6 0.9 CN1CCN(c2nc(N)nc(-c3ccccc3)n2)CC1 10.1016/j.ejmech.2014.06.032
10688021 156202 None 0 Human Binding pKi = 8.0 8.0 -1 2
Antagonist activity at H4 receptor in human SH-SY5Y cells assessed as inhibition of imetit-induced GTPgamma[35S] binding after 30 mins by microbeta scintillation counting methodAntagonist activity at H4 receptor in human SH-SY5Y cells assessed as inhibition of imetit-induced GTPgamma[35S] binding after 30 mins by microbeta scintillation counting method
ChEMBL 332 8 1 3 4.3 O=C(/C=C/c1ccccc1)c1ccc(OCCCc2c[nH]cn2)cc1 10.1016/j.ejmech.2016.09.074
CHEMBL4063170 156202 None 0 Human Binding pKi = 8.0 8.0 -1 2
Antagonist activity at H4 receptor in human SH-SY5Y cells assessed as inhibition of imetit-induced GTPgamma[35S] binding after 30 mins by microbeta scintillation counting methodAntagonist activity at H4 receptor in human SH-SY5Y cells assessed as inhibition of imetit-induced GTPgamma[35S] binding after 30 mins by microbeta scintillation counting method
ChEMBL 332 8 1 3 4.3 O=C(/C=C/c1ccccc1)c1ccc(OCCCc2c[nH]cn2)cc1 10.1016/j.ejmech.2016.09.074
9944571 117081 None 0 Human Binding pKi = 8.0 8.0 - 1
Antagonist activity at Homo sapiens (human) histamine H4 receptorAntagonist activity at Homo sapiens (human) histamine H4 receptor
ChEMBL 311 1 1 2 2.9 CN1CCN(C(=O)c2cc3cc(Cl)cc(Cl)c3[nH]2)CC1 10.1007/s00044-004-0106-7
CHEMBL338937 117081 None 0 Human Binding pKi = 8.0 8.0 - 1
Antagonist activity at Homo sapiens (human) histamine H4 receptorAntagonist activity at Homo sapiens (human) histamine H4 receptor
ChEMBL 311 1 1 2 2.9 CN1CCN(C(=O)c2cc3cc(Cl)cc(Cl)c3[nH]2)CC1 10.1007/s00044-004-0106-7
9944571 117081 None 0 Human Binding pKi = 8.0 8.0 - 1
Displacement of [3H]- histamine from the recombinant human histamine H4 receptorDisplacement of [3H]- histamine from the recombinant human histamine H4 receptor
ChEMBL 311 1 1 2 2.9 CN1CCN(C(=O)c2cc3cc(Cl)cc(Cl)c3[nH]2)CC1 10.1021/jm0341047
CHEMBL338937 117081 None 0 Human Binding pKi = 8.0 8.0 - 1
Displacement of [3H]- histamine from the recombinant human histamine H4 receptorDisplacement of [3H]- histamine from the recombinant human histamine H4 receptor
ChEMBL 311 1 1 2 2.9 CN1CCN(C(=O)c2cc3cc(Cl)cc(Cl)c3[nH]2)CC1 10.1021/jm0341047
23650961 3846 None 28 Human Binding pKi = 8.0 8.0 - 1
Displacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in human SK-N-MC cells or African green monkey COS7 cell membranes after 45 mins by scintillation counting methodDisplacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in human SK-N-MC cells or African green monkey COS7 cell membranes after 45 mins by scintillation counting method
ChEMBL 392 6 2 5 4.5 CN1CCC(CC1)CCCNc1ncc(c(n1)C)c1nc2c([nH]1)cc(cc2C)C nan
9276 3846 None 28 Human Binding pKi = 8.0 8.0 - 1
Displacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in human SK-N-MC cells or African green monkey COS7 cell membranes after 45 mins by scintillation counting methodDisplacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in human SK-N-MC cells or African green monkey COS7 cell membranes after 45 mins by scintillation counting method
ChEMBL 392 6 2 5 4.5 CN1CCC(CC1)CCCNc1ncc(c(n1)C)c1nc2c([nH]1)cc(cc2C)C nan
CHEMBL3301609 3846 None 28 Human Binding pKi = 8.0 8.0 - 1
Displacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in human SK-N-MC cells or African green monkey COS7 cell membranes after 45 mins by scintillation counting methodDisplacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in human SK-N-MC cells or African green monkey COS7 cell membranes after 45 mins by scintillation counting method
ChEMBL 392 6 2 5 4.5 CN1CCC(CC1)CCCNc1ncc(c(n1)C)c1nc2c([nH]1)cc(cc2C)C nan
DB12522 3846 None 28 Human Binding pKi = 8.0 8.0 - 1
Displacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in human SK-N-MC cells or African green monkey COS7 cell membranes after 45 mins by scintillation counting methodDisplacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in human SK-N-MC cells or African green monkey COS7 cell membranes after 45 mins by scintillation counting method
ChEMBL 392 6 2 5 4.5 CN1CCC(CC1)CCCNc1ncc(c(n1)C)c1nc2c([nH]1)cc(cc2C)C nan
24803710 150417 None 0 Human Binding pKi = 8.0 8.0 - 1
Displacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in human SK-N-MC cells or African green monkey COS7 cell membranes after 45 mins by scintillation counting methodDisplacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in human SK-N-MC cells or African green monkey COS7 cell membranes after 45 mins by scintillation counting method
ChEMBL 400 6 2 5 4.1 Cc1nc(NCCCC2CCN(C)CC2)ncc1-c1nc2c(F)c(F)ccc2[nH]1 nan
CHEMBL3953011 150417 None 0 Human Binding pKi = 8.0 8.0 - 1
Displacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in human SK-N-MC cells or African green monkey COS7 cell membranes after 45 mins by scintillation counting methodDisplacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in human SK-N-MC cells or African green monkey COS7 cell membranes after 45 mins by scintillation counting method
ChEMBL 400 6 2 5 4.1 Cc1nc(NCCCC2CCN(C)CC2)ncc1-c1nc2c(F)c(F)ccc2[nH]1 nan
25101945 193215 None 0 Human Binding pKi = 8.0 8.0 -3 2
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells
ChEMBL 295 2 2 5 1.6 CNC1CN(c2nc(N)nc3c2CCCc2ccccc2-3)C1 10.1021/jm800670r
CHEMBL522673 193215 None 0 Human Binding pKi = 8.0 8.0 -3 2
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells
ChEMBL 295 2 2 5 1.6 CNC1CN(c2nc(N)nc3c2CCCc2ccccc2-3)C1 10.1021/jm800670r
118720437 115977 None 0 Human Binding pKi = 8.0 8.0 - 1
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 275 3 2 5 1.0 CN[C@@H]1CCN(c2cc(CC(F)(F)F)nc(N)n2)C1 10.1016/j.bmcl.2014.10.013
CHEMBL3354811 115977 None 0 Human Binding pKi = 8.0 8.0 - 1
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 275 3 2 5 1.0 CN[C@@H]1CCN(c2cc(CC(F)(F)F)nc(N)n2)C1 10.1016/j.bmcl.2014.10.013
24737952 68156 None 0 Human Binding pKi = 8.0 8.0 - 1
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 313 3 2 7 1.8 CN[C@@H]1CCN(c2nc(N)nc3c2oc2ccc(OC)cc23)C1 10.1016/j.bmcl.2011.08.014
CHEMBL1914784 68156 None 0 Human Binding pKi = 8.0 8.0 - 1
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 313 3 2 7 1.8 CN[C@@H]1CCN(c2nc(N)nc3c2oc2ccc(OC)cc23)C1 10.1016/j.bmcl.2011.08.014
9944571 117081 None 0 Human Binding pKi = 8.0 8.0 - 1
Displacement of [3H]histamine from recombinant human histamine H4 receptor in SK-N-MC cellsDisplacement of [3H]histamine from recombinant human histamine H4 receptor in SK-N-MC cells
ChEMBL 311 1 1 2 2.9 CN1CCN(C(=O)c2cc3cc(Cl)cc(Cl)c3[nH]2)CC1 10.1021/jm0502081
CHEMBL338937 117081 None 0 Human Binding pKi = 8.0 8.0 - 1
Displacement of [3H]histamine from recombinant human histamine H4 receptor in SK-N-MC cellsDisplacement of [3H]histamine from recombinant human histamine H4 receptor in SK-N-MC cells
ChEMBL 311 1 1 2 2.9 CN1CCN(C(=O)c2cc3cc(Cl)cc(Cl)c3[nH]2)CC1 10.1021/jm0502081
24996854 110192 None 0 Human Binding pKi = 8.0 8.0 - 1
Displacement of [3H]histamine from human recombinant histamine H4 receptor expressed in SK-N-MC cells after 45 mins by competition binding analysisDisplacement of [3H]histamine from human recombinant histamine H4 receptor expressed in SK-N-MC cells after 45 mins by competition binding analysis
ChEMBL 287 2 2 5 2.0 Nc1nc(C2CCCC2)cc(N2CCC3(CCCN3)C2)n1 10.1021/jm401727m
CHEMBL3236564 110192 None 0 Human Binding pKi = 8.0 8.0 - 1
Displacement of [3H]histamine from human recombinant histamine H4 receptor expressed in SK-N-MC cells after 45 mins by competition binding analysisDisplacement of [3H]histamine from human recombinant histamine H4 receptor expressed in SK-N-MC cells after 45 mins by competition binding analysis
ChEMBL 287 2 2 5 2.0 Nc1nc(C2CCCC2)cc(N2CCC3(CCCN3)C2)n1 10.1021/jm401727m
71603142 89755 None 0 Human Binding pKi = 8.0 8.0 54 2
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 257 3 2 5 1.2 CCc1ccc2c(N3CC(NC)C3)nc(N)nc2c1 10.1016/j.bmcl.2013.02.091
CHEMBL2376796 89755 None 0 Human Binding pKi = 8.0 8.0 54 2
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 257 3 2 5 1.2 CCc1ccc2c(N3CC(NC)C3)nc(N)nc2c1 10.1016/j.bmcl.2013.02.091
44129282 201655 None 0 Human Binding pKi = 8.0 8.0 - 1
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells
ChEMBL 494 7 2 7 3.5 CN1CCN(c2nc(NCCS(=O)(=O)Nc3ccccc3)c3cc(Cl)cc(Cl)c3n2)CC1 10.1021/jm901379s
CHEMBL589746 201655 None 0 Human Binding pKi = 8.0 8.0 - 1
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells
ChEMBL 494 7 2 7 3.5 CN1CCN(c2nc(NCCS(=O)(=O)Nc3ccccc3)c3cc(Cl)cc(Cl)c3n2)CC1 10.1021/jm901379s
71603139 89752 None 0 Human Binding pKi = 7.9 7.9 13 2
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 269 2 2 5 1.5 Nc1nc(N2CCNCC2)c2ccc(C3CC3)cc2n1 10.1016/j.bmcl.2013.02.091
CHEMBL2376793 89752 None 0 Human Binding pKi = 7.9 7.9 13 2
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 269 2 2 5 1.5 Nc1nc(N2CCNCC2)c2ccc(C3CC3)cc2n1 10.1016/j.bmcl.2013.02.091
45257132 3682 None 14 Human Binding pKi = 7.9 7.9 42 4
Displacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2Displacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2
ChEMBL 366 4 2 6 2.7 CN1CCN(CC1)c1cc(NCc2c(Cl)cccc2Cl)nc(n1)N 10.1016/j.bmc.2009.08.059
8983 3682 None 14 Human Binding pKi = 7.9 7.9 42 4
Displacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2Displacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2
ChEMBL 366 4 2 6 2.7 CN1CCN(CC1)c1cc(NCc2c(Cl)cccc2Cl)nc(n1)N 10.1016/j.bmc.2009.08.059
CHEMBL595180 3682 None 14 Human Binding pKi = 7.9 7.9 42 4
Displacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2Displacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2
ChEMBL 366 4 2 6 2.7 CN1CCN(CC1)c1cc(NCc2c(Cl)cccc2Cl)nc(n1)N 10.1016/j.bmc.2009.08.059
155513612 176425 None 0 Human Binding pKi = 7.9 7.9 1 4
Displacement of 10 nM [3H]-histamine from human H4R expressed in Sf9 cell membranes co-expressing Gia2 and beta1gamma2 by competition binding assayDisplacement of 10 nM [3H]-histamine from human H4R expressed in Sf9 cell membranes co-expressing Gia2 and beta1gamma2 by competition binding 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 176425 None 0 Human Binding pKi = 7.9 7.9 1 4
Displacement of 10 nM [3H]-histamine from human H4R expressed in Sf9 cell membranes co-expressing Gia2 and beta1gamma2 by competition binding assayDisplacement of 10 nM [3H]-histamine from human H4R expressed in Sf9 cell membranes co-expressing Gia2 and beta1gamma2 by competition binding 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 176425 None 0 Human Binding pKi = 7.9 7.9 1 4
Displacement of 10 nM [3H]-histamine from human H4R expressed in Sf9 cell membranes co-expressing Gia2 and beta1gamma2 by competition binding assayDisplacement of 10 nM [3H]-histamine from human H4R expressed in Sf9 cell membranes co-expressing Gia2 and beta1gamma2 by competition binding 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 176425 None 0 Human Binding pKi = 7.9 7.9 1 4
Displacement of 10 nM [3H]-histamine from human H4R expressed in Sf9 cell membranes co-expressing Gia2 and beta1gamma2 by competition binding assayDisplacement of 10 nM [3H]-histamine from human H4R expressed in Sf9 cell membranes co-expressing Gia2 and beta1gamma2 by competition binding 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
44450493 96587 None 0 Human Binding pKi = 7.9 7.9 - 1
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells
ChEMBL 278 1 1 4 1.3 CN1CCN(c2nc3cc(Cl)ccc3[nH]c2=O)CC1 10.1021/jm7014217
CHEMBL262859 96587 None 0 Human Binding pKi = 7.9 7.9 - 1
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells
ChEMBL 278 1 1 4 1.3 CN1CCN(c2nc3cc(Cl)ccc3[nH]c2=O)CC1 10.1021/jm7014217
1278 2150 None 56 Mouse Binding pKi = 7.9 7.9 -4 8
Inhibition of UR-DEBa242 binding to mouse recombinant NLuc/GPCR-fused H4R expressed in HEK293T cells measured after 30 mins by furimazine substrate based BRET assayInhibition of UR-DEBa242 binding to mouse recombinant NLuc/GPCR-fused H4R expressed in HEK293T cells measured after 30 mins by furimazine substrate based BRET assay
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/acs.jmedchem.0c00160
1279 2150 None 56 Mouse Binding pKi = 7.9 7.9 -4 8
Inhibition of UR-DEBa242 binding to mouse recombinant NLuc/GPCR-fused H4R expressed in HEK293T cells measured after 30 mins by furimazine substrate based BRET assayInhibition of UR-DEBa242 binding to mouse recombinant NLuc/GPCR-fused H4R expressed in HEK293T cells measured after 30 mins by furimazine substrate based BRET assay
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/acs.jmedchem.0c00160
4908365 2150 None 56 Mouse Binding pKi = 7.9 7.9 -4 8
Inhibition of UR-DEBa242 binding to mouse recombinant NLuc/GPCR-fused H4R expressed in HEK293T cells measured after 30 mins by furimazine substrate based BRET assayInhibition of UR-DEBa242 binding to mouse recombinant NLuc/GPCR-fused H4R expressed in HEK293T cells measured after 30 mins by furimazine substrate based BRET assay
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/acs.jmedchem.0c00160
CHEMBL129198 2150 None 56 Mouse Binding pKi = 7.9 7.9 -4 8
Inhibition of UR-DEBa242 binding to mouse recombinant NLuc/GPCR-fused H4R expressed in HEK293T cells measured after 30 mins by furimazine substrate based BRET assayInhibition of UR-DEBa242 binding to mouse recombinant NLuc/GPCR-fused H4R expressed in HEK293T cells measured after 30 mins by furimazine substrate based BRET assay
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/acs.jmedchem.0c00160
126963283 161057 None 0 Human Binding pKi = 6.0 6.0 - 1
Binding Assay: The specific binding of the radioactive ligand to the receptor was defined as the difference between total binding and nonspecific binding, determined in the presence of excess unlabeled ligand. [3H]-histamine was used as the ligand in this study and the affinity values were determined according to the Cheng-Prusoff equation.Binding Assay: The specific binding of the radioactive ligand to the receptor was defined as the difference between total binding and nonspecific binding, determined in the presence of excess unlabeled ligand. [3H]-histamine was used as the ligand in this study and the affinity values were determined according to the Cheng-Prusoff equation.
ChEMBL 311 1 1 3 4.2 CO[C@@H]1Cc2ccccc2C(=C2CCNCC2)c2ccsc21 nan
CHEMBL4115677 161057 None 0 Human Binding pKi = 6.0 6.0 - 1
Binding Assay: The specific binding of the radioactive ligand to the receptor was defined as the difference between total binding and nonspecific binding, determined in the presence of excess unlabeled ligand. [3H]-histamine was used as the ligand in this study and the affinity values were determined according to the Cheng-Prusoff equation.Binding Assay: The specific binding of the radioactive ligand to the receptor was defined as the difference between total binding and nonspecific binding, determined in the presence of excess unlabeled ligand. [3H]-histamine was used as the ligand in this study and the affinity values were determined according to the Cheng-Prusoff equation.
ChEMBL 311 1 1 3 4.2 CO[C@@H]1Cc2ccccc2C(=C2CCNCC2)c2ccsc21 nan
1224 1432 None 51 Human Binding pKi = 5.0 5.0 -194 13
Binding Assay: The specific binding of the radioactive ligand to the receptor was defined as the difference between total binding and nonspecific binding, determined in the presence of excess unlabeled ligand. [3H]-histamine was used as the ligand in this study and the affinity values were determined according to the Cheng-Prusoff equation.Binding Assay: The specific binding of the radioactive ligand to the receptor was defined as the difference between total binding and nonspecific binding, determined in the presence of excess unlabeled ligand. [3H]-histamine was used as the ligand in this study and the affinity values were determined according to the Cheng-Prusoff equation.
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C nan
3100 1432 None 51 Human Binding pKi = 5.0 5.0 -194 13
Binding Assay: The specific binding of the radioactive ligand to the receptor was defined as the difference between total binding and nonspecific binding, determined in the presence of excess unlabeled ligand. [3H]-histamine was used as the ligand in this study and the affinity values were determined according to the Cheng-Prusoff equation.Binding Assay: The specific binding of the radioactive ligand to the receptor was defined as the difference between total binding and nonspecific binding, determined in the presence of excess unlabeled ligand. [3H]-histamine was used as the ligand in this study and the affinity values were determined according to the Cheng-Prusoff equation.
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C nan
3100.0 1432 None 51 Human Binding pKi = 5.0 5.0 -194 13
Binding Assay: The specific binding of the radioactive ligand to the receptor was defined as the difference between total binding and nonspecific binding, determined in the presence of excess unlabeled ligand. [3H]-histamine was used as the ligand in this study and the affinity values were determined according to the Cheng-Prusoff equation.Binding Assay: The specific binding of the radioactive ligand to the receptor was defined as the difference between total binding and nonspecific binding, determined in the presence of excess unlabeled ligand. [3H]-histamine was used as the ligand in this study and the affinity values were determined according to the Cheng-Prusoff equation.
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C nan
8980 1432 None 51 Human Binding pKi = 5.0 5.0 -194 13
Binding Assay: The specific binding of the radioactive ligand to the receptor was defined as the difference between total binding and nonspecific binding, determined in the presence of excess unlabeled ligand. [3H]-histamine was used as the ligand in this study and the affinity values were determined according to the Cheng-Prusoff equation.Binding Assay: The specific binding of the radioactive ligand to the receptor was defined as the difference between total binding and nonspecific binding, determined in the presence of excess unlabeled ligand. [3H]-histamine was used as the ligand in this study and the affinity values were determined according to the Cheng-Prusoff equation.
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C nan
916 1432 None 51 Human Binding pKi = 5.0 5.0 -194 13
Binding Assay: The specific binding of the radioactive ligand to the receptor was defined as the difference between total binding and nonspecific binding, determined in the presence of excess unlabeled ligand. [3H]-histamine was used as the ligand in this study and the affinity values were determined according to the Cheng-Prusoff equation.Binding Assay: The specific binding of the radioactive ligand to the receptor was defined as the difference between total binding and nonspecific binding, determined in the presence of excess unlabeled ligand. [3H]-histamine was used as the ligand in this study and the affinity values were determined according to the Cheng-Prusoff equation.
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C nan
CHEMBL657 1432 None 51 Human Binding pKi = 5.0 5.0 -194 13
Binding Assay: The specific binding of the radioactive ligand to the receptor was defined as the difference between total binding and nonspecific binding, determined in the presence of excess unlabeled ligand. [3H]-histamine was used as the ligand in this study and the affinity values were determined according to the Cheng-Prusoff equation.Binding Assay: The specific binding of the radioactive ligand to the receptor was defined as the difference between total binding and nonspecific binding, determined in the presence of excess unlabeled ligand. [3H]-histamine was used as the ligand in this study and the affinity values were determined according to the Cheng-Prusoff equation.
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C nan
DB01075 1432 None 51 Human Binding pKi = 5.0 5.0 -194 13
Binding Assay: The specific binding of the radioactive ligand to the receptor was defined as the difference between total binding and nonspecific binding, determined in the presence of excess unlabeled ligand. [3H]-histamine was used as the ligand in this study and the affinity values were determined according to the Cheng-Prusoff equation.Binding Assay: The specific binding of the radioactive ligand to the receptor was defined as the difference between total binding and nonspecific binding, determined in the presence of excess unlabeled ligand. [3H]-histamine was used as the ligand in this study and the affinity values were determined according to the Cheng-Prusoff equation.
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C nan
1241 2037 None 39 Human Binding pKi = 5.0 5.0 -89 5
Binding affinity to histamine H4 receptor (unknown origin)Binding affinity to histamine H4 receptor (unknown origin)
ChEMBL 125 2 1 3 -0.1 Cn1cc(nc1)CCN 10.1016/j.bmcl.2016.09.049
1242 2037 None 39 Human Binding pKi = 5.0 5.0 -89 5
Binding affinity to histamine H4 receptor (unknown origin)Binding affinity to histamine H4 receptor (unknown origin)
ChEMBL 125 2 1 3 -0.1 Cn1cc(nc1)CCN 10.1016/j.bmcl.2016.09.049
3614 2037 None 39 Human Binding pKi = 5.0 5.0 -89 5
Binding affinity to histamine H4 receptor (unknown origin)Binding affinity to histamine H4 receptor (unknown origin)
ChEMBL 125 2 1 3 -0.1 Cn1cc(nc1)CCN 10.1016/j.bmcl.2016.09.049
CHEMBL507 2037 None 39 Human Binding pKi = 5.0 5.0 -89 5
Binding affinity to histamine H4 receptor (unknown origin)Binding affinity to histamine H4 receptor (unknown origin)
ChEMBL 125 2 1 3 -0.1 Cn1cc(nc1)CCN 10.1016/j.bmcl.2016.09.049
49841609 69744 None 15 Human Binding pKi = 7.0 7.0 - 1
Displacement of [3H]histamine from human H4 receptor expressed in HEK cell membranesDisplacement of [3H]histamine from human H4 receptor expressed in HEK cell membranes
ChEMBL 321 1 1 5 1.7 CN1CCN(c2nc(N)nc3c(Br)cccc23)CC1 10.1016/j.bmcl.2011.10.104
CHEMBL1935556 69744 None 15 Human Binding pKi = 7.0 7.0 - 1
Displacement of [3H]histamine from human H4 receptor expressed in HEK cell membranesDisplacement of [3H]histamine from human H4 receptor expressed in HEK cell membranes
ChEMBL 321 1 1 5 1.7 CN1CCN(c2nc(N)nc3c(Br)cccc23)CC1 10.1016/j.bmcl.2011.10.104
51354871 58922 None 0 Human Binding pKi = 5.0 5.0 -22 2
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells after 60 mins by liquid scintillation countingDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells after 60 mins by liquid scintillation counting
ChEMBL 290 6 0 4 3.3 c1c(CC2CCCCC2)nnn1CCCN1CCCCC1 10.1021/jm1013488
CHEMBL1688982 58922 None 0 Human Binding pKi = 5.0 5.0 -22 2
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells after 60 mins by liquid scintillation countingDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells after 60 mins by liquid scintillation counting
ChEMBL 290 6 0 4 3.3 c1c(CC2CCCCC2)nnn1CCCN1CCCCC1 10.1021/jm1013488
164618508 186038 None 0 Human Binding pKi = 5.0 5.0 -363 4
Displacement of [3H]histamine from human histamine H4 receptor expressed in sf9 insect cell membranes co-expressing Galphai2/Gbeta1gamma2 incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]histamine from human histamine H4 receptor expressed in sf9 insect cell membranes co-expressing Galphai2/Gbeta1gamma2 incubated for 60 mins by microbeta scintillation counting method
ChEMBL 374 6 4 4 2.7 Cc1ccc(C(C)NC(=O)/N=C(\N)NCCCc2sc(N)nc2C)cc1 10.1016/j.ejmech.2021.113190
CHEMBL4869194 186038 None 0 Human Binding pKi = 5.0 5.0 -363 4
Displacement of [3H]histamine from human histamine H4 receptor expressed in sf9 insect cell membranes co-expressing Galphai2/Gbeta1gamma2 incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]histamine from human histamine H4 receptor expressed in sf9 insect cell membranes co-expressing Galphai2/Gbeta1gamma2 incubated for 60 mins by microbeta scintillation counting method
ChEMBL 374 6 4 4 2.7 Cc1ccc(C(C)NC(=O)/N=C(\N)NCCCc2sc(N)nc2C)cc1 10.1016/j.ejmech.2021.113190
164620678 186125 None 0 Human Binding pKi = 5.0 5.0 -177 4
Displacement of [3H]histamine from human histamine H4 receptor expressed in sf9 insect cell membranes co-expressing Galphai2/Gbeta1gamma2 incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]histamine from human histamine H4 receptor expressed in sf9 insect cell membranes co-expressing Galphai2/Gbeta1gamma2 incubated for 60 mins by microbeta scintillation counting method
ChEMBL 374 7 4 4 2.7 CCC(NC(=O)/N=C(\N)NCCCc1sc(N)nc1C)c1ccccc1 10.1016/j.ejmech.2021.113190
CHEMBL4870510 186125 None 0 Human Binding pKi = 5.0 5.0 -177 4
Displacement of [3H]histamine from human histamine H4 receptor expressed in sf9 insect cell membranes co-expressing Galphai2/Gbeta1gamma2 incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]histamine from human histamine H4 receptor expressed in sf9 insect cell membranes co-expressing Galphai2/Gbeta1gamma2 incubated for 60 mins by microbeta scintillation counting method
ChEMBL 374 7 4 4 2.7 CCC(NC(=O)/N=C(\N)NCCCc1sc(N)nc1C)c1ccccc1 10.1016/j.ejmech.2021.113190
58227159 176490 None 0 Human Binding pKi = 6.9 6.9 47 2
Displacement of 10 nM [3H]-histamine from human H4R expressed in Sf9 cell membranes co-expressing Gia2 and beta1gamma2 by competition binding assayDisplacement of 10 nM [3H]-histamine from human H4R expressed in Sf9 cell membranes co-expressing Gia2 and beta1gamma2 by competition binding assay
ChEMBL 263 3 1 5 1.7 CN1CCN(c2ccnc(NCC(C)(C)C)n2)CC1 10.1021/acs.jmedchem.9b01342
CHEMBL4534254 176490 None 0 Human Binding pKi = 6.9 6.9 47 2
Displacement of 10 nM [3H]-histamine from human H4R expressed in Sf9 cell membranes co-expressing Gia2 and beta1gamma2 by competition binding assayDisplacement of 10 nM [3H]-histamine from human H4R expressed in Sf9 cell membranes co-expressing Gia2 and beta1gamma2 by competition binding assay
ChEMBL 263 3 1 5 1.7 CN1CCN(c2ccnc(NCC(C)(C)C)n2)CC1 10.1021/acs.jmedchem.9b01342
CHEMBL4595907 176490 None 0 Human Binding pKi = 6.9 6.9 47 2
Displacement of 10 nM [3H]-histamine from human H4R expressed in Sf9 cell membranes co-expressing Gia2 and beta1gamma2 by competition binding assayDisplacement of 10 nM [3H]-histamine from human H4R expressed in Sf9 cell membranes co-expressing Gia2 and beta1gamma2 by competition binding assay
ChEMBL 263 3 1 5 1.7 CN1CCN(c2ccnc(NCC(C)(C)C)n2)CC1 10.1021/acs.jmedchem.9b01342
122193099 123985 None 0 Human Binding pKi = 5.9 5.9 - 1
Displacement of [3H]histamine from human H4 receptor expressed in Sf9 cell membranes co-expressing Galphai2 and Gbeta1gamma2 after 60 mins by liquid scintillation counting assayDisplacement of [3H]histamine from human H4 receptor expressed in Sf9 cell membranes co-expressing Galphai2 and Gbeta1gamma2 after 60 mins by liquid scintillation counting assay
ChEMBL 374 3 1 6 2.1 CN1CCN(c2nc(N)nc(/C=C/c3cccc(Br)c3)n2)CC1 10.1016/j.ejmech.2015.08.014
CHEMBL3628046 123985 None 0 Human Binding pKi = 5.9 5.9 - 1
Displacement of [3H]histamine from human H4 receptor expressed in Sf9 cell membranes co-expressing Galphai2 and Gbeta1gamma2 after 60 mins by liquid scintillation counting assayDisplacement of [3H]histamine from human H4 receptor expressed in Sf9 cell membranes co-expressing Galphai2 and Gbeta1gamma2 after 60 mins by liquid scintillation counting assay
ChEMBL 374 3 1 6 2.1 CN1CCN(c2nc(N)nc(/C=C/c3cccc(Br)c3)n2)CC1 10.1016/j.ejmech.2015.08.014
51354008 58899 None 0 Human Binding pKi = 5.9 5.9 -3 2
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells after 60 mins by liquid scintillation countingDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells after 60 mins by liquid scintillation counting
ChEMBL 253 5 1 4 1.8 c1ccc(Cc2cn(CCc3c[nH]cn3)nn2)cc1 10.1021/jm1013488
CHEMBL1688939 58899 None 0 Human Binding pKi = 5.9 5.9 -3 2
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells after 60 mins by liquid scintillation countingDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells after 60 mins by liquid scintillation counting
ChEMBL 253 5 1 4 1.8 c1ccc(Cc2cn(CCc3c[nH]cn3)nn2)cc1 10.1021/jm1013488
51354586 58919 None 0 Human Binding pKi = 5.9 5.9 -15 2
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells after 60 mins by liquid scintillation countingDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells after 60 mins by liquid scintillation counting
ChEMBL 273 5 1 4 2.9 CC(c1cn(CCc2c[nH]cn2)nn1)C1CCCCC1 10.1021/jm1013488
CHEMBL1688978 58919 None 0 Human Binding pKi = 5.9 5.9 -15 2
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells after 60 mins by liquid scintillation countingDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells after 60 mins by liquid scintillation counting
ChEMBL 273 5 1 4 2.9 CC(c1cn(CCc2c[nH]cn2)nn1)C1CCCCC1 10.1021/jm1013488
16082824 77977 None 0 Human Binding pKi = 6.9 6.9 1 2
Displacement of [3H]histamine form human H4 receptorDisplacement of [3H]histamine form human H4 receptor
ChEMBL 261 5 2 2 3.0 Clc1ccc(CNC[C@H]2C[C@@H]2c2c[nH]cn2)cc1 10.1021/jm0603318
CHEMBL209598 77977 None 0 Human Binding pKi = 6.9 6.9 1 2
Displacement of [3H]histamine form human H4 receptorDisplacement of [3H]histamine form human H4 receptor
ChEMBL 261 5 2 2 3.0 Clc1ccc(CNC[C@H]2C[C@@H]2c2c[nH]cn2)cc1 10.1021/jm0603318
54585778 61569 None 0 Human Binding pKi = 5.9 5.9 - 1
Displacement of [3H]histamine from human histamine H4 receptorDisplacement of [3H]histamine from human histamine H4 receptor
ChEMBL 252 4 3 7 -0.8 CN1CCN(c2cc(N)nc(NCCO)n2)CC1 10.1016/j.bmcl.2011.03.017
CHEMBL1770989 61569 None 0 Human Binding pKi = 5.9 5.9 - 1
Displacement of [3H]histamine from human histamine H4 receptorDisplacement of [3H]histamine from human histamine H4 receptor
ChEMBL 252 4 3 7 -0.8 CN1CCN(c2cc(N)nc(NCCO)n2)CC1 10.1016/j.bmcl.2011.03.017
58227165 117186 None 0 Human Binding pKi = 6.9 6.9 - 1
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 235 3 1 5 1.0 CC(C)Nc1nccc(N2CCN(C)CC2)n1 10.1016/j.bmcl.2014.12.027
CHEMBL3393536 117186 None 0 Human Binding pKi = 6.9 6.9 - 1
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 235 3 1 5 1.0 CC(C)Nc1nccc(N2CCN(C)CC2)n1 10.1016/j.bmcl.2014.12.027
24853664 96394 None 0 Human Binding pKi = 5.9 5.9 - 1
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells
ChEMBL 388 3 0 5 4.5 CN1CCN(c2nc3cc(Cl)c(Cl)cc3nc2Oc2ccccc2)CC1 10.1021/jm7014217
CHEMBL261517 96394 None 0 Human Binding pKi = 5.9 5.9 - 1
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells
ChEMBL 388 3 0 5 4.5 CN1CCN(c2nc3cc(Cl)c(Cl)cc3nc2Oc2ccccc2)CC1 10.1021/jm7014217
10773349 8093 None 1 Human Binding pKi = 4.9 4.9 -11 2
Histamine H4 receptor competition binding using [3H]Na-methylhistamineHistamine H4 receptor competition binding using [3H]Na-methylhistamine
ChEMBL 165 2 2 3 0.4 NC[C@H]1C=C[C@H](c2c[nH]cn2)O1 10.1021/jm0300025
CHEMBL109130 8093 None 1 Human Binding pKi = 4.9 4.9 -11 2
Histamine H4 receptor competition binding using [3H]Na-methylhistamineHistamine H4 receptor competition binding using [3H]Na-methylhistamine
ChEMBL 165 2 2 3 0.4 NC[C@H]1C=C[C@H](c2c[nH]cn2)O1 10.1021/jm0300025
10715857 75042 None 0 Human Binding pKi = 6.9 6.9 -3 3
Antagonist activity at human H4 receptor expressed in CHO cells co-expressing Galphai2 assessed as inhibition of imetit-induced GTPgamma[35S] binding after 30 mins by microbeta scintillation counting methodAntagonist activity at human H4 receptor expressed in CHO cells co-expressing Galphai2 assessed as inhibition of imetit-induced GTPgamma[35S] binding after 30 mins by microbeta scintillation counting method
ChEMBL 398 8 1 3 3.5 O=C(CCCc1ccc(I)cc1)OCCCc1c[nH]cn1 10.1016/j.ejmech.2016.09.074
CHEMBL20338 75042 None 0 Human Binding pKi = 6.9 6.9 -3 3
Antagonist activity at human H4 receptor expressed in CHO cells co-expressing Galphai2 assessed as inhibition of imetit-induced GTPgamma[35S] binding after 30 mins by microbeta scintillation counting methodAntagonist activity at human H4 receptor expressed in CHO cells co-expressing Galphai2 assessed as inhibition of imetit-induced GTPgamma[35S] binding after 30 mins by microbeta scintillation counting method
ChEMBL 398 8 1 3 3.5 O=C(CCCc1ccc(I)cc1)OCCCc1c[nH]cn1 10.1016/j.ejmech.2016.09.074
16082820 80149 None 0 Human Binding pKi = 6.9 6.9 - 1
Displacement of [3H]histamine form human H4 receptorDisplacement of [3H]histamine form human H4 receptor
ChEMBL 261 5 2 2 3.0 Clc1ccc(CNC[C@@H]2C[C@H]2c2c[nH]cn2)cc1 10.1021/jm0603318
CHEMBL213250 80149 None 0 Human Binding pKi = 6.9 6.9 - 1
Displacement of [3H]histamine form human H4 receptorDisplacement of [3H]histamine form human H4 receptor
ChEMBL 261 5 2 2 3.0 Clc1ccc(CNC[C@@H]2C[C@H]2c2c[nH]cn2)cc1 10.1021/jm0603318
10776393 5498 None 0 Human Binding pKi = 6.9 6.9 -25 3
Displacement of [3H]histamine from human histamine H4 receptor expressed in SF9 cells coexpressing Galphai2, Gbeta1gamma2Displacement of [3H]histamine from human histamine H4 receptor expressed in SF9 cells coexpressing Galphai2, Gbeta1gamma2
ChEMBL 239 7 2 3 2.1 CC[C@H](C)CNC(=O)OCCCc1c[nH]cn1 10.1016/j.bmcl.2009.10.005
CHEMBL1076267 5498 None 0 Human Binding pKi = 6.9 6.9 -25 3
Displacement of [3H]histamine from human histamine H4 receptor expressed in SF9 cells coexpressing Galphai2, Gbeta1gamma2Displacement of [3H]histamine from human histamine H4 receptor expressed in SF9 cells coexpressing Galphai2, Gbeta1gamma2
ChEMBL 239 7 2 3 2.1 CC[C@H](C)CNC(=O)OCCCc1c[nH]cn1 10.1016/j.bmcl.2009.10.005
CHEMBL156912 5498 None 0 Human Binding pKi = 6.9 6.9 -25 3
Displacement of [3H]histamine from human histamine H4 receptor expressed in SF9 cells coexpressing Galphai2, Gbeta1gamma2Displacement of [3H]histamine from human histamine H4 receptor expressed in SF9 cells coexpressing Galphai2, Gbeta1gamma2
ChEMBL 239 7 2 3 2.1 CC[C@H](C)CNC(=O)OCCCc1c[nH]cn1 10.1016/j.bmcl.2009.10.005
118725542 117187 None 0 Human Binding pKi = 6.9 6.9 - 1
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 235 4 2 5 1.1 CN[C@H]1CCN(c2ccnc(NC(C)C)n2)C1 10.1016/j.bmcl.2014.12.027
CHEMBL3393537 117187 None 0 Human Binding pKi = 6.9 6.9 - 1
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 235 4 2 5 1.1 CN[C@H]1CCN(c2ccnc(NC(C)C)n2)C1 10.1016/j.bmcl.2014.12.027
1278 2150 None 56 Human Binding pKi = 6.9 6.9 -3 8
Displacement of [3H]histamine from human recombinant histamine H4 receptor expressed in CHO cells coexpressing Ga15 by radioligand filtration binding assayDisplacement of [3H]histamine from human recombinant histamine H4 receptor expressed in CHO cells coexpressing Ga15 by radioligand filtration binding assay
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1016/j.bmcl.2011.11.098
1279 2150 None 56 Human Binding pKi = 6.9 6.9 -3 8
Displacement of [3H]histamine from human recombinant histamine H4 receptor expressed in CHO cells coexpressing Ga15 by radioligand filtration binding assayDisplacement of [3H]histamine from human recombinant histamine H4 receptor expressed in CHO cells coexpressing Ga15 by radioligand filtration binding assay
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1016/j.bmcl.2011.11.098
4908365 2150 None 56 Human Binding pKi = 6.9 6.9 -3 8
Displacement of [3H]histamine from human recombinant histamine H4 receptor expressed in CHO cells coexpressing Ga15 by radioligand filtration binding assayDisplacement of [3H]histamine from human recombinant histamine H4 receptor expressed in CHO cells coexpressing Ga15 by radioligand filtration binding assay
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1016/j.bmcl.2011.11.098
CHEMBL129198 2150 None 56 Human Binding pKi = 6.9 6.9 -3 8
Displacement of [3H]histamine from human recombinant histamine H4 receptor expressed in CHO cells coexpressing Ga15 by radioligand filtration binding assayDisplacement of [3H]histamine from human recombinant histamine H4 receptor expressed in CHO cells coexpressing Ga15 by radioligand filtration binding assay
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1016/j.bmcl.2011.11.098
90645161 112251 None 0 Human Binding pKi = 5.9 5.9 - 1
Displacement of [3H]-histamine from human histamine H4 receptor expressed in insect Sf9 cell membrane co-expressing Galphai2/Gbeta1gamma2 subunits after 60 mins by liquid scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor expressed in insect Sf9 cell membrane co-expressing Galphai2/Gbeta1gamma2 subunits after 60 mins by liquid scintillation counting analysis
ChEMBL 306 2 1 6 1.2 CN1CCN(c2nc(N)nc(-c3cc(F)cc(F)c3)n2)CC1 10.1016/j.ejmech.2014.06.032
CHEMBL3290588 112251 None 0 Human Binding pKi = 5.9 5.9 - 1
Displacement of [3H]-histamine from human histamine H4 receptor expressed in insect Sf9 cell membrane co-expressing Galphai2/Gbeta1gamma2 subunits after 60 mins by liquid scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor expressed in insect Sf9 cell membrane co-expressing Galphai2/Gbeta1gamma2 subunits after 60 mins by liquid scintillation counting analysis
ChEMBL 306 2 1 6 1.2 CN1CCN(c2nc(N)nc(-c3cc(F)cc(F)c3)n2)CC1 10.1016/j.ejmech.2014.06.032
1278 2150 None 56 Human Binding pKi = 7.9 7.9 -3 8
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/jm800670r
1279 2150 None 56 Human Binding pKi = 7.9 7.9 -3 8
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/jm800670r
4908365 2150 None 56 Human Binding pKi = 7.9 7.9 -3 8
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/jm800670r
CHEMBL129198 2150 None 56 Human Binding pKi = 7.9 7.9 -3 8
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/jm800670r
45257132 3682 None 14 Human Binding pKi = 7.9 7.9 42 4
Displacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2Displacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2
ChEMBL 366 4 2 6 2.7 CN1CCN(CC1)c1cc(NCc2c(Cl)cccc2Cl)nc(n1)N 10.1016/j.bmc.2009.08.059
8983 3682 None 14 Human Binding pKi = 7.9 7.9 42 4
Displacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2Displacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2
ChEMBL 366 4 2 6 2.7 CN1CCN(CC1)c1cc(NCc2c(Cl)cccc2Cl)nc(n1)N 10.1016/j.bmc.2009.08.059
CHEMBL595180 3682 None 14 Human Binding pKi = 7.9 7.9 42 4
Displacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2Displacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2
ChEMBL 366 4 2 6 2.7 CN1CCN(CC1)c1cc(NCc2c(Cl)cccc2Cl)nc(n1)N 10.1016/j.bmc.2009.08.059
24994634 2142 None 30 Human Binding pKi = 7.9 7.9 -2 7
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 221 2 2 5 0.7 N[C@@H]1CCN(C1)c1cc(nc(n1)N)C(C)C 10.1016/j.bmcl.2014.12.027
24994634 2142 None 30 Human Binding pKi = 7.9 7.9 -2 7
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 221 2 2 5 0.7 N[C@@H]1CCN(C1)c1cc(nc(n1)N)C(C)C 10.1021/acs.jmedchem.5b00516
8984 2142 None 30 Human Binding pKi = 7.9 7.9 -2 7
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 221 2 2 5 0.7 N[C@@H]1CCN(C1)c1cc(nc(n1)N)C(C)C 10.1016/j.bmcl.2014.12.027
8984 2142 None 30 Human Binding pKi = 7.9 7.9 -2 7
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 221 2 2 5 0.7 N[C@@H]1CCN(C1)c1cc(nc(n1)N)C(C)C 10.1021/acs.jmedchem.5b00516
CHEMBL3236549 2142 None 30 Human Binding pKi = 7.9 7.9 -2 7
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 221 2 2 5 0.7 N[C@@H]1CCN(C1)c1cc(nc(n1)N)C(C)C 10.1016/j.bmcl.2014.12.027
CHEMBL3236549 2142 None 30 Human Binding pKi = 7.9 7.9 -2 7
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 221 2 2 5 0.7 N[C@@H]1CCN(C1)c1cc(nc(n1)N)C(C)C 10.1021/acs.jmedchem.5b00516
24994635 110198 None 0 Human Binding pKi = 7.9 7.9 - 1
Displacement of [3H]histamine from human recombinant histamine H4 receptor expressed in SK-N-MC cells after 45 mins by competition binding analysisDisplacement of [3H]histamine from human recombinant histamine H4 receptor expressed in SK-N-MC cells after 45 mins by competition binding analysis
ChEMBL 235 3 2 5 1.0 CN[C@@H]1CCN(c2cc(C(C)C)nc(N)n2)C1 10.1021/jm401727m
CHEMBL3236570 110198 None 0 Human Binding pKi = 7.9 7.9 - 1
Displacement of [3H]histamine from human recombinant histamine H4 receptor expressed in SK-N-MC cells after 45 mins by competition binding analysisDisplacement of [3H]histamine from human recombinant histamine H4 receptor expressed in SK-N-MC cells after 45 mins by competition binding analysis
ChEMBL 235 3 2 5 1.0 CN[C@@H]1CCN(c2cc(C(C)C)nc(N)n2)C1 10.1021/jm401727m
24826442 68129 None 0 Human Binding pKi = 7.9 7.9 - 1
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 313 2 1 7 1.7 COc1ccc2oc3c(N4CCN(C)CC4)nc(N)nc3c2c1 10.1016/j.bmcl.2011.08.014
CHEMBL1914756 68129 None 0 Human Binding pKi = 7.9 7.9 - 1
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 313 2 1 7 1.7 COc1ccc2oc3c(N4CCN(C)CC4)nc(N)nc3c2c1 10.1016/j.bmcl.2011.08.014
1278 2150 None 56 Human Binding pKi = 7.9 7.9 -3 8
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/jm8005959
1278 2150 None 56 Human Binding pKi = 7.9 7.9 -3 8
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/jm800670r
1279 2150 None 56 Human Binding pKi = 7.9 7.9 -3 8
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/jm8005959
1279 2150 None 56 Human Binding pKi = 7.9 7.9 -3 8
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/jm800670r
4908365 2150 None 56 Human Binding pKi = 7.9 7.9 -3 8
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/jm8005959
4908365 2150 None 56 Human Binding pKi = 7.9 7.9 -3 8
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/jm800670r
CHEMBL129198 2150 None 56 Human Binding pKi = 7.9 7.9 -3 8
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/jm8005959
CHEMBL129198 2150 None 56 Human Binding pKi = 7.9 7.9 -3 8
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/jm800670r
1204 1932 None 74 Human Binding pKi = 7.9 7.9 -3 24
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells after 60 mins by liquid scintillation countingDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells after 60 mins by liquid scintillation counting
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm1013488
1247 1932 None 74 Human Binding pKi = 7.9 7.9 -3 24
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells after 60 mins by liquid scintillation countingDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells after 60 mins by liquid scintillation counting
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm1013488
1375 1932 None 74 Human Binding pKi = 7.9 7.9 -3 24
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells after 60 mins by liquid scintillation countingDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells after 60 mins by liquid scintillation counting
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm1013488
774 1932 None 74 Human Binding pKi = 7.9 7.9 -3 24
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells after 60 mins by liquid scintillation countingDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells after 60 mins by liquid scintillation counting
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm1013488
774.0 1932 None 74 Human Binding pKi = 7.9 7.9 -3 24
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells after 60 mins by liquid scintillation countingDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells after 60 mins by liquid scintillation counting
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm1013488
CHEMBL90 1932 None 74 Human Binding pKi = 7.9 7.9 -3 24
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells after 60 mins by liquid scintillation countingDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells after 60 mins by liquid scintillation counting
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm1013488
DB05381 1932 None 74 Human Binding pKi = 7.9 7.9 -3 24
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells after 60 mins by liquid scintillation countingDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells after 60 mins by liquid scintillation counting
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm1013488
1278 2150 None 56 Human Binding pKi = 7.9 7.9 -3 8
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/jm8007618
1279 2150 None 56 Human Binding pKi = 7.9 7.9 -3 8
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/jm8007618
4908365 2150 None 56 Human Binding pKi = 7.9 7.9 -3 8
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/jm8007618
CHEMBL129198 2150 None 56 Human Binding pKi = 7.9 7.9 -3 8
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/jm8007618
1204 1932 None 74 Human Binding pKi = 7.9 7.9 -3 24
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm7014217
1204 1932 None 74 Human Binding pKi = 7.9 7.9 -3 24
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm901379s
1247 1932 None 74 Human Binding pKi = 7.9 7.9 -3 24
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm7014217
1247 1932 None 74 Human Binding pKi = 7.9 7.9 -3 24
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm901379s
1375 1932 None 74 Human Binding pKi = 7.9 7.9 -3 24
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm7014217
1375 1932 None 74 Human Binding pKi = 7.9 7.9 -3 24
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm901379s
774 1932 None 74 Human Binding pKi = 7.9 7.9 -3 24
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm7014217
774 1932 None 74 Human Binding pKi = 7.9 7.9 -3 24
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm901379s
774.0 1932 None 74 Human Binding pKi = 7.9 7.9 -3 24
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm7014217
774.0 1932 None 74 Human Binding pKi = 7.9 7.9 -3 24
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm901379s
CHEMBL90 1932 None 74 Human Binding pKi = 7.9 7.9 -3 24
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm7014217
CHEMBL90 1932 None 74 Human Binding pKi = 7.9 7.9 -3 24
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm901379s
DB05381 1932 None 74 Human Binding pKi = 7.9 7.9 -3 24
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm7014217
DB05381 1932 None 74 Human Binding pKi = 7.9 7.9 -3 24
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm901379s
155513612 176425 None 0 Human Binding pKi = 7.9 7.9 1 4
Inhibition of UR-DEBa242 binding to human recombinant NLuc/GPCR-fused H4R expressed in HEK293T cells measured after 30 mins by furimazine substrate based BRET assayInhibition of UR-DEBa242 binding to human recombinant NLuc/GPCR-fused H4R expressed in HEK293T cells measured after 30 mins by furimazine substrate based BRET assay
ChEMBL 277 4 1 5 2.1 CN(C)[C@@H]1CCN(c2ccnc(NCC(C)(C)C)n2)C1 10.1021/acs.jmedchem.0c00160
CHEMBL4439142 176425 None 0 Human Binding pKi = 7.9 7.9 1 4
Inhibition of UR-DEBa242 binding to human recombinant NLuc/GPCR-fused H4R expressed in HEK293T cells measured after 30 mins by furimazine substrate based BRET assayInhibition of UR-DEBa242 binding to human recombinant NLuc/GPCR-fused H4R expressed in HEK293T cells measured after 30 mins by furimazine substrate based BRET assay
ChEMBL 277 4 1 5 2.1 CN(C)[C@@H]1CCN(c2ccnc(NCC(C)(C)C)n2)C1 10.1021/acs.jmedchem.0c00160
CHEMBL4515149 176425 None 0 Human Binding pKi = 7.9 7.9 1 4
Inhibition of UR-DEBa242 binding to human recombinant NLuc/GPCR-fused H4R expressed in HEK293T cells measured after 30 mins by furimazine substrate based BRET assayInhibition of UR-DEBa242 binding to human recombinant NLuc/GPCR-fused H4R expressed in HEK293T cells measured after 30 mins by furimazine substrate based BRET assay
ChEMBL 277 4 1 5 2.1 CN(C)[C@@H]1CCN(c2ccnc(NCC(C)(C)C)n2)C1 10.1021/acs.jmedchem.0c00160
CHEMBL4595327 176425 None 0 Human Binding pKi = 7.9 7.9 1 4
Inhibition of UR-DEBa242 binding to human recombinant NLuc/GPCR-fused H4R expressed in HEK293T cells measured after 30 mins by furimazine substrate based BRET assayInhibition of UR-DEBa242 binding to human recombinant NLuc/GPCR-fused H4R expressed in HEK293T cells measured after 30 mins by furimazine substrate based BRET assay
ChEMBL 277 4 1 5 2.1 CN(C)[C@@H]1CCN(c2ccnc(NCC(C)(C)C)n2)C1 10.1021/acs.jmedchem.0c00160
1226 2019 None 19 Human Binding pKi = 7.9 7.9 2 7
Binding affinity to the human histamine H4 receptorBinding affinity to the human histamine H4 receptor
ChEMBL 321 9 4 4 1.2 NC(=NCCCc1cnc[nH]1)NCCSCc1nc[nH]c1C 10.1021/jm0341047
41376 2019 None 19 Human Binding pKi = 7.9 7.9 2 7
Binding affinity to the human histamine H4 receptorBinding affinity to the human histamine H4 receptor
ChEMBL 321 9 4 4 1.2 NC(=NCCCc1cnc[nH]1)NCCSCc1nc[nH]c1C 10.1021/jm0341047
CHEMBL12608 2019 None 19 Human Binding pKi = 7.9 7.9 2 7
Binding affinity to the human histamine H4 receptorBinding affinity to the human histamine H4 receptor
ChEMBL 321 9 4 4 1.2 NC(=NCCCc1cnc[nH]1)NCCSCc1nc[nH]c1C 10.1021/jm0341047
24745335 295 None 13 Rat Binding pKi = 7.9 7.9 -4 5
Displacement of [3H]-histamine from rat H4R expressed in HEK293T cellsDisplacement of [3H]-histamine from rat H4R expressed in HEK293T cells
ChEMBL 262 5 3 6 0.7 CN[C@@H]1CCN(C1)c1cc(NCC2CC2)nc(n1)N 10.1016/j.bmcl.2011.07.125
8985 295 None 13 Rat Binding pKi = 7.9 7.9 -4 5
Displacement of [3H]-histamine from rat H4R expressed in HEK293T cellsDisplacement of [3H]-histamine from rat H4R expressed in HEK293T cells
ChEMBL 262 5 3 6 0.7 CN[C@@H]1CCN(C1)c1cc(NCC2CC2)nc(n1)N 10.1016/j.bmcl.2011.07.125
CHEMBL1915540 295 None 13 Rat Binding pKi = 7.9 7.9 -4 5
Displacement of [3H]-histamine from rat H4R expressed in HEK293T cellsDisplacement of [3H]-histamine from rat H4R expressed in HEK293T cells
ChEMBL 262 5 3 6 0.7 CN[C@@H]1CCN(C1)c1cc(NCC2CC2)nc(n1)N 10.1016/j.bmcl.2011.07.125
DB15027 295 None 13 Rat Binding pKi = 7.9 7.9 -4 5
Displacement of [3H]-histamine from rat H4R expressed in HEK293T cellsDisplacement of [3H]-histamine from rat H4R expressed in HEK293T cells
ChEMBL 262 5 3 6 0.7 CN[C@@H]1CCN(C1)c1cc(NCC2CC2)nc(n1)N 10.1016/j.bmcl.2011.07.125
71603135 89748 None 0 Human Binding pKi = 7.9 7.9 26 2
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 297 2 2 5 2.3 Nc1nc(N2CCNCC2)c2ccc(C3CCCC3)cc2n1 10.1016/j.bmcl.2013.02.091
CHEMBL2376789 89748 None 0 Human Binding pKi = 7.9 7.9 26 2
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 297 2 2 5 2.3 Nc1nc(N2CCNCC2)c2ccc(C3CCCC3)cc2n1 10.1016/j.bmcl.2013.02.091
71525589 89766 None 0 Human Binding pKi = 7.9 7.9 11 2
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 286 3 2 6 1.5 CN[C@@H]1CCN(c2nc(N)nc3cc(C(C)C)cnc23)C1 10.1016/j.bmcl.2013.02.091
CHEMBL2376807 89766 None 0 Human Binding pKi = 7.9 7.9 11 2
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 286 3 2 6 1.5 CN[C@@H]1CCN(c2nc(N)nc3cc(C(C)C)cnc23)C1 10.1016/j.bmcl.2013.02.091
24745335 295 None 13 Rat Binding pKi = 7.9 7.9 -4 5
Displacement of [3H]histamine from rat histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from rat histamine H4 receptor expressed in HEK293T cells
ChEMBL 262 5 3 6 0.7 CN[C@@H]1CCN(C1)c1cc(NCC2CC2)nc(n1)N 10.1021/acs.jmedchem.5b00516
8985 295 None 13 Rat Binding pKi = 7.9 7.9 -4 5
Displacement of [3H]histamine from rat histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from rat histamine H4 receptor expressed in HEK293T cells
ChEMBL 262 5 3 6 0.7 CN[C@@H]1CCN(C1)c1cc(NCC2CC2)nc(n1)N 10.1021/acs.jmedchem.5b00516
CHEMBL1915540 295 None 13 Rat Binding pKi = 7.9 7.9 -4 5
Displacement of [3H]histamine from rat histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from rat histamine H4 receptor expressed in HEK293T cells
ChEMBL 262 5 3 6 0.7 CN[C@@H]1CCN(C1)c1cc(NCC2CC2)nc(n1)N 10.1021/acs.jmedchem.5b00516
DB15027 295 None 13 Rat Binding pKi = 7.9 7.9 -4 5
Displacement of [3H]histamine from rat histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from rat histamine H4 receptor expressed in HEK293T cells
ChEMBL 262 5 3 6 0.7 CN[C@@H]1CCN(C1)c1cc(NCC2CC2)nc(n1)N 10.1021/acs.jmedchem.5b00516
24994634 2142 None 30 Human Binding pKi = 7.9 7.9 -2 7
Binding assayBinding assay
ChEMBL 221 2 2 5 0.7 N[C@@H]1CCN(C1)c1cc(nc(n1)N)C(C)C 10.6019/CHEMBL5058644
8984 2142 None 30 Human Binding pKi = 7.9 7.9 -2 7
Binding assayBinding assay
ChEMBL 221 2 2 5 0.7 N[C@@H]1CCN(C1)c1cc(nc(n1)N)C(C)C 10.6019/CHEMBL5058644
CHEMBL3236549 2142 None 30 Human Binding pKi = 7.9 7.9 -2 7
Binding assayBinding assay
ChEMBL 221 2 2 5 0.7 N[C@@H]1CCN(C1)c1cc(nc(n1)N)C(C)C 10.6019/CHEMBL5058644
24994634 2142 None 30 Human Binding pKi = 7.9 7.9 -2 7
Displacement of [3H]histamine from human recombinant histamine H4 receptor expressed in SK-N-MC cells after 45 mins by competition binding analysisDisplacement of [3H]histamine from human recombinant histamine H4 receptor expressed in SK-N-MC cells after 45 mins by competition binding analysis
ChEMBL 221 2 2 5 0.7 N[C@@H]1CCN(C1)c1cc(nc(n1)N)C(C)C 10.1021/jm401727m
8984 2142 None 30 Human Binding pKi = 7.9 7.9 -2 7
Displacement of [3H]histamine from human recombinant histamine H4 receptor expressed in SK-N-MC cells after 45 mins by competition binding analysisDisplacement of [3H]histamine from human recombinant histamine H4 receptor expressed in SK-N-MC cells after 45 mins by competition binding analysis
ChEMBL 221 2 2 5 0.7 N[C@@H]1CCN(C1)c1cc(nc(n1)N)C(C)C 10.1021/jm401727m
CHEMBL3236549 2142 None 30 Human Binding pKi = 7.9 7.9 -2 7
Displacement of [3H]histamine from human recombinant histamine H4 receptor expressed in SK-N-MC cells after 45 mins by competition binding analysisDisplacement of [3H]histamine from human recombinant histamine H4 receptor expressed in SK-N-MC cells after 45 mins by competition binding analysis
ChEMBL 221 2 2 5 0.7 N[C@@H]1CCN(C1)c1cc(nc(n1)N)C(C)C 10.1021/jm401727m
3035746 188286 None 6 Human Binding pKi = 7.9 7.9 -1 2
Binding affinity to human H4RBinding affinity to human H4R
ChEMBL 414 7 2 3 3.2 N/C(=N/CCc1ccc(I)cc1)SCCCc1cnc[nH]1 10.1021/acs.jmedchem.9b01342
CHEMBL1237146 188286 None 6 Human Binding pKi = 7.9 7.9 -1 2
Binding affinity to human H4RBinding affinity to human H4R
ChEMBL 414 7 2 3 3.2 N/C(=N/CCc1ccc(I)cc1)SCCCc1cnc[nH]1 10.1021/acs.jmedchem.9b01342
CHEMBL498770 188286 None 6 Human Binding pKi = 7.9 7.9 -1 2
Binding affinity to human H4RBinding affinity to human H4R
ChEMBL 414 7 2 3 3.2 N/C(=N/CCc1ccc(I)cc1)SCCCc1cnc[nH]1 10.1021/acs.jmedchem.9b01342
1204 1932 None 74 Human Binding pKi = 7.9 7.9 -3 24
Binding affinity to human recombinant histamine H4 receptor expressed in human SK-N-MC cells by radioligand displacement assayBinding affinity to human recombinant histamine H4 receptor expressed in human SK-N-MC cells by radioligand displacement assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmcl.2010.10.041
1247 1932 None 74 Human Binding pKi = 7.9 7.9 -3 24
Binding affinity to human recombinant histamine H4 receptor expressed in human SK-N-MC cells by radioligand displacement assayBinding affinity to human recombinant histamine H4 receptor expressed in human SK-N-MC cells by radioligand displacement assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmcl.2010.10.041
1375 1932 None 74 Human Binding pKi = 7.9 7.9 -3 24
Binding affinity to human recombinant histamine H4 receptor expressed in human SK-N-MC cells by radioligand displacement assayBinding affinity to human recombinant histamine H4 receptor expressed in human SK-N-MC cells by radioligand displacement assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmcl.2010.10.041
774 1932 None 74 Human Binding pKi = 7.9 7.9 -3 24
Binding affinity to human recombinant histamine H4 receptor expressed in human SK-N-MC cells by radioligand displacement assayBinding affinity to human recombinant histamine H4 receptor expressed in human SK-N-MC cells by radioligand displacement assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmcl.2010.10.041
774.0 1932 None 74 Human Binding pKi = 7.9 7.9 -3 24
Binding affinity to human recombinant histamine H4 receptor expressed in human SK-N-MC cells by radioligand displacement assayBinding affinity to human recombinant histamine H4 receptor expressed in human SK-N-MC cells by radioligand displacement assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmcl.2010.10.041
CHEMBL90 1932 None 74 Human Binding pKi = 7.9 7.9 -3 24
Binding affinity to human recombinant histamine H4 receptor expressed in human SK-N-MC cells by radioligand displacement assayBinding affinity to human recombinant histamine H4 receptor expressed in human SK-N-MC cells by radioligand displacement assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmcl.2010.10.041
DB05381 1932 None 74 Human Binding pKi = 7.9 7.9 -3 24
Binding affinity to human recombinant histamine H4 receptor expressed in human SK-N-MC cells by radioligand displacement assayBinding affinity to human recombinant histamine H4 receptor expressed in human SK-N-MC cells by radioligand displacement assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmcl.2010.10.041
155513612 176425 None 0 Human Binding pKi = 7.9 7.9 1 4
Displacement of [3H]-histamine from Galphai2/Gbeta1gamma2-coupled human recombinant H4R expressed in baculovirus infected Sf9 insect cell membranesDisplacement of [3H]-histamine from Galphai2/Gbeta1gamma2-coupled human recombinant H4R expressed in baculovirus infected Sf9 insect cell membranes
ChEMBL 277 4 1 5 2.1 CN(C)[C@@H]1CCN(c2ccnc(NCC(C)(C)C)n2)C1 10.1021/acs.jmedchem.0c00160
CHEMBL4439142 176425 None 0 Human Binding pKi = 7.9 7.9 1 4
Displacement of [3H]-histamine from Galphai2/Gbeta1gamma2-coupled human recombinant H4R expressed in baculovirus infected Sf9 insect cell membranesDisplacement of [3H]-histamine from Galphai2/Gbeta1gamma2-coupled human recombinant H4R expressed in baculovirus infected Sf9 insect cell membranes
ChEMBL 277 4 1 5 2.1 CN(C)[C@@H]1CCN(c2ccnc(NCC(C)(C)C)n2)C1 10.1021/acs.jmedchem.0c00160
CHEMBL4515149 176425 None 0 Human Binding pKi = 7.9 7.9 1 4
Displacement of [3H]-histamine from Galphai2/Gbeta1gamma2-coupled human recombinant H4R expressed in baculovirus infected Sf9 insect cell membranesDisplacement of [3H]-histamine from Galphai2/Gbeta1gamma2-coupled human recombinant H4R expressed in baculovirus infected Sf9 insect cell membranes
ChEMBL 277 4 1 5 2.1 CN(C)[C@@H]1CCN(c2ccnc(NCC(C)(C)C)n2)C1 10.1021/acs.jmedchem.0c00160
CHEMBL4595327 176425 None 0 Human Binding pKi = 7.9 7.9 1 4
Displacement of [3H]-histamine from Galphai2/Gbeta1gamma2-coupled human recombinant H4R expressed in baculovirus infected Sf9 insect cell membranesDisplacement of [3H]-histamine from Galphai2/Gbeta1gamma2-coupled human recombinant H4R expressed in baculovirus infected Sf9 insect cell membranes
ChEMBL 277 4 1 5 2.1 CN(C)[C@@H]1CCN(c2ccnc(NCC(C)(C)C)n2)C1 10.1021/acs.jmedchem.0c00160
1204 1932 None 74 Human Binding pKi = 7.9 7.9 -3 24
Displacement of [3H]-histamine from Galphai2/Gbeta1gamma2-coupled human recombinant H4R expressed in baculovirus infected Sf9 insect cell membranes measured after 60 mins by microbeta scintillation counting methodDisplacement of [3H]-histamine from Galphai2/Gbeta1gamma2-coupled human recombinant H4R expressed in baculovirus infected Sf9 insect cell membranes measured after 60 mins by microbeta scintillation counting method
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.0c00160
1247 1932 None 74 Human Binding pKi = 7.9 7.9 -3 24
Displacement of [3H]-histamine from Galphai2/Gbeta1gamma2-coupled human recombinant H4R expressed in baculovirus infected Sf9 insect cell membranes measured after 60 mins by microbeta scintillation counting methodDisplacement of [3H]-histamine from Galphai2/Gbeta1gamma2-coupled human recombinant H4R expressed in baculovirus infected Sf9 insect cell membranes measured after 60 mins by microbeta scintillation counting method
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.0c00160
1375 1932 None 74 Human Binding pKi = 7.9 7.9 -3 24
Displacement of [3H]-histamine from Galphai2/Gbeta1gamma2-coupled human recombinant H4R expressed in baculovirus infected Sf9 insect cell membranes measured after 60 mins by microbeta scintillation counting methodDisplacement of [3H]-histamine from Galphai2/Gbeta1gamma2-coupled human recombinant H4R expressed in baculovirus infected Sf9 insect cell membranes measured after 60 mins by microbeta scintillation counting method
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.0c00160
774 1932 None 74 Human Binding pKi = 7.9 7.9 -3 24
Displacement of [3H]-histamine from Galphai2/Gbeta1gamma2-coupled human recombinant H4R expressed in baculovirus infected Sf9 insect cell membranes measured after 60 mins by microbeta scintillation counting methodDisplacement of [3H]-histamine from Galphai2/Gbeta1gamma2-coupled human recombinant H4R expressed in baculovirus infected Sf9 insect cell membranes measured after 60 mins by microbeta scintillation counting method
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.0c00160
774.0 1932 None 74 Human Binding pKi = 7.9 7.9 -3 24
Displacement of [3H]-histamine from Galphai2/Gbeta1gamma2-coupled human recombinant H4R expressed in baculovirus infected Sf9 insect cell membranes measured after 60 mins by microbeta scintillation counting methodDisplacement of [3H]-histamine from Galphai2/Gbeta1gamma2-coupled human recombinant H4R expressed in baculovirus infected Sf9 insect cell membranes measured after 60 mins by microbeta scintillation counting method
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.0c00160
CHEMBL90 1932 None 74 Human Binding pKi = 7.9 7.9 -3 24
Displacement of [3H]-histamine from Galphai2/Gbeta1gamma2-coupled human recombinant H4R expressed in baculovirus infected Sf9 insect cell membranes measured after 60 mins by microbeta scintillation counting methodDisplacement of [3H]-histamine from Galphai2/Gbeta1gamma2-coupled human recombinant H4R expressed in baculovirus infected Sf9 insect cell membranes measured after 60 mins by microbeta scintillation counting method
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.0c00160
DB05381 1932 None 74 Human Binding pKi = 7.9 7.9 -3 24
Displacement of [3H]-histamine from Galphai2/Gbeta1gamma2-coupled human recombinant H4R expressed in baculovirus infected Sf9 insect cell membranes measured after 60 mins by microbeta scintillation counting methodDisplacement of [3H]-histamine from Galphai2/Gbeta1gamma2-coupled human recombinant H4R expressed in baculovirus infected Sf9 insect cell membranes measured after 60 mins by microbeta scintillation counting method
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.0c00160
1249 2009 None 10 Human Binding pKi = 7.9 7.9 -3 3
Displacement of [3H]-histamine from Galphai2/Gbeta1gamma2-coupled human recombinant H4R expressed in baculovirus infected Sf9 insect cell membranes measured after 60 mins by microbeta scintillation counting methodDisplacement of [3H]-histamine from Galphai2/Gbeta1gamma2-coupled human recombinant H4R expressed in baculovirus infected Sf9 insect cell membranes measured after 60 mins by microbeta scintillation counting method
ChEMBL 139 4 2 2 0.7 NCCCCc1cnc[nH]1 10.1021/acs.jmedchem.0c00160
13499360 2009 None 10 Human Binding pKi = 7.9 7.9 -3 3
Displacement of [3H]-histamine from Galphai2/Gbeta1gamma2-coupled human recombinant H4R expressed in baculovirus infected Sf9 insect cell membranes measured after 60 mins by microbeta scintillation counting methodDisplacement of [3H]-histamine from Galphai2/Gbeta1gamma2-coupled human recombinant H4R expressed in baculovirus infected Sf9 insect cell membranes measured after 60 mins by microbeta scintillation counting method
ChEMBL 139 4 2 2 0.7 NCCCCc1cnc[nH]1 10.1021/acs.jmedchem.0c00160
CHEMBL90019 2009 None 10 Human Binding pKi = 7.9 7.9 -3 3
Displacement of [3H]-histamine from Galphai2/Gbeta1gamma2-coupled human recombinant H4R expressed in baculovirus infected Sf9 insect cell membranes measured after 60 mins by microbeta scintillation counting methodDisplacement of [3H]-histamine from Galphai2/Gbeta1gamma2-coupled human recombinant H4R expressed in baculovirus infected Sf9 insect cell membranes measured after 60 mins by microbeta scintillation counting method
ChEMBL 139 4 2 2 0.7 NCCCCc1cnc[nH]1 10.1021/acs.jmedchem.0c00160
1253 2058 None 4 Human Binding pKi = 7.9 7.9 -11 4
Displacement of [3H]-histamine from human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2Displacement of [3H]-histamine from human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2
ChEMBL 342 6 1 2 3.2 Ic1ccc(cc1)COCCCc1cnc[nH]1 10.1016/j.bmcl.2010.10.041
132937 2058 None 4 Human Binding pKi = 7.9 7.9 -11 4
Displacement of [3H]-histamine from human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2Displacement of [3H]-histamine from human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2
ChEMBL 342 6 1 2 3.2 Ic1ccc(cc1)COCCCc1cnc[nH]1 10.1016/j.bmcl.2010.10.041
CHEMBL19010 2058 None 4 Human Binding pKi = 7.9 7.9 -11 4
Displacement of [3H]-histamine from human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2Displacement of [3H]-histamine from human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2
ChEMBL 342 6 1 2 3.2 Ic1ccc(cc1)COCCCc1cnc[nH]1 10.1016/j.bmcl.2010.10.041
10023327 169119 None 0 Human Binding pKi = 7.9 7.9 -144 3
Displacement of [3H]histamine from human H4 receptor Q7.42L mutant expressed in HEK293 cells after 1 to 1.5 hrs by scintillation countingDisplacement of [3H]histamine from human H4 receptor Q7.42L mutant expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting
ChEMBL 390 7 2 3 5.2 Clc1ccc(CN/C(=N\C2CCCCC2)SCCCc2c[nH]cn2)cc1 10.1021/jm201042n
CHEMBL43934 169119 None 0 Human Binding pKi = 7.9 7.9 -144 3
Displacement of [3H]histamine from human H4 receptor Q7.42L mutant expressed in HEK293 cells after 1 to 1.5 hrs by scintillation countingDisplacement of [3H]histamine from human H4 receptor Q7.42L mutant expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting
ChEMBL 390 7 2 3 5.2 Clc1ccc(CN/C(=N\C2CCCCC2)SCCCc2c[nH]cn2)cc1 10.1021/jm201042n
10023327 169119 None 0 Human Binding pKi = 7.9 7.9 -144 3
Displacement of [3H]histamine from human H4 receptor T5.42A mutant expressed in HEK293 cells after 1 to 1.5 hrs by scintillation countingDisplacement of [3H]histamine from human H4 receptor T5.42A mutant expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting
ChEMBL 390 7 2 3 5.2 Clc1ccc(CN/C(=N\C2CCCCC2)SCCCc2c[nH]cn2)cc1 10.1021/jm201042n
CHEMBL43934 169119 None 0 Human Binding pKi = 7.9 7.9 -144 3
Displacement of [3H]histamine from human H4 receptor T5.42A mutant expressed in HEK293 cells after 1 to 1.5 hrs by scintillation countingDisplacement of [3H]histamine from human H4 receptor T5.42A mutant expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting
ChEMBL 390 7 2 3 5.2 Clc1ccc(CN/C(=N\C2CCCCC2)SCCCc2c[nH]cn2)cc1 10.1021/jm201042n
10023327 169119 None 0 Human Binding pKi = 7.9 7.9 -144 3
Displacement of [3H]histamine from human H4 receptor T6.55M mutant expressed in HEK293 cells after 1 to 1.5 hrs by scintillation countingDisplacement of [3H]histamine from human H4 receptor T6.55M mutant expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting
ChEMBL 390 7 2 3 5.2 Clc1ccc(CN/C(=N\C2CCCCC2)SCCCc2c[nH]cn2)cc1 10.1021/jm201042n
CHEMBL43934 169119 None 0 Human Binding pKi = 7.9 7.9 -144 3
Displacement of [3H]histamine from human H4 receptor T6.55M mutant expressed in HEK293 cells after 1 to 1.5 hrs by scintillation countingDisplacement of [3H]histamine from human H4 receptor T6.55M mutant expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting
ChEMBL 390 7 2 3 5.2 Clc1ccc(CN/C(=N\C2CCCCC2)SCCCc2c[nH]cn2)cc1 10.1021/jm201042n
1253 2058 None 4 Human Binding pKi = 7.9 7.9 -11 4
Displacement of [3H]histamine from human H4 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation countingDisplacement of [3H]histamine from human H4 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting
ChEMBL 342 6 1 2 3.2 Ic1ccc(cc1)COCCCc1cnc[nH]1 10.1021/jm201042n
132937 2058 None 4 Human Binding pKi = 7.9 7.9 -11 4
Displacement of [3H]histamine from human H4 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation countingDisplacement of [3H]histamine from human H4 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting
ChEMBL 342 6 1 2 3.2 Ic1ccc(cc1)COCCCc1cnc[nH]1 10.1021/jm201042n
CHEMBL19010 2058 None 4 Human Binding pKi = 7.9 7.9 -11 4
Displacement of [3H]histamine from human H4 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation countingDisplacement of [3H]histamine from human H4 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting
ChEMBL 342 6 1 2 3.2 Ic1ccc(cc1)COCCCc1cnc[nH]1 10.1021/jm201042n
1204 1932 None 74 Human Binding pKi = 7.9 7.9 -3 24
Displacement of [3H]histamine from human histamine H4 receptorDisplacement of [3H]histamine from human histamine H4 receptor
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm060880d
1247 1932 None 74 Human Binding pKi = 7.9 7.9 -3 24
Displacement of [3H]histamine from human histamine H4 receptorDisplacement of [3H]histamine from human histamine H4 receptor
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm060880d
1375 1932 None 74 Human Binding pKi = 7.9 7.9 -3 24
Displacement of [3H]histamine from human histamine H4 receptorDisplacement of [3H]histamine from human histamine H4 receptor
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm060880d
774 1932 None 74 Human Binding pKi = 7.9 7.9 -3 24
Displacement of [3H]histamine from human histamine H4 receptorDisplacement of [3H]histamine from human histamine H4 receptor
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm060880d
774.0 1932 None 74 Human Binding pKi = 7.9 7.9 -3 24
Displacement of [3H]histamine from human histamine H4 receptorDisplacement of [3H]histamine from human histamine H4 receptor
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm060880d
CHEMBL90 1932 None 74 Human Binding pKi = 7.9 7.9 -3 24
Displacement of [3H]histamine from human histamine H4 receptorDisplacement of [3H]histamine from human histamine H4 receptor
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm060880d
DB05381 1932 None 74 Human Binding pKi = 7.9 7.9 -3 24
Displacement of [3H]histamine from human histamine H4 receptorDisplacement of [3H]histamine from human histamine H4 receptor
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm060880d
11065080 19441 None 0 Human Binding pKi = 7.9 7.9 - 1
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 257 1 1 2 1.9 Cc1cccc2cc(C(=O)N3CCN(C)CC3)[nH]c12 10.1016/j.ejmech.2012.06.016
CHEMBL129488 19441 None 0 Human Binding pKi = 7.9 7.9 - 1
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 257 1 1 2 1.9 Cc1cccc2cc(C(=O)N3CCN(C)CC3)[nH]c12 10.1016/j.ejmech.2012.06.016
66573460 75695 None 0 Human Binding pKi = 7.9 7.9 - 1
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 277 1 2 2 2.2 Cc1cc(Cl)cc2cc(C(=O)N3CCNCC3)[nH]c12 10.1016/j.ejmech.2012.06.016
CHEMBL2047451 75695 None 0 Human Binding pKi = 7.9 7.9 - 1
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 277 1 2 2 2.2 Cc1cc(Cl)cc2cc(C(=O)N3CCNCC3)[nH]c12 10.1016/j.ejmech.2012.06.016
21638785 188765 None 2 Human Binding pKi = 7.9 7.9 -4 2
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 263 1 2 2 1.9 O=C(c1cc2cc(Cl)ccc2[nH]1)N1CCNCC1 10.1016/j.ejmech.2012.06.016
CHEMBL503605 188765 None 2 Human Binding pKi = 7.9 7.9 -4 2
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL 263 1 2 2 1.9 O=C(c1cc2cc(Cl)ccc2[nH]1)N1CCNCC1 10.1016/j.ejmech.2012.06.016
44129132 201990 None 0 Human Binding pKi = 7.9 7.9 - 1
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells
ChEMBL 412 6 1 7 1.3 CN1CCN(c2nc(NCCS(=O)(=O)N(C)C)c3cc(Cl)ccc3n2)CC1 10.1021/jm901379s
CHEMBL592188 201990 None 0 Human Binding pKi = 7.9 7.9 - 1
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells
ChEMBL 412 6 1 7 1.3 CN1CCN(c2nc(NCCS(=O)(=O)N(C)C)c3cc(Cl)ccc3n2)CC1 10.1021/jm901379s
10176414 4063 None 15 Human Binding pKi = 7.9 7.9 -3 3
Displacement of [3H]histamine from human histamine H4 receptor expressed in human SK-N-MC cells by liquid scintillation countingDisplacement of [3H]histamine from human histamine H4 receptor expressed in human SK-N-MC cells by liquid scintillation counting
ChEMBL 184 4 3 3 1.0 NC(=N)SCCCc1cnc[nH]1 10.1016/j.bmc.2009.04.007
1246 4063 None 15 Human Binding pKi = 7.9 7.9 -3 3
Displacement of [3H]histamine from human histamine H4 receptor expressed in human SK-N-MC cells by liquid scintillation countingDisplacement of [3H]histamine from human histamine H4 receptor expressed in human SK-N-MC cells by liquid scintillation counting
ChEMBL 184 4 3 3 1.0 NC(=N)SCCCc1cnc[nH]1 10.1016/j.bmc.2009.04.007
CHEMBL281576 4063 None 15 Human Binding pKi = 7.9 7.9 -3 3
Displacement of [3H]histamine from human histamine H4 receptor expressed in human SK-N-MC cells by liquid scintillation countingDisplacement of [3H]histamine from human histamine H4 receptor expressed in human SK-N-MC cells by liquid scintillation counting
ChEMBL 184 4 3 3 1.0 NC(=N)SCCCc1cnc[nH]1 10.1016/j.bmc.2009.04.007
45267233 195839 None 0 Human Binding pKi = 7.9 7.9 -1 2
Displacement of [3H]histamine from human histamine H4 receptor expressed in human SK-N-MC cells by liquid scintillation countingDisplacement of [3H]histamine from human histamine H4 receptor expressed in human SK-N-MC cells by liquid scintillation counting
ChEMBL 304 7 3 4 2.8 COc1ccc(CNC(=N)SCCCc2c[nH]cn2)cc1 10.1016/j.bmc.2009.04.007
CHEMBL1202319 195839 None 0 Human Binding pKi = 7.9 7.9 -1 2
Displacement of [3H]histamine from human histamine H4 receptor expressed in human SK-N-MC cells by liquid scintillation countingDisplacement of [3H]histamine from human histamine H4 receptor expressed in human SK-N-MC cells by liquid scintillation counting
ChEMBL 304 7 3 4 2.8 COc1ccc(CNC(=N)SCCCc2c[nH]cn2)cc1 10.1016/j.bmc.2009.04.007
CHEMBL541171 195839 None 0 Human Binding pKi = 7.9 7.9 -1 2
Displacement of [3H]histamine from human histamine H4 receptor expressed in human SK-N-MC cells by liquid scintillation countingDisplacement of [3H]histamine from human histamine H4 receptor expressed in human SK-N-MC cells by liquid scintillation counting
ChEMBL 304 7 3 4 2.8 COc1ccc(CNC(=N)SCCCc2c[nH]cn2)cc1 10.1016/j.bmc.2009.04.007
1278 2150 None 56 Human Binding pKi = 7.9 7.9 -3 8
Displacement of clobenpropit-BODIPY-630/650 from recombinant human NLuc-fused H4R expressed in HEK293T cells by Nano-BRET assayDisplacement of clobenpropit-BODIPY-630/650 from recombinant human NLuc-fused H4R expressed in HEK293T cells by Nano-BRET assay
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/acs.jmedchem.0c00160
1279 2150 None 56 Human Binding pKi = 7.9 7.9 -3 8
Displacement of clobenpropit-BODIPY-630/650 from recombinant human NLuc-fused H4R expressed in HEK293T cells by Nano-BRET assayDisplacement of clobenpropit-BODIPY-630/650 from recombinant human NLuc-fused H4R expressed in HEK293T cells by Nano-BRET assay
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/acs.jmedchem.0c00160
4908365 2150 None 56 Human Binding pKi = 7.9 7.9 -3 8
Displacement of clobenpropit-BODIPY-630/650 from recombinant human NLuc-fused H4R expressed in HEK293T cells by Nano-BRET assayDisplacement of clobenpropit-BODIPY-630/650 from recombinant human NLuc-fused H4R expressed in HEK293T cells by Nano-BRET assay
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/acs.jmedchem.0c00160
CHEMBL129198 2150 None 56 Human Binding pKi = 7.9 7.9 -3 8
Displacement of clobenpropit-BODIPY-630/650 from recombinant human NLuc-fused H4R expressed in HEK293T cells by Nano-BRET assayDisplacement of clobenpropit-BODIPY-630/650 from recombinant human NLuc-fused H4R expressed in HEK293T cells by Nano-BRET assay
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/acs.jmedchem.0c00160
1249 2009 None 10 Human Binding pKi = 7.9 7.9 -3 3
Displacement of [3H]histamine from human histamine H4 receptor expressed in human SK-N-MC cell membrane incubated for 60 minsDisplacement of [3H]histamine from human histamine H4 receptor expressed in human SK-N-MC cell membrane incubated for 60 mins
ChEMBL 139 4 2 2 0.7 NCCCCc1cnc[nH]1 10.1021/acs.jmedchem.6b00120
13499360 2009 None 10 Human Binding pKi = 7.9 7.9 -3 3
Displacement of [3H]histamine from human histamine H4 receptor expressed in human SK-N-MC cell membrane incubated for 60 minsDisplacement of [3H]histamine from human histamine H4 receptor expressed in human SK-N-MC cell membrane incubated for 60 mins
ChEMBL 139 4 2 2 0.7 NCCCCc1cnc[nH]1 10.1021/acs.jmedchem.6b00120
CHEMBL90019 2009 None 10 Human Binding pKi = 7.9 7.9 -3 3
Displacement of [3H]histamine from human histamine H4 receptor expressed in human SK-N-MC cell membrane incubated for 60 minsDisplacement of [3H]histamine from human histamine H4 receptor expressed in human SK-N-MC cell membrane incubated for 60 mins
ChEMBL 139 4 2 2 0.7 NCCCCc1cnc[nH]1 10.1021/acs.jmedchem.6b00120
25128823 192826 None 0 Human Binding pKi = 7.9 7.9 -2 2
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells
ChEMBL 267 1 2 5 1.0 Nc1nc2c(c(N3CCNCC3)n1)Cc1ccccc1-2 10.1021/jm800670r
CHEMBL521995 192826 None 0 Human Binding pKi = 7.9 7.9 -2 2
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells
ChEMBL 267 1 2 5 1.0 Nc1nc2c(c(N3CCNCC3)n1)Cc1ccccc1-2 10.1021/jm800670r
127050431 140402 None 0 Human Binding pKi = 6.9 6.9 4 2
Displacement of [3H]UR-PI294 from human histamine H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 60 mins by liquid scintillation counting methodDisplacement of [3H]UR-PI294 from human histamine H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 60 mins by liquid scintillation counting method
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 140402 None 0 Human Binding pKi = 6.9 6.9 4 2
Displacement of [3H]UR-PI294 from human histamine H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 60 mins by liquid scintillation counting methodDisplacement of [3H]UR-PI294 from human histamine H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 60 mins by liquid scintillation counting method
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
11451949 68067 None 0 Human Binding pKi = 6.9 6.9 - 1
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 384 6 1 4 3.9 CN1CCN(CCCOc2ccc(-c3nc4cc(Cl)ccc4[nH]3)cc2)CC1 10.1016/j.bmcl.2011.08.014
CHEMBL1914533 68067 None 0 Human Binding pKi = 6.9 6.9 - 1
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 384 6 1 4 3.9 CN1CCN(CCCOc2ccc(-c3nc4cc(Cl)ccc4[nH]3)cc2)CC1 10.1016/j.bmcl.2011.08.014
46228126 205069 None 0 Human Binding pKi = 5.9 5.9 - 1
Displacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2Displacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2
ChEMBL 366 4 2 6 2.4 CN1CCN(c2cc(NCc3ccc(C(F)(F)F)cc3)nc(N)n2)CC1 10.1016/j.bmc.2009.08.059
CHEMBL612131 205069 None 0 Human Binding pKi = 5.9 5.9 - 1
Displacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2Displacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2
ChEMBL 366 4 2 6 2.4 CN1CCN(c2cc(NCc3ccc(C(F)(F)F)cc3)nc(N)n2)CC1 10.1016/j.bmc.2009.08.059
60150166 174828 None 0 Human Binding pKi = 5.9 5.9 -323 5
Displacement of [3H]-Nalpha-Methylhistamine from human recombinant histamine H4 receptor expressed in CHO cell membranes after 1 hrs by liquid scintillation counting analysisDisplacement of [3H]-Nalpha-Methylhistamine from human recombinant histamine H4 receptor expressed in CHO cell membranes after 1 hrs by liquid scintillation counting analysis
ChEMBL 524 17 2 6 4.7 N=C(N)N(CCCCN1CCN(CCCCCCCOc2ccccc2)CC1)Cc1ccc([N+](=O)[O-])cc1 10.1039/C8MD00527C
CHEMBL4560123 174828 None 0 Human Binding pKi = 5.9 5.9 -323 5
Displacement of [3H]-Nalpha-Methylhistamine from human recombinant histamine H4 receptor expressed in CHO cell membranes after 1 hrs by liquid scintillation counting analysisDisplacement of [3H]-Nalpha-Methylhistamine from human recombinant histamine H4 receptor expressed in CHO cell membranes after 1 hrs by liquid scintillation counting analysis
ChEMBL 524 17 2 6 4.7 N=C(N)N(CCCCN1CCN(CCCCCCCOc2ccccc2)CC1)Cc1ccc([N+](=O)[O-])cc1 10.1039/C8MD00527C
168295543 193150 None 0 Human Binding pKi = 4.9 4.9 -8 4
Displacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis
ChEMBL 380 4 4 4 3.3 Cc1nc(N)sc1-c1ccc(N/C(N)=N/C(=O)NCc2ccccc2)cc1 10.1021/acs.jmedchem.1c00692
CHEMBL5209021 193150 None 0 Human Binding pKi = 4.9 4.9 -8 4
Displacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis
ChEMBL 380 4 4 4 3.3 Cc1nc(N)sc1-c1ccc(N/C(N)=N/C(=O)NCc2ccccc2)cc1 10.1021/acs.jmedchem.1c00692
CHEMBL5222929 193150 None 0 Human Binding pKi = 4.9 4.9 -8 4
Displacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis
ChEMBL 380 4 4 4 3.3 Cc1nc(N)sc1-c1ccc(N/C(N)=N/C(=O)NCc2ccccc2)cc1 10.1021/acs.jmedchem.1c00692
164610648 184944 None 0 Human Binding pKi = 4.9 4.9 -120 4
Displacement of [3H]histamine from human histamine H4 receptor expressed in sf9 insect cell membranes co-expressing Galphai2/Gbeta1gamma2 incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]histamine from human histamine H4 receptor expressed in sf9 insect cell membranes co-expressing Galphai2/Gbeta1gamma2 incubated for 60 mins by microbeta scintillation counting method
ChEMBL 374 7 4 4 2.4 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NC[C@H](C)c1ccccc1 10.1016/j.ejmech.2021.113190
CHEMBL4852212 184944 None 0 Human Binding pKi = 4.9 4.9 -120 4
Displacement of [3H]histamine from human histamine H4 receptor expressed in sf9 insect cell membranes co-expressing Galphai2/Gbeta1gamma2 incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]histamine from human histamine H4 receptor expressed in sf9 insect cell membranes co-expressing Galphai2/Gbeta1gamma2 incubated for 60 mins by microbeta scintillation counting method
ChEMBL 374 7 4 4 2.4 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NC[C@H](C)c1ccccc1 10.1016/j.ejmech.2021.113190
10820930 5801 None 0 Human Binding pKi = 4.9 4.9 1 2
Histamine H4 receptor competition binding using [3H]Na-methylhistamineHistamine H4 receptor competition binding using [3H]Na-methylhistamine
ChEMBL 165 2 2 3 0.4 NC[C@H]1C=C[C@@H](c2c[nH]cn2)O1 10.1021/jm0300025
CHEMBL107877 5801 None 0 Human Binding pKi = 4.9 4.9 1 2
Histamine H4 receptor competition binding using [3H]Na-methylhistamineHistamine H4 receptor competition binding using [3H]Na-methylhistamine
ChEMBL 165 2 2 3 0.4 NC[C@H]1C=C[C@@H](c2c[nH]cn2)O1 10.1021/jm0300025
24826443 68143 None 0 Human Binding pKi = 6.9 6.9 - 1
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 337 1 2 6 2.4 Nc1nc(N2CCNCC2)c2oc3cccc(C(F)(F)F)c3c2n1 10.1016/j.bmcl.2011.08.014
CHEMBL1914770 68143 None 0 Human Binding pKi = 6.9 6.9 - 1
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 337 1 2 6 2.4 Nc1nc(N2CCNCC2)c2oc3cccc(C(F)(F)F)c3c2n1 10.1016/j.bmcl.2011.08.014
10800875 6282 None 0 Human Binding pKi = 6.9 6.9 -75 3
Displacement of [3H]histamine from human histamine H4 receptor expressed in SF9 cells coexpressing Galphai2, Gbeta1gamma2Displacement of [3H]histamine from human histamine H4 receptor expressed in SF9 cells coexpressing Galphai2, Gbeta1gamma2
ChEMBL 253 8 2 3 2.5 CCC(C)CCNC(=O)OCCCc1c[nH]cn1 10.1016/j.bmcl.2009.10.005
CHEMBL1081718 6282 None 0 Human Binding pKi = 6.9 6.9 -75 3
Displacement of [3H]histamine from human histamine H4 receptor expressed in SF9 cells coexpressing Galphai2, Gbeta1gamma2Displacement of [3H]histamine from human histamine H4 receptor expressed in SF9 cells coexpressing Galphai2, Gbeta1gamma2
ChEMBL 253 8 2 3 2.5 CCC(C)CCNC(=O)OCCCc1c[nH]cn1 10.1016/j.bmcl.2009.10.005
CHEMBL345828 6282 None 0 Human Binding pKi = 6.9 6.9 -75 3
Displacement of [3H]histamine from human histamine H4 receptor expressed in SF9 cells coexpressing Galphai2, Gbeta1gamma2Displacement of [3H]histamine from human histamine H4 receptor expressed in SF9 cells coexpressing Galphai2, Gbeta1gamma2
ChEMBL 253 8 2 3 2.5 CCC(C)CCNC(=O)OCCCc1c[nH]cn1 10.1016/j.bmcl.2009.10.005
24745335 295 None 13 Guinea pig Binding pKi = 6.9 6.9 -22 5
Displacement of [3H]-histamine from guinea pig H4R expressed in HEK293T cellsDisplacement of [3H]-histamine from guinea pig H4R expressed in HEK293T cells
ChEMBL 262 5 3 6 0.7 CN[C@@H]1CCN(C1)c1cc(NCC2CC2)nc(n1)N 10.1016/j.bmcl.2011.07.125
8985 295 None 13 Guinea pig Binding pKi = 6.9 6.9 -22 5
Displacement of [3H]-histamine from guinea pig H4R expressed in HEK293T cellsDisplacement of [3H]-histamine from guinea pig H4R expressed in HEK293T cells
ChEMBL 262 5 3 6 0.7 CN[C@@H]1CCN(C1)c1cc(NCC2CC2)nc(n1)N 10.1016/j.bmcl.2011.07.125
CHEMBL1915540 295 None 13 Guinea pig Binding pKi = 6.9 6.9 -22 5
Displacement of [3H]-histamine from guinea pig H4R expressed in HEK293T cellsDisplacement of [3H]-histamine from guinea pig H4R expressed in HEK293T cells
ChEMBL 262 5 3 6 0.7 CN[C@@H]1CCN(C1)c1cc(NCC2CC2)nc(n1)N 10.1016/j.bmcl.2011.07.125
DB15027 295 None 13 Guinea pig Binding pKi = 6.9 6.9 -22 5
Displacement of [3H]-histamine from guinea pig H4R expressed in HEK293T cellsDisplacement of [3H]-histamine from guinea pig H4R expressed in HEK293T cells
ChEMBL 262 5 3 6 0.7 CN[C@@H]1CCN(C1)c1cc(NCC2CC2)nc(n1)N 10.1016/j.bmcl.2011.07.125
24745335 295 None 13 Guinea pig Binding pKi = 6.9 6.9 -22 5
Displacement of [3H]histamine from guinea pig histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from guinea pig histamine H4 receptor expressed in HEK293T cells
ChEMBL 262 5 3 6 0.7 CN[C@@H]1CCN(C1)c1cc(NCC2CC2)nc(n1)N 10.1021/acs.jmedchem.5b00516
8985 295 None 13 Guinea pig Binding pKi = 6.9 6.9 -22 5
Displacement of [3H]histamine from guinea pig histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from guinea pig histamine H4 receptor expressed in HEK293T cells
ChEMBL 262 5 3 6 0.7 CN[C@@H]1CCN(C1)c1cc(NCC2CC2)nc(n1)N 10.1021/acs.jmedchem.5b00516
CHEMBL1915540 295 None 13 Guinea pig Binding pKi = 6.9 6.9 -22 5
Displacement of [3H]histamine from guinea pig histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from guinea pig histamine H4 receptor expressed in HEK293T cells
ChEMBL 262 5 3 6 0.7 CN[C@@H]1CCN(C1)c1cc(NCC2CC2)nc(n1)N 10.1021/acs.jmedchem.5b00516
DB15027 295 None 13 Guinea pig Binding pKi = 6.9 6.9 -22 5
Displacement of [3H]histamine from guinea pig histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from guinea pig histamine H4 receptor expressed in HEK293T cells
ChEMBL 262 5 3 6 0.7 CN[C@@H]1CCN(C1)c1cc(NCC2CC2)nc(n1)N 10.1021/acs.jmedchem.5b00516
1223 953 None 33 Mouse Binding pKi = 6.9 6.9 -363 11
Inhibition of UR-DEBa242 binding to mouse recombinant NLuc/GPCR-fused H4R expressed in HEK293T cells measured after 30 mins by furimazine substrate based BRET assayInhibition of UR-DEBa242 binding to mouse recombinant NLuc/GPCR-fused H4R expressed in HEK293T cells measured after 30 mins by furimazine substrate based BRET assay
ChEMBL 308 6 2 3 3.2 Clc1ccc(cc1)CN=C(SCCCc1cnc[nH]1)N 10.1021/acs.jmedchem.0c00160
2790 953 None 33 Mouse Binding pKi = 6.9 6.9 -363 11
Inhibition of UR-DEBa242 binding to mouse recombinant NLuc/GPCR-fused H4R expressed in HEK293T cells measured after 30 mins by furimazine substrate based BRET assayInhibition of UR-DEBa242 binding to mouse recombinant NLuc/GPCR-fused H4R expressed in HEK293T cells measured after 30 mins by furimazine substrate based BRET assay
ChEMBL 308 6 2 3 3.2 Clc1ccc(cc1)CN=C(SCCCc1cnc[nH]1)N 10.1021/acs.jmedchem.0c00160
CHEMBL14690 953 None 33 Mouse Binding pKi = 6.9 6.9 -363 11
Inhibition of UR-DEBa242 binding to mouse recombinant NLuc/GPCR-fused H4R expressed in HEK293T cells measured after 30 mins by furimazine substrate based BRET assayInhibition of UR-DEBa242 binding to mouse recombinant NLuc/GPCR-fused H4R expressed in HEK293T cells measured after 30 mins by furimazine substrate based BRET assay
ChEMBL 308 6 2 3 3.2 Clc1ccc(cc1)CN=C(SCCCc1cnc[nH]1)N 10.1021/acs.jmedchem.0c00160
10800875 6282 None 0 Human Binding pKi = 5.9 5.9 -75 3
Displacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Gai2 and Gb1c2 subunitDisplacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Gai2 and Gb1c2 subunit
ChEMBL 253 8 2 3 2.5 CCC(C)CCNC(=O)OCCCc1c[nH]cn1 10.1016/j.bmcl.2013.06.075
CHEMBL1081718 6282 None 0 Human Binding pKi = 5.9 5.9 -75 3
Displacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Gai2 and Gb1c2 subunitDisplacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Gai2 and Gb1c2 subunit
ChEMBL