Ligand source activities (1 row/activity)





Ligands Receptor Assay information Chemical information
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name
GPCRdb ID #Vendors Reference
ligand
Fold selectivity
(Potency)
# tested GPCRs
(Potency)
Species p-value
(-log)
Type Activity
Relation
Activity
Value
Assay Type Assay Description Source Mol
weight
Rot
Bonds
H don H acc LogP Smiles DOI
155524115 175973 0 None -1 3 Rat 10.3 pEC50 = 10.3 Functional
Agonist activity at rat H4R expressed in HEK293-SF-rH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at rat H4R expressed in HEK293-SF-rH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 286 3 2 5 2.2 CC(C)(C)CNc1nccc(N2CCc3nc[nH]c3C2)n1 10.1021/acs.jmedchem.9b01342
CHEMBL4454158 175973 0 None -1 3 Rat 10.3 pEC50 = 10.3 Functional
Agonist activity at rat H4R expressed in HEK293-SF-rH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at rat H4R expressed in HEK293-SF-rH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 286 3 2 5 2.2 CC(C)(C)CNc1nccc(N2CCc3nc[nH]c3C2)n1 10.1021/acs.jmedchem.9b01342
CHEMBL4597218 175973 0 None -1 3 Rat 10.3 pEC50 = 10.3 Functional
Agonist activity at rat H4R expressed in HEK293-SF-rH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at rat H4R expressed in HEK293-SF-rH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 286 3 2 5 2.2 CC(C)(C)CNc1nccc(N2CCc3nc[nH]c3C2)n1 10.1021/acs.jmedchem.9b01342
155524115 175973 0 None 1 3 Human 9.9 pEC50 = 9.9 Functional
Agonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 286 3 2 5 2.2 CC(C)(C)CNc1nccc(N2CCc3nc[nH]c3C2)n1 10.1021/acs.jmedchem.9b01342
CHEMBL4454158 175973 0 None 1 3 Human 9.9 pEC50 = 9.9 Functional
Agonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 286 3 2 5 2.2 CC(C)(C)CNc1nccc(N2CCc3nc[nH]c3C2)n1 10.1021/acs.jmedchem.9b01342
CHEMBL4597218 175973 0 None 1 3 Human 9.9 pEC50 = 9.9 Functional
Agonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 286 3 2 5 2.2 CC(C)(C)CNc1nccc(N2CCc3nc[nH]c3C2)n1 10.1021/acs.jmedchem.9b01342
155524115 175973 0 None -4 3 Mouse 9.6 pEC50 = 9.6 Functional
Agonist activity at mouse H4R expressed in HEK293-SF-mH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at mouse H4R expressed in HEK293-SF-mH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 286 3 2 5 2.2 CC(C)(C)CNc1nccc(N2CCc3nc[nH]c3C2)n1 10.1021/acs.jmedchem.9b01342
CHEMBL4454158 175973 0 None -4 3 Mouse 9.6 pEC50 = 9.6 Functional
Agonist activity at mouse H4R expressed in HEK293-SF-mH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at mouse H4R expressed in HEK293-SF-mH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 286 3 2 5 2.2 CC(C)(C)CNc1nccc(N2CCc3nc[nH]c3C2)n1 10.1021/acs.jmedchem.9b01342
CHEMBL4597218 175973 0 None -4 3 Mouse 9.6 pEC50 = 9.6 Functional
Agonist activity at mouse H4R expressed in HEK293-SF-mH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at mouse H4R expressed in HEK293-SF-mH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 286 3 2 5 2.2 CC(C)(C)CNc1nccc(N2CCc3nc[nH]c3C2)n1 10.1021/acs.jmedchem.9b01342
46235428 6526 0 None 263 3 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human histamine H4 receptor in SK-N-MC cells assessed as forskolin-stimulated cAMP release preincubated for 10 mins before forskolin challengeAgonist activity at human histamine H4 receptor in SK-N-MC cells assessed as forskolin-stimulated cAMP release preincubated for 10 mins before forskolin challenge
ChEMBL 407 9 3 4 4.3 Cc1cc(OCCCNCCc2c[nH]cn2)ccc1-c1nc2c(C)c(F)ccc2[nH]1 10.1016/j.bmcl.2010.04.017
CHEMBL1083162 6526 0 None 263 3 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human histamine H4 receptor in SK-N-MC cells assessed as forskolin-stimulated cAMP release preincubated for 10 mins before forskolin challengeAgonist activity at human histamine H4 receptor in SK-N-MC cells assessed as forskolin-stimulated cAMP release preincubated for 10 mins before forskolin challenge
ChEMBL 407 9 3 4 4.3 Cc1cc(OCCCNCCc2c[nH]cn2)ccc1-c1nc2c(C)c(F)ccc2[nH]1 10.1016/j.bmcl.2010.04.017
58227401 175877 0 None 2 3 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 263 4 2 5 1.7 CN[C@@H]1CCN(c2ccnc(NCC(C)(C)C)n2)C1 10.1021/acs.jmedchem.9b01342
CHEMBL4443126 175877 0 None 2 3 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 263 4 2 5 1.7 CN[C@@H]1CCN(c2ccnc(NCC(C)(C)C)n2)C1 10.1021/acs.jmedchem.9b01342
CHEMBL4596409 175877 0 None 2 3 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 263 4 2 5 1.7 CN[C@@H]1CCN(c2ccnc(NCC(C)(C)C)n2)C1 10.1021/acs.jmedchem.9b01342
58227401 175877 0 None -2 3 Rat 9.2 pEC50 = 9.2 Functional
Agonist activity at rat H4R expressed in HEK293-SF-rH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at rat H4R expressed in HEK293-SF-rH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 263 4 2 5 1.7 CN[C@@H]1CCN(c2ccnc(NCC(C)(C)C)n2)C1 10.1021/acs.jmedchem.9b01342
CHEMBL4443126 175877 0 None -2 3 Rat 9.2 pEC50 = 9.2 Functional
Agonist activity at rat H4R expressed in HEK293-SF-rH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at rat H4R expressed in HEK293-SF-rH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 263 4 2 5 1.7 CN[C@@H]1CCN(c2ccnc(NCC(C)(C)C)n2)C1 10.1021/acs.jmedchem.9b01342
CHEMBL4596409 175877 0 None -2 3 Rat 9.2 pEC50 = 9.2 Functional
Agonist activity at rat H4R expressed in HEK293-SF-rH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at rat H4R expressed in HEK293-SF-rH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 263 4 2 5 1.7 CN[C@@H]1CCN(c2ccnc(NCC(C)(C)C)n2)C1 10.1021/acs.jmedchem.9b01342
155513612 175746 0 None -18 3 Rat 9.2 pEC50 = 9.2 Functional
Agonist activity at rat H4R expressed in HEK293-SF-rH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at rat H4R expressed in HEK293-SF-rH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 277 4 1 5 2.1 CN(C)[C@@H]1CCN(c2ccnc(NCC(C)(C)C)n2)C1 10.1021/acs.jmedchem.9b01342
CHEMBL4439142 175746 0 None -18 3 Rat 9.2 pEC50 = 9.2 Functional
Agonist activity at rat H4R expressed in HEK293-SF-rH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at rat H4R expressed in HEK293-SF-rH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 277 4 1 5 2.1 CN(C)[C@@H]1CCN(c2ccnc(NCC(C)(C)C)n2)C1 10.1021/acs.jmedchem.9b01342
CHEMBL4515149 175746 0 None -18 3 Rat 9.2 pEC50 = 9.2 Functional
Agonist activity at rat H4R expressed in HEK293-SF-rH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at rat H4R expressed in HEK293-SF-rH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 277 4 1 5 2.1 CN(C)[C@@H]1CCN(c2ccnc(NCC(C)(C)C)n2)C1 10.1021/acs.jmedchem.9b01342
CHEMBL4595327 175746 0 None -18 3 Rat 9.2 pEC50 = 9.2 Functional
Agonist activity at rat H4R expressed in HEK293-SF-rH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at rat H4R expressed in HEK293-SF-rH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 277 4 1 5 2.1 CN(C)[C@@H]1CCN(c2ccnc(NCC(C)(C)C)n2)C1 10.1021/acs.jmedchem.9b01342
51354300 58581 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human histamine H4 receptor expressed in HEK293 cells assessed by forskolin induced cAMP response element activation by luciferase reporter gene assayAgonist activity at human histamine H4 receptor expressed in HEK293 cells assessed by forskolin induced cAMP response element activation by luciferase reporter gene assay
ChEMBL 273 6 1 4 2.8 c1nc(CCCn2cc(CC3CCCCC3)nn2)c[nH]1 10.1021/jm1013488
CHEMBL1688946 58581 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human histamine H4 receptor expressed in HEK293 cells assessed by forskolin induced cAMP response element activation by luciferase reporter gene assayAgonist activity at human histamine H4 receptor expressed in HEK293 cells assessed by forskolin induced cAMP response element activation by luciferase reporter gene assay
ChEMBL 273 6 1 4 2.8 c1nc(CCCn2cc(CC3CCCCC3)nn2)c[nH]1 10.1021/jm1013488
155491015 175921 3 None -10 4 Mouse 9.0 pEC50 = 9 Functional
Agonist activity at mouse H4R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by luciferase reporter gene assayAgonist activity at mouse H4R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by luciferase reporter gene assay
ChEMBL 207 4 2 5 0.2 CCCNC1CN(c2ccnc(N)n2)C1 10.1021/acs.jmedchem.9b01462
CHEMBL4441731 175921 3 None -10 4 Mouse 9.0 pEC50 = 9 Functional
Agonist activity at mouse H4R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by luciferase reporter gene assayAgonist activity at mouse H4R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by luciferase reporter gene assay
ChEMBL 207 4 2 5 0.2 CCCNC1CN(c2ccnc(N)n2)C1 10.1021/acs.jmedchem.9b01462
CHEMBL4596734 175921 3 None -10 4 Mouse 9.0 pEC50 = 9 Functional
Agonist activity at mouse H4R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by luciferase reporter gene assayAgonist activity at mouse H4R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by luciferase reporter gene assay
ChEMBL 207 4 2 5 0.2 CCCNC1CN(c2ccnc(N)n2)C1 10.1021/acs.jmedchem.9b01462
155513612 175746 0 None -14 3 Mouse 9.0 pEC50 = 9.0 Functional
Agonist activity at mouse H4R expressed in HEK293-SF-mH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at mouse H4R expressed in HEK293-SF-mH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 277 4 1 5 2.1 CN(C)[C@@H]1CCN(c2ccnc(NCC(C)(C)C)n2)C1 10.1021/acs.jmedchem.9b01342
CHEMBL4439142 175746 0 None -14 3 Mouse 9.0 pEC50 = 9.0 Functional
Agonist activity at mouse H4R expressed in HEK293-SF-mH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at mouse H4R expressed in HEK293-SF-mH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 277 4 1 5 2.1 CN(C)[C@@H]1CCN(c2ccnc(NCC(C)(C)C)n2)C1 10.1021/acs.jmedchem.9b01342
CHEMBL4515149 175746 0 None -14 3 Mouse 9.0 pEC50 = 9.0 Functional
Agonist activity at mouse H4R expressed in HEK293-SF-mH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at mouse H4R expressed in HEK293-SF-mH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 277 4 1 5 2.1 CN(C)[C@@H]1CCN(c2ccnc(NCC(C)(C)C)n2)C1 10.1021/acs.jmedchem.9b01342
CHEMBL4595327 175746 0 None -14 3 Mouse 9.0 pEC50 = 9.0 Functional
Agonist activity at mouse H4R expressed in HEK293-SF-mH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at mouse H4R expressed in HEK293-SF-mH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 277 4 1 5 2.1 CN(C)[C@@H]1CCN(c2ccnc(NCC(C)(C)C)n2)C1 10.1021/acs.jmedchem.9b01342
58227401 175877 0 None -2 3 Mouse 9.0 pEC50 = 9.0 Functional
Agonist activity at mouse H4R expressed in HEK293-SF-mH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at mouse H4R expressed in HEK293-SF-mH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 263 4 2 5 1.7 CN[C@@H]1CCN(c2ccnc(NCC(C)(C)C)n2)C1 10.1021/acs.jmedchem.9b01342
CHEMBL4443126 175877 0 None -2 3 Mouse 9.0 pEC50 = 9.0 Functional
Agonist activity at mouse H4R expressed in HEK293-SF-mH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at mouse H4R expressed in HEK293-SF-mH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 263 4 2 5 1.7 CN[C@@H]1CCN(c2ccnc(NCC(C)(C)C)n2)C1 10.1021/acs.jmedchem.9b01342
CHEMBL4596409 175877 0 None -2 3 Mouse 9.0 pEC50 = 9.0 Functional
Agonist activity at mouse H4R expressed in HEK293-SF-mH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at mouse H4R expressed in HEK293-SF-mH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 263 4 2 5 1.7 CN[C@@H]1CCN(c2ccnc(NCC(C)(C)C)n2)C1 10.1021/acs.jmedchem.9b01342
45257132 3626 3 None - 1 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 366 4 2 6 2.7 CN1CCN(CC1)c1cc(NCc2c(Cl)cccc2Cl)nc(n1)N 10.1016/j.bmc.2009.08.059
8983 3626 3 None - 1 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 366 4 2 6 2.7 CN1CCN(CC1)c1cc(NCc2c(Cl)cccc2Cl)nc(n1)N 10.1016/j.bmc.2009.08.059
CHEMBL595180 3626 3 None - 1 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 366 4 2 6 2.7 CN1CCN(CC1)c1cc(NCc2c(Cl)cccc2Cl)nc(n1)N 10.1016/j.bmc.2009.08.059
155552061 175904 0 None 2 3 Rat 8.9 pEC50 = 8.9 Functional
Agonist activity at rat H4R expressed in HEK293-SF-rH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at rat H4R expressed in HEK293-SF-rH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 277 3 1 5 2.1 CN1CCCN(c2ccnc(NCC(C)(C)C)n2)CC1 10.1021/acs.jmedchem.9b01342
CHEMBL4543119 175904 0 None 2 3 Rat 8.9 pEC50 = 8.9 Functional
Agonist activity at rat H4R expressed in HEK293-SF-rH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at rat H4R expressed in HEK293-SF-rH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 277 3 1 5 2.1 CN1CCCN(c2ccnc(NCC(C)(C)C)n2)CC1 10.1021/acs.jmedchem.9b01342
CHEMBL4596606 175904 0 None 2 3 Rat 8.9 pEC50 = 8.9 Functional
Agonist activity at rat H4R expressed in HEK293-SF-rH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at rat H4R expressed in HEK293-SF-rH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 277 3 1 5 2.1 CN1CCCN(c2ccnc(NCC(C)(C)C)n2)CC1 10.1021/acs.jmedchem.9b01342
155517880 176093 0 None 2 3 Rat 8.9 pEC50 = 8.9 Functional
Agonist activity at rat H4R expressed in HEK293-SF-rH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at rat H4R expressed in HEK293-SF-rH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 291 4 4 5 1.0 CC(C)(C)CNc1nccc(N2CC[C@@H](NC(=N)N)C2)n1 10.1021/acs.jmedchem.9b01342
CHEMBL4445423 176093 0 None 2 3 Rat 8.9 pEC50 = 8.9 Functional
Agonist activity at rat H4R expressed in HEK293-SF-rH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at rat H4R expressed in HEK293-SF-rH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 291 4 4 5 1.0 CC(C)(C)CNc1nccc(N2CC[C@@H](NC(=N)N)C2)n1 10.1021/acs.jmedchem.9b01342
CHEMBL4598198 176093 0 None 2 3 Rat 8.9 pEC50 = 8.9 Functional
Agonist activity at rat H4R expressed in HEK293-SF-rH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at rat H4R expressed in HEK293-SF-rH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 291 4 4 5 1.0 CC(C)(C)CNc1nccc(N2CC[C@@H](NC(=N)N)C2)n1 10.1021/acs.jmedchem.9b01342
45257132 3626 3 None - 1 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of GTPase by [gamma-32P]GTP spontaneous degradation assayAgonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of GTPase by [gamma-32P]GTP spontaneous degradation assay
ChEMBL 366 4 2 6 2.7 CN1CCN(CC1)c1cc(NCc2c(Cl)cccc2Cl)nc(n1)N 10.1016/j.bmc.2009.08.059
8983 3626 3 None - 1 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of GTPase by [gamma-32P]GTP spontaneous degradation assayAgonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of GTPase by [gamma-32P]GTP spontaneous degradation assay
ChEMBL 366 4 2 6 2.7 CN1CCN(CC1)c1cc(NCc2c(Cl)cccc2Cl)nc(n1)N 10.1016/j.bmc.2009.08.059
CHEMBL595180 3626 3 None - 1 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of GTPase by [gamma-32P]GTP spontaneous degradation assayAgonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of GTPase by [gamma-32P]GTP spontaneous degradation assay
ChEMBL 366 4 2 6 2.7 CN1CCN(CC1)c1cc(NCc2c(Cl)cccc2Cl)nc(n1)N 10.1016/j.bmc.2009.08.059
58227373 175934 0 None -1 3 Rat 8.8 pEC50 = 8.8 Functional
Agonist activity at rat H4R expressed in HEK293-SF-rH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at rat H4R expressed in HEK293-SF-rH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 249 3 2 5 1.5 CC(C)(C)CNc1nccc(N2CC[C@@H](N)C2)n1 10.1021/acs.jmedchem.9b01342
CHEMBL4455324 175934 0 None -1 3 Rat 8.8 pEC50 = 8.8 Functional
Agonist activity at rat H4R expressed in HEK293-SF-rH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at rat H4R expressed in HEK293-SF-rH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 249 3 2 5 1.5 CC(C)(C)CNc1nccc(N2CC[C@@H](N)C2)n1 10.1021/acs.jmedchem.9b01342
CHEMBL4596881 175934 0 None -1 3 Rat 8.8 pEC50 = 8.8 Functional
Agonist activity at rat H4R expressed in HEK293-SF-rH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at rat H4R expressed in HEK293-SF-rH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 249 3 2 5 1.5 CC(C)(C)CNc1nccc(N2CC[C@@H](N)C2)n1 10.1021/acs.jmedchem.9b01342
155513612 175746 0 None 14 3 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 277 4 1 5 2.1 CN(C)[C@@H]1CCN(c2ccnc(NCC(C)(C)C)n2)C1 10.1021/acs.jmedchem.9b01342
CHEMBL4439142 175746 0 None 14 3 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 277 4 1 5 2.1 CN(C)[C@@H]1CCN(c2ccnc(NCC(C)(C)C)n2)C1 10.1021/acs.jmedchem.9b01342
CHEMBL4515149 175746 0 None 14 3 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 277 4 1 5 2.1 CN(C)[C@@H]1CCN(c2ccnc(NCC(C)(C)C)n2)C1 10.1021/acs.jmedchem.9b01342
CHEMBL4595327 175746 0 None 14 3 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 277 4 1 5 2.1 CN(C)[C@@H]1CCN(c2ccnc(NCC(C)(C)C)n2)C1 10.1021/acs.jmedchem.9b01342
136030655 56188 0 None 1 3 Mouse 8.0 pEC50 = 8 Functional
Agonist activity at mouse histamine H4 receptor by luciferase reporter gene assayAgonist activity at mouse histamine H4 receptor by luciferase reporter gene assay
ChEMBL 292 1 2 3 2.2 CN1CCN(/C(=N\O)c2cc3cc(Cl)ccc3[nH]2)CC1 10.1016/j.bmcl.2010.10.041
CHEMBL1632413 56188 0 None 1 3 Mouse 8.0 pEC50 = 8 Functional
Agonist activity at mouse histamine H4 receptor by luciferase reporter gene assayAgonist activity at mouse histamine H4 receptor by luciferase reporter gene assay
ChEMBL 292 1 2 3 2.2 CN1CCN(/C(=N\O)c2cc3cc(Cl)ccc3[nH]2)CC1 10.1016/j.bmcl.2010.10.041
136030655 56188 0 None -1 3 Rat 8.0 pEC50 = 8 Functional
Agonist activity at rat histamine H4 receptor by luciferase reporter gene assayAgonist activity at rat histamine H4 receptor by luciferase reporter gene assay
ChEMBL 292 1 2 3 2.2 CN1CCN(/C(=N\O)c2cc3cc(Cl)ccc3[nH]2)CC1 10.1016/j.bmcl.2010.10.041
CHEMBL1632413 56188 0 None -1 3 Rat 8.0 pEC50 = 8 Functional
Agonist activity at rat histamine H4 receptor by luciferase reporter gene assayAgonist activity at rat histamine H4 receptor by luciferase reporter gene assay
ChEMBL 292 1 2 3 2.2 CN1CCN(/C(=N\O)c2cc3cc(Cl)ccc3[nH]2)CC1 10.1016/j.bmcl.2010.10.041
25068753 187854 15 None -1 2 Rat 8.0 pEC50 = 8 Functional
Antagonist activity at rat histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assayAntagonist activity at rat histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assay
ChEMBL 295 1 2 5 1.8 Nc1nc2c(c(N3CC[C@@H](N)C3)n1)CCCc1ccccc1-2 10.1021/jm800670r
CHEMBL502347 187854 15 None -1 2 Rat 8.0 pEC50 = 8 Functional
Antagonist activity at rat histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assayAntagonist activity at rat histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assay
ChEMBL 295 1 2 5 1.8 Nc1nc2c(c(N3CC[C@@H](N)C3)n1)CCCc1ccccc1-2 10.1021/jm800670r
10105117 103718 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 226 6 3 2 1.6 CC/N=C(\S)NCCCCc1c[nH]cn1 10.1016/j.bmcl.2010.10.041
CHEMBL309819 103718 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 226 6 3 2 1.6 CC/N=C(\S)NCCCCc1c[nH]cn1 10.1016/j.bmcl.2010.10.041
127051301 139670 0 None 4 3 Human 7.0 pEC50 = 7 Functional
Agonist activity at human histamine H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assayAgonist activity at human histamine H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 246 3 3 3 0.9 CN/C(=N\C#N)NC[C@H]1CC[C@H](c2c[nH]cn2)C1 10.1021/acs.jmedchem.6b00120
CHEMBL3804906 139670 0 None 4 3 Human 7.0 pEC50 = 7 Functional
Agonist activity at human histamine H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assayAgonist activity at human histamine H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 246 3 3 3 0.9 CN/C(=N\C#N)NC[C@H]1CC[C@H](c2c[nH]cn2)C1 10.1021/acs.jmedchem.6b00120
136141537 56187 1 None 1 3 Human 7.0 pEC50 = 7 Functional
Agonist activity at human recombinant histamine H4 receptor expressed in human SK-N-MC cells co-expressing SRE-Luc by luciferase reporter gene assayAgonist activity at human recombinant histamine H4 receptor expressed in human SK-N-MC cells co-expressing SRE-Luc by luciferase reporter gene assay
ChEMBL 271 2 2 3 3.0 Cc1ccc2[nH]c(/C(=N\O)C3CCN(C)CC3)cc2c1 10.1016/j.bmcl.2010.10.041
CHEMBL1632412 56187 1 None 1 3 Human 7.0 pEC50 = 7 Functional
Agonist activity at human recombinant histamine H4 receptor expressed in human SK-N-MC cells co-expressing SRE-Luc by luciferase reporter gene assayAgonist activity at human recombinant histamine H4 receptor expressed in human SK-N-MC cells co-expressing SRE-Luc by luciferase reporter gene assay
ChEMBL 271 2 2 3 3.0 Cc1ccc2[nH]c(/C(=N\O)C3CCN(C)CC3)cc2c1 10.1016/j.bmcl.2010.10.041
4024 1984 14 None -3388 2 Human 6.0 pEC50 = 6 Functional
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 159 2 1 2 1.4 n1ccc(cc1)Cc1c[nH]cn1 10.1016/j.bmcl.2010.10.041
9989505 1984 14 None -3388 2 Human 6.0 pEC50 = 6 Functional
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 159 2 1 2 1.4 n1ccc(cc1)Cc1c[nH]cn1 10.1016/j.bmcl.2010.10.041
CHEMBL82298 1984 14 None -3388 2 Human 6.0 pEC50 = 6 Functional
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 159 2 1 2 1.4 n1ccc(cc1)Cc1c[nH]cn1 10.1016/j.bmcl.2010.10.041
58227259 116640 0 None - 1 Human 6.0 pEC50 = 6 Functional
Agonist activity at human recombinant histamine H4 receptor expressed in SK-N-MC cells assessed as effect on forskolin-stimulated cAMP-mediated reporter gene activityAgonist activity at human recombinant histamine H4 receptor expressed in SK-N-MC cells assessed as effect on forskolin-stimulated cAMP-mediated reporter gene activity
ChEMBL 287 4 2 5 1.9 CN[C@@H]1CCN(c2cnnc(NC3CC4CCC3C4)c2)C1 10.1016/j.bmcl.2014.12.027
CHEMBL3393556 116640 0 None - 1 Human 6.0 pEC50 = 6 Functional
Agonist activity at human recombinant histamine H4 receptor expressed in SK-N-MC cells assessed as effect on forskolin-stimulated cAMP-mediated reporter gene activityAgonist activity at human recombinant histamine H4 receptor expressed in SK-N-MC cells assessed as effect on forskolin-stimulated cAMP-mediated reporter gene activity
ChEMBL 287 4 2 5 1.9 CN[C@@H]1CCN(c2cnnc(NC3CC4CCC3C4)c2)C1 10.1016/j.bmcl.2014.12.027
1194 46 3 None -50 2 Human 5.0 pEC50 = 5 Functional
Agonist activity at human recombinant histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2 by steady-state GTPase activity assayAgonist activity at human recombinant histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2 by steady-state GTPase activity assay
ChEMBL 265 3 2 2 2.3 NCCc1cnc([nH]1)c1cccc(c1)Br 10.1016/j.bmcl.2010.10.041
23786499 46 3 None -50 2 Human 5.0 pEC50 = 5 Functional
Agonist activity at human recombinant histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2 by steady-state GTPase activity assayAgonist activity at human recombinant histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2 by steady-state GTPase activity assay
ChEMBL 265 3 2 2 2.3 NCCc1cnc([nH]1)c1cccc(c1)Br 10.1016/j.bmcl.2010.10.041
CHEMBL26116 46 3 None -50 2 Human 5.0 pEC50 = 5 Functional
Agonist activity at human recombinant histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2 by steady-state GTPase activity assayAgonist activity at human recombinant histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2 by steady-state GTPase activity assay
ChEMBL 265 3 2 2 2.3 NCCc1cnc([nH]1)c1cccc(c1)Br 10.1016/j.bmcl.2010.10.041
24797598 61233 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells assessed as effect on forskolin-induced cAMP accumulation after 6 hrsAgonist activity at human histamine H4 receptor expressed in human SK-N-MC cells assessed as effect on forskolin-induced cAMP accumulation after 6 hrs
ChEMBL 276 3 2 6 1.2 CN1CCN(c2cc(NC3CCCC3)nc(N)n2)CC1 10.1016/j.bmcl.2011.03.017
CHEMBL1771001 61233 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells assessed as effect on forskolin-induced cAMP accumulation after 6 hrsAgonist activity at human histamine H4 receptor expressed in human SK-N-MC cells assessed as effect on forskolin-induced cAMP accumulation after 6 hrs
ChEMBL 276 3 2 6 1.2 CN1CCN(c2cc(NC3CCCC3)nc(N)n2)CC1 10.1016/j.bmcl.2011.03.017
11846299 138690 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Activity at human histamine H4 receptor transfected in SK-N-MC cells by cAMP assayActivity at human histamine H4 receptor transfected in SK-N-MC cells by cAMP assay
ChEMBL 361 0 0 4 4.4 CN1CCN(C2=Nc3cc(Cl)ccc3Oc3cc(Cl)ccc32)CC1 10.1021/jm051008s
CHEMBL378788 138690 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Activity at human histamine H4 receptor transfected in SK-N-MC cells by cAMP assayActivity at human histamine H4 receptor transfected in SK-N-MC cells by cAMP assay
ChEMBL 361 0 0 4 4.4 CN1CCN(C2=Nc3cc(Cl)ccc3Oc3cc(Cl)ccc32)CC1 10.1021/jm051008s
46228114 198492 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 314 4 3 7 1.1 CN1CCN(c2cc(NCc3ccc(O)cc3)nc(N)n2)CC1 10.1016/j.bmc.2009.08.059
CHEMBL596551 198492 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 314 4 3 7 1.1 CN1CCN(c2cc(NCc3ccc(O)cc3)nc(N)n2)CC1 10.1016/j.bmc.2009.08.059
25130576 187043 1 None 2 2 Mouse 7.0 pEC50 = 7.0 Functional
Agonist activity at mouse histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at mouse histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 280 2 2 6 1.0 N#Cc1ccc(-c2cc(N3CCNCC3)nc(N)n2)cc1 10.1021/jm8005959
CHEMBL494890 187043 1 None 2 2 Mouse 7.0 pEC50 = 7.0 Functional
Agonist activity at mouse histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at mouse histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 280 2 2 6 1.0 N#Cc1ccc(-c2cc(N3CCNCC3)nc(N)n2)cc1 10.1021/jm8005959
25130232 186980 0 None - 1 Rat 7.0 pEC50 = 7.0 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 273 2 1 7 0.2 CN1CCN(c2cc(-c3cn(C)cn3)nc(N)n2)CC1 10.1021/jm8005959
CHEMBL494576 186980 0 None - 1 Rat 7.0 pEC50 = 7.0 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 273 2 1 7 0.2 CN1CCN(c2cc(-c3cn(C)cn3)nc(N)n2)CC1 10.1021/jm8005959
25131229 187012 0 None - 1 Rat 7.0 pEC50 = 7.0 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 299 3 1 6 1.5 COc1cccc(-c2cc(N3CCN(C)CC3)nc(N)n2)c1 10.1021/jm8005959
CHEMBL494724 187012 0 None - 1 Rat 7.0 pEC50 = 7.0 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 299 3 1 6 1.5 COc1cccc(-c2cc(N3CCN(C)CC3)nc(N)n2)c1 10.1021/jm8005959
25130576 187043 1 None 2 2 Mouse 7.0 pEC50 = 7.0 Functional
Antagonist activity at mouse histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assayAntagonist activity at mouse histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assay
ChEMBL 280 2 2 6 1.0 N#Cc1ccc(-c2cc(N3CCNCC3)nc(N)n2)cc1 10.1021/jm800670r
CHEMBL494890 187043 1 None 2 2 Mouse 7.0 pEC50 = 7.0 Functional
Antagonist activity at mouse histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assayAntagonist activity at mouse histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assay
ChEMBL 280 2 2 6 1.0 N#Cc1ccc(-c2cc(N3CCNCC3)nc(N)n2)cc1 10.1021/jm800670r
11846635 78270 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Activity at human histamine H4 receptor transfected in SK-N-MC cells by cAMP assayActivity at human histamine H4 receptor transfected in SK-N-MC cells by cAMP assay
ChEMBL 307 0 0 4 3.4 Cc1ccc2c(c1)Oc1ccccc1C(N1CCN(C)CC1)=N2 10.1021/jm051008s
CHEMBL211242 78270 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Activity at human histamine H4 receptor transfected in SK-N-MC cells by cAMP assayActivity at human histamine H4 receptor transfected in SK-N-MC cells by cAMP assay
ChEMBL 307 0 0 4 3.4 Cc1ccc2c(c1)Oc1ccccc1C(N1CCN(C)CC1)=N2 10.1021/jm051008s
46228132 200459 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Antagonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as inhibition of 100 nM dopamine-induced stimulation of [35S]GTPgammaS bindingAntagonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as inhibition of 100 nM dopamine-induced stimulation of [35S]GTPgammaS binding
ChEMBL 312 4 2 6 1.7 Cc1ccc(CNc2cc(N3CCN(C)CC3)nc(N)n2)cc1 10.1016/j.bmc.2009.08.059
CHEMBL609161 200459 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Antagonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as inhibition of 100 nM dopamine-induced stimulation of [35S]GTPgammaS bindingAntagonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as inhibition of 100 nM dopamine-induced stimulation of [35S]GTPgammaS binding
ChEMBL 312 4 2 6 1.7 Cc1ccc(CNc2cc(N3CCN(C)CC3)nc(N)n2)cc1 10.1016/j.bmc.2009.08.059
25129178 187046 1 None - 1 Rat 5.0 pEC50 = 5.0 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 223 2 1 6 -0.2 COc1cc(N2CCN(C)CC2)nc(N)n1 10.1021/jm8005959
CHEMBL494910 187046 1 None - 1 Rat 5.0 pEC50 = 5.0 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 223 2 1 6 -0.2 COc1cc(N2CCN(C)CC2)nc(N)n1 10.1021/jm8005959
1267 3744 43 None -17 5 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19 protein by steady-state GTPase assayAgonist activity at human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19 protein by steady-state GTPase assay
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1021/jm900526h
3035905 3744 43 None -17 5 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19 protein by steady-state GTPase assayAgonist activity at human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19 protein by steady-state GTPase assay
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1021/jm900526h
CHEMBL260374 3744 43 None -17 5 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19 protein by steady-state GTPase assayAgonist activity at human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19 protein by steady-state GTPase assay
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1021/jm900526h
44480708 5698 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19 protein by steady-state GTPase assayAgonist activity at human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19 protein by steady-state GTPase assay
ChEMBL 310 8 3 3 2.0 N#C/N=C(/NCCCCc1c[nH]cn1)NCCc1ccccc1 10.1021/jm900526h
CHEMBL1078632 5698 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19 protein by steady-state GTPase assayAgonist activity at human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19 protein by steady-state GTPase assay
ChEMBL 310 8 3 3 2.0 N#C/N=C(/NCCCCc1c[nH]cn1)NCCc1ccccc1 10.1021/jm900526h
53233804 61197 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells assessed as effect on forskolin-induced cAMP accumulation after 6 hrsAgonist activity at human histamine H4 receptor expressed in human SK-N-MC cells assessed as effect on forskolin-induced cAMP accumulation after 6 hrs
ChEMBL 275 3 2 5 1.8 CN1CCN(c2cc(N)nc(NC3CCCC3)c2)CC1 10.1016/j.bmcl.2011.03.017
CHEMBL1770966 61197 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells assessed as effect on forskolin-induced cAMP accumulation after 6 hrsAgonist activity at human histamine H4 receptor expressed in human SK-N-MC cells assessed as effect on forskolin-induced cAMP accumulation after 6 hrs
ChEMBL 275 3 2 5 1.8 CN1CCN(c2cc(N)nc(NC3CCCC3)c2)CC1 10.1016/j.bmcl.2011.03.017
1204 1901 114 None -1 10 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human histamine H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assayAgonist activity at human histamine H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.6b00120
1247 1901 114 None -1 10 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human histamine H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assayAgonist activity at human histamine H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.6b00120
1375 1901 114 None -1 10 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human histamine H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assayAgonist activity at human histamine H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.6b00120
774 1901 114 None -1 10 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human histamine H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assayAgonist activity at human histamine H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.6b00120
CHEMBL90 1901 114 None -1 10 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human histamine H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assayAgonist activity at human histamine H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.6b00120
DB05381 1901 114 None -1 10 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human histamine H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assayAgonist activity at human histamine H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.6b00120
127052293 139708 1 None 10 2 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human histamine H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assayAgonist activity at human histamine H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 368 7 3 4 3.1 N#C/N=C(/NCCSc1ccccc1)NC[C@H]1CC[C@H](c2c[nH]cn2)C1 10.1021/acs.jmedchem.6b00120
CHEMBL3805361 139708 1 None 10 2 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human histamine H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assayAgonist activity at human histamine H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 368 7 3 4 3.1 N#C/N=C(/NCCSc1ccccc1)NC[C@H]1CC[C@H](c2c[nH]cn2)C1 10.1021/acs.jmedchem.6b00120
1204 1901 114 None -1 10 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of GTPase by [gamma-32P]GTP spontaneous degradation assayAgonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of GTPase by [gamma-32P]GTP spontaneous degradation assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmc.2009.08.059
1247 1901 114 None -1 10 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of GTPase by [gamma-32P]GTP spontaneous degradation assayAgonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of GTPase by [gamma-32P]GTP spontaneous degradation assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmc.2009.08.059
1375 1901 114 None -1 10 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of GTPase by [gamma-32P]GTP spontaneous degradation assayAgonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of GTPase by [gamma-32P]GTP spontaneous degradation assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmc.2009.08.059
774 1901 114 None -1 10 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of GTPase by [gamma-32P]GTP spontaneous degradation assayAgonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of GTPase by [gamma-32P]GTP spontaneous degradation assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmc.2009.08.059
CHEMBL90 1901 114 None -1 10 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of GTPase by [gamma-32P]GTP spontaneous degradation assayAgonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of GTPase by [gamma-32P]GTP spontaneous degradation assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmc.2009.08.059
DB05381 1901 114 None -1 10 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of GTPase by [gamma-32P]GTP spontaneous degradation assayAgonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of GTPase by [gamma-32P]GTP spontaneous degradation assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmc.2009.08.059
45257131 198226 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of GTPase by [gamma-32P]GTP spontaneous degradation assayAgonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of GTPase by [gamma-32P]GTP spontaneous degradation assay
ChEMBL 312 4 2 6 1.7 Cc1ccccc1CNc1cc(N2CCN(C)CC2)nc(N)n1 10.1016/j.bmc.2009.08.059
CHEMBL594731 198226 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of GTPase by [gamma-32P]GTP spontaneous degradation assayAgonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of GTPase by [gamma-32P]GTP spontaneous degradation assay
ChEMBL 312 4 2 6 1.7 Cc1ccccc1CNc1cc(N2CCN(C)CC2)nc(N)n1 10.1016/j.bmc.2009.08.059
56593499 139712 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human histamine H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assayAgonist activity at human histamine H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 368 6 3 4 3.2 N#C/N=C(/NCCSc1ccccc1)N[C@H]1CC[C@@H](c2c[nH]cn2)CC1 10.1021/acs.jmedchem.6b00120
CHEMBL3805392 139712 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human histamine H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assayAgonist activity at human histamine H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 368 6 3 4 3.2 N#C/N=C(/NCCSc1ccccc1)N[C@H]1CC[C@@H](c2c[nH]cn2)CC1 10.1021/acs.jmedchem.6b00120
127050776 139717 0 None 3 3 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human histamine H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assayAgonist activity at human histamine H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 246 3 3 3 0.9 CN/C(=N\C#N)NC[C@@H]1CC[C@@H](c2c[nH]cn2)C1 10.1021/acs.jmedchem.6b00120
CHEMBL3805437 139717 0 None 3 3 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human histamine H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assayAgonist activity at human histamine H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 246 3 3 3 0.9 CN/C(=N\C#N)NC[C@@H]1CC[C@@H](c2c[nH]cn2)C1 10.1021/acs.jmedchem.6b00120
127050431 139785 0 None 3 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human histamine H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assayAgonist activity at human histamine H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 246 3 3 3 0.9 CN/C(=N\C#N)NC[C@@H]1CC[C@H](c2c[nH]cn2)C1 10.1021/acs.jmedchem.6b00120
CHEMBL3806206 139785 0 None 3 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human histamine H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assayAgonist activity at human histamine H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 246 3 3 3 0.9 CN/C(=N\C#N)NC[C@@H]1CC[C@H](c2c[nH]cn2)C1 10.1021/acs.jmedchem.6b00120
58227165 116620 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human recombinant histamine H4 receptor expressed in SK-N-MC cells assessed as effect on forskolin-stimulated cAMP-mediated reporter gene activityAgonist activity at human recombinant histamine H4 receptor expressed in SK-N-MC cells assessed as effect on forskolin-stimulated cAMP-mediated reporter gene activity
ChEMBL 235 3 1 5 1.0 CC(C)Nc1nccc(N2CCN(C)CC2)n1 10.1016/j.bmcl.2014.12.027
CHEMBL3393536 116620 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human recombinant histamine H4 receptor expressed in SK-N-MC cells assessed as effect on forskolin-stimulated cAMP-mediated reporter gene activityAgonist activity at human recombinant histamine H4 receptor expressed in SK-N-MC cells assessed as effect on forskolin-stimulated cAMP-mediated reporter gene activity
ChEMBL 235 3 1 5 1.0 CC(C)Nc1nccc(N2CCN(C)CC2)n1 10.1016/j.bmcl.2014.12.027
25130578 186750 0 None - 1 Rat 6.0 pEC50 = 6.0 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 251 4 1 5 1.4 CN(C)CCN(C)c1cc(C(C)(C)C)nc(N)n1 10.1021/jm8005959
CHEMBL493099 186750 0 None - 1 Rat 6.0 pEC50 = 6.0 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 251 4 1 5 1.4 CN(C)CCN(C)c1cc(C(C)(C)C)nc(N)n1 10.1021/jm8005959
25129525 187000 0 None - 1 Rat 6.9 pEC50 = 6.9 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 299 3 1 6 1.5 COc1ccc(-c2cc(N3CCN(C)CC3)nc(N)n2)cc1 10.1021/jm8005959
CHEMBL494648 187000 0 None - 1 Rat 6.9 pEC50 = 6.9 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 299 3 1 6 1.5 COc1ccc(-c2cc(N3CCN(C)CC3)nc(N)n2)cc1 10.1021/jm8005959
25128833 187818 30 None -2 2 Rat 6.9 pEC50 = 6.9 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 193 1 1 5 -0.2 CN1CCN(c2ccnc(N)n2)CC1 10.1021/jm8005959
CHEMBL501882 187818 30 None -2 2 Rat 6.9 pEC50 = 6.9 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 193 1 1 5 -0.2 CN1CCN(c2ccnc(N)n2)CC1 10.1021/jm8005959
25128831 172044 0 None 1 2 Human 4.9 pEC50 = 4.9 Functional
Agonist activity at human histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at human histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 277 2 0 5 1.6 CN1CCN(c2cc(C(C)(C)C)nc(N(C)C)n2)CC1 10.1021/jm8005959
CHEMBL449157 172044 0 None 1 2 Human 4.9 pEC50 = 4.9 Functional
Agonist activity at human histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at human histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 277 2 0 5 1.6 CN1CCN(c2cc(C(C)(C)C)nc(N(C)C)n2)CC1 10.1021/jm8005959
11043445 56185 1 None -1 2 Human 4.9 pEC50 = 4.9 Functional
Inhibition of the forskolin-stimulated cAMP production in SK-N-MC cells expressing human Histamine H4 receptorInhibition of the forskolin-stimulated cAMP production in SK-N-MC cells expressing human Histamine H4 receptor
ChEMBL 258 5 1 3 2.8 c1ccc(COC[C@H]2CC[C@@H](c3c[nH]cn3)O2)cc1 10.1021/jm0300025
CHEMBL1632410 56185 1 None -1 2 Human 4.9 pEC50 = 4.9 Functional
Inhibition of the forskolin-stimulated cAMP production in SK-N-MC cells expressing human Histamine H4 receptorInhibition of the forskolin-stimulated cAMP production in SK-N-MC cells expressing human Histamine H4 receptor
ChEMBL 258 5 1 3 2.8 c1ccc(COC[C@H]2CC[C@@H](c3c[nH]cn3)O2)cc1 10.1021/jm0300025
16061839 187834 0 None - 1 Rat 6.9 pEC50 = 6.9 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 284 3 2 6 1.6 CN1CCN(c2cc(Nc3ccccc3)nc(N)n2)CC1 10.1021/jm8005959
CHEMBL502104 187834 0 None - 1 Rat 6.9 pEC50 = 6.9 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 284 3 2 6 1.6 CN1CCN(c2cc(Nc3ccccc3)nc(N)n2)CC1 10.1021/jm8005959
127050431 139785 0 None 3 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human histamine H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assayAgonist activity at human histamine H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 246 3 3 3 0.9 CN/C(=N\C#N)NC[C@@H]1CC[C@H](c2c[nH]cn2)C1 10.1021/acs.jmedchem.6b00120
CHEMBL3806206 139785 0 None 3 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human histamine H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assayAgonist activity at human histamine H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 246 3 3 3 0.9 CN/C(=N\C#N)NC[C@@H]1CC[C@H](c2c[nH]cn2)C1 10.1021/acs.jmedchem.6b00120
54585780 61229 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells assessed as effect on forskolin-induced cAMP accumulation after 6 hrsAgonist activity at human histamine H4 receptor expressed in human SK-N-MC cells assessed as effect on forskolin-induced cAMP accumulation after 6 hrs
ChEMBL 250 3 2 6 0.6 CC(C)Nc1cc(N2CCN(C)CC2)nc(N)n1 10.1016/j.bmcl.2011.03.017
CHEMBL1770998 61229 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells assessed as effect on forskolin-induced cAMP accumulation after 6 hrsAgonist activity at human histamine H4 receptor expressed in human SK-N-MC cells assessed as effect on forskolin-induced cAMP accumulation after 6 hrs
ChEMBL 250 3 2 6 0.6 CC(C)Nc1cc(N2CCN(C)CC2)nc(N)n1 10.1016/j.bmcl.2011.03.017
1204 1901 114 None -1 10 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19 protein by steady-state GTPase assayAgonist activity at human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19 protein by steady-state GTPase assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm900526h
1247 1901 114 None -1 10 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19 protein by steady-state GTPase assayAgonist activity at human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19 protein by steady-state GTPase assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm900526h
1375 1901 114 None -1 10 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19 protein by steady-state GTPase assayAgonist activity at human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19 protein by steady-state GTPase assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm900526h
774 1901 114 None -1 10 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19 protein by steady-state GTPase assayAgonist activity at human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19 protein by steady-state GTPase assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm900526h
CHEMBL90 1901 114 None -1 10 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19 protein by steady-state GTPase assayAgonist activity at human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19 protein by steady-state GTPase assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm900526h
DB05381 1901 114 None -1 10 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19 protein by steady-state GTPase assayAgonist activity at human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19 protein by steady-state GTPase assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm900526h
25130914 186671 0 None 15 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at histamine H4 receptor (unknown origin) expressed in HEK293T cells harboring CRE-luciferase after 6 hrs by luciferase reporter gene assayAgonist activity at histamine H4 receptor (unknown origin) expressed in HEK293T cells harboring CRE-luciferase after 6 hrs by luciferase reporter gene assay
ChEMBL 298 4 2 6 1.4 CN1CCN(c2cc(NCc3ccccc3)nc(N)n2)CC1 10.1021/acs.jmedchem.8b00435
CHEMBL492677 186671 0 None 15 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at histamine H4 receptor (unknown origin) expressed in HEK293T cells harboring CRE-luciferase after 6 hrs by luciferase reporter gene assayAgonist activity at histamine H4 receptor (unknown origin) expressed in HEK293T cells harboring CRE-luciferase after 6 hrs by luciferase reporter gene assay
ChEMBL 298 4 2 6 1.4 CN1CCN(c2cc(NCc3ccccc3)nc(N)n2)CC1 10.1021/acs.jmedchem.8b00435
11957573 1979 29 None -54 5 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human histamine H4 receptorAgonist activity at human histamine H4 receptor
ChEMBL 170 3 3 3 0.6 NC(=N)SCCc1cnc[nH]1 10.1021/jm100064d
1250 1979 29 None -54 5 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human histamine H4 receptorAgonist activity at human histamine H4 receptor
ChEMBL 170 3 3 3 0.6 NC(=N)SCCc1cnc[nH]1 10.1021/jm100064d
3692 1979 29 None -54 5 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human histamine H4 receptorAgonist activity at human histamine H4 receptor
ChEMBL 170 3 3 3 0.6 NC(=N)SCCc1cnc[nH]1 10.1021/jm100064d
CHEMBL19439 1979 29 None -54 5 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human histamine H4 receptorAgonist activity at human histamine H4 receptor
ChEMBL 170 3 3 3 0.6 NC(=N)SCCc1cnc[nH]1 10.1021/jm100064d
11957573 1979 29 None -54 5 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 170 3 3 3 0.6 NC(=N)SCCc1cnc[nH]1 10.1016/j.bmcl.2010.10.041
1250 1979 29 None -54 5 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 170 3 3 3 0.6 NC(=N)SCCc1cnc[nH]1 10.1016/j.bmcl.2010.10.041
3692 1979 29 None -54 5 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 170 3 3 3 0.6 NC(=N)SCCc1cnc[nH]1 10.1016/j.bmcl.2010.10.041
CHEMBL19439 1979 29 None -54 5 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 170 3 3 3 0.6 NC(=N)SCCc1cnc[nH]1 10.1016/j.bmcl.2010.10.041
1253 2027 7 None -251 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 342 6 1 2 3.2 Ic1ccc(cc1)COCCCc1cnc[nH]1 10.1016/j.bmcl.2010.10.041
132937 2027 7 None -251 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 342 6 1 2 3.2 Ic1ccc(cc1)COCCCc1cnc[nH]1 10.1016/j.bmcl.2010.10.041
CHEMBL19010 2027 7 None -251 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 342 6 1 2 3.2 Ic1ccc(cc1)COCCCc1cnc[nH]1 10.1016/j.bmcl.2010.10.041
10176414 4000 13 None -25 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 184 4 3 3 1.0 NC(=N)SCCCc1cnc[nH]1 10.1016/j.bmcl.2010.10.041
1246 4000 13 None -25 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 184 4 3 3 1.0 NC(=N)SCCCc1cnc[nH]1 10.1016/j.bmcl.2010.10.041
CHEMBL281576 4000 13 None -25 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 184 4 3 3 1.0 NC(=N)SCCCc1cnc[nH]1 10.1016/j.bmcl.2010.10.041
1204 1901 114 None -1 10 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human recombinant histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2 by steady-state GTPase activity assayAgonist activity at human recombinant histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2 by steady-state GTPase activity assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmcl.2010.10.041
1247 1901 114 None -1 10 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human recombinant histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2 by steady-state GTPase activity assayAgonist activity at human recombinant histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2 by steady-state GTPase activity assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmcl.2010.10.041
1375 1901 114 None -1 10 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human recombinant histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2 by steady-state GTPase activity assayAgonist activity at human recombinant histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2 by steady-state GTPase activity assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmcl.2010.10.041
774 1901 114 None -1 10 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human recombinant histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2 by steady-state GTPase activity assayAgonist activity at human recombinant histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2 by steady-state GTPase activity assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmcl.2010.10.041
CHEMBL90 1901 114 None -1 10 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human recombinant histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2 by steady-state GTPase activity assayAgonist activity at human recombinant histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2 by steady-state GTPase activity assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmcl.2010.10.041
DB05381 1901 114 None -1 10 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human recombinant histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2 by steady-state GTPase activity assayAgonist activity at human recombinant histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2 by steady-state GTPase activity assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmcl.2010.10.041
1267 3744 43 None -17 5 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1021/acs.jmedchem.0c00160
3035905 3744 43 None -17 5 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1021/acs.jmedchem.0c00160
CHEMBL260374 3744 43 None -17 5 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1021/acs.jmedchem.0c00160
44482032 5655 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19 protein by steady-state GTPase assayAgonist activity at human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19 protein by steady-state GTPase assay
ChEMBL 262 7 3 3 1.4 CC(C)CN/C(=N\C#N)NCCCCc1c[nH]cn1 10.1021/jm900526h
CHEMBL1078346 5655 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19 protein by steady-state GTPase assayAgonist activity at human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19 protein by steady-state GTPase assay
ChEMBL 262 7 3 3 1.4 CC(C)CN/C(=N\C#N)NCCCCc1c[nH]cn1 10.1021/jm900526h
25130581 186642 0 None 3 2 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at human histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 264 2 0 5 1.5 COc1nc(N2CCN(C)CC2)cc(C(C)(C)C)n1 10.1021/jm8005959
CHEMBL492489 186642 0 None 3 2 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at human histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 264 2 0 5 1.5 COc1nc(N2CCN(C)CC2)cc(C(C)(C)C)n1 10.1021/jm8005959
44482029 5560 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19 protein by steady-state GTPase assayAgonist activity at human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19 protein by steady-state GTPase assay
ChEMBL 325 9 3 4 1.8 N#C/N=C(/NCCCCc1c[nH]cn1)NCCCc1cccnc1 10.1021/jm900526h
CHEMBL1077737 5560 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19 protein by steady-state GTPase assayAgonist activity at human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19 protein by steady-state GTPase assay
ChEMBL 325 9 3 4 1.8 N#C/N=C(/NCCCCc1c[nH]cn1)NCCCc1cccnc1 10.1021/jm900526h
25131234 187079 0 None - 1 Rat 5.9 pEC50 = 5.9 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 294 2 1 6 1.3 CN1CCN(c2cc(-c3ccccc3C#N)nc(N)n2)CC1 10.1021/jm8005959
CHEMBL495083 187079 0 None - 1 Rat 5.9 pEC50 = 5.9 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 294 2 1 6 1.3 CN1CCN(c2cc(-c3ccccc3C#N)nc(N)n2)CC1 10.1021/jm8005959
25130235 187004 1 None 4 3 Mouse 6.9 pEC50 = 6.9 Functional
Agonist activity at mouse histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at mouse histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 294 2 1 6 1.3 CN1CCN(c2cc(-c3ccc(C#N)cc3)nc(N)n2)CC1 10.1021/jm8005959
CHEMBL494678 187004 1 None 4 3 Mouse 6.9 pEC50 = 6.9 Functional
Agonist activity at mouse histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at mouse histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 294 2 1 6 1.3 CN1CCN(c2cc(-c3ccc(C#N)cc3)nc(N)n2)CC1 10.1021/jm8005959
25130235 187004 1 None 4 3 Mouse 6.9 pEC50 = 6.9 Functional
Antagonist activity at mouse histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assayAntagonist activity at mouse histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assay
ChEMBL 294 2 1 6 1.3 CN1CCN(c2cc(-c3ccc(C#N)cc3)nc(N)n2)CC1 10.1021/jm800670r
CHEMBL494678 187004 1 None 4 3 Mouse 6.9 pEC50 = 6.9 Functional
Antagonist activity at mouse histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assayAntagonist activity at mouse histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assay
ChEMBL 294 2 1 6 1.3 CN1CCN(c2cc(-c3ccc(C#N)cc3)nc(N)n2)CC1 10.1021/jm800670r
25130234 186820 0 None - 1 Rat 4.9 pEC50 = 4.9 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 277 2 2 6 -0.7 CN1CCN(c2cc(N3CCNC3=O)nc(N)n2)CC1 10.1021/jm8005959
CHEMBL493663 186820 0 None - 1 Rat 4.9 pEC50 = 4.9 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 277 2 2 6 -0.7 CN1CCN(c2cc(N3CCNC3=O)nc(N)n2)CC1 10.1021/jm8005959
127051986 139774 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human histamine H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assayAgonist activity at human histamine H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 350 7 3 3 2.9 N#C/N=C(/NCCCc1ccccc1)NC[C@H]1CC[C@H](c2c[nH]cn2)C1 10.1021/acs.jmedchem.6b00120
CHEMBL3806098 139774 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human histamine H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assayAgonist activity at human histamine H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 350 7 3 3 2.9 N#C/N=C(/NCCCc1ccccc1)NC[C@H]1CC[C@H](c2c[nH]cn2)C1 10.1021/acs.jmedchem.6b00120
51354301 58584 0 None -1 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at histamine H4 receptor (unknown origin) expressed in HEK293T cells harboring CRE-luciferase after 6 hrs by luciferase reporter gene assayAgonist activity at histamine H4 receptor (unknown origin) expressed in HEK293T cells harboring CRE-luciferase after 6 hrs by luciferase reporter gene assay
ChEMBL 259 5 1 4 2.4 c1nc(CCn2cc(CC3CCCCC3)nn2)c[nH]1 10.1021/acs.jmedchem.8b00435
CHEMBL1688969 58584 0 None -1 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at histamine H4 receptor (unknown origin) expressed in HEK293T cells harboring CRE-luciferase after 6 hrs by luciferase reporter gene assayAgonist activity at histamine H4 receptor (unknown origin) expressed in HEK293T cells harboring CRE-luciferase after 6 hrs by luciferase reporter gene assay
ChEMBL 259 5 1 4 2.4 c1nc(CCn2cc(CC3CCCCC3)nn2)c[nH]1 10.1021/acs.jmedchem.8b00435
10934158 108090 1 None 1 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 258 5 1 3 2.8 c1ccc(COC[C@@H]2CC[C@H](c3c[nH]cn3)O2)cc1 10.1016/j.bmcl.2010.10.041
CHEMBL320331 108090 1 None 1 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 258 5 1 3 2.8 c1ccc(COC[C@@H]2CC[C@H](c3c[nH]cn3)O2)cc1 10.1016/j.bmcl.2010.10.041
10017821 103310 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 302 8 3 2 2.4 S=C(NCCCCc1c[nH]cn1)NCCc1ccccc1 10.1016/j.bmcl.2010.10.041
CHEMBL308913 103310 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 302 8 3 2 2.4 S=C(NCCCCc1c[nH]cn1)NCCc1ccccc1 10.1016/j.bmcl.2010.10.041
1238 2051 11 None -1258 2 Human 4.9 pEC50 = 4.9 Functional
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 125 2 2 2 0.3 C[C@@H](Cc1cnc[nH]1)N 10.1016/j.bmcl.2010.10.041
6603865 2051 11 None -1258 2 Human 4.9 pEC50 = 4.9 Functional
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 125 2 2 2 0.3 C[C@@H](Cc1cnc[nH]1)N 10.1016/j.bmcl.2010.10.041
CHEMBL11919 2051 11 None -1258 2 Human 4.9 pEC50 = 4.9 Functional
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 125 2 2 2 0.3 C[C@@H](Cc1cnc[nH]1)N 10.1016/j.bmcl.2010.10.041
11043445 56185 1 None -1 2 Human 4.9 pEC50 = 4.9 Functional
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 258 5 1 3 2.8 c1ccc(COC[C@H]2CC[C@@H](c3c[nH]cn3)O2)cc1 10.1016/j.bmcl.2010.10.041
CHEMBL1632410 56185 1 None -1 2 Human 4.9 pEC50 = 4.9 Functional
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 258 5 1 3 2.8 c1ccc(COC[C@H]2CC[C@@H](c3c[nH]cn3)O2)cc1 10.1016/j.bmcl.2010.10.041
10945113 109141 1 None -1 2 Human 4.9 pEC50 = 4.9 Functional
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 258 5 1 3 2.8 c1ccc(COC[C@@H]2CC[C@@H](c3c[nH]cn3)O2)cc1 10.1016/j.bmcl.2010.10.041
CHEMBL322256 109141 1 None -1 2 Human 4.9 pEC50 = 4.9 Functional
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 258 5 1 3 2.8 c1ccc(COC[C@@H]2CC[C@@H](c3c[nH]cn3)O2)cc1 10.1016/j.bmcl.2010.10.041
44480707 5686 0 None 5 2 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19 protein by steady-state GTPase assayAgonist activity at human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19 protein by steady-state GTPase assay
ChEMBL 328 8 3 4 2.2 N#C/N=C(/NCCCc1c[nH]cn1)NCCSc1ccccc1 10.1021/jm900526h
CHEMBL1078529 5686 0 None 5 2 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19 protein by steady-state GTPase assayAgonist activity at human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19 protein by steady-state GTPase assay
ChEMBL 328 8 3 4 2.2 N#C/N=C(/NCCCc1c[nH]cn1)NCCSc1ccccc1 10.1021/jm900526h
10945113 109141 1 None -1 2 Human 4.9 pEC50 = 4.9 Functional
Inhibition of the forskolin-stimulated cAMP production in SK-N-MC cells expressing human Histamine H4 receptorInhibition of the forskolin-stimulated cAMP production in SK-N-MC cells expressing human Histamine H4 receptor
ChEMBL 258 5 1 3 2.8 c1ccc(COC[C@@H]2CC[C@@H](c3c[nH]cn3)O2)cc1 10.1021/jm0300025
CHEMBL322256 109141 1 None -1 2 Human 4.9 pEC50 = 4.9 Functional
Inhibition of the forskolin-stimulated cAMP production in SK-N-MC cells expressing human Histamine H4 receptorInhibition of the forskolin-stimulated cAMP production in SK-N-MC cells expressing human Histamine H4 receptor
ChEMBL 258 5 1 3 2.8 c1ccc(COC[C@@H]2CC[C@@H](c3c[nH]cn3)O2)cc1 10.1021/jm0300025
127052294 139772 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human histamine H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assayAgonist activity at human histamine H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 368 7 3 4 3.1 N#C/N=C(/NCCSc1ccccc1)NC[C@@H]1CC[C@H](c2c[nH]cn2)C1 10.1021/acs.jmedchem.6b00120
CHEMBL3806079 139772 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human histamine H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assayAgonist activity at human histamine H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 368 7 3 4 3.1 N#C/N=C(/NCCSc1ccccc1)NC[C@@H]1CC[C@H](c2c[nH]cn2)C1 10.1021/acs.jmedchem.6b00120
1204 1901 114 None -1 10 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmc.2009.08.059
1247 1901 114 None -1 10 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmc.2009.08.059
1375 1901 114 None -1 10 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmc.2009.08.059
774 1901 114 None -1 10 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmc.2009.08.059
CHEMBL90 1901 114 None -1 10 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmc.2009.08.059
DB05381 1901 114 None -1 10 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmc.2009.08.059
10934158 108090 1 None 1 2 Human 6.9 pEC50 = 6.9 Functional
Inhibition of the forskolin-stimulated cAMP production in SK-N-MC cells expressing human Histamine H4 receptorInhibition of the forskolin-stimulated cAMP production in SK-N-MC cells expressing human Histamine H4 receptor
ChEMBL 258 5 1 3 2.8 c1ccc(COC[C@@H]2CC[C@H](c3c[nH]cn3)O2)cc1 10.1021/jm0300025
CHEMBL320331 108090 1 None 1 2 Human 6.9 pEC50 = 6.9 Functional
Inhibition of the forskolin-stimulated cAMP production in SK-N-MC cells expressing human Histamine H4 receptorInhibition of the forskolin-stimulated cAMP production in SK-N-MC cells expressing human Histamine H4 receptor
ChEMBL 258 5 1 3 2.8 c1ccc(COC[C@@H]2CC[C@H](c3c[nH]cn3)O2)cc1 10.1021/jm0300025
25129182 186700 0 None - 1 Rat 5.9 pEC50 = 5.9 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 291 2 1 7 -0.4 CN1CCN(c2cc(N3CCN(C)CC3)nc(N)n2)CC1 10.1021/jm8005959
CHEMBL492869 186700 0 None - 1 Rat 5.9 pEC50 = 5.9 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 291 2 1 7 -0.4 CN1CCN(c2cc(N3CCN(C)CC3)nc(N)n2)CC1 10.1021/jm8005959
127052293 139708 1 None 10 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human histamine H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assayAgonist activity at human histamine H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 368 7 3 4 3.1 N#C/N=C(/NCCSc1ccccc1)NC[C@H]1CC[C@H](c2c[nH]cn2)C1 10.1021/acs.jmedchem.6b00120
CHEMBL3805361 139708 1 None 10 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human histamine H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assayAgonist activity at human histamine H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 368 7 3 4 3.1 N#C/N=C(/NCCSc1ccccc1)NC[C@H]1CC[C@H](c2c[nH]cn2)C1 10.1021/acs.jmedchem.6b00120
11846634 77655 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Activity at human histamine H4 receptor transfected in SK-N-MC cells by cAMP assayActivity at human histamine H4 receptor transfected in SK-N-MC cells by cAMP assay
ChEMBL 345 0 0 4 3.9 CN1CCN(C2=Nc3cc(Cl)ccc3Oc3c(F)cccc32)CC1 10.1021/jm051008s
CHEMBL209758 77655 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Activity at human histamine H4 receptor transfected in SK-N-MC cells by cAMP assayActivity at human histamine H4 receptor transfected in SK-N-MC cells by cAMP assay
ChEMBL 345 0 0 4 3.9 CN1CCN(C2=Nc3cc(Cl)ccc3Oc3c(F)cccc32)CC1 10.1021/jm051008s
11846464 78051 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Activity at human histamine H4 receptor transfected in SK-N-MC cells by cAMP assayActivity at human histamine H4 receptor transfected in SK-N-MC cells by cAMP assay
ChEMBL 361 0 0 4 4.4 CN1CCN(C2=Nc3ccc(Cl)cc3Oc3c(Cl)cccc32)CC1 10.1021/jm051008s
CHEMBL211170 78051 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Activity at human histamine H4 receptor transfected in SK-N-MC cells by cAMP assayActivity at human histamine H4 receptor transfected in SK-N-MC cells by cAMP assay
ChEMBL 361 0 0 4 4.4 CN1CCN(C2=Nc3ccc(Cl)cc3Oc3c(Cl)cccc32)CC1 10.1021/jm051008s
25071319 188474 8 None 1 2 Rat 7.8 pEC50 = 7.8 Functional
Antagonist activity at rat histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assayAntagonist activity at rat histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assay
ChEMBL 295 1 2 5 1.6 Nc1nc2c(c(N3CCNCC3)n1)CCCc1ccccc1-2 10.1021/jm800670r
CHEMBL509540 188474 8 None 1 2 Rat 7.8 pEC50 = 7.8 Functional
Antagonist activity at rat histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assayAntagonist activity at rat histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assay
ChEMBL 295 1 2 5 1.6 Nc1nc2c(c(N3CCNCC3)n1)CCCc1ccccc1-2 10.1021/jm800670r
44482030 5599 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19 protein by steady-state GTPase assayAgonist activity at human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19 protein by steady-state GTPase assay
ChEMBL 338 9 3 3 2.9 CC(CCN/C(=N\C#N)NCCCCc1c[nH]cn1)c1ccccc1 10.1021/jm900526h
CHEMBL1077860 5599 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19 protein by steady-state GTPase assayAgonist activity at human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19 protein by steady-state GTPase assay
ChEMBL 338 9 3 3 2.9 CC(CCN/C(=N\C#N)NCCCCc1c[nH]cn1)c1ccccc1 10.1021/jm900526h
25131561 186821 0 None -3 2 Rat 4.9 pEC50 = 4.9 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 286 2 1 7 -0.0 CN1CCN(c2cc(-n3ccccc3=O)nc(N)n2)CC1 10.1021/jm8005959
CHEMBL493664 186821 0 None -3 2 Rat 4.9 pEC50 = 4.9 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 286 2 1 7 -0.0 CN1CCN(c2cc(-n3ccccc3=O)nc(N)n2)CC1 10.1021/jm8005959
135897837 187045 12 None - 1 Rat 5.8 pEC50 = 5.8 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 209 1 2 6 -0.5 CN1CCN(c2cc(O)nc(N)n2)CC1 10.1021/jm8005959
CHEMBL494909 187045 12 None - 1 Rat 5.8 pEC50 = 5.8 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 209 1 2 6 -0.5 CN1CCN(c2cc(O)nc(N)n2)CC1 10.1021/jm8005959
127048828 139790 0 None 38 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human histamine H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assayAgonist activity at human histamine H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 288 5 3 3 2.0 CC(C)CN/C(=N/C#N)NC[C@H]1CC[C@H](c2c[nH]cn2)C1 10.1021/acs.jmedchem.6b00120
CHEMBL3806255 139790 0 None 38 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human histamine H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assayAgonist activity at human histamine H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 288 5 3 3 2.0 CC(C)CN/C(=N/C#N)NC[C@H]1CC[C@H](c2c[nH]cn2)C1 10.1021/acs.jmedchem.6b00120
58227255 116623 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human recombinant histamine H4 receptor expressed in SK-N-MC cells assessed as effect on forskolin-stimulated cAMP-mediated reporter gene activityAgonist activity at human recombinant histamine H4 receptor expressed in SK-N-MC cells assessed as effect on forskolin-stimulated cAMP-mediated reporter gene activity
ChEMBL 249 5 2 5 1.3 CN[C@@H]1CCN(c2ccnc(NCC(C)C)n2)C1 10.1016/j.bmcl.2014.12.027
CHEMBL3393539 116623 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human recombinant histamine H4 receptor expressed in SK-N-MC cells assessed as effect on forskolin-stimulated cAMP-mediated reporter gene activityAgonist activity at human recombinant histamine H4 receptor expressed in SK-N-MC cells assessed as effect on forskolin-stimulated cAMP-mediated reporter gene activity
ChEMBL 249 5 2 5 1.3 CN[C@@H]1CCN(c2ccnc(NCC(C)C)n2)C1 10.1016/j.bmcl.2014.12.027
44568832 186600 0 None - 1 Rat 7.8 pEC50 = 7.8 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 306 2 1 6 1.2 CN1CCN(c2cc(-c3ccc(F)nc3F)nc(N)n2)CC1 10.1021/jm8005959
CHEMBL492242 186600 0 None - 1 Rat 7.8 pEC50 = 7.8 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 306 2 1 6 1.2 CN1CCN(c2cc(-c3ccc(F)nc3F)nc(N)n2)CC1 10.1021/jm8005959
25128822 186898 0 None 19 2 Rat 7.8 pEC50 = 7.8 Functional
Antagonist activity at rat histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assayAntagonist activity at rat histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assay
ChEMBL 295 1 1 5 1.6 CN1CCN(c2nc(N)nc3c2CCc2ccccc2-3)CC1 10.1021/jm800670r
CHEMBL494093 186898 0 None 19 2 Rat 7.8 pEC50 = 7.8 Functional
Antagonist activity at rat histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assayAntagonist activity at rat histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assay
ChEMBL 295 1 1 5 1.6 CN1CCN(c2nc(N)nc3c2CCc2ccccc2-3)CC1 10.1021/jm800670r
1251 1983 34 None -204 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human histamine H4 receptorAgonist activity at human histamine H4 receptor
ChEMBL 165 2 2 2 1.0 N1CCC(CC1)Cc1[nH]cnc1 10.1021/jm100064d
3035842 1983 34 None -204 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human histamine H4 receptorAgonist activity at human histamine H4 receptor
ChEMBL 165 2 2 2 1.0 N1CCC(CC1)Cc1[nH]cnc1 10.1021/jm100064d
CHEMBL18661 1983 34 None -204 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human histamine H4 receptorAgonist activity at human histamine H4 receptor
ChEMBL 165 2 2 2 1.0 N1CCC(CC1)Cc1[nH]cnc1 10.1021/jm100064d
1251 1983 34 None -204 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 165 2 2 2 1.0 N1CCC(CC1)Cc1[nH]cnc1 10.1016/j.bmcl.2010.10.041
3035842 1983 34 None -204 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 165 2 2 2 1.0 N1CCC(CC1)Cc1[nH]cnc1 10.1016/j.bmcl.2010.10.041
CHEMBL18661 1983 34 None -204 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 165 2 2 2 1.0 N1CCC(CC1)Cc1[nH]cnc1 10.1016/j.bmcl.2010.10.041
25149712 178408 0 None -6 3 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human recombinant histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2 by steady-state GTPase activity assayAgonist activity at human recombinant histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2 by steady-state GTPase activity assay
ChEMBL 299 7 4 3 1.6 N=C(NCCCc1c[nH]cn1)NC(=O)CCc1ccccc1 10.1016/j.bmcl.2010.10.041
CHEMBL470790 178408 0 None -6 3 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human recombinant histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2 by steady-state GTPase activity assayAgonist activity at human recombinant histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2 by steady-state GTPase activity assay
ChEMBL 299 7 4 3 1.6 N=C(NCCCc1c[nH]cn1)NC(=O)CCc1ccccc1 10.1016/j.bmcl.2010.10.041
25149335 183643 0 None -6 3 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human recombinant histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2 by steady-state GTPase activity assayAgonist activity at human recombinant histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2 by steady-state GTPase activity assay
ChEMBL 313 7 3 2 2.0 CC(CC(=O)/N=C(\N)NCCCc1c[nH]cn1)c1ccccc1 10.1016/j.bmcl.2010.10.041
CHEMBL483406 183643 0 None -6 3 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human recombinant histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2 by steady-state GTPase activity assayAgonist activity at human recombinant histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2 by steady-state GTPase activity assay
ChEMBL 313 7 3 2 2.0 CC(CC(=O)/N=C(\N)NCCCc1c[nH]cn1)c1ccccc1 10.1016/j.bmcl.2010.10.041
1278 2119 79 None 1 4 Human 7.8 pEC50 = 7.8 Functional
Inverse agonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of [35S]GTPgammaS bindingInverse agonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1016/j.bmc.2009.08.059
1279 2119 79 None 1 4 Human 7.8 pEC50 = 7.8 Functional
Inverse agonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of [35S]GTPgammaS bindingInverse agonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1016/j.bmc.2009.08.059
4908365 2119 79 None 1 4 Human 7.8 pEC50 = 7.8 Functional
Inverse agonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of [35S]GTPgammaS bindingInverse agonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1016/j.bmc.2009.08.059
CHEMBL129198 2119 79 None 1 4 Human 7.8 pEC50 = 7.8 Functional
Inverse agonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of [35S]GTPgammaS bindingInverse agonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1016/j.bmc.2009.08.059
127048890 139765 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human histamine H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assayAgonist activity at human histamine H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 165 2 2 2 1.3 NC[C@@H]1CC[C@H](c2c[nH]cn2)C1 10.1021/acs.jmedchem.6b00120
CHEMBL3805995 139765 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human histamine H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assayAgonist activity at human histamine H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 165 2 2 2 1.3 NC[C@@H]1CC[C@H](c2c[nH]cn2)C1 10.1021/acs.jmedchem.6b00120
46890548 6506 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human histamine H4 receptor in SK-N-MC cells assessed as forskolin-stimulated cAMP release preincubated for 10 mins before forskolin challengeAgonist activity at human histamine H4 receptor in SK-N-MC cells assessed as forskolin-stimulated cAMP release preincubated for 10 mins before forskolin challenge
ChEMBL 410 7 1 4 4.4 Cc1cc(OCCCN2CCC(N(C)C)C2)ccc1-c1nc2c(C)c(F)ccc2[nH]1 10.1016/j.bmcl.2010.04.017
CHEMBL1083084 6506 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human histamine H4 receptor in SK-N-MC cells assessed as forskolin-stimulated cAMP release preincubated for 10 mins before forskolin challengeAgonist activity at human histamine H4 receptor in SK-N-MC cells assessed as forskolin-stimulated cAMP release preincubated for 10 mins before forskolin challenge
ChEMBL 410 7 1 4 4.4 Cc1cc(OCCCN2CCC(N(C)C)C2)ccc1-c1nc2c(C)c(F)ccc2[nH]1 10.1016/j.bmcl.2010.04.017
44481761 5697 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19 protein by steady-state GTPase assayAgonist activity at human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19 protein by steady-state GTPase assay
ChEMBL 324 9 3 3 2.4 N#C/N=C(/NCCCCc1c[nH]cn1)NCCCc1ccccc1 10.1021/jm900526h
CHEMBL1078631 5697 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19 protein by steady-state GTPase assayAgonist activity at human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19 protein by steady-state GTPase assay
ChEMBL 324 9 3 3 2.4 N#C/N=C(/NCCCCc1c[nH]cn1)NCCCc1ccccc1 10.1021/jm900526h
51354301 58584 0 None -1 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human histamine H4 receptor expressed in HEK293 cells assessed by forskolin induced cAMP response element activation by luciferase reporter gene assayAgonist activity at human histamine H4 receptor expressed in HEK293 cells assessed by forskolin induced cAMP response element activation by luciferase reporter gene assay
ChEMBL 259 5 1 4 2.4 c1nc(CCn2cc(CC3CCCCC3)nn2)c[nH]1 10.1021/jm1013488
CHEMBL1688969 58584 0 None -1 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human histamine H4 receptor expressed in HEK293 cells assessed by forskolin induced cAMP response element activation by luciferase reporter gene assayAgonist activity at human histamine H4 receptor expressed in HEK293 cells assessed by forskolin induced cAMP response element activation by luciferase reporter gene assay
ChEMBL 259 5 1 4 2.4 c1nc(CCn2cc(CC3CCCCC3)nn2)c[nH]1 10.1021/jm1013488
155513612 175746 0 None -18 3 Rat 6.8 pEC50 = 6.8 Functional
Agonist activity at rat H4R expressed in in HEK293T cells by CRE-luciferase reporter gene assayAgonist activity at rat H4R expressed in in HEK293T cells by CRE-luciferase reporter gene assay
ChEMBL 277 4 1 5 2.1 CN(C)[C@@H]1CCN(c2ccnc(NCC(C)(C)C)n2)C1 10.1021/acs.jmedchem.9b01342
CHEMBL4439142 175746 0 None -18 3 Rat 6.8 pEC50 = 6.8 Functional
Agonist activity at rat H4R expressed in in HEK293T cells by CRE-luciferase reporter gene assayAgonist activity at rat H4R expressed in in HEK293T cells by CRE-luciferase reporter gene assay
ChEMBL 277 4 1 5 2.1 CN(C)[C@@H]1CCN(c2ccnc(NCC(C)(C)C)n2)C1 10.1021/acs.jmedchem.9b01342
CHEMBL4515149 175746 0 None -18 3 Rat 6.8 pEC50 = 6.8 Functional
Agonist activity at rat H4R expressed in in HEK293T cells by CRE-luciferase reporter gene assayAgonist activity at rat H4R expressed in in HEK293T cells by CRE-luciferase reporter gene assay
ChEMBL 277 4 1 5 2.1 CN(C)[C@@H]1CCN(c2ccnc(NCC(C)(C)C)n2)C1 10.1021/acs.jmedchem.9b01342
CHEMBL4595327 175746 0 None -18 3 Rat 6.8 pEC50 = 6.8 Functional
Agonist activity at rat H4R expressed in in HEK293T cells by CRE-luciferase reporter gene assayAgonist activity at rat H4R expressed in in HEK293T cells by CRE-luciferase reporter gene assay
ChEMBL 277 4 1 5 2.1 CN(C)[C@@H]1CCN(c2ccnc(NCC(C)(C)C)n2)C1 10.1021/acs.jmedchem.9b01342
1204 1901 114 None -97 10 Rat 6.8 pEC50 = 6.8 Functional
Agonist activity at rat histamine H4 receptor by luciferase reporter gene assayAgonist activity at rat histamine H4 receptor by luciferase reporter gene assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmcl.2010.10.041
1247 1901 114 None -97 10 Rat 6.8 pEC50 = 6.8 Functional
Agonist activity at rat histamine H4 receptor by luciferase reporter gene assayAgonist activity at rat histamine H4 receptor by luciferase reporter gene assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmcl.2010.10.041
1375 1901 114 None -97 10 Rat 6.8 pEC50 = 6.8 Functional
Agonist activity at rat histamine H4 receptor by luciferase reporter gene assayAgonist activity at rat histamine H4 receptor by luciferase reporter gene assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmcl.2010.10.041
774 1901 114 None -97 10 Rat 6.8 pEC50 = 6.8 Functional
Agonist activity at rat histamine H4 receptor by luciferase reporter gene assayAgonist activity at rat histamine H4 receptor by luciferase reporter gene assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmcl.2010.10.041
CHEMBL90 1901 114 None -97 10 Rat 6.8 pEC50 = 6.8 Functional
Agonist activity at rat histamine H4 receptor by luciferase reporter gene assayAgonist activity at rat histamine H4 receptor by luciferase reporter gene assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmcl.2010.10.041
DB05381 1901 114 None -97 10 Rat 6.8 pEC50 = 6.8 Functional
Agonist activity at rat histamine H4 receptor by luciferase reporter gene assayAgonist activity at rat histamine H4 receptor by luciferase reporter gene assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmcl.2010.10.041
1248 1396 27 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 161 4 2 3 0.6 CN(CCCSC(=N)N)C 10.1016/j.bmcl.2010.10.041
3077 1396 27 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 161 4 2 3 0.6 CN(CCCSC(=N)N)C 10.1016/j.bmcl.2010.10.041
90045 1396 27 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 161 4 2 3 0.6 CN(CCCSC(=N)N)C 10.1016/j.bmcl.2010.10.041
CHEMBL12344 1396 27 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 161 4 2 3 0.6 CN(CCCSC(=N)N)C 10.1016/j.bmcl.2010.10.041
5310982 93179 4 None -3 2 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human recombinant histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2 by steady-state GTPase activity assayAgonist activity at human recombinant histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2 by steady-state GTPase activity assay
ChEMBL 255 3 2 2 2.6 NCCc1c[nH]c(-c2cccc(C(F)(F)F)c2)n1 10.1016/j.bmcl.2010.10.041
CHEMBL24665 93179 4 None -3 2 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human recombinant histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2 by steady-state GTPase activity assayAgonist activity at human recombinant histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2 by steady-state GTPase activity assay
ChEMBL 255 3 2 2 2.6 NCCc1c[nH]c(-c2cccc(C(F)(F)F)c2)n1 10.1016/j.bmcl.2010.10.041
1269 121 33 None -35 6 Mouse 5.8 pEC50 = 5.8 Functional
Agonist activity at mouse histamine H4 receptorAgonist activity at mouse histamine H4 receptor
ChEMBL 125 2 2 2 0.2 Cc1c(CCN)nc[nH]1 10.1016/j.bmcl.2010.10.041
37463 121 33 None -35 6 Mouse 5.8 pEC50 = 5.8 Functional
Agonist activity at mouse histamine H4 receptorAgonist activity at mouse histamine H4 receptor
ChEMBL 125 2 2 2 0.2 Cc1c(CCN)nc[nH]1 10.1016/j.bmcl.2010.10.041
CHEMBL275443 121 33 None -35 6 Mouse 5.8 pEC50 = 5.8 Functional
Agonist activity at mouse histamine H4 receptorAgonist activity at mouse histamine H4 receptor
ChEMBL 125 2 2 2 0.2 Cc1c(CCN)nc[nH]1 10.1016/j.bmcl.2010.10.041
53233802 61218 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells assessed as effect on forskolin-induced cAMP accumulation after 6 hrsAgonist activity at human histamine H4 receptor expressed in human SK-N-MC cells assessed as effect on forskolin-induced cAMP accumulation after 6 hrs
ChEMBL 276 3 2 6 1.2 CN1CCN(c2cc(N)nc(NC3CCCC3)n2)CC1 10.1016/j.bmcl.2011.03.017
CHEMBL1770987 61218 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells assessed as effect on forskolin-induced cAMP accumulation after 6 hrsAgonist activity at human histamine H4 receptor expressed in human SK-N-MC cells assessed as effect on forskolin-induced cAMP accumulation after 6 hrs
ChEMBL 276 3 2 6 1.2 CN1CCN(c2cc(N)nc(NC3CCCC3)n2)CC1 10.1016/j.bmcl.2011.03.017
25131559 187002 0 None 23 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at human histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 259 2 2 6 0.2 CN1CCN(c2cc(-c3c[nH]cn3)nc(N)n2)CC1 10.1021/jm8005959
CHEMBL494667 187002 0 None 23 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at human histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 259 2 2 6 0.2 CN1CCN(c2cc(-c3c[nH]cn3)nc(N)n2)CC1 10.1021/jm8005959
1204 1901 114 None -1 10 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.0c00160
1204 1901 114 None -1 10 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.9b01342
1247 1901 114 None -1 10 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.0c00160
1247 1901 114 None -1 10 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.9b01342
1375 1901 114 None -1 10 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.0c00160
1375 1901 114 None -1 10 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.9b01342
774 1901 114 None -1 10 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.0c00160
774 1901 114 None -1 10 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.9b01342
CHEMBL90 1901 114 None -1 10 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.0c00160
CHEMBL90 1901 114 None -1 10 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.9b01342
DB05381 1901 114 None -1 10 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.0c00160
DB05381 1901 114 None -1 10 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.9b01342
44480959 5600 2 None 1 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19 protein by steady-state GTPase assayAgonist activity at human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19 protein by steady-state GTPase assay
ChEMBL 206 5 3 3 0.1 N#C/N=C(\N)NCCCCc1c[nH]cn1 10.1021/jm900526h
CHEMBL1077861 5600 2 None 1 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19 protein by steady-state GTPase assayAgonist activity at human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19 protein by steady-state GTPase assay
ChEMBL 206 5 3 3 0.1 N#C/N=C(\N)NCCCCc1c[nH]cn1 10.1021/jm900526h
1484519 173324 52 None - 1 Rat 4.8 pEC50 = 4.8 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 227 1 1 5 0.5 CN1CCN(c2cc(Cl)nc(N)n2)CC1 10.1021/jm8005959
CHEMBL454007 173324 52 None - 1 Rat 4.8 pEC50 = 4.8 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 227 1 1 5 0.5 CN1CCN(c2cc(Cl)nc(N)n2)CC1 10.1021/jm8005959
21638785 188073 4 None 1 2 Mouse 7.8 pEC50 = 7.8 Functional
Antagonist activity at mouse histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assayAntagonist activity at mouse histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assay
ChEMBL 263 1 2 2 1.9 O=C(c1cc2cc(Cl)ccc2[nH]1)N1CCNCC1 10.1021/jm800670r
CHEMBL503605 188073 4 None 1 2 Mouse 7.8 pEC50 = 7.8 Functional
Antagonist activity at mouse histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assayAntagonist activity at mouse histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assay
ChEMBL 263 1 2 2 1.9 O=C(c1cc2cc(Cl)ccc2[nH]1)N1CCNCC1 10.1021/jm800670r
127051958 139748 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human histamine H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assayAgonist activity at human histamine H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 165 2 2 2 1.3 NC[C@H]1CC[C@H](c2c[nH]cn2)C1 10.1021/acs.jmedchem.6b00120
CHEMBL3805813 139748 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human histamine H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assayAgonist activity at human histamine H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 165 2 2 2 1.3 NC[C@H]1CC[C@H](c2c[nH]cn2)C1 10.1021/acs.jmedchem.6b00120
25129880 192528 0 None - 1 Rat 6.8 pEC50 = 6.8 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 319 2 1 5 2.6 CN1CCN(c2cc(-c3ccc4ccccc4c3)nc(N)n2)CC1 10.1021/jm8005959
CHEMBL522841 192528 0 None - 1 Rat 6.8 pEC50 = 6.8 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 319 2 1 5 2.6 CN1CCN(c2cc(-c3ccc4ccccc4c3)nc(N)n2)CC1 10.1021/jm8005959
25130231 187121 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at human histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 309 2 1 7 1.2 CN1CCN(c2cc(-n3cnc4ccccc43)nc(N)n2)CC1 10.1021/jm8005959
CHEMBL495280 187121 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at human histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 309 2 1 7 1.2 CN1CCN(c2cc(-n3cnc4ccccc43)nc(N)n2)CC1 10.1021/jm8005959
25131228 187011 0 None - 1 Rat 6.8 pEC50 = 6.8 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 283 2 1 5 1.8 Cc1ccccc1-c1cc(N2CCN(C)CC2)nc(N)n1 10.1021/jm8005959
CHEMBL494723 187011 0 None - 1 Rat 6.8 pEC50 = 6.8 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 283 2 1 5 1.8 Cc1ccccc1-c1cc(N2CCN(C)CC2)nc(N)n1 10.1021/jm8005959
25128828 187669 2 None - 1 Rat 5.8 pEC50 = 5.8 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 237 4 2 5 1.3 CN(C)CCNc1cc(C(C)(C)C)nc(N)n1 10.1021/jm8005959
CHEMBL499631 187669 2 None - 1 Rat 5.8 pEC50 = 5.8 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 237 4 2 5 1.3 CN(C)CCNc1cc(C(C)(C)C)nc(N)n1 10.1021/jm8005959
58227163 175889 0 None 4 3 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 263 3 2 5 1.7 CC(C)(C)CNc1nccc(N2CCCNCC2)n1 10.1021/acs.jmedchem.9b01342
CHEMBL4518374 175889 0 None 4 3 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 263 3 2 5 1.7 CC(C)(C)CNc1nccc(N2CCCNCC2)n1 10.1021/acs.jmedchem.9b01342
CHEMBL4596491 175889 0 None 4 3 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 263 3 2 5 1.7 CC(C)(C)CNc1nccc(N2CCCNCC2)n1 10.1021/acs.jmedchem.9b01342
25071319 188474 8 None -1 2 Mouse 7.7 pEC50 = 7.7 Functional
Antagonist activity at mouse histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assayAntagonist activity at mouse histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assay
ChEMBL 295 1 2 5 1.6 Nc1nc2c(c(N3CCNCC3)n1)CCCc1ccccc1-2 10.1021/jm800670r
CHEMBL509540 188474 8 None -1 2 Mouse 7.7 pEC50 = 7.7 Functional
Antagonist activity at mouse histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assayAntagonist activity at mouse histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assay
ChEMBL 295 1 2 5 1.6 Nc1nc2c(c(N3CCNCC3)n1)CCCc1ccccc1-2 10.1021/jm800670r
1204 1901 114 None -1 10 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human H4 receptor expressed in 293-EBNA cells by luciferase reporter gene assayAgonist activity at human H4 receptor expressed in 293-EBNA cells by luciferase reporter gene assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm0603318
1247 1901 114 None -1 10 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human H4 receptor expressed in 293-EBNA cells by luciferase reporter gene assayAgonist activity at human H4 receptor expressed in 293-EBNA cells by luciferase reporter gene assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm0603318
1375 1901 114 None -1 10 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human H4 receptor expressed in 293-EBNA cells by luciferase reporter gene assayAgonist activity at human H4 receptor expressed in 293-EBNA cells by luciferase reporter gene assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm0603318
774 1901 114 None -1 10 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human H4 receptor expressed in 293-EBNA cells by luciferase reporter gene assayAgonist activity at human H4 receptor expressed in 293-EBNA cells by luciferase reporter gene assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm0603318
CHEMBL90 1901 114 None -1 10 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human H4 receptor expressed in 293-EBNA cells by luciferase reporter gene assayAgonist activity at human H4 receptor expressed in 293-EBNA cells by luciferase reporter gene assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm0603318
DB05381 1901 114 None -1 10 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human H4 receptor expressed in 293-EBNA cells by luciferase reporter gene assayAgonist activity at human H4 receptor expressed in 293-EBNA cells by luciferase reporter gene assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm0603318
25130233 170046 6 None - 1 Rat 5.7 pEC50 = 5.7 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 259 2 2 6 0.2 CN1CCN(c2cc(-c3cn[nH]c3)nc(N)n2)CC1 10.1021/jm8005959
CHEMBL445091 170046 6 None - 1 Rat 5.7 pEC50 = 5.7 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 259 2 2 6 0.2 CN1CCN(c2cc(-c3cn[nH]c3)nc(N)n2)CC1 10.1021/jm8005959
25128831 172044 0 None -1 2 Rat 4.7 pEC50 = 4.7 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 277 2 0 5 1.6 CN1CCN(c2cc(C(C)(C)C)nc(N(C)C)n2)CC1 10.1021/jm8005959
CHEMBL449157 172044 0 None -1 2 Rat 4.7 pEC50 = 4.7 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 277 2 0 5 1.6 CN1CCN(c2cc(C(C)(C)C)nc(N(C)C)n2)CC1 10.1021/jm8005959
25130574 186793 0 None - 1 Rat 5.7 pEC50 = 5.7 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 293 2 1 5 2.0 CN1CCN(c2cc(N)nc(-c3ccc(C#N)cc3)c2)CC1 10.1021/jm8005959
CHEMBL493461 186793 0 None - 1 Rat 5.7 pEC50 = 5.7 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 293 2 1 5 2.0 CN1CCN(c2cc(N)nc(-c3ccc(C#N)cc3)c2)CC1 10.1021/jm8005959
44568790 170848 0 None - 1 Rat 7.7 pEC50 = 7.7 Functional
Antagonist activity at rat histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assayAntagonist activity at rat histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assay
ChEMBL 281 2 2 5 1.4 CN[C@@H]1CCN(c2nc(N)nc3c2Cc2ccccc2-3)C1 10.1021/jm800670r
CHEMBL446269 170848 0 None - 1 Rat 7.7 pEC50 = 7.7 Functional
Antagonist activity at rat histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assayAntagonist activity at rat histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assay
ChEMBL 281 2 2 5 1.4 CN[C@@H]1CCN(c2nc(N)nc3c2Cc2ccccc2-3)C1 10.1021/jm800670r
155552061 175904 0 None -2 3 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 277 3 1 5 2.1 CN1CCCN(c2ccnc(NCC(C)(C)C)n2)CC1 10.1021/acs.jmedchem.9b01342
CHEMBL4543119 175904 0 None -2 3 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 277 3 1 5 2.1 CN1CCCN(c2ccnc(NCC(C)(C)C)n2)CC1 10.1021/acs.jmedchem.9b01342
CHEMBL4596606 175904 0 None -2 3 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 277 3 1 5 2.1 CN1CCCN(c2ccnc(NCC(C)(C)C)n2)CC1 10.1021/acs.jmedchem.9b01342
45257133 198222 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of GTPase by [gamma-32P]GTP spontaneous degradation assayAgonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of GTPase by [gamma-32P]GTP spontaneous degradation assay
ChEMBL 332 4 2 6 2.1 CN1CCN(c2cc(NCc3ccccc3Cl)nc(N)n2)CC1 10.1016/j.bmc.2009.08.059
CHEMBL594721 198222 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of GTPase by [gamma-32P]GTP spontaneous degradation assayAgonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of GTPase by [gamma-32P]GTP spontaneous degradation assay
ChEMBL 332 4 2 6 2.1 CN1CCN(c2cc(NCc3ccccc3Cl)nc(N)n2)CC1 10.1016/j.bmc.2009.08.059
11846300 79856 3 None -2 2 Human 7.7 pEC50 = 7.7 Functional
Activity at human histamine H4 receptor transfected in SK-N-MC cells by cAMP assayActivity at human histamine H4 receptor transfected in SK-N-MC cells by cAMP assay
ChEMBL 327 0 0 4 3.8 CN1CCN(C2=Nc3ccc(Cl)cc3Oc3ccccc32)CC1 10.1021/jm051008s
CHEMBL213912 79856 3 None -2 2 Human 7.7 pEC50 = 7.7 Functional
Activity at human histamine H4 receptor transfected in SK-N-MC cells by cAMP assayActivity at human histamine H4 receptor transfected in SK-N-MC cells by cAMP assay
ChEMBL 327 0 0 4 3.8 CN1CCN(C2=Nc3ccc(Cl)cc3Oc3ccccc32)CC1 10.1021/jm051008s
1204 1901 114 None -1 10 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmcl.2010.10.041
1247 1901 114 None -1 10 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmcl.2010.10.041
1375 1901 114 None -1 10 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmcl.2010.10.041
774 1901 114 None -1 10 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmcl.2010.10.041
CHEMBL90 1901 114 None -1 10 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmcl.2010.10.041
DB05381 1901 114 None -1 10 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmcl.2010.10.041
3032915 15321 20 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 212 5 3 2 1.2 C/N=C(\S)NCCCCc1c[nH]cn1 10.1016/j.bmcl.2010.10.041
CHEMBL12160 15321 20 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 212 5 3 2 1.2 C/N=C(\S)NCCCCc1c[nH]cn1 10.1016/j.bmcl.2010.10.041
53321919 56184 0 None -50 2 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 322 7 3 3 3.8 N=C(NCc1ccc(Cl)cc1)SCCCCc1c[nH]cn1 10.1016/j.bmcl.2010.10.041
CHEMBL1632409 56184 0 None -50 2 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 322 7 3 3 3.8 N=C(NCc1ccc(Cl)cc1)SCCCCc1c[nH]cn1 10.1016/j.bmcl.2010.10.041
10060213 102438 1 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 240 6 3 2 2.0 CC(C)/N=C(\S)NCCCCc1c[nH]cn1 10.1016/j.bmcl.2010.10.041
CHEMBL306077 102438 1 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 240 6 3 2 2.0 CC(C)/N=C(\S)NCCCCc1c[nH]cn1 10.1016/j.bmcl.2010.10.041
25128823 192115 0 None - 1 Rat 7.7 pEC50 = 7.7 Functional
Antagonist activity at rat histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assayAntagonist activity at rat histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assay
ChEMBL 267 1 2 5 1.0 Nc1nc2c(c(N3CCNCC3)n1)Cc1ccccc1-2 10.1021/jm800670r
CHEMBL521995 192115 0 None - 1 Rat 7.7 pEC50 = 7.7 Functional
Antagonist activity at rat histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assayAntagonist activity at rat histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assay
ChEMBL 267 1 2 5 1.0 Nc1nc2c(c(N3CCNCC3)n1)Cc1ccccc1-2 10.1021/jm800670r
25131230 192507 0 None - 1 Rat 6.7 pEC50 = 6.7 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 329 4 1 7 1.5 COc1cccc(OC)c1-c1cc(N2CCN(C)CC2)nc(N)n1 10.1021/jm8005959
CHEMBL522679 192507 0 None - 1 Rat 6.7 pEC50 = 6.7 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 329 4 1 7 1.5 COc1cccc(OC)c1-c1cc(N2CCN(C)CC2)nc(N)n1 10.1021/jm8005959
10037650 5138 0 None 47 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 248 3 3 4 0.3 C/N=C(\NC#N)NC[C@@H]1CC[C@H](c2c[nH]cn2)O1 10.1016/j.bmcl.2010.10.041
CHEMBL106158 5138 0 None 47 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 248 3 3 4 0.3 C/N=C(\NC#N)NC[C@@H]1CC[C@H](c2c[nH]cn2)O1 10.1016/j.bmcl.2010.10.041
170389 205253 31 None -4 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 125 3 2 2 0.3 NCCCc1c[nH]cn1 10.1016/j.bmcl.2010.10.041
CHEMBL4634086 205253 31 None -4 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 125 3 2 2 0.3 NCCCc1c[nH]cn1 10.1016/j.bmcl.2010.10.041
CHEMBL91353 205253 31 None -4 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 125 3 2 2 0.3 NCCCc1c[nH]cn1 10.1016/j.bmcl.2010.10.041
155513612 175746 0 None -14 3 Mouse 6.7 pEC50 = 6.7 Functional
Agonist activity at mouse H4R expressed in HEK293T cells by CRE-luciferase reporter gene assayAgonist activity at mouse H4R expressed in HEK293T cells by CRE-luciferase reporter gene assay
ChEMBL 277 4 1 5 2.1 CN(C)[C@@H]1CCN(c2ccnc(NCC(C)(C)C)n2)C1 10.1021/acs.jmedchem.9b01342
CHEMBL4439142 175746 0 None -14 3 Mouse 6.7 pEC50 = 6.7 Functional
Agonist activity at mouse H4R expressed in HEK293T cells by CRE-luciferase reporter gene assayAgonist activity at mouse H4R expressed in HEK293T cells by CRE-luciferase reporter gene assay
ChEMBL 277 4 1 5 2.1 CN(C)[C@@H]1CCN(c2ccnc(NCC(C)(C)C)n2)C1 10.1021/acs.jmedchem.9b01342
CHEMBL4515149 175746 0 None -14 3 Mouse 6.7 pEC50 = 6.7 Functional
Agonist activity at mouse H4R expressed in HEK293T cells by CRE-luciferase reporter gene assayAgonist activity at mouse H4R expressed in HEK293T cells by CRE-luciferase reporter gene assay
ChEMBL 277 4 1 5 2.1 CN(C)[C@@H]1CCN(c2ccnc(NCC(C)(C)C)n2)C1 10.1021/acs.jmedchem.9b01342
CHEMBL4595327 175746 0 None -14 3 Mouse 6.7 pEC50 = 6.7 Functional
Agonist activity at mouse H4R expressed in HEK293T cells by CRE-luciferase reporter gene assayAgonist activity at mouse H4R expressed in HEK293T cells by CRE-luciferase reporter gene assay
ChEMBL 277 4 1 5 2.1 CN(C)[C@@H]1CCN(c2ccnc(NCC(C)(C)C)n2)C1 10.1021/acs.jmedchem.9b01342
136141537 56187 1 None -1 3 Mouse 6.7 pEC50 = 6.7 Functional
Agonist activity at mouse histamine H4 receptor by luciferase reporter gene assayAgonist activity at mouse histamine H4 receptor by luciferase reporter gene assay
ChEMBL 271 2 2 3 3.0 Cc1ccc2[nH]c(/C(=N\O)C3CCN(C)CC3)cc2c1 10.1016/j.bmcl.2010.10.041
CHEMBL1632412 56187 1 None -1 3 Mouse 6.7 pEC50 = 6.7 Functional
Agonist activity at mouse histamine H4 receptor by luciferase reporter gene assayAgonist activity at mouse histamine H4 receptor by luciferase reporter gene assay
ChEMBL 271 2 2 3 3.0 Cc1ccc2[nH]c(/C(=N\O)C3CCN(C)CC3)cc2c1 10.1016/j.bmcl.2010.10.041
136192874 56189 0 None -3 3 Rat 6.7 pEC50 = 6.7 Functional
Agonist activity at rat histamine H4 receptor by luciferase reporter gene assayAgonist activity at rat histamine H4 receptor by luciferase reporter gene assay
ChEMBL 292 2 2 4 2.7 CN1CCC(/C(=N/O)c2nc3cc(Cl)ccc3[nH]2)CC1 10.1016/j.bmcl.2010.10.041
CHEMBL1632414 56189 0 None -3 3 Rat 6.7 pEC50 = 6.7 Functional
Agonist activity at rat histamine H4 receptor by luciferase reporter gene assayAgonist activity at rat histamine H4 receptor by luciferase reporter gene assay
ChEMBL 292 2 2 4 2.7 CN1CCC(/C(=N/O)c2nc3cc(Cl)ccc3[nH]2)CC1 10.1016/j.bmcl.2010.10.041
46228133 198371 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Inverse agonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of [35S]GTPgammaS bindingInverse agonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 332 4 2 6 2.1 CN1CCN(c2cc(NCc3cccc(Cl)c3)nc(N)n2)CC1 10.1016/j.bmc.2009.08.059
CHEMBL595639 198371 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Inverse agonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of [35S]GTPgammaS bindingInverse agonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 332 4 2 6 2.1 CN1CCN(c2cc(NCc3cccc(Cl)c3)nc(N)n2)CC1 10.1016/j.bmc.2009.08.059
10197870 5229 0 None -47 2 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 167 2 2 3 0.6 NC[C@H]1CC[C@H](c2c[nH]cn2)O1 10.1016/j.bmcl.2010.10.041
CHEMBL106612 5229 0 None -47 2 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 167 2 2 3 0.6 NC[C@H]1CC[C@H](c2c[nH]cn2)O1 10.1016/j.bmcl.2010.10.041
10197870 5229 0 None -47 2 Human 5.7 pEC50 = 5.7 Functional
Inhibition of the forskolin-stimulated cAMP production in SK-N-MC cells expressing human Histamine H4 receptorInhibition of the forskolin-stimulated cAMP production in SK-N-MC cells expressing human Histamine H4 receptor
ChEMBL 167 2 2 3 0.6 NC[C@H]1CC[C@H](c2c[nH]cn2)O1 10.1021/jm0300025
CHEMBL106612 5229 0 None -47 2 Human 5.7 pEC50 = 5.7 Functional
Inhibition of the forskolin-stimulated cAMP production in SK-N-MC cells expressing human Histamine H4 receptorInhibition of the forskolin-stimulated cAMP production in SK-N-MC cells expressing human Histamine H4 receptor
ChEMBL 167 2 2 3 0.6 NC[C@H]1CC[C@H](c2c[nH]cn2)O1 10.1021/jm0300025
10879463 5218 0 None - 1 Human 4.7 pEC50 = 4.7 Functional
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 248 3 3 4 0.3 C/N=C(\NC#N)NC[C@@H]1CC[C@@H](c2c[nH]cn2)O1 10.1016/j.bmcl.2010.10.041
CHEMBL106570 5218 0 None - 1 Human 4.7 pEC50 = 4.7 Functional
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 248 3 3 4 0.3 C/N=C(\NC#N)NC[C@@H]1CC[C@@H](c2c[nH]cn2)O1 10.1016/j.bmcl.2010.10.041
1278 2119 79 None -1 4 Mouse 8.6 pEC50 = 8.6 Functional
Antagonist activity at mouse histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assayAntagonist activity at mouse histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assay
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/jm800670r
1279 2119 79 None -1 4 Mouse 8.6 pEC50 = 8.6 Functional
Antagonist activity at mouse histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assayAntagonist activity at mouse histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assay
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/jm800670r
4908365 2119 79 None -1 4 Mouse 8.6 pEC50 = 8.6 Functional
Antagonist activity at mouse histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assayAntagonist activity at mouse histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assay
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/jm800670r
CHEMBL129198 2119 79 None -1 4 Mouse 8.6 pEC50 = 8.6 Functional
Antagonist activity at mouse histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assayAntagonist activity at mouse histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assay
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/jm800670r
1278 2119 79 None -1 4 Rat 8.6 pEC50 = 8.6 Functional
Antagonist activity at rat histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assayAntagonist activity at rat histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assay
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/jm800670r
1279 2119 79 None -1 4 Rat 8.6 pEC50 = 8.6 Functional
Antagonist activity at rat histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assayAntagonist activity at rat histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assay
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/jm800670r
4908365 2119 79 None -1 4 Rat 8.6 pEC50 = 8.6 Functional
Antagonist activity at rat histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assayAntagonist activity at rat histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assay
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/jm800670r
CHEMBL129198 2119 79 None -1 4 Rat 8.6 pEC50 = 8.6 Functional
Antagonist activity at rat histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assayAntagonist activity at rat histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assay
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/jm800670r
58227260 116630 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human recombinant histamine H4 receptor expressed in SK-N-MC cells assessed as effect on forskolin-stimulated cAMP-mediated reporter gene activityAgonist activity at human recombinant histamine H4 receptor expressed in SK-N-MC cells assessed as effect on forskolin-stimulated cAMP-mediated reporter gene activity
ChEMBL 287 3 1 5 1.8 CN1CCN(c2ccnc(NC3CC4CCC3C4)n2)CC1 10.1016/j.bmcl.2014.12.027
CHEMBL3393546 116630 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human recombinant histamine H4 receptor expressed in SK-N-MC cells assessed as effect on forskolin-stimulated cAMP-mediated reporter gene activityAgonist activity at human recombinant histamine H4 receptor expressed in SK-N-MC cells assessed as effect on forskolin-stimulated cAMP-mediated reporter gene activity
ChEMBL 287 3 1 5 1.8 CN1CCN(c2ccnc(NC3CC4CCC3C4)n2)CC1 10.1016/j.bmcl.2014.12.027
11846636 77598 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Activity at human histamine H4 receptor transfected in SK-N-MC cells by cAMP assayActivity at human histamine H4 receptor transfected in SK-N-MC cells by cAMP assay
ChEMBL 345 0 0 4 3.9 CN1CCN(C2=Nc3ccc(Cl)cc3Oc3c(F)cccc32)CC1 10.1021/jm051008s
CHEMBL209628 77598 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Activity at human histamine H4 receptor transfected in SK-N-MC cells by cAMP assayActivity at human histamine H4 receptor transfected in SK-N-MC cells by cAMP assay
ChEMBL 345 0 0 4 3.9 CN1CCN(C2=Nc3ccc(Cl)cc3Oc3c(F)cccc32)CC1 10.1021/jm051008s
1204 1901 114 None -1 10 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human recombinant histamine H4 receptor-RGS19 fusion protein expressed in Sf9 cells coexpressing Galphai2,Gbeta1gamma2 assessed as [35S]GTPgammaS binding after 90 mins by liquid scintillation countingAgonist activity at human recombinant histamine H4 receptor-RGS19 fusion protein expressed in Sf9 cells coexpressing Galphai2,Gbeta1gamma2 assessed as [35S]GTPgammaS binding after 90 mins by liquid scintillation counting
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1039/C3MD00245D
1247 1901 114 None -1 10 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human recombinant histamine H4 receptor-RGS19 fusion protein expressed in Sf9 cells coexpressing Galphai2,Gbeta1gamma2 assessed as [35S]GTPgammaS binding after 90 mins by liquid scintillation countingAgonist activity at human recombinant histamine H4 receptor-RGS19 fusion protein expressed in Sf9 cells coexpressing Galphai2,Gbeta1gamma2 assessed as [35S]GTPgammaS binding after 90 mins by liquid scintillation counting
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1039/C3MD00245D
1375 1901 114 None -1 10 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human recombinant histamine H4 receptor-RGS19 fusion protein expressed in Sf9 cells coexpressing Galphai2,Gbeta1gamma2 assessed as [35S]GTPgammaS binding after 90 mins by liquid scintillation countingAgonist activity at human recombinant histamine H4 receptor-RGS19 fusion protein expressed in Sf9 cells coexpressing Galphai2,Gbeta1gamma2 assessed as [35S]GTPgammaS binding after 90 mins by liquid scintillation counting
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1039/C3MD00245D
774 1901 114 None -1 10 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human recombinant histamine H4 receptor-RGS19 fusion protein expressed in Sf9 cells coexpressing Galphai2,Gbeta1gamma2 assessed as [35S]GTPgammaS binding after 90 mins by liquid scintillation countingAgonist activity at human recombinant histamine H4 receptor-RGS19 fusion protein expressed in Sf9 cells coexpressing Galphai2,Gbeta1gamma2 assessed as [35S]GTPgammaS binding after 90 mins by liquid scintillation counting
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1039/C3MD00245D
CHEMBL90 1901 114 None -1 10 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human recombinant histamine H4 receptor-RGS19 fusion protein expressed in Sf9 cells coexpressing Galphai2,Gbeta1gamma2 assessed as [35S]GTPgammaS binding after 90 mins by liquid scintillation countingAgonist activity at human recombinant histamine H4 receptor-RGS19 fusion protein expressed in Sf9 cells coexpressing Galphai2,Gbeta1gamma2 assessed as [35S]GTPgammaS binding after 90 mins by liquid scintillation counting
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1039/C3MD00245D
DB05381 1901 114 None -1 10 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human recombinant histamine H4 receptor-RGS19 fusion protein expressed in Sf9 cells coexpressing Galphai2,Gbeta1gamma2 assessed as [35S]GTPgammaS binding after 90 mins by liquid scintillation countingAgonist activity at human recombinant histamine H4 receptor-RGS19 fusion protein expressed in Sf9 cells coexpressing Galphai2,Gbeta1gamma2 assessed as [35S]GTPgammaS binding after 90 mins by liquid scintillation counting
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1039/C3MD00245D
16061961 197997 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 316 4 2 6 1.6 CN1CCN(c2cc(NCc3ccc(F)cc3)nc(N)n2)CC1 10.1016/j.bmc.2009.08.059
CHEMBL593103 197997 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 316 4 2 6 1.6 CN1CCN(c2cc(NCc3ccc(F)cc3)nc(N)n2)CC1 10.1016/j.bmc.2009.08.059
1204 1901 114 None -1 10 Human 7.7 pEC50 = 7.7 Functional
Inhibition of the forskolin-stimulated cAMP production in SK-N-MC cells expressing human Histamine H4 receptorInhibition of the forskolin-stimulated cAMP production in SK-N-MC cells expressing human Histamine H4 receptor
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm0300025
1247 1901 114 None -1 10 Human 7.7 pEC50 = 7.7 Functional
Inhibition of the forskolin-stimulated cAMP production in SK-N-MC cells expressing human Histamine H4 receptorInhibition of the forskolin-stimulated cAMP production in SK-N-MC cells expressing human Histamine H4 receptor
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm0300025
1375 1901 114 None -1 10 Human 7.7 pEC50 = 7.7 Functional
Inhibition of the forskolin-stimulated cAMP production in SK-N-MC cells expressing human Histamine H4 receptorInhibition of the forskolin-stimulated cAMP production in SK-N-MC cells expressing human Histamine H4 receptor
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm0300025
774 1901 114 None -1 10 Human 7.7 pEC50 = 7.7 Functional
Inhibition of the forskolin-stimulated cAMP production in SK-N-MC cells expressing human Histamine H4 receptorInhibition of the forskolin-stimulated cAMP production in SK-N-MC cells expressing human Histamine H4 receptor
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm0300025
CHEMBL90 1901 114 None -1 10 Human 7.7 pEC50 = 7.7 Functional
Inhibition of the forskolin-stimulated cAMP production in SK-N-MC cells expressing human Histamine H4 receptorInhibition of the forskolin-stimulated cAMP production in SK-N-MC cells expressing human Histamine H4 receptor
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm0300025
DB05381 1901 114 None -1 10 Human 7.7 pEC50 = 7.7 Functional
Inhibition of the forskolin-stimulated cAMP production in SK-N-MC cells expressing human Histamine H4 receptorInhibition of the forskolin-stimulated cAMP production in SK-N-MC cells expressing human Histamine H4 receptor
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm0300025
127052635 139677 0 None 4 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human histamine H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assayAgonist activity at human histamine H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 288 5 3 3 2.0 CC(C)CN/C(=N/C#N)NC[C@@H]1CC[C@H](c2c[nH]cn2)C1 10.1021/acs.jmedchem.6b00120
CHEMBL3805003 139677 0 None 4 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human histamine H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assayAgonist activity at human histamine H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 288 5 3 3 2.0 CC(C)CN/C(=N/C#N)NC[C@@H]1CC[C@H](c2c[nH]cn2)C1 10.1021/acs.jmedchem.6b00120
25130237 186699 2 None - 1 Rat 5.7 pEC50 = 5.7 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 319 1 1 5 0.4 CN1CCN(c2cc(I)nc(N)n2)CC1 10.1021/jm8005959
CHEMBL492864 186699 2 None - 1 Rat 5.7 pEC50 = 5.7 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 319 1 1 5 0.4 CN1CCN(c2cc(I)nc(N)n2)CC1 10.1021/jm8005959
127051301 139670 0 None 4 3 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human histamine H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assayAgonist activity at human histamine H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 246 3 3 3 0.9 CN/C(=N\C#N)NC[C@H]1CC[C@H](c2c[nH]cn2)C1 10.1021/acs.jmedchem.6b00120
CHEMBL3804906 139670 0 None 4 3 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human histamine H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assayAgonist activity at human histamine H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 246 3 3 3 0.9 CN/C(=N\C#N)NC[C@H]1CC[C@H](c2c[nH]cn2)C1 10.1021/acs.jmedchem.6b00120
25131555 186596 0 None - 1 Rat 6.7 pEC50 = 6.7 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 270 2 1 6 0.9 CN1CCN(c2cc(-c3cccnc3)nc(N)n2)CC1 10.1021/jm8005959
CHEMBL492227 186596 0 None - 1 Rat 6.7 pEC50 = 6.7 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 270 2 1 6 0.9 CN1CCN(c2cc(-c3cccnc3)nc(N)n2)CC1 10.1021/jm8005959
25130914 186671 0 None 15 2 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 298 4 2 6 1.4 CN1CCN(c2cc(NCc3ccccc3)nc(N)n2)CC1 10.1016/j.bmc.2009.08.059
CHEMBL492677 186671 0 None 15 2 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 298 4 2 6 1.4 CN1CCN(c2cc(NCc3ccccc3)nc(N)n2)CC1 10.1016/j.bmc.2009.08.059
10879463 5218 0 None - 1 Human 4.7 pEC50 = 4.7 Functional
Inhibition of the forskolin-stimulated cAMP production in SK-N-MC cells expressing human Histamine H4 receptorInhibition of the forskolin-stimulated cAMP production in SK-N-MC cells expressing human Histamine H4 receptor
ChEMBL 248 3 3 4 0.3 C/N=C(\NC#N)NC[C@@H]1CC[C@@H](c2c[nH]cn2)O1 10.1021/jm0300025
CHEMBL106570 5218 0 None - 1 Human 4.7 pEC50 = 4.7 Functional
Inhibition of the forskolin-stimulated cAMP production in SK-N-MC cells expressing human Histamine H4 receptorInhibition of the forskolin-stimulated cAMP production in SK-N-MC cells expressing human Histamine H4 receptor
ChEMBL 248 3 3 4 0.3 C/N=C(\NC#N)NC[C@@H]1CC[C@@H](c2c[nH]cn2)O1 10.1021/jm0300025
1613 2316 44 None -16 8 Human 6.7 pEC50 = 6.7 Functional
Activity at human histamine H4 receptor transfected in SK-N-MC cells by cAMP assayActivity at human histamine H4 receptor transfected in SK-N-MC cells by cAMP assay
ChEMBL 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 10.1021/jm051008s
205 2316 44 None -16 8 Human 6.7 pEC50 = 6.7 Functional
Activity at human histamine H4 receptor transfected in SK-N-MC cells by cAMP assayActivity at human histamine H4 receptor transfected in SK-N-MC cells by cAMP assay
ChEMBL 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 10.1021/jm051008s
3964 2316 44 None -16 8 Human 6.7 pEC50 = 6.7 Functional
Activity at human histamine H4 receptor transfected in SK-N-MC cells by cAMP assayActivity at human histamine H4 receptor transfected in SK-N-MC cells by cAMP assay
ChEMBL 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 10.1021/jm051008s
CHEMBL831 2316 44 None -16 8 Human 6.7 pEC50 = 6.7 Functional
Activity at human histamine H4 receptor transfected in SK-N-MC cells by cAMP assayActivity at human histamine H4 receptor transfected in SK-N-MC cells by cAMP assay
ChEMBL 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 10.1021/jm051008s
DB00408 2316 44 None -16 8 Human 6.7 pEC50 = 6.7 Functional
Activity at human histamine H4 receptor transfected in SK-N-MC cells by cAMP assayActivity at human histamine H4 receptor transfected in SK-N-MC cells by cAMP assay
ChEMBL 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 10.1021/jm051008s
753256 178770 10 None - 1 Rat 6.7 pEC50 = 6.7 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 208 1 2 6 -0.6 CN1CCN(c2cc(N)nc(N)n2)CC1 10.1021/jm8005959
CHEMBL473662 178770 10 None - 1 Rat 6.7 pEC50 = 6.7 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 208 1 2 6 -0.6 CN1CCN(c2cc(N)nc(N)n2)CC1 10.1021/jm8005959
25131560 186763 0 None - 1 Rat 6.7 pEC50 = 6.7 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 273 2 1 7 0.2 CN1CCN(c2cc(-c3cnn(C)c3)nc(N)n2)CC1 10.1021/jm8005959
CHEMBL493229 186763 0 None - 1 Rat 6.7 pEC50 = 6.7 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 273 2 1 7 0.2 CN1CCN(c2cc(-c3cnn(C)c3)nc(N)n2)CC1 10.1021/jm8005959
1223 940 32 None -21 4 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human H4R by [35S]-GTPgammaS-binding assayAgonist activity at human H4R by [35S]-GTPgammaS-binding assay
ChEMBL 308 6 2 3 3.2 Clc1ccc(cc1)CN=C(SCCCc1cnc[nH]1)N 10.1021/acs.jmedchem.9b01342
2790 940 32 None -21 4 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human H4R by [35S]-GTPgammaS-binding assayAgonist activity at human H4R by [35S]-GTPgammaS-binding assay
ChEMBL 308 6 2 3 3.2 Clc1ccc(cc1)CN=C(SCCCc1cnc[nH]1)N 10.1021/acs.jmedchem.9b01342
CHEMBL14690 940 32 None -21 4 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human H4R by [35S]-GTPgammaS-binding assayAgonist activity at human H4R by [35S]-GTPgammaS-binding assay
ChEMBL 308 6 2 3 3.2 Clc1ccc(cc1)CN=C(SCCCc1cnc[nH]1)N 10.1021/acs.jmedchem.9b01342
155512725 175667 0 None -1 3 Rat 7.6 pEC50 = 7.6 Functional
Agonist activity at rat H4R expressed in HEK293-SF-rH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at rat H4R expressed in HEK293-SF-rH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 237 6 3 5 1.7 CC(C)(C)CNc1nccc(NCCCN)n1 10.1021/acs.jmedchem.9b01342
CHEMBL4437371 175667 0 None -1 3 Rat 7.6 pEC50 = 7.6 Functional
Agonist activity at rat H4R expressed in HEK293-SF-rH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at rat H4R expressed in HEK293-SF-rH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 237 6 3 5 1.7 CC(C)(C)CNc1nccc(NCCCN)n1 10.1021/acs.jmedchem.9b01342
CHEMBL4594753 175667 0 None -1 3 Rat 7.6 pEC50 = 7.6 Functional
Agonist activity at rat H4R expressed in HEK293-SF-rH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at rat H4R expressed in HEK293-SF-rH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 237 6 3 5 1.7 CC(C)(C)CNc1nccc(NCCCN)n1 10.1021/acs.jmedchem.9b01342
10037650 5138 0 None 47 2 Human 6.7 pEC50 = 6.7 Functional
Inhibition of the forskolin-stimulated cAMP production in SK-N-MC cells expressing human Histamine H4 receptorInhibition of the forskolin-stimulated cAMP production in SK-N-MC cells expressing human Histamine H4 receptor
ChEMBL 248 3 3 4 0.3 C/N=C(\NC#N)NC[C@@H]1CC[C@H](c2c[nH]cn2)O1 10.1021/jm0300025
CHEMBL106158 5138 0 None 47 2 Human 6.7 pEC50 = 6.7 Functional
Inhibition of the forskolin-stimulated cAMP production in SK-N-MC cells expressing human Histamine H4 receptorInhibition of the forskolin-stimulated cAMP production in SK-N-MC cells expressing human Histamine H4 receptor
ChEMBL 248 3 3 4 0.3 C/N=C(\NC#N)NC[C@@H]1CC[C@H](c2c[nH]cn2)O1 10.1021/jm0300025
25129881 186599 4 None - 1 Rat 6.6 pEC50 = 6.6 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 270 2 1 6 0.9 CN1CCN(c2cc(-c3ccncc3)nc(N)n2)CC1 10.1021/jm8005959
CHEMBL492241 186599 4 None - 1 Rat 6.6 pEC50 = 6.6 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 270 2 1 6 0.9 CN1CCN(c2cc(-c3ccncc3)nc(N)n2)CC1 10.1021/jm8005959
44568855 192591 0 None - 1 Rat 5.6 pEC50 = 5.6 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 285 2 1 5 2.0 CC(C)(C)c1cc(N2CCNCC2)nc(-n2cccc2)n1 10.1021/jm8005959
CHEMBL523335 192591 0 None - 1 Rat 5.6 pEC50 = 5.6 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 285 2 1 5 2.0 CC(C)(C)c1cc(N2CCNCC2)nc(-n2cccc2)n1 10.1021/jm8005959
25128832 171446 0 None - 1 Rat 4.6 pEC50 = 4.6 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 250 1 1 5 1.2 CN1CCN(c2cc(C(C)(C)C)nc(O)n2)CC1 10.1021/jm8005959
CHEMBL447151 171446 0 None - 1 Rat 4.6 pEC50 = 4.6 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 250 1 1 5 1.2 CN1CCN(c2cc(C(C)(C)C)nc(O)n2)CC1 10.1021/jm8005959
25071940 186771 0 None - 1 Rat 7.6 pEC50 = 7.6 Functional
Antagonist activity at rat histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assayAntagonist activity at rat histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assay
ChEMBL 281 1 2 5 1.2 Nc1nc2c(c(N3CCNCC3)n1)CCc1ccccc1-2 10.1021/jm800670r
CHEMBL493281 186771 0 None - 1 Rat 7.6 pEC50 = 7.6 Functional
Antagonist activity at rat histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assayAntagonist activity at rat histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assay
ChEMBL 281 1 2 5 1.2 Nc1nc2c(c(N3CCNCC3)n1)CCc1ccccc1-2 10.1021/jm800670r
127049156 139664 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human histamine H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assayAgonist activity at human histamine H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 272 4 3 3 1.5 N#C/N=C(\NC[C@H]1CC[C@H](c2c[nH]cn2)C1)NC1CC1 10.1021/acs.jmedchem.6b00120
CHEMBL3804837 139664 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human histamine H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assayAgonist activity at human histamine H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 272 4 3 3 1.5 N#C/N=C(\NC[C@H]1CC[C@H](c2c[nH]cn2)C1)NC1CC1 10.1021/acs.jmedchem.6b00120
11437850 187078 1 None - 1 Rat 6.6 pEC50 = 6.6 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 294 2 1 6 1.3 CN1CCN(c2cc(-c3cccc(C#N)c3)nc(N)n2)CC1 10.1021/jm8005959
CHEMBL495082 187078 1 None - 1 Rat 6.6 pEC50 = 6.6 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 294 2 1 6 1.3 CN1CCN(c2cc(-c3cccc(C#N)c3)nc(N)n2)CC1 10.1021/jm8005959
25129883 192121 0 None - 1 Rat 6.6 pEC50 = 6.6 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 300 3 1 7 0.9 COc1ccncc1-c1cc(N2CCN(C)CC2)nc(N)n1 10.1021/jm8005959
CHEMBL522019 192121 0 None - 1 Rat 6.6 pEC50 = 6.6 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 300 3 1 7 0.9 COc1ccncc1-c1cc(N2CCN(C)CC2)nc(N)n1 10.1021/jm8005959
25133972 186767 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at human histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 293 2 1 5 2.0 CN1CCN(c2cc(-c3ccc(C#N)cc3)cc(N)n2)CC1 10.1021/jm8005959
CHEMBL493262 186767 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at human histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 293 2 1 5 2.0 CN1CCN(c2cc(-c3ccc(C#N)cc3)cc(N)n2)CC1 10.1021/jm8005959
25130575 187006 1 None - 1 Rat 4.6 pEC50 = 4.6 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 248 1 1 4 2.6 CC1CCN(c2cc(C(C)(C)C)nc(N)n2)CC1 10.1021/jm8005959
CHEMBL494687 187006 1 None - 1 Rat 4.6 pEC50 = 4.6 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 248 1 1 4 2.6 CC1CCN(c2cc(C(C)(C)C)nc(N)n2)CC1 10.1021/jm8005959
25130577 172029 0 None - 1 Rat 5.6 pEC50 = 5.6 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 306 4 1 6 1.0 CN(C)CCN1CCN(c2cc(C(C)(C)C)nc(N)n2)CC1 10.1021/jm8005959
CHEMBL449021 172029 0 None - 1 Rat 5.6 pEC50 = 5.6 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 306 4 1 6 1.0 CN(C)CCN1CCN(c2cc(C(C)(C)C)nc(N)n2)CC1 10.1021/jm8005959
10773349 8007 1 None -89 2 Human 4.6 pEC50 = 4.6 Functional
Inhibition of the forskolin-stimulated cAMP production in SK-N-MC cells expressing human Histamine H4 receptorInhibition of the forskolin-stimulated cAMP production in SK-N-MC cells expressing human Histamine H4 receptor
ChEMBL 165 2 2 3 0.4 NC[C@H]1C=C[C@H](c2c[nH]cn2)O1 10.1021/jm0300025
CHEMBL109130 8007 1 None -89 2 Human 4.6 pEC50 = 4.6 Functional
Inhibition of the forskolin-stimulated cAMP production in SK-N-MC cells expressing human Histamine H4 receptorInhibition of the forskolin-stimulated cAMP production in SK-N-MC cells expressing human Histamine H4 receptor
ChEMBL 165 2 2 3 0.4 NC[C@H]1C=C[C@H](c2c[nH]cn2)O1 10.1021/jm0300025
127052634 139779 0 None 6 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human histamine H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assayAgonist activity at human histamine H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 272 4 3 3 1.5 N#C/N=C(\NC[C@@H]1CC[C@H](c2c[nH]cn2)C1)NC1CC1 10.1021/acs.jmedchem.6b00120
CHEMBL3806146 139779 0 None 6 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human histamine H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assayAgonist activity at human histamine H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 272 4 3 3 1.5 N#C/N=C(\NC[C@@H]1CC[C@H](c2c[nH]cn2)C1)NC1CC1 10.1021/acs.jmedchem.6b00120
90667240 108991 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human recombinant histamine H4 receptor-RGS19 fusion protein expressed in Sf9 cells coexpressing Galphai2,Gbeta1gamma2 assessed as [35S]GTPgammaS binding after 90 mins by liquid scintillation countingAgonist activity at human recombinant histamine H4 receptor-RGS19 fusion protein expressed in Sf9 cells coexpressing Galphai2,Gbeta1gamma2 assessed as [35S]GTPgammaS binding after 90 mins by liquid scintillation counting
ChEMBL 356 9 3 4 2.8 Cc1[nH]cnc1CCCCN/C(=N\C#N)NCCSc1ccccc1 10.1039/C3MD00245D
CHEMBL3220642 108991 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human recombinant histamine H4 receptor-RGS19 fusion protein expressed in Sf9 cells coexpressing Galphai2,Gbeta1gamma2 assessed as [35S]GTPgammaS binding after 90 mins by liquid scintillation countingAgonist activity at human recombinant histamine H4 receptor-RGS19 fusion protein expressed in Sf9 cells coexpressing Galphai2,Gbeta1gamma2 assessed as [35S]GTPgammaS binding after 90 mins by liquid scintillation counting
ChEMBL 356 9 3 4 2.8 Cc1[nH]cnc1CCCCN/C(=N\C#N)NCCSc1ccccc1 10.1039/C3MD00245D
25130576 187043 1 None -2 2 Rat 6.6 pEC50 = 6.6 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 280 2 2 6 1.0 N#Cc1ccc(-c2cc(N3CCNCC3)nc(N)n2)cc1 10.1021/jm8005959
CHEMBL494890 187043 1 None -2 2 Rat 6.6 pEC50 = 6.6 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 280 2 2 6 1.0 N#Cc1ccc(-c2cc(N3CCNCC3)nc(N)n2)cc1 10.1021/jm8005959
25128826 188229 0 None - 1 Rat 6.6 pEC50 = 6.6 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 263 2 1 5 1.5 CCN1CCN(c2cc(C(C)(C)C)nc(N)n2)CC1 10.1021/jm8005959
CHEMBL506187 188229 0 None - 1 Rat 6.6 pEC50 = 6.6 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 263 2 1 5 1.5 CCN1CCN(c2cc(C(C)(C)C)nc(N)n2)CC1 10.1021/jm8005959
25130576 187043 1 None -2 2 Rat 6.6 pEC50 = 6.6 Functional
Antagonist activity at rat histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assayAntagonist activity at rat histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assay
ChEMBL 280 2 2 6 1.0 N#Cc1ccc(-c2cc(N3CCNCC3)nc(N)n2)cc1 10.1021/jm800670r
CHEMBL494890 187043 1 None -2 2 Rat 6.6 pEC50 = 6.6 Functional
Antagonist activity at rat histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assayAntagonist activity at rat histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assay
ChEMBL 280 2 2 6 1.0 N#Cc1ccc(-c2cc(N3CCNCC3)nc(N)n2)cc1 10.1021/jm800670r
58227157 115417 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human recombinant histamine H4 receptor expressed in SK-N-MC cells assessed as effect on forskolin-stimulated cAMP-mediated reporter gene activityAgonist activity at human recombinant histamine H4 receptor expressed in SK-N-MC cells assessed as effect on forskolin-stimulated cAMP-mediated reporter gene activity
ChEMBL 235 4 2 5 1.1 CN[C@@H]1CCN(c2ccnc(NC(C)C)n2)C1 10.1016/j.bmcl.2014.12.027
CHEMBL3354815 115417 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human recombinant histamine H4 receptor expressed in SK-N-MC cells assessed as effect on forskolin-stimulated cAMP-mediated reporter gene activityAgonist activity at human recombinant histamine H4 receptor expressed in SK-N-MC cells assessed as effect on forskolin-stimulated cAMP-mediated reporter gene activity
ChEMBL 235 4 2 5 1.1 CN[C@@H]1CCN(c2ccnc(NC(C)C)n2)C1 10.1016/j.bmcl.2014.12.027
1204 1901 114 None -1 10 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human histamine H4 receptor expressed in HEK293 cells assessed by forskolin induced cAMP response element activation by luciferase reporter gene assayAgonist activity at human histamine H4 receptor expressed in HEK293 cells assessed by forskolin induced cAMP response element activation by luciferase reporter gene assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm1013488
1247 1901 114 None -1 10 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human histamine H4 receptor expressed in HEK293 cells assessed by forskolin induced cAMP response element activation by luciferase reporter gene assayAgonist activity at human histamine H4 receptor expressed in HEK293 cells assessed by forskolin induced cAMP response element activation by luciferase reporter gene assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm1013488
1375 1901 114 None -1 10 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human histamine H4 receptor expressed in HEK293 cells assessed by forskolin induced cAMP response element activation by luciferase reporter gene assayAgonist activity at human histamine H4 receptor expressed in HEK293 cells assessed by forskolin induced cAMP response element activation by luciferase reporter gene assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm1013488
774 1901 114 None -1 10 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human histamine H4 receptor expressed in HEK293 cells assessed by forskolin induced cAMP response element activation by luciferase reporter gene assayAgonist activity at human histamine H4 receptor expressed in HEK293 cells assessed by forskolin induced cAMP response element activation by luciferase reporter gene assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm1013488
CHEMBL90 1901 114 None -1 10 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human histamine H4 receptor expressed in HEK293 cells assessed by forskolin induced cAMP response element activation by luciferase reporter gene assayAgonist activity at human histamine H4 receptor expressed in HEK293 cells assessed by forskolin induced cAMP response element activation by luciferase reporter gene assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm1013488
DB05381 1901 114 None -1 10 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human histamine H4 receptor expressed in HEK293 cells assessed by forskolin induced cAMP response element activation by luciferase reporter gene assayAgonist activity at human histamine H4 receptor expressed in HEK293 cells assessed by forskolin induced cAMP response element activation by luciferase reporter gene assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm1013488
1226 1988 16 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 321 9 4 4 1.2 NC(=NCCCc1cnc[nH]1)NCCSCc1nc[nH]c1C 10.1016/j.bmcl.2010.10.041
41376 1988 16 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 321 9 4 4 1.2 NC(=NCCCc1cnc[nH]1)NCCSCc1nc[nH]c1C 10.1016/j.bmcl.2010.10.041
CHEMBL12608 1988 16 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 321 9 4 4 1.2 NC(=NCCCc1cnc[nH]1)NCCSCc1nc[nH]c1C 10.1016/j.bmcl.2010.10.041
25133970 187005 2 None - 1 Rat 6.6 pEC50 = 6.6 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 250 1 1 6 0.5 CN1CCN(c2nc(N)nc(C(C)(C)C)n2)CC1 10.1021/jm8005959
CHEMBL494679 187005 2 None - 1 Rat 6.6 pEC50 = 6.6 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 250 1 1 6 0.5 CN1CCN(c2nc(N)nc(C(C)(C)C)n2)CC1 10.1021/jm8005959
25130230 171889 2 None 3 2 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at human histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 259 2 1 7 -0.0 CN1CCN(c2cc(-n3ccnc3)nc(N)n2)CC1 10.1021/jm8005959
CHEMBL448085 171889 2 None 3 2 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at human histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 259 2 1 7 -0.0 CN1CCN(c2cc(-n3ccnc3)nc(N)n2)CC1 10.1021/jm8005959
1269 121 33 None -56 6 Rat 5.6 pEC50 = 5.6 Functional
Agonist activity at rat histamine H4 receptorAgonist activity at rat histamine H4 receptor
ChEMBL 125 2 2 2 0.2 Cc1c(CCN)nc[nH]1 10.1016/j.bmcl.2010.10.041
37463 121 33 None -56 6 Rat 5.6 pEC50 = 5.6 Functional
Agonist activity at rat histamine H4 receptorAgonist activity at rat histamine H4 receptor
ChEMBL 125 2 2 2 0.2 Cc1c(CCN)nc[nH]1 10.1016/j.bmcl.2010.10.041
CHEMBL275443 121 33 None -56 6 Rat 5.6 pEC50 = 5.6 Functional
Agonist activity at rat histamine H4 receptorAgonist activity at rat histamine H4 receptor
ChEMBL 125 2 2 2 0.2 Cc1c(CCN)nc[nH]1 10.1016/j.bmcl.2010.10.041
44480958 5597 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19 protein by steady-state GTPase assayAgonist activity at human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19 protein by steady-state GTPase assay
ChEMBL 325 9 3 4 1.8 N#C/N=C(/NCCCCc1c[nH]cn1)NCCCc1ccncc1 10.1021/jm900526h
CHEMBL1077859 5597 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19 protein by steady-state GTPase assayAgonist activity at human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19 protein by steady-state GTPase assay
ChEMBL 325 9 3 4 1.8 N#C/N=C(/NCCCCc1c[nH]cn1)NCCCc1ccncc1 10.1021/jm900526h
25131556 188284 7 None 3 2 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at human histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 300 3 1 7 0.9 COc1ncccc1-c1cc(N2CCN(C)CC2)nc(N)n1 10.1021/jm8005959
CHEMBL507063 188284 7 None 3 2 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at human histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 300 3 1 7 0.9 COc1ncccc1-c1cc(N2CCN(C)CC2)nc(N)n1 10.1021/jm8005959
127051047 139781 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human histamine H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assayAgonist activity at human histamine H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 246 3 3 3 0.9 CN/C(=N\C#N)NC[C@H]1CC[C@@H](c2c[nH]cn2)C1 10.1021/acs.jmedchem.6b00120
CHEMBL3806162 139781 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human histamine H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assayAgonist activity at human histamine H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 246 3 3 3 0.9 CN/C(=N\C#N)NC[C@H]1CC[C@@H](c2c[nH]cn2)C1 10.1021/acs.jmedchem.6b00120
45257134 198261 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Inverse agonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of [35S]GTPgammaS bindingInverse agonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 312 4 2 6 1.7 Cc1cccc(CNc2cc(N3CCN(C)CC3)nc(N)n2)c1 10.1016/j.bmc.2009.08.059
CHEMBL594949 198261 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Inverse agonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of [35S]GTPgammaS bindingInverse agonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 312 4 2 6 1.7 Cc1cccc(CNc2cc(N3CCN(C)CC3)nc(N)n2)c1 10.1016/j.bmc.2009.08.059
25131231 186604 0 None - 1 Rat 6.6 pEC50 = 6.6 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 395 2 1 5 2.1 CN1CCN(c2cc(-c3ccc(I)cc3)nc(N)n2)CC1 10.1021/jm8005959
CHEMBL492288 186604 0 None - 1 Rat 6.6 pEC50 = 6.6 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 395 2 1 5 2.1 CN1CCN(c2cc(-c3ccc(I)cc3)nc(N)n2)CC1 10.1021/jm8005959
10381810 203463 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Activity at human histamine H4 receptor transfected in SK-N-MC cells by cAMP assayActivity at human histamine H4 receptor transfected in SK-N-MC cells by cAMP assay
ChEMBL 327 0 0 4 3.8 CN1CCN(C2=Nc3cc(Cl)ccc3Oc3ccccc32)CC1 10.1021/jm051008s
CHEMBL7828 203463 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Activity at human histamine H4 receptor transfected in SK-N-MC cells by cAMP assayActivity at human histamine H4 receptor transfected in SK-N-MC cells by cAMP assay
ChEMBL 327 0 0 4 3.8 CN1CCN(C2=Nc3cc(Cl)ccc3Oc3ccccc32)CC1 10.1021/jm051008s
155512725 175667 0 None 1 3 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 237 6 3 5 1.7 CC(C)(C)CNc1nccc(NCCCN)n1 10.1021/acs.jmedchem.9b01342
CHEMBL4437371 175667 0 None 1 3 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 237 6 3 5 1.7 CC(C)(C)CNc1nccc(NCCCN)n1 10.1021/acs.jmedchem.9b01342
CHEMBL4594753 175667 0 None 1 3 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 237 6 3 5 1.7 CC(C)(C)CNc1nccc(NCCCN)n1 10.1021/acs.jmedchem.9b01342
127052294 139772 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human histamine H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assayAgonist activity at human histamine H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 368 7 3 4 3.1 N#C/N=C(/NCCSc1ccccc1)NC[C@@H]1CC[C@H](c2c[nH]cn2)C1 10.1021/acs.jmedchem.6b00120
CHEMBL3806079 139772 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human histamine H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assayAgonist activity at human histamine H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 368 7 3 4 3.1 N#C/N=C(/NCCSc1ccccc1)NC[C@@H]1CC[C@H](c2c[nH]cn2)C1 10.1021/acs.jmedchem.6b00120
1204 1901 114 None -97 10 Rat 6.5 pEC50 = 6.5 Functional
Agonist activity at rat H4R expressed in HEK293-SF-rH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at rat H4R expressed in HEK293-SF-rH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.9b01342
1247 1901 114 None -97 10 Rat 6.5 pEC50 = 6.5 Functional
Agonist activity at rat H4R expressed in HEK293-SF-rH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at rat H4R expressed in HEK293-SF-rH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.9b01342
1375 1901 114 None -97 10 Rat 6.5 pEC50 = 6.5 Functional
Agonist activity at rat H4R expressed in HEK293-SF-rH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at rat H4R expressed in HEK293-SF-rH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.9b01342
774 1901 114 None -97 10 Rat 6.5 pEC50 = 6.5 Functional
Agonist activity at rat H4R expressed in HEK293-SF-rH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at rat H4R expressed in HEK293-SF-rH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.9b01342
CHEMBL90 1901 114 None -97 10 Rat 6.5 pEC50 = 6.5 Functional
Agonist activity at rat H4R expressed in HEK293-SF-rH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at rat H4R expressed in HEK293-SF-rH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.9b01342
DB05381 1901 114 None -97 10 Rat 6.5 pEC50 = 6.5 Functional
Agonist activity at rat H4R expressed in HEK293-SF-rH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at rat H4R expressed in HEK293-SF-rH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.9b01342
25128822 186898 0 None -19 2 Human 6.5 pEC50 = 6.5 Functional
Antagonist activity at human histamine 4 receptor expressed in Sf9 cell membranes co-expressing Galphai2 and Gbeta1gamma2 assessed as [35S]GTPgammaS binding by scintillation countingAntagonist activity at human histamine 4 receptor expressed in Sf9 cell membranes co-expressing Galphai2 and Gbeta1gamma2 assessed as [35S]GTPgammaS binding by scintillation counting
ChEMBL 295 1 1 5 1.6 CN1CCN(c2nc(N)nc3c2CCc2ccccc2-3)CC1 10.1016/j.bmcl.2015.12.035
CHEMBL494093 186898 0 None -19 2 Human 6.5 pEC50 = 6.5 Functional
Antagonist activity at human histamine 4 receptor expressed in Sf9 cell membranes co-expressing Galphai2 and Gbeta1gamma2 assessed as [35S]GTPgammaS binding by scintillation countingAntagonist activity at human histamine 4 receptor expressed in Sf9 cell membranes co-expressing Galphai2 and Gbeta1gamma2 assessed as [35S]GTPgammaS binding by scintillation counting
ChEMBL 295 1 1 5 1.6 CN1CCN(c2nc(N)nc3c2CCc2ccccc2-3)CC1 10.1016/j.bmcl.2015.12.035
155491015 175921 3 None -31 4 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human H4R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by CRE-luciferase reporter gene assayAgonist activity at human H4R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by CRE-luciferase reporter gene assay
ChEMBL 207 4 2 5 0.2 CCCNC1CN(c2ccnc(N)n2)C1 10.1021/acs.jmedchem.9b01462
CHEMBL4441731 175921 3 None -31 4 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human H4R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by CRE-luciferase reporter gene assayAgonist activity at human H4R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by CRE-luciferase reporter gene assay
ChEMBL 207 4 2 5 0.2 CCCNC1CN(c2ccnc(N)n2)C1 10.1021/acs.jmedchem.9b01462
CHEMBL4596734 175921 3 None -31 4 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human H4R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by CRE-luciferase reporter gene assayAgonist activity at human H4R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by CRE-luciferase reporter gene assay
ChEMBL 207 4 2 5 0.2 CCCNC1CN(c2ccnc(N)n2)C1 10.1021/acs.jmedchem.9b01462
46890072 6832 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human histamine H4 receptor in SK-N-MC cells assessed as forskolin-stimulated cAMP release preincubated for 10 mins before forskolin challengeAgonist activity at human histamine H4 receptor in SK-N-MC cells assessed as forskolin-stimulated cAMP release preincubated for 10 mins before forskolin challenge
ChEMBL 404 8 2 4 4.9 Cc1cc(OCCCNCc2cccnc2)ccc1-c1nc2c(C)c(F)ccc2[nH]1 10.1016/j.bmcl.2010.04.017
CHEMBL1084355 6832 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human histamine H4 receptor in SK-N-MC cells assessed as forskolin-stimulated cAMP release preincubated for 10 mins before forskolin challengeAgonist activity at human histamine H4 receptor in SK-N-MC cells assessed as forskolin-stimulated cAMP release preincubated for 10 mins before forskolin challenge
ChEMBL 404 8 2 4 4.9 Cc1cc(OCCCNCc2cccnc2)ccc1-c1nc2c(C)c(F)ccc2[nH]1 10.1016/j.bmcl.2010.04.017
46890166 7235 0 None 3 4 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human histamine H4 receptor in SK-N-MC cells assessed as forskolin-stimulated cAMP release preincubated for 10 mins before forskolin challengeAgonist activity at human histamine H4 receptor in SK-N-MC cells assessed as forskolin-stimulated cAMP release preincubated for 10 mins before forskolin challenge
ChEMBL 419 6 2 4 4.5 Cc1cc(OCCCN2CCc3nc[nH]c3C2)ccc1-c1nc2c(C)c(F)ccc2[nH]1 10.1016/j.bmcl.2010.04.017
CHEMBL1086105 7235 0 None 3 4 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human histamine H4 receptor in SK-N-MC cells assessed as forskolin-stimulated cAMP release preincubated for 10 mins before forskolin challengeAgonist activity at human histamine H4 receptor in SK-N-MC cells assessed as forskolin-stimulated cAMP release preincubated for 10 mins before forskolin challenge
ChEMBL 419 6 2 4 4.5 Cc1cc(OCCCN2CCc3nc[nH]c3C2)ccc1-c1nc2c(C)c(F)ccc2[nH]1 10.1016/j.bmcl.2010.04.017
58227373 175934 0 None 1 3 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 249 3 2 5 1.5 CC(C)(C)CNc1nccc(N2CC[C@@H](N)C2)n1 10.1021/acs.jmedchem.9b01342
CHEMBL4455324 175934 0 None 1 3 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 249 3 2 5 1.5 CC(C)(C)CNc1nccc(N2CC[C@@H](N)C2)n1 10.1021/acs.jmedchem.9b01342
CHEMBL4596881 175934 0 None 1 3 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 249 3 2 5 1.5 CC(C)(C)CNc1nccc(N2CC[C@@H](N)C2)n1 10.1021/acs.jmedchem.9b01342
21638785 188073 4 None -1 2 Rat 7.5 pEC50 = 7.5 Functional
Antagonist activity at rat histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assayAntagonist activity at rat histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assay
ChEMBL 263 1 2 2 1.9 O=C(c1cc2cc(Cl)ccc2[nH]1)N1CCNCC1 10.1021/jm800670r
CHEMBL503605 188073 4 None -1 2 Rat 7.5 pEC50 = 7.5 Functional
Antagonist activity at rat histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assayAntagonist activity at rat histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assay
ChEMBL 263 1 2 2 1.9 O=C(c1cc2cc(Cl)ccc2[nH]1)N1CCNCC1 10.1021/jm800670r
25130911 184647 0 None - 1 Rat 5.5 pEC50 = 5.5 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 236 2 1 6 -0.1 CN1CCN(c2cc(N(C)C)nc(N)n2)CC1 10.1021/jm8005959
CHEMBL485802 184647 0 None - 1 Rat 5.5 pEC50 = 5.5 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 236 2 1 6 -0.1 CN1CCN(c2cc(N(C)C)nc(N)n2)CC1 10.1021/jm8005959
16352 116683 11 None - 1 Human 6.5 pEC50 = 6.5 Functional
Activity at human histamine H4 receptor transfected in SK-N-MC cells by cAMP assayActivity at human histamine H4 receptor transfected in SK-N-MC cells by cAMP assay
ChEMBL 293 0 0 4 3.1 CN1CCN(C2=Nc3ccccc3Oc3ccccc32)CC1 10.1021/jm051008s
CHEMBL339414 116683 11 None - 1 Human 6.5 pEC50 = 6.5 Functional
Activity at human histamine H4 receptor transfected in SK-N-MC cells by cAMP assayActivity at human histamine H4 receptor transfected in SK-N-MC cells by cAMP assay
ChEMBL 293 0 0 4 3.1 CN1CCN(C2=Nc3ccccc3Oc3ccccc32)CC1 10.1021/jm051008s
1267 3744 43 None -8 5 Mouse 6.5 pEC50 = 6.5 Functional
Agonist activity at mouse H4R expressed in HEK293-SF-mH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at mouse H4R expressed in HEK293-SF-mH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1021/acs.jmedchem.0c00160
3035905 3744 43 None -8 5 Mouse 6.5 pEC50 = 6.5 Functional
Agonist activity at mouse H4R expressed in HEK293-SF-mH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at mouse H4R expressed in HEK293-SF-mH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1021/acs.jmedchem.0c00160
CHEMBL260374 3744 43 None -8 5 Mouse 6.5 pEC50 = 6.5 Functional
Agonist activity at mouse H4R expressed in HEK293-SF-mH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at mouse H4R expressed in HEK293-SF-mH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1021/acs.jmedchem.0c00160
25130579 187129 2 None - 1 Rat 6.5 pEC50 = 6.5 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 238 4 1 5 1.3 CN(C)CCOc1cc(C(C)(C)C)nc(N)n1 10.1021/jm8005959
CHEMBL495341 187129 2 None - 1 Rat 6.5 pEC50 = 6.5 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 238 4 1 5 1.3 CN(C)CCOc1cc(C(C)(C)C)nc(N)n1 10.1021/jm8005959
10678661 5290 1 None -309 2 Human 4.5 pEC50 = 4.5 Functional
Inhibition of the forskolin-stimulated cAMP production in SK-N-MC cells expressing human Histamine H4 receptorInhibition of the forskolin-stimulated cAMP production in SK-N-MC cells expressing human Histamine H4 receptor
ChEMBL 167 2 2 3 0.6 NC[C@@H]1CC[C@@H](c2c[nH]cn2)O1 10.1021/jm0300025
CHEMBL106931 5290 1 None -309 2 Human 4.5 pEC50 = 4.5 Functional
Inhibition of the forskolin-stimulated cAMP production in SK-N-MC cells expressing human Histamine H4 receptorInhibition of the forskolin-stimulated cAMP production in SK-N-MC cells expressing human Histamine H4 receptor
ChEMBL 167 2 2 3 0.6 NC[C@@H]1CC[C@@H](c2c[nH]cn2)O1 10.1021/jm0300025
46228101 198116 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 332 4 2 6 2.1 CN1CCN(c2cc(NCc3ccc(Cl)cc3)nc(N)n2)CC1 10.1016/j.bmc.2009.08.059
CHEMBL594022 198116 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 332 4 2 6 2.1 CN1CCN(c2cc(NCc3ccc(Cl)cc3)nc(N)n2)CC1 10.1016/j.bmc.2009.08.059
1249 1978 14 None -18 2 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 139 4 2 2 0.7 NCCCCc1cnc[nH]1 10.1016/j.bmcl.2010.10.041
13499360 1978 14 None -18 2 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 139 4 2 2 0.7 NCCCCc1cnc[nH]1 10.1016/j.bmcl.2010.10.041
CHEMBL90019 1978 14 None -18 2 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 139 4 2 2 0.7 NCCCCc1cnc[nH]1 10.1016/j.bmcl.2010.10.041
1269 121 33 None 35 6 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human recombinant histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2 by steady-state GTPase activity assayAgonist activity at human recombinant histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2 by steady-state GTPase activity assay
ChEMBL 125 2 2 2 0.2 Cc1c(CCN)nc[nH]1 10.1016/j.bmcl.2010.10.041
37463 121 33 None 35 6 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human recombinant histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2 by steady-state GTPase activity assayAgonist activity at human recombinant histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2 by steady-state GTPase activity assay
ChEMBL 125 2 2 2 0.2 Cc1c(CCN)nc[nH]1 10.1016/j.bmcl.2010.10.041
CHEMBL275443 121 33 None 35 6 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human recombinant histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2 by steady-state GTPase activity assayAgonist activity at human recombinant histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2 by steady-state GTPase activity assay
ChEMBL 125 2 2 2 0.2 Cc1c(CCN)nc[nH]1 10.1016/j.bmcl.2010.10.041
25129528 186603 0 None - 1 Rat 7.5 pEC50 = 7.5 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 303 2 1 5 2.1 CN1CCN(c2cc(-c3cccc(Cl)c3)nc(N)n2)CC1 10.1021/jm8005959
CHEMBL492287 186603 0 None - 1 Rat 7.5 pEC50 = 7.5 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 303 2 1 5 2.1 CN1CCN(c2cc(-c3cccc(Cl)c3)nc(N)n2)CC1 10.1021/jm8005959
44568923 192501 0 None - 1 Rat 6.5 pEC50 = 6.5 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 327 2 1 5 2.3 CN1CCN(c2cc(C34CC5CC(CC(C5)C3)C4)nc(N)n2)CC1 10.1021/jm8005959
CHEMBL522661 192501 0 None - 1 Rat 6.5 pEC50 = 6.5 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 327 2 1 5 2.3 CN1CCN(c2cc(C34CC5CC(CC(C5)C3)C4)nc(N)n2)CC1 10.1021/jm8005959
67087450 116634 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human recombinant histamine H4 receptor expressed in SK-N-MC cells assessed as effect on forskolin-stimulated cAMP-mediated reporter gene activityAgonist activity at human recombinant histamine H4 receptor expressed in SK-N-MC cells assessed as effect on forskolin-stimulated cAMP-mediated reporter gene activity
ChEMBL 249 5 2 5 1.3 CN[C@@H]1CCN(c2cnnc(NCC(C)C)c2)C1 10.1016/j.bmcl.2014.12.027
CHEMBL3393550 116634 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human recombinant histamine H4 receptor expressed in SK-N-MC cells assessed as effect on forskolin-stimulated cAMP-mediated reporter gene activityAgonist activity at human recombinant histamine H4 receptor expressed in SK-N-MC cells assessed as effect on forskolin-stimulated cAMP-mediated reporter gene activity
ChEMBL 249 5 2 5 1.3 CN[C@@H]1CCN(c2cnnc(NCC(C)C)c2)C1 10.1016/j.bmcl.2014.12.027
44547127 115418 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human recombinant histamine H4 receptor expressed in SK-N-MC cells assessed as effect on forskolin-stimulated cAMP-mediated reporter gene activityAgonist activity at human recombinant histamine H4 receptor expressed in SK-N-MC cells assessed as effect on forskolin-stimulated cAMP-mediated reporter gene activity
ChEMBL 234 4 2 4 1.7 CN[C@@H]1CCN(c2ccnc(NC(C)C)c2)C1 10.1016/j.bmcl.2014.12.027
CHEMBL3354816 115418 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human recombinant histamine H4 receptor expressed in SK-N-MC cells assessed as effect on forskolin-stimulated cAMP-mediated reporter gene activityAgonist activity at human recombinant histamine H4 receptor expressed in SK-N-MC cells assessed as effect on forskolin-stimulated cAMP-mediated reporter gene activity
ChEMBL 234 4 2 4 1.7 CN[C@@H]1CCN(c2ccnc(NC(C)C)c2)C1 10.1016/j.bmcl.2014.12.027
58227148 116631 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human recombinant histamine H4 receptor expressed in SK-N-MC cells assessed as effect on forskolin-stimulated cAMP-mediated reporter gene activityAgonist activity at human recombinant histamine H4 receptor expressed in SK-N-MC cells assessed as effect on forskolin-stimulated cAMP-mediated reporter gene activity
ChEMBL 287 4 2 5 1.9 CN[C@@H]1CCN(c2ccnc(NC3CC4CCC3C4)n2)C1 10.1016/j.bmcl.2014.12.027
CHEMBL3393547 116631 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human recombinant histamine H4 receptor expressed in SK-N-MC cells assessed as effect on forskolin-stimulated cAMP-mediated reporter gene activityAgonist activity at human recombinant histamine H4 receptor expressed in SK-N-MC cells assessed as effect on forskolin-stimulated cAMP-mediated reporter gene activity
ChEMBL 287 4 2 5 1.9 CN[C@@H]1CCN(c2ccnc(NC3CC4CCC3C4)n2)C1 10.1016/j.bmcl.2014.12.027
10678661 5290 1 None -309 2 Human 4.5 pEC50 = 4.5 Functional
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 167 2 2 3 0.6 NC[C@@H]1CC[C@@H](c2c[nH]cn2)O1 10.1016/j.bmcl.2010.10.041
CHEMBL106931 5290 1 None -309 2 Human 4.5 pEC50 = 4.5 Functional
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 167 2 2 3 0.6 NC[C@@H]1CC[C@@H](c2c[nH]cn2)O1 10.1016/j.bmcl.2010.10.041
25131557 192656 0 None - 1 Rat 5.5 pEC50 = 5.5 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 301 3 1 8 0.3 COc1ncc(-c2cc(N3CCN(C)CC3)nc(N)n2)cn1 10.1021/jm8005959
CHEMBL523835 192656 0 None - 1 Rat 5.5 pEC50 = 5.5 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 301 3 1 8 0.3 COc1ncc(-c2cc(N3CCN(C)CC3)nc(N)n2)cn1 10.1021/jm8005959
25130909 186797 0 None 1 2 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at human histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 208 1 2 6 -0.6 CN1CCN(c2nc(N)ncc2N)CC1 10.1021/jm8005959
CHEMBL493478 186797 0 None 1 2 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at human histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 208 1 2 6 -0.6 CN1CCN(c2nc(N)ncc2N)CC1 10.1021/jm8005959
44478385 5699 2 None 20 2 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19 protein by steady-state GTPase assayAgonist activity at human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19 protein by steady-state GTPase assay
ChEMBL 342 9 3 4 2.5 N#C/N=C(/NCCCCc1c[nH]cn1)NCCSc1ccccc1 10.1021/jm900526h
CHEMBL1078642 5699 2 None 20 2 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19 protein by steady-state GTPase assayAgonist activity at human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19 protein by steady-state GTPase assay
ChEMBL 342 9 3 4 2.5 N#C/N=C(/NCCCCc1c[nH]cn1)NCCSc1ccccc1 10.1021/jm900526h
46890549 6507 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human histamine H4 receptor in SK-N-MC cells assessed as forskolin-stimulated cAMP release preincubated for 10 mins before forskolin challengeAgonist activity at human histamine H4 receptor in SK-N-MC cells assessed as forskolin-stimulated cAMP release preincubated for 10 mins before forskolin challenge
ChEMBL 396 6 2 4 4.2 Cc1cc(OCCCN2CCCC(N)C2)ccc1-c1nc2c(C)c(F)ccc2[nH]1 10.1016/j.bmcl.2010.04.017
CHEMBL1083085 6507 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human histamine H4 receptor in SK-N-MC cells assessed as forskolin-stimulated cAMP release preincubated for 10 mins before forskolin challengeAgonist activity at human histamine H4 receptor in SK-N-MC cells assessed as forskolin-stimulated cAMP release preincubated for 10 mins before forskolin challenge
ChEMBL 396 6 2 4 4.2 Cc1cc(OCCCN2CCCC(N)C2)ccc1-c1nc2c(C)c(F)ccc2[nH]1 10.1016/j.bmcl.2010.04.017
44480960 5554 2 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19 protein by steady-state GTPase assayAgonist activity at human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19 protein by steady-state GTPase assay
ChEMBL 248 6 3 3 1.2 CC(C)N/C(=N\C#N)NCCCCc1c[nH]cn1 10.1021/jm900526h
CHEMBL1077636 5554 2 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19 protein by steady-state GTPase assayAgonist activity at human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19 protein by steady-state GTPase assay
ChEMBL 248 6 3 3 1.2 CC(C)N/C(=N\C#N)NCCCCc1c[nH]cn1 10.1021/jm900526h
42625303 180184 0 None -2089 6 Rat 5.5 pEC50 = 5.5 Functional
Agonist activity at rat H4R by [35S]-GTPgammaS-binding assayAgonist activity at rat H4R by [35S]-GTPgammaS-binding assay
ChEMBL 223 5 3 2 0.2 CCC(=O)/N=C(\N)NCCCc1c[nH]cn1 10.1021/acs.jmedchem.9b01342
CHEMBL475621 180184 0 None -2089 6 Rat 5.5 pEC50 = 5.5 Functional
Agonist activity at rat H4R by [35S]-GTPgammaS-binding assayAgonist activity at rat H4R by [35S]-GTPgammaS-binding assay
ChEMBL 223 5 3 2 0.2 CCC(=O)/N=C(\N)NCCCc1c[nH]cn1 10.1021/acs.jmedchem.9b01342
56954425 81669 0 None -13 2 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human H4R-RGS19 Galphai2 Gbeta1gamma2 expressed in Sf9 cells at 0.1 nM to 1 mM by steady state GTPase activity assayAgonist activity at human H4R-RGS19 Galphai2 Gbeta1gamma2 expressed in Sf9 cells at 0.1 nM to 1 mM by steady state GTPase activity assay
ChEMBL 584 23 6 4 4.0 N/C(=N\C(=O)CCCCCCCCCCCCCCC(=O)/N=C(\N)NCCCc1c[nH]cn1)NCCCc1c[nH]cn1 10.1021/jm201128q
CHEMBL2165643 81669 0 None -13 2 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human H4R-RGS19 Galphai2 Gbeta1gamma2 expressed in Sf9 cells at 0.1 nM to 1 mM by steady state GTPase activity assayAgonist activity at human H4R-RGS19 Galphai2 Gbeta1gamma2 expressed in Sf9 cells at 0.1 nM to 1 mM by steady state GTPase activity assay
ChEMBL 584 23 6 4 4.0 N/C(=N\C(=O)CCCCCCCCCCCCCCC(=O)/N=C(\N)NCCCc1c[nH]cn1)NCCCc1c[nH]cn1 10.1021/jm201128q
25130913 169620 0 None - 1 Rat 6.5 pEC50 = 6.5 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 278 2 1 7 -0.4 CN1CCN(c2cc(N3CCOCC3)nc(N)n2)CC1 10.1021/jm8005959
CHEMBL444484 169620 0 None - 1 Rat 6.5 pEC50 = 6.5 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 278 2 1 7 -0.4 CN1CCN(c2cc(N3CCOCC3)nc(N)n2)CC1 10.1021/jm8005959
1274 4001 12 None -776 4 Rat 4.5 pEC50 = 4.5 Functional
Agonist activity at rat H4R by [35S]-GTPgammaS-binding assayAgonist activity at rat H4R by [35S]-GTPgammaS-binding assay
ChEMBL 161 3 4 3 -1.1 NC(=N)SCCN=C(N)N 10.1021/acs.jmedchem.9b01342
3063228 4001 12 None -776 4 Rat 4.5 pEC50 = 4.5 Functional
Agonist activity at rat H4R by [35S]-GTPgammaS-binding assayAgonist activity at rat H4R by [35S]-GTPgammaS-binding assay
ChEMBL 161 3 4 3 -1.1 NC(=N)SCCN=C(N)N 10.1021/acs.jmedchem.9b01342
CHEMBL1196470 4001 12 None -776 4 Rat 4.5 pEC50 = 4.5 Functional
Agonist activity at rat H4R by [35S]-GTPgammaS-binding assayAgonist activity at rat H4R by [35S]-GTPgammaS-binding assay
ChEMBL 161 3 4 3 -1.1 NC(=N)SCCN=C(N)N 10.1021/acs.jmedchem.9b01342
155517880 176093 0 None -3 3 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 291 4 4 5 1.0 CC(C)(C)CNc1nccc(N2CC[C@@H](NC(=N)N)C2)n1 10.1021/acs.jmedchem.9b01342
CHEMBL4445423 176093 0 None -3 3 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 291 4 4 5 1.0 CC(C)(C)CNc1nccc(N2CC[C@@H](NC(=N)N)C2)n1 10.1021/acs.jmedchem.9b01342
CHEMBL4598198 176093 0 None -3 3 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 291 4 4 5 1.0 CC(C)(C)CNc1nccc(N2CC[C@@H](NC(=N)N)C2)n1 10.1021/acs.jmedchem.9b01342
155552061 175904 0 None -8 3 Mouse 7.5 pEC50 = 7.5 Functional
Agonist activity at mouse H4R expressed in HEK293-SF-mH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at mouse H4R expressed in HEK293-SF-mH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 277 3 1 5 2.1 CN1CCCN(c2ccnc(NCC(C)(C)C)n2)CC1 10.1021/acs.jmedchem.9b01342
CHEMBL4543119 175904 0 None -8 3 Mouse 7.5 pEC50 = 7.5 Functional
Agonist activity at mouse H4R expressed in HEK293-SF-mH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at mouse H4R expressed in HEK293-SF-mH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 277 3 1 5 2.1 CN1CCCN(c2ccnc(NCC(C)(C)C)n2)CC1 10.1021/acs.jmedchem.9b01342
CHEMBL4596606 175904 0 None -8 3 Mouse 7.5 pEC50 = 7.5 Functional
Agonist activity at mouse H4R expressed in HEK293-SF-mH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at mouse H4R expressed in HEK293-SF-mH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 277 3 1 5 2.1 CN1CCCN(c2ccnc(NCC(C)(C)C)n2)CC1 10.1021/acs.jmedchem.9b01342
25129180 186668 0 None - 1 Rat 6.5 pEC50 = 6.5 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 264 4 1 6 0.7 CCN(CC)c1cc(N2CCN(C)CC2)nc(N)n1 10.1021/jm8005959
CHEMBL492662 186668 0 None - 1 Rat 6.5 pEC50 = 6.5 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 264 4 1 6 0.7 CCN(CC)c1cc(N2CCN(C)CC2)nc(N)n1 10.1021/jm8005959
3228743 186798 5 None - 1 Rat 6.4 pEC50 = 6.4 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 207 1 1 5 0.1 Cc1cc(N2CCN(C)CC2)nc(N)n1 10.1021/jm8005959
CHEMBL493479 186798 5 None - 1 Rat 6.4 pEC50 = 6.4 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 207 1 1 5 0.1 Cc1cc(N2CCN(C)CC2)nc(N)n1 10.1021/jm8005959
12769844 108990 0 None -3 2 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human recombinant histamine H4 receptor-RGS19 fusion protein expressed in Sf9 cells coexpressing Galphai2,Gbeta1gamma2 assessed as [35S]GTPgammaS binding after 90 mins by liquid scintillation countingAgonist activity at human recombinant histamine H4 receptor-RGS19 fusion protein expressed in Sf9 cells coexpressing Galphai2,Gbeta1gamma2 assessed as [35S]GTPgammaS binding after 90 mins by liquid scintillation counting
ChEMBL 234 5 3 3 0.7 CN/C(=N/C#N)NCCCCc1nc[nH]c1C 10.1039/C3MD00245D
CHEMBL3220641 108990 0 None -3 2 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human recombinant histamine H4 receptor-RGS19 fusion protein expressed in Sf9 cells coexpressing Galphai2,Gbeta1gamma2 assessed as [35S]GTPgammaS binding after 90 mins by liquid scintillation countingAgonist activity at human recombinant histamine H4 receptor-RGS19 fusion protein expressed in Sf9 cells coexpressing Galphai2,Gbeta1gamma2 assessed as [35S]GTPgammaS binding after 90 mins by liquid scintillation counting
ChEMBL 234 5 3 3 0.7 CN/C(=N/C#N)NCCCCc1nc[nH]c1C 10.1039/C3MD00245D
25129181 186669 0 None - 1 Rat 5.4 pEC50 = 5.4 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 305 3 1 7 -0.0 CN1CCN(c2cc(N3CCC(N(C)C)C3)nc(N)n2)CC1 10.1021/jm8005959
CHEMBL492663 186669 0 None - 1 Rat 5.4 pEC50 = 5.4 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 305 3 1 7 -0.0 CN1CCN(c2cc(N3CCC(N(C)C)C3)nc(N)n2)CC1 10.1021/jm8005959
25128825 186981 0 None - 1 Rat 5.4 pEC50 = 5.4 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 248 1 1 4 2.2 CN1CCC(c2cc(C(C)(C)C)nc(N)n2)CC1 10.1021/jm8005959
CHEMBL494585 186981 0 None - 1 Rat 5.4 pEC50 = 5.4 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 248 1 1 4 2.2 CN1CCC(c2cc(C(C)(C)C)nc(N)n2)CC1 10.1021/jm8005959
44478385 5699 2 None 20 2 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human histamine H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assayAgonist activity at human histamine H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 342 9 3 4 2.5 N#C/N=C(/NCCCCc1c[nH]cn1)NCCSc1ccccc1 10.1021/acs.jmedchem.6b00120
CHEMBL1078642 5699 2 None 20 2 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human histamine H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assayAgonist activity at human histamine H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 342 9 3 4 2.5 N#C/N=C(/NCCCCc1c[nH]cn1)NCCSc1ccccc1 10.1021/acs.jmedchem.6b00120
44478385 5699 2 None 20 2 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human recombinant histamine H4 receptor-RGS19 fusion protein expressed in Sf9 cells coexpressing Galphai2,Gbeta1gamma2 assessed as [35S]GTPgammaS binding after 90 mins by liquid scintillation countingAgonist activity at human recombinant histamine H4 receptor-RGS19 fusion protein expressed in Sf9 cells coexpressing Galphai2,Gbeta1gamma2 assessed as [35S]GTPgammaS binding after 90 mins by liquid scintillation counting
ChEMBL 342 9 3 4 2.5 N#C/N=C(/NCCCCc1c[nH]cn1)NCCSc1ccccc1 10.1039/C3MD00245D
CHEMBL1078642 5699 2 None 20 2 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human recombinant histamine H4 receptor-RGS19 fusion protein expressed in Sf9 cells coexpressing Galphai2,Gbeta1gamma2 assessed as [35S]GTPgammaS binding after 90 mins by liquid scintillation countingAgonist activity at human recombinant histamine H4 receptor-RGS19 fusion protein expressed in Sf9 cells coexpressing Galphai2,Gbeta1gamma2 assessed as [35S]GTPgammaS binding after 90 mins by liquid scintillation counting
ChEMBL 342 9 3 4 2.5 N#C/N=C(/NCCCCc1c[nH]cn1)NCCSc1ccccc1 10.1039/C3MD00245D
25129527 186831 0 None - 1 Rat 7.4 pEC50 = 7.4 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 303 2 1 5 2.1 CN1CCN(c2cc(-c3ccc(Cl)cc3)nc(N)n2)CC1 10.1021/jm8005959
CHEMBL493720 186831 0 None - 1 Rat 7.4 pEC50 = 7.4 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 303 2 1 5 2.1 CN1CCN(c2cc(-c3ccc(Cl)cc3)nc(N)n2)CC1 10.1021/jm8005959
24798596 198185 2 None - 1 Human 7.4 pEC50 = 7.4 Functional
Inverse agonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of [35S]GTPgammaS bindingInverse agonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 310 2 1 6 1.3 CN1CCN(c2cc(N3Cc4ccccc4C3)nc(N)n2)CC1 10.1016/j.bmc.2009.08.059
CHEMBL594491 198185 2 None - 1 Human 7.4 pEC50 = 7.4 Functional
Inverse agonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of [35S]GTPgammaS bindingInverse agonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 310 2 1 6 1.3 CN1CCN(c2cc(N3Cc4ccccc4C3)nc(N)n2)CC1 10.1016/j.bmc.2009.08.059
127052292 139736 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human histamine H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assayAgonist activity at human histamine H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 350 7 3 3 2.9 N#C/N=C(/NCCCc1ccccc1)NC[C@@H]1CC[C@H](c2c[nH]cn2)C1 10.1021/acs.jmedchem.6b00120
CHEMBL3805663 139736 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human histamine H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assayAgonist activity at human histamine H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 350 7 3 3 2.9 N#C/N=C(/NCCCc1ccccc1)NC[C@@H]1CC[C@H](c2c[nH]cn2)C1 10.1021/acs.jmedchem.6b00120
1274 4001 12 None 7 4 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human H4R by [35S]-GTPgammaS-binding assayAgonist activity at human H4R by [35S]-GTPgammaS-binding assay
ChEMBL 161 3 4 3 -1.1 NC(=N)SCCN=C(N)N 10.1021/acs.jmedchem.9b01342
3063228 4001 12 None 7 4 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human H4R by [35S]-GTPgammaS-binding assayAgonist activity at human H4R by [35S]-GTPgammaS-binding assay
ChEMBL 161 3 4 3 -1.1 NC(=N)SCCN=C(N)N 10.1021/acs.jmedchem.9b01342
CHEMBL1196470 4001 12 None 7 4 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human H4R by [35S]-GTPgammaS-binding assayAgonist activity at human H4R by [35S]-GTPgammaS-binding assay
ChEMBL 161 3 4 3 -1.1 NC(=N)SCCN=C(N)N 10.1021/acs.jmedchem.9b01342
11846465 141400 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Activity at human histamine H4 receptor transfected in SK-N-MC cells by cAMP assayActivity at human histamine H4 receptor transfected in SK-N-MC cells by cAMP assay
ChEMBL 345 0 0 4 3.9 CN1CCN(C2=Nc3ccc(Cl)cc3Oc3cc(F)ccc32)CC1 10.1021/jm051008s
CHEMBL387054 141400 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Activity at human histamine H4 receptor transfected in SK-N-MC cells by cAMP assayActivity at human histamine H4 receptor transfected in SK-N-MC cells by cAMP assay
ChEMBL 345 0 0 4 3.9 CN1CCN(C2=Nc3ccc(Cl)cc3Oc3cc(F)ccc32)CC1 10.1021/jm051008s
25131559 187002 0 None -23 2 Rat 6.4 pEC50 = 6.4 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 259 2 2 6 0.2 CN1CCN(c2cc(-c3c[nH]cn3)nc(N)n2)CC1 10.1021/jm8005959
CHEMBL494667 187002 0 None -23 2 Rat 6.4 pEC50 = 6.4 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 259 2 2 6 0.2 CN1CCN(c2cc(-c3c[nH]cn3)nc(N)n2)CC1 10.1021/jm8005959
25131561 186821 0 None 3 2 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at human histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 286 2 1 7 -0.0 CN1CCN(c2cc(-n3ccccc3=O)nc(N)n2)CC1 10.1021/jm8005959
CHEMBL493664 186821 0 None 3 2 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at human histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 286 2 1 7 -0.0 CN1CCN(c2cc(-n3ccccc3=O)nc(N)n2)CC1 10.1021/jm8005959
46235428 6526 0 None -263 3 Mouse 7.4 pEC50 = 7.4 Functional
Intrinsic activity at mouse histamine H4 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-induced cAMP responsive element-beta-galactosidase activity after 6 hrs by colorimetric cAMP assayIntrinsic activity at mouse histamine H4 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-induced cAMP responsive element-beta-galactosidase activity after 6 hrs by colorimetric cAMP assay
ChEMBL 407 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 6526 0 None -263 3 Mouse 7.4 pEC50 = 7.4 Functional
Intrinsic activity at mouse histamine H4 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-induced cAMP responsive element-beta-galactosidase activity after 6 hrs by colorimetric cAMP assayIntrinsic activity at mouse histamine H4 receptor expressed in human SK-N-MC cells assessed as inhibition of forskolin-induced cAMP responsive element-beta-galactosidase activity after 6 hrs by colorimetric cAMP assay
ChEMBL 407 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 33 None 35 6 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 125 2 2 2 0.2 Cc1c(CCN)nc[nH]1 10.1016/j.bmcl.2010.10.041
37463 121 33 None 35 6 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 125 2 2 2 0.2 Cc1c(CCN)nc[nH]1 10.1016/j.bmcl.2010.10.041
CHEMBL275443 121 33 None 35 6 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 125 2 2 2 0.2 Cc1c(CCN)nc[nH]1 10.1016/j.bmcl.2010.10.041
136030655 56188 0 None -3 3 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human recombinant histamine H4 receptor expressed in human SK-N-MC cells co-expressing SRE-Luc by luciferase reporter gene assayAgonist activity at human recombinant histamine H4 receptor expressed in human SK-N-MC cells co-expressing SRE-Luc by luciferase reporter gene assay
ChEMBL 292 1 2 3 2.2 CN1CCN(/C(=N\O)c2cc3cc(Cl)ccc3[nH]2)CC1 10.1016/j.bmcl.2010.10.041
CHEMBL1632413 56188 0 None -3 3 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human recombinant histamine H4 receptor expressed in human SK-N-MC cells co-expressing SRE-Luc by luciferase reporter gene assayAgonist activity at human recombinant histamine H4 receptor expressed in human SK-N-MC cells co-expressing SRE-Luc by luciferase reporter gene assay
ChEMBL 292 1 2 3 2.2 CN1CCN(/C(=N\O)c2cc3cc(Cl)ccc3[nH]2)CC1 10.1016/j.bmcl.2010.10.041
25129523 186704 40 None - 1 Rat 7.4 pEC50 = 7.4 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 269 2 1 5 1.5 CN1CCN(c2cc(-c3ccccc3)nc(N)n2)CC1 10.1021/jm8005959
CHEMBL492884 186704 40 None - 1 Rat 7.4 pEC50 = 7.4 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 269 2 1 5 1.5 CN1CCN(c2cc(-c3ccccc3)nc(N)n2)CC1 10.1021/jm8005959
25129523 186704 40 None - 1 Rat 7.4 pEC50 = 7.4 Functional
Antagonist activity at rat histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assayAntagonist activity at rat histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assay
ChEMBL 269 2 1 5 1.5 CN1CCN(c2cc(-c3ccccc3)nc(N)n2)CC1 10.1021/jm800670r
CHEMBL492884 186704 40 None - 1 Rat 7.4 pEC50 = 7.4 Functional
Antagonist activity at rat histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assayAntagonist activity at rat histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assay
ChEMBL 269 2 1 5 1.5 CN1CCN(c2cc(-c3ccccc3)nc(N)n2)CC1 10.1021/jm800670r
70692530 75339 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at histamine H4 receptor (unknown origin) expressed in HEK293T cells harboring CRE-luciferase after 6 hrs by luciferase reporter gene assayAgonist activity at histamine H4 receptor (unknown origin) expressed in HEK293T cells harboring CRE-luciferase after 6 hrs by luciferase reporter gene assay
ChEMBL 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 75339 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at histamine H4 receptor (unknown origin) expressed in HEK293T cells harboring CRE-luciferase after 6 hrs by luciferase reporter gene assayAgonist activity at histamine H4 receptor (unknown origin) expressed in HEK293T cells harboring CRE-luciferase after 6 hrs by luciferase reporter gene assay
ChEMBL 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 17804 31 None -5 2 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human recombinant histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2 by steady-state GTPase activity assayAgonist activity at human recombinant histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2 by steady-state GTPase activity assay
ChEMBL 125 2 2 2 0.2 Cc1ncc(CCN)[nH]1 10.1016/j.bmcl.2010.10.041
CHEMBL12620 17804 31 None -5 2 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human recombinant histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2 by steady-state GTPase activity assayAgonist activity at human recombinant histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2 by steady-state GTPase activity assay
ChEMBL 125 2 2 2 0.2 Cc1ncc(CCN)[nH]1 10.1016/j.bmcl.2010.10.041
58227326 116626 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human recombinant histamine H4 receptor expressed in SK-N-MC cells assessed as effect on forskolin-stimulated cAMP-mediated reporter gene activityAgonist activity at human recombinant histamine H4 receptor expressed in SK-N-MC cells assessed as effect on forskolin-stimulated cAMP-mediated reporter gene activity
ChEMBL 249 6 2 5 1.5 CCCCNc1nccc(N2CC[C@@H](NC)C2)n1 10.1016/j.bmcl.2014.12.027
CHEMBL3393542 116626 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human recombinant histamine H4 receptor expressed in SK-N-MC cells assessed as effect on forskolin-stimulated cAMP-mediated reporter gene activityAgonist activity at human recombinant histamine H4 receptor expressed in SK-N-MC cells assessed as effect on forskolin-stimulated cAMP-mediated reporter gene activity
ChEMBL 249 6 2 5 1.5 CCCCNc1nccc(N2CC[C@@H](NC)C2)n1 10.1016/j.bmcl.2014.12.027
58227373 175934 0 None -3 3 Mouse 8.4 pEC50 = 8.4 Functional
Agonist activity at mouse H4R expressed in HEK293-SF-mH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at mouse H4R expressed in HEK293-SF-mH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 249 3 2 5 1.5 CC(C)(C)CNc1nccc(N2CC[C@@H](N)C2)n1 10.1021/acs.jmedchem.9b01342
CHEMBL4455324 175934 0 None -3 3 Mouse 8.4 pEC50 = 8.4 Functional
Agonist activity at mouse H4R expressed in HEK293-SF-mH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at mouse H4R expressed in HEK293-SF-mH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 249 3 2 5 1.5 CC(C)(C)CNc1nccc(N2CC[C@@H](N)C2)n1 10.1021/acs.jmedchem.9b01342
CHEMBL4596881 175934 0 None -3 3 Mouse 8.4 pEC50 = 8.4 Functional
Agonist activity at mouse H4R expressed in HEK293-SF-mH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at mouse H4R expressed in HEK293-SF-mH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 249 3 2 5 1.5 CC(C)(C)CNc1nccc(N2CC[C@@H](N)C2)n1 10.1021/acs.jmedchem.9b01342
25071004 192116 0 None 1 2 Mouse 8.4 pEC50 = 8.4 Functional
Antagonist activity at mouse histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assayAntagonist activity at mouse histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assay
ChEMBL 309 2 2 5 2.0 CN[C@@H]1CCN(c2nc(N)nc3c2CCCc2ccccc2-3)C1 10.1021/jm800670r
CHEMBL521996 192116 0 None 1 2 Mouse 8.4 pEC50 = 8.4 Functional
Antagonist activity at mouse histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assayAntagonist activity at mouse histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assay
ChEMBL 309 2 2 5 2.0 CN[C@@H]1CCN(c2nc(N)nc3c2CCCc2ccccc2-3)C1 10.1021/jm800670r
42625303 180184 0 None -2 6 Human 8.4 pEC50 = 8.4 Functional
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 180184 0 None -2 6 Human 8.4 pEC50 = 8.4 Functional
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 192575 0 None 1 2 Mouse 8.3 pEC50 = 8.3 Functional
Antagonist activity at mouse histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assayAntagonist activity at mouse histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assay
ChEMBL 313 1 2 5 1.8 Nc1nc2c(c(N3CCNCC3)n1)CCCc1ccc(F)cc1-2 10.1021/jm800670r
CHEMBL523225 192575 0 None 1 2 Mouse 8.3 pEC50 = 8.3 Functional
Antagonist activity at mouse histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assayAntagonist activity at mouse histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assay
ChEMBL 313 1 2 5 1.8 Nc1nc2c(c(N3CCNCC3)n1)CCCc1ccc(F)cc1-2 10.1021/jm800670r
10702196 108081 1 None -1 2 Human 4.4 pEC50 = 4.4 Functional
Inhibition of the forskolin-stimulated cAMP production in SK-N-MC cells expressing human Histamine H4 receptorInhibition of the forskolin-stimulated cAMP production in SK-N-MC cells expressing human Histamine H4 receptor
ChEMBL 165 2 2 3 0.4 NC[C@@H]1C=C[C@H](c2c[nH]cn2)O1 10.1021/jm0300025
CHEMBL320279 108081 1 None -1 2 Human 4.4 pEC50 = 4.4 Functional
Inhibition of the forskolin-stimulated cAMP production in SK-N-MC cells expressing human Histamine H4 receptorInhibition of the forskolin-stimulated cAMP production in SK-N-MC cells expressing human Histamine H4 receptor
ChEMBL 165 2 2 3 0.4 NC[C@@H]1C=C[C@H](c2c[nH]cn2)O1 10.1021/jm0300025
56954320 81667 0 None -10 3 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human H4R-RGS19 Galphai2 Gbeta1gamma2 expressed in Sf9 cells at 0.1 nM to 1 mM by steady state GTPase activity assayAgonist activity at human H4R-RGS19 Galphai2 Gbeta1gamma2 expressed in Sf9 cells at 0.1 nM to 1 mM by steady state GTPase activity assay
ChEMBL 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 81667 0 None -10 3 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human H4R-RGS19 Galphai2 Gbeta1gamma2 expressed in Sf9 cells at 0.1 nM to 1 mM by steady state GTPase activity assayAgonist activity at human H4R-RGS19 Galphai2 Gbeta1gamma2 expressed in Sf9 cells at 0.1 nM to 1 mM by steady state GTPase activity assay
ChEMBL 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 3744 43 None -17 5 Human 6.4 pEC50 = 6.4 Functional
Antagonist activity at human histamine 4 receptor expressed in Sf9 cell membranes co-expressing Galphai2 and Gbeta1gamma2 assessed as [35S]GTPgammaS binding by scintillation countingAntagonist activity at human histamine 4 receptor expressed in Sf9 cell membranes co-expressing Galphai2 and Gbeta1gamma2 assessed as [35S]GTPgammaS binding by scintillation counting
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1016/j.bmcl.2015.12.035
3035905 3744 43 None -17 5 Human 6.4 pEC50 = 6.4 Functional
Antagonist activity at human histamine 4 receptor expressed in Sf9 cell membranes co-expressing Galphai2 and Gbeta1gamma2 assessed as [35S]GTPgammaS binding by scintillation countingAntagonist activity at human histamine 4 receptor expressed in Sf9 cell membranes co-expressing Galphai2 and Gbeta1gamma2 assessed as [35S]GTPgammaS binding by scintillation counting
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1016/j.bmcl.2015.12.035
CHEMBL260374 3744 43 None -17 5 Human 6.4 pEC50 = 6.4 Functional
Antagonist activity at human histamine 4 receptor expressed in Sf9 cell membranes co-expressing Galphai2 and Gbeta1gamma2 assessed as [35S]GTPgammaS binding by scintillation countingAntagonist activity at human histamine 4 receptor expressed in Sf9 cell membranes co-expressing Galphai2 and Gbeta1gamma2 assessed as [35S]GTPgammaS binding by scintillation counting
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1016/j.bmcl.2015.12.035
25129524 186601 0 None - 1 Rat 7.4 pEC50 = 7.4 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 283 2 1 5 1.8 Cc1cccc(-c2cc(N3CCN(C)CC3)nc(N)n2)c1 10.1021/jm8005959
CHEMBL492274 186601 0 None - 1 Rat 7.4 pEC50 = 7.4 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 283 2 1 5 1.8 Cc1cccc(-c2cc(N3CCN(C)CC3)nc(N)n2)c1 10.1021/jm8005959
25130909 186797 0 None -1 2 Rat 7.4 pEC50 = 7.4 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 208 1 2 6 -0.6 CN1CCN(c2nc(N)ncc2N)CC1 10.1021/jm8005959
CHEMBL493478 186797 0 None -1 2 Rat 7.4 pEC50 = 7.4 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 208 1 2 6 -0.6 CN1CCN(c2nc(N)ncc2N)CC1 10.1021/jm8005959
1278 2119 79 None -1 4 Rat 7.4 pEC50 = 7.4 Functional
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 2119 79 None -1 4 Rat 7.4 pEC50 = 7.4 Functional
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 2119 79 None -1 4 Rat 7.4 pEC50 = 7.4 Functional
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 2119 79 None -1 4 Rat 7.4 pEC50 = 7.4 Functional
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 187818 30 None 2 2 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at human histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 193 1 1 5 -0.2 CN1CCN(c2ccnc(N)n2)CC1 10.1021/jm8005959
CHEMBL501882 187818 30 None 2 2 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at human histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 193 1 1 5 -0.2 CN1CCN(c2ccnc(N)n2)CC1 10.1021/jm8005959
25129526 186830 0 None - 1 Rat 7.4 pEC50 = 7.4 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 299 3 1 6 1.5 COc1ccccc1-c1cc(N2CCN(C)CC2)nc(N)n1 10.1021/jm8005959
CHEMBL493719 186830 0 None - 1 Rat 7.4 pEC50 = 7.4 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 299 3 1 6 1.5 COc1ccccc1-c1cc(N2CCN(C)CC2)nc(N)n1 10.1021/jm8005959
24797248 198184 2 None - 1 Human 7.4 pEC50 = 7.4 Functional
Inverse agonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of [35S]GTPgammaS bindingInverse agonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 324 2 1 6 1.4 CN1CCN(c2cc(N3CCc4ccccc4C3)nc(N)n2)CC1 10.1016/j.bmc.2009.08.059
CHEMBL594490 198184 2 None - 1 Human 7.4 pEC50 = 7.4 Functional
Inverse agonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of [35S]GTPgammaS bindingInverse agonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 324 2 1 6 1.4 CN1CCN(c2cc(N3CCc4ccccc4C3)nc(N)n2)CC1 10.1016/j.bmc.2009.08.059
127050434 139720 0 None 3 2 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human histamine H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assayAgonist activity at human histamine H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 160 3 4 3 0.2 CC(=N)SCCNC(=N)N 10.1021/acs.jmedchem.6b00120
CHEMBL3805514 139720 0 None 3 2 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human histamine H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assayAgonist activity at human histamine H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 160 3 4 3 0.2 CC(=N)SCCNC(=N)N 10.1021/acs.jmedchem.6b00120
25129169 186598 0 None 1 2 Mouse 7.3 pEC50 = 7.3 Functional
Antagonist activity at mouse histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assayAntagonist activity at mouse histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assay
ChEMBL 323 2 2 5 2.3 Nc1nc2c(c(N3CCNCC3)n1)CCCCC2c1ccccc1 10.1021/jm800670r
CHEMBL492231 186598 0 None 1 2 Mouse 7.3 pEC50 = 7.3 Functional
Antagonist activity at mouse histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assayAntagonist activity at mouse histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assay
ChEMBL 323 2 2 5 2.3 Nc1nc2c(c(N3CCNCC3)n1)CCCCC2c1ccccc1 10.1021/jm800670r
24798595 169808 2 None - 1 Rat 7.3 pEC50 = 7.3 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 276 2 1 6 0.8 CN1CCN(c2cc(N3CCCCC3)nc(N)n2)CC1 10.1021/jm8005959
CHEMBL444782 169808 2 None - 1 Rat 7.3 pEC50 = 7.3 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 276 2 1 6 0.8 CN1CCN(c2cc(N3CCCCC3)nc(N)n2)CC1 10.1021/jm8005959
90667239 108989 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human recombinant histamine H4 receptor-RGS19 fusion protein expressed in Sf9 cells coexpressing Galphai2,Gbeta1gamma2 assessed as [35S]GTPgammaS binding after 90 mins by liquid scintillation countingAgonist activity at human recombinant histamine H4 receptor-RGS19 fusion protein expressed in Sf9 cells coexpressing Galphai2,Gbeta1gamma2 assessed as [35S]GTPgammaS binding after 90 mins by liquid scintillation counting
ChEMBL 342 8 3 4 2.5 Cc1nc(CCCN/C(=N\C#N)NCCSc2ccccc2)c[nH]1 10.1039/C3MD00245D
CHEMBL3220640 108989 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human recombinant histamine H4 receptor-RGS19 fusion protein expressed in Sf9 cells coexpressing Galphai2,Gbeta1gamma2 assessed as [35S]GTPgammaS binding after 90 mins by liquid scintillation countingAgonist activity at human recombinant histamine H4 receptor-RGS19 fusion protein expressed in Sf9 cells coexpressing Galphai2,Gbeta1gamma2 assessed as [35S]GTPgammaS binding after 90 mins by liquid scintillation counting
ChEMBL 342 8 3 4 2.5 Cc1nc(CCCN/C(=N\C#N)NCCSc2ccccc2)c[nH]1 10.1039/C3MD00245D
25130573 186302 2 None - 1 Rat 5.3 pEC50 = 5.3 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 249 1 1 5 1.1 CN1CCN(c2cc(N)nc(C(C)(C)C)n2)CC1 10.1021/jm8005959
CHEMBL489663 186302 2 None - 1 Rat 5.3 pEC50 = 5.3 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 249 1 1 5 1.1 CN1CCN(c2cc(N)nc(C(C)(C)C)n2)CC1 10.1021/jm8005959
25130581 186642 0 None -3 2 Rat 5.3 pEC50 = 5.3 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 264 2 0 5 1.5 COc1nc(N2CCN(C)CC2)cc(C(C)(C)C)n1 10.1021/jm8005959
CHEMBL492489 186642 0 None -3 2 Rat 5.3 pEC50 = 5.3 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 264 2 0 5 1.5 COc1nc(N2CCN(C)CC2)cc(C(C)(C)C)n1 10.1021/jm8005959
25130235 187004 1 None -4 3 Rat 5.3 pEC50 = 5.3 Functional
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 187004 1 None -4 3 Rat 5.3 pEC50 = 5.3 Functional
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 6437 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human histamine H4 receptor in SK-N-MC cells assessed as forskolin-stimulated cAMP release preincubated for 10 mins before forskolin challengeAgonist activity at human histamine H4 receptor in SK-N-MC cells assessed as forskolin-stimulated cAMP release preincubated for 10 mins before forskolin challenge
ChEMBL 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 6437 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human histamine H4 receptor in SK-N-MC cells assessed as forskolin-stimulated cAMP release preincubated for 10 mins before forskolin challengeAgonist activity at human histamine H4 receptor in SK-N-MC cells assessed as forskolin-stimulated cAMP release preincubated for 10 mins before forskolin challenge
ChEMBL 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 198400 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Inverse agonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of [35S]GTPgammaS bindingInverse agonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 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 198400 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Inverse agonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of [35S]GTPgammaS bindingInverse agonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 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 116613 2 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human recombinant histamine H4 receptor expressed in SK-N-MC cells assessed as effect on forskolin-stimulated cAMP-mediated reporter gene activityAgonist activity at human recombinant histamine H4 receptor expressed in SK-N-MC cells assessed as effect on forskolin-stimulated cAMP-mediated reporter gene activity
ChEMBL 248 6 2 4 2.1 CCCCNc1cc(N2CC[C@@H](NC)C2)ccn1 10.1016/j.bmcl.2014.12.027
CHEMBL3393529 116613 2 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human recombinant histamine H4 receptor expressed in SK-N-MC cells assessed as effect on forskolin-stimulated cAMP-mediated reporter gene activityAgonist activity at human recombinant histamine H4 receptor expressed in SK-N-MC cells assessed as effect on forskolin-stimulated cAMP-mediated reporter gene activity
ChEMBL 248 6 2 4 2.1 CCCCNc1cc(N2CC[C@@H](NC)C2)ccn1 10.1016/j.bmcl.2014.12.027
25130914 186671 0 None -15 2 Rat 6.3 pEC50 = 6.3 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 298 4 2 6 1.4 CN1CCN(c2cc(NCc3ccccc3)nc(N)n2)CC1 10.1021/jm8005959
CHEMBL492677 186671 0 None -15 2 Rat 6.3 pEC50 = 6.3 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 298 4 2 6 1.4 CN1CCN(c2cc(NCc3ccccc3)nc(N)n2)CC1 10.1021/jm8005959
25129179 187085 4 None - 1 Rat 6.3 pEC50 = 6.3 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 222 2 2 6 -0.1 CNc1cc(N2CCN(C)CC2)nc(N)n1 10.1021/jm8005959
CHEMBL495112 187085 4 None - 1 Rat 6.3 pEC50 = 6.3 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 222 2 2 6 -0.1 CNc1cc(N2CCN(C)CC2)nc(N)n1 10.1021/jm8005959
25130236 187118 0 None 1 2 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at human histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 268 1 0 4 2.2 CN1CCN(c2cc(C(C)(C)C)nc(Cl)n2)CC1 10.1021/jm8005959
CHEMBL495265 187118 0 None 1 2 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at human histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 268 1 0 4 2.2 CN1CCN(c2cc(C(C)(C)C)nc(Cl)n2)CC1 10.1021/jm8005959
25068753 187854 15 None 1 2 Mouse 8.2 pEC50 = 8.2 Functional
Antagonist activity at mouse histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assayAntagonist activity at mouse histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assay
ChEMBL 295 1 2 5 1.8 Nc1nc2c(c(N3CC[C@@H](N)C3)n1)CCCc1ccccc1-2 10.1021/jm800670r
CHEMBL502347 187854 15 None 1 2 Mouse 8.2 pEC50 = 8.2 Functional
Antagonist activity at mouse histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assayAntagonist activity at mouse histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assay
ChEMBL 295 1 2 5 1.8 Nc1nc2c(c(N3CC[C@@H](N)C3)n1)CCCc1ccccc1-2 10.1021/jm800670r
53233805 61195 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells assessed as effect on forskolin-induced cAMP accumulation after 6 hrsAgonist activity at human histamine H4 receptor expressed in human SK-N-MC cells assessed as effect on forskolin-induced cAMP accumulation after 6 hrs
ChEMBL 263 4 2 5 1.5 CC(C)CNc1cc(N2CCN(C)CC2)cc(N)n1 10.1016/j.bmcl.2011.03.017
CHEMBL1770964 61195 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells assessed as effect on forskolin-induced cAMP accumulation after 6 hrsAgonist activity at human histamine H4 receptor expressed in human SK-N-MC cells assessed as effect on forskolin-induced cAMP accumulation after 6 hrs
ChEMBL 263 4 2 5 1.5 CC(C)CNc1cc(N2CCN(C)CC2)cc(N)n1 10.1016/j.bmcl.2011.03.017
46890545 7304 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human histamine H4 receptor in SK-N-MC cells assessed as forskolin-stimulated cAMP release preincubated for 10 mins before forskolin challengeAgonist activity at human histamine H4 receptor in SK-N-MC cells assessed as forskolin-stimulated cAMP release preincubated for 10 mins before forskolin challenge
ChEMBL 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 7304 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human histamine H4 receptor in SK-N-MC cells assessed as forskolin-stimulated cAMP release preincubated for 10 mins before forskolin challengeAgonist activity at human histamine H4 receptor in SK-N-MC cells assessed as forskolin-stimulated cAMP release preincubated for 10 mins before forskolin challenge
ChEMBL 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 4001 12 None 7 4 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 161 3 4 3 -1.1 NC(=N)SCCN=C(N)N 10.1016/j.bmcl.2010.10.041
3063228 4001 12 None 7 4 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 161 3 4 3 -1.1 NC(=N)SCCN=C(N)N 10.1016/j.bmcl.2010.10.041
CHEMBL1196470 4001 12 None 7 4 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 161 3 4 3 -1.1 NC(=N)SCCN=C(N)N 10.1016/j.bmcl.2010.10.041
1274 4001 12 None 7 4 Human 7.3 pEC50 = 7.3 Functional
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 4001 12 None 7 4 Human 7.3 pEC50 = 7.3 Functional
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 4001 12 None 7 4 Human 7.3 pEC50 = 7.3 Functional
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 56187 1 None -5 3 Rat 6.3 pEC50 = 6.3 Functional
Agonist activity at rat histamine H4 receptor by luciferase reporter gene assayAgonist activity at rat histamine H4 receptor by luciferase reporter gene assay
ChEMBL 271 2 2 3 3.0 Cc1ccc2[nH]c(/C(=N\O)C3CCN(C)CC3)cc2c1 10.1016/j.bmcl.2010.10.041
CHEMBL1632412 56187 1 None -5 3 Rat 6.3 pEC50 = 6.3 Functional
Agonist activity at rat histamine H4 receptor by luciferase reporter gene assayAgonist activity at rat histamine H4 receptor by luciferase reporter gene assay
ChEMBL 271 2 2 3 3.0 Cc1ccc2[nH]c(/C(=N\O)C3CCN(C)CC3)cc2c1 10.1016/j.bmcl.2010.10.041
11313837 2464 7 None -15848 2 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 179 2 1 2 1.3 CN1CCC(CC1)Cc1[nH]cnc1 10.1016/j.bmcl.2010.10.041
1254 2464 7 None -15848 2 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 179 2 1 2 1.3 CN1CCC(CC1)Cc1[nH]cnc1 10.1016/j.bmcl.2010.10.041
CHEMBL175782 2464 7 None -15848 2 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 179 2 1 2 1.3 CN1CCC(CC1)Cc1[nH]cnc1 10.1016/j.bmcl.2010.10.041
10583206 108872 0 None -6 2 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 167 2 2 3 0.6 NC[C@@H]1CC[C@H](c2c[nH]cn2)O1 10.1016/j.bmcl.2010.10.041
CHEMBL321920 108872 0 None -6 2 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 167 2 2 3 0.6 NC[C@@H]1CC[C@H](c2c[nH]cn2)O1 10.1016/j.bmcl.2010.10.041
1204 1901 114 None -51 10 Mouse 5.3 pEC50 = 5.3 Functional
Agonist activity at mouse histamine H4 receptor by luciferase reporter gene assayAgonist activity at mouse histamine H4 receptor by luciferase reporter gene assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmcl.2010.10.041
1247 1901 114 None -51 10 Mouse 5.3 pEC50 = 5.3 Functional
Agonist activity at mouse histamine H4 receptor by luciferase reporter gene assayAgonist activity at mouse histamine H4 receptor by luciferase reporter gene assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmcl.2010.10.041
1375 1901 114 None -51 10 Mouse 5.3 pEC50 = 5.3 Functional
Agonist activity at mouse histamine H4 receptor by luciferase reporter gene assayAgonist activity at mouse histamine H4 receptor by luciferase reporter gene assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmcl.2010.10.041
774 1901 114 None -51 10 Mouse 5.3 pEC50 = 5.3 Functional
Agonist activity at mouse histamine H4 receptor by luciferase reporter gene assayAgonist activity at mouse histamine H4 receptor by luciferase reporter gene assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmcl.2010.10.041
CHEMBL90 1901 114 None -51 10 Mouse 5.3 pEC50 = 5.3 Functional
Agonist activity at mouse histamine H4 receptor by luciferase reporter gene assayAgonist activity at mouse histamine H4 receptor by luciferase reporter gene assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmcl.2010.10.041
DB05381 1901 114 None -51 10 Mouse 5.3 pEC50 = 5.3 Functional
Agonist activity at mouse histamine H4 receptor by luciferase reporter gene assayAgonist activity at mouse histamine H4 receptor by luciferase reporter gene assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmcl.2010.10.041
155513612 175746 0 None -18 3 Rat 4.3 pEC50 = 4.3 Functional
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 175746 0 None -18 3 Rat 4.3 pEC50 = 4.3 Functional
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 175746 0 None -18 3 Rat 4.3 pEC50 = 4.3 Functional
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 175746 0 None -18 3 Rat 4.3 pEC50 = 4.3 Functional
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 175667 0 None -6 3 Mouse 7.3 pEC50 = 7.3 Functional
Agonist activity at mouse H4R expressed in HEK293-SF-mH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at mouse H4R expressed in HEK293-SF-mH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 237 6 3 5 1.7 CC(C)(C)CNc1nccc(NCCCN)n1 10.1021/acs.jmedchem.9b01342
CHEMBL4437371 175667 0 None -6 3 Mouse 7.3 pEC50 = 7.3 Functional
Agonist activity at mouse H4R expressed in HEK293-SF-mH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at mouse H4R expressed in HEK293-SF-mH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 237 6 3 5 1.7 CC(C)(C)CNc1nccc(NCCCN)n1 10.1021/acs.jmedchem.9b01342
CHEMBL4594753 175667 0 None -6 3 Mouse 7.3 pEC50 = 7.3 Functional
Agonist activity at mouse H4R expressed in HEK293-SF-mH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at mouse H4R expressed in HEK293-SF-mH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 237 6 3 5 1.7 CC(C)(C)CNc1nccc(NCCCN)n1 10.1021/acs.jmedchem.9b01342
58227163 175889 0 None -4 3 Mouse 7.3 pEC50 = 7.3 Functional
Agonist activity at mouse H4R expressed in HEK293-SF-mH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at mouse H4R expressed in HEK293-SF-mH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 263 3 2 5 1.7 CC(C)(C)CNc1nccc(N2CCCNCC2)n1 10.1021/acs.jmedchem.9b01342
CHEMBL4518374 175889 0 None -4 3 Mouse 7.3 pEC50 = 7.3 Functional
Agonist activity at mouse H4R expressed in HEK293-SF-mH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at mouse H4R expressed in HEK293-SF-mH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 263 3 2 5 1.7 CC(C)(C)CNc1nccc(N2CCCNCC2)n1 10.1021/acs.jmedchem.9b01342
CHEMBL4596491 175889 0 None -4 3 Mouse 7.3 pEC50 = 7.3 Functional
Agonist activity at mouse H4R expressed in HEK293-SF-mH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at mouse H4R expressed in HEK293-SF-mH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 263 3 2 5 1.7 CC(C)(C)CNc1nccc(N2CCCNCC2)n1 10.1021/acs.jmedchem.9b01342
25130580 173730 0 None - 1 Rat 5.3 pEC50 = 5.3 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 263 2 1 5 1.6 CNc1nc(N2CCN(C)CC2)cc(C(C)(C)C)n1 10.1021/jm8005959
CHEMBL455016 173730 0 None - 1 Rat 5.3 pEC50 = 5.3 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 263 2 1 5 1.6 CNc1nc(N2CCN(C)CC2)cc(C(C)(C)C)n1 10.1021/jm8005959
25129878 186752 0 None - 1 Rat 5.3 pEC50 = 5.3 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 324 3 1 7 1.4 COc1c(-c2ccc(C#N)cc2)nc(N)nc1N1CCN(C)CC1 10.1021/jm8005959
CHEMBL493103 186752 0 None - 1 Rat 5.3 pEC50 = 5.3 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 324 3 1 7 1.4 COc1c(-c2ccc(C#N)cc2)nc(N)nc1N1CCN(C)CC1 10.1021/jm8005959
127052295 139667 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human histamine H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assayAgonist activity at human histamine H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 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 139667 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human histamine H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assayAgonist activity at human histamine H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 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 1901 114 None -97 10 Rat 4.3 pEC50 = 4.3 Functional
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 1901 114 None -97 10 Rat 4.3 pEC50 = 4.3 Functional
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 1901 114 None -97 10 Rat 4.3 pEC50 = 4.3 Functional
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 1901 114 None -97 10 Rat 4.3 pEC50 = 4.3 Functional
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 1901 114 None -97 10 Rat 4.3 pEC50 = 4.3 Functional
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 1901 114 None -97 10 Rat 4.3 pEC50 = 4.3 Functional
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 61193 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells assessed as effect on forskolin-induced cAMP accumulation after 6 hrsAgonist activity at human histamine H4 receptor expressed in human SK-N-MC cells assessed as effect on forskolin-induced cAMP accumulation after 6 hrs
ChEMBL 249 3 2 5 1.2 CC(C)Nc1cc(N2CCN(C)CC2)cc(N)n1 10.1016/j.bmcl.2011.03.017
CHEMBL1770962 61193 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells assessed as effect on forskolin-induced cAMP accumulation after 6 hrsAgonist activity at human histamine H4 receptor expressed in human SK-N-MC cells assessed as effect on forskolin-induced cAMP accumulation after 6 hrs
ChEMBL 249 3 2 5 1.2 CC(C)Nc1cc(N2CCN(C)CC2)cc(N)n1 10.1016/j.bmcl.2011.03.017
25129169 186598 0 None -1 2 Rat 7.3 pEC50 = 7.3 Functional
Antagonist activity at rat histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assayAntagonist activity at rat histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assay
ChEMBL 323 2 2 5 2.3 Nc1nc2c(c(N3CCNCC3)n1)CCCCC2c1ccccc1 10.1021/jm800670r
CHEMBL492231 186598 0 None -1 2 Rat 7.3 pEC50 = 7.3 Functional
Antagonist activity at rat histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assayAntagonist activity at rat histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assay
ChEMBL 323 2 2 5 2.3 Nc1nc2c(c(N3CCNCC3)n1)CCCCC2c1ccccc1 10.1021/jm800670r
127049856 139715 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human histamine H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assayAgonist activity at human histamine H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 368 7 3 4 3.1 N#C/N=C(/NCCSc1ccccc1)NC[C@H]1CC[C@@H](c2c[nH]cn2)C1 10.1021/acs.jmedchem.6b00120
CHEMBL3805431 139715 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human histamine H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assayAgonist activity at human histamine H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 368 7 3 4 3.1 N#C/N=C(/NCCSc1ccccc1)NC[C@H]1CC[C@@H](c2c[nH]cn2)C1 10.1021/acs.jmedchem.6b00120
90667238 108988 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human recombinant histamine H4 receptor-RGS19 fusion protein expressed in Sf9 cells coexpressing Galphai2,Gbeta1gamma2 assessed as [35S]GTPgammaS binding after 90 mins by liquid scintillation countingAgonist activity at human recombinant histamine H4 receptor-RGS19 fusion protein expressed in Sf9 cells coexpressing Galphai2,Gbeta1gamma2 assessed as [35S]GTPgammaS binding after 90 mins by liquid scintillation counting
ChEMBL 220 4 3 3 0.3 CN/C(=N/C#N)NCCCc1c[nH]c(C)n1 10.1039/C3MD00245D
CHEMBL3220639 108988 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human recombinant histamine H4 receptor-RGS19 fusion protein expressed in Sf9 cells coexpressing Galphai2,Gbeta1gamma2 assessed as [35S]GTPgammaS binding after 90 mins by liquid scintillation countingAgonist activity at human recombinant histamine H4 receptor-RGS19 fusion protein expressed in Sf9 cells coexpressing Galphai2,Gbeta1gamma2 assessed as [35S]GTPgammaS binding after 90 mins by liquid scintillation counting
ChEMBL 220 4 3 3 0.3 CN/C(=N/C#N)NCCCc1c[nH]c(C)n1 10.1039/C3MD00245D
565544 109255 9 None -4466 2 Human 6.3 pEC50 = 6.3 Functional
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 109255 9 None -4466 2 Human 6.3 pEC50 = 6.3 Functional
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 108872 0 None -6 2 Human 5.3 pEC50 = 5.3 Functional
Inhibition of the forskolin-stimulated cAMP production in SK-N-MC cells expressing human Histamine H4 receptorInhibition of the forskolin-stimulated cAMP production in SK-N-MC cells expressing human Histamine H4 receptor
ChEMBL 167 2 2 3 0.6 NC[C@@H]1CC[C@H](c2c[nH]cn2)O1 10.1021/jm0300025
CHEMBL321920 108872 0 None -6 2 Human 5.3 pEC50 = 5.3 Functional
Inhibition of the forskolin-stimulated cAMP production in SK-N-MC cells expressing human Histamine H4 receptorInhibition of the forskolin-stimulated cAMP production in SK-N-MC cells expressing human Histamine H4 receptor
ChEMBL 167 2 2 3 0.6 NC[C@@H]1CC[C@H](c2c[nH]cn2)O1 10.1021/jm0300025
25130915 186705 0 None - 1 Rat 7.3 pEC50 = 7.3 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 283 2 1 5 1.8 Cc1ccc(-c2cc(N3CCN(C)CC3)nc(N)n2)cc1 10.1021/jm8005959
CHEMBL492885 186705 0 None - 1 Rat 7.3 pEC50 = 7.3 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 283 2 1 5 1.8 Cc1ccc(-c2cc(N3CCN(C)CC3)nc(N)n2)cc1 10.1021/jm8005959
46228125 198305 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Inverse agonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of [35S]GTPgammaS bindingInverse agonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 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 198305 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Inverse agonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of [35S]GTPgammaS bindingInverse agonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 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 5548 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19 protein by steady-state GTPase assayAgonist activity at human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19 protein by steady-state GTPase assay
ChEMBL 325 9 3 4 1.8 N#C/N=C(/NCCCCc1c[nH]cn1)NCCCc1ccccn1 10.1021/jm900526h
CHEMBL1077580 5548 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19 protein by steady-state GTPase assayAgonist activity at human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19 protein by steady-state GTPase assay
ChEMBL 325 9 3 4 1.8 N#C/N=C(/NCCCCc1c[nH]cn1)NCCCc1ccccn1 10.1021/jm900526h
25131232 186707 0 None - 1 Rat 7.2 pEC50 = 7.2 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 308 2 1 6 1.7 Cc1c(-c2ccc(C#N)cc2)nc(N)nc1N1CCN(C)CC1 10.1021/jm8005959
CHEMBL492900 186707 0 None - 1 Rat 7.2 pEC50 = 7.2 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 308 2 1 6 1.7 Cc1c(-c2ccc(C#N)cc2)nc(N)nc1N1CCN(C)CC1 10.1021/jm8005959
25130235 187004 1 None -4 3 Rat 7.2 pEC50 = 7.2 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 294 2 1 6 1.3 CN1CCN(c2cc(-c3ccc(C#N)cc3)nc(N)n2)CC1 10.1021/jm8005959
CHEMBL494678 187004 1 None -4 3 Rat 7.2 pEC50 = 7.2 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 294 2 1 6 1.3 CN1CCN(c2cc(-c3ccc(C#N)cc3)nc(N)n2)CC1 10.1021/jm8005959
25130235 187004 1 None -4 3 Rat 7.2 pEC50 = 7.2 Functional
Antagonist activity at rat histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assayAntagonist activity at rat histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assay
ChEMBL 294 2 1 6 1.3 CN1CCN(c2cc(-c3ccc(C#N)cc3)nc(N)n2)CC1 10.1021/jm800670r
CHEMBL494678 187004 1 None -4 3 Rat 7.2 pEC50 = 7.2 Functional
Antagonist activity at rat histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assayAntagonist activity at rat histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assay
ChEMBL 294 2 1 6 1.3 CN1CCN(c2cc(-c3ccc(C#N)cc3)nc(N)n2)CC1 10.1021/jm800670r
45257133 198222 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 332 4 2 6 2.1 CN1CCN(c2cc(NCc3ccccc3Cl)nc(N)n2)CC1 10.1016/j.bmc.2009.08.059
CHEMBL594721 198222 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 332 4 2 6 2.1 CN1CCN(c2cc(NCc3ccccc3Cl)nc(N)n2)CC1 10.1016/j.bmc.2009.08.059
25128824 192575 0 None -1 2 Rat 8.2 pEC50 = 8.2 Functional
Antagonist activity at rat histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assayAntagonist activity at rat histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assay
ChEMBL 313 1 2 5 1.8 Nc1nc2c(c(N3CCNCC3)n1)CCCc1ccc(F)cc1-2 10.1021/jm800670r
CHEMBL523225 192575 0 None -1 2 Rat 8.2 pEC50 = 8.2 Functional
Antagonist activity at rat histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assayAntagonist activity at rat histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assay
ChEMBL 313 1 2 5 1.8 Nc1nc2c(c(N3CCNCC3)n1)CCCc1ccc(F)cc1-2 10.1021/jm800670r
155517880 176093 0 None -2 3 Mouse 8.2 pEC50 = 8.2 Functional
Agonist activity at mouse H4R expressed in HEK293-SF-mH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at mouse H4R expressed in HEK293-SF-mH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 291 4 4 5 1.0 CC(C)(C)CNc1nccc(N2CC[C@@H](NC(=N)N)C2)n1 10.1021/acs.jmedchem.9b01342
CHEMBL4445423 176093 0 None -2 3 Mouse 8.2 pEC50 = 8.2 Functional
Agonist activity at mouse H4R expressed in HEK293-SF-mH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at mouse H4R expressed in HEK293-SF-mH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 291 4 4 5 1.0 CC(C)(C)CNc1nccc(N2CC[C@@H](NC(=N)N)C2)n1 10.1021/acs.jmedchem.9b01342
CHEMBL4598198 176093 0 None -2 3 Mouse 8.2 pEC50 = 8.2 Functional
Agonist activity at mouse H4R expressed in HEK293-SF-mH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at mouse H4R expressed in HEK293-SF-mH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 291 4 4 5 1.0 CC(C)(C)CNc1nccc(N2CC[C@@H](NC(=N)N)C2)n1 10.1021/acs.jmedchem.9b01342
45269820 193679 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at histamine H4 receptor (unknown origin) expressed in HEK293T cells harboring CRE-luciferase after 6 hrs by luciferase reporter gene assayAgonist activity at histamine H4 receptor (unknown origin) expressed in HEK293T cells harboring CRE-luciferase after 6 hrs by luciferase reporter gene assay
ChEMBL 308 6 3 3 3.5 N=C(NCc1cccc(Cl)c1)SCCCc1c[nH]cn1 10.1021/acs.jmedchem.8b00435
CHEMBL1202326 193679 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at histamine H4 receptor (unknown origin) expressed in HEK293T cells harboring CRE-luciferase after 6 hrs by luciferase reporter gene assayAgonist activity at histamine H4 receptor (unknown origin) expressed in HEK293T cells harboring CRE-luciferase after 6 hrs by luciferase reporter gene assay
ChEMBL 308 6 3 3 3.5 N=C(NCc1cccc(Cl)c1)SCCCc1c[nH]cn1 10.1021/acs.jmedchem.8b00435
CHEMBL551790 193679 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at histamine H4 receptor (unknown origin) expressed in HEK293T cells harboring CRE-luciferase after 6 hrs by luciferase reporter gene assayAgonist activity at histamine H4 receptor (unknown origin) expressed in HEK293T cells harboring CRE-luciferase after 6 hrs by luciferase reporter gene assay
ChEMBL 308 6 3 3 3.5 N=C(NCc1cccc(Cl)c1)SCCCc1c[nH]cn1 10.1021/acs.jmedchem.8b00435
25071004 192116 0 None -1 2 Rat 8.2 pEC50 = 8.2 Functional
Antagonist activity at rat histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assayAntagonist activity at rat histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assay
ChEMBL 309 2 2 5 2.0 CN[C@@H]1CCN(c2nc(N)nc3c2CCCc2ccccc2-3)C1 10.1021/jm800670r
CHEMBL521996 192116 0 None -1 2 Rat 8.2 pEC50 = 8.2 Functional
Antagonist activity at rat histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assayAntagonist activity at rat histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assay
ChEMBL 309 2 2 5 2.0 CN[C@@H]1CCN(c2nc(N)nc3c2CCCc2ccccc2-3)C1 10.1021/jm800670r
46890022 6968 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human histamine H4 receptor in SK-N-MC cells assessed as forskolin-stimulated cAMP release preincubated for 10 mins before forskolin challengeAgonist activity at human histamine H4 receptor in SK-N-MC cells assessed as forskolin-stimulated cAMP release preincubated for 10 mins before forskolin challenge
ChEMBL 410 8 3 4 4.3 Cc1cc(OCCCNCC2CCCNC2)ccc1-c1nc2c(C)c(F)ccc2[nH]1 10.1016/j.bmcl.2010.04.017
CHEMBL1084869 6968 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human histamine H4 receptor in SK-N-MC cells assessed as forskolin-stimulated cAMP release preincubated for 10 mins before forskolin challengeAgonist activity at human histamine H4 receptor in SK-N-MC cells assessed as forskolin-stimulated cAMP release preincubated for 10 mins before forskolin challenge
ChEMBL 410 8 3 4 4.3 Cc1cc(OCCCNCC2CCCNC2)ccc1-c1nc2c(C)c(F)ccc2[nH]1 10.1016/j.bmcl.2010.04.017
46228158 200472 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 323 4 2 7 1.3 CN1CCN(c2cc(NCc3ccc(C#N)cc3)nc(N)n2)CC1 10.1016/j.bmc.2009.08.059
CHEMBL609289 200472 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 323 4 2 7 1.3 CN1CCN(c2cc(NCc3ccc(C#N)cc3)nc(N)n2)CC1 10.1016/j.bmc.2009.08.059
46890547 6438 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human histamine H4 receptor in SK-N-MC cells assessed as forskolin-stimulated cAMP release preincubated for 10 mins before forskolin challengeAgonist activity at human histamine H4 receptor in SK-N-MC cells assessed as forskolin-stimulated cAMP release preincubated for 10 mins before forskolin challenge
ChEMBL 396 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 6438 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human histamine H4 receptor in SK-N-MC cells assessed as forskolin-stimulated cAMP release preincubated for 10 mins before forskolin challengeAgonist activity at human histamine H4 receptor in SK-N-MC cells assessed as forskolin-stimulated cAMP release preincubated for 10 mins before forskolin challenge
ChEMBL 396 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 3146 11 None -19 2 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 216 6 1 2 2.6 C(CCc1cnc[nH]1)OCc1ccccc1 10.1016/j.bmcl.2010.10.041
6421522 3146 11 None -19 2 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 216 6 1 2 2.6 C(CCc1cnc[nH]1)OCc1ccccc1 10.1016/j.bmcl.2010.10.041
CHEMBL19173 3146 11 None -19 2 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 216 6 1 2 2.6 C(CCc1cnc[nH]1)OCc1ccccc1 10.1016/j.bmcl.2010.10.041
9974306 202769 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 336 8 3 2 3.4 S=C(NCCCCCc1c[nH]cn1)NCc1ccc(Cl)cc1 10.1016/j.bmcl.2010.10.041
CHEMBL72372 202769 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 336 8 3 2 3.4 S=C(NCCCCCc1c[nH]cn1)NCc1ccc(Cl)cc1 10.1016/j.bmcl.2010.10.041
10060212 202829 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 240 7 3 2 2.0 CCC/N=C(\S)NCCCCc1c[nH]cn1 10.1016/j.bmcl.2010.10.041
CHEMBL72769 202829 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 240 7 3 2 2.0 CCC/N=C(\S)NCCCCc1c[nH]cn1 10.1016/j.bmcl.2010.10.041
136192874 56189 0 None 1 3 Mouse 7.2 pEC50 = 7.2 Functional
Agonist activity at mouse histamine H4 receptor by luciferase reporter gene assayAgonist activity at mouse histamine H4 receptor by luciferase reporter gene assay
ChEMBL 292 2 2 4 2.7 CN1CCC(/C(=N/O)c2nc3cc(Cl)ccc3[nH]2)CC1 10.1016/j.bmcl.2010.10.041
CHEMBL1632414 56189 0 None 1 3 Mouse 7.2 pEC50 = 7.2 Functional
Agonist activity at mouse histamine H4 receptor by luciferase reporter gene assayAgonist activity at mouse histamine H4 receptor by luciferase reporter gene assay
ChEMBL 292 2 2 4 2.7 CN1CCC(/C(=N/O)c2nc3cc(Cl)ccc3[nH]2)CC1 10.1016/j.bmcl.2010.10.041
1236 2036 23 None -549 3 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 125 2 2 2 0.3 C[C@H](Cc1cnc[nH]1)N 10.1016/j.bmcl.2010.10.041
1237 2036 23 None -549 3 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 125 2 2 2 0.3 C[C@H](Cc1cnc[nH]1)N 10.1016/j.bmcl.2010.10.041
156615 2036 23 None -549 3 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 125 2 2 2 0.3 C[C@H](Cc1cnc[nH]1)N 10.1016/j.bmcl.2010.10.041
CHEMBL268229 2036 23 None -549 3 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 125 2 2 2 0.3 C[C@H](Cc1cnc[nH]1)N 10.1016/j.bmcl.2010.10.041
25129175 186796 0 None - 1 Rat 6.2 pEC50 = 6.2 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 223 2 1 6 -0.2 COc1cnc(N)nc1N1CCN(C)CC1 10.1021/jm8005959
CHEMBL493477 186796 0 None - 1 Rat 6.2 pEC50 = 6.2 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 223 2 1 6 -0.2 COc1cnc(N)nc1N1CCN(C)CC1 10.1021/jm8005959
25130914 186671 0 None 15 2 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at human histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 298 4 2 6 1.4 CN1CCN(c2cc(NCc3ccccc3)nc(N)n2)CC1 10.1021/jm8005959
CHEMBL492677 186671 0 None 15 2 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at human histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 298 4 2 6 1.4 CN1CCN(c2cc(NCc3ccccc3)nc(N)n2)CC1 10.1021/jm8005959
25130908 171285 2 None - 1 Rat 7.2 pEC50 = 7.2 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 207 1 1 5 0.1 Cc1cnc(N)nc1N1CCN(C)CC1 10.1021/jm8005959
CHEMBL446896 171285 2 None - 1 Rat 7.2 pEC50 = 7.2 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 207 1 1 5 0.1 Cc1cnc(N)nc1N1CCN(C)CC1 10.1021/jm8005959
24797775 186662 0 None - 1 Rat 7.2 pEC50 = 7.2 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 249 1 1 5 1.1 CN1CCN(c2cc(C(C)(C)C)nc(N)n2)CC1 10.1021/jm8005959
CHEMBL492631 186662 0 None - 1 Rat 7.2 pEC50 = 7.2 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 249 1 1 5 1.1 CN1CCN(c2cc(C(C)(C)C)nc(N)n2)CC1 10.1021/jm8005959
1204 1901 114 None -51 10 Mouse 5.2 pEC50 = 5.2 Functional
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 1901 114 None -51 10 Mouse 5.2 pEC50 = 5.2 Functional
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 1901 114 None -51 10 Mouse 5.2 pEC50 = 5.2 Functional
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 1901 114 None -51 10 Mouse 5.2 pEC50 = 5.2 Functional
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 1901 114 None -51 10 Mouse 5.2 pEC50 = 5.2 Functional
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 1901 114 None -51 10 Mouse 5.2 pEC50 = 5.2 Functional
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 188153 0 None - 1 Rat 7.2 pEC50 = 7.2 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 262 2 1 6 0.4 CN1CCN(c2cc(N3CCCC3)nc(N)n2)CC1 10.1021/jm8005959
CHEMBL505061 188153 0 None - 1 Rat 7.2 pEC50 = 7.2 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 262 2 1 6 0.4 CN1CCN(c2cc(N3CCCC3)nc(N)n2)CC1 10.1021/jm8005959
1204 1901 114 None -1 10 Human 8.1 pEC50 = 8.1 Functional
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 1901 114 None -1 10 Human 8.1 pEC50 = 8.1 Functional
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 1901 114 None -1 10 Human 8.1 pEC50 = 8.1 Functional
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 1901 114 None -1 10 Human 8.1 pEC50 = 8.1 Functional
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 1901 114 None -1 10 Human 8.1 pEC50 = 8.1 Functional
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 1901 114 None -1 10 Human 8.1 pEC50 = 8.1 Functional
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 178474 0 None 9 2 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human recombinant histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2 by steady-state GTPase activity assayAgonist activity at human recombinant histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2 by steady-state GTPase activity assay
ChEMBL 375 8 4 3 3.2 N=C(NCCCc1c[nH]cn1)NC(=O)CC(c1ccccc1)c1ccccc1 10.1016/j.bmcl.2010.10.041
CHEMBL471413 178474 0 None 9 2 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human recombinant histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2 by steady-state GTPase activity assayAgonist activity at human recombinant histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2 by steady-state GTPase activity assay
ChEMBL 375 8 4 3 3.2 N=C(NCCCc1c[nH]cn1)NC(=O)CC(c1ccccc1)c1ccccc1 10.1016/j.bmcl.2010.10.041
1204 1901 114 None -1 10 Human 8.1 pEC50 = 8.1 Functional
Antagonist activity at human histamine 4 receptor expressed in Sf9 cell membranes co-expressing Galphai2 and Gbeta1gamma2 assessed as [35S]GTPgammaS binding by scintillation countingAntagonist activity at human histamine 4 receptor expressed in Sf9 cell membranes co-expressing Galphai2 and Gbeta1gamma2 assessed as [35S]GTPgammaS binding by scintillation counting
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmcl.2015.12.035
1247 1901 114 None -1 10 Human 8.1 pEC50 = 8.1 Functional
Antagonist activity at human histamine 4 receptor expressed in Sf9 cell membranes co-expressing Galphai2 and Gbeta1gamma2 assessed as [35S]GTPgammaS binding by scintillation countingAntagonist activity at human histamine 4 receptor expressed in Sf9 cell membranes co-expressing Galphai2 and Gbeta1gamma2 assessed as [35S]GTPgammaS binding by scintillation counting
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmcl.2015.12.035
1375 1901 114 None -1 10 Human 8.1 pEC50 = 8.1 Functional
Antagonist activity at human histamine 4 receptor expressed in Sf9 cell membranes co-expressing Galphai2 and Gbeta1gamma2 assessed as [35S]GTPgammaS binding by scintillation countingAntagonist activity at human histamine 4 receptor expressed in Sf9 cell membranes co-expressing Galphai2 and Gbeta1gamma2 assessed as [35S]GTPgammaS binding by scintillation counting
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmcl.2015.12.035
774 1901 114 None -1 10 Human 8.1 pEC50 = 8.1 Functional
Antagonist activity at human histamine 4 receptor expressed in Sf9 cell membranes co-expressing Galphai2 and Gbeta1gamma2 assessed as [35S]GTPgammaS binding by scintillation countingAntagonist activity at human histamine 4 receptor expressed in Sf9 cell membranes co-expressing Galphai2 and Gbeta1gamma2 assessed as [35S]GTPgammaS binding by scintillation counting
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmcl.2015.12.035
CHEMBL90 1901 114 None -1 10 Human 8.1 pEC50 = 8.1 Functional
Antagonist activity at human histamine 4 receptor expressed in Sf9 cell membranes co-expressing Galphai2 and Gbeta1gamma2 assessed as [35S]GTPgammaS binding by scintillation countingAntagonist activity at human histamine 4 receptor expressed in Sf9 cell membranes co-expressing Galphai2 and Gbeta1gamma2 assessed as [35S]GTPgammaS binding by scintillation counting
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmcl.2015.12.035
DB05381 1901 114 None -1 10 Human 8.1 pEC50 = 8.1 Functional
Antagonist activity at human histamine 4 receptor expressed in Sf9 cell membranes co-expressing Galphai2 and Gbeta1gamma2 assessed as [35S]GTPgammaS binding by scintillation countingAntagonist activity at human histamine 4 receptor expressed in Sf9 cell membranes co-expressing Galphai2 and Gbeta1gamma2 assessed as [35S]GTPgammaS binding by scintillation counting
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmcl.2015.12.035
1267 3744 43 None -17 5 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1016/j.bmc.2009.08.059
3035905 3744 43 None -17 5 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1016/j.bmc.2009.08.059
CHEMBL260374 3744 43 None -17 5 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1016/j.bmc.2009.08.059
1269 121 33 None 35 6 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19 protein by steady-state GTPase assayAgonist activity at human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19 protein by steady-state GTPase assay
ChEMBL 125 2 2 2 0.2 Cc1c(CCN)nc[nH]1 10.1021/jm900526h
37463 121 33 None 35 6 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19 protein by steady-state GTPase assayAgonist activity at human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19 protein by steady-state GTPase assay
ChEMBL 125 2 2 2 0.2 Cc1c(CCN)nc[nH]1 10.1021/jm900526h
CHEMBL275443 121 33 None 35 6 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19 protein by steady-state GTPase assayAgonist activity at human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19 protein by steady-state GTPase assay
ChEMBL 125 2 2 2 0.2 Cc1c(CCN)nc[nH]1 10.1021/jm900526h
1267 3744 43 None -17 5 Human 7.2 pEC50 = 7.2 Functional
Inverse agonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of [35S]GTPgammaS bindingInverse agonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1016/j.bmc.2009.08.059
3035905 3744 43 None -17 5 Human 7.2 pEC50 = 7.2 Functional
Inverse agonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of [35S]GTPgammaS bindingInverse agonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1016/j.bmc.2009.08.059
CHEMBL260374 3744 43 None -17 5 Human 7.2 pEC50 = 7.2 Functional
Inverse agonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of [35S]GTPgammaS bindingInverse agonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1016/j.bmc.2009.08.059
44482031 5566 1 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19 protein by steady-state GTPase assayAgonist activity at human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19 protein by steady-state GTPase assay
ChEMBL 234 6 3 3 0.8 CCN/C(=N\C#N)NCCCCc1c[nH]cn1 10.1021/jm900526h
CHEMBL1077756 5566 1 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19 protein by steady-state GTPase assayAgonist activity at human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19 protein by steady-state GTPase assay
ChEMBL 234 6 3 3 0.8 CCN/C(=N\C#N)NCCCCc1c[nH]cn1 10.1021/jm900526h
46890019 7231 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human histamine H4 receptor in SK-N-MC cells assessed as forskolin-stimulated cAMP release preincubated for 10 mins before forskolin challengeAgonist activity at human histamine H4 receptor in SK-N-MC cells assessed as forskolin-stimulated cAMP release preincubated for 10 mins before forskolin challenge
ChEMBL 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 7231 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human histamine H4 receptor in SK-N-MC cells assessed as forskolin-stimulated cAMP release preincubated for 10 mins before forskolin challengeAgonist activity at human histamine H4 receptor in SK-N-MC cells assessed as forskolin-stimulated cAMP release preincubated for 10 mins before forskolin challenge
ChEMBL 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 177697 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 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 177697 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 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 177697 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 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 2119 79 None -1 4 Rat 6.1 pEC50 = 6.1 Functional
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 2119 79 None -1 4 Rat 6.1 pEC50 = 6.1 Functional
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 2119 79 None -1 4 Rat 6.1 pEC50 = 6.1 Functional
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 2119 79 None -1 4 Rat 6.1 pEC50 = 6.1 Functional
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 5081 1 None -7 2 Human 6.1 pEC50 = 6.1 Functional
Inhibition of the forskolin-stimulated cAMP production in SK-N-MC cells expressing human Histamine H4 receptorInhibition of the forskolin-stimulated cAMP production in SK-N-MC cells expressing human Histamine H4 receptor
ChEMBL 258 5 1 3 2.8 c1ccc(COC[C@H]2CC[C@H](c3c[nH]cn3)O2)cc1 10.1021/jm0300025
CHEMBL105803 5081 1 None -7 2 Human 6.1 pEC50 = 6.1 Functional
Inhibition of the forskolin-stimulated cAMP production in SK-N-MC cells expressing human Histamine H4 receptorInhibition of the forskolin-stimulated cAMP production in SK-N-MC cells expressing human Histamine H4 receptor
ChEMBL 258 5 1 3 2.8 c1ccc(COC[C@H]2CC[C@H](c3c[nH]cn3)O2)cc1 10.1021/jm0300025
58227127 116627 1 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human recombinant histamine H4 receptor expressed in SK-N-MC cells assessed as effect on forskolin-stimulated cAMP-mediated reporter gene activityAgonist activity at human recombinant histamine H4 receptor expressed in SK-N-MC cells assessed as effect on forskolin-stimulated cAMP-mediated reporter gene activity
ChEMBL 261 3 1 5 1.6 CN1CCN(c2ccnc(NC3CCCC3)n2)CC1 10.1016/j.bmcl.2014.12.027
CHEMBL3393543 116627 1 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human recombinant histamine H4 receptor expressed in SK-N-MC cells assessed as effect on forskolin-stimulated cAMP-mediated reporter gene activityAgonist activity at human recombinant histamine H4 receptor expressed in SK-N-MC cells assessed as effect on forskolin-stimulated cAMP-mediated reporter gene activity
ChEMBL 261 3 1 5 1.6 CN1CCN(c2ccnc(NC3CCCC3)n2)CC1 10.1016/j.bmcl.2014.12.027
44481489 5637 0 None 18 2 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19 protein by steady-state GTPase assayAgonist activity at human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19 protein by steady-state GTPase assay
ChEMBL 310 8 3 3 2.0 N#C/N=C(\NCCCc1ccccc1)NCCCc1c[nH]cn1 10.1021/jm900526h
CHEMBL1078210 5637 0 None 18 2 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19 protein by steady-state GTPase assayAgonist activity at human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19 protein by steady-state GTPase assay
ChEMBL 310 8 3 3 2.0 N#C/N=C(\NCCCc1ccccc1)NCCCc1c[nH]cn1 10.1021/jm900526h
10419556 5286 0 None -9 2 Human 5.1 pEC50 = 5.1 Functional
Inhibition of the forskolin-stimulated cAMP production in SK-N-MC cells expressing human Histamine H4 receptorInhibition of the forskolin-stimulated cAMP production in SK-N-MC cells expressing human Histamine H4 receptor
ChEMBL 167 2 2 3 0.6 NC[C@H]1CC[C@@H](c2c[nH]cn2)O1 10.1021/jm0300025
CHEMBL106913 5286 0 None -9 2 Human 5.1 pEC50 = 5.1 Functional
Inhibition of the forskolin-stimulated cAMP production in SK-N-MC cells expressing human Histamine H4 receptorInhibition of the forskolin-stimulated cAMP production in SK-N-MC cells expressing human Histamine H4 receptor
ChEMBL 167 2 2 3 0.6 NC[C@H]1CC[C@@H](c2c[nH]cn2)O1 10.1021/jm0300025
11086114 7313 0 None - 1 Human 5.1 pEC50 = 5.1 Functional
Inhibition of the forskolin-stimulated cAMP production in SK-N-MC cells expressing human Histamine H4 receptorInhibition of the forskolin-stimulated cAMP production in SK-N-MC cells expressing human Histamine H4 receptor
ChEMBL 248 3 3 4 0.3 C/N=C(\NC#N)NC[C@H]1CC[C@@H](c2c[nH]cn2)O1 10.1021/jm0300025
CHEMBL108649 7313 0 None - 1 Human 5.1 pEC50 = 5.1 Functional
Inhibition of the forskolin-stimulated cAMP production in SK-N-MC cells expressing human Histamine H4 receptorInhibition of the forskolin-stimulated cAMP production in SK-N-MC cells expressing human Histamine H4 receptor
ChEMBL 248 3 3 4 0.3 C/N=C(\NC#N)NC[C@H]1CC[C@@H](c2c[nH]cn2)O1 10.1021/jm0300025
10820930 5722 0 None - 1 Human 4.1 pEC50 = 4.1 Functional
Inhibition of the forskolin-stimulated cAMP production in SK-N-MC cells expressing human Histamine H4 receptorInhibition of the forskolin-stimulated cAMP production in SK-N-MC cells expressing human Histamine H4 receptor
ChEMBL 165 2 2 3 0.4 NC[C@H]1C=C[C@@H](c2c[nH]cn2)O1 10.1021/jm0300025
CHEMBL107877 5722 0 None - 1 Human 4.1 pEC50 = 4.1 Functional
Inhibition of the forskolin-stimulated cAMP production in SK-N-MC cells expressing human Histamine H4 receptorInhibition of the forskolin-stimulated cAMP production in SK-N-MC cells expressing human Histamine H4 receptor
ChEMBL 165 2 2 3 0.4 NC[C@H]1C=C[C@@H](c2c[nH]cn2)O1 10.1021/jm0300025
10106063 108783 6 None 40 2 Human 7.1 pEC50 = 7.1 Functional
Inhibition of the forskolin-stimulated cAMP production in SK-N-MC cells expressing human Histamine H4 receptorInhibition of the forskolin-stimulated cAMP production in SK-N-MC cells expressing human Histamine H4 receptor
ChEMBL 248 3 3 4 0.3 C/N=C(\NC#N)NC[C@H]1CC[C@H](c2c[nH]cn2)O1 10.1021/jm0300025
CHEMBL321860 108783 6 None 40 2 Human 7.1 pEC50 = 7.1 Functional
Inhibition of the forskolin-stimulated cAMP production in SK-N-MC cells expressing human Histamine H4 receptorInhibition of the forskolin-stimulated cAMP production in SK-N-MC cells expressing human Histamine H4 receptor
ChEMBL 248 3 3 4 0.3 C/N=C(\NC#N)NC[C@H]1CC[C@H](c2c[nH]cn2)O1 10.1021/jm0300025
10106063 108783 6 None 40 2 Human 7.1 pEC50 = 7.1 Functional
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 108783 6 None 40 2 Human 7.1 pEC50 = 7.1 Functional
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 81666 0 None 2 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human H4R-RGS19 Galphai2 Gbeta1gamma2 expressed in Sf9 cells at 0.1 nM to 1 mM by steady state GTPase activity assayAgonist activity at human H4R-RGS19 Galphai2 Gbeta1gamma2 expressed in Sf9 cells at 0.1 nM to 1 mM by steady state GTPase activity assay
ChEMBL 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 81666 0 None 2 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human H4R-RGS19 Galphai2 Gbeta1gamma2 expressed in Sf9 cells at 0.1 nM to 1 mM by steady state GTPase activity assayAgonist activity at human H4R-RGS19 Galphai2 Gbeta1gamma2 expressed in Sf9 cells at 0.1 nM to 1 mM by steady state GTPase activity assay
ChEMBL 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 108783 6 None 40 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 248 3 3 4 0.3 C/N=C(\NC#N)NC[C@H]1CC[C@H](c2c[nH]cn2)O1 10.1016/j.bmcl.2010.10.041
CHEMBL321860 108783 6 None 40 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 248 3 3 4 0.3 C/N=C(\NC#N)NC[C@H]1CC[C@H](c2c[nH]cn2)O1 10.1016/j.bmcl.2010.10.041
10017000 202780 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 288 7 3 2 2.4 S=C(NCCCCc1c[nH]cn1)NCc1ccccc1 10.1016/j.bmcl.2010.10.041
CHEMBL72431 202780 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 288 7 3 2 2.4 S=C(NCCCCc1c[nH]cn1)NCc1ccccc1 10.1016/j.bmcl.2010.10.041
1204 1901 114 None -1 10 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human recombinant histamine H4 receptor expressed in human SK-N-MC cells co-expressing SRE-Luc by luciferase reporter gene assayAgonist activity at human recombinant histamine H4 receptor expressed in human SK-N-MC cells co-expressing SRE-Luc by luciferase reporter gene assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmcl.2010.10.041
1247 1901 114 None -1 10 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human recombinant histamine H4 receptor expressed in human SK-N-MC cells co-expressing SRE-Luc by luciferase reporter gene assayAgonist activity at human recombinant histamine H4 receptor expressed in human SK-N-MC cells co-expressing SRE-Luc by luciferase reporter gene assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmcl.2010.10.041
1375 1901 114 None -1 10 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human recombinant histamine H4 receptor expressed in human SK-N-MC cells co-expressing SRE-Luc by luciferase reporter gene assayAgonist activity at human recombinant histamine H4 receptor expressed in human SK-N-MC cells co-expressing SRE-Luc by luciferase reporter gene assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmcl.2010.10.041
774 1901 114 None -1 10 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human recombinant histamine H4 receptor expressed in human SK-N-MC cells co-expressing SRE-Luc by luciferase reporter gene assayAgonist activity at human recombinant histamine H4 receptor expressed in human SK-N-MC cells co-expressing SRE-Luc by luciferase reporter gene assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmcl.2010.10.041
CHEMBL90 1901 114 None -1 10 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human recombinant histamine H4 receptor expressed in human SK-N-MC cells co-expressing SRE-Luc by luciferase reporter gene assayAgonist activity at human recombinant histamine H4 receptor expressed in human SK-N-MC cells co-expressing SRE-Luc by luciferase reporter gene assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmcl.2010.10.041
DB05381 1901 114 None -1 10 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human recombinant histamine H4 receptor expressed in human SK-N-MC cells co-expressing SRE-Luc by luciferase reporter gene assayAgonist activity at human recombinant histamine H4 receptor expressed in human SK-N-MC cells co-expressing SRE-Luc by luciferase reporter gene assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmcl.2010.10.041
136192874 56189 0 None -1 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human recombinant histamine H4 receptor expressed in human SK-N-MC cells co-expressing SRE-Luc by luciferase reporter gene assayAgonist activity at human recombinant histamine H4 receptor expressed in human SK-N-MC cells co-expressing SRE-Luc by luciferase reporter gene assay
ChEMBL 292 2 2 4 2.7 CN1CCC(/C(=N/O)c2nc3cc(Cl)ccc3[nH]2)CC1 10.1016/j.bmcl.2010.10.041
CHEMBL1632414 56189 0 None -1 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human recombinant histamine H4 receptor expressed in human SK-N-MC cells co-expressing SRE-Luc by luciferase reporter gene assayAgonist activity at human recombinant histamine H4 receptor expressed in human SK-N-MC cells co-expressing SRE-Luc by luciferase reporter gene assay
ChEMBL 292 2 2 4 2.7 CN1CCC(/C(=N/O)c2nc3cc(Cl)ccc3[nH]2)CC1 10.1016/j.bmcl.2010.10.041
1267 3744 43 None -17 5 Human 7.1 pEC50 = 7.1 Functional
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 3744 43 None -17 5 Human 7.1 pEC50 = 7.1 Functional
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 3744 43 None -17 5 Human 7.1 pEC50 = 7.1 Functional
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 2002 23 None -1995 2 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 125 3 2 2 0.2 CNCCc1cnc[nH]1 10.1016/j.bmcl.2010.10.041
1240 2002 23 None -1995 2 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 125 3 2 2 0.2 CNCCc1cnc[nH]1 10.1016/j.bmcl.2010.10.041
912 2002 23 None -1995 2 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 125 3 2 2 0.2 CNCCc1cnc[nH]1 10.1016/j.bmcl.2010.10.041
CHEMBL268490 2002 23 None -1995 2 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 125 3 2 2 0.2 CNCCc1cnc[nH]1 10.1016/j.bmcl.2010.10.041
10978141 5081 1 None -7 2 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 258 5 1 3 2.8 c1ccc(COC[C@H]2CC[C@H](c3c[nH]cn3)O2)cc1 10.1016/j.bmcl.2010.10.041
CHEMBL105803 5081 1 None -7 2 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 258 5 1 3 2.8 c1ccc(COC[C@H]2CC[C@H](c3c[nH]cn3)O2)cc1 10.1016/j.bmcl.2010.10.041
1278 2119 79 None -1 4 Mouse 6.1 pEC50 = 6.1 Functional
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 2119 79 None -1 4 Mouse 6.1 pEC50 = 6.1 Functional
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 2119 79 None -1 4 Mouse 6.1 pEC50 = 6.1 Functional
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 2119 79 None -1 4 Mouse 6.1 pEC50 = 6.1 Functional
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 180184 0 None -501 6 Mouse 6.1 pEC50 = 6.1 Functional
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 180184 0 None -501 6 Mouse 6.1 pEC50 = 6.1 Functional
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 5286 0 None -9 2 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 167 2 2 3 0.6 NC[C@H]1CC[C@@H](c2c[nH]cn2)O1 10.1016/j.bmcl.2010.10.041
CHEMBL106913 5286 0 None -9 2 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 167 2 2 3 0.6 NC[C@H]1CC[C@@H](c2c[nH]cn2)O1 10.1016/j.bmcl.2010.10.041
11086114 7313 0 None - 1 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 248 3 3 4 0.3 C/N=C(\NC#N)NC[C@H]1CC[C@@H](c2c[nH]cn2)O1 10.1016/j.bmcl.2010.10.041
CHEMBL108649 7313 0 None - 1 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 248 3 3 4 0.3 C/N=C(\NC#N)NC[C@H]1CC[C@@H](c2c[nH]cn2)O1 10.1016/j.bmcl.2010.10.041
155513612 175746 0 None -14 3 Mouse 5.1 pEC50 = 5.1 Functional
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 175746 0 None -14 3 Mouse 5.1 pEC50 = 5.1 Functional
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 175746 0 None -14 3 Mouse 5.1 pEC50 = 5.1 Functional
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 175746 0 None -14 3 Mouse 5.1 pEC50 = 5.1 Functional
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 171889 2 None -3 2 Rat 5.1 pEC50 = 5.1 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 259 2 1 7 -0.0 CN1CCN(c2cc(-n3ccnc3)nc(N)n2)CC1 10.1021/jm8005959
CHEMBL448085 171889 2 None -3 2 Rat 5.1 pEC50 = 5.1 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 259 2 1 7 -0.0 CN1CCN(c2cc(-n3ccnc3)nc(N)n2)CC1 10.1021/jm8005959
25133971 186766 2 None - 1 Rat 5.1 pEC50 = 5.1 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 249 1 1 5 1.1 CN1CCN(c2nc(N)cc(C(C)(C)C)n2)CC1 10.1021/jm8005959
CHEMBL493261 186766 2 None - 1 Rat 5.1 pEC50 = 5.1 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 249 1 1 5 1.1 CN1CCN(c2nc(N)cc(C(C)(C)C)n2)CC1 10.1021/jm8005959
25130229 188169 6 None - 1 Rat 5.1 pEC50 = 5.1 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 271 2 1 7 0.3 CN1CCN(c2cc(-c3cncnc3)nc(N)n2)CC1 10.1021/jm8005959
CHEMBL505346 188169 6 None - 1 Rat 5.1 pEC50 = 5.1 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 271 2 1 7 0.3 CN1CCN(c2cc(-c3cncnc3)nc(N)n2)CC1 10.1021/jm8005959
56954515 81653 0 None -2 3 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human H4R-RGS19 Galphai2 Gbeta1gamma2 expressed in Sf9 cells at 0.1 nM to 1 mM by steady state GTPase activity assayAgonist activity at human H4R-RGS19 Galphai2 Gbeta1gamma2 expressed in Sf9 cells at 0.1 nM to 1 mM by steady state GTPase activity assay
ChEMBL 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 81653 0 None -2 3 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human H4R-RGS19 Galphai2 Gbeta1gamma2 expressed in Sf9 cells at 0.1 nM to 1 mM by steady state GTPase activity assayAgonist activity at human H4R-RGS19 Galphai2 Gbeta1gamma2 expressed in Sf9 cells at 0.1 nM to 1 mM by steady state GTPase activity assay
ChEMBL 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 81668 0 None -4 3 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human H4R-RGS19 Galphai2 Gbeta1gamma2 expressed in Sf9 cells at 0.1 nM to 1 mM by steady state GTPase activity assayAgonist activity at human H4R-RGS19 Galphai2 Gbeta1gamma2 expressed in Sf9 cells at 0.1 nM to 1 mM by steady state GTPase activity assay
ChEMBL 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 81668 0 None -4 3 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human H4R-RGS19 Galphai2 Gbeta1gamma2 expressed in Sf9 cells at 0.1 nM to 1 mM by steady state GTPase activity assayAgonist activity at human H4R-RGS19 Galphai2 Gbeta1gamma2 expressed in Sf9 cells at 0.1 nM to 1 mM by steady state GTPase activity assay
ChEMBL 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 198226 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 312 4 2 6 1.7 Cc1ccccc1CNc1cc(N2CCN(C)CC2)nc(N)n1 10.1016/j.bmc.2009.08.059
CHEMBL594731 198226 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 312 4 2 6 1.7 Cc1ccccc1CNc1cc(N2CCN(C)CC2)nc(N)n1 10.1016/j.bmc.2009.08.059
11846298 138751 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Activity at human histamine H4 receptor transfected in SK-N-MC cells by cAMP assayActivity at human histamine H4 receptor transfected in SK-N-MC cells by cAMP assay
ChEMBL 345 0 0 4 3.9 CN1CCN(C2=Nc3cc(Cl)ccc3Oc3ccc(F)cc32)CC1 10.1021/jm051008s
CHEMBL379102 138751 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Activity at human histamine H4 receptor transfected in SK-N-MC cells by cAMP assayActivity at human histamine H4 receptor transfected in SK-N-MC cells by cAMP assay
ChEMBL 345 0 0 4 3.9 CN1CCN(C2=Nc3cc(Cl)ccc3Oc3ccc(F)cc32)CC1 10.1021/jm051008s
25129176 172192 0 None - 1 Rat 5.1 pEC50 = 5.1 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 269 2 1 5 1.5 CN1CCN(c2nc(N)ncc2-c2ccccc2)CC1 10.1021/jm8005959
CHEMBL451108 172192 0 None - 1 Rat 5.1 pEC50 = 5.1 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 269 2 1 5 1.5 CN1CCN(c2nc(N)ncc2-c2ccccc2)CC1 10.1021/jm8005959
58227388 116622 1 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human recombinant histamine H4 receptor expressed in SK-N-MC cells assessed as effect on forskolin-stimulated cAMP-mediated reporter gene activityAgonist activity at human recombinant histamine H4 receptor expressed in SK-N-MC cells assessed as effect on forskolin-stimulated cAMP-mediated reporter gene activity
ChEMBL 249 4 1 5 1.3 CC(C)CNc1nccc(N2CCN(C)CC2)n1 10.1016/j.bmcl.2014.12.027
CHEMBL3393538 116622 1 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human recombinant histamine H4 receptor expressed in SK-N-MC cells assessed as effect on forskolin-stimulated cAMP-mediated reporter gene activityAgonist activity at human recombinant histamine H4 receptor expressed in SK-N-MC cells assessed as effect on forskolin-stimulated cAMP-mediated reporter gene activity
ChEMBL 249 4 1 5 1.3 CC(C)CNc1nccc(N2CCN(C)CC2)n1 10.1016/j.bmcl.2014.12.027
1223 940 32 None -812 4 Mouse 6.1 pEC50 = 6.1 Functional
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 940 32 None -812 4 Mouse 6.1 pEC50 = 6.1 Functional
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 940 32 None -812 4 Mouse 6.1 pEC50 = 6.1 Functional
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 107721 1 None -30 2 Human 4.1 pEC50 = 4.1 Functional
Inhibition of the forskolin-stimulated cAMP production in SK-N-MC cells expressing human Histamine H4 receptorInhibition of the forskolin-stimulated cAMP production in SK-N-MC cells expressing human Histamine H4 receptor
ChEMBL 165 2 2 3 0.4 NC[C@@H]1C=C[C@@H](c2c[nH]cn2)O1 10.1021/jm0300025
CHEMBL319658 107721 1 None -30 2 Human 4.1 pEC50 = 4.1 Functional
Inhibition of the forskolin-stimulated cAMP production in SK-N-MC cells expressing human Histamine H4 receptorInhibition of the forskolin-stimulated cAMP production in SK-N-MC cells expressing human Histamine H4 receptor
ChEMBL 165 2 2 3 0.4 NC[C@@H]1C=C[C@@H](c2c[nH]cn2)O1 10.1021/jm0300025
53233801 61216 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells assessed as effect on forskolin-induced cAMP accumulation after 6 hrsAgonist activity at human histamine H4 receptor expressed in human SK-N-MC cells assessed as effect on forskolin-induced cAMP accumulation after 6 hrs
ChEMBL 264 4 2 6 0.9 CC(C)CNc1nc(N)cc(N2CCN(C)CC2)n1 10.1016/j.bmcl.2011.03.017
CHEMBL1770985 61216 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells assessed as effect on forskolin-induced cAMP accumulation after 6 hrsAgonist activity at human histamine H4 receptor expressed in human SK-N-MC cells assessed as effect on forskolin-induced cAMP accumulation after 6 hrs
ChEMBL 264 4 2 6 0.9 CC(C)CNc1nc(N)cc(N2CCN(C)CC2)n1 10.1016/j.bmcl.2011.03.017
58227252 116628 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human recombinant histamine H4 receptor expressed in SK-N-MC cells assessed as effect on forskolin-stimulated cAMP-mediated reporter gene activityAgonist activity at human recombinant histamine H4 receptor expressed in SK-N-MC cells assessed as effect on forskolin-stimulated cAMP-mediated reporter gene activity
ChEMBL 261 4 2 5 1.6 CN[C@@H]1CCN(c2ccnc(NC3CCCC3)n2)C1 10.1016/j.bmcl.2014.12.027
CHEMBL3393544 116628 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human recombinant histamine H4 receptor expressed in SK-N-MC cells assessed as effect on forskolin-stimulated cAMP-mediated reporter gene activityAgonist activity at human recombinant histamine H4 receptor expressed in SK-N-MC cells assessed as effect on forskolin-stimulated cAMP-mediated reporter gene activity
ChEMBL 261 4 2 5 1.6 CN[C@@H]1CCN(c2ccnc(NC3CCCC3)n2)C1 10.1016/j.bmcl.2014.12.027
1204 1901 114 None -51 10 Mouse 7.1 pEC50 = 7.1 Functional
Agonist activity at mouse H4R expressed in HEK293-SF-mH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at mouse H4R expressed in HEK293-SF-mH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.0c00160
1204 1901 114 None -51 10 Mouse 7.1 pEC50 = 7.1 Functional
Agonist activity at mouse H4R expressed in HEK293-SF-mH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at mouse H4R expressed in HEK293-SF-mH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.9b01342
1247 1901 114 None -51 10 Mouse 7.1 pEC50 = 7.1 Functional
Agonist activity at mouse H4R expressed in HEK293-SF-mH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at mouse H4R expressed in HEK293-SF-mH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.0c00160
1247 1901 114 None -51 10 Mouse 7.1 pEC50 = 7.1 Functional
Agonist activity at mouse H4R expressed in HEK293-SF-mH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at mouse H4R expressed in HEK293-SF-mH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.9b01342
1375 1901 114 None -51 10 Mouse 7.1 pEC50 = 7.1 Functional
Agonist activity at mouse H4R expressed in HEK293-SF-mH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at mouse H4R expressed in HEK293-SF-mH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.0c00160
1375 1901 114 None -51 10 Mouse 7.1 pEC50 = 7.1 Functional
Agonist activity at mouse H4R expressed in HEK293-SF-mH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at mouse H4R expressed in HEK293-SF-mH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.9b01342
774 1901 114 None -51 10 Mouse 7.1 pEC50 = 7.1 Functional
Agonist activity at mouse H4R expressed in HEK293-SF-mH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at mouse H4R expressed in HEK293-SF-mH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.0c00160
774 1901 114 None -51 10 Mouse 7.1 pEC50 = 7.1 Functional
Agonist activity at mouse H4R expressed in HEK293-SF-mH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at mouse H4R expressed in HEK293-SF-mH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.9b01342
CHEMBL90 1901 114 None -51 10 Mouse 7.1 pEC50 = 7.1 Functional
Agonist activity at mouse H4R expressed in HEK293-SF-mH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at mouse H4R expressed in HEK293-SF-mH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.0c00160
CHEMBL90 1901 114 None -51 10 Mouse 7.1 pEC50 = 7.1 Functional
Agonist activity at mouse H4R expressed in HEK293-SF-mH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at mouse H4R expressed in HEK293-SF-mH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.9b01342
DB05381 1901 114 None -51 10 Mouse 7.1 pEC50 = 7.1 Functional
Agonist activity at mouse H4R expressed in HEK293-SF-mH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at mouse H4R expressed in HEK293-SF-mH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.0c00160
DB05381 1901 114 None -51 10 Mouse 7.1 pEC50 = 7.1 Functional
Agonist activity at mouse H4R expressed in HEK293-SF-mH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at mouse H4R expressed in HEK293-SF-mH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.9b01342
1274 4001 12 None -199 4 Mouse 5.1 pEC50 = 5.1 Functional
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 4001 12 None -199 4 Mouse 5.1 pEC50 = 5.1 Functional
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 4001 12 None -199 4 Mouse 5.1 pEC50 = 5.1 Functional
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 187118 0 None -1 2 Rat 5.1 pEC50 = 5.1 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 268 1 0 4 2.2 CN1CCN(c2cc(C(C)(C)C)nc(Cl)n2)CC1 10.1021/jm8005959
CHEMBL495265 187118 0 None -1 2 Rat 5.1 pEC50 = 5.1 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 268 1 0 4 2.2 CN1CCN(c2cc(C(C)(C)C)nc(Cl)n2)CC1 10.1021/jm8005959
1267 3744 43 None -17 5 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of GTPase by [gamma-32P]GTP spontaneous degradation assayAgonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of GTPase by [gamma-32P]GTP spontaneous degradation assay
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1016/j.bmc.2009.08.059
3035905 3744 43 None -17 5 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of GTPase by [gamma-32P]GTP spontaneous degradation assayAgonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of GTPase by [gamma-32P]GTP spontaneous degradation assay
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1016/j.bmc.2009.08.059
CHEMBL260374 3744 43 None -17 5 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of GTPase by [gamma-32P]GTP spontaneous degradation assayAgonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of GTPase by [gamma-32P]GTP spontaneous degradation assay
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1016/j.bmc.2009.08.059
25129877 168893 0 None - 1 Rat 6.1 pEC50 = 6.1 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 395 2 1 5 2.1 CN1CCN(c2cc(-c3cccc(I)c3)nc(N)n2)CC1 10.1021/jm8005959
CHEMBL442865 168893 0 None - 1 Rat 6.1 pEC50 = 6.1 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 395 2 1 5 2.1 CN1CCN(c2cc(-c3cccc(I)c3)nc(N)n2)CC1 10.1021/jm8005959
44568847 186666 0 None - 1 Rat 5.1 pEC50 = 5.1 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 301 3 1 6 2.0 CN1CCN(c2cc(Sc3ccccc3)nc(N)n2)CC1 10.1021/jm8005959
CHEMBL492652 186666 0 None - 1 Rat 5.1 pEC50 = 5.1 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 301 3 1 6 2.0 CN1CCN(c2cc(Sc3ccccc3)nc(N)n2)CC1 10.1021/jm8005959
25101945 192504 0 None 1 2 Mouse 8.0 pEC50 = 8.0 Functional
Antagonist activity at mouse histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assayAntagonist activity at mouse histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assay
ChEMBL 295 2 2 5 1.6 CNC1CN(c2nc(N)nc3c2CCCc2ccccc2-3)C1 10.1021/jm800670r
CHEMBL522673 192504 0 None 1 2 Mouse 8.0 pEC50 = 8.0 Functional
Antagonist activity at mouse histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assayAntagonist activity at mouse histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assay
ChEMBL 295 2 2 5 1.6 CNC1CN(c2nc(N)nc3c2CCCc2ccccc2-3)C1 10.1021/jm800670r
25101945 192504 0 None -1 2 Rat 8.0 pEC50 = 8.0 Functional
Antagonist activity at rat histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assayAntagonist activity at rat histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assay
ChEMBL 295 2 2 5 1.6 CNC1CN(c2nc(N)nc3c2CCCc2ccccc2-3)C1 10.1021/jm800670r
CHEMBL522673 192504 0 None -1 2 Rat 8.0 pEC50 = 8.0 Functional
Antagonist activity at rat histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assayAntagonist activity at rat histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assay
ChEMBL 295 2 2 5 1.6 CNC1CN(c2nc(N)nc3c2CCCc2ccccc2-3)C1 10.1021/jm800670r
58227143 116625 1 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human recombinant histamine H4 receptor expressed in SK-N-MC cells assessed as effect on forskolin-stimulated cAMP-mediated reporter gene activityAgonist activity at human recombinant histamine H4 receptor expressed in SK-N-MC cells assessed as effect on forskolin-stimulated cAMP-mediated reporter gene activity
ChEMBL 249 5 1 5 1.4 CCCCNc1nccc(N2CCN(C)CC2)n1 10.1016/j.bmcl.2014.12.027
CHEMBL3393541 116625 1 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human recombinant histamine H4 receptor expressed in SK-N-MC cells assessed as effect on forskolin-stimulated cAMP-mediated reporter gene activityAgonist activity at human recombinant histamine H4 receptor expressed in SK-N-MC cells assessed as effect on forskolin-stimulated cAMP-mediated reporter gene activity
ChEMBL 249 5 1 5 1.4 CCCCNc1nccc(N2CCN(C)CC2)n1 10.1016/j.bmcl.2014.12.027
16061961 197997 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of 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 197997 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of 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 136742 1 None - 1 Human 6.0 pEC50 = 6.0 Functional
Antagonist activity at human histamine 4 receptor expressed in Sf9 cell membranes co-expressing Galphai2 and Gbeta1gamma2 assessed as [35S]GTPgammaS binding by scintillation countingAntagonist activity at human histamine 4 receptor expressed in Sf9 cell membranes co-expressing Galphai2 and Gbeta1gamma2 assessed as [35S]GTPgammaS binding by scintillation counting
ChEMBL 359 5 1 5 3.5 CN1CCN(c2cc(-c3ccccc3)nc(NCc3ccccc3)n2)CC1 10.1016/j.bmcl.2015.12.035
CHEMBL3752085 136742 1 None - 1 Human 6.0 pEC50 = 6.0 Functional
Antagonist activity at human histamine 4 receptor expressed in Sf9 cell membranes co-expressing Galphai2 and Gbeta1gamma2 assessed as [35S]GTPgammaS binding by scintillation countingAntagonist activity at human histamine 4 receptor expressed in Sf9 cell membranes co-expressing Galphai2 and Gbeta1gamma2 assessed as [35S]GTPgammaS binding by scintillation counting
ChEMBL 359 5 1 5 3.5 CN1CCN(c2cc(-c3ccccc3)nc(NCc3ccccc3)n2)CC1 10.1016/j.bmcl.2015.12.035
58227163 175889 0 None -8 3 Rat 7.0 pEC50 = 7.0 Functional
Agonist activity at rat H4R expressed in HEK293-SF-rH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at rat H4R expressed in HEK293-SF-rH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 263 3 2 5 1.7 CC(C)(C)CNc1nccc(N2CCCNCC2)n1 10.1021/acs.jmedchem.9b01342
CHEMBL4518374 175889 0 None -8 3 Rat 7.0 pEC50 = 7.0 Functional
Agonist activity at rat H4R expressed in HEK293-SF-rH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at rat H4R expressed in HEK293-SF-rH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 263 3 2 5 1.7 CC(C)(C)CNc1nccc(N2CCCNCC2)n1 10.1021/acs.jmedchem.9b01342
CHEMBL4596491 175889 0 None -8 3 Rat 7.0 pEC50 = 7.0 Functional
Agonist activity at rat H4R expressed in HEK293-SF-rH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at rat H4R expressed in HEK293-SF-rH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 263 3 2 5 1.7 CC(C)(C)CNc1nccc(N2CCCNCC2)n1 10.1021/acs.jmedchem.9b01342
25131556 188284 7 None -3 2 Rat 7.0 pEC50 = 7.0 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 300 3 1 7 0.9 COc1ncccc1-c1cc(N2CCN(C)CC2)nc(N)n1 10.1021/jm8005959
CHEMBL507063 188284 7 None -3 2 Rat 7.0 pEC50 = 7.0 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 300 3 1 7 0.9 COc1ncccc1-c1cc(N2CCN(C)CC2)nc(N)n1 10.1021/jm8005959
25128830 187130 0 None - 1 Rat 6.0 pEC50 = 6.0 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 234 1 0 4 1.5 CN1CCN(c2cc(C(C)(C)C)ncn2)CC1 10.1021/jm8005959
CHEMBL495342 187130 0 None - 1 Rat 6.0 pEC50 = 6.0 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 234 1 0 4 1.5 CN1CCN(c2cc(C(C)(C)C)ncn2)CC1 10.1021/jm8005959
127035835 136761 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Antagonist activity at human histamine 4 receptor expressed in Sf9 cell membranes co-expressing Galphai2 and Gbeta1gamma2 assessed as [35S]GTPgammaS binding by scintillation countingAntagonist activity at human histamine 4 receptor expressed in Sf9 cell membranes co-expressing Galphai2 and Gbeta1gamma2 assessed as [35S]GTPgammaS binding by scintillation counting
ChEMBL 385 4 1 5 3.6 CN1CCN(c2nc(NCc3ccccc3)nc3c2CCc2ccccc2-3)CC1 10.1016/j.bmcl.2015.12.035
CHEMBL3752270 136761 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Antagonist activity at human histamine 4 receptor expressed in Sf9 cell membranes co-expressing Galphai2 and Gbeta1gamma2 assessed as [35S]GTPgammaS binding by scintillation countingAntagonist activity at human histamine 4 receptor expressed in Sf9 cell membranes co-expressing Galphai2 and Gbeta1gamma2 assessed as [35S]GTPgammaS binding by scintillation counting
ChEMBL 385 4 1 5 3.6 CN1CCN(c2nc(NCc3ccccc3)nc3c2CCc2ccccc2-3)CC1 10.1016/j.bmcl.2015.12.035
11983344 5601 5 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19 protein by steady-state GTPase assayAgonist activity at human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19 protein by steady-state GTPase assay
ChEMBL 220 5 3 3 0.4 CN/C(=N\C#N)NCCCCc1c[nH]cn1 10.1021/jm900526h
CHEMBL1077862 5601 5 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19 protein by steady-state GTPase assayAgonist activity at human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19 protein by steady-state GTPase assay
ChEMBL 220 5 3 3 0.4 CN/C(=N\C#N)NCCCCc1c[nH]cn1 10.1021/jm900526h
25128829 186751 0 None - 1 Rat 5.0 pEC50 = 5.0 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 265 5 1 5 1.7 CN(C)CCCN(C)c1cc(C(C)(C)C)nc(N)n1 10.1021/jm8005959
CHEMBL493100 186751 0 None - 1 Rat 5.0 pEC50 = 5.0 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 265 5 1 5 1.7 CN(C)CCCN(C)c1cc(C(C)(C)C)nc(N)n1 10.1021/jm8005959
24745335 292 7 None - 1 Human 9.2 pIC50 = 9.2 Functional
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 292 7 None - 1 Human 9.2 pIC50 = 9.2 Functional
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 292 7 None - 1 Human 9.2 pIC50 = 9.2 Functional
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 292 7 None - 1 Human 9.2 pIC50 = 9.2 Functional
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 292 7 None - 1 Human 8.9 pIC50 = 8.9 Functional
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 292 7 None - 1 Human 8.9 pIC50 = 8.9 Functional
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 292 7 None - 1 Human 8.9 pIC50 = 8.9 Functional
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 292 7 None - 1 Human 8.9 pIC50 = 8.9 Functional
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 177665 0 None -3 3 Human 8.8 pIC50 = 8.8 Functional
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 177665 0 None -3 3 Human 8.8 pIC50 = 8.8 Functional
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 177665 0 None -3 3 Human 8.8 pIC50 = 8.8 Functional
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 197827 0 None - 1 Human 8.0 pIC50 = 8 Functional
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 197827 0 None - 1 Human 8.0 pIC50 = 8 Functional
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 69397 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
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 69397 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
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 79850 0 None -6 3 Human 7.0 pIC50 = 7.0 Functional
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 79850 0 None -6 3 Human 7.0 pIC50 = 7.0 Functional
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 89295 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
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 89295 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
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 89296 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
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 89296 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
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 2119 79 None 1 4 Human 7.9 pIC50 = 7.9 Functional
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 2119 79 None 1 4 Human 7.9 pIC50 = 7.9 Functional
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 2119 79 None 1 4 Human 7.9 pIC50 = 7.9 Functional
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 2119 79 None 1 4 Human 7.9 pIC50 = 7.9 Functional
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 2101 29 None 11 2 Human 6.9 pIC50 = 6.9 Functional
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 2101 29 None 11 2 Human 6.9 pIC50 = 6.9 Functional
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 2101 29 None 11 2 Human 6.9 pIC50 = 6.9 Functional
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 174731 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
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 174731 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
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 173666 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
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 173666 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
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 79937 0 None -40 2 Human 5.8 pIC50 = 5.8 Functional
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 79937 0 None -40 2 Human 5.8 pIC50 = 5.8 Functional
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 111686 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
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 111686 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
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 3744 43 None -17 5 Human 7.7 pIC50 = 7.7 Functional
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 3744 43 None -17 5 Human 7.7 pIC50 = 7.7 Functional
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 3744 43 None -17 5 Human 7.7 pIC50 = 7.7 Functional
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 2119 79 None 1 4 Human 6.7 pIC50 = 6.7 Functional
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 2119 79 None 1 4 Human 6.7 pIC50 = 6.7 Functional
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 2119 79 None 1 4 Human 6.7 pIC50 = 6.7 Functional
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 2119 79 None 1 4 Human 6.7 pIC50 = 6.7 Functional
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 2119 79 None 1 4 Human 6.7 pIC50 = 6.7 Functional
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 2119 79 None 1 4 Human 6.7 pIC50 = 6.7 Functional
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 2119 79 None 1 4 Human 6.7 pIC50 = 6.7 Functional
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 2119 79 None 1 4 Human 6.7 pIC50 = 6.7 Functional
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 15593 3 None -22 2 Human 4.7 pIC50 = 4.7 Functional
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 15593 3 None -22 2 Human 4.7 pIC50 = 4.7 Functional
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 2119 79 None 1 4 Human 6.7 pIC50 = 6.7 Functional
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 2119 79 None 1 4 Human 6.7 pIC50 = 6.7 Functional
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 2119 79 None 1 4 Human 6.7 pIC50 = 6.7 Functional
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 2119 79 None 1 4 Human 6.7 pIC50 = 6.7 Functional
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 173679 2 None - 1 Human 6.6 pIC50 = 6.6 Functional
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 173679 2 None - 1 Human 6.6 pIC50 = 6.6 Functional
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 1878 14 None 14 2 Human 7.6 pIC50 = 7.6 Functional
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 1878 14 None 14 2 Human 7.6 pIC50 = 7.6 Functional
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 1878 14 None 14 2 Human 7.6 pIC50 = 7.6 Functional
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 7894 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
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 7894 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
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 8078 0 None 3311 2 Human 8.5 pIC50 = 8.5 Functional
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 8078 0 None 3311 2 Human 8.5 pIC50 = 8.5 Functional
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 2119 79 None 1 4 Human 7.5 pIC50 = 7.5 Functional
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 2119 79 None 1 4 Human 7.5 pIC50 = 7.5 Functional
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 2119 79 None 1 4 Human 7.5 pIC50 = 7.5 Functional
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 2119 79 None 1 4 Human 7.5 pIC50 = 7.5 Functional
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 171974 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
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 171974 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
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 197875 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
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 197875 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
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 8190 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
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 8190 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
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 8079 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
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 8079 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
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 292 7 None - 1 Human 8.3 pIC50 = 8.3 Functional
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 292 7 None - 1 Human 8.3 pIC50 = 8.3 Functional
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 292 7 None - 1 Human 8.3 pIC50 = 8.3 Functional
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 292 7 None - 1 Human 8.3 pIC50 = 8.3 Functional
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 2119 79 None 1 4 Human 7.4 pIC50 = 7.4 Functional
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 2119 79 None 1 4 Human 7.4 pIC50 = 7.4 Functional
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 2119 79 None 1 4 Human 7.4 pIC50 = 7.4 Functional
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 2119 79 None 1 4 Human 7.4 pIC50 = 7.4 Functional
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 7830 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
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 7830 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
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 123396 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
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 123396 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
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 69395 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
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 69395 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
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 69394 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
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 69394 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
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 2119 79 None 1 4 Human 8.3 pIC50 = 8.3 Functional
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 2119 79 None 1 4 Human 8.3 pIC50 = 8.3 Functional
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 2119 79 None 1 4 Human 8.3 pIC50 = 8.3 Functional
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 2119 79 None 1 4 Human 8.3 pIC50 = 8.3 Functional
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 111684 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
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 111684 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
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 292 7 None - 1 Human 7.3 pIC50 = 7.3 Functional
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 292 7 None - 1 Human 7.3 pIC50 = 7.3 Functional
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 292 7 None - 1 Human 7.3 pIC50 = 7.3 Functional
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 292 7 None - 1 Human 7.3 pIC50 = 7.3 Functional
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 2101 29 None 11 2 Human 6.3 pIC50 = 6.3 Functional
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 2101 29 None 11 2 Human 6.3 pIC50 = 6.3 Functional
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 2101 29 None 11 2 Human 6.3 pIC50 = 6.3 Functional
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 123503 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
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 123503 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
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 3744 43 None -17 5 Human 6.2 pIC50 = 6.2 Functional
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 3744 43 None -17 5 Human 6.2 pIC50 = 6.2 Functional
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 3744 43 None -17 5 Human 6.2 pIC50 = 6.2 Functional
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 3744 43 None -17 5 Human 6.2 pIC50 = 6.2 Functional
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 3744 43 None -17 5 Human 6.2 pIC50 = 6.2 Functional
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 3744 43 None -17 5 Human 6.2 pIC50 = 6.2 Functional
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 172837 4 None - 1 Human 7.2 pIC50 = 7.2 Functional
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 172837 4 None - 1 Human 7.2 pIC50 = 7.2 Functional
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 1878 14 None -14 2 Mouse 6.2 pIC50 = 6.2 Functional
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 1878 14 None -14 2 Mouse 6.2 pIC50 = 6.2 Functional
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 1878 14 None -14 2 Mouse 6.2 pIC50 = 6.2 Functional
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 8162 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
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 8162 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
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 89299 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
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 89299 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
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 8022 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
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 8022 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
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 69396 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
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 69396 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
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 177665 0 None -38 3 Mouse 7.1 pIC50 = 7.1 Functional
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 177665 0 None -38 3 Mouse 7.1 pIC50 = 7.1 Functional
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 177665 0 None -38 3 Mouse 7.1 pIC50 = 7.1 Functional
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 2119 79 None 1 4 Human 7.1 pIC50 = 7.1 Functional
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 2119 79 None 1 4 Human 7.1 pIC50 = 7.1 Functional
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 2119 79 None 1 4 Human 7.1 pIC50 = 7.1 Functional
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 2119 79 None 1 4 Human 7.1 pIC50 = 7.1 Functional
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 79936 0 None -100 3 Human 6.1 pIC50 = 6.1 Functional
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 79936 0 None -100 3 Human 6.1 pIC50 = 6.1 Functional
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 89298 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
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 89298 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
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 3744 43 None -17 5 Human 6.0 pIC50 = 6.0 Functional
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 3744 43 None -17 5 Human 6.0 pIC50 = 6.0 Functional
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 3744 43 None -17 5 Human 6.0 pIC50 = 6.0 Functional
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 116631 0 None - 1 Human 10.1 pKd = 10.1 Functional
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 116631 0 None - 1 Human 10.1 pKd = 10.1 Functional
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 109644 0 None - 0 Human 10.0 pKd = 10 Functional
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 109644 0 None - 0 Human 10.0 pKd = 10 Functional
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 109635 2 None - 0 Human 9.9 pKd = 9.9 Functional
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 109635 2 None - 0 Human 9.9 pKd = 9.9 Functional
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 109637 0 None - 0 Human 9.6 pKd = 9.6 Functional
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 109637 0 None - 0 Human 9.6 pKd = 9.6 Functional
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 109636 2 None - 1 Human 9.5 pKd = 9.5 Functional
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 109636 2 None - 1 Human 9.5 pKd = 9.5 Functional
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 109658 0 None - 0 Human 9.4 pKd = 9.4 Functional
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 109658 0 None - 0 Human 9.4 pKd = 9.4 Functional
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 61211 0 None - 0 Human 9.4 pKd = 9.4 Functional
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 61211 0 None - 0 Human 9.4 pKd = 9.4 Functional
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 61210 0 None - 0 Human 9.3 pKd = 9.3 Functional
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 61210 0 None - 0 Human 9.3 pKd = 9.3 Functional
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 109639 0 None - 0 Human 9.2 pKd = 9.2 Functional
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 109639 0 None - 0 Human 9.2 pKd = 9.2 Functional
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 116610 0 None - 0 Human 9.2 pKd = 9.2 Functional
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 116610 0 None - 0 Human 9.2 pKd = 9.2 Functional
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 116616 0 None - 0 Human 9.0 pKd = 9 Functional
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 116616 0 None - 0 Human 9.0 pKd = 9 Functional
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 116619 0 None - 0 Human 9.0 pKd = 9 Functional
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 116619 0 None - 0 Human 9.0 pKd = 9 Functional
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 61232 0 None - 0 Human 8.9 pKd = 8.9 Functional
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 61232 0 None - 0 Human 8.9 pKd = 8.9 Functional
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 61200 0 None - 0 Human 8.8 pKd = 8.8 Functional
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 61200 0 None - 0 Human 8.8 pKd = 8.8 Functional
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 61202 0 None - 0 Human 8.8 pKd = 8.8 Functional
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 61202 0 None - 0 Human 8.8 pKd = 8.8 Functional
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 61223 0 None - 0 Human 8.8 pKd = 8.8 Functional
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 61223 0 None - 0 Human 8.8 pKd = 8.8 Functional
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 188153 0 None - 1 Human 8.7 pKd = 8.7 Functional
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 188153 0 None - 1 Human 8.7 pKd = 8.7 Functional
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 67706 2 None - 0 Human 8.7 pKd = 8.7 Functional
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 67706 2 None - 0 Human 8.7 pKd = 8.7 Functional
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 109648 0 None - 0 Human 8.0 pKd = 8 Functional
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 109648 0 None - 0 Human 8.0 pKd = 8 Functional
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 109651 1 None - 0 Human 8.0 pKd = 8 Functional
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 109651 1 None - 0 Human 8.0 pKd = 8 Functional
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 109655 0 None - 0 Human 8.0 pKd = 8 Functional
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 109655 0 None - 0 Human 8.0 pKd = 8 Functional
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 61208 0 None - 0 Human 8.0 pKd = 8 Functional
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 61208 0 None - 0 Human 8.0 pKd = 8 Functional
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 116637 0 None - 0 Human 8.0 pKd = 8 Functional
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 116637 0 None - 0 Human 8.0 pKd = 8 Functional
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 116640 0 None - 1 Human 8.0 pKd = 8 Functional
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 116640 0 None - 1 Human 8.0 pKd = 8 Functional
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 109636 2 None - 1 Mouse 8.0 pKd = 8 Functional
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 109636 2 None - 1 Mouse 8.0 pKd = 8 Functional
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 67759 0 None - 0 Human 8.0 pKd = 8 Functional
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 67759 0 None - 0 Human 8.0 pKd = 8 Functional
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 116516 0 None - 0 Human 8.0 pKd = 8 Functional
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 116516 0 None - 0 Human 8.0 pKd = 8 Functional
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 2111 26 None - 1 Human 7.9 pKd = 7.9 Functional
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 2111 26 None - 1 Human 7.9 pKd = 7.9 Functional
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 2111 26 None - 1 Human 7.9 pKd = 7.9 Functional
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 109652 1 None - 0 Human 7.9 pKd = 7.9 Functional
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 109652 1 None - 0 Human 7.9 pKd = 7.9 Functional
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 109653 0 None - 0 Human 7.9 pKd = 7.9 Functional
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 109653 0 None - 0 Human 7.9 pKd = 7.9 Functional
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 61190 0 None - 0 Human 7.9 pKd = 7.9 Functional
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 61190 0 None - 0 Human 7.9 pKd = 7.9 Functional
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 61221 0 None - 0 Human 7.9 pKd = 7.9 Functional
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 61221 0 None - 0 Human 7.9 pKd = 7.9 Functional
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 124531 3 None - 0 Human 7.9 pKd = 7.9 Functional
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 124531 3 None - 0 Human 7.9 pKd = 7.9 Functional
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 6511 0 None - 0 Human 7.9 pKd = 7.9 Functional
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 6511 0 None - 0 Human 7.9 pKd = 7.9 Functional
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 109310 0 None - 0 Human 6.9 pKd = 6.9 Functional
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 109310 0 None - 0 Human 6.9 pKd = 6.9 Functional
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 14796 0 None - 0 Human 6.9 pKd = 6.9 Functional
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 14796 0 None - 0 Human 6.9 pKd = 6.9 Functional
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 18687 4 None - 0 Human 6.9 pKd = 6.9 Functional
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 18687 4 None - 0 Human 6.9 pKd = 6.9 Functional
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 61203 0 None - 0 Human 7.8 pKd = 7.8 Functional
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 61203 0 None - 0 Human 7.8 pKd = 7.8 Functional
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 116634 0 None - 1 Human 7.8 pKd = 7.8 Functional
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 116634 0 None - 1 Human 7.8 pKd = 7.8 Functional
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 14521 0 None - 0 Human 7.8 pKd = 7.8 Functional
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 14521 0 None - 0 Human 7.8 pKd = 7.8 Functional
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 18751 5 None - 1 Human 7.8 pKd = 7.8 Functional
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 18751 5 None - 1 Human 7.8 pKd = 7.8 Functional
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 18730 1 None - 0 Human 6.8 pKd = 6.8 Functional
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 18730 1 None - 0 Human 6.8 pKd = 6.8 Functional
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 7210 0 None - 0 Human 6.8 pKd = 6.8 Functional
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 7210 0 None - 0 Human 6.8 pKd = 6.8 Functional
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 7235 0 None -3 4 Mouse 4.8 pKd = 4.8 Functional
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 7235 0 None -3 4 Mouse 4.8 pKd = 4.8 Functional
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 109645 0 None - 0 Human 7.7 pKd = 7.7 Functional
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 109645 0 None - 0 Human 7.7 pKd = 7.7 Functional
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 193918 0 None - 0 Human 7.7 pKd = 7.7 Functional
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 193918 0 None - 0 Human 7.7 pKd = 7.7 Functional
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 193918 0 None - 0 Human 7.7 pKd = 7.7 Functional
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 61196 0 None - 0 Human 7.7 pKd = 7.7 Functional
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 61196 0 None - 0 Human 7.7 pKd = 7.7 Functional
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 2101 29 None 11 2 Human 7.7 pKd = 7.7 Functional
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 2101 29 None 11 2 Human 7.7 pKd = 7.7 Functional
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 2101 29 None 11 2 Human 7.7 pKd = 7.7 Functional
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 18654 9 None - 0 Human 7.7 pKd = 7.7 Functional
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 18654 9 None - 0 Human 7.7 pKd = 7.7 Functional
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 19226 0 None - 0 Human 7.7 pKd = 7.7 Functional
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 19226 0 None - 0 Human 7.7 pKd = 7.7 Functional
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 72174 0 None - 0 Human 7.7 pKd = 7.7 Functional
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 72174 0 None - 0 Human 7.7 pKd = 7.7 Functional
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 96771 0 None - 0 Human 7.7 pKd = 7.7 Functional
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 96771 0 None - 0 Human 7.7 pKd = 7.7 Functional
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 168097 10 None - 0 Human 7.7 pKd = 7.7 Functional
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 168097 10 None - 0 Human 7.7 pKd = 7.7 Functional
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 109647 0 None - 0 Human 8.6 pKd = 8.6 Functional
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 109647 0 None - 0 Human 8.6 pKd = 8.6 Functional
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 109660 0 None - 0 Human 8.6 pKd = 8.6 Functional
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 109660 0 None - 0 Human 8.6 pKd = 8.6 Functional
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 109641 3 None - 1 Human 7.6 pKd = 7.6 Functional
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 109641 3 None - 1 Human 7.6 pKd = 7.6 Functional
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 109666 0 None - 0 Human 7.6 pKd = 7.6 Functional
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 109666 0 None - 0 Human 7.6 pKd = 7.6 Functional
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 140782 3 None - 0 Human 7.6 pKd = 7.6 Functional
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 140782 3 None - 0 Human 7.6 pKd = 7.6 Functional
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 6315 0 None - 2 Human 7.6 pKd = 7.6 Functional
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 6315 0 None - 2 Human 7.6 pKd = 7.6 Functional
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 115418 0 None - 1 Human 8.5 pKd = 8.5 Functional
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 115418 0 None - 1 Human 8.5 pKd = 8.5 Functional
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 109654 0 None - 0 Human 8.4 pKd = 8.4 Functional
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 109654 0 None - 0 Human 8.4 pKd = 8.4 Functional
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 19062 1 None - 0 Human 7.5 pKd = 7.5 Functional
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 19062 1 None - 0 Human 7.5 pKd = 7.5 Functional
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 72226 0 None - 0 Human 7.5 pKd = 7.5 Functional
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 72226 0 None - 0 Human 7.5 pKd = 7.5 Functional
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 116617 2 None - 0 Human 7.4 pKd = 7.4 Functional
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 116617 2 None - 0 Human 7.4 pKd = 7.4 Functional
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 19183 51 None - 0 Human 7.4 pKd = 7.4 Functional
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 19183 51 None - 0 Human 7.4 pKd = 7.4 Functional
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 109661 0 None - 0 Human 8.3 pKd = 8.3 Functional
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 109661 0 None - 0 Human 8.3 pKd = 8.3 Functional
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 2111 26 None - 1 Mouse 8.3 pKd = 8.3 Functional
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 2111 26 None - 1 Mouse 8.3 pKd = 8.3 Functional
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 2111 26 None - 1 Mouse 8.3 pKd = 8.3 Functional
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 67841 0 None - 0 Human 8.3 pKd = 8.3 Functional
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 67841 0 None - 0 Human 8.3 pKd = 8.3 Functional
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 109651 1 None - 0 Mouse 7.3 pKd = 7.3 Functional
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 109651 1 None - 0 Mouse 7.3 pKd = 7.3 Functional
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 6946 0 None - 0 Mouse 7.3 pKd = 7.3 Functional
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 6946 0 None - 0 Mouse 7.3 pKd = 7.3 Functional
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 66745 0 None - 0 Human 7.3 pKd = 7.3 Functional
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 66745 0 None - 0 Human 7.3 pKd = 7.3 Functional
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 113928 0 None - 0 Human 7.3 pKd = 7.3 Functional
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 113928 0 None - 0 Human 7.3 pKd = 7.3 Functional
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 132296 0 None - 0 Human 7.3 pKd = 7.3 Functional
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 132296 0 None - 0 Human 7.3 pKd = 7.3 Functional
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 6437 0 None - 1 Human 7.3 pKd = 7.3 Functional
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 6437 0 None - 1 Human 7.3 pKd = 7.3 Functional
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 6946 0 None - 0 Human 7.3 pKd = 7.3 Functional
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 6946 0 None - 0 Human 7.3 pKd = 7.3 Functional
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 8293 9 None - 1 Human 8.2 pKd = 8.2 Functional
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 8293 9 None - 1 Human 8.2 pKd = 8.2 Functional
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 19225 1 None - 0 Human 8.2 pKd = 8.2 Functional
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 19225 1 None - 0 Human 8.2 pKd = 8.2 Functional
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 2111 26 None - 1 Rat 7.2 pKd = 7.2 Functional
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 2111 26 None - 1 Rat 7.2 pKd = 7.2 Functional
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 2111 26 None - 1 Rat 7.2 pKd = 7.2 Functional
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 140403 3 None - 0 Human 7.2 pKd = 7.2 Functional
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 140403 3 None - 0 Human 7.2 pKd = 7.2 Functional
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 7231 0 None - 1 Human 7.2 pKd = 7.2 Functional
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 7231 0 None - 1 Human 7.2 pKd = 7.2 Functional
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 2119 79 None 1 4 Human 8.1 pKd = 8.1 Functional
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 2119 79 None 1 4 Human 8.1 pKd = 8.1 Functional
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 2119 79 None 1 4 Human 8.1 pKd = 8.1 Functional
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 2119 79 None 1 4 Human 8.1 pKd = 8.1 Functional
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 19242 3 None - 0 Human 8.1 pKd = 8.1 Functional
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 19242 3 None - 0 Human 8.1 pKd = 8.1 Functional
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 109657 0 None - 0 Human 8.1 pKd = 8.1 Functional
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 109657 0 None - 0 Human 8.1 pKd = 8.1 Functional
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 61226 0 None - 0 Human 8.1 pKd = 8.1 Functional
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 61226 0 None - 0 Human 8.1 pKd = 8.1 Functional
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 116632 0 None - 0 Human 8.1 pKd = 8.1 Functional
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 116632 0 None - 0 Human 8.1 pKd = 8.1 Functional
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 116641 0 None - 0 Human 8.1 pKd = 8.1 Functional
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 116641 0 None - 0 Human 8.1 pKd = 8.1 Functional
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 2119 79 None 1 4 Human 8.1 pKd = 8.1 Functional
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 2119 79 None 1 4 Human 8.1 pKd = 8.1 Functional
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 2119 79 None 1 4 Human 8.1 pKd = 8.1 Functional
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 2119 79 None 1 4 Human 8.1 pKd = 8.1 Functional
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 19242 3 None - 0 Human 8.1 pKd = 8.1 Functional
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 19242 3 None - 0 Human 8.1 pKd = 8.1 Functional
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 117605 4 None - 0 Human 8.1 pKd = 8.1 Functional
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 117605 4 None - 0 Human 8.1 pKd = 8.1 Functional
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 18972 1 None - 0 Human 7.1 pKd = 7.1 Functional
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 18972 1 None - 0 Human 7.1 pKd = 7.1 Functional
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 116344 1 None - 0 Human 7.1 pKd = 7.1 Functional
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 116344 1 None - 0 Human 7.1 pKd = 7.1 Functional
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 116522 0 None - 0 Human 7.1 pKd = 7.1 Functional
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 116522 0 None - 0 Human 7.1 pKd = 7.1 Functional
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 67876 0 None - 0 Human 10.5 pKi = 10.5 Functional
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 67876 0 None - 0 Human 10.5 pKi = 10.5 Functional
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 67877 0 None - 0 Human 8.8 pKi = 8.8 Functional
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 67877 0 None - 0 Human 8.8 pKi = 8.8 Functional
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 292 7 None - 1 Human 8.8 pKi = 8.8 Functional
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 292 7 None - 1 Human 8.8 pKi = 8.8 Functional
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 292 7 None - 1 Human 8.8 pKi = 8.8 Functional
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 292 7 None - 1 Human 8.8 pKi = 8.8 Functional
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 193827 0 None - 0 Human 8.8 pKi = 8.8 Functional
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 193827 0 None - 0 Human 8.8 pKi = 8.8 Functional
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 193827 0 None - 0 Human 8.8 pKi = 8.8 Functional
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 67870 0 None - 0 Human 8.0 pKi = 8 Functional
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 67870 0 None - 0 Human 8.0 pKi = 8 Functional
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 69572 0 None - 0 Human 7.9 pKi = 7.9 Functional
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 69572 0 None - 0 Human 7.9 pKi = 7.9 Functional
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 67878 0 None - 0 Human 7.9 pKi = 7.9 Functional
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 67878 0 None - 0 Human 7.9 pKi = 7.9 Functional
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 69526 0 None - 0 Human 6.9 pKi = 6.9 Functional
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 69526 0 None - 0 Human 6.9 pKi = 6.9 Functional
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 67868 0 None - 0 Human 6.8 pKi = 6.8 Functional
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 67868 0 None - 0 Human 6.8 pKi = 6.8 Functional
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 67870 0 None - 0 Human 7.8 pKi = 7.8 Functional
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 67870 0 None - 0 Human 7.8 pKi = 7.8 Functional
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 69559 0 None - 0 Human 6.7 pKi = 6.7 Functional
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 69559 0 None - 0 Human 6.7 pKi = 6.7 Functional
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 69571 0 None - 0 Human 7.7 pKi = 7.7 Functional
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 69571 0 None - 0 Human 7.7 pKi = 7.7 Functional
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 69524 0 None - 0 Human 6.7 pKi = 6.7 Functional
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 69524 0 None - 0 Human 6.7 pKi = 6.7 Functional
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 67869 0 None - 0 Human 6.6 pKi = 6.6 Functional
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 67869 0 None - 0 Human 6.6 pKi = 6.6 Functional
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 69569 0 None - 0 Human 7.6 pKi = 7.6 Functional
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 69569 0 None - 0 Human 7.6 pKi = 7.6 Functional
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 67867 0 None - 0 Human 7.6 pKi = 7.6 Functional
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 67867 0 None - 0 Human 7.6 pKi = 7.6 Functional
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 67867 0 None - 0 Human 7.6 pKi = 7.6 Functional
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 67867 0 None - 0 Human 7.6 pKi = 7.6 Functional
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 69395 0 None - 1 Human 8.5 pKi = 8.5 Functional
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 69395 0 None - 1 Human 8.5 pKi = 8.5 Functional
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 69560 0 None - 0 Human 5.5 pKi = 5.5 Functional
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 69560 0 None - 0 Human 5.5 pKi = 5.5 Functional
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 67875 0 None - 0 Human 7.4 pKi = 7.4 Functional
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 67875 0 None - 0 Human 7.4 pKi = 7.4 Functional
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 67868 0 None - 0 Human 7.4 pKi = 7.4 Functional
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 67868 0 None - 0 Human 7.4 pKi = 7.4 Functional
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 2101 29 None 11 2 Human 7.4 pKi = 7.4 Functional
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 2101 29 None 11 2 Human 7.4 pKi = 7.4 Functional
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 2101 29 None 11 2 Human 7.4 pKi = 7.4 Functional
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 2101 29 None 11 2 Human 7.4 pKi = 7.4 Functional
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 2101 29 None 11 2 Human 7.4 pKi = 7.4 Functional
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 2101 29 None 11 2 Human 7.4 pKi = 7.4 Functional
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 69394 0 None - 1 Human 8.4 pKi = 8.4 Functional
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 69394 0 None - 1 Human 8.4 pKi = 8.4 Functional
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 69561 0 None - 0 Human 5.4 pKi = 5.4 Functional
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 69561 0 None - 0 Human 5.4 pKi = 5.4 Functional
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 2119 79 None 1 4 Human 7.3 pKi = 7.3 Functional
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 2119 79 None 1 4 Human 7.3 pKi = 7.3 Functional
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 2119 79 None 1 4 Human 7.3 pKi = 7.3 Functional
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 2119 79 None 1 4 Human 7.3 pKi = 7.3 Functional
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 69396 0 None - 1 Human 8.3 pKi = 8.3 Functional
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 69396 0 None - 1 Human 8.3 pKi = 8.3 Functional
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 67869 0 None - 0 Human 7.3 pKi = 7.3 Functional
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 67869 0 None - 0 Human 7.3 pKi = 7.3 Functional
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 69567 0 None - 0 Human 7.3 pKi = 7.3 Functional
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 69567 0 None - 0 Human 7.3 pKi = 7.3 Functional
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 67874 0 None - 0 Human 6.2 pKi = 6.2 Functional
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 67874 0 None - 0 Human 6.2 pKi = 6.2 Functional
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 67874 0 None - 0 Human 6.2 pKi = 6.2 Functional
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 67874 0 None - 0 Human 6.2 pKi = 6.2 Functional
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 2119 79 None 1 4 Human 8.2 pKi = 8.2 Functional
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 2119 79 None 1 4 Human 8.2 pKi = 8.2 Functional
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 2119 79 None 1 4 Human 8.2 pKi = 8.2 Functional
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 2119 79 None 1 4 Human 8.2 pKi = 8.2 Functional
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 2119 79 None 1 4 Human 8.2 pKi = 8.2 Functional
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 2119 79 None 1 4 Human 8.2 pKi = 8.2 Functional
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 2119 79 None 1 4 Human 8.2 pKi = 8.2 Functional
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 2119 79 None 1 4 Human 8.2 pKi = 8.2 Functional
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 2119 79 None 1 4 Human 8.2 pKi = 8.2 Functional
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 2119 79 None 1 4 Human 8.2 pKi = 8.2 Functional
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 2119 79 None 1 4 Human 8.2 pKi = 8.2 Functional
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 2119 79 None 1 4 Human 8.2 pKi = 8.2 Functional
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 3744 43 None -17 5 Human 7.2 pKi = 7.2 Functional
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 3744 43 None -17 5 Human 7.2 pKi = 7.2 Functional
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 3744 43 None -17 5 Human 7.2 pKi = 7.2 Functional
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 69397 0 None - 1 Human 8.2 pKi = 8.2 Functional
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 69397 0 None - 1 Human 8.2 pKi = 8.2 Functional
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 69563 0 None - 0 Human 5.1 pKi = 5.1 Functional
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 69563 0 None - 0 Human 5.1 pKi = 5.1 Functional
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 69570 0 None - 0 Human 8.0 pKi = 8.0 Functional
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 69570 0 None - 0 Human 8.0 pKi = 8.0 Functional
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 69568 0 None - 0 Human 8.0 pKi = 8.0 Functional
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 69568 0 None - 0 Human 8.0 pKi = 8.0 Functional
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 67875 0 None - 0 Human 7.0 pKi = 7.0 Functional
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 67875 0 None - 0 Human 7.0 pKi = 7.0 Functional
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 69525 0 None - 0 Human 7.0 pKi = 7.0 Functional
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 69525 0 None - 0 Human 7.0 pKi = 7.0 Functional
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 2496 38 None -2 30 Human 8.2 pEC50 = 8.2 Functional
NoneNone
Drug Central 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
1796 2496 38 None -2 30 Human 8.2 pEC50 = 8.2 Functional
NoneNone
Drug Central 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
4184 2496 38 None -2 30 Human 8.2 pEC50 = 8.2 Functional
NoneNone
Drug Central 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
CHEMBL6437 2496 38 None -2 30 Human 8.2 pEC50 = 8.2 Functional
NoneNone
Drug Central 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
DB06148 2496 38 None -2 30 Human 8.2 pEC50 = 8.2 Functional
NoneNone
Drug Central 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
1225 1443 24 None -3 11 Human 8.2 pEC50 = 8.2 Functional
NoneNone
Drug Central 279 3 0 2 4.0 CN(CC/C=C\1/c2ccccc2OCc2c1cccc2)C None
3958 1443 24 None -3 11 Human 8.2 pEC50 = 8.2 Functional
NoneNone
Drug Central 279 3 0 2 4.0 CN(CC/C=C\1/c2ccccc2OCc2c1cccc2)C None
667477 1443 24 None -3 11 Human 8.2 pEC50 = 8.2 Functional
NoneNone
Drug Central 279 3 0 2 4.0 CN(CC/C=C\1/c2ccccc2OCc2c1cccc2)C None
CHEMBL860 1443 24 None -3 11 Human 8.2 pEC50 = 8.2 Functional
NoneNone
Drug Central 279 3 0 2 4.0 CN(CC/C=C\1/c2ccccc2OCc2c1cccc2)C None
DB01142 1443 24 None -3 11 Human 8.2 pEC50 = 8.2 Functional
NoneNone
Drug Central 279 3 0 2 4.0 CN(CC/C=C\1/c2ccccc2OCc2c1cccc2)C None
5344 172901 98 None 60 5 Human 8.3 pIC50 = 8.3 Functional
NoneNone
Drug Central 267 3 2 5 1.7 Cc1noc(NS(=O)(=O)c2ccc(N)cc2)c1C None
CHEMBL453 172901 98 None 60 5 Human 8.3 pIC50 = 8.3 Functional
NoneNone
Drug Central 267 3 2 5 1.7 Cc1noc(NS(=O)(=O)c2ccc(N)cc2)c1C None
1272 818 0 None - 1 Human 8.1 pIC50 None 8.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 15265943




Ligands Receptor Assay information Chemical information
Sel. page Common
name
GPCRdb ID #Vendors Reference
ligand
Fold selectivity
(Affinity)
# tested GPCRs
(Affinity)
Species p-value
(-log)
Type Activity
Relation
Activity
Value
Assay Type Assay Description Source Mol
weight
Rot
Bonds
H don H acc LogP Smiles DOI
51354301 58584 0 None -10 2 Human 6.0 pEC50 = 6 Binding
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 58584 0 None -10 2 Human 6.0 pEC50 = 6 Binding
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 75339 0 None - 1 Human 6.0 pEC50 = 6 Binding
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 75339 0 None - 1 Human 6.0 pEC50 = 6 Binding
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 109001 0 None - 1 Human 6.0 pEC50 = 6 Binding
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 109001 0 None - 1 Human 6.0 pEC50 = 6 Binding
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 45484 5 None - 1 Human 6.0 pEC50 = 6.0 Binding
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 45484 5 None - 1 Human 6.0 pEC50 = 6.0 Binding
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 203901 1 None -4 2 Human 5.0 pEC50 = 5.0 Binding
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 203901 1 None -4 2 Human 5.0 pEC50 = 5.0 Binding
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 175667 0 None - 2 Mouse 6.0 pEC50 = 6.0 Binding
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 175667 0 None - 2 Mouse 6.0 pEC50 = 6.0 Binding
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 175667 0 None - 2 Mouse 6.0 pEC50 = 6.0 Binding
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 3744 43 None -33 25 Human 7.0 pEC50 = 7.0 Binding
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 3744 43 None -33 25 Human 7.0 pEC50 = 7.0 Binding
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 3744 43 None -33 25 Human 7.0 pEC50 = 7.0 Binding
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 45759 3 None - 1 Human 6.0 pEC50 = 6.0 Binding
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 45759 3 None - 1 Human 6.0 pEC50 = 6.0 Binding
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 175973 0 None 1 3 Mouse 7.9 pEC50 = 7.9 Binding
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 175973 0 None 1 3 Mouse 7.9 pEC50 = 7.9 Binding
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 175973 0 None 1 3 Mouse 7.9 pEC50 = 7.9 Binding
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 1901 114 None -3 23 Human 7.9 pEC50 = 7.9 Binding
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 1901 114 None -3 23 Human 7.9 pEC50 = 7.9 Binding
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 1901 114 None -3 23 Human 7.9 pEC50 = 7.9 Binding
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 1901 114 None -3 23 Human 7.9 pEC50 = 7.9 Binding
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 1901 114 None -3 23 Human 7.9 pEC50 = 7.9 Binding
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 1901 114 None -3 23 Human 7.9 pEC50 = 7.9 Binding
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 2036 23 None -204 7 Human 6.0 pEC50 = 6.0 Binding
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 2036 23 None -204 7 Human 6.0 pEC50 = 6.0 Binding
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 2036 23 None -204 7 Human 6.0 pEC50 = 6.0 Binding
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 2036 23 None -204 7 Human 6.0 pEC50 = 6.0 Binding
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 6315 0 None - 1 Mouse 5.9 pEC50 = 5.9 Binding
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 6315 0 None - 1 Mouse 5.9 pEC50 = 5.9 Binding
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 7235 0 None -4786 2 Mouse 7.9 pEC50 = 7.9 Binding
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 7235 0 None -4786 2 Mouse 7.9 pEC50 = 7.9 Binding
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 1901 114 None -3 23 Human 7.9 pEC50 = 7.9 Binding
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 1901 114 None -3 23 Human 7.9 pEC50 = 7.9 Binding
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 1901 114 None -3 23 Human 7.9 pEC50 = 7.9 Binding
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 1901 114 None -3 23 Human 7.9 pEC50 = 7.9 Binding
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 1901 114 None -3 23 Human 7.9 pEC50 = 7.9 Binding
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 1901 114 None -3 23 Human 7.9 pEC50 = 7.9 Binding
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 1901 114 None -3 23 Human 7.9 pEC50 = 7.9 Binding
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 1901 114 None -3 23 Human 7.9 pEC50 = 7.9 Binding
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 1901 114 None -3 23 Human 7.9 pEC50 = 7.9 Binding
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 1901 114 None -3 23 Human 7.9 pEC50 = 7.9 Binding
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 1901 114 None -3 23 Human 7.9 pEC50 = 7.9 Binding
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 1901 114 None -3 23 Human 7.9 pEC50 = 7.9 Binding
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 2119 79 None -3 8 Human 7.9 pEC50 = 7.9 Binding
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 2119 79 None -3 8 Human 7.9 pEC50 = 7.9 Binding
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 2119 79 None -3 8 Human 7.9 pEC50 = 7.9 Binding
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 2119 79 None -3 8 Human 7.9 pEC50 = 7.9 Binding
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 175973 0 None 1 3 Mouse 7.9 pEC50 = 7.9 Binding
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 175973 0 None 1 3 Mouse 7.9 pEC50 = 7.9 Binding
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 175973 0 None 1 3 Mouse 7.9 pEC50 = 7.9 Binding
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 203487 2 None -14 2 Human 5.9 pEC50 = 5.9 Binding
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 203487 2 None -14 2 Human 5.9 pEC50 = 5.9 Binding
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 1901 114 None -3 23 Human 7.9 pEC50 = 7.9 Binding
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 1901 114 None -3 23 Human 7.9 pEC50 = 7.9 Binding
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 1901 114 None -3 23 Human 7.9 pEC50 = 7.9 Binding
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 1901 114 None -3 23 Human 7.9 pEC50 = 7.9 Binding
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 1901 114 None -3 23 Human 7.9 pEC50 = 7.9 Binding
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 1901 114 None -3 23 Human 7.9 pEC50 = 7.9 Binding
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 109641 3 None - 1 Human 5.9 pEC50 = 5.9 Binding
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 109641 3 None - 1 Human 5.9 pEC50 = 5.9 Binding
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 175934 0 None - 2 Mouse 6.9 pEC50 = 6.9 Binding
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 175934 0 None - 2 Mouse 6.9 pEC50 = 6.9 Binding
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 175934 0 None - 2 Mouse 6.9 pEC50 = 6.9 Binding
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 175904 0 None 38 2 Human 6.9 pEC50 = 6.9 Binding
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 175904 0 None 38 2 Human 6.9 pEC50 = 6.9 Binding
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 175904 0 None 38 2 Human 6.9 pEC50 = 6.9 Binding
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 8426 0 None - 0 Human 5.9 pEC50 = 5.9 Binding
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 8426 0 None - 0 Human 5.9 pEC50 = 5.9 Binding
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 175934 0 None 1 2 Human 7.8 pEC50 = 7.8 Binding
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 175934 0 None 1 2 Human 7.8 pEC50 = 7.8 Binding
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 175934 0 None 1 2 Human 7.8 pEC50 = 7.8 Binding
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 176093 0 None - 2 Rat 6.8 pEC50 = 6.8 Binding
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 176093 0 None - 2 Rat 6.8 pEC50 = 6.8 Binding
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 176093 0 None - 2 Rat 6.8 pEC50 = 6.8 Binding
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 183643 0 None - 1 Human 7.8 pEC50 = 7.8 Binding
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 183643 0 None - 1 Human 7.8 pEC50 = 7.8 Binding
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 183643 0 None - 1 Human 7.8 pEC50 = 7.8 Binding
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 183643 0 None - 1 Human 7.8 pEC50 = 7.8 Binding
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 183643 0 None - 1 Human 7.8 pEC50 = 7.8 Binding
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 183643 0 None - 1 Human 7.8 pEC50 = 7.8 Binding
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 194808 0 None -1 2 Human 7.8 pEC50 = 7.8 Binding
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 194808 0 None -1 2 Human 7.8 pEC50 = 7.8 Binding
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 194808 0 None -1 2 Human 7.8 pEC50 = 7.8 Binding
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 179345 0 None - 1 Human 6.8 pEC50 = 6.8 Binding
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 179345 0 None - 1 Human 6.8 pEC50 = 6.8 Binding
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 104734 5 None -190 2 Human 5.8 pEC50 = 5.8 Binding
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 104734 5 None -190 2 Human 5.8 pEC50 = 5.8 Binding
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 203533 1 None -4 2 Human 4.8 pEC50 = 4.8 Binding
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 203533 1 None -4 2 Human 4.8 pEC50 = 4.8 Binding
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 103691 2 None -64 2 Human 5.8 pEC50 = 5.8 Binding
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 103691 2 None -64 2 Human 5.8 pEC50 = 5.8 Binding
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 175973 0 None - 3 Rat 7.8 pEC50 = 7.8 Binding
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 175973 0 None - 3 Rat 7.8 pEC50 = 7.8 Binding
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 175973 0 None - 3 Rat 7.8 pEC50 = 7.8 Binding
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 139708 1 None - 4 Mouse 6.8 pEC50 = 6.8 Binding
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 139708 1 None - 4 Mouse 6.8 pEC50 = 6.8 Binding
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 175746 0 None 1 4 Human 7.7 pEC50 = 7.7 Binding
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 175746 0 None 1 4 Human 7.7 pEC50 = 7.7 Binding
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 175746 0 None 1 4 Human 7.7 pEC50 = 7.7 Binding
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 175746 0 None 1 4 Human 7.7 pEC50 = 7.7 Binding
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 179188 0 None - 1 Human 7.7 pEC50 = 7.7 Binding
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 179188 0 None - 1 Human 7.7 pEC50 = 7.7 Binding
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 175667 0 None - 2 Rat 6.7 pEC50 = 6.7 Binding
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 175667 0 None - 2 Rat 6.7 pEC50 = 6.7 Binding
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 175667 0 None - 2 Rat 6.7 pEC50 = 6.7 Binding
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 177778 0 None - 1 Human 8.6 pEC50 = 8.6 Binding
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 177778 0 None - 1 Human 8.6 pEC50 = 8.6 Binding
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 8673 0 None - 0 Human 8.6 pEC50 = 8.6 Binding
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 8673 0 None - 0 Human 8.6 pEC50 = 8.6 Binding
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 45669 5 None - 1 Human 5.7 pEC50 = 5.7 Binding
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 45669 5 None - 1 Human 5.7 pEC50 = 5.7 Binding
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 205253 31 None 1 3 Human 6.7 pEC50 = 6.7 Binding
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 205253 31 None 1 3 Human 6.7 pEC50 = 6.7 Binding
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 205253 31 None 1 3 Human 6.7 pEC50 = 6.7 Binding
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 8672 0 None - 0 Human 7.6 pEC50 = 7.6 Binding
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 8672 0 None - 0 Human 7.6 pEC50 = 7.6 Binding
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 176093 0 None - 2 Mouse 6.6 pEC50 = 6.6 Binding
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 176093 0 None - 2 Mouse 6.6 pEC50 = 6.6 Binding
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 176093 0 None - 2 Mouse 6.6 pEC50 = 6.6 Binding
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 1901 114 None -15 23 Mouse 5.6 pEC50 = 5.6 Binding
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 1901 114 None -15 23 Mouse 5.6 pEC50 = 5.6 Binding
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 1901 114 None -15 23 Mouse 5.6 pEC50 = 5.6 Binding
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 1901 114 None -15 23 Mouse 5.6 pEC50 = 5.6 Binding
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 1901 114 None -15 23 Mouse 5.6 pEC50 = 5.6 Binding
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 1901 114 None -15 23 Mouse 5.6 pEC50 = 5.6 Binding
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 1901 114 None -15 23 Mouse 5.6 pEC50 = 5.6 Binding
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 1901 114 None -15 23 Mouse 5.6 pEC50 = 5.6 Binding
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 1901 114 None -15 23 Mouse 5.6 pEC50 = 5.6 Binding
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 1901 114 None -15 23 Mouse 5.6 pEC50 = 5.6 Binding
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 1901 114 None -15 23 Mouse 5.6 pEC50 = 5.6 Binding
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 1901 114 None -15 23 Mouse 5.6 pEC50 = 5.6 Binding
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 139708 1 None 34 4 Human 7.6 pEC50 = 7.6 Binding
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 139708 1 None 34 4 Human 7.6 pEC50 = 7.6 Binding
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 95707 6 None - 1 Human 7.6 pEC50 = 7.6 Binding
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 95707 6 None - 1 Human 7.6 pEC50 = 7.6 Binding
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 2119 79 None -3 8 Human 7.6 pEC50 = 7.6 Binding
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 2119 79 None -3 8 Human 7.6 pEC50 = 7.6 Binding
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 2119 79 None -3 8 Human 7.6 pEC50 = 7.6 Binding
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 2119 79 None -3 8 Human 7.6 pEC50 = 7.6 Binding
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 175877 0 None - 2 Mouse 7.6 pEC50 = 7.6 Binding
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 175877 0 None - 2 Mouse 7.6 pEC50 = 7.6 Binding
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 175877 0 None - 2 Mouse 7.6 pEC50 = 7.6 Binding
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 175746 0 None -2 4 Rat 7.6 pEC50 = 7.6 Binding
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 175746 0 None -2 4 Rat 7.6 pEC50 = 7.6 Binding
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 175746 0 None -2 4 Rat 7.6 pEC50 = 7.6 Binding
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 175746 0 None -2 4 Rat 7.6 pEC50 = 7.6 Binding
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 179190 0 None - 0 Human 7.6 pEC50 = 7.6 Binding
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 179190 0 None - 0 Human 7.6 pEC50 = 7.6 Binding
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 3744 43 None -21 25 Mouse 7.6 pEC50 = 7.6 Binding
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 3744 43 None -21 25 Mouse 7.6 pEC50 = 7.6 Binding
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 3744 43 None -21 25 Mouse 7.6 pEC50 = 7.6 Binding
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 108981 0 None - 0 Human 5.5 pEC50 = 5.5 Binding
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 108981 0 None - 0 Human 5.5 pEC50 = 5.5 Binding
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 175877 0 None - 2 Rat 7.5 pEC50 = 7.5 Binding
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 175877 0 None - 2 Rat 7.5 pEC50 = 7.5 Binding
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 175877 0 None - 2 Rat 7.5 pEC50 = 7.5 Binding
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 180184 0 None - 1 Human 8.5 pEC50 = 8.5 Binding
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 180184 0 None - 1 Human 8.5 pEC50 = 8.5 Binding
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 178522 0 None - 1 Human 8.4 pEC50 = 8.4 Binding
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 178522 0 None - 1 Human 8.4 pEC50 = 8.4 Binding
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 203573 2 None -1 2 Human 5.5 pEC50 = 5.5 Binding
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 203573 2 None -1 2 Human 5.5 pEC50 = 5.5 Binding
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 203974 11 None -36 2 Human 4.5 pEC50 = 4.5 Binding
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 203974 11 None -36 2 Human 4.5 pEC50 = 4.5 Binding
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 189102 0 None - 0 Human 7.5 pEC50 = 7.5 Binding
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 189102 0 None - 0 Human 7.5 pEC50 = 7.5 Binding
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 1901 114 None -3 23 Human 7.5 pEC50 = 7.5 Binding
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 1901 114 None -3 23 Human 7.5 pEC50 = 7.5 Binding
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 1901 114 None -3 23 Human 7.5 pEC50 = 7.5 Binding
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 1901 114 None -3 23 Human 7.5 pEC50 = 7.5 Binding
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 1901 114 None -3 23 Human 7.5 pEC50 = 7.5 Binding
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 1901 114 None -3 23 Human 7.5 pEC50 = 7.5 Binding
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 1901 114 None -3 23 Human 7.5 pEC50 = 7.5 Binding
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 1901 114 None -3 23 Human 7.5 pEC50 = 7.5 Binding
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 1901 114 None -3 23 Human 7.5 pEC50 = 7.5 Binding
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 1901 114 None -3 23 Human 7.5 pEC50 = 7.5 Binding
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 1901 114 None -3 23 Human 7.5 pEC50 = 7.5 Binding
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 1901 114 None -3 23 Human 7.5 pEC50 = 7.5 Binding
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 175934 0 None - 2 Rat 7.5 pEC50 = 7.5 Binding
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 175934 0 None - 2 Rat 7.5 pEC50 = 7.5 Binding
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 175934 0 None - 2 Rat 7.5 pEC50 = 7.5 Binding
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 175904 0 None - 2 Rat 6.5 pEC50 = 6.5 Binding
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 175904 0 None - 2 Rat 6.5 pEC50 = 6.5 Binding
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 175904 0 None - 2 Rat 6.5 pEC50 = 6.5 Binding
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 175889 0 None - 2 Mouse 6.5 pEC50 = 6.5 Binding
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 175889 0 None - 2 Mouse 6.5 pEC50 = 6.5 Binding
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 175889 0 None - 2 Mouse 6.5 pEC50 = 6.5 Binding
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 139717 0 None - 2 Mouse 5.4 pEC50 = 5.4 Binding
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 139717 0 None - 2 Mouse 5.4 pEC50 = 5.4 Binding
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 1901 114 None -12 23 Rat 5.4 pEC50 = 5.4 Binding
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 1901 114 None -12 23 Rat 5.4 pEC50 = 5.4 Binding
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 1901 114 None -12 23 Rat 5.4 pEC50 = 5.4 Binding
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 1901 114 None -12 23 Rat 5.4 pEC50 = 5.4 Binding
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 1901 114 None -12 23 Rat 5.4 pEC50 = 5.4 Binding
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 1901 114 None -12 23 Rat 5.4 pEC50 = 5.4 Binding
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 193679 0 None -1 2 Human 7.4 pEC50 = 7.4 Binding
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 193679 0 None -1 2 Human 7.4 pEC50 = 7.4 Binding
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 193679 0 None -1 2 Human 7.4 pEC50 = 7.4 Binding
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 175667 0 None 154 2 Human 7.4 pEC50 = 7.4 Binding
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 175667 0 None 154 2 Human 7.4 pEC50 = 7.4 Binding
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 175667 0 None 154 2 Human 7.4 pEC50 = 7.4 Binding
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 43823 12 None - 1 Human 5.4 pEC50 = 5.4 Binding
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 43823 12 None - 1 Human 5.4 pEC50 = 5.4 Binding
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 175973 0 None -2 3 Human 8.4 pEC50 = 8.4 Binding
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 175973 0 None -2 3 Human 8.4 pEC50 = 8.4 Binding
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 175973 0 None -2 3 Human 8.4 pEC50 = 8.4 Binding
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 8675 0 None - 0 Human 8.3 pEC50 = 8.3 Binding
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 8675 0 None - 0 Human 8.3 pEC50 = 8.3 Binding
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 169206 0 None - 1 Human 8.3 pEC50 = 8.3 Binding
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 169206 0 None - 1 Human 8.3 pEC50 = 8.3 Binding
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 168635 3 None - 1 Human 6.4 pEC50 = 6.4 Binding
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 168635 3 None - 1 Human 6.4 pEC50 = 6.4 Binding
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 175889 0 None 40 2 Human 7.4 pEC50 = 7.4 Binding
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 175889 0 None 40 2 Human 7.4 pEC50 = 7.4 Binding
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 175889 0 None 40 2 Human 7.4 pEC50 = 7.4 Binding
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 175746 0 None -1 4 Mouse 7.3 pEC50 = 7.3 Binding
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 175746 0 None -1 4 Mouse 7.3 pEC50 = 7.3 Binding
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 175746 0 None -1 4 Mouse 7.3 pEC50 = 7.3 Binding
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 175746 0 None -1 4 Mouse 7.3 pEC50 = 7.3 Binding
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 177665 0 None -22 4 Mouse 7.3 pEC50 = 7.3 Binding
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 177665 0 None -22 4 Mouse 7.3 pEC50 = 7.3 Binding
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 177665 0 None -22 4 Mouse 7.3 pEC50 = 7.3 Binding
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 139698 0 None -1 4 Human 6.3 pEC50 = 6.3 Binding
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 139698 0 None -1 4 Human 6.3 pEC50 = 6.3 Binding
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 1979 29 None -40 6 Human 7.3 pEC50 = 7.3 Binding
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 1979 29 None -40 6 Human 7.3 pEC50 = 7.3 Binding
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 1979 29 None -40 6 Human 7.3 pEC50 = 7.3 Binding
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 1979 29 None -40 6 Human 7.3 pEC50 = 7.3 Binding
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 175746 0 None -1 4 Mouse 7.3 pEC50 = 7.3 Binding
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 175746 0 None -1 4 Mouse 7.3 pEC50 = 7.3 Binding
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 175746 0 None -1 4 Mouse 7.3 pEC50 = 7.3 Binding
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 175746 0 None -1 4 Mouse 7.3 pEC50 = 7.3 Binding
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 139670 0 None - 2 Mouse 6.3 pEC50 = 6.3 Binding
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 139670 0 None - 2 Mouse 6.3 pEC50 = 6.3 Binding
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 1901 114 None -3 23 Human 7.3 pEC50 = 7.3 Binding
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 1901 114 None -3 23 Human 7.3 pEC50 = 7.3 Binding
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 1901 114 None -3 23 Human 7.3 pEC50 = 7.3 Binding
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 1901 114 None -3 23 Human 7.3 pEC50 = 7.3 Binding
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 1901 114 None -3 23 Human 7.3 pEC50 = 7.3 Binding
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 1901 114 None -3 23 Human 7.3 pEC50 = 7.3 Binding
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 6526 0 None - 1 Mouse 6.3 pEC50 = 6.3 Binding
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 6526 0 None - 1 Mouse 6.3 pEC50 = 6.3 Binding
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 1983 34 None -100 5 Human 7.3 pEC50 = 7.3 Binding
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 1983 34 None -100 5 Human 7.3 pEC50 = 7.3 Binding
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 1983 34 None -100 5 Human 7.3 pEC50 = 7.3 Binding
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 1983 34 None -100 5 Human 7.3 pEC50 = 7.3 Binding
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 1983 34 None -100 5 Human 7.3 pEC50 = 7.3 Binding
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 1983 34 None -100 5 Human 7.3 pEC50 = 7.3 Binding
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 103936 9 None -10 2 Human 4.2 pEC50 = 4.2 Binding
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 103936 9 None -10 2 Human 4.2 pEC50 = 4.2 Binding
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 139698 0 None - 4 Mouse 6.2 pEC50 = 6.2 Binding
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 139698 0 None - 4 Mouse 6.2 pEC50 = 6.2 Binding
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 187852 0 None - 0 Human 8.2 pEC50 = 8.2 Binding
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 187852 0 None - 0 Human 8.2 pEC50 = 8.2 Binding
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 175877 0 None 7 2 Human 8.2 pEC50 = 8.2 Binding
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 175877 0 None 7 2 Human 8.2 pEC50 = 8.2 Binding
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 175877 0 None 7 2 Human 8.2 pEC50 = 8.2 Binding
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 8424 0 None - 0 Human 5.2 pEC50 = 5.2 Binding
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 8424 0 None - 0 Human 5.2 pEC50 = 5.2 Binding
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 139670 0 None 5 2 Human 7.2 pEC50 = 7.2 Binding
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 139670 0 None 5 2 Human 7.2 pEC50 = 7.2 Binding
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 186671 0 None - 1 Human 7.2 pEC50 = 7.2 Binding
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 186671 0 None - 1 Human 7.2 pEC50 = 7.2 Binding
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 177697 0 None -58 4 Human 7.2 pEC50 = 7.2 Binding
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 177697 0 None -58 4 Human 7.2 pEC50 = 7.2 Binding
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 177697 0 None -58 4 Human 7.2 pEC50 = 7.2 Binding
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 175889 0 None - 2 Rat 6.2 pEC50 = 6.2 Binding
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 175889 0 None - 2 Rat 6.2 pEC50 = 6.2 Binding
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 175889 0 None - 2 Rat 6.2 pEC50 = 6.2 Binding
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 178621 0 None - 1 Human 7.2 pEC50 = 7.2 Binding
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 178621 0 None - 1 Human 7.2 pEC50 = 7.2 Binding
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 156823 0 None - 1 Human 5.2 pEC50 = 5.2 Binding
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 156823 0 None - 1 Human 5.2 pEC50 = 5.2 Binding
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 188997 0 None - 1 Human 8.2 pEC50 = 8.2 Binding
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 188997 0 None - 1 Human 8.2 pEC50 = 8.2 Binding
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 109636 2 None -19 3 Mouse 8.1 pEC50 = 8.1 Binding
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 109636 2 None -19 3 Mouse 8.1 pEC50 = 8.1 Binding
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 28682 2 None - 2 Human 5.2 pEC50 = 5.2 Binding
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 28682 2 None - 2 Human 5.2 pEC50 = 5.2 Binding
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 45503 3 None - 1 Human 6.1 pEC50 = 6.1 Binding
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 45503 3 None - 1 Human 6.1 pEC50 = 6.1 Binding
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 1901 114 None -3 23 Human 7.1 pEC50 = 7.1 Binding
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 1901 114 None -3 23 Human 7.1 pEC50 = 7.1 Binding
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 1901 114 None -3 23 Human 7.1 pEC50 = 7.1 Binding
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 1901 114 None -3 23 Human 7.1 pEC50 = 7.1 Binding
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 1901 114 None -3 23 Human 7.1 pEC50 = 7.1 Binding
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 1901 114 None -3 23 Human 7.1 pEC50 = 7.1 Binding
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 108982 0 None - 0 Human 6.1 pEC50 = 6.1 Binding
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 108982 0 None - 0 Human 6.1 pEC50 = 6.1 Binding
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 95040 2 None - 1 Human 5.1 pEC50 = 5.1 Binding
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 95040 2 None - 1 Human 5.1 pEC50 = 5.1 Binding
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 110079 7 None - 0 Human 8.1 pEC50 = 8.1 Binding
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 110079 7 None - 0 Human 8.1 pEC50 = 8.1 Binding
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 8674 0 None - 0 Human 8.1 pEC50 = 8.1 Binding
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 8674 0 None - 0 Human 8.1 pEC50 = 8.1 Binding
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 178474 0 None - 1 Human 8.1 pEC50 = 8.1 Binding
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 178474 0 None - 1 Human 8.1 pEC50 = 8.1 Binding
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 175904 0 None - 2 Mouse 6.1 pEC50 = 6.1 Binding
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 175904 0 None - 2 Mouse 6.1 pEC50 = 6.1 Binding
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 175904 0 None - 2 Mouse 6.1 pEC50 = 6.1 Binding
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 176093 0 None 16 2 Human 7.1 pEC50 = 7.1 Binding
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 176093 0 None 16 2 Human 7.1 pEC50 = 7.1 Binding
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 176093 0 None 16 2 Human 7.1 pEC50 = 7.1 Binding
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 1978 14 None -3 3 Human 7.1 pEC50 = 7.1 Binding
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 1978 14 None -3 3 Human 7.1 pEC50 = 7.1 Binding
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 1978 14 None -3 3 Human 7.1 pEC50 = 7.1 Binding
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 1978 14 None -3 3 Human 7.1 pEC50 = 7.1 Binding
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 1978 14 None -3 3 Human 7.1 pEC50 = 7.1 Binding
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 1978 14 None -3 3 Human 7.1 pEC50 = 7.1 Binding
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 1901 114 None -3 23 Human 8.0 pEC50 = 8.0 Binding
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 1901 114 None -3 23 Human 8.0 pEC50 = 8.0 Binding
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 1901 114 None -3 23 Human 8.0 pEC50 = 8.0 Binding
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 1901 114 None -3 23 Human 8.0 pEC50 = 8.0 Binding
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 1901 114 None -3 23 Human 8.0 pEC50 = 8.0 Binding
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 1901 114 None -3 23 Human 8.0 pEC50 = 8.0 Binding
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 1984 14 None -301 2 Human 6.0 pEC50 = 6.0 Binding
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 1984 14 None -301 2 Human 6.0 pEC50 = 6.0 Binding
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 1984 14 None -301 2 Human 6.0 pEC50 = 6.0 Binding
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 1901 114 None -15 23 Mouse 7.0 pEC50 = 7.0 Binding
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 1901 114 None -15 23 Mouse 7.0 pEC50 = 7.0 Binding
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 1901 114 None -15 23 Mouse 7.0 pEC50 = 7.0 Binding
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 1901 114 None -15 23 Mouse 7.0 pEC50 = 7.0 Binding
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 1901 114 None -15 23 Mouse 7.0 pEC50 = 7.0 Binding
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 1901 114 None -15 23 Mouse 7.0 pEC50 = 7.0 Binding
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 8078 0 None - 1 Human 9.0 pIC50 = 9 Binding
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 8078 0 None - 1 Human 9.0 pIC50 = 9 Binding
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 8330 0 None - 0 Human 6.0 pIC50 = 6 Binding
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 8330 0 None - 0 Human 6.0 pIC50 = 6 Binding
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 61000 8 None - 4 Human 5.0 pIC50 = 5 Binding
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 61000 8 None - 4 Human 5.0 pIC50 = 5 Binding
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 8161 0 None - 0 Human 5.0 pIC50 = 5 Binding
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 8161 0 None - 0 Human 5.0 pIC50 = 5 Binding
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 182529 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
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 182529 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
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 160418 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
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 160418 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
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 1404 79 None -194 13 Human 5.0 pIC50 = 5.0 Binding
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 1404 79 None -194 13 Human 5.0 pIC50 = 5.0 Binding
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 1404 79 None -194 13 Human 5.0 pIC50 = 5.0 Binding
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 1404 79 None -194 13 Human 5.0 pIC50 = 5.0 Binding
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 1404 79 None -194 13 Human 5.0 pIC50 = 5.0 Binding
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 1404 79 None -194 13 Human 5.0 pIC50 = 5.0 Binding
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 8162 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
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 8162 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
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 181577 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
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 181577 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
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 7895 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
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 7895 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
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 8079 0 None - 1 Human 7.9 pIC50 = 7.9 Binding
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 8079 0 None - 1 Human 7.9 pIC50 = 7.9 Binding
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 182363 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
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 182363 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
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 7888 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
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 7888 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
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 7889 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
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 7889 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
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 8191 0 None - 0 Human 4.9 pIC50 = 4.9 Binding
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 8191 0 None - 0 Human 4.9 pIC50 = 4.9 Binding
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 177665 0 None -7 4 Human 7.8 pIC50 = 7.8 Binding
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 177665 0 None -7 4 Human 7.8 pIC50 = 7.8 Binding
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 177665 0 None -7 4 Human 7.8 pIC50 = 7.8 Binding
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 8020 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
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 8020 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
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 1362 106 None -5888 15 Human 4.8 pIC50 = 4.8 Binding
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 1362 106 None -5888 15 Human 4.8 pIC50 = 4.8 Binding
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 1362 106 None -5888 15 Human 4.8 pIC50 = 4.8 Binding
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 1362 106 None -5888 15 Human 4.8 pIC50 = 4.8 Binding
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 1362 106 None -5888 15 Human 4.8 pIC50 = 4.8 Binding
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 8262 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
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 8262 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
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 182185 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
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 182185 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
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 182852 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
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 182852 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
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 8110 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
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 8110 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
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 182137 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
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 182137 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
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 8293 9 None - 1 Human 7.7 pIC50 = 7.7 Binding
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 8293 9 None - 1 Human 7.7 pIC50 = 7.7 Binding
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 8160 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
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 8160 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
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 13962 16 None - 1 Human 5.7 pIC50 = 5.7 Binding
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 13962 16 None - 1 Human 5.7 pIC50 = 5.7 Binding
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 7639 0 None - 0 Human 4.7 pIC50 = 4.7 Binding
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 7639 0 None - 0 Human 4.7 pIC50 = 4.7 Binding
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 2151 44 None -21379 20 Human 4.7 pIC50 = 4.7 Binding
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 2151 44 None -21379 20 Human 4.7 pIC50 = 4.7 Binding
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 2151 44 None -21379 20 Human 4.7 pIC50 = 4.7 Binding
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 2151 44 None -21379 20 Human 4.7 pIC50 = 4.7 Binding
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 2151 44 None -21379 20 Human 4.7 pIC50 = 4.7 Binding
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 181290 5 None - 0 Human 7.7 pIC50 = 7.7 Binding
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 181290 5 None - 0 Human 7.7 pIC50 = 7.7 Binding
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 102468 10 None - 0 Human 5.6 pIC50 = 5.6 Binding
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 102468 10 None - 0 Human 5.6 pIC50 = 5.6 Binding
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 146826 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
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 146826 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
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 7915 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
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 7915 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
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 181278 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
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 181278 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
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 182408 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
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 182408 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
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 1878 14 None - 0 Human 7.6 pIC50 = 7.6 Binding
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 1878 14 None - 0 Human 7.6 pIC50 = 7.6 Binding
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 1878 14 None - 0 Human 7.6 pIC50 = 7.6 Binding
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 181771 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
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 181771 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
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 181658 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
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 181658 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
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 182326 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
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 182326 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
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 7894 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
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 7894 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
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 2119 79 None -3 8 Human 7.5 pIC50 = 7.5 Binding
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 2119 79 None -3 8 Human 7.5 pIC50 = 7.5 Binding
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 2119 79 None -3 8 Human 7.5 pIC50 = 7.5 Binding
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 2119 79 None -3 8 Human 7.5 pIC50 = 7.5 Binding
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 1878 14 None - 0 Mouse 6.5 pIC50 = 6.5 Binding
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 1878 14 None - 0 Mouse 6.5 pIC50 = 6.5 Binding
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 1878 14 None - 0 Mouse 6.5 pIC50 = 6.5 Binding
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 182656 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
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 182656 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
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 7632 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
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 7632 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
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 181946 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
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 181946 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
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 181486 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
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 181486 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
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 182245 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
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 182245 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
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 8286 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
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 8286 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
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 7830 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
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 7830 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
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 181268 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
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 181268 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
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 8019 23 None - 0 Human 7.4 pIC50 = 7.4 Binding
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 8019 23 None - 0 Human 7.4 pIC50 = 7.4 Binding
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 182491 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
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 182491 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
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 2119 79 None -4 8 Mouse 7.4 pIC50 = 7.4 Binding
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 2119 79 None -4 8 Mouse 7.4 pIC50 = 7.4 Binding
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 2119 79 None -4 8 Mouse 7.4 pIC50 = 7.4 Binding
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 2119 79 None -4 8 Mouse 7.4 pIC50 = 7.4 Binding
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 182992 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
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 182992 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
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 182866 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
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 182866 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
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 8263 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
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 8263 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
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 182705 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
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 182705 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
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 3744 43 None -33 25 Human 6.3 pIC50 = 6.3 Binding
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 3744 43 None -33 25 Human 6.3 pIC50 = 6.3 Binding
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 3744 43 None -33 25 Human 6.3 pIC50 = 6.3 Binding
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 182112 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
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 182112 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
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 182549 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
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 182549 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
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 182455 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
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 182455 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
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 181906 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
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 181906 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
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 181620 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
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 181620 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
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 181494 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
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 181494 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
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 181070 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
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 181070 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
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 181997 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
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 181997 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
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 182222 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
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 182222 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
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 8253 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
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 8253 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
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 182128 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
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 182128 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
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 181562 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
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 181562 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
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 181222 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
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 181222 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
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
89477445 181468 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
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 181468 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
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 182758 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
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 182758 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
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 2111 26 None 2 7 Mouse 8.1 pIC50 = 8.1 Binding
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 2111 26 None 2 7 Mouse 8.1 pIC50 = 8.1 Binding
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 2111 26 None 2 7 Mouse 8.1 pIC50 = 8.1 Binding
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 8190 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
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 8190 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
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 8045 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
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 8045 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
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 2119 79 None -3 8 Human 7.1 pIC50 = 7.1 Binding
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 2119 79 None -3 8 Human 7.1 pIC50 = 7.1 Binding
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 2119 79 None -3 8 Human 7.1 pIC50 = 7.1 Binding
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 2119 79 None -3 8 Human 7.1 pIC50 = 7.1 Binding
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 8022 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
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 8022 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
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 8331 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
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 8331 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
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 7640 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
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 7640 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
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 2119 79 None -3 8 Human 8.0 pKd = 8 Binding
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 2119 79 None -3 8 Human 8.0 pKd = 8 Binding
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 2119 79 None -3 8 Human 8.0 pKd = 8 Binding
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 2119 79 None -3 8 Human 8.0 pKd = 8 Binding
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 89298 0 None 2 6 Human 8.0 pKd = 8.0 Binding
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 89298 0 None 2 6 Human 8.0 pKd = 8.0 Binding
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 79856 3 None -2 4 Human 8.0 pKd = 8.0 Binding
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 79856 3 None -2 4 Human 8.0 pKd = 8.0 Binding
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 177665 0 None -7 4 Human 8.0 pKd = 8.0 Binding
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 177665 0 None -7 4 Human 8.0 pKd = 8.0 Binding
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 177665 0 None -7 4 Human 8.0 pKd = 8.0 Binding
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 944 89 None -57 91 Human 7.9 pKd = 7.9 Binding
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
38 944 89 None -57 91 Human 7.9 pKd = 7.9 Binding
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
722 944 89 None -57 91 Human 7.9 pKd = 7.9 Binding
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 944 89 None -57 91 Human 7.9 pKd = 7.9 Binding
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 944 89 None -57 91 Human 7.9 pKd = 7.9 Binding
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 2111 26 None -2 7 Human 7.9 pKd = 7.9 Binding
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 2111 26 None -2 7 Human 7.9 pKd = 7.9 Binding
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 2111 26 None -2 7 Human 7.9 pKd = 7.9 Binding
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 79856 3 None -2 4 Human 7.9 pKd = 7.9 Binding
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 79856 3 None -2 4 Human 7.9 pKd = 7.9 Binding
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 89299 0 None 1 5 Human 7.9 pKd = 7.9 Binding
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 89299 0 None 1 5 Human 7.9 pKd = 7.9 Binding
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 1901 114 None -12 23 Rat 6.9 pKd = 6.9 Binding
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 1901 114 None -12 23 Rat 6.9 pKd = 6.9 Binding
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 1901 114 None -12 23 Rat 6.9 pKd = 6.9 Binding
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 1901 114 None -12 23 Rat 6.9 pKd = 6.9 Binding
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 1901 114 None -12 23 Rat 6.9 pKd = 6.9 Binding
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 1901 114 None -12 23 Rat 6.9 pKd = 6.9 Binding
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 944 89 None -57 91 Human 7.8 pKd = 7.8 Binding
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
38 944 89 None -57 91 Human 7.8 pKd = 7.8 Binding
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
722 944 89 None -57 91 Human 7.8 pKd = 7.8 Binding
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 944 89 None -57 91 Human 7.8 pKd = 7.8 Binding
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 944 89 None -57 91 Human 7.8 pKd = 7.8 Binding
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 175746 0 None -1 4 Mouse 7.8 pKd = 7.8 Binding
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 175746 0 None -1 4 Mouse 7.8 pKd = 7.8 Binding
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 175746 0 None -1 4 Mouse 7.8 pKd = 7.8 Binding
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 175746 0 None -1 4 Mouse 7.8 pKd = 7.8 Binding
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 177697 0 None -158 4 Mouse 6.8 pKd = 6.8 Binding
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 177697 0 None -158 4 Mouse 6.8 pKd = 6.8 Binding
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 177697 0 None -158 4 Mouse 6.8 pKd = 6.8 Binding
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 1901 114 None -3 23 Human 7.8 pKd = 7.8 Binding
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 1901 114 None -3 23 Human 7.8 pKd = 7.8 Binding
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 1901 114 None -3 23 Human 7.8 pKd = 7.8 Binding
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 1901 114 None -3 23 Human 7.8 pKd = 7.8 Binding
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 1901 114 None -3 23 Human 7.8 pKd = 7.8 Binding
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 1901 114 None -3 23 Human 7.8 pKd = 7.8 Binding
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 3110 90 None -301 40 Human 7.8 pKd = 7.8 Binding
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 3110 90 None -301 40 Human 7.8 pKd = 7.8 Binding
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 3110 90 None -301 40 Human 7.8 pKd = 7.8 Binding
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 3110 90 None -301 40 Human 7.8 pKd = 7.8 Binding
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 3110 90 None -301 40 Human 7.8 pKd = 7.8 Binding
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 192160 0 None -3 4 Human 7.8 pKd = 7.8 Binding
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 192160 0 None -3 4 Human 7.8 pKd = 7.8 Binding
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 192160 0 None -3 4 Human 7.8 pKd = 7.8 Binding
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 192164 0 None -2 4 Human 7.8 pKd = 7.8 Binding
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 192164 0 None -2 4 Human 7.8 pKd = 7.8 Binding
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 192164 0 None -2 4 Human 7.8 pKd = 7.8 Binding
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 192177 0 None -6 4 Human 7.8 pKd = 7.8 Binding
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 192177 0 None -6 4 Human 7.8 pKd = 7.8 Binding
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 192177 0 None -6 4 Human 7.8 pKd = 7.8 Binding
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 192183 0 None -83 6 Human 7.8 pKd = 7.8 Binding
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 192183 0 None -83 6 Human 7.8 pKd = 7.8 Binding
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 192183 0 None -83 6 Human 7.8 pKd = 7.8 Binding
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 192199 0 None -50 4 Human 7.8 pKd = 7.8 Binding
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 192199 0 None -50 4 Human 7.8 pKd = 7.8 Binding
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 192199 0 None -50 4 Human 7.8 pKd = 7.8 Binding
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 192201 0 None -5 4 Human 7.8 pKd = 7.8 Binding
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 192201 0 None -5 4 Human 7.8 pKd = 7.8 Binding
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 192201 0 None -5 4 Human 7.8 pKd = 7.8 Binding
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 192203 0 None -12 6 Human 7.8 pKd = 7.8 Binding
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 192203 0 None -12 6 Human 7.8 pKd = 7.8 Binding
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 192203 0 None -12 6 Human 7.8 pKd = 7.8 Binding
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 192206 0 None -11 6 Human 7.8 pKd = 7.8 Binding
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 192206 0 None -11 6 Human 7.8 pKd = 7.8 Binding
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 192206 0 None -11 6 Human 7.8 pKd = 7.8 Binding
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 192207 0 None -5 4 Human 7.8 pKd = 7.8 Binding
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 192207 0 None -5 4 Human 7.8 pKd = 7.8 Binding
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 192207 0 None -5 4 Human 7.8 pKd = 7.8 Binding
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 192224 0 None -5 4 Human 7.8 pKd = 7.8 Binding
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 192224 0 None -5 4 Human 7.8 pKd = 7.8 Binding
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 192224 0 None -5 4 Human 7.8 pKd = 7.8 Binding
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 192233 0 None -4 4 Human 7.8 pKd = 7.8 Binding
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 192233 0 None -4 4 Human 7.8 pKd = 7.8 Binding
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 192233 0 None -4 4 Human 7.8 pKd = 7.8 Binding
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 192244 0 None -5 4 Human 7.8 pKd = 7.8 Binding
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 192244 0 None -5 4 Human 7.8 pKd = 7.8 Binding
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 192244 0 None -5 4 Human 7.8 pKd = 7.8 Binding
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 192246 0 None -17 6 Human 7.8 pKd = 7.8 Binding
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 192246 0 None -17 6 Human 7.8 pKd = 7.8 Binding
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 192246 0 None -17 6 Human 7.8 pKd = 7.8 Binding
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 192249 0 None -4 4 Human 7.8 pKd = 7.8 Binding
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 192249 0 None -4 4 Human 7.8 pKd = 7.8 Binding
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 192249 0 None -4 4 Human 7.8 pKd = 7.8 Binding
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 192263 0 None -3 4 Human 7.8 pKd = 7.8 Binding
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 192263 0 None -3 4 Human 7.8 pKd = 7.8 Binding
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 192263 0 None -3 4 Human 7.8 pKd = 7.8 Binding
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 192279 0 None 2 4 Human 7.8 pKd = 7.8 Binding
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 192279 0 None 2 4 Human 7.8 pKd = 7.8 Binding
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 192279 0 None 2 4 Human 7.8 pKd = 7.8 Binding
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 192280 0 None -1071 6 Human 7.8 pKd = 7.8 Binding
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 192280 0 None -1071 6 Human 7.8 pKd = 7.8 Binding
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 192280 0 None -1071 6 Human 7.8 pKd = 7.8 Binding
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 192291 0 None -5 4 Human 7.8 pKd = 7.8 Binding
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 192291 0 None -5 4 Human 7.8 pKd = 7.8 Binding
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 192291 0 None -5 4 Human 7.8 pKd = 7.8 Binding
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 192293 0 None -6 4 Human 7.8 pKd = 7.8 Binding
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 192293 0 None -6 4 Human 7.8 pKd = 7.8 Binding
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 192293 0 None -6 4 Human 7.8 pKd = 7.8 Binding
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 192298 0 None -5 4 Human 7.8 pKd = 7.8 Binding
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 192298 0 None -5 4 Human 7.8 pKd = 7.8 Binding
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 192298 0 None -5 4 Human 7.8 pKd = 7.8 Binding
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 192304 0 None -7 4 Human 7.8 pKd = 7.8 Binding
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 192304 0 None -7 4 Human 7.8 pKd = 7.8 Binding
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 192304 0 None -7 4 Human 7.8 pKd = 7.8 Binding
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 192308 0 None -5 4 Human 7.8 pKd = 7.8 Binding
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 192308 0 None -5 4 Human 7.8 pKd = 7.8 Binding
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 192308 0 None -5 4 Human 7.8 pKd = 7.8 Binding
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 192322 0 None -5 4 Human 7.8 pKd = 7.8 Binding
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 192322 0 None -5 4 Human 7.8 pKd = 7.8 Binding
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 192322 0 None -5 4 Human 7.8 pKd = 7.8 Binding
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 192324 0 None -109 6 Human 7.8 pKd = 7.8 Binding
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 192324 0 None -109 6 Human 7.8 pKd = 7.8 Binding
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 192324 0 None -109 6 Human 7.8 pKd = 7.8 Binding
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 192366 0 None -1071 20 Human 7.8 pKd = 7.8 Binding
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 192366 0 None -1071 20 Human 7.8 pKd = 7.8 Binding
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 192366 0 None -1071 20 Human 7.8 pKd = 7.8 Binding
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 192371 0 None -1071 6 Human 7.8 pKd = 7.8 Binding
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 192371 0 None -1071 6 Human 7.8 pKd = 7.8 Binding
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 192371 0 None -1071 6 Human 7.8 pKd = 7.8 Binding
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 192377 0 None 5 4 Human 7.8 pKd = 7.8 Binding
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 192377 0 None 5 4 Human 7.8 pKd = 7.8 Binding
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 192377 0 None 5 4 Human 7.8 pKd = 7.8 Binding
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 192395 0 None -112 6 Human 7.8 pKd = 7.8 Binding
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 192395 0 None -112 6 Human 7.8 pKd = 7.8 Binding
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 192395 0 None -112 6 Human 7.8 pKd = 7.8 Binding
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 192404 0 None -7 4 Human 7.8 pKd = 7.8 Binding
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 192404 0 None -7 4 Human 7.8 pKd = 7.8 Binding
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 192404 0 None -7 4 Human 7.8 pKd = 7.8 Binding
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 192408 0 None -8 4 Human 7.8 pKd = 7.8 Binding
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 192408 0 None -8 4 Human 7.8 pKd = 7.8 Binding
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 192408 0 None -8 4 Human 7.8 pKd = 7.8 Binding
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 192412 0 None -4 4 Human 7.8 pKd = 7.8 Binding
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 192412 0 None -4 4 Human 7.8 pKd = 7.8 Binding
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 192412 0 None -4 4 Human 7.8 pKd = 7.8 Binding
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 192416 0 None -181 6 Human 7.8 pKd = 7.8 Binding
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 192416 0 None -181 6 Human 7.8 pKd = 7.8 Binding
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 192416 0 None -181 6 Human 7.8 pKd = 7.8 Binding
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 192417 0 None -301 20 Human 7.8 pKd = 7.8 Binding
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 192417 0 None -301 20 Human 7.8 pKd = 7.8 Binding
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 192417 0 None -301 20 Human 7.8 pKd = 7.8 Binding
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 192418 0 None -6 4 Human 7.8 pKd = 7.8 Binding
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 192418 0 None -6 4 Human 7.8 pKd = 7.8 Binding
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 192418 0 None -6 4 Human 7.8 pKd = 7.8 Binding
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 192424 0 None 7 4 Human 7.8 pKd = 7.8 Binding
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 192424 0 None 7 4 Human 7.8 pKd = 7.8 Binding
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 192424 0 None 7 4 Human 7.8 pKd = 7.8 Binding
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 192429 0 None -301 20 Human 7.8 pKd = 7.8 Binding
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 192429 0 None -301 20 Human 7.8 pKd = 7.8 Binding
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 192429 0 None -301 20 Human 7.8 pKd = 7.8 Binding
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 192433 0 None -5 4 Human 7.8 pKd = 7.8 Binding
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 192433 0 None -5 4 Human 7.8 pKd = 7.8 Binding
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 192433 0 None -5 4 Human 7.8 pKd = 7.8 Binding
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 192438 0 None -1071 6 Human 7.8 pKd = 7.8 Binding
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 192438 0 None -1071 6 Human 7.8 pKd = 7.8 Binding
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 192438 0 None -1071 6 Human 7.8 pKd = 7.8 Binding
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 192439 0 None -8 4 Human 7.8 pKd = 7.8 Binding
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 192439 0 None -8 4 Human 7.8 pKd = 7.8 Binding
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 192439 0 None -8 4 Human 7.8 pKd = 7.8 Binding
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 192443 0 None -6 4 Human 7.8 pKd = 7.8 Binding
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 192443 0 None -6 4 Human 7.8 pKd = 7.8 Binding
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 192443 0 None -6 4 Human 7.8 pKd = 7.8 Binding
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 192446 0 None -5 4 Human 7.8 pKd = 7.8 Binding
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 192446 0 None -5 4 Human 7.8 pKd = 7.8 Binding
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 192446 0 None -5 4 Human 7.8 pKd = 7.8 Binding
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 177665 0 None -7 4 Human 7.8 pKd = 7.8 Binding
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 177665 0 None -7 4 Human 7.8 pKd = 7.8 Binding
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 177665 0 None -7 4 Human 7.8 pKd = 7.8 Binding
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 177697 0 None -158 4 Mouse 6.8 pKd = 6.8 Binding
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 177697 0 None -158 4 Mouse 6.8 pKd = 6.8 Binding
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 177697 0 None -158 4 Mouse 6.8 pKd = 6.8 Binding
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 175746 0 None -1 4 Mouse 7.8 pKd = 7.8 Binding
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 175746 0 None -1 4 Mouse 7.8 pKd = 7.8 Binding
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 175746 0 None -1 4 Mouse 7.8 pKd = 7.8 Binding
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 175746 0 None -1 4 Mouse 7.8 pKd = 7.8 Binding
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 177665 0 None -7 4 Human 7.8 pKd = 7.8 Binding
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 177665 0 None -7 4 Human 7.8 pKd = 7.8 Binding
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 177665 0 None -7 4 Human 7.8 pKd = 7.8 Binding
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 944 89 None -57 91 Human 7.7 pKd = 7.7 Binding
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
38 944 89 None -57 91 Human 7.7 pKd = 7.7 Binding
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
722 944 89 None -57 91 Human 7.7 pKd = 7.7 Binding
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 944 89 None -57 91 Human 7.7 pKd = 7.7 Binding
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 944 89 None -57 91 Human 7.7 pKd = 7.7 Binding
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 89296 0 None 6 6 Human 7.7 pKd = 7.7 Binding
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 89296 0 None 6 6 Human 7.7 pKd = 7.7 Binding
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 175746 0 None -2 4 Rat 7.7 pKd = 7.7 Binding
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 175746 0 None -2 4 Rat 7.7 pKd = 7.7 Binding
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 175746 0 None -2 4 Rat 7.7 pKd = 7.7 Binding
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 175746 0 None -2 4 Rat 7.7 pKd = 7.7 Binding
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 175746 0 None -2 4 Rat 7.7 pKd = 7.7 Binding
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 175746 0 None -2 4 Rat 7.7 pKd = 7.7 Binding
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 175746 0 None -2 4 Rat 7.7 pKd = 7.7 Binding
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 175746 0 None -2 4 Rat 7.7 pKd = 7.7 Binding
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 79856 3 None -2 4 Human 7.7 pKd = 7.7 Binding
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 79856 3 None -2 4 Human 7.7 pKd = 7.7 Binding
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 292 7 None 4 5 Human 7.6 pKd = 7.6 Binding
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 292 7 None 4 5 Human 7.6 pKd = 7.6 Binding
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 292 7 None 4 5 Human 7.6 pKd = 7.6 Binding
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 292 7 None 4 5 Human 7.6 pKd = 7.6 Binding
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 2119 79 None -3 8 Human 8.4 pKd = 8.4 Binding
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 2119 79 None -3 8 Human 8.4 pKd = 8.4 Binding
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 2119 79 None -3 8 Human 8.4 pKd = 8.4 Binding
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 2119 79 None -3 8 Human 8.4 pKd = 8.4 Binding
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 940 32 None -60 11 Human 7.5 pKd = 7.5 Binding
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 940 32 None -60 11 Human 7.5 pKd = 7.5 Binding
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 940 32 None -60 11 Human 7.5 pKd = 7.5 Binding
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 940 32 None -60 11 Human 7.5 pKd = 7.5 Binding
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 940 32 None -60 11 Human 7.5 pKd = 7.5 Binding
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 940 32 None -60 11 Human 7.5 pKd = 7.5 Binding
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 177665 0 None -22 4 Mouse 7.5 pKd = 7.5 Binding
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 177665 0 None -22 4 Mouse 7.5 pKd = 7.5 Binding
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 177665 0 None -22 4 Mouse 7.5 pKd = 7.5 Binding
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 175746 0 None -1 4 Mouse 7.5 pKd = 7.5 Binding
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 175746 0 None -1 4 Mouse 7.5 pKd = 7.5 Binding
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 175746 0 None -1 4 Mouse 7.5 pKd = 7.5 Binding
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 175746 0 None -1 4 Mouse 7.5 pKd = 7.5 Binding
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 175746 0 None -1 4 Mouse 7.5 pKd = 7.5 Binding
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 175746 0 None -1 4 Mouse 7.5 pKd = 7.5 Binding
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 175746 0 None -1 4 Mouse 7.5 pKd = 7.5 Binding
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 175746 0 None -1 4 Mouse 7.5 pKd = 7.5 Binding
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 175746 0 None -2 4 Rat 7.5 pKd = 7.5 Binding
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 175746 0 None -2 4 Rat 7.5 pKd = 7.5 Binding
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 175746 0 None -2 4 Rat 7.5 pKd = 7.5 Binding
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 175746 0 None -2 4 Rat 7.5 pKd = 7.5 Binding
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 175746 0 None -2 4 Rat 7.5 pKd = 7.5 Binding
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 175746 0 None -2 4 Rat 7.5 pKd = 7.5 Binding
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 175746 0 None -2 4 Rat 7.5 pKd = 7.5 Binding
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 175746 0 None -2 4 Rat 7.5 pKd = 7.5 Binding
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 175746 0 None 1 4 Human 7.4 pKd = 7.4 Binding
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 175746 0 None 1 4 Human 7.4 pKd = 7.4 Binding
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 175746 0 None 1 4 Human 7.4 pKd = 7.4 Binding
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 175746 0 None 1 4 Human 7.4 pKd = 7.4 Binding
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 177665 0 None -7 4 Human 7.4 pKd = 7.4 Binding
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 177665 0 None -7 4 Human 7.4 pKd = 7.4 Binding
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 177665 0 None -7 4 Human 7.4 pKd = 7.4 Binding
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 69397 0 None 1 9 Human 7.4 pKd = 7.4 Binding
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 69397 0 None 1 9 Human 7.4 pKd = 7.4 Binding
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 175746 0 None 1 4 Human 7.4 pKd = 7.4 Binding
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 175746 0 None 1 4 Human 7.4 pKd = 7.4 Binding
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 175746 0 None 1 4 Human 7.4 pKd = 7.4 Binding
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 175746 0 None 1 4 Human 7.4 pKd = 7.4 Binding
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 177665 0 None -7 4 Human 7.4 pKd = 7.4 Binding
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 177665 0 None -7 4 Human 7.4 pKd = 7.4 Binding
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 177665 0 None -7 4 Human 7.4 pKd = 7.4 Binding
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 1901 114 None -15 23 Mouse 7.4 pKd = 7.4 Binding
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 1901 114 None -15 23 Mouse 7.4 pKd = 7.4 Binding
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 1901 114 None -15 23 Mouse 7.4 pKd = 7.4 Binding
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 1901 114 None -15 23 Mouse 7.4 pKd = 7.4 Binding
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 1901 114 None -15 23 Mouse 7.4 pKd = 7.4 Binding
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 1901 114 None -15 23 Mouse 7.4 pKd = 7.4 Binding
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 177665 0 None -22 4 Mouse 7.3 pKd = 7.3 Binding
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 177665 0 None -22 4 Mouse 7.3 pKd = 7.3 Binding
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 177665 0 None -22 4 Mouse 7.3 pKd = 7.3 Binding
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 1901 114 None -3 23 Human 8.3 pKd = 8.3 Binding
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 1901 114 None -3 23 Human 8.3 pKd = 8.3 Binding
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 1901 114 None -3 23 Human 8.3 pKd = 8.3 Binding
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 1901 114 None -3 23 Human 8.3 pKd = 8.3 Binding
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 1901 114 None -3 23 Human 8.3 pKd = 8.3 Binding
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 1901 114 None -3 23 Human 8.3 pKd = 8.3 Binding
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 177665 0 None -22 4 Mouse 7.3 pKd = 7.3 Binding
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 177665 0 None -22 4 Mouse 7.3 pKd = 7.3 Binding
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 177665 0 None -22 4 Mouse 7.3 pKd = 7.3 Binding
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 175746 0 None 1 4 Human 7.2 pKd = 7.2 Binding
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 175746 0 None 1 4 Human 7.2 pKd = 7.2 Binding
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 175746 0 None 1 4 Human 7.2 pKd = 7.2 Binding
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 175746 0 None 1 4 Human 7.2 pKd = 7.2 Binding
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 175746 0 None 1 4 Human 7.2 pKd = 7.2 Binding
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 175746 0 None 1 4 Human 7.2 pKd = 7.2 Binding
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 175746 0 None 1 4 Human 7.2 pKd = 7.2 Binding
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 175746 0 None 1 4 Human 7.2 pKd = 7.2 Binding
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 177665 0 None -22 4 Mouse 7.2 pKd = 7.2 Binding
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 177665 0 None -22 4 Mouse 7.2 pKd = 7.2 Binding
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 177665 0 None -22 4 Mouse 7.2 pKd = 7.2 Binding
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 177665 0 None -22 4 Mouse 7.2 pKd = 7.2 Binding
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 177665 0 None -22 4 Mouse 7.2 pKd = 7.2 Binding
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 177665 0 None -22 4 Mouse 7.2 pKd = 7.2 Binding
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 177665 0 None -22 4 Mouse 7.2 pKd = 7.2 Binding
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 177665 0 None -22 4 Mouse 7.2 pKd = 7.2 Binding
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 177665 0 None -22 4 Mouse 7.2 pKd = 7.2 Binding
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 944 89 None -57 91 Human 7.2 pKd = 7.2 Binding
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
38 944 89 None -57 91 Human 7.2 pKd = 7.2 Binding
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
722 944 89 None -57 91 Human 7.2 pKd = 7.2 Binding
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 944 89 None -57 91 Human 7.2 pKd = 7.2 Binding
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 944 89 None -57 91 Human 7.2 pKd = 7.2 Binding
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 79856 3 None -2 4 Human 7.1 pKd = 7.1 Binding
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 79856 3 None -2 4 Human 7.1 pKd = 7.1 Binding
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 177697 0 None -58 4 Human 7.1 pKd = 7.1 Binding
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 177697 0 None -58 4 Human 7.1 pKd = 7.1 Binding
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 177697 0 None -58 4 Human 7.1 pKd = 7.1 Binding
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 177697 0 None -58 4 Human 7.1 pKd = 7.1 Binding
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 177697 0 None -58 4 Human 7.1 pKd = 7.1 Binding
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 177697 0 None -58 4 Human 7.1 pKd = 7.1 Binding
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 89295 0 None 5 6 Human 8.1 pKd = 8.1 Binding
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 89295 0 None 5 6 Human 8.1 pKd = 8.1 Binding
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 177665 0 None -7 4 Human 8.0 pKd = 8.0 Binding
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 177665 0 None -7 4 Human 8.0 pKd = 8.0 Binding
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 177665 0 None -7 4 Human 8.0 pKd = 8.0 Binding
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 61206 0 None - 1 Human 10.4 pKi = 10.4 Binding
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 61206 0 None - 1 Human 10.4 pKi = 10.4 Binding
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 67706 2 None - 1 Human 10.0 pKi = 10 Binding
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 67706 2 None - 1 Human 10.0 pKi = 10 Binding
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 61202 0 None - 1 Human 9.7 pKi = 9.7 Binding
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 61202 0 None - 1 Human 9.7 pKi = 9.7 Binding
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 6526 0 None - 1 Human 9.7 pKi = 9.7 Binding
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 6526 0 None - 1 Human 9.7 pKi = 9.7 Binding
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 61199 0 None - 1 Human 9.5 pKi = 9.5 Binding
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 61199 0 None - 1 Human 9.5 pKi = 9.5 Binding
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 67698 0 None - 1 Human 9.5 pKi = 9.5 Binding
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 67698 0 None - 1 Human 9.5 pKi = 9.5 Binding
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 8078 0 None - 1 Human 9.4 pKi = 9.4 Binding
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 8078 0 None - 1 Human 9.4 pKi = 9.4 Binding
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 67789 0 None - 1 Human 9.2 pKi = 9.2 Binding
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 67789 0 None - 1 Human 9.2 pKi = 9.2 Binding
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 116631 0 None - 1 Human 9.1 pKi = 9.1 Binding
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 116631 0 None - 1 Human 9.1 pKi = 9.1 Binding
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 67764 0 None - 1 Human 9.1 pKi = 9.1 Binding
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 67764 0 None - 1 Human 9.1 pKi = 9.1 Binding
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 61204 0 None - 1 Human 9.1 pKi = 9.1 Binding
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 61204 0 None - 1 Human 9.1 pKi = 9.1 Binding
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 67759 0 None - 1 Human 9.1 pKi = 9.1 Binding
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 67759 0 None - 1 Human 9.1 pKi = 9.1 Binding
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 109639 0 None - 1 Human 9.0 pKi = 9.0 Binding
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 109639 0 None - 1 Human 9.0 pKi = 9.0 Binding
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 1901 114 None -3 23 Human 9.0 pKi = 9 Binding
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 1901 114 None -3 23 Human 9.0 pKi = 9 Binding
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 1901 114 None -3 23 Human 9.0 pKi = 9 Binding
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 1901 114 None -3 23 Human 9.0 pKi = 9 Binding
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 1901 114 None -3 23 Human 9.0 pKi = 9 Binding
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 1901 114 None -3 23 Human 9.0 pKi = 9 Binding
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 940 32 None -60 11 Human 9.0 pKi = 9 Binding
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 940 32 None -60 11 Human 9.0 pKi = 9 Binding
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 940 32 None -60 11 Human 9.0 pKi = 9 Binding
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 61223 0 None - 1 Human 9.0 pKi = 9 Binding
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 61223 0 None - 1 Human 9.0 pKi = 9 Binding
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 61233 0 None - 1 Human 9.0 pKi = 9 Binding
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 61233 0 None - 1 Human 9.0 pKi = 9 Binding
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 135934 0 None - 1 Human 9.0 pKi = 9 Binding
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 135934 0 None - 1 Human 9.0 pKi = 9 Binding
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 109636 2 None 19 3 Human 9.0 pKi = 9 Binding
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 109636 2 None 19 3 Human 9.0 pKi = 9 Binding
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 116618 0 None - 1 Human 9.0 pKi = 9 Binding
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 116618 0 None - 1 Human 9.0 pKi = 9 Binding
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 135934 0 None - 1 Human 9.0 pKi = 9 Binding
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 135934 0 None - 1 Human 9.0 pKi = 9 Binding
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 67769 0 None - 1 Human 9.0 pKi = 9 Binding
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 67769 0 None - 1 Human 9.0 pKi = 9 Binding
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 67791 0 None - 1 Human 9.0 pKi = 9 Binding
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 67791 0 None - 1 Human 9.0 pKi = 9 Binding
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 140304 0 None - 1 Human 9.0 pKi = 9 Binding
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 140304 0 None - 1 Human 9.0 pKi = 9 Binding
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 8896 0 None -4 13 Human 9.0 pKi = 9.0 Binding
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 8896 0 None -4 13 Human 9.0 pKi = 9.0 Binding
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 109637 0 None - 1 Human 9.0 pKi = 9.0 Binding
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 109637 0 None - 1 Human 9.0 pKi = 9.0 Binding
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 67705 2 None - 1 Human 9.0 pKi = 9.0 Binding
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 67705 2 None - 1 Human 9.0 pKi = 9.0 Binding
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 67707 2 None - 1 Human 9.0 pKi = 9.0 Binding
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 67707 2 None - 1 Human 9.0 pKi = 9.0 Binding
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 8896 0 None -4 13 Human 9.0 pKi = 9.0 Binding
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 8896 0 None -4 13 Human 9.0 pKi = 9.0 Binding
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 175973 0 None -2 3 Human 8.9 pKi = 8.9 Binding
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 175973 0 None -2 3 Human 8.9 pKi = 8.9 Binding
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 175973 0 None -2 3 Human 8.9 pKi = 8.9 Binding
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 109636 2 None 19 3 Human 8.9 pKi = 8.9 Binding
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 109636 2 None 19 3 Human 8.9 pKi = 8.9 Binding
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 175973 0 None 1 3 Mouse 8.9 pKi = 8.9 Binding
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 175973 0 None 1 3 Mouse 8.9 pKi = 8.9 Binding
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 175973 0 None 1 3 Mouse 8.9 pKi = 8.9 Binding
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 109635 2 None - 1 Human 8.9 pKi = 8.9 Binding
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 109635 2 None - 1 Human 8.9 pKi = 8.9 Binding
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 5813 0 None 1 4 Rat 8.8 pKi = 8.8 Binding
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 5813 0 None 1 4 Rat 8.8 pKi = 8.8 Binding
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 192575 0 None 3 2 Rat 8.8 pKi = 8.8 Binding
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 192575 0 None 3 2 Rat 8.8 pKi = 8.8 Binding
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 109654 0 None - 1 Human 8.8 pKi = 8.8 Binding
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 109654 0 None - 1 Human 8.8 pKi = 8.8 Binding
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 5813 0 None -1 4 Human 8.8 pKi = 8.8 Binding
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 5813 0 None -1 4 Human 8.8 pKi = 8.8 Binding
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 197875 0 None 2 2 Rat 8.8 pKi = 8.8 Binding
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 197875 0 None 2 2 Rat 8.8 pKi = 8.8 Binding
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 940 32 None -60 11 Human 8.8 pKi = 8.8 Binding
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 940 32 None -60 11 Human 8.8 pKi = 8.8 Binding
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 940 32 None -60 11 Human 8.8 pKi = 8.8 Binding
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 193827 0 None 3 2 Human 8.8 pKi = 8.8 Binding
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 193827 0 None 3 2 Human 8.8 pKi = 8.8 Binding
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 193827 0 None 3 2 Human 8.8 pKi = 8.8 Binding
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 1901 114 None -3 23 Human 8.8 pKi = 8.8 Binding
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 1901 114 None -3 23 Human 8.8 pKi = 8.8 Binding
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 1901 114 None -3 23 Human 8.8 pKi = 8.8 Binding
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 1901 114 None -3 23 Human 8.8 pKi = 8.8 Binding
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 1901 114 None -3 23 Human 8.8 pKi = 8.8 Binding
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 1901 114 None -3 23 Human 8.8 pKi = 8.8 Binding
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 1979 29 None -40 6 Human 8.8 pKi = 8.8 Binding
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 1979 29 None -40 6 Human 8.8 pKi = 8.8 Binding
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 1979 29 None -40 6 Human 8.8 pKi = 8.8 Binding
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 1979 29 None -40 6 Human 8.8 pKi = 8.8 Binding
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 67876 0 None - 1 Human 8.8 pKi = 8.8 Binding
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 67876 0 None - 1 Human 8.8 pKi = 8.8 Binding
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 109662 0 None - 1 Human 8.8 pKi = 8.8 Binding
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 109662 0 None - 1 Human 8.8 pKi = 8.8 Binding
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 109643 0 None - 1 Human 8.7 pKi = 8.7 Binding
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 109643 0 None - 1 Human 8.7 pKi = 8.7 Binding
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 7703 0 None 1 4 Human 8.7 pKi = 8.7 Binding
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 7703 0 None 1 4 Human 8.7 pKi = 8.7 Binding
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 186831 0 None - 1 Human 8.7 pKi = 8.7 Binding
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 186831 0 None - 1 Human 8.7 pKi = 8.7 Binding
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
135525668 67870 0 None 263 2 Human 8.0 pKi = 8 Binding
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 67870 0 None 263 2 Human 8.0 pKi = 8 Binding
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 111678 0 None - 1 Human 8.0 pKi = 8 Binding
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 111678 0 None - 1 Human 8.0 pKi = 8 Binding
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 1978 14 None -3 3 Human 8.0 pKi = 8 Binding
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 1978 14 None -3 3 Human 8.0 pKi = 8 Binding
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 1978 14 None -3 3 Human 8.0 pKi = 8 Binding
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 4000 13 None -3 3 Human 8.0 pKi = 8 Binding
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 4000 13 None -3 3 Human 8.0 pKi = 8 Binding
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 4000 13 None -3 3 Human 8.0 pKi = 8 Binding
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 202829 0 None 5 2 Human 8.0 pKi = 8 Binding
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 202829 0 None 5 2 Human 8.0 pKi = 8 Binding
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 89216 0 None - 1 Human 8.0 pKi = 8 Binding
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 89216 0 None - 1 Human 8.0 pKi = 8 Binding
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 89241 0 None - 1 Human 8.0 pKi = 8 Binding
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 89241 0 None - 1 Human 8.0 pKi = 8 Binding
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 940 32 None -60 11 Human 8.0 pKi = 8 Binding
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 940 32 None -60 11 Human 8.0 pKi = 8 Binding
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 940 32 None -60 11 Human 8.0 pKi = 8 Binding
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 940 32 None -60 11 Human 8.0 pKi = 8 Binding
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 940 32 None -60 11 Human 8.0 pKi = 8 Binding
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 940 32 None -60 11 Human 8.0 pKi = 8 Binding
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 1978 14 None -3 3 Human 8.0 pKi = 8 Binding
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 1978 14 None -3 3 Human 8.0 pKi = 8 Binding
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 1978 14 None -3 3 Human 8.0 pKi = 8 Binding
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 61218 0 None - 1 Human 8.0 pKi = 8 Binding
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 61218 0 None - 1 Human 8.0 pKi = 8 Binding
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 75331 0 None - 1 Human 8.0 pKi = 8 Binding
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 75331 0 None - 1 Human 8.0 pKi = 8 Binding
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 197748 0 None - 1 Human 8.0 pKi = 8 Binding
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 197748 0 None - 1 Human 8.0 pKi = 8 Binding
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 940 32 None -60 11 Human 8.0 pKi = 8 Binding
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 940 32 None -60 11 Human 8.0 pKi = 8 Binding
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 940 32 None -60 11 Human 8.0 pKi = 8 Binding
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 194340 0 None -3 2 Human 8.0 pKi = 8 Binding
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 194340 0 None -3 2 Human 8.0 pKi = 8 Binding
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 194340 0 None -3 2 Human 8.0 pKi = 8 Binding
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 194341 0 None -3 2 Human 8.0 pKi = 8 Binding
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 194341 0 None -3 2 Human 8.0 pKi = 8 Binding
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 194341 0 None -3 2 Human 8.0 pKi = 8 Binding
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 194808 0 None -1 2 Human 8.0 pKi = 8 Binding
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 194808 0 None -1 2 Human 8.0 pKi = 8 Binding
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 194808 0 None -1 2 Human 8.0 pKi = 8 Binding
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 67787 0 None - 1 Human 8.0 pKi = 8 Binding
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 67787 0 None - 1 Human 8.0 pKi = 8 Binding
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 67794 0 None - 1 Human 8.0 pKi = 8 Binding
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 67794 0 None - 1 Human 8.0 pKi = 8 Binding
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 67797 0 None - 1 Human 8.0 pKi = 8 Binding
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 67797 0 None - 1 Human 8.0 pKi = 8 Binding
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 292 7 None 4 5 Human 8.0 pKi = 8.0 Binding
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 292 7 None 4 5 Human 8.0 pKi = 8.0 Binding
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 292 7 None 4 5 Human 8.0 pKi = 8.0 Binding
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 292 7 None 4 5 Human 8.0 pKi = 8.0 Binding
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 89301 0 None 97 2 Human 8.0 pKi = 8.0 Binding
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 89301 0 None 97 2 Human 8.0 pKi = 8.0 Binding
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 89295 0 None 5 6 Human 8.0 pKi = 8.0 Binding
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 89295 0 None 5 6 Human 8.0 pKi = 8.0 Binding
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 192504 0 None -3 2 Human 8.0 pKi = 8.0 Binding
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 192504 0 None -3 2 Human 8.0 pKi = 8.0 Binding
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 56186 0 None -1 4 Mouse 7.0 pKi = 7 Binding
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 56186 0 None -1 4 Mouse 7.0 pKi = 7 Binding
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 197827 0 None -22 2 Rat 7.0 pKi = 7 Binding
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 197827 0 None -22 2 Rat 7.0 pKi = 7 Binding
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 75447 4 None -3 2 Human 7.0 pKi = 7 Binding
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 75447 4 None -3 2 Human 7.0 pKi = 7 Binding
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 140766 0 None -3 2 Human 7.0 pKi = 7 Binding
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 140766 0 None -3 2 Human 7.0 pKi = 7 Binding
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 203533 1 None -4 2 Human 7.0 pKi = 7 Binding
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 203533 1 None -4 2 Human 7.0 pKi = 7 Binding
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 61196 0 None - 1 Human 7.0 pKi = 7 Binding
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 61196 0 None - 1 Human 7.0 pKi = 7 Binding
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 75328 2 None - 1 Human 7.0 pKi = 7 Binding
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 75328 2 None - 1 Human 7.0 pKi = 7 Binding
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 75336 0 None - 1 Human 7.0 pKi = 7 Binding
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 75336 0 None - 1 Human 7.0 pKi = 7 Binding
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 58579 2 None 1 2 Human 7.0 pKi = 7 Binding
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 58579 2 None 1 2 Human 7.0 pKi = 7 Binding
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 194528 0 None -7 2 Human 7.0 pKi = 7 Binding
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 194528 0 None -7 2 Human 7.0 pKi = 7 Binding
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 194528 0 None -7 2 Human 7.0 pKi = 7 Binding
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 109656 0 None - 1 Human 7.0 pKi = 7 Binding
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 109656 0 None - 1 Human 7.0 pKi = 7 Binding
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 75292 0 None - 1 Human 7.0 pKi = 7 Binding
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 75292 0 None - 1 Human 7.0 pKi = 7 Binding
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 66727 0 None 25 2 Human 6.0 pKi = 6 Binding
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 66727 0 None 25 2 Human 6.0 pKi = 6 Binding
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 5081 1 None -4 2 Human 6.0 pKi = 6 Binding
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 5081 1 None -4 2 Human 6.0 pKi = 6 Binding
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 89228 0 None - 1 Human 6.0 pKi = 6 Binding
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 89228 0 None - 1 Human 6.0 pKi = 6 Binding
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 89239 0 None - 1 Human 6.0 pKi = 6 Binding
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 89239 0 None - 1 Human 6.0 pKi = 6 Binding
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 18756 7 None - 1 Human 6.0 pKi = 6 Binding
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 18756 7 None - 1 Human 6.0 pKi = 6 Binding
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 75287 1 None - 1 Human 6.0 pKi = 6 Binding
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 75287 1 None - 1 Human 6.0 pKi = 6 Binding
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 75307 0 None - 1 Human 6.0 pKi = 6 Binding
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 75307 0 None - 1 Human 6.0 pKi = 6 Binding
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 103691 2 None -64 2 Human 6.0 pKi = 6 Binding
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 103691 2 None -64 2 Human 6.0 pKi = 6 Binding
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 6947 0 None - 1 Human 6.0 pKi = 6 Binding
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 6947 0 None - 1 Human 6.0 pKi = 6 Binding
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 98513 0 None -9120 10 Human 5.0 pKi = 5 Binding
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 98513 0 None -9120 10 Human 5.0 pKi = 5 Binding
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 116929 11 None - 1 Human 5.0 pKi = 5 Binding
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 116929 11 None - 1 Human 5.0 pKi = 5 Binding
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 89223 0 None - 1 Human 5.0 pKi = 5 Binding
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 89223 0 None - 1 Human 5.0 pKi = 5 Binding
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 116633 0 None - 1 Human 5.0 pKi = 5 Binding
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 116633 0 None - 1 Human 5.0 pKi = 5 Binding
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
57391926 69559 0 None - 1 Human 7.0 pKi = 7.0 Binding
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 69559 0 None - 1 Human 7.0 pKi = 7.0 Binding
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 79856 3 None -2 4 Human 7.0 pKi = 7.0 Binding
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 79856 3 None -2 4 Human 7.0 pKi = 7.0 Binding
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 95676 0 None - 1 Human 5.0 pKi = 5.0 Binding
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 95676 0 None - 1 Human 5.0 pKi = 5.0 Binding
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 138082 0 None -7 2 Human 7.0 pKi = 7.0 Binding
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 138082 0 None -7 2 Human 7.0 pKi = 7.0 Binding
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 67758 0 None - 1 Human 7.0 pKi = 7.0 Binding
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 67758 0 None - 1 Human 7.0 pKi = 7.0 Binding
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 173259 0 None - 1 Human 7.0 pKi = 7.0 Binding
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 173259 0 None - 1 Human 7.0 pKi = 7.0 Binding
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 178729 0 None - 1 Human 7.0 pKi = 7.0 Binding
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 178729 0 None - 1 Human 7.0 pKi = 7.0 Binding
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 186204 0 None - 1 Human 7.0 pKi = 7.0 Binding
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 186204 0 None - 1 Human 7.0 pKi = 7.0 Binding
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 173259 0 None - 1 Human 7.0 pKi = 7.0 Binding
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 173259 0 None - 1 Human 7.0 pKi = 7.0 Binding
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 186204 0 None - 1 Human 7.0 pKi = 7.0 Binding
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 186204 0 None - 1 Human 7.0 pKi = 7.0 Binding
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 86060 0 None - 1 Human 5.0 pKi = 5.0 Binding
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 86060 0 None - 1 Human 5.0 pKi = 5.0 Binding
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 5081 1 None -4 2 Human 6.0 pKi = 6.0 Binding
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 5081 1 None -4 2 Human 6.0 pKi = 6.0 Binding
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 67542 0 None -2754 3 Human 5.0 pKi = 5.0 Binding
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 67542 0 None -2754 3 Human 5.0 pKi = 5.0 Binding
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 67777 0 None - 1 Human 6.0 pKi = 6.0 Binding
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 67777 0 None - 1 Human 6.0 pKi = 6.0 Binding
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 139698 0 None -1 4 Human 6.0 pKi = 6.0 Binding
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 139698 0 None -1 4 Human 6.0 pKi = 6.0 Binding
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 62790 0 None -19 3 Human 6.0 pKi = 6.0 Binding
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 62790 0 None -19 3 Human 6.0 pKi = 6.0 Binding
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 62790 0 None -19 3 Human 6.0 pKi = 6.0 Binding
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 111698 0 None - 1 Human 5.0 pKi = 5.0 Binding
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 111698 0 None - 1 Human 5.0 pKi = 5.0 Binding
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 16244 4 None - 1 Human 6.0 pKi = 6.0 Binding
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 16244 4 None - 1 Human 6.0 pKi = 6.0 Binding
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 165934 0 None - 1 Human 5.0 pKi = 5.0 Binding
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 165934 0 None - 1 Human 5.0 pKi = 5.0 Binding
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 173667 0 None - 1 Human 7.0 pKi = 7.0 Binding
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 173667 0 None - 1 Human 7.0 pKi = 7.0 Binding
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 173667 0 None - 1 Human 7.0 pKi = 7.0 Binding
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 173667 0 None - 1 Human 7.0 pKi = 7.0 Binding
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 172339 0 None -67 5 Human 6.0 pKi = 6.0 Binding
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 172339 0 None -67 5 Human 6.0 pKi = 6.0 Binding
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 2119 79 None -281 8 Guinea pig 6.0 pKi = 6.0 Binding
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 2119 79 None -281 8 Guinea pig 6.0 pKi = 6.0 Binding
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 2119 79 None -281 8 Guinea pig 6.0 pKi = 6.0 Binding
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 2119 79 None -281 8 Guinea pig 6.0 pKi = 6.0 Binding
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 12292 6 None - 1 Human 6.0 pKi = 6.0 Binding
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 12292 6 None - 1 Human 6.0 pKi = 6.0 Binding
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 12292 6 None - 1 Human 6.0 pKi = 6.0 Binding
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 12292 6 None - 1 Human 6.0 pKi = 6.0 Binding
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 138187 0 None - 1 Human 6.0 pKi = 6.0 Binding
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 138187 0 None - 1 Human 6.0 pKi = 6.0 Binding
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 61219 0 None - 1 Human 6.0 pKi = 6.0 Binding
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 61219 0 None - 1 Human 6.0 pKi = 6.0 Binding
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 187005 2 None - 1 Human 6.0 pKi = 6.0 Binding
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 187005 2 None - 1 Human 6.0 pKi = 6.0 Binding
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 69385 0 None - 1 Human 7.0 pKi = 7.0 Binding
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 69385 0 None - 1 Human 7.0 pKi = 7.0 Binding
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 116614 2 None - 1 Human 7.0 pKi = 7.0 Binding
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 116614 2 None - 1 Human 7.0 pKi = 7.0 Binding
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 158104 0 None - 1 Human 6.0 pKi = 6.0 Binding
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 158104 0 None - 1 Human 6.0 pKi = 6.0 Binding
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 136892 0 None -5 2 Human 5.0 pKi = 5.0 Binding
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 136892 0 None -5 2 Human 5.0 pKi = 5.0 Binding
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 111679 2 None - 1 Human 6.0 pKi = 6.0 Binding
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 111679 2 None - 1 Human 6.0 pKi = 6.0 Binding
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 155570 0 None -1 2 Human 8.0 pKi = 8.0 Binding
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 155570 0 None -1 2 Human 8.0 pKi = 8.0 Binding
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 116516 0 None - 1 Human 8.0 pKi = 8.0 Binding
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 116516 0 None - 1 Human 8.0 pKi = 8.0 Binding
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 116516 0 None - 1 Human 8.0 pKi = 8.0 Binding
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 116516 0 None - 1 Human 8.0 pKi = 8.0 Binding
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 3785 18 None - 1 Human 8.0 pKi = 8.0 Binding
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 3785 18 None - 1 Human 8.0 pKi = 8.0 Binding
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 3785 18 None - 1 Human 8.0 pKi = 8.0 Binding
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 3785 18 None - 1 Human 8.0 pKi = 8.0 Binding
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 149796 0 None - 1 Human 8.0 pKi = 8.0 Binding
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 149796 0 None - 1 Human 8.0 pKi = 8.0 Binding
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 192504 0 None -3 2 Human 8.0 pKi = 8.0 Binding
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 192504 0 None -3 2 Human 8.0 pKi = 8.0 Binding
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 115413 0 None - 1 Human 8.0 pKi = 8.0 Binding
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 115413 0 None - 1 Human 8.0 pKi = 8.0 Binding
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 67792 0 None - 1 Human 8.0 pKi = 8.0 Binding
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 67792 0 None - 1 Human 8.0 pKi = 8.0 Binding
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 116516 0 None - 1 Human 8.0 pKi = 8.0 Binding
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 116516 0 None - 1 Human 8.0 pKi = 8.0 Binding
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 109647 0 None - 1 Human 8.0 pKi = 8.0 Binding
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 109647 0 None - 1 Human 8.0 pKi = 8.0 Binding
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 89291 0 None 54 2 Human 8.0 pKi = 8.0 Binding
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 89291 0 None 54 2 Human 8.0 pKi = 8.0 Binding
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 197520 0 None - 1 Human 8.0 pKi = 8.0 Binding
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 197520 0 None - 1 Human 8.0 pKi = 8.0 Binding
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 89288 0 None 13 2 Human 7.9 pKi = 7.9 Binding
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 89288 0 None 13 2 Human 7.9 pKi = 7.9 Binding
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 3626 3 None 42 4 Human 7.9 pKi = 7.9 Binding
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 3626 3 None 42 4 Human 7.9 pKi = 7.9 Binding
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 3626 3 None 42 4 Human 7.9 pKi = 7.9 Binding
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 175746 0 None 1 4 Human 7.9 pKi = 7.9 Binding
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 175746 0 None 1 4 Human 7.9 pKi = 7.9 Binding
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 175746 0 None 1 4 Human 7.9 pKi = 7.9 Binding
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 175746 0 None 1 4 Human 7.9 pKi = 7.9 Binding
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 96087 0 None - 1 Human 7.9 pKi = 7.9 Binding
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 96087 0 None - 1 Human 7.9 pKi = 7.9 Binding
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 2119 79 None -4 8 Mouse 7.9 pKi = 7.9 Binding
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 2119 79 None -4 8 Mouse 7.9 pKi = 7.9 Binding
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 2119 79 None -4 8 Mouse 7.9 pKi = 7.9 Binding
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 2119 79 None -4 8 Mouse 7.9 pKi = 7.9 Binding
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 160416 0 None - 1 Human 6.0 pKi = 6.0 Binding
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 160416 0 None - 1 Human 6.0 pKi = 6.0 Binding
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 1404 79 None -194 13 Human 5.0 pKi = 5.0 Binding
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 1404 79 None -194 13 Human 5.0 pKi = 5.0 Binding
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 1404 79 None -194 13 Human 5.0 pKi = 5.0 Binding
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 1404 79 None -194 13 Human 5.0 pKi = 5.0 Binding
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 1404 79 None -194 13 Human 5.0 pKi = 5.0 Binding
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 1404 79 None -194 13 Human 5.0 pKi = 5.0 Binding
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 2006 46 None -89 5 Human 5.0 pKi = 5.0 Binding
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 2006 46 None -89 5 Human 5.0 pKi = 5.0 Binding
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 2006 46 None -89 5 Human 5.0 pKi = 5.0 Binding
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 2006 46 None -89 5 Human 5.0 pKi = 5.0 Binding
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 69379 13 None - 1 Human 7.0 pKi = 7.0 Binding
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 69379 13 None - 1 Human 7.0 pKi = 7.0 Binding
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 58597 0 None -22 2 Human 5.0 pKi = 5.0 Binding
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 58597 0 None -22 2 Human 5.0 pKi = 5.0 Binding
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 185350 0 None -363 4 Human 5.0 pKi = 5.0 Binding
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 185350 0 None -363 4 Human 5.0 pKi = 5.0 Binding
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 185437 0 None -177 4 Human 5.0 pKi = 5.0 Binding
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 185437 0 None -177 4 Human 5.0 pKi = 5.0 Binding
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 175811 0 None 47 2 Human 6.9 pKi = 6.9 Binding
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 175811 0 None 47 2 Human 6.9 pKi = 6.9 Binding
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 175811 0 None 47 2 Human 6.9 pKi = 6.9 Binding
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 123400 0 None - 1 Human 5.9 pKi = 5.9 Binding
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 123400 0 None - 1 Human 5.9 pKi = 5.9 Binding
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 58574 0 None -3 2 Human 5.9 pKi = 5.9 Binding
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 58574 0 None -3 2 Human 5.9 pKi = 5.9 Binding
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 58594 0 None -15 2 Human 5.9 pKi = 5.9 Binding
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 58594 0 None -15 2 Human 5.9 pKi = 5.9 Binding
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 77594 0 None 1 2 Human 6.9 pKi = 6.9 Binding
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 77594 0 None 1 2 Human 6.9 pKi = 6.9 Binding
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 61220 0 None - 1 Human 5.9 pKi = 5.9 Binding
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 61220 0 None - 1 Human 5.9 pKi = 5.9 Binding
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 116620 0 None - 1 Human 6.9 pKi = 6.9 Binding
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 116620 0 None - 1 Human 6.9 pKi = 6.9 Binding
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 95894 0 None - 1 Human 5.9 pKi = 5.9 Binding
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 95894 0 None - 1 Human 5.9 pKi = 5.9 Binding
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 8007 1 None -11 2 Human 4.9 pKi = 4.9 Binding
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 8007 1 None -11 2 Human 4.9 pKi = 4.9 Binding
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 74666 1 None -3 3 Human 6.9 pKi = 6.9 Binding
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 74666 1 None -3 3 Human 6.9 pKi = 6.9 Binding
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 79708 0 None - 1 Human 6.9 pKi = 6.9 Binding
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 79708 0 None - 1 Human 6.9 pKi = 6.9 Binding
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 5422 0 None -25 3 Human 6.9 pKi = 6.9 Binding
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 5422 0 None -25 3 Human 6.9 pKi = 6.9 Binding
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 5422 0 None -25 3 Human 6.9 pKi = 6.9 Binding
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 116621 0 None - 1 Human 6.9 pKi = 6.9 Binding
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 116621 0 None - 1 Human 6.9 pKi = 6.9 Binding
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 2119 79 None -3 8 Human 6.9 pKi = 6.9 Binding
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 2119 79 None -3 8 Human 6.9 pKi = 6.9 Binding
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 2119 79 None -3 8 Human 6.9 pKi = 6.9 Binding
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 2119 79 None -3 8 Human 6.9 pKi = 6.9 Binding
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 111696 0 None - 1 Human 5.9 pKi = 5.9 Binding
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 111696 0 None - 1 Human 5.9 pKi = 5.9 Binding
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 2119 79 None -3 8 Human 7.9 pKi = 7.9 Binding
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 2119 79 None -3 8 Human 7.9 pKi = 7.9 Binding
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 2119 79 None -3 8 Human 7.9 pKi = 7.9 Binding
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 2119 79 None -3 8 Human 7.9 pKi = 7.9 Binding
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 3626 3 None 42 4 Human 7.9 pKi = 7.9 Binding
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 3626 3 None 42 4 Human 7.9 pKi = 7.9 Binding
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 3626 3 None 42 4 Human 7.9 pKi = 7.9 Binding
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 2111 26 None -2 7 Human 7.9 pKi = 7.9 Binding
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 2111 26 None -2 7 Human 7.9 pKi = 7.9 Binding
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 2111 26 None -2 7 Human 7.9 pKi = 7.9 Binding
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 2111 26 None -2 7 Human 7.9 pKi = 7.9 Binding
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 2111 26 None -2 7 Human 7.9 pKi = 7.9 Binding
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 2111 26 None -2 7 Human 7.9 pKi = 7.9 Binding
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 109653 0 None - 1 Human 7.9 pKi = 7.9 Binding
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 109653 0 None - 1 Human 7.9 pKi = 7.9 Binding
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 67765 0 None - 1 Human 7.9 pKi = 7.9 Binding
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 67765 0 None - 1 Human 7.9 pKi = 7.9 Binding
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 2119 79 None -3 8 Human 7.9 pKi = 7.9 Binding
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 2119 79 None -3 8 Human 7.9 pKi = 7.9 Binding
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 2119 79 None -3 8 Human 7.9 pKi = 7.9 Binding
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 2119 79 None -3 8 Human 7.9 pKi = 7.9 Binding
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 2119 79 None -3 8 Human 7.9 pKi = 7.9 Binding
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 2119 79 None -3 8 Human 7.9 pKi = 7.9 Binding
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 2119 79 None -3 8 Human 7.9 pKi = 7.9 Binding
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 2119 79 None -3 8 Human 7.9 pKi = 7.9 Binding
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 1901 114 None -3 23 Human 7.9 pKi = 7.9 Binding
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 1901 114 None -3 23 Human 7.9 pKi = 7.9 Binding
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 1901 114 None -3 23 Human 7.9 pKi = 7.9 Binding
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 1901 114 None -3 23 Human 7.9 pKi = 7.9 Binding
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 1901 114 None -3 23 Human 7.9 pKi = 7.9 Binding
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 1901 114 None -3 23 Human 7.9 pKi = 7.9 Binding
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 2119 79 None -3 8 Human 7.9 pKi = 7.9 Binding
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 2119 79 None -3 8 Human 7.9 pKi = 7.9 Binding
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 2119 79 None -3 8 Human 7.9 pKi = 7.9 Binding
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 2119 79 None -3 8 Human 7.9 pKi = 7.9 Binding
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 1901 114 None -3 23 Human 7.9 pKi = 7.9 Binding
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 1901 114 None -3 23 Human 7.9 pKi = 7.9 Binding
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 1901 114 None -3 23 Human 7.9 pKi = 7.9 Binding
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 1901 114 None -3 23 Human 7.9 pKi = 7.9 Binding
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 1901 114 None -3 23 Human 7.9 pKi = 7.9 Binding
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 1901 114 None -3 23 Human 7.9 pKi = 7.9 Binding
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 1901 114 None -3 23 Human 7.9 pKi = 7.9 Binding
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 1901 114 None -3 23 Human 7.9 pKi = 7.9 Binding
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 1901 114 None -3 23 Human 7.9 pKi = 7.9 Binding
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 1901 114 None -3 23 Human 7.9 pKi = 7.9 Binding
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 1901 114 None -3 23 Human 7.9 pKi = 7.9 Binding
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 1901 114 None -3 23 Human 7.9 pKi = 7.9 Binding
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 175746 0 None 1 4 Human 7.9 pKi = 7.9 Binding
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 175746 0 None 1 4 Human 7.9 pKi = 7.9 Binding
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 175746 0 None 1 4 Human 7.9 pKi = 7.9 Binding
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 175746 0 None 1 4 Human 7.9 pKi = 7.9 Binding
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 1988 16 None 2 6 Human 7.9 pKi = 7.9 Binding
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 1988 16 None 2 6 Human 7.9 pKi = 7.9 Binding
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 1988 16 None 2 6 Human 7.9 pKi = 7.9 Binding
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 292 7 None -4 5 Rat 7.9 pKi = 7.9 Binding
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 292 7 None -4 5 Rat 7.9 pKi = 7.9 Binding
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 292 7 None -4 5 Rat 7.9 pKi = 7.9 Binding
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 292 7 None -4 5 Rat 7.9 pKi = 7.9 Binding
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 89284 0 None 26 2 Human 7.9 pKi = 7.9 Binding
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 89284 0 None 26 2 Human 7.9 pKi = 7.9 Binding
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 89302 0 None 11 2 Human 7.9 pKi = 7.9 Binding
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 89302 0 None 11 2 Human 7.9 pKi = 7.9 Binding
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 292 7 None -4 5 Rat 7.9 pKi = 7.9 Binding
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 292 7 None -4 5 Rat 7.9 pKi = 7.9 Binding
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 292 7 None -4 5 Rat 7.9 pKi = 7.9 Binding
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 292 7 None -4 5 Rat 7.9 pKi = 7.9 Binding
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 2111 26 None -2 7 Human 7.9 pKi = 7.9 Binding
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 2111 26 None -2 7 Human 7.9 pKi = 7.9 Binding
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 2111 26 None -2 7 Human 7.9 pKi = 7.9 Binding
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 2111 26 None -2 7 Human 7.9 pKi = 7.9 Binding
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 2111 26 None -2 7 Human 7.9 pKi = 7.9 Binding
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 2111 26 None -2 7 Human 7.9 pKi = 7.9 Binding
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 187597 6 None -1 2 Human 7.9 pKi = 7.9 Binding
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 187597 6 None -1 2 Human 7.9 pKi = 7.9 Binding
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 187597 6 None -1 2 Human 7.9 pKi = 7.9 Binding
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 1901 114 None -3 23 Human 7.9 pKi = 7.9 Binding
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 1901 114 None -3 23 Human 7.9 pKi = 7.9 Binding
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 1901 114 None -3 23 Human 7.9 pKi = 7.9 Binding
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 1901 114 None -3 23 Human 7.9 pKi = 7.9 Binding
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 1901 114 None -3 23 Human 7.9 pKi = 7.9 Binding
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 1901 114 None -3 23 Human 7.9 pKi = 7.9 Binding
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 175746 0 None 1 4 Human 7.9 pKi = 7.9 Binding
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 175746 0 None 1 4 Human 7.9 pKi = 7.9 Binding
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 175746 0 None 1 4 Human 7.9 pKi = 7.9 Binding
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 175746 0 None 1 4 Human 7.9 pKi = 7.9 Binding
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 1901 114 None -3 23 Human 7.9 pKi = 7.9 Binding
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 1901 114 None -3 23 Human 7.9 pKi = 7.9 Binding
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 1901 114 None -3 23 Human 7.9 pKi = 7.9 Binding
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 1901 114 None -3 23 Human 7.9 pKi = 7.9 Binding
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 1901 114 None -3 23 Human 7.9 pKi = 7.9 Binding
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 1901 114 None -3 23 Human 7.9 pKi = 7.9 Binding
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 1978 14 None -3 3 Human 7.9 pKi = 7.9 Binding
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 1978 14 None -3 3 Human 7.9 pKi = 7.9 Binding
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 1978 14 None -3 3 Human 7.9 pKi = 7.9 Binding
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 2027 7 None -11 4 Human 7.9 pKi = 7.9 Binding
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 2027 7 None -11 4 Human 7.9 pKi = 7.9 Binding
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 2027 7 None -11 4 Human 7.9 pKi = 7.9 Binding
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 168450 0 None -144 3 Human 7.9 pKi = 7.9 Binding
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 168450 0 None -144 3 Human 7.9 pKi = 7.9 Binding
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 168450 0 None -144 3 Human 7.9 pKi = 7.9 Binding
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 168450 0 None -144 3 Human 7.9 pKi = 7.9 Binding
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 168450 0 None -144 3 Human 7.9 pKi = 7.9 Binding
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 168450 0 None -144 3 Human 7.9 pKi = 7.9 Binding
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 2027 7 None -11 4 Human 7.9 pKi = 7.9 Binding
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 2027 7 None -11 4 Human 7.9 pKi = 7.9 Binding
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 2027 7 None -11 4 Human 7.9 pKi = 7.9 Binding
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 1901 114 None -3 23 Human 7.9 pKi = 7.9 Binding
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 1901 114 None -3 23 Human 7.9 pKi = 7.9 Binding
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 1901 114 None -3 23 Human 7.9 pKi = 7.9 Binding
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 1901 114 None -3 23 Human 7.9 pKi = 7.9 Binding
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 1901 114 None -3 23 Human 7.9 pKi = 7.9 Binding
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 1901 114 None -3 23 Human 7.9 pKi = 7.9 Binding
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 19236 2 None - 1 Human 7.9 pKi = 7.9 Binding
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 19236 2 None - 1 Human 7.9 pKi = 7.9 Binding
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 75316 0 None - 1 Human 7.9 pKi = 7.9 Binding
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 75316 0 None - 1 Human 7.9 pKi = 7.9 Binding
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 188073 4 None -4 2 Human 7.9 pKi = 7.9 Binding
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 188073 4 None -4 2 Human 7.9 pKi = 7.9 Binding
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 197853 0 None - 1 Human 7.9 pKi = 7.9 Binding
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 197853 0 None - 1 Human 7.9 pKi = 7.9 Binding
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 4000 13 None -3 3 Human 7.9 pKi = 7.9 Binding
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 4000 13 None -3 3 Human 7.9 pKi = 7.9 Binding
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 4000 13 None -3 3 Human 7.9 pKi = 7.9 Binding
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 193238 0 None -1 2 Human 7.9 pKi = 7.9 Binding
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 193238 0 None -1 2 Human 7.9 pKi = 7.9 Binding
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 193238 0 None -1 2 Human 7.9 pKi = 7.9 Binding
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 2119 79 None -3 8 Human 7.9 pKi = 7.9 Binding
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 2119 79 None -3 8 Human 7.9 pKi = 7.9 Binding
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 2119 79 None -3 8 Human 7.9 pKi = 7.9 Binding
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 2119 79 None -3 8 Human 7.9 pKi = 7.9 Binding
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 1978 14 None -3 3 Human 7.9 pKi = 7.9 Binding
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 1978 14 None -3 3 Human 7.9 pKi = 7.9 Binding
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 1978 14 None -3 3 Human 7.9 pKi = 7.9 Binding
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 192115 0 None -2 2 Human 7.9 pKi = 7.9 Binding
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 192115 0 None -2 2 Human 7.9 pKi = 7.9 Binding
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 139785 0 None 4 2 Human 6.9 pKi = 6.9 Binding
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 139785 0 None 4 2 Human 6.9 pKi = 6.9 Binding
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 67703 0 None - 1 Human 6.9 pKi = 6.9 Binding
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 67703 0 None - 1 Human 6.9 pKi = 6.9 Binding
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 200925 0 None - 1 Human 5.9 pKi = 5.9 Binding
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 200925 0 None - 1 Human 5.9 pKi = 5.9 Binding
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 174152 0 None -323 5 Human 5.9 pKi = 5.9 Binding
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 174152 0 None -323 5 Human 5.9 pKi = 5.9 Binding
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 192439 0 None -8 4 Human 4.9 pKi = 4.9 Binding
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 192439 0 None -8 4 Human 4.9 pKi = 4.9 Binding
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 192439 0 None -8 4 Human 4.9 pKi = 4.9 Binding
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 184255 0 None -120 4 Human 4.9 pKi = 4.9 Binding
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 184255 0 None -120 4 Human 4.9 pKi = 4.9 Binding
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 5722 0 None 1 2 Human 4.9 pKi = 4.9 Binding
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 5722 0 None 1 2 Human 4.9 pKi = 4.9 Binding
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 67779 0 None - 1 Human 6.9 pKi = 6.9 Binding
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 67779 0 None - 1 Human 6.9 pKi = 6.9 Binding
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 6203 0 None -75 3 Human 6.9 pKi = 6.9 Binding
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 6203 0 None -75 3 Human 6.9 pKi = 6.9 Binding
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 6203 0 None -75 3 Human 6.9 pKi = 6.9 Binding
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 292 7 None -22 5 Guinea pig 6.9 pKi = 6.9 Binding
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 292 7 None -22 5 Guinea pig 6.9 pKi = 6.9 Binding
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 292 7 None -22 5 Guinea pig 6.9 pKi = 6.9 Binding
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 292 7 None -22 5 Guinea pig 6.9 pKi = 6.9 Binding
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 292 7 None -22 5 Guinea pig 6.9 pKi = 6.9 Binding
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 292 7 None -22 5 Guinea pig 6.9 pKi = 6.9 Binding
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 292 7 None -22 5 Guinea pig 6.9 pKi = 6.9 Binding
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 292 7 None -22 5 Guinea pig 6.9 pKi = 6.9 Binding
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 940 32 None -363 11 Mouse 6.9 pKi = 6.9 Binding
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 940 32 None -363 11 Mouse 6.9 pKi = 6.9 Binding
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 940 32 None -363 11 Mouse 6.9 pKi = 6.9 Binding
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 6203 0 None -75 3 Human 5.9 pKi = 5.9 Binding
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 6203 0 None -75 3 Human 5.9 pKi = 5.9 Binding
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
CHEMBL345828 6203 0 None -75 3 Human 5.9 pKi = 5.9 Binding
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
11206058 103936 9 None -10 2 Human 4.9 pKi = 4.9 Binding
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 173 3 1 2 1.6 c1ccc(CCc2c[nH]cn2)nc1 10.1021/jm049932u
CHEMBL310360 103936 9 None -10 2 Human 4.9 pKi = 4.9 Binding
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 173 3 1 2 1.6 c1ccc(CCc2c[nH]cn2)nc1 10.1021/jm049932u
1267 3744 43 None -33 25 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]histamine form human H4 receptorDisplacement of [3H]histamine form human H4 receptor
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1021/jm0603318
3035905 3744 43 None -33 25 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]histamine form human H4 receptorDisplacement of [3H]histamine form human H4 receptor
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1021/jm0603318
CHEMBL260374 3744 43 None -33 25 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]histamine form human H4 receptorDisplacement of [3H]histamine form human H4 receptor
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1021/jm0603318
3062060 10283 5 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in SK-NM-C cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in SK-NM-C cells
ChEMBL 221 4 6 3 -1.0 N=C(N)NCc1cccc(CNC(=N)N)n1 10.1021/jm7014777
CHEMBL1162346 10283 5 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in SK-NM-C cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in SK-NM-C cells
ChEMBL 221 4 6 3 -1.0 N=C(N)NCc1cccc(CNC(=N)N)n1 10.1021/jm7014777
11511026 15860 0 None -208 4 Human 6.9 pKi = 6.9 Binding
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 428 7 1 4 5.6 Clc1cccc(N2CCN(CCCCNc3ccc4ccccc4n3)CC2)c1Cl 10.1016/j.ejmech.2016.09.074
CHEMBL1223683 15860 0 None -208 4 Human 6.9 pKi = 6.9 Binding
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 428 7 1 4 5.6 Clc1cccc(N2CCN(CCCCNc3ccc4ccccc4n3)CC2)c1Cl 10.1016/j.ejmech.2016.09.074
1267 3744 43 None -33 25 Human 6.9 pKi = 6.9 Binding
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 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1021/acs.jmedchem.6b00120
3035905 3744 43 None -33 25 Human 6.9 pKi = 6.9 Binding
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 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1021/acs.jmedchem.6b00120
CHEMBL260374 3744 43 None -33 25 Human 6.9 pKi = 6.9 Binding
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 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1021/acs.jmedchem.6b00120
10106063 108783 6 None 16 2 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in human SK-N-MC cell membrane incubated for 60 mins by liquid scintillation counting methodDisplacement of [3H]histamine from human histamine H4 receptor expressed in human SK-N-MC cell membrane incubated for 60 mins by liquid scintillation counting method
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 108783 6 None 16 2 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in human SK-N-MC cell membrane incubated for 60 mins by liquid scintillation counting methodDisplacement of [3H]histamine from human histamine H4 receptor expressed in human SK-N-MC cell membrane incubated for 60 mins by liquid scintillation counting method
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
24826000 67801 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 367 2 2 6 3.2 CN[C@@H]1CCN(c2nc(N)nc3c2sc2cc(C(F)(F)F)ccc23)C1 10.1016/j.bmcl.2011.08.014
CHEMBL1914793 67801 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 367 2 2 6 3.2 CN[C@@H]1CCN(c2nc(N)nc3c2sc2cc(C(F)(F)F)ccc23)C1 10.1016/j.bmcl.2011.08.014
1267 3744 43 None -33 25 Human 6.9 pKi = 6.9 Binding
Binding affinity to human histamine H4 receptorBinding affinity to human histamine H4 receptor
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1021/jm100064d
3035905 3744 43 None -33 25 Human 6.9 pKi = 6.9 Binding
Binding affinity to human histamine H4 receptorBinding affinity to human histamine H4 receptor
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1021/jm100064d
CHEMBL260374 3744 43 None -33 25 Human 6.9 pKi = 6.9 Binding
Binding affinity to human histamine H4 receptorBinding affinity to human histamine H4 receptor
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1021/jm100064d
1278 2119 79 None -4 8 Mouse 6.9 pKi = 6.9 Binding
Displacement of UR-DEBa176 from mouse recombinant H4R expressed in HEK293T-SF-His6-CRE-Luc cellsDisplacement of UR-DEBa176 from mouse recombinant H4R expressed in HEK293T-SF-His6-CRE-Luc cells
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/acs.jmedchem.0c00160
1279 2119 79 None -4 8 Mouse 6.9 pKi = 6.9 Binding
Displacement of UR-DEBa176 from mouse recombinant H4R expressed in HEK293T-SF-His6-CRE-Luc cellsDisplacement of UR-DEBa176 from mouse recombinant H4R expressed in HEK293T-SF-His6-CRE-Luc cells
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/acs.jmedchem.0c00160
4908365 2119 79 None -4 8 Mouse 6.9 pKi = 6.9 Binding
Displacement of UR-DEBa176 from mouse recombinant H4R expressed in HEK293T-SF-His6-CRE-Luc cellsDisplacement of UR-DEBa176 from mouse recombinant H4R expressed in HEK293T-SF-His6-CRE-Luc cells
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/acs.jmedchem.0c00160
CHEMBL129198 2119 79 None -4 8 Mouse 6.9 pKi = 6.9 Binding
Displacement of UR-DEBa176 from mouse recombinant H4R expressed in HEK293T-SF-His6-CRE-Luc cellsDisplacement of UR-DEBa176 from mouse recombinant H4R expressed in HEK293T-SF-His6-CRE-Luc cells
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/acs.jmedchem.0c00160
10106063 108783 6 None 16 2 Human 6.9 pKi = 6.9 Binding
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 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 108783 6 None 16 2 Human 6.9 pKi = 6.9 Binding
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 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
9974306 202769 0 None -15 4 Human 6.9 pKi = 6.9 Binding
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 336 8 3 2 3.4 S=C(NCCCCCc1c[nH]cn1)NCc1ccc(Cl)cc1 10.1016/j.bmcl.2010.10.041
CHEMBL72372 202769 0 None -15 4 Human 6.9 pKi = 6.9 Binding
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 336 8 3 2 3.4 S=C(NCCCCCc1c[nH]cn1)NCc1ccc(Cl)cc1 10.1016/j.bmcl.2010.10.041
56849569 71268 0 None -77 2 Human 6.9 pKi = 6.9 Binding
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 381 7 2 4 4.4 N#Cc1ccc(C/N=C(/NC2CCCCC2)SCCCc2c[nH]cn2)cc1 10.1021/jm201042n
CHEMBL1923033 71268 0 None -77 2 Human 6.9 pKi = 6.9 Binding
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 381 7 2 4 4.4 N#Cc1ccc(C/N=C(/NC2CCCCC2)SCCCc2c[nH]cn2)cc1 10.1021/jm201042n
CHEMBL1963332 71268 0 None -77 2 Human 6.9 pKi = 6.9 Binding
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 381 7 2 4 4.4 N#Cc1ccc(C/N=C(/NC2CCCCC2)SCCCc2c[nH]cn2)cc1 10.1021/jm201042n
11499453 75858 0 None -79 2 Human 6.9 pKi = 6.9 Binding
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 209 8 2 2 2.4 CC(C)CNCCCCCc1c[nH]cn1 10.1021/jm0504353
CHEMBL205834 75858 0 None -79 2 Human 6.9 pKi = 6.9 Binding
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 209 8 2 2 2.4 CC(C)CNCCCCCc1c[nH]cn1 10.1021/jm0504353
11672850 76320 2 None -10 2 Human 6.9 pKi = 6.9 Binding
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 195 7 2 2 2.1 CC(C)NCCCCCc1c[nH]cn1 10.1021/jm0504353
CHEMBL206451 76320 2 None -10 2 Human 6.9 pKi = 6.9 Binding
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 195 7 2 2 2.1 CC(C)NCCCCCc1c[nH]cn1 10.1021/jm0504353
1267 3744 43 None -33 25 Human 6.9 pKi = 6.9 Binding
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 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1016/j.bmc.2009.04.007
3035905 3744 43 None -33 25 Human 6.9 pKi = 6.9 Binding
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 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1016/j.bmc.2009.04.007
CHEMBL260374 3744 43 None -33 25 Human 6.9 pKi = 6.9 Binding
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 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1016/j.bmc.2009.04.007
10106063 108783 6 None 16 2 Human 6.9 pKi = 6.9 Binding
Histamine H4 receptor competition binding using [3H]Na-methylhistamineHistamine H4 receptor competition binding using [3H]Na-methylhistamine
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 108783 6 None 16 2 Human 6.9 pKi = 6.9 Binding
Histamine H4 receptor competition binding using [3H]Na-methylhistamineHistamine H4 receptor competition binding using [3H]Na-methylhistamine
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
5310982 93179 4 None -1348 3 Human 5.9 pKi = 5.9 Binding
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 255 3 2 2 2.6 NCCc1c[nH]c(-c2cccc(C(F)(F)F)c2)n1 10.1016/j.bmcl.2010.10.041
CHEMBL24665 93179 4 None -1348 3 Human 5.9 pKi = 5.9 Binding
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 255 3 2 2 2.6 NCCc1c[nH]c(-c2cccc(C(F)(F)F)c2)n1 10.1016/j.bmcl.2010.10.041
71681975 89220 0 None - 1 Human 5.9 pKi = 5.9 Binding
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 296 5 4 5 1.4 Nc1nccc(NCCNC(=O)c2cc3ccccc3[nH]2)n1 10.1021/jm301886t
CHEMBL2375750 89220 0 None - 1 Human 5.9 pKi = 5.9 Binding
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 296 5 4 5 1.4 Nc1nccc(NCCNC(=O)c2cc3ccccc3[nH]2)n1 10.1021/jm301886t
71681642 89235 0 None - 1 Human 5.9 pKi = 5.9 Binding
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 378 9 4 8 3.1 CC(C)CNc1nc(NCCNc2ccnc(N)n2)cc(-c2ccccc2)n1 10.1021/jm301886t
CHEMBL2375765 89235 0 None - 1 Human 5.9 pKi = 5.9 Binding
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 378 9 4 8 3.1 CC(C)CNc1nc(NCCNc2ccnc(N)n2)cc(-c2ccccc2)n1 10.1021/jm301886t
11286909 203573 2 None -1 2 Human 5.9 pKi = 5.9 Binding
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 c1ccc(CCCc2c[nH]cn2)nc1 10.1021/jm049932u
CHEMBL79126 203573 2 None -1 2 Human 5.9 pKi = 5.9 Binding
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 c1ccc(CCCc2c[nH]cn2)nc1 10.1021/jm049932u
10678661 5290 1 None -61 2 Human 4.9 pKi = 4.9 Binding
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 167 2 2 3 0.6 NC[C@@H]1CC[C@@H](c2c[nH]cn2)O1 10.1016/j.bmcl.2010.10.041
CHEMBL106931 5290 1 None -61 2 Human 4.9 pKi = 4.9 Binding
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 167 2 2 3 0.6 NC[C@@H]1CC[C@@H](c2c[nH]cn2)O1 10.1016/j.bmcl.2010.10.041
11043445 56185 1 None -1 2 Human 4.9 pKi = 4.9 Binding
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
CHEMBL1632410 56185 1 None -1 2 Human 4.9 pKi = 4.9 Binding
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
168294449 192416 0 None -181 6 Human 4.9 pKi = 4.9 Binding
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 192416 0 None -181 6 Human 4.9 pKi = 4.9 Binding
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 192416 0 None -181 6 Human 4.9 pKi = 4.9 Binding
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
66572111 75293 0 None - 1 Human 4.9 pKi = 4.9 Binding
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 285 2 1 3 1.8 CC(=O)c1ccc2[nH]c(C(=O)N3CCN(C)CC3)cc2c1 10.1016/j.ejmech.2012.06.016
CHEMBL2047271 75293 0 None - 1 Human 4.9 pKi = 4.9 Binding
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 285 2 1 3 1.8 CC(=O)c1ccc2[nH]c(C(=O)N3CCN(C)CC3)cc2c1 10.1016/j.ejmech.2012.06.016
118720435 115412 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 225 3 2 5 0.3 CN[C@@H]1CCN(c2cc(CF)nc(N)n2)C1 10.1016/j.bmcl.2014.10.013
CHEMBL3354809 115412 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 225 3 2 5 0.3 CN[C@@H]1CCN(c2cc(CF)nc(N)n2)C1 10.1016/j.bmcl.2014.10.013
90645151 111680 0 None - 1 Human 5.9 pKi = 5.9 Binding
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 304 2 1 6 1.5 CN1CCN(c2nc(N)nc(-c3ccccc3Cl)n2)CC1 10.1016/j.ejmech.2014.06.032
CHEMBL3290572 111680 0 None - 1 Human 5.9 pKi = 5.9 Binding
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 304 2 1 6 1.5 CN1CCN(c2nc(N)nc(-c3ccccc3Cl)n2)CC1 10.1016/j.ejmech.2014.06.032
16082833 79937 0 None -23 2 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]histamine form human H4 receptorDisplacement of [3H]histamine form human H4 receptor
ChEMBL 247 6 2 2 3.1 c1nc([C@H]2C[C@@H]2CCNCC2CCCCC2)c[nH]1 10.1021/jm0603318
CHEMBL214312 79937 0 None -23 2 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]histamine form human H4 receptorDisplacement of [3H]histamine form human H4 receptor
ChEMBL 247 6 2 2 3.1 c1nc([C@H]2C[C@@H]2CCNCC2CCCCC2)c[nH]1 10.1021/jm0603318
54584826 61224 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]histamine from human histamine H4 receptorDisplacement of [3H]histamine from human histamine H4 receptor
ChEMBL 262 3 2 6 0.5 CN[C@@H]1CCN(c2cc(N)nc(N3CCCC3)n2)C1 10.1016/j.bmcl.2011.03.017
CHEMBL1770993 61224 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]histamine from human histamine H4 receptorDisplacement of [3H]histamine from human histamine H4 receptor
ChEMBL 262 3 2 6 0.5 CN[C@@H]1CCN(c2cc(N)nc(N3CCCC3)n2)C1 10.1016/j.bmcl.2011.03.017
57395538 67869 0 None 151 2 Human 6.9 pKi = 6.9 Binding
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 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 67869 0 None 151 2 Human 6.9 pKi = 6.9 Binding
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 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
57395538 67869 0 None 151 2 Human 6.9 pKi = 6.9 Binding
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 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 67869 0 None 151 2 Human 6.9 pKi = 6.9 Binding
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 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
25178343 172022 0 None - 1 Human 6.9 pKi = 6.9 Binding
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 392 4 1 6 3.5 CN1CCN(c2nc(NCc3ccc(C#N)cc3)c3cc(Cl)ccc3n2)CC1 10.1021/jm800876b
CHEMBL448962 172022 0 None - 1 Human 6.9 pKi = 6.9 Binding
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 392 4 1 6 3.5 CN1CCN(c2nc(NCc3ccc(C#N)cc3)c3cc(Cl)ccc3n2)CC1 10.1021/jm800876b
25178343 172022 0 None - 1 Human 6.9 pKi = 6.9 Binding
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 392 4 1 6 3.5 CN1CCN(c2nc(NCc3ccc(C#N)cc3)c3cc(Cl)ccc3n2)CC1 10.1021/jm901379s
CHEMBL448962 172022 0 None - 1 Human 6.9 pKi = 6.9 Binding
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 392 4 1 6 3.5 CN1CCN(c2nc(NCc3ccc(C#N)cc3)c3cc(Cl)ccc3n2)CC1 10.1021/jm901379s
57403269 67775 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 349 1 1 6 2.5 CN1CCN(c2nc(N)nc3c4cc(Cl)ccc4[s+]([O-])c23)CC1 10.1016/j.bmcl.2011.08.014
CHEMBL1914766 67775 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 349 1 1 6 2.5 CN1CCN(c2nc(N)nc3c4cc(Cl)ccc4[s+]([O-])c23)CC1 10.1016/j.bmcl.2011.08.014
24854705 95665 0 None - 1 Human 5.9 pKi = 5.9 Binding
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 321 3 0 6 2.6 CN1CCN(c2nc3ccccc3nc2Oc2cccnc2)CC1 10.1021/jm7014217
CHEMBL260274 95665 0 None - 1 Human 5.9 pKi = 5.9 Binding
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 321 3 0 6 2.6 CN1CCN(c2nc3ccccc3nc2Oc2cccnc2)CC1 10.1021/jm7014217
164619208 185080 0 None -446 4 Human 4.9 pKi = 4.9 Binding
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 378 6 4 4 2.5 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NC(C)c1ccccc1F 10.1016/j.ejmech.2021.113190
CHEMBL4864852 185080 0 None -446 4 Human 4.9 pKi = 4.9 Binding
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 378 6 4 4 2.5 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NC(C)c1ccccc1F 10.1016/j.ejmech.2021.113190
10678661 5290 1 None -61 2 Human 4.9 pKi = 4.9 Binding
Histamine H4 receptor competition binding using [3H]Na-methylhistamineHistamine H4 receptor competition binding using [3H]Na-methylhistamine
ChEMBL 167 2 2 3 0.6 NC[C@@H]1CC[C@@H](c2c[nH]cn2)O1 10.1021/jm0300025
CHEMBL106931 5290 1 None -61 2 Human 4.9 pKi = 4.9 Binding
Histamine H4 receptor competition binding using [3H]Na-methylhistamineHistamine H4 receptor competition binding using [3H]Na-methylhistamine
ChEMBL 167 2 2 3 0.6 NC[C@@H]1CC[C@@H](c2c[nH]cn2)O1 10.1021/jm0300025
57402929 69524 0 None - 1 Human 6.9 pKi = 6.9 Binding
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 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 69524 0 None - 1 Human 6.9 pKi = 6.9 Binding
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 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
1278 2119 79 None -3 8 Human 7.9 pKi = 7.9 Binding
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 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/acs.jmedchem.6b00120
1279 2119 79 None -3 8 Human 7.9 pKi = 7.9 Binding
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 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/acs.jmedchem.6b00120
4908365 2119 79 None -3 8 Human 7.9 pKi = 7.9 Binding
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 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/acs.jmedchem.6b00120
CHEMBL129198 2119 79 None -3 8 Human 7.9 pKi = 7.9 Binding
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 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/acs.jmedchem.6b00120
57392827 67781 0 None - 1 Human 7.9 pKi = 7.9 Binding
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)c2oc3ccc(C(F)(F)F)cc3c2n1 10.1016/j.bmcl.2011.08.014
CHEMBL1914772 67781 0 None - 1 Human 7.9 pKi = 7.9 Binding
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)c2oc3ccc(C(F)(F)F)cc3c2n1 10.1016/j.bmcl.2011.08.014
58227163 175889 0 None 40 2 Human 7.9 pKi = 7.9 Binding
Displacement of 40 nM [3H]-histamine from human H4R expressed in Sf9 cell membranes co-expressing Gia2 and beta1gamma2 by competition binding assayDisplacement of 40 nM [3H]-histamine from human H4R expressed in Sf9 cell membranes co-expressing Gia2 and beta1gamma2 by competition binding assay
ChEMBL 263 3 2 5 1.7 CC(C)(C)CNc1nccc(N2CCCNCC2)n1 10.1021/acs.jmedchem.9b01342
CHEMBL4518374 175889 0 None 40 2 Human 7.9 pKi = 7.9 Binding
Displacement of 40 nM [3H]-histamine from human H4R expressed in Sf9 cell membranes co-expressing Gia2 and beta1gamma2 by competition binding assayDisplacement of 40 nM [3H]-histamine from human H4R expressed in Sf9 cell membranes co-expressing Gia2 and beta1gamma2 by competition binding assay
ChEMBL 263 3 2 5 1.7 CC(C)(C)CNc1nccc(N2CCCNCC2)n1 10.1021/acs.jmedchem.9b01342
CHEMBL4596491 175889 0 None 40 2 Human 7.9 pKi = 7.9 Binding
Displacement of 40 nM [3H]-histamine from human H4R expressed in Sf9 cell membranes co-expressing Gia2 and beta1gamma2 by competition binding assayDisplacement of 40 nM [3H]-histamine from human H4R expressed in Sf9 cell membranes co-expressing Gia2 and beta1gamma2 by competition binding assay
ChEMBL 263 3 2 5 1.7 CC(C)(C)CNc1nccc(N2CCCNCC2)n1 10.1021/acs.jmedchem.9b01342
1204 1901 114 None -3 23 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in SK-NM-C cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in SK-NM-C cells
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm7014777
1247 1901 114 None -3 23 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in SK-NM-C cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in SK-NM-C cells
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm7014777
1375 1901 114 None -3 23 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in SK-NM-C cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in SK-NM-C cells
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm7014777
774 1901 114 None -3 23 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in SK-NM-C cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in SK-NM-C cells
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm7014777
CHEMBL90 1901 114 None -3 23 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in SK-NM-C cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in SK-NM-C cells
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm7014777
DB05381 1901 114 None -3 23 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in SK-NM-C cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in SK-NM-C cells
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm7014777
16082856 80701 0 None -2 2 Human 6.9 pKi = 6.9 Binding
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
CHEMBL215628 80701 0 None -2 2 Human 6.9 pKi = 6.9 Binding
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
46929647 16579 0 None -91 3 Human 5.9 pKi = 5.9 Binding
Binding affinity to human histamine H4 receptorBinding affinity to human histamine H4 receptor
ChEMBL 355 5 2 3 4.3 FC(F)(F)c1ccc(SC[C@H](c2c[nH]cn2)C2CCNCC2)cc1 10.1021/jm100643t
CHEMBL1243394 16579 0 None -91 3 Human 5.9 pKi = 5.9 Binding
Binding affinity to human histamine H4 receptorBinding affinity to human histamine H4 receptor
ChEMBL 355 5 2 3 4.3 FC(F)(F)c1ccc(SC[C@H](c2c[nH]cn2)C2CCNCC2)cc1 10.1021/jm100643t
11858011 158457 0 None - 1 Human 4.9 pKi = 4.9 Binding
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 337 9 0 3 4.6 O=C(c1ccccc1)c1ccc(OCCCCCN2CCCC2)cc1 10.1016/j.ejmech.2016.09.074
CHEMBL4096444 158457 0 None - 1 Human 4.9 pKi = 4.9 Binding
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 337 9 0 3 4.6 O=C(c1ccccc1)c1ccc(OCCCCCN2CCCC2)cc1 10.1016/j.ejmech.2016.09.074
16352 116683 11 None - 1 Human 6.9 pKi = 6.9 Binding
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 293 0 0 4 3.1 CN1CCN(C2=Nc3ccccc3Oc3ccccc32)CC1 10.1021/jm051008s
CHEMBL339414 116683 11 None - 1 Human 6.9 pKi = 6.9 Binding
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 293 0 0 4 3.1 CN1CCN(C2=Nc3ccccc3Oc3ccccc32)CC1 10.1021/jm051008s
11240759 104734 5 None -190 2 Human 5.9 pKi = 5.9 Binding
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 173 3 1 2 1.6 c1cc(CCc2c[nH]cn2)ccn1 10.1021/jm049932u
CHEMBL311473 104734 5 None -190 2 Human 5.9 pKi = 5.9 Binding
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 173 3 1 2 1.6 c1cc(CCc2c[nH]cn2)ccn1 10.1021/jm049932u
24853662 95629 0 None - 1 Human 4.9 pKi = 4.9 Binding
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 326 3 0 5 3.1 CN1CCN(c2nc3ccccc3nc2OC2CCCCC2)CC1 10.1021/jm7014217
CHEMBL260043 95629 0 None - 1 Human 4.9 pKi = 4.9 Binding
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 326 3 0 5 3.1 CN1CCN(c2nc3ccccc3nc2OC2CCCCC2)CC1 10.1021/jm7014217
54584378 62829 0 None -50 2 Human 4.9 pKi = 4.9 Binding
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 251 8 2 3 2.4 CC/C=C/CCNC(=O)OCCCc1c[nH]cn1 10.1016/j.bmcl.2013.06.075
CHEMBL1774595 62829 0 None -50 2 Human 4.9 pKi = 4.9 Binding
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 251 8 2 3 2.4 CC/C=C/CCNC(=O)OCCCc1c[nH]cn1 10.1016/j.bmcl.2013.06.075
CHEMBL1789782 62829 0 None -50 2 Human 4.9 pKi = 4.9 Binding
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 251 8 2 3 2.4 CC/C=C/CCNC(=O)OCCCc1c[nH]cn1 10.1016/j.bmcl.2013.06.075
164626153 185796 0 None -6456 6 Human 4.9 pKi = 4.9 Binding
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 378 6 4 4 2.5 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NC(C)c1cccc(F)c1 10.1016/j.ejmech.2021.113190
CHEMBL4875600 185796 0 None -6456 6 Human 4.9 pKi = 4.9 Binding
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 378 6 4 4 2.5 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NC(C)c1cccc(F)c1 10.1016/j.ejmech.2021.113190
54583874 61217 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]histamine from human histamine H4 receptorDisplacement of [3H]histamine from human histamine H4 receptor
ChEMBL 262 2 1 6 0.4 CN1CCN(c2cc(N)nc(N3CCCC3)n2)CC1 10.1016/j.bmcl.2011.03.017
CHEMBL1770986 61217 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]histamine from human histamine H4 receptorDisplacement of [3H]histamine from human histamine H4 receptor
ChEMBL 262 2 1 6 0.4 CN1CCN(c2cc(N)nc(N3CCCC3)n2)CC1 10.1016/j.bmcl.2011.03.017
54584378 62829 0 None -50 2 Human 5.9 pKi = 5.9 Binding
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 251 8 2 3 2.4 CC/C=C/CCNC(=O)OCCCc1c[nH]cn1 10.1016/j.bmc.2011.03.046
CHEMBL1774595 62829 0 None -50 2 Human 5.9 pKi = 5.9 Binding
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 251 8 2 3 2.4 CC/C=C/CCNC(=O)OCCCc1c[nH]cn1 10.1016/j.bmc.2011.03.046
CHEMBL1789782 62829 0 None -50 2 Human 5.9 pKi = 5.9 Binding
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 251 8 2 3 2.4 CC/C=C/CCNC(=O)OCCCc1c[nH]cn1 10.1016/j.bmc.2011.03.046
46890122 7292 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 421 9 2 5 4.3 Cc1cc(OCCCNCCc2cn(C)cn2)ccc1-c1nc2c(C)c(F)ccc2[nH]1 10.1016/j.bmcl.2010.04.017
CHEMBL1086344 7292 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 421 9 2 5 4.3 Cc1cc(OCCCNCCc2cn(C)cn2)ccc1-c1nc2c(C)c(F)ccc2[nH]1 10.1016/j.bmcl.2010.04.017
155568016 175464 0 None - 1 Human 5.9 pKi = 5.9 Binding
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 264 4 1 6 1.1 CCC(CC)c1nc(N)nc(N2CCN(C)CC2)n1 10.1016/j.bmc.2019.02.020
CHEMBL4590367 175464 0 None - 1 Human 5.9 pKi = 5.9 Binding
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 264 4 1 6 1.1 CCC(CC)c1nc(N)nc(N2CCN(C)CC2)n1 10.1016/j.bmc.2019.02.020
58227319 116624 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 249 5 2 5 1.3 CN[C@H]1CCN(c2ccnc(NCC(C)C)n2)C1 10.1016/j.bmcl.2014.12.027
CHEMBL3393540 116624 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 249 5 2 5 1.3 CN[C@H]1CCN(c2ccnc(NCC(C)C)n2)C1 10.1016/j.bmcl.2014.12.027
56849571 71269 0 None -117 2 Human 6.9 pKi = 6.9 Binding
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 401 8 2 5 4.5 O=[N+]([O-])c1ccc(C/N=C(/NC2CCCCC2)SCCCc2c[nH]cn2)cc1 10.1021/jm201042n
CHEMBL1923034 71269 0 None -117 2 Human 6.9 pKi = 6.9 Binding
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 401 8 2 5 4.5 O=[N+]([O-])c1ccc(C/N=C(/NC2CCCCC2)SCCCc2c[nH]cn2)cc1 10.1021/jm201042n
CHEMBL1963347 71269 0 None -117 2 Human 6.9 pKi = 6.9 Binding
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 401 8 2 5 4.5 O=[N+]([O-])c1ccc(C/N=C(/NC2CCCCC2)SCCCc2c[nH]cn2)cc1 10.1021/jm201042n
25179126 172841 0 None - 1 Human 6.9 pKi = 6.9 Binding
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 371 4 1 6 3.5 Cc1ccc(CNc2nc(N3CCN(C)CC3)nc3ccc(Cl)cc23)o1 10.1021/jm800876b
CHEMBL452849 172841 0 None - 1 Human 6.9 pKi = 6.9 Binding
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 371 4 1 6 3.5 Cc1ccc(CNc2nc(N3CCN(C)CC3)nc3ccc(Cl)cc23)o1 10.1021/jm800876b
25179126 172841 0 None - 1 Human 6.9 pKi = 6.9 Binding
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 371 4 1 6 3.5 Cc1ccc(CNc2nc(N3CCN(C)CC3)nc3ccc(Cl)cc23)o1 10.1021/jm901379s
CHEMBL452849 172841 0 None - 1 Human 6.9 pKi = 6.9 Binding
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 371 4 1 6 3.5 Cc1ccc(CNc2nc(N3CCN(C)CC3)nc3ccc(Cl)cc23)o1 10.1021/jm901379s
164609729 184515 0 None -2187 6 Human 4.9 pKi = 4.9 Binding
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 360 6 4 4 2.3 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)N[C@H](C)c1ccccc1 10.1016/j.ejmech.2021.113190
CHEMBL4856059 184515 0 None -2187 6 Human 4.9 pKi = 4.9 Binding
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 360 6 4 4 2.3 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)N[C@H](C)c1ccccc1 10.1016/j.ejmech.2021.113190
164622886 185360 0 None -131 4 Human 4.9 pKi = 4.9 Binding
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
CHEMBL4869389 185360 0 None -131 4 Human 4.9 pKi = 4.9 Binding
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
164626509 185753 0 None -3 2 Human 4.9 pKi = 4.9 Binding
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 358 3 4 4 3.2 N/C(=N\C(=O)NC1CCCCC1)Nc1cccc(-c2csc(N)n2)c1 10.1016/j.ejmech.2021.113190
CHEMBL4874969 185753 0 None -3 2 Human 4.9 pKi = 4.9 Binding
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 358 3 4 4 3.2 N/C(=N\C(=O)NC1CCCCC1)Nc1cccc(-c2csc(N)n2)c1 10.1016/j.ejmech.2021.113190
11043445 56185 1 None -1 2 Human 4.9 pKi = 4.9 Binding
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
CHEMBL1632410 56185 1 None -1 2 Human 4.9 pKi = 4.9 Binding
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
1204 1901 114 None -12 23 Rat 6.9 pKi = 6.9 Binding
Binding affinity to rat histamine H4 receptorBinding affinity to rat histamine H4 receptor
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.5b00516
1247 1901 114 None -12 23 Rat 6.9 pKi = 6.9 Binding
Binding affinity to rat histamine H4 receptorBinding affinity to rat histamine H4 receptor
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.5b00516
1375 1901 114 None -12 23 Rat 6.9 pKi = 6.9 Binding
Binding affinity to rat histamine H4 receptorBinding affinity to rat histamine H4 receptor
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.5b00516
774 1901 114 None -12 23 Rat 6.9 pKi = 6.9 Binding
Binding affinity to rat histamine H4 receptorBinding affinity to rat histamine H4 receptor
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.5b00516
CHEMBL90 1901 114 None -12 23 Rat 6.9 pKi = 6.9 Binding
Binding affinity to rat histamine H4 receptorBinding affinity to rat histamine H4 receptor
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.5b00516
DB05381 1901 114 None -12 23 Rat 6.9 pKi = 6.9 Binding
Binding affinity to rat histamine H4 receptorBinding affinity to rat histamine H4 receptor
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.5b00516
11609325 14361 0 None - 1 Human 6.9 pKi = 6.9 Binding
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 312 1 1 3 2.3 CN1CCN(C(=O)c2nc3c(Cl)cc(Cl)cc3[nH]2)CC1 10.1021/jm0502081
CHEMBL120221 14361 0 None - 1 Human 6.9 pKi = 6.9 Binding
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 312 1 1 3 2.3 CN1CCN(C(=O)c2nc3c(Cl)cc(Cl)cc3[nH]2)CC1 10.1021/jm0502081
24825796 67753 0 None - 1 Human 6.9 pKi = 6.9 Binding
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 NC[C@H]1CCN(c2nc(N)nc3c2oc2ccc(Cl)cc23)C1 10.1016/j.bmcl.2011.08.014
CHEMBL1914744 67753 0 None - 1 Human 6.9 pKi = 6.9 Binding
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 NC[C@H]1CCN(c2nc(N)nc3c2oc2ccc(Cl)cc23)C1 10.1016/j.bmcl.2011.08.014
46228100 198333 0 None - 1 Human 4.9 pKi = 4.9 Binding
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 315 4 1 6 2.1 CN1CCN(c2cc(SCc3ccccc3)nc(N)n2)CC1 10.1016/j.bmc.2009.08.059
CHEMBL595413 198333 0 None - 1 Human 4.9 pKi = 4.9 Binding
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 315 4 1 6 2.1 CN1CCN(c2cc(SCc3ccccc3)nc(N)n2)CC1 10.1016/j.bmc.2009.08.059
44628631 67782 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 337 1 2 6 2.7 Nc1nc(N2CCNCC2)c2oc3c(Cl)cc(Cl)cc3c2n1 10.1016/j.bmcl.2011.08.014
CHEMBL1914773 67782 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 337 1 2 6 2.7 Nc1nc(N2CCNCC2)c2oc3c(Cl)cc(Cl)cc3c2n1 10.1016/j.bmcl.2011.08.014
71525679 89296 0 None -9 6 Rat 6.9 pKi = 6.9 Binding
Binding affinity to rat histamine H4 receptorBinding affinity to rat histamine H4 receptor
ChEMBL 272 3 2 6 1.0 CCc1cnc2c(N3CC[C@@H](NC)C3)nc(N)nc2c1 10.1016/j.bmcl.2013.02.091
CHEMBL2376801 89296 0 None -9 6 Rat 6.9 pKi = 6.9 Binding
Binding affinity to rat histamine H4 receptorBinding affinity to rat histamine H4 receptor
ChEMBL 272 3 2 6 1.0 CCc1cnc2c(N3CC[C@@H](NC)C3)nc(N)nc2c1 10.1016/j.bmcl.2013.02.091
4060730 19183 51 None - 1 Human 6.9 pKi = 6.9 Binding
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 243 1 1 2 1.6 CN1CCN(C(=O)c2cc3ccccc3[nH]2)CC1 10.1016/j.bmcl.2011.09.001
CHEMBL129199 19183 51 None - 1 Human 6.9 pKi = 6.9 Binding
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 243 1 1 2 1.6 CN1CCN(C(=O)c2cc3ccccc3[nH]2)CC1 10.1016/j.bmcl.2011.09.001
24853594 95691 0 None - 1 Human 5.9 pKi = 5.9 Binding
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 348 4 0 5 3.3 Cc1ccc(COc2nc3ccccc3nc2N2CCN(C)CC2)cc1 10.1021/jm7014217
CHEMBL260470 95691 0 None - 1 Human 5.9 pKi = 5.9 Binding
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 348 4 0 5 3.3 Cc1ccc(COc2nc3ccccc3nc2N2CCN(C)CC2)cc1 10.1021/jm7014217
44414495 79609 0 None -34 3 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]RAMHA from human histamine H4 receptor expressed in SK-N-MC cellsDisplacement of [3H]RAMHA from human histamine H4 receptor expressed in SK-N-MC cells
ChEMBL 404 5 0 2 6.3 CC1CC(C)CN(Cc2ccc(-c3ccc(CN4CC(C)CC(C)C4)cc3)cc2)C1 10.1016/j.bmc.2008.10.029
CHEMBL212869 79609 0 None -34 3 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]RAMHA from human histamine H4 receptor expressed in SK-N-MC cellsDisplacement of [3H]RAMHA from human histamine H4 receptor expressed in SK-N-MC cells
ChEMBL 404 5 0 2 6.3 CC1CC(C)CN(Cc2ccc(-c3ccc(CN4CC(C)CC(C)C4)cc3)cc2)C1 10.1016/j.bmc.2008.10.029
127026017 136833 0 None -12 2 Human 4.9 pKi = 4.9 Binding
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 415 5 1 6 3.6 COc1ccc(CNc2nc3c(c(N4CCN(C)CC4)n2)-c2ccccc2CC3)cc1 10.1016/j.bmcl.2015.12.035
CHEMBL3752972 136833 0 None -12 2 Human 4.9 pKi = 4.9 Binding
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 415 5 1 6 3.6 COc1ccc(CNc2nc3c(c(N4CCN(C)CC4)n2)-c2ccccc2CC3)cc1 10.1016/j.bmcl.2015.12.035
164614907 184001 0 None -436 4 Human 4.9 pKi = 4.9 Binding
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 378 6 4 4 2.5 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NC(C)c1ccc(F)cc1 10.1016/j.ejmech.2021.113190
CHEMBL4848697 184001 0 None -436 4 Human 4.9 pKi = 4.9 Binding
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 378 6 4 4 2.5 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NC(C)c1ccc(F)cc1 10.1016/j.ejmech.2021.113190
57390263 67845 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 330 1 2 7 1.8 Nc1nc(N2CC3CCNC3C2)c2oc3ncc(Cl)cc3c2n1 10.1016/j.bmcl.2011.08.014
CHEMBL1915052 67845 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 330 1 2 7 1.8 Nc1nc(N2CC3CCNC3C2)c2oc3ncc(Cl)cc3c2n1 10.1016/j.bmcl.2011.08.014
9900313 19226 0 None - 1 Human 7.9 pKi = 7.9 Binding
Antagonist activity at Homo sapiens (human) histamine H4 receptorAntagonist activity at Homo sapiens (human) histamine H4 receptor
ChEMBL 279 1 1 2 1.8 CN1CCN(C(=O)c2cc3cc(F)cc(F)c3[nH]2)CC1 10.1007/s00044-004-0106-7
CHEMBL129444 19226 0 None - 1 Human 7.9 pKi = 7.9 Binding
Antagonist activity at Homo sapiens (human) histamine H4 receptorAntagonist activity at Homo sapiens (human) histamine H4 receptor
ChEMBL 279 1 1 2 1.8 CN1CCN(C(=O)c2cc3cc(F)cc(F)c3[nH]2)CC1 10.1007/s00044-004-0106-7
9900313 19226 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]- histamine from the recombinant human histamine H4 receptorDisplacement of [3H]- histamine from the recombinant human histamine H4 receptor
ChEMBL 279 1 1 2 1.8 CN1CCN(C(=O)c2cc3cc(F)cc(F)c3[nH]2)CC1 10.1021/jm0341047
CHEMBL129444 19226 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]- histamine from the recombinant human histamine H4 receptorDisplacement of [3H]- histamine from the recombinant human histamine H4 receptor
ChEMBL 279 1 1 2 1.8 CN1CCN(C(=O)c2cc3cc(F)cc(F)c3[nH]2)CC1 10.1021/jm0341047
1278 2119 79 None -3 8 Human 7.9 pKi = 7.9 Binding
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 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1016/j.bmc.2009.08.059
1279 2119 79 None -3 8 Human 7.9 pKi = 7.9 Binding
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 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1016/j.bmc.2009.08.059
4908365 2119 79 None -3 8 Human 7.9 pKi = 7.9 Binding
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 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1016/j.bmc.2009.08.059
CHEMBL129198 2119 79 None -3 8 Human 7.9 pKi = 7.9 Binding
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 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1016/j.bmc.2009.08.059
46890592 6315 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human 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 6315 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human 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
9900313 19226 0 None - 1 Human 7.9 pKi = 7.9 Binding
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 279 1 1 2 1.8 CN1CCN(C(=O)c2cc3cc(F)cc(F)c3[nH]2)CC1 10.1021/jm0502081
CHEMBL129444 19226 0 None - 1 Human 7.9 pKi = 7.9 Binding
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 279 1 1 2 1.8 CN1CCN(C(=O)c2cc3cc(F)cc(F)c3[nH]2)CC1 10.1021/jm0502081
156013896 177665 0 None -7 4 Human 7.9 pKi = 7.9 Binding
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 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 177665 0 None -7 4 Human 7.9 pKi = 7.9 Binding
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 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 177665 0 None -7 4 Human 7.9 pKi = 7.9 Binding
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 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
25129523 186704 40 None -1 2 Rat 7.9 pKi = 7.9 Binding
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 269 2 1 5 1.5 CN1CCN(c2cc(-c3ccccc3)nc(N)n2)CC1 10.1021/jm800670r
CHEMBL492884 186704 40 None -1 2 Rat 7.9 pKi = 7.9 Binding
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 269 2 1 5 1.5 CN1CCN(c2cc(-c3ccccc3)nc(N)n2)CC1 10.1021/jm800670r
1249 1978 14 None -3 3 Human 7.8 pKi = 7.8 Binding
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 139 4 2 2 0.7 NCCCCc1cnc[nH]1 10.1021/jm049932u
13499360 1978 14 None -3 3 Human 7.8 pKi = 7.8 Binding
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 139 4 2 2 0.7 NCCCCc1cnc[nH]1 10.1021/jm049932u
CHEMBL90019 1978 14 None -3 3 Human 7.8 pKi = 7.8 Binding
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 139 4 2 2 0.7 NCCCCc1cnc[nH]1 10.1021/jm049932u
1204 1901 114 None -3 23 Human 7.8 pKi = 7.8 Binding
Inhibition of [3H]-histamine binding to membranes of SK-N-MC cells expressing the human Histamine H4 receptorInhibition of [3H]-histamine binding to membranes of SK-N-MC cells expressing the human Histamine H4 receptor
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm030905y
1247 1901 114 None -3 23 Human 7.8 pKi = 7.8 Binding
Inhibition of [3H]-histamine binding to membranes of SK-N-MC cells expressing the human Histamine H4 receptorInhibition of [3H]-histamine binding to membranes of SK-N-MC cells expressing the human Histamine H4 receptor
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm030905y
1375 1901 114 None -3 23 Human 7.8 pKi = 7.8 Binding
Inhibition of [3H]-histamine binding to membranes of SK-N-MC cells expressing the human Histamine H4 receptorInhibition of [3H]-histamine binding to membranes of SK-N-MC cells expressing the human Histamine H4 receptor
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm030905y
774 1901 114 None -3 23 Human 7.8 pKi = 7.8 Binding
Inhibition of [3H]-histamine binding to membranes of SK-N-MC cells expressing the human Histamine H4 receptorInhibition of [3H]-histamine binding to membranes of SK-N-MC cells expressing the human Histamine H4 receptor
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm030905y
CHEMBL90 1901 114 None -3 23 Human 7.8 pKi = 7.8 Binding
Inhibition of [3H]-histamine binding to membranes of SK-N-MC cells expressing the human Histamine H4 receptorInhibition of [3H]-histamine binding to membranes of SK-N-MC cells expressing the human Histamine H4 receptor
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm030905y
DB05381 1901 114 None -3 23 Human 7.8 pKi = 7.8 Binding
Inhibition of [3H]-histamine binding to membranes of SK-N-MC cells expressing the human Histamine H4 receptorInhibition of [3H]-histamine binding to membranes of SK-N-MC cells expressing the human Histamine H4 receptor
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm030905y
137655927 158342 0 None 17 2 Human 7.8 pKi = 7.8 Binding
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 403 7 2 3 5.2 O=C(NC(c1ccc(Cl)cc1)c1ccc(Cl)cc1)OCCCc1c[nH]cn1 10.1016/j.ejmech.2016.09.074
CHEMBL4095224 158342 0 None 17 2 Human 7.8 pKi = 7.8 Binding
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 403 7 2 3 5.2 O=C(NC(c1ccc(Cl)cc1)c1ccc(Cl)cc1)OCCCc1c[nH]cn1 10.1016/j.ejmech.2016.09.074
71603141 89290 0 None 14 2 Human 7.8 pKi = 7.8 Binding
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 2 2 5 1.2 CCc1ccc2c(N3CCNCC3)nc(N)nc2c1 10.1016/j.bmcl.2013.02.091
CHEMBL2376795 89290 0 None 14 2 Human 7.8 pKi = 7.8 Binding
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 2 2 5 1.2 CCc1ccc2c(N3CCNCC3)nc(N)nc2c1 10.1016/j.bmcl.2013.02.091
54585779 61222 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]histamine from human histamine H4 receptorDisplacement of [3H]histamine from human histamine H4 receptor
ChEMBL 264 4 2 6 0.7 CN[C@@H]1CCN(c2cc(N)nc(N(C)C(C)C)n2)C1 10.1016/j.bmcl.2011.03.017
CHEMBL1770991 61222 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]histamine from human histamine H4 receptorDisplacement of [3H]histamine from human histamine H4 receptor
ChEMBL 264 4 2 6 0.7 CN[C@@H]1CCN(c2cc(N)nc(N(C)C(C)C)n2)C1 10.1016/j.bmcl.2011.03.017
25179303 188757 0 None - 1 Human 6.9 pKi = 6.9 Binding
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 317 2 1 5 2.6 CNc1nc(N2CCN3CCCC3C2)nc2ccc(Cl)cc12 10.1021/jm800876b
CHEMBL512568 188757 0 None - 1 Human 6.9 pKi = 6.9 Binding
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 317 2 1 5 2.6 CNc1nc(N2CCN3CCCC3C2)nc2ccc(Cl)cc12 10.1021/jm800876b
51354304 58588 0 None -3 2 Human 6.9 pKi = 6.9 Binding
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 287 7 1 4 3.1 c1nc(CCCn2cc(CCC3CCCCC3)nn2)c[nH]1 10.1021/jm1013488
CHEMBL1688972 58588 0 None -3 2 Human 6.9 pKi = 6.9 Binding
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 287 7 1 4 3.1 c1nc(CCCn2cc(CCC3CCCCC3)nn2)c[nH]1 10.1021/jm1013488
71519016 86042 0 None - 1 Human 5.9 pKi = 5.9 Binding
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 322 2 2 5 2.3 CN1CCCN(c2nc(N)nc3[nH]c(-c4ccccc4)cc23)CC1 10.1016/j.bmcl.2012.10.139
CHEMBL2314501 86042 0 None - 1 Human 5.9 pKi = 5.9 Binding
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 322 2 2 5 2.3 CN1CCCN(c2nc(N)nc3[nH]c(-c4ccccc4)cc23)CC1 10.1016/j.bmcl.2012.10.139
71518859 86068 0 None - 1 Human 5.9 pKi = 5.9 Binding
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 294 2 3 5 1.6 Nc1nc(N2CCNCC2)c2cc(-c3ccccc3)[nH]c2n1 10.1016/j.bmcl.2012.10.139
CHEMBL2314772 86068 0 None - 1 Human 5.9 pKi = 5.9 Binding
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 294 2 3 5 1.6 Nc1nc(N2CCNCC2)c2cc(-c3ccccc3)[nH]c2n1 10.1016/j.bmcl.2012.10.139
156014317 177702 0 None 1 2 Human 5.9 pKi = 5.9 Binding
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 575 10 1 3 8.2 Cc1cc(OCCC[n+]2c(C)cc(/C=C/C=C/c3ccc(N(C)C)cc3)cc2C)ccc1-c1nc2c(C)c(F)ccc2[nH]1 10.1021/acs.jmedchem.0c00160
CHEMBL4634728 177702 0 None 1 2 Human 5.9 pKi = 5.9 Binding
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 575 10 1 3 8.2 Cc1cc(OCCC[n+]2c(C)cc(/C=C/C=C/c3ccc(N(C)C)cc3)cc2C)ccc1-c1nc2c(C)c(F)ccc2[nH]1 10.1021/acs.jmedchem.0c00160
CHEMBL4650854 177702 0 None 1 2 Human 5.9 pKi = 5.9 Binding
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 575 10 1 3 8.2 Cc1cc(OCCC[n+]2c(C)cc(/C=C/C=C/c3ccc(N(C)C)cc3)cc2C)ccc1-c1nc2c(C)c(F)ccc2[nH]1 10.1021/acs.jmedchem.0c00160
11724853 96572 0 None -19 4 Human 5.9 pKi = 5.9 Binding
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 340 0 0 4 3.7 CN1CCN(C2=Nc3cc(Cl)ccc3N(C)c3ccccc32)CC1 10.1021/jm051008s
CHEMBL266723 96572 0 None -19 4 Human 5.9 pKi = 5.9 Binding
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 340 0 0 4 3.7 CN1CCN(C2=Nc3cc(Cl)ccc3N(C)c3ccccc32)CC1 10.1021/jm051008s
57398985 67541 0 None -1122 3 Human 4.9 pKi = 4.9 Binding
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 569 12 2 7 4.4 COc1ccc(CN(CCN(C)CC(C)Nc2ccc3[nH]c(C(=O)N4CCN(C)CC4)cc3c2)c2ccccn2)cc1 10.1016/j.bmcl.2011.09.001
CHEMBL1910385 67541 0 None -1122 3 Human 4.9 pKi = 4.9 Binding
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 569 12 2 7 4.4 COc1ccc(CN(CCN(C)CC(C)Nc2ccc3[nH]c(C(=O)N4CCN(C)CC4)cc3c2)c2ccccn2)cc1 10.1016/j.bmcl.2011.09.001
118725539 116607 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 260 2 0 4 1.8 CN1CCN(c2ccnc(N3CCCCC3)c2)CC1 10.1016/j.bmcl.2014.12.027
CHEMBL3393523 116607 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 260 2 0 4 1.8 CN1CCN(c2ccnc(N3CCCCC3)c2)CC1 10.1016/j.bmcl.2014.12.027
16082822 79570 0 None -4 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]histamine form human H4 receptorDisplacement of [3H]histamine form human H4 receptor
ChEMBL 233 5 2 2 2.7 c1nc([C@@H]2C[C@H]2CNCC2CCCCC2)c[nH]1 10.1021/jm0603318
CHEMBL212705 79570 0 None -4 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]histamine form human H4 receptorDisplacement of [3H]histamine form human H4 receptor
ChEMBL 233 5 2 2 2.7 c1nc([C@@H]2C[C@H]2CNCC2CCCCC2)c[nH]1 10.1021/jm0603318
46228160 198177 0 None - 1 Human 4.8 pKi = 4.8 Binding
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 308 3 0 6 1.6 CN1CCN(c2ncnc3c2ncn3Cc2ccccc2)CC1 10.1016/j.bmc.2009.08.059
CHEMBL594468 198177 0 None - 1 Human 4.8 pKi = 4.8 Binding
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 308 3 0 6 1.6 CN1CCN(c2ncnc3c2ncn3Cc2ccccc2)CC1 10.1016/j.bmc.2009.08.059
2306318 86580 12 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-histamine from human histamine H4 receptor expressed in HEK293T cells after 1 to 1.5 hrs by liquid scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor expressed in HEK293T cells after 1 to 1.5 hrs by liquid scintillation counting analysis
ChEMBL 268 1 0 5 2.1 CN1CCN(c2ncnc3c2oc2ccccc23)CC1 10.1039/C5MD00022J
CHEMBL232421 86580 12 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-histamine from human histamine H4 receptor expressed in HEK293T cells after 1 to 1.5 hrs by liquid scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor expressed in HEK293T cells after 1 to 1.5 hrs by liquid scintillation counting analysis
ChEMBL 268 1 0 5 2.1 CN1CCN(c2ncnc3c2oc2ccccc23)CC1 10.1039/C5MD00022J
127036980 136822 0 None -16 2 Human 4.8 pKi = 4.8 Binding
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 385 4 1 5 3.6 CN1CCN(c2nc(NCc3ccccc3)c3c(n2)-c2ccccc2CC3)CC1 10.1016/j.bmcl.2015.12.035
CHEMBL3752885 136822 0 None -16 2 Human 4.8 pKi = 4.8 Binding
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 385 4 1 5 3.6 CN1CCN(c2nc(NCc3ccccc3)c3c(n2)-c2ccccc2CC3)CC1 10.1016/j.bmcl.2015.12.035
57391033 67778 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 287 1 2 6 1.5 Nc1nc(N2CCNCC2)c2oc3cccc(F)c3c2n1 10.1016/j.bmcl.2011.08.014
CHEMBL1914769 67778 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 287 1 2 6 1.5 Nc1nc(N2CCNCC2)c2oc3cccc(F)c3c2n1 10.1016/j.bmcl.2011.08.014
1236 2036 23 None -204 7 Human 6.8 pKi = 6.8 Binding
Binding affinity to the human histamine H4 receptorBinding affinity to the human histamine H4 receptor
ChEMBL 125 2 2 2 0.3 C[C@H](Cc1cnc[nH]1)N 10.1021/jm0341047
1237 2036 23 None -204 7 Human 6.8 pKi = 6.8 Binding
Binding affinity to the human histamine H4 receptorBinding affinity to the human histamine H4 receptor
ChEMBL 125 2 2 2 0.3 C[C@H](Cc1cnc[nH]1)N 10.1021/jm0341047
156615 2036 23 None -204 7 Human 6.8 pKi = 6.8 Binding
Binding affinity to the human histamine H4 receptorBinding affinity to the human histamine H4 receptor
ChEMBL 125 2 2 2 0.3 C[C@H](Cc1cnc[nH]1)N 10.1021/jm0341047
CHEMBL268229 2036 23 None -204 7 Human 6.8 pKi = 6.8 Binding
Binding affinity to the human histamine H4 receptorBinding affinity to the human histamine H4 receptor
ChEMBL 125 2 2 2 0.3 C[C@H](Cc1cnc[nH]1)N 10.1021/jm0341047
24797248 198184 2 None - 1 Human 6.8 pKi = 6.8 Binding
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 324 2 1 6 1.4 CN1CCN(c2cc(N3CCc4ccccc4C3)nc(N)n2)CC1 10.1016/j.bmc.2009.08.059
CHEMBL594490 198184 2 None - 1 Human 6.8 pKi = 6.8 Binding
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 324 2 1 6 1.4 CN1CCN(c2cc(N3CCc4ccccc4C3)nc(N)n2)CC1 10.1016/j.bmc.2009.08.059
9951970 5426 1 None -81 3 Human 5.8 pKi = 5.8 Binding
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 267 9 2 3 3.0 CCCCC[C@H](C)NC(=O)OCCCc1c[nH]cn1 10.1016/j.bmcl.2009.10.005
CHEMBL1076300 5426 1 None -81 3 Human 5.8 pKi = 5.8 Binding
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 267 9 2 3 3.0 CCCCC[C@H](C)NC(=O)OCCCc1c[nH]cn1 10.1016/j.bmcl.2009.10.005
CHEMBL154797 5426 1 None -81 3 Human 5.8 pKi = 5.8 Binding
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 267 9 2 3 3.0 CCCCC[C@H](C)NC(=O)OCCCc1c[nH]cn1 10.1016/j.bmcl.2009.10.005
121238066 166139 0 None - 1 Human 4.8 pKi = 4.8 Binding
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 3 2 8 -1.0 CN1CCN(c2nc(N)nc(CN3C(=O)NC(C)(C)C3=O)n2)CC1 10.1016/j.ejmech.2017.09.035
CHEMBL4282283 166139 0 None - 1 Human 4.8 pKi = 4.8 Binding
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 3 2 8 -1.0 CN1CCN(c2nc(N)nc(CN3C(=O)NC(C)(C)C3=O)n2)CC1 10.1016/j.ejmech.2017.09.035
10860228 116335 1 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]- histamine from the recombinant human histamine H4 receptorDisplacement of [3H]- histamine from the recombinant human histamine H4 receptor
ChEMBL 321 1 1 2 2.3 CN1CCN(C(=O)c2cc3ccc(Br)cc3[nH]2)CC1 10.1021/jm0341047
CHEMBL338001 116335 1 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]- histamine from the recombinant human histamine H4 receptorDisplacement of [3H]- histamine from the recombinant human histamine H4 receptor
ChEMBL 321 1 1 2 2.3 CN1CCN(C(=O)c2cc3ccc(Br)cc3[nH]2)CC1 10.1021/jm0341047
10860228 116335 1 None - 1 Human 6.8 pKi = 6.8 Binding
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 321 1 1 2 2.3 CN1CCN(C(=O)c2cc3ccc(Br)cc3[nH]2)CC1 10.1021/jm0502081
CHEMBL338001 116335 1 None - 1 Human 6.8 pKi = 6.8 Binding
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 321 1 1 2 2.3 CN1CCN(C(=O)c2cc3ccc(Br)cc3[nH]2)CC1 10.1021/jm0502081
3840250 136094 16 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-histamine from human histamine H4 receptor expressed in HEK293T cells after 1 to 1.5 hrs by liquid scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor expressed in HEK293T cells after 1 to 1.5 hrs by liquid scintillation counting analysis
ChEMBL 282 1 0 5 2.4 Cc1nc(N2CCN(C)CC2)c2oc3ccccc3c2n1 10.1039/C5MD00022J
CHEMBL3739776 136094 16 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-histamine from human histamine H4 receptor expressed in HEK293T cells after 1 to 1.5 hrs by liquid scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor expressed in HEK293T cells after 1 to 1.5 hrs by liquid scintillation counting analysis
ChEMBL 282 1 0 5 2.4 Cc1nc(N2CCN(C)CC2)c2oc3ccccc3c2n1 10.1039/C5MD00022J
56851447 71281 0 None -144 2 Human 6.8 pKi = 6.8 Binding
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 424 7 2 3 5.9 Clc1ccc(C/N=C(/NC2CCCCC2)SCCCc2c[nH]cn2)cc1Cl 10.1021/jm201042n
CHEMBL1923026 71281 0 None -144 2 Human 6.8 pKi = 6.8 Binding
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 424 7 2 3 5.9 Clc1ccc(C/N=C(/NC2CCCCC2)SCCCc2c[nH]cn2)cc1Cl 10.1021/jm201042n
CHEMBL1963433 71281 0 None -144 2 Human 6.8 pKi = 6.8 Binding
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 424 7 2 3 5.9 Clc1ccc(C/N=C(/NC2CCCCC2)SCCCc2c[nH]cn2)cc1Cl 10.1021/jm201042n
90645157 111692 0 None - 1 Human 5.8 pKi = 5.8 Binding
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 334 3 1 7 1.5 COc1ccc(-c2nc(N)nc(N3CCN(C)CC3)n2)cc1Cl 10.1016/j.ejmech.2014.06.032
CHEMBL3290584 111692 0 None - 1 Human 5.8 pKi = 5.8 Binding
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 334 3 1 7 1.5 COc1ccc(-c2nc(N)nc(N3CCN(C)CC3)n2)cc1Cl 10.1016/j.ejmech.2014.06.032
2971762 192624 4 None - 1 Human 5.8 pKi = 5.8 Binding
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 347 5 1 5 3.0 CN1CCN(c2nc(NCCc3ccccc3)c3ccccc3n2)CC1 10.1021/jm800876b
CHEMBL523617 192624 4 None - 1 Human 5.8 pKi = 5.8 Binding
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 347 5 1 5 3.0 CN1CCN(c2nc(NCCc3ccccc3)c3ccccc3n2)CC1 10.1021/jm800876b
44450401 155590 0 None - 1 Human 5.8 pKi = 5.8 Binding
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 3 2 4 2.0 O=c1[nH]c2ccc(Cl)cc2nc1NCN1CCCC1 10.1021/jm7014217
CHEMBL406345 155590 0 None - 1 Human 5.8 pKi = 5.8 Binding
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 3 2 4 2.0 O=c1[nH]c2ccc(Cl)cc2nc1NCN1CCCC1 10.1021/jm7014217
2971762 192624 4 None - 1 Human 5.8 pKi = 5.8 Binding
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 347 5 1 5 3.0 CN1CCN(c2nc(NCCc3ccccc3)c3ccccc3n2)CC1 10.1021/jm901379s
CHEMBL523617 192624 4 None - 1 Human 5.8 pKi = 5.8 Binding
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 347 5 1 5 3.0 CN1CCN(c2nc(NCCc3ccccc3)c3ccccc3n2)CC1 10.1021/jm901379s
164622190 185034 0 None -93 2 Human 4.8 pKi = 4.8 Binding
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 360 7 4 4 1.8 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCCc1ccccc1 10.1016/j.ejmech.2021.113190
CHEMBL4864067 185034 0 None -93 2 Human 4.8 pKi = 4.8 Binding
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 360 7 4 4 1.8 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCCc1ccccc1 10.1016/j.ejmech.2021.113190
54586762 61198 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]histamine from human histamine H4 receptorDisplacement of [3H]histamine from human histamine H4 receptor
ChEMBL 297 4 2 5 2.0 CN1CCN(c2cc(N)nc(NCc3ccccc3)c2)CC1 10.1016/j.bmcl.2011.03.017
CHEMBL1770967 61198 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]histamine from human histamine H4 receptorDisplacement of [3H]histamine from human histamine H4 receptor
ChEMBL 297 4 2 5 2.0 CN1CCN(c2cc(N)nc(NCc3ccccc3)c2)CC1 10.1016/j.bmcl.2011.03.017
136066109 198750 0 None -3 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]histamine from human histamine H4 receptorDisplacement of [3H]histamine from human histamine H4 receptor
ChEMBL 289 6 2 2 3.7 Cc1[nH]cnc1[C@@H]1C[C@H]1CCNCc1ccc(Cl)cc1 10.1016/j.bmc.2009.12.046
46231557 198750 0 None -3 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]histamine from human histamine H4 receptorDisplacement of [3H]histamine from human histamine H4 receptor
ChEMBL 289 6 2 2 3.7 Cc1[nH]cnc1[C@@H]1C[C@H]1CCNCc1ccc(Cl)cc1 10.1016/j.bmc.2009.12.046
CHEMBL598291 198750 0 None -3 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]histamine from human histamine H4 receptorDisplacement of [3H]histamine from human histamine H4 receptor
ChEMBL 289 6 2 2 3.7 Cc1[nH]cnc1[C@@H]1C[C@H]1CCNCc1ccc(Cl)cc1 10.1016/j.bmc.2009.12.046
5477514 10282 1 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in SK-NM-C cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in SK-NM-C cells
ChEMBL 408 4 4 5 2.6 C/N=C(\N)N/N=C(/C)c1ccc2sc3ccc(/C(C)=N\N/C(N)=N/C)cc3c2c1 10.1021/jm7014777
CHEMBL1162345 10282 1 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in SK-NM-C cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in SK-NM-C cells
ChEMBL 408 4 4 5 2.6 C/N=C(\N)N/N=C(/C)c1ccc2sc3ccc(/C(C)=N\N/C(N)=N/C)cc3c2c1 10.1021/jm7014777
24826083 67805 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 377 2 2 6 3.0 CN[C@H]1CCN(c2nc(N)nc3c2sc2cc(Br)ccc23)C1 10.1016/j.bmcl.2011.08.014
CHEMBL1914797 67805 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 377 2 2 6 3.0 CN[C@H]1CCN(c2nc(N)nc3c2sc2cc(Br)ccc23)C1 10.1016/j.bmcl.2011.08.014
10988959 117605 4 None - 1 Human 7.8 pKi = 7.8 Binding
Antagonist activity at Homo sapiens (human) histamine H4 receptorAntagonist activity at Homo sapiens (human) histamine H4 receptor
ChEMBL 258 1 2 3 1.1 CN1CCN(C(=O)c2cc3cc(N)ccc3[nH]2)CC1 10.1007/s00044-004-0106-7
CHEMBL340740 117605 4 None - 1 Human 7.8 pKi = 7.8 Binding
Antagonist activity at Homo sapiens (human) histamine H4 receptorAntagonist activity at Homo sapiens (human) histamine H4 receptor
ChEMBL 258 1 2 3 1.1 CN1CCN(C(=O)c2cc3cc(N)ccc3[nH]2)CC1 10.1007/s00044-004-0106-7
4906599 168097 10 None - 1 Human 7.8 pKi = 7.8 Binding
Antagonist activity at Homo sapiens (human) histamine H4 receptorAntagonist activity at Homo sapiens (human) histamine H4 receptor
ChEMBL 261 1 1 2 1.7 CN1CCN(C(=O)c2cc3cc(F)ccc3[nH]2)CC1 10.1007/s00044-004-0106-7
CHEMBL436381 168097 10 None - 1 Human 7.8 pKi = 7.8 Binding
Antagonist activity at Homo sapiens (human) histamine H4 receptorAntagonist activity at Homo sapiens (human) histamine H4 receptor
ChEMBL 261 1 1 2 1.7 CN1CCN(C(=O)c2cc3cc(F)ccc3[nH]2)CC1 10.1007/s00044-004-0106-7
10988959 117605 4 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]- histamine from the recombinant human histamine H4 receptorDisplacement of [3H]- histamine from the recombinant human histamine H4 receptor
ChEMBL 258 1 2 3 1.1 CN1CCN(C(=O)c2cc3cc(N)ccc3[nH]2)CC1 10.1021/jm0341047
CHEMBL340740 117605 4 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]- histamine from the recombinant human histamine H4 receptorDisplacement of [3H]- histamine from the recombinant human histamine H4 receptor
ChEMBL 258 1 2 3 1.1 CN1CCN(C(=O)c2cc3cc(N)ccc3[nH]2)CC1 10.1021/jm0341047
4906599 168097 10 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]- histamine from the recombinant human histamine H4 receptorDisplacement of [3H]- histamine from the recombinant human histamine H4 receptor
ChEMBL 261 1 1 2 1.7 CN1CCN(C(=O)c2cc3cc(F)ccc3[nH]2)CC1 10.1021/jm0341047
CHEMBL436381 168097 10 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]- histamine from the recombinant human histamine H4 receptorDisplacement of [3H]- histamine from the recombinant human histamine H4 receptor
ChEMBL 261 1 1 2 1.7 CN1CCN(C(=O)c2cc3cc(F)ccc3[nH]2)CC1 10.1021/jm0341047
57391819 69393 0 None - 1 Human 7.8 pKi = 7.8 Binding
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 361 3 1 6 2.8 CC(=O)c1cccc(-c2ccc3c(N4CCN(C)CC4)nc(N)nc3c2)c1 10.1016/j.bmcl.2011.10.104
CHEMBL1935570 69393 0 None - 1 Human 7.8 pKi = 7.8 Binding
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 361 3 1 6 2.8 CC(=O)c1cccc(-c2ccc3c(N4CCN(C)CC4)nc(N)nc3c2)c1 10.1016/j.bmcl.2011.10.104
53233801 61216 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]histamine from human histamine H4 receptorDisplacement of [3H]histamine from human histamine H4 receptor
ChEMBL 264 4 2 6 0.9 CC(C)CNc1nc(N)cc(N2CCN(C)CC2)n1 10.1016/j.bmcl.2011.03.017
CHEMBL1770985 61216 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]histamine from human histamine H4 receptorDisplacement of [3H]histamine from human histamine H4 receptor
ChEMBL 264 4 2 6 0.9 CC(C)CNc1nc(N)cc(N2CCN(C)CC2)n1 10.1016/j.bmcl.2011.03.017
10988959 117605 4 None - 1 Human 7.8 pKi = 7.8 Binding
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 258 1 2 3 1.1 CN1CCN(C(=O)c2cc3cc(N)ccc3[nH]2)CC1 10.1021/jm0502081
CHEMBL340740 117605 4 None - 1 Human 7.8 pKi = 7.8 Binding
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 258 1 2 3 1.1 CN1CCN(C(=O)c2cc3cc(N)ccc3[nH]2)CC1 10.1021/jm0502081
4906599 168097 10 None - 1 Human 7.8 pKi = 7.8 Binding
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 261 1 1 2 1.7 CN1CCN(C(=O)c2cc3cc(F)ccc3[nH]2)CC1 10.1021/jm0502081
CHEMBL436381 168097 10 None - 1 Human 7.8 pKi = 7.8 Binding
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 261 1 1 2 1.7 CN1CCN(C(=O)c2cc3cc(F)ccc3[nH]2)CC1 10.1021/jm0502081
71519674 89299 0 None -1 5 Mouse 7.8 pKi = 7.8 Binding
Binding affinity to mouse histamine H4 receptorBinding affinity to mouse histamine H4 receptor
ChEMBL 270 3 2 6 0.9 CNC1CN(c2nc(N)nc3cc(C4CC4)cnc23)C1 10.1016/j.bmcl.2013.02.091
CHEMBL2376804 89299 0 None -1 5 Mouse 7.8 pKi = 7.8 Binding
Binding affinity to mouse histamine H4 receptorBinding affinity to mouse histamine H4 receptor
ChEMBL 270 3 2 6 0.9 CNC1CN(c2nc(N)nc3cc(C4CC4)cnc23)C1 10.1016/j.bmcl.2013.02.091
56835171 69397 0 None 1 9 Human 7.8 pKi = 7.8 Binding
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 295 2 2 6 1.9 Nc1nc(N2CCNCC2)c2ccc(-c3ccco3)cc2n1 10.1016/j.bmcl.2013.02.091
CHEMBL1935574 69397 0 None 1 9 Human 7.8 pKi = 7.8 Binding
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 295 2 2 6 1.9 Nc1nc(N2CCNCC2)c2ccc(-c3ccco3)cc2n1 10.1016/j.bmcl.2013.02.091
71603138 89287 0 None 32 2 Human 7.8 pKi = 7.8 Binding
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 285 2 2 5 1.9 CNC1CN(c2nc(N)nc3cc(C(C)(C)C)ccc23)C1 10.1016/j.bmcl.2013.02.091
CHEMBL2376792 89287 0 None 32 2 Human 7.8 pKi = 7.8 Binding
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 285 2 2 5 1.9 CNC1CN(c2nc(N)nc3cc(C(C)(C)C)ccc23)C1 10.1016/j.bmcl.2013.02.091
25128822 186898 0 None -10 5 Human 7.8 pKi = 7.8 Binding
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 1 1 5 1.6 CN1CCN(c2nc(N)nc3c2CCc2ccccc2-3)CC1 10.1021/jm800670r
CHEMBL494093 186898 0 None -10 5 Human 7.8 pKi = 7.8 Binding
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 1 1 5 1.6 CN1CCN(c2nc(N)nc3c2CCc2ccccc2-3)CC1 10.1021/jm800670r
44129214 197522 0 None - 1 Human 7.8 pKi = 7.8 Binding
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 538 7 2 7 3.7 CN1CCN(c2nc(NCCS(=O)(=O)Nc3ccccc3)c3cc(Br)c(Cl)cc3n2)CC1 10.1021/jm901379s
CHEMBL589782 197522 0 None - 1 Human 7.8 pKi = 7.8 Binding
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 538 7 2 7 3.7 CN1CCN(c2nc(NCCS(=O)(=O)Nc3ccccc3)c3cc(Br)c(Cl)cc3n2)CC1 10.1021/jm901379s
136192874 56189 0 None -1 3 Human 7.8 pKi = 7.8 Binding
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 292 2 2 4 2.7 CN1CCC(/C(=N/O)c2nc3cc(Cl)ccc3[nH]2)CC1 10.1016/j.bmcl.2010.10.041
CHEMBL1632414 56189 0 None -1 3 Human 7.8 pKi = 7.8 Binding
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 292 2 2 4 2.7 CN1CCC(/C(=N/O)c2nc3cc(Cl)ccc3[nH]2)CC1 10.1016/j.bmcl.2010.10.041
25147772 172837 4 None 1 3 Rat 7.8 pKi = 7.8 Binding
Binding affinity to rat histamine H4 receptorBinding affinity to rat histamine H4 receptor
ChEMBL 373 4 1 6 3.7 CN1CCN(c2nc(NCc3cccs3)c3cc(Cl)ccc3n2)CC1 10.1021/jm800876b
CHEMBL452847 172837 4 None 1 3 Rat 7.8 pKi = 7.8 Binding
Binding affinity to rat histamine H4 receptorBinding affinity to rat histamine H4 receptor
ChEMBL 373 4 1 6 3.7 CN1CCN(c2nc(NCc3cccs3)c3cc(Cl)ccc3n2)CC1 10.1021/jm800876b
136192874 56189 0 None -1 3 Rat 7.8 pKi = 7.8 Binding
Binding affinity to rat histamine H4 receptor expressed in human SK-N-MC cells by radioligand displacement assayBinding affinity to rat histamine H4 receptor expressed in human SK-N-MC cells by radioligand displacement 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 56189 0 None -1 3 Rat 7.8 pKi = 7.8 Binding
Binding affinity to rat histamine H4 receptor expressed in human SK-N-MC cells by radioligand displacement assayBinding affinity to rat histamine H4 receptor expressed in human SK-N-MC cells by radioligand displacement 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
1204 1901 114 None -3 23 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-histamine from human histamine H4 receptor expressed in human SK-N-MC cells after 1 hrDisplacement of [3H]-histamine from human histamine H4 receptor expressed in human SK-N-MC cells after 1 hr
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1039/C5MD00022J
1247 1901 114 None -3 23 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-histamine from human histamine H4 receptor expressed in human SK-N-MC cells after 1 hrDisplacement of [3H]-histamine from human histamine H4 receptor expressed in human SK-N-MC cells after 1 hr
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1039/C5MD00022J
1375 1901 114 None -3 23 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-histamine from human histamine H4 receptor expressed in human SK-N-MC cells after 1 hrDisplacement of [3H]-histamine from human histamine H4 receptor expressed in human SK-N-MC cells after 1 hr
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1039/C5MD00022J
774 1901 114 None -3 23 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-histamine from human histamine H4 receptor expressed in human SK-N-MC cells after 1 hrDisplacement of [3H]-histamine from human histamine H4 receptor expressed in human SK-N-MC cells after 1 hr
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1039/C5MD00022J
CHEMBL90 1901 114 None -3 23 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-histamine from human histamine H4 receptor expressed in human SK-N-MC cells after 1 hrDisplacement of [3H]-histamine from human histamine H4 receptor expressed in human SK-N-MC cells after 1 hr
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1039/C5MD00022J
DB05381 1901 114 None -3 23 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-histamine from human histamine H4 receptor expressed in human SK-N-MC cells after 1 hrDisplacement of [3H]-histamine from human histamine H4 receptor expressed in human SK-N-MC cells after 1 hr
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1039/C5MD00022J
1223 940 32 None -60 11 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]histamine from human H4 receptor N4.57Y mutant expressed in HEK293 cells after 1 to 1.5 hrs by scintillation countingDisplacement of [3H]histamine from human H4 receptor N4.57Y 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 940 32 None -60 11 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]histamine from human H4 receptor N4.57Y mutant expressed in HEK293 cells after 1 to 1.5 hrs by scintillation countingDisplacement of [3H]histamine from human H4 receptor N4.57Y 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 940 32 None -60 11 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]histamine from human H4 receptor N4.57Y mutant expressed in HEK293 cells after 1 to 1.5 hrs by scintillation countingDisplacement of [3H]histamine from human H4 receptor N4.57Y 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
1204 1901 114 None -3 23 Human 7.8 pKi = 7.8 Binding
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 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm201042n
1247 1901 114 None -3 23 Human 7.8 pKi = 7.8 Binding
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 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm201042n
1375 1901 114 None -3 23 Human 7.8 pKi = 7.8 Binding
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 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm201042n
774 1901 114 None -3 23 Human 7.8 pKi = 7.8 Binding
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 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm201042n
CHEMBL90 1901 114 None -3 23 Human 7.8 pKi = 7.8 Binding
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 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm201042n
DB05381 1901 114 None -3 23 Human 7.8 pKi = 7.8 Binding
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 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/jm201042n
1278 2119 79 None -3 8 Human 7.8 pKi = 7.8 Binding
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 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/jm201042n
1279 2119 79 None -3 8 Human 7.8 pKi = 7.8 Binding
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 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/jm201042n
4908365 2119 79 None -3 8 Human 7.8 pKi = 7.8 Binding
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 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/jm201042n
CHEMBL129198 2119 79 None -3 8 Human 7.8 pKi = 7.8 Binding
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 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/jm201042n
10967174 19242 3 None -2 2 Human 7.8 pKi = 7.8 Binding
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 1 2 3 1.1 CN1CCN(C(=O)c2cc3cccc(N)c3[nH]2)CC1 10.1016/j.ejmech.2012.06.016
CHEMBL129540 19242 3 None -2 2 Human 7.8 pKi = 7.8 Binding
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 1 2 3 1.1 CN1CCN(C(=O)c2cc3cccc(N)c3[nH]2)CC1 10.1016/j.ejmech.2012.06.016
70681963 75335 0 None - 1 Human 7.8 pKi = 7.8 Binding
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 321 2 1 2 2.9 O=C(c1cc2cc(Cl)cc(F)c2[nH]1)N1CC(N2CCCC2)C1 10.1016/j.ejmech.2012.06.016
CHEMBL2047470 75335 0 None - 1 Human 7.8 pKi = 7.8 Binding
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 321 2 1 2 2.9 O=C(c1cc2cc(Cl)cc(F)c2[nH]1)N1CC(N2CCCC2)C1 10.1016/j.ejmech.2012.06.016
4906599 168097 10 None - 1 Human 7.8 pKi = 7.8 Binding
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 261 1 1 2 1.7 CN1CCN(C(=O)c2cc3cc(F)ccc3[nH]2)CC1 10.1016/j.ejmech.2012.06.016
CHEMBL436381 168097 10 None - 1 Human 7.8 pKi = 7.8 Binding
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 261 1 1 2 1.7 CN1CCN(C(=O)c2cc3cc(F)ccc3[nH]2)CC1 10.1016/j.ejmech.2012.06.016
1278 2119 79 None -3 8 Human 7.8 pKi = 7.8 Binding
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 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/jm7014217
1279 2119 79 None -3 8 Human 7.8 pKi = 7.8 Binding
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 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/jm7014217
4908365 2119 79 None -3 8 Human 7.8 pKi = 7.8 Binding
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 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/jm7014217
CHEMBL129198 2119 79 None -3 8 Human 7.8 pKi = 7.8 Binding
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 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/jm7014217
3035746 187597 6 None -1 2 Human 7.8 pKi = 7.8 Binding
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 414 7 2 3 3.2 N/C(=N/CCc1ccc(I)cc1)SCCCc1cnc[nH]1 10.1016/j.bmc.2009.04.007
CHEMBL1237146 187597 6 None -1 2 Human 7.8 pKi = 7.8 Binding
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 414 7 2 3 3.2 N/C(=N/CCc1ccc(I)cc1)SCCCc1cnc[nH]1 10.1016/j.bmc.2009.04.007
CHEMBL498770 187597 6 None -1 2 Human 7.8 pKi = 7.8 Binding
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 414 7 2 3 3.2 N/C(=N/CCc1ccc(I)cc1)SCCCc1cnc[nH]1 10.1016/j.bmc.2009.04.007
45269820 193679 0 None -1 2 Human 7.8 pKi = 7.8 Binding
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(NCc1cccc(Cl)c1)SCCCc1c[nH]cn1 10.1016/j.bmc.2009.04.007
CHEMBL1202326 193679 0 None -1 2 Human 7.8 pKi = 7.8 Binding
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(NCc1cccc(Cl)c1)SCCCc1c[nH]cn1 10.1016/j.bmc.2009.04.007
CHEMBL551790 193679 0 None -1 2 Human 7.8 pKi = 7.8 Binding
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(NCc1cccc(Cl)c1)SCCCc1c[nH]cn1 10.1016/j.bmc.2009.04.007
1278 2119 79 None -3 8 Human 7.8 pKi = 7.8 Binding
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 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/jm051008s
1279 2119 79 None -3 8 Human 7.8 pKi = 7.8 Binding
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 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/jm051008s
4908365 2119 79 None -3 8 Human 7.8 pKi = 7.8 Binding
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 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/jm051008s
CHEMBL129198 2119 79 None -3 8 Human 7.8 pKi = 7.8 Binding
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 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/jm051008s
155491015 175921 3 None -15 4 Mouse 7.8 pKi = 7.8 Binding
Displacement of [3H]histamine from mouse H4R expressed in HEK293T cells incubated for 2 hrs by microbeta scintillation counting analysisDisplacement of [3H]histamine from mouse H4R expressed in HEK293T cells incubated for 2 hrs by microbeta scintillation counting analysis
ChEMBL 207 4 2 5 0.2 CCCNC1CN(c2ccnc(N)n2)C1 10.1021/acs.jmedchem.9b01462
CHEMBL4441731 175921 3 None -15 4 Mouse 7.8 pKi = 7.8 Binding
Displacement of [3H]histamine from mouse H4R expressed in HEK293T cells incubated for 2 hrs by microbeta scintillation counting analysisDisplacement of [3H]histamine from mouse H4R expressed in HEK293T cells incubated for 2 hrs by microbeta scintillation counting analysis
ChEMBL 207 4 2 5 0.2 CCCNC1CN(c2ccnc(N)n2)C1 10.1021/acs.jmedchem.9b01462
CHEMBL4596734 175921 3 None -15 4 Mouse 7.8 pKi = 7.8 Binding
Displacement of [3H]histamine from mouse H4R expressed in HEK293T cells incubated for 2 hrs by microbeta scintillation counting analysisDisplacement of [3H]histamine from mouse H4R expressed in HEK293T cells incubated for 2 hrs by microbeta scintillation counting analysis
ChEMBL 207 4 2 5 0.2 CCCNC1CN(c2ccnc(N)n2)C1 10.1021/acs.jmedchem.9b01462
25129525 187000 0 None - 1 Human 7.8 pKi = 7.8 Binding
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 299 3 1 6 1.5 COc1ccc(-c2cc(N3CCN(C)CC3)nc(N)n2)cc1 10.1039/C2MD20212C
CHEMBL494648 187000 0 None - 1 Human 7.8 pKi = 7.8 Binding
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 299 3 1 6 1.5 COc1ccc(-c2cc(N3CCN(C)CC3)nc(N)n2)cc1 10.1039/C2MD20212C
46228125 198305 0 None - 1 Human 6.8 pKi = 6.8 Binding
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(c2cc(NCc3ccc(Cl)c(Cl)c3)nc(N)n2)CC1 10.1016/j.bmc.2009.08.059
CHEMBL595215 198305 0 None - 1 Human 6.8 pKi = 6.8 Binding
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(c2cc(NCc3ccc(Cl)c(Cl)c3)nc(N)n2)CC1 10.1016/j.bmc.2009.08.059
46890020 7287 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 410 8 3 4 4.5 Cc1cc(OCCCNCC2CCCCN2)ccc1-c1nc2c(C)c(F)ccc2[nH]1 10.1016/j.bmcl.2010.04.017
CHEMBL1086327 7287 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 410 8 3 4 4.5 Cc1cc(OCCCNCC2CCCCN2)ccc1-c1nc2c(C)c(F)ccc2[nH]1 10.1016/j.bmcl.2010.04.017
42641407 197705 0 None - 1 Human 6.8 pKi = 6.8 Binding
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)c3c(Cl)cc(Cl)cc3n2)CC1 10.1021/jm901379s
CHEMBL591013 197705 0 None - 1 Human 6.8 pKi = 6.8 Binding
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)c3c(Cl)cc(Cl)cc3n2)CC1 10.1021/jm901379s
127036981 136925 0 None -1 2 Human 4.8 pKi = 4.8 Binding
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 399 5 1 5 3.6 CN1CCN(c2nc(NCCc3ccccc3)c3c(n2)-c2ccccc2CC3)CC1 10.1016/j.bmcl.2015.12.035
CHEMBL3753621 136925 0 None -1 2 Human 4.8 pKi = 4.8 Binding
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 399 5 1 5 3.6 CN1CCN(c2nc(NCCc3ccccc3)c3c(n2)-c2ccccc2CC3)CC1 10.1016/j.bmcl.2015.12.035
135570464 178519 3 None - 1 Human 4.8 pKi = 4.8 Binding
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 278 1 1 5 1.7 CN1CCN(c2nc(O)c3cc(Cl)ccc3n2)CC1 10.1021/jm800876b
CHEMBL471712 178519 3 None - 1 Human 4.8 pKi = 4.8 Binding
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 278 1 1 5 1.7 CN1CCN(c2nc(O)c3cc(Cl)ccc3n2)CC1 10.1021/jm800876b
51354297 58578 0 None -5 2 Human 4.8 pKi = 4.8 Binding
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 289 6 1 6 0.4 CN1CCN(Cc2cn(CCCc3c[nH]cn3)nn2)CC1 10.1021/jm1013488
CHEMBL1688943 58578 0 None -5 2 Human 4.8 pKi = 4.8 Binding
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 289 6 1 6 0.4 CN1CCN(Cc2cn(CCCc3c[nH]cn3)nn2)CC1 10.1021/jm1013488
46890074 6525 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 403 8 1 3 6.2 Cc1cc(OCCCCCc2cccnc2)ccc1-c1nc2c(C)c(F)ccc2[nH]1 10.1016/j.bmcl.2010.04.017
CHEMBL1083160 6525 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 403 8 1 3 6.2 Cc1cc(OCCCCCc2cccnc2)ccc1-c1nc2c(C)c(F)ccc2[nH]1 10.1016/j.bmcl.2010.04.017
10107667 62835 0 None -6 2 Human 6.8 pKi = 6.8 Binding
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 279 7 2 3 3.0 O=C(NCCC1CCCCC1)OCCCc1c[nH]cn1 10.1016/j.bmc.2011.03.046
CHEMBL1774599 62835 0 None -6 2 Human 6.8 pKi = 6.8 Binding
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 279 7 2 3 3.0 O=C(NCCC1CCCCC1)OCCCc1c[nH]cn1 10.1016/j.bmc.2011.03.046
CHEMBL1789800 62835 0 None -6 2 Human 6.8 pKi = 6.8 Binding
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 279 7 2 3 3.0 O=C(NCCC1CCCCC1)OCCCc1c[nH]cn1 10.1016/j.bmc.2011.03.046
25178755 176300 0 None - 1 Human 6.8 pKi = 6.8 Binding
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 317 2 1 5 2.6 CNc1nc(N2CCN3CCC[C@H]3C2)nc2ccc(Cl)cc12 10.1021/jm800876b
CHEMBL461537 176300 0 None - 1 Human 6.8 pKi = 6.8 Binding
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 317 2 1 5 2.6 CNc1nc(N2CCN3CCC[C@H]3C2)nc2ccc(Cl)cc12 10.1021/jm800876b
24759518 178729 0 None - 1 Human 6.8 pKi = 6.8 Binding
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 277 1 1 5 1.6 CN1CCN(c2nc(N)c3cc(Cl)ccc3n2)CC1 10.1021/jm901379s
CHEMBL473302 178729 0 None - 1 Human 6.8 pKi = 6.8 Binding
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 277 1 1 5 1.6 CN1CCN(c2nc(N)c3cc(Cl)ccc3n2)CC1 10.1021/jm901379s
1267 3744 43 None -33 25 Human 6.8 pKi = 6.8 Binding
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 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1021/acs.jmedchem.0c00160
3035905 3744 43 None -33 25 Human 6.8 pKi = 6.8 Binding
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 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1021/acs.jmedchem.0c00160
CHEMBL260374 3744 43 None -33 25 Human 6.8 pKi = 6.8 Binding
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 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1021/acs.jmedchem.0c00160
118720439 115419 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 246 2 2 4 2.2 Nc1nc(C2CCCC2)cc(C2CCNCC2)n1 10.1016/j.bmcl.2014.10.013
CHEMBL3354817 115419 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 246 2 2 4 2.2 Nc1nc(C2CCCC2)cc(C2CCNCC2)n1 10.1016/j.bmcl.2014.10.013
24853527 166873 0 None - 1 Human 5.8 pKi = 5.8 Binding
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 363 4 0 6 3.2 CN1CCN(c2nc3ccccc3nc2Oc2cccc(N(C)C)c2)CC1 10.1021/jm7014217
CHEMBL429691 166873 0 None - 1 Human 5.8 pKi = 5.8 Binding
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 363 4 0 6 3.2 CN1CCN(c2nc3ccccc3nc2Oc2cccc(N(C)C)c2)CC1 10.1021/jm7014217
10107667 62835 0 None -6 2 Human 5.8 pKi = 5.8 Binding
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 279 7 2 3 3.0 O=C(NCCC1CCCCC1)OCCCc1c[nH]cn1 10.1016/j.bmcl.2013.06.075
CHEMBL1774599 62835 0 None -6 2 Human 5.8 pKi = 5.8 Binding
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 279 7 2 3 3.0 O=C(NCCC1CCCCC1)OCCCc1c[nH]cn1 10.1016/j.bmcl.2013.06.075
CHEMBL1789800 62835 0 None -6 2 Human 5.8 pKi = 5.8 Binding
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 279 7 2 3 3.0 O=C(NCCC1CCCCC1)OCCCc1c[nH]cn1 10.1016/j.bmcl.2013.06.075
10760516 62842 0 None -9 2 Human 5.8 pKi = 5.8 Binding
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 237 7 2 3 1.9 O=C(NCCC1CC1)OCCCc1c[nH]cn1 10.1016/j.bmcl.2013.06.075
CHEMBL1774598 62842 0 None -9 2 Human 5.8 pKi = 5.8 Binding
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 237 7 2 3 1.9 O=C(NCCC1CC1)OCCCc1c[nH]cn1 10.1016/j.bmcl.2013.06.075
CHEMBL1789829 62842 0 None -9 2 Human 5.8 pKi = 5.8 Binding
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 237 7 2 3 1.9 O=C(NCCC1CC1)OCCCc1c[nH]cn1 10.1016/j.bmcl.2013.06.075
127050431 139785 0 None 4 2 Human 6.8 pKi = 6.8 Binding
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 139785 0 None 4 2 Human 6.8 pKi = 6.8 Binding
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
10760516 62842 0 None -9 2 Human 6.8 pKi = 6.8 Binding
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 237 7 2 3 1.9 O=C(NCCC1CC1)OCCCc1c[nH]cn1 10.1016/j.bmc.2011.03.046
CHEMBL1774598 62842 0 None -9 2 Human 6.8 pKi = 6.8 Binding
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 237 7 2 3 1.9 O=C(NCCC1CC1)OCCCc1c[nH]cn1 10.1016/j.bmc.2011.03.046
CHEMBL1789829 62842 0 None -9 2 Human 6.8 pKi = 6.8 Binding
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 237 7 2 3 1.9 O=C(NCCC1CC1)OCCCc1c[nH]cn1 10.1016/j.bmc.2011.03.046
57391034 67802 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 329 3 2 7 2.2 CN[C@@H]1CCN(c2nc(N)nc3c2sc2cc(OC)ccc23)C1 10.1016/j.bmcl.2011.08.014
CHEMBL1914794 67802 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 329 3 2 7 2.2 CN[C@@H]1CCN(c2nc(N)nc3c2sc2cc(OC)ccc23)C1 10.1016/j.bmcl.2011.08.014
57396299 67767 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 319 1 1 6 2.0 CN1CCN(c2nc(N)nc3c2oc2ccc(F)c(F)c23)CC1 10.1016/j.bmcl.2011.08.014
CHEMBL1914758 67767 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 319 1 1 6 2.0 CN1CCN(c2nc(N)nc3c2oc2ccc(F)c(F)c23)CC1 10.1016/j.bmcl.2011.08.014
57396300 67784 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 305 1 2 6 1.6 Nc1nc(N2CCNCC2)c2oc3ccc(F)c(F)c3c2n1 10.1016/j.bmcl.2011.08.014
CHEMBL1914775 67784 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 305 1 2 6 1.6 Nc1nc(N2CCNCC2)c2oc3ccc(F)c(F)c3c2n1 10.1016/j.bmcl.2011.08.014
46228161 198218 12 None - 1 Human 4.8 pKi = 4.8 Binding
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 233 1 2 6 -0.3 CN1CCN(c2nc(N)nc3[nH]cnc23)CC1 10.1016/j.bmc.2009.08.059
CHEMBL594694 198218 12 None - 1 Human 4.8 pKi = 4.8 Binding
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 233 1 2 6 -0.3 CN1CCN(c2nc(N)nc3[nH]cnc23)CC1 10.1016/j.bmc.2009.08.059
1223 940 32 None -363 11 Mouse 6.8 pKi = 6.8 Binding
Displacement of UR-DEBa176 from mouse recombinant H4R expressed in HEK293T-SF-His6-CRE-Luc cellsDisplacement of UR-DEBa176 from mouse recombinant H4R expressed in HEK293T-SF-His6-CRE-Luc cells
ChEMBL 308 6 2 3 3.2 Clc1ccc(cc1)CN=C(SCCCc1cnc[nH]1)N 10.1021/acs.jmedchem.0c00160
2790 940 32 None -363 11 Mouse 6.8 pKi = 6.8 Binding
Displacement of UR-DEBa176 from mouse recombinant H4R expressed in HEK293T-SF-His6-CRE-Luc cellsDisplacement of UR-DEBa176 from mouse recombinant H4R expressed in HEK293T-SF-His6-CRE-Luc cells
ChEMBL 308 6 2 3 3.2 Clc1ccc(cc1)CN=C(SCCCc1cnc[nH]1)N 10.1021/acs.jmedchem.0c00160
CHEMBL14690 940 32 None -363 11 Mouse 6.8 pKi = 6.8 Binding
Displacement of UR-DEBa176 from mouse recombinant H4R expressed in HEK293T-SF-His6-CRE-Luc cellsDisplacement of UR-DEBa176 from mouse recombinant H4R expressed in HEK293T-SF-His6-CRE-Luc cells
ChEMBL 308 6 2 3 3.2 Clc1ccc(cc1)CN=C(SCCCc1cnc[nH]1)N 10.1021/acs.jmedchem.0c00160
10023327 168450 0 None -144 3 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]JNJ7777120 from human H4 receptor E5.46Q mutant expressed in HEK293 cells after 1 to 1.5 hrs by scintillation countingDisplacement of [3H]JNJ7777120 from human H4 receptor E5.46Q 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 168450 0 None -144 3 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]JNJ7777120 from human H4 receptor E5.46Q mutant expressed in HEK293 cells after 1 to 1.5 hrs by scintillation countingDisplacement of [3H]JNJ7777120 from human H4 receptor E5.46Q 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
11615601 74670 0 None -10 2 Human 6.8 pKi = 6.8 Binding
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 235 6 1 2 3.0 c1nc(CCCCCN2CCCCCC2)c[nH]1 10.1021/jm0504353
CHEMBL203390 74670 0 None -10 2 Human 6.8 pKi = 6.8 Binding
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 235 6 1 2 3.0 c1nc(CCCCCN2CCCCCC2)c[nH]1 10.1021/jm0504353
11600849 140014 0 None -31 2 Human 6.8 pKi = 6.8 Binding
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 195 8 2 2 2.1 CCCNCCCCCc1c[nH]cn1 10.1021/jm0504353
CHEMBL381074 140014 0 None -31 2 Human 6.8 pKi = 6.8 Binding
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 195 8 2 2 2.1 CCCNCCCCCc1c[nH]cn1 10.1021/jm0504353
66572108 75288 0 None - 1 Human 6.8 pKi = 6.8 Binding
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 259 1 2 3 1.3 CN1CCN(C(=O)c2cc3c(O)cccc3[nH]2)CC1 10.1016/j.ejmech.2012.06.016
CHEMBL2047266 75288 0 None - 1 Human 6.8 pKi = 6.8 Binding
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 259 1 2 3 1.3 CN1CCN(C(=O)c2cc3c(O)cccc3[nH]2)CC1 10.1016/j.ejmech.2012.06.016
9965450 75294 3 None - 1 Human 6.8 pKi = 6.8 Binding
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 2 2.2 CN1CCN(C(=O)c2cc3ccc(Cl)cc3[nH]2)CC1 10.1016/j.ejmech.2012.06.016
CHEMBL2047272 75294 3 None - 1 Human 6.8 pKi = 6.8 Binding
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 2 2.2 CN1CCN(C(=O)c2cc3ccc(Cl)cc3[nH]2)CC1 10.1016/j.ejmech.2012.06.016
45268970 194509 0 None -7 2 Human 6.8 pKi = 6.8 Binding
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 318 8 3 4 2.9 COc1ccc(CCNC(=N)SCCCc2c[nH]cn2)cc1 10.1016/j.bmc.2009.04.007
CHEMBL1202325 194509 0 None -7 2 Human 6.8 pKi = 6.8 Binding
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 318 8 3 4 2.9 COc1ccc(CCNC(=N)SCCCc2c[nH]cn2)cc1 10.1016/j.bmc.2009.04.007
CHEMBL561369 194509 0 None -7 2 Human 6.8 pKi = 6.8 Binding
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 318 8 3 4 2.9 COc1ccc(CCNC(=N)SCCCc2c[nH]cn2)cc1 10.1016/j.bmc.2009.04.007
45267238 194556 0 None 1 2 Human 6.8 pKi = 6.8 Binding
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 345 7 4 2 3.5 N=C(NC=C(c1ccccc1)c1ccccc1)NCCCc1c[nH]cn1 10.1016/j.bmc.2009.04.007
CHEMBL561651 194556 0 None 1 2 Human 6.8 pKi = 6.8 Binding
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 345 7 4 2 3.5 N=C(NC=C(c1ccccc1)c1ccccc1)NCCCc1c[nH]cn1 10.1016/j.bmc.2009.04.007
1204 1901 114 None -3 23 Human 6.8 pKi = 6.8 Binding
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 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.0c00160
1247 1901 114 None -3 23 Human 6.8 pKi = 6.8 Binding
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 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.0c00160
1375 1901 114 None -3 23 Human 6.8 pKi = 6.8 Binding
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 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.0c00160
774 1901 114 None -3 23 Human 6.8 pKi = 6.8 Binding
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 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.0c00160
CHEMBL90 1901 114 None -3 23 Human 6.8 pKi = 6.8 Binding
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 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.0c00160
DB05381 1901 114 None -3 23 Human 6.8 pKi = 6.8 Binding
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 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.0c00160
127050019 140234 0 None - 1 Human 6.8 pKi = 6.8 Binding
Inhibition of histamine H4 receptor (unknown origin)Inhibition of histamine H4 receptor (unknown origin)
ChEMBL 233 2 2 5 0.3 CN[C@H]1CCN(c2nc(N)nc3c2CCC3)C1 10.1039/C6MD00108D
CHEMBL3818355 140234 0 None - 1 Human 6.8 pKi = 6.8 Binding
Inhibition of histamine H4 receptor (unknown origin)Inhibition of histamine H4 receptor (unknown origin)
ChEMBL 233 2 2 5 0.3 CN[C@H]1CCN(c2nc(N)nc3c2CCC3)C1 10.1039/C6MD00108D
1194 46 3 None -1318 4 Human 5.8 pKi = 5.8 Binding
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 265 3 2 2 2.3 NCCc1cnc([nH]1)c1cccc(c1)Br 10.1016/j.bmcl.2010.10.041
23786499 46 3 None -1318 4 Human 5.8 pKi = 5.8 Binding
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 265 3 2 2 2.3 NCCc1cnc([nH]1)c1cccc(c1)Br 10.1016/j.bmcl.2010.10.041
CHEMBL26116 46 3 None -1318 4 Human 5.8 pKi = 5.8 Binding
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 265 3 2 2 2.3 NCCc1cnc([nH]1)c1cccc(c1)Br 10.1016/j.bmcl.2010.10.041
127035835 136761 0 None 1 4 Human 5.8 pKi = 5.8 Binding
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 385 4 1 5 3.6 CN1CCN(c2nc(NCc3ccccc3)nc3c2CCc2ccccc2-3)CC1 10.1016/j.bmcl.2015.12.035
CHEMBL3752270 136761 0 None 1 4 Human 5.8 pKi = 5.8 Binding
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 385 4 1 5 3.6 CN1CCN(c2nc(NCc3ccccc3)nc3c2CCc2ccccc2-3)CC1 10.1016/j.bmcl.2015.12.035
70690368 75326 0 None - 1 Human 5.8 pKi = 5.8 Binding
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 271 1 1 2 2.3 Cc1cccc2cc(C(=O)N3CCCN(C)CC3)[nH]c12 10.1016/j.ejmech.2012.06.016
CHEMBL2047461 75326 0 None - 1 Human 5.8 pKi = 5.8 Binding
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 271 1 1 2 2.3 Cc1cccc2cc(C(=O)N3CCCN(C)CC3)[nH]c12 10.1016/j.ejmech.2012.06.016
24854707 95848 0 None - 1 Human 5.8 pKi = 5.8 Binding
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 338 3 0 5 3.3 CN1CCN(c2nc3ccccc3nc2Oc2ccc(F)cc2)CC1 10.1021/jm7014217
CHEMBL261222 95848 0 None - 1 Human 5.8 pKi = 5.8 Binding
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 338 3 0 5 3.3 CN1CCN(c2nc3ccccc3nc2Oc2ccc(F)cc2)CC1 10.1021/jm7014217
57390224 67535 0 None -776 3 Human 4.8 pKi = 4.8 Binding
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 503 8 1 5 4.7 COc1ccc(CN(CCN2CCN(C(=O)c3cc4cc(Cl)ccc4[nH]3)CC2)c2ccccn2)cc1 10.1016/j.bmcl.2011.09.001
CHEMBL1910379 67535 0 None -776 3 Human 4.8 pKi = 4.8 Binding
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 503 8 1 5 4.7 COc1ccc(CN(CCN2CCN(C(=O)c3cc4cc(Cl)ccc4[nH]3)CC2)c2ccccn2)cc1 10.1016/j.bmcl.2011.09.001
4905344 35109 9 None - 1 Human 4.8 pKi = 4.8 Binding
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 COc1ccc2cc(C(=O)N3CCN(C)CC3)[nH]c2c1 10.1016/j.ejmech.2012.06.016
CHEMBL1437043 35109 9 None - 1 Human 4.8 pKi = 4.8 Binding
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 COc1ccc2cc(C(=O)N3CCN(C)CC3)[nH]c2c1 10.1016/j.ejmech.2012.06.016
70690367 75324 0 None - 1 Human 4.8 pKi = 4.8 Binding
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 287 2 1 3 2.0 COc1cccc2cc(C(=O)N3CCCN(C)CC3)[nH]c12 10.1016/j.ejmech.2012.06.016
CHEMBL2047459 75324 0 None - 1 Human 4.8 pKi = 4.8 Binding
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 287 2 1 3 2.0 COc1cccc2cc(C(=O)N3CCCN(C)CC3)[nH]c12 10.1016/j.ejmech.2012.06.016
59777309 109665 0 None - 1 Human 6.8 pKi = 6.8 Binding
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 233 2 2 5 0.3 CN[C@@H]1CCN(c2nc(N)nc3c2CCC3)C1 10.1021/jm401727m
CHEMBL3236581 109665 0 None - 1 Human 6.8 pKi = 6.8 Binding
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 233 2 2 5 0.3 CN[C@@H]1CCN(c2nc(N)nc3c2CCC3)C1 10.1021/jm401727m
57400777 67867 0 None 426 2 Human 7.8 pKi = 7.8 Binding
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 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 67867 0 None 426 2 Human 7.8 pKi = 7.8 Binding
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 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
56835171 69397 0 None 1 9 Human 7.8 pKi = 7.8 Binding
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 295 2 2 6 1.9 Nc1nc(N2CCNCC2)c2ccc(-c3ccco3)cc2n1 10.1016/j.bmcl.2011.10.104
CHEMBL1935574 69397 0 None 1 9 Human 7.8 pKi = 7.8 Binding
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 295 2 2 6 1.9 Nc1nc(N2CCNCC2)c2ccc(-c3ccco3)cc2n1 10.1016/j.bmcl.2011.10.104
3035746 187597 6 None -1 2 Human 7.8 pKi = 7.8 Binding
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 414 7 2 3 3.2 N/C(=N/CCc1ccc(I)cc1)SCCCc1cnc[nH]1 10.1021/acs.jmedchem.6b00120
CHEMBL1237146 187597 6 None -1 2 Human 7.8 pKi = 7.8 Binding
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 414 7 2 3 3.2 N/C(=N/CCc1ccc(I)cc1)SCCCc1cnc[nH]1 10.1021/acs.jmedchem.6b00120
CHEMBL498770 187597 6 None -1 2 Human 7.8 pKi = 7.8 Binding
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 414 7 2 3 3.2 N/C(=N/CCc1ccc(I)cc1)SCCCc1cnc[nH]1 10.1021/acs.jmedchem.6b00120
53378928 115414 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 289 4 2 5 1.4 CN[C@@H]1CCN(c2cc(CCC(F)(F)F)nc(N)n2)C1 10.1016/j.bmcl.2014.10.013
CHEMBL3354812 115414 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 289 4 2 5 1.4 CN[C@@H]1CCN(c2cc(CCC(F)(F)F)nc(N)n2)C1 10.1016/j.bmcl.2014.10.013
44547564 116615 2 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 260 3 1 4 2.2 CN1CCN(c2ccnc(NC3CCCC3)c2)CC1 10.1016/j.bmcl.2014.12.027
CHEMBL3393531 116615 2 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 260 3 1 4 2.2 CN1CCN(c2ccnc(NC3CCCC3)c2)CC1 10.1016/j.bmcl.2014.12.027
57400777 67867 0 None 426 2 Human 7.8 pKi = 7.8 Binding
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 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 67867 0 None 426 2 Human 7.8 pKi = 7.8 Binding
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 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
57400738 67842 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 304 1 2 7 1.5 Nc1nc(N2CC[C@@H](N)C2)c2oc3ncc(Cl)cc3c2n1 10.1016/j.bmcl.2011.08.014
CHEMBL1915049 67842 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 304 1 2 7 1.5 Nc1nc(N2CC[C@@H](N)C2)c2oc3ncc(Cl)cc3c2n1 10.1016/j.bmcl.2011.08.014
56851445 71297 0 None 2 2 Human 7.8 pKi = 7.8 Binding
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 8 2 3 3.8 CCCCN/C(=N/C1CCCC1)SCCCc1c[nH]cn1 10.1021/jm201042n
CHEMBL1923025 71297 0 None 2 2 Human 7.8 pKi = 7.8 Binding
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 8 2 3 3.8 CCCCN/C(=N/C1CCCC1)SCCCc1c[nH]cn1 10.1021/jm201042n
CHEMBL1963551 71297 0 None 2 2 Human 7.8 pKi = 7.8 Binding
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 8 2 3 3.8 CCCCN/C(=N/C1CCCC1)SCCCc1c[nH]cn1 10.1021/jm201042n
71603194 89292 0 None 35 2 Human 7.8 pKi = 7.8 Binding
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 271 3 2 5 1.6 CCc1ccc2c(N3CC[C@@H](NC)C3)nc(N)nc2c1 10.1016/j.bmcl.2013.02.091
CHEMBL2376797 89292 0 None 35 2 Human 7.8 pKi = 7.8 Binding
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 271 3 2 5 1.6 CCc1ccc2c(N3CC[C@@H](NC)C3)nc(N)nc2c1 10.1016/j.bmcl.2013.02.091
45257133 198222 0 None 19 2 Human 7.8 pKi = 7.8 Binding
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 332 4 2 6 2.1 CN1CCN(c2cc(NCc3ccccc3Cl)nc(N)n2)CC1 10.1016/j.bmc.2009.08.059
CHEMBL594721 198222 0 None 19 2 Human 7.8 pKi = 7.8 Binding
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 332 4 2 6 2.1 CN1CCN(c2cc(NCc3ccccc3Cl)nc(N)n2)CC1 10.1016/j.bmc.2009.08.059
155540438 171974 0 None 7 2 Human 6.8 pKi = 6.8 Binding
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 290 3 1 6 1.3 CN1CCN(c2nc(N)nc(CC3CCCCC3)n2)CC1 10.1016/j.bmc.2019.02.020
CHEMBL4483783 171974 0 None 7 2 Human 6.8 pKi = 6.8 Binding
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 290 3 1 6 1.3 CN1CCN(c2nc(N)nc(CC3CCCCC3)n2)CC1 10.1016/j.bmc.2019.02.020
57394625 67975 0 None - 1 Human 5.8 pKi = 5.8 Binding
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 325 7 2 6 1.7 COc1ccccc1Cn1ccc(NCCc2cnc[nH]2)nc1=O 10.1016/j.bmcl.2011.07.114
CHEMBL1916493 67975 0 None - 1 Human 5.8 pKi = 5.8 Binding
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 325 7 2 6 1.7 COc1ccccc1Cn1ccc(NCCc2cnc[nH]2)nc1=O 10.1016/j.bmcl.2011.07.114
124087 1362 106 None -5888 15 Human 4.8 pKi = 4.8 Binding
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 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 nan
7157 1362 106 None -5888 15 Human 4.8 pKi = 4.8 Binding
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 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 nan
814 1362 106 None -5888 15 Human 4.8 pKi = 4.8 Binding
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 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 nan
CHEMBL1172 1362 106 None -5888 15 Human 4.8 pKi = 4.8 Binding
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 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 nan
DB00967 1362 106 None -5888 15 Human 4.8 pKi = 4.8 Binding
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 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 nan
54587791 61214 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]histamine from human histamine H4 receptorDisplacement of [3H]histamine from human histamine H4 receptor
ChEMBL 250 3 2 6 0.6 CC(C)Nc1nc(N)cc(N2CCN(C)CC2)n1 10.1016/j.bmcl.2011.03.017
CHEMBL1770983 61214 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]histamine from human histamine H4 receptorDisplacement of [3H]histamine from human histamine H4 receptor
ChEMBL 250 3 2 6 0.6 CC(C)Nc1nc(N)cc(N2CCN(C)CC2)n1 10.1016/j.bmcl.2011.03.017
10515050 6172 0 None -19 3 Human 6.8 pKi = 6.8 Binding
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 CCCC(C)CNC(=O)OCCCc1c[nH]cn1 10.1016/j.bmcl.2009.10.005
CHEMBL1081541 6172 0 None -19 3 Human 6.8 pKi = 6.8 Binding
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 CCCC(C)CNC(=O)OCCCc1c[nH]cn1 10.1016/j.bmcl.2009.10.005
CHEMBL350478 6172 0 None -19 3 Human 6.8 pKi = 6.8 Binding
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 CCCC(C)CNC(=O)OCCCc1c[nH]cn1 10.1016/j.bmcl.2009.10.005
73355143 91438 0 None -22 2 Human 4.8 pKi = 4.8 Binding
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 323 8 2 4 2.8 O=C(NCCOc1ccccc1Cl)OCCCc1c[nH]cn1 10.1016/j.bmcl.2013.06.075
CHEMBL2413362 91438 0 None -22 2 Human 4.8 pKi = 4.8 Binding
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 323 8 2 4 2.8 O=C(NCCOc1ccccc1Cl)OCCCc1c[nH]cn1 10.1016/j.bmcl.2013.06.075
56678756 65298 3 None - 1 Human 5.8 pKi = 5.8 Binding
Selectivity interaction (GPCR panel (PDSP screen)) EUB0000738a HRH4Selectivity interaction (GPCR panel (PDSP screen)) EUB0000738a HRH4
ChEMBL 391 5 1 4 4.2 CCC(=O)N[C@@H]1CC[C@H](C(=O)N(C)c2ccc(-c3nc4ccccc4o3)cc2)C1 nan
CHEMBL1834199 65298 3 None - 1 Human 5.8 pKi = 5.8 Binding
Selectivity interaction (GPCR panel (PDSP screen)) EUB0000738a HRH4Selectivity interaction (GPCR panel (PDSP screen)) EUB0000738a HRH4
ChEMBL 391 5 1 4 4.2 CCC(=O)N[C@@H]1CC[C@H](C(=O)N(C)c2ccc(-c3nc4ccccc4o3)cc2)C1 nan
137634349 155474 0 None -741 2 Human 4.8 pKi = 4.8 Binding
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 337 6 0 3 4.7 CC(=O)c1ccc(OCc2ccc(CN3CCCC(C)C3)cc2)cc1 10.1016/j.ejmech.2016.09.074
CHEMBL4062122 155474 0 None -741 2 Human 4.8 pKi = 4.8 Binding
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 337 6 0 3 4.7 CC(=O)c1ccc(OCc2ccc(CN3CCCC(C)C3)cc2)cc1 10.1016/j.ejmech.2016.09.074
164626370 185891 0 None -14 6 Human 4.8 pKi = 4.8 Binding
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 338 6 4 4 1.8 CCCCCCNC(=O)/N=C(\N)NC1CCc2nc(N)sc2C1 10.1016/j.ejmech.2021.113190
CHEMBL4876799 185891 0 None -14 6 Human 4.8 pKi = 4.8 Binding
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 338 6 4 4 1.8 CCCCCCNC(=O)/N=C(\N)NC1CCc2nc(N)sc2C1 10.1016/j.ejmech.2021.113190
155568977 175578 0 None -3 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptor expressed in CHO cell membranes after 30 mins by liquid scintillation analysisDisplacement of [3H]histamine from human recombinant histamine H4 receptor expressed in CHO cell membranes after 30 mins by liquid scintillation analysis
ChEMBL 281 6 3 3 2.6 c1ccc2[nH]c(CNCC[C@@H]3C[C@H]3c3c[nH]cn3)nc2c1 10.1016/j.bmcl.2018.10.041
CHEMBL4592695 175578 0 None -3 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptor expressed in CHO cell membranes after 30 mins by liquid scintillation analysisDisplacement of [3H]histamine from human recombinant histamine H4 receptor expressed in CHO cell membranes after 30 mins by liquid scintillation analysis
ChEMBL 281 6 3 3 2.6 c1ccc2[nH]c(CNCC[C@@H]3C[C@H]3c3c[nH]cn3)nc2c1 10.1016/j.bmcl.2018.10.041
24854706 95532 0 None - 1 Human 5.8 pKi = 5.8 Binding
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(c2nc3ccccc3nc2Oc2ccc(Cl)c(Cl)c2)CC1 10.1021/jm7014217
CHEMBL259536 95532 0 None - 1 Human 5.8 pKi = 5.8 Binding
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(c2nc3ccccc3nc2Oc2ccc(Cl)c(Cl)c2)CC1 10.1021/jm7014217
1278 2119 79 None -3 8 Human 7.8 pKi = 7.8 Binding
Antagonist activity at Homo sapiens (human) histamine H4 receptorAntagonist activity at Homo sapiens (human) histamine H4 receptor
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1007/s00044-004-0106-7
1279 2119 79 None -3 8 Human 7.8 pKi = 7.8 Binding
Antagonist activity at Homo sapiens (human) histamine H4 receptorAntagonist activity at Homo sapiens (human) histamine H4 receptor
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1007/s00044-004-0106-7
4908365 2119 79 None -3 8 Human 7.8 pKi = 7.8 Binding
Antagonist activity at Homo sapiens (human) histamine H4 receptorAntagonist activity at Homo sapiens (human) histamine H4 receptor
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1007/s00044-004-0106-7
CHEMBL129198 2119 79 None -3 8 Human 7.8 pKi = 7.8 Binding
Antagonist activity at Homo sapiens (human) histamine H4 receptorAntagonist activity at Homo sapiens (human) histamine H4 receptor
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1007/s00044-004-0106-7
46929554 16575 0 None 11 3 Human 7.8 pKi = 7.8 Binding
Binding affinity to human histamine H4 receptorBinding affinity to human histamine H4 receptor
ChEMBL 349 5 1 3 4.7 FC(F)(F)c1ccc(SCC(c2ccncc2)c2c[nH]cn2)cc1 10.1021/jm100643t
CHEMBL1243367 16575 0 None 11 3 Human 7.8 pKi = 7.8 Binding
Binding affinity to human histamine H4 receptorBinding affinity to human histamine H4 receptor
ChEMBL 349 5 1 3 4.7 FC(F)(F)c1ccc(SCC(c2ccncc2)c2c[nH]cn2)cc1 10.1021/jm100643t
4060730 19183 51 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]- histamine from the recombinant human histamine H4 receptorDisplacement of [3H]- histamine from the recombinant human histamine H4 receptor
ChEMBL 243 1 1 2 1.6 CN1CCN(C(=O)c2cc3ccccc3[nH]2)CC1 10.1021/jm0341047
CHEMBL129199 19183 51 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]- histamine from the recombinant human histamine H4 receptorDisplacement of [3H]- histamine from the recombinant human histamine H4 receptor
ChEMBL 243 1 1 2 1.6 CN1CCN(C(=O)c2cc3ccccc3[nH]2)CC1 10.1021/jm0341047
49841608 69388 0 None - 1 Human 7.8 pKi = 7.8 Binding
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)nc3cc(Br)ccc23)CC1 10.1016/j.bmcl.2011.10.104
CHEMBL1935565 69388 0 None - 1 Human 7.8 pKi = 7.8 Binding
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)nc3cc(Br)ccc23)CC1 10.1016/j.bmcl.2011.10.104
1278 2119 79 None -3 8 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in SK-NM-C cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in SK-NM-C cells
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/jm7014777
1279 2119 79 None -3 8 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in SK-NM-C cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in SK-NM-C cells
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/jm7014777
4908365 2119 79 None -3 8 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in SK-NM-C cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in SK-NM-C cells
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/jm7014777
CHEMBL129198 2119 79 None -3 8 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in SK-NM-C cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in SK-NM-C cells
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/jm7014777
4060730 19183 51 None - 1 Human 7.8 pKi = 7.8 Binding
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 243 1 1 2 1.6 CN1CCN(C(=O)c2cc3ccccc3[nH]2)CC1 10.1021/jm0502081
CHEMBL129199 19183 51 None - 1 Human 7.8 pKi = 7.8 Binding
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 243 1 1 2 1.6 CN1CCN(C(=O)c2cc3ccccc3[nH]2)CC1 10.1021/jm0502081
45379805 197747 0 None - 1 Human 7.8 pKi = 7.8 Binding
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 438 6 1 7 1.9 CN1CCN(c2nc(NCCS(=O)(=O)N3CCCC3)c3cc(Cl)ccc3n2)CC1 10.1021/jm901379s
CHEMBL591248 197747 0 None - 1 Human 7.8 pKi = 7.8 Binding
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 438 6 1 7 1.9 CN1CCN(c2nc(NCCS(=O)(=O)N3CCCC3)c3cc(Cl)ccc3n2)CC1 10.1021/jm901379s
164585473 183979 0 None -3 5 Human 5.8 pKi = 5.8 Binding
Binding affinity to H4 receptor (unknown origin)Binding affinity to H4 receptor (unknown origin)
ChEMBL 503 5 1 2 7.2 O=CN1CCC(c2ccc(-c3cc(C(=O)O)cc4cc(-c5ccc(C(F)(F)F)cc5)ccc34)cc2)CC1 10.1021/acs.jmedchem.1c00164
CHEMBL4848380 183979 0 None -3 5 Human 5.8 pKi = 5.8 Binding
Binding affinity to H4 receptor (unknown origin)Binding affinity to H4 receptor (unknown origin)
ChEMBL 503 5 1 2 7.2 O=CN1CCC(c2ccc(-c3cc(C(=O)O)cc4cc(-c5ccc(C(F)(F)F)cc5)ccc34)cc2)CC1 10.1021/acs.jmedchem.1c00164
71519177 86057 0 None - 1 Human 5.8 pKi = 5.8 Binding
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 312 2 3 5 1.9 Nc1nc(N2CC[C@@H](N)C2)c2cc(-c3ccc(F)cc3)[nH]c2n1 10.1016/j.bmcl.2012.10.139
CHEMBL2314760 86057 0 None - 1 Human 5.8 pKi = 5.8 Binding
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 312 2 3 5 1.9 Nc1nc(N2CC[C@@H](N)C2)c2cc(-c3ccc(F)cc3)[nH]c2n1 10.1016/j.bmcl.2012.10.139
112936262 136752 1 None 3 2 Human 5.8 pKi = 5.8 Binding
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 389 6 1 6 3.5 COc1ccc(CNc2nc(-c3ccccc3)cc(N3CCN(C)CC3)n2)cc1 10.1016/j.bmcl.2015.12.035
CHEMBL3752195 136752 1 None 3 2 Human 5.8 pKi = 5.8 Binding
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 389 6 1 6 3.5 COc1ccc(CNc2nc(-c3ccccc3)cc(N3CCN(C)CC3)n2)cc1 10.1016/j.bmcl.2015.12.035
1403136 179927 7 None - 1 Human 5.8 pKi = 5.8 Binding
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 243 1 1 5 1.0 CN1CCN(c2nc(N)c3ccccc3n2)CC1 10.1021/jm901379s
CHEMBL475331 179927 7 None - 1 Human 5.8 pKi = 5.8 Binding
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 243 1 1 5 1.0 CN1CCN(c2nc(N)c3ccccc3n2)CC1 10.1021/jm901379s
164611143 184133 0 None -75 4 Human 4.8 pKi = 4.8 Binding
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 414 6 4 4 2.9 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NC(c1ccccc1)C(F)(F)F 10.1016/j.ejmech.2021.113190
CHEMBL4850448 184133 0 None -75 4 Human 4.8 pKi = 4.8 Binding
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 414 6 4 4 2.9 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NC(c1ccccc1)C(F)(F)F 10.1016/j.ejmech.2021.113190
137646744 157278 0 None - 1 Human 6.8 pKi = 6.8 Binding
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 391 10 1 5 3.0 O=C(CCNC(=O)C(Cc1ccccc1)Cn1ccnc1)OCc1ccccc1 10.1016/j.ejmech.2016.09.074
CHEMBL4083336 157278 0 None - 1 Human 6.8 pKi = 6.8 Binding
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 391 10 1 5 3.0 O=C(CCNC(=O)C(Cc1ccccc1)Cn1ccnc1)OCc1ccccc1 10.1016/j.ejmech.2016.09.074
56835171 69397 0 None -10 9 Rat 6.8 pKi = 6.8 Binding
Displacement of [3H]histamine from rat H4RDisplacement of [3H]histamine from rat H4R
ChEMBL 295 2 2 6 1.9 Nc1nc(N2CCNCC2)c2ccc(-c3ccco3)cc2n1 10.1016/j.bmcl.2011.10.104
CHEMBL1935574 69397 0 None -10 9 Rat 6.8 pKi = 6.8 Binding
Displacement of [3H]histamine from rat H4RDisplacement of [3H]histamine from rat H4R
ChEMBL 295 2 2 6 1.9 Nc1nc(N2CCNCC2)c2ccc(-c3ccco3)cc2n1 10.1016/j.bmcl.2011.10.104
90645149 111682 0 None - 1 Human 5.8 pKi = 5.8 Binding
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 284 2 1 6 1.2 Cc1cccc(-c2nc(N)nc(N3CCN(C)CC3)n2)c1 10.1016/j.ejmech.2014.06.032
CHEMBL3290574 111682 0 None - 1 Human 5.8 pKi = 5.8 Binding
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 284 2 1 6 1.2 Cc1cccc(-c2nc(N)nc(N3CCN(C)CC3)n2)c1 10.1016/j.ejmech.2014.06.032
46890021 7288 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 424 8 2 4 4.8 Cc1cc(OCCCNCC2CCCCN2C)ccc1-c1nc2c(C)c(F)ccc2[nH]1 10.1016/j.bmcl.2010.04.017
CHEMBL1086328 7288 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 424 8 2 4 4.8 Cc1cc(OCCCNCC2CCCCN2C)ccc1-c1nc2c(C)c(F)ccc2[nH]1 10.1016/j.bmcl.2010.04.017
118725541 116612 2 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 248 5 1 4 2.0 CCCCNc1cc(N2CCN(C)CC2)ccn1 10.1016/j.bmcl.2014.12.027
CHEMBL3393528 116612 2 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 248 5 1 4 2.0 CCCCNc1cc(N2CCN(C)CC2)ccn1 10.1016/j.bmcl.2014.12.027
16082858 79682 0 None -8 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]histamine form human H4 receptorDisplacement of [3H]histamine form human H4 receptor
ChEMBL 247 6 2 2 3.1 c1nc([C@H]2C[C@H]2CCNCC2CCCCC2)c[nH]1 10.1021/jm0603318
CHEMBL213133 79682 0 None -8 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]histamine form human H4 receptorDisplacement of [3H]histamine form human H4 receptor
ChEMBL 247 6 2 2 3.1 c1nc([C@H]2C[C@H]2CCNCC2CCCCC2)c[nH]1 10.1021/jm0603318
45379809 197708 0 None - 1 Human 6.8 pKi = 6.8 Binding
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 420 5 1 8 2.1 CN1CCN(c2nc(NCCN3C(=O)CSC3=O)c3cc(Cl)ccc3n2)CC1 10.1021/jm901379s
CHEMBL591027 197708 0 None - 1 Human 6.8 pKi = 6.8 Binding
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 420 5 1 8 2.1 CN1CCN(c2nc(NCCN3C(=O)CSC3=O)c3cc(Cl)ccc3n2)CC1 10.1021/jm901379s
135398737 944 89 None -57 91 Human 6.8 pKi = 6.8 Binding
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
38 944 89 None -57 91 Human 6.8 pKi = 6.8 Binding
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
722 944 89 None -57 91 Human 6.8 pKi = 6.8 Binding
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 944 89 None -57 91 Human 6.8 pKi = 6.8 Binding
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 944 89 None -57 91 Human 6.8 pKi = 6.8 Binding
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
10575070 67539 0 None -79 2 Human 4.8 pKi = 4.8 Binding
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 439 7 1 3 4.7 O=C(c1cc2ccccc2[nH]1)N1CCN(CCOC(c2ccccc2)c2ccccc2)CC1 10.1016/j.bmcl.2011.09.001
CHEMBL1910383 67539 0 None -79 2 Human 4.8 pKi = 4.8 Binding
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 439 7 1 3 4.7 O=C(c1cc2ccccc2[nH]1)N1CCN(CCOC(c2ccccc2)c2ccccc2)CC1 10.1016/j.bmcl.2011.09.001
164622330 185280 0 None -724 6 Human 4.8 pKi = 4.8 Binding
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 360 6 4 4 2.3 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)N[C@@H](C)c1ccccc1 10.1016/j.ejmech.2021.113190
CHEMBL4867962 185280 0 None -724 6 Human 4.8 pKi = 4.8 Binding
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 360 6 4 4 2.3 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)N[C@@H](C)c1ccccc1 10.1016/j.ejmech.2021.113190
1267 3744 43 None -33 25 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in sf9 cells co-expressing mammalian Galphai2 and Gbeta1gamma2Displacement of [3H]histamine from human histamine H4 receptor expressed in sf9 cells co-expressing mammalian Galphai2 and Gbeta1gamma2
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1021/acs.jmedchem.6b00120
3035905 3744 43 None -33 25 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in sf9 cells co-expressing mammalian Galphai2 and Gbeta1gamma2Displacement of [3H]histamine from human histamine H4 receptor expressed in sf9 cells co-expressing mammalian Galphai2 and Gbeta1gamma2
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1021/acs.jmedchem.6b00120
CHEMBL260374 3744 43 None -33 25 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in sf9 cells co-expressing mammalian Galphai2 and Gbeta1gamma2Displacement of [3H]histamine from human histamine H4 receptor expressed in sf9 cells co-expressing mammalian Galphai2 and Gbeta1gamma2
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1021/acs.jmedchem.6b00120
122193098 123399 0 None - 1 Human 5.8 pKi = 5.8 Binding
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 364 3 1 6 2.7 CN1CCN(c2nc(N)nc(/C=C/c3ccc(Cl)c(Cl)c3)n2)CC1 10.1016/j.ejmech.2015.08.014
CHEMBL3628045 123399 0 None - 1 Human 5.8 pKi = 5.8 Binding
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 364 3 1 6 2.7 CN1CCN(c2nc(N)nc(/C=C/c3ccc(Cl)c(Cl)c3)n2)CC1 10.1016/j.ejmech.2015.08.014
90645162 111697 0 None - 1 Human 5.8 pKi = 5.8 Binding
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 324 2 1 6 1.3 CN1CCN(c2nc(N)nc(-c3cc(F)c(F)c(F)c3)n2)CC1 10.1016/j.ejmech.2014.06.032
CHEMBL3290589 111697 0 None - 1 Human 5.8 pKi = 5.8 Binding
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 324 2 1 6 1.3 CN1CCN(c2nc(N)nc(-c3cc(F)c(F)c(F)c3)n2)CC1 10.1016/j.ejmech.2014.06.032
24745507 67878 0 None - 1 Human 7.8 pKi = 7.8 Binding
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 302 5 3 6 1.2 CNC1CN(c2cc(NCc3cccc(F)c3)nc(N)n2)C1 10.1016/j.bmcl.2011.07.125
CHEMBL1915538 67878 0 None - 1 Human 7.8 pKi = 7.8 Binding
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 302 5 3 6 1.2 CNC1CN(c2cc(NCc3cccc(F)c3)nc(N)n2)C1 10.1016/j.bmcl.2011.07.125
45257133 198222 0 None 19 2 Human 7.8 pKi = 7.8 Binding
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 332 4 2 6 2.1 CN1CCN(c2cc(NCc3ccccc3Cl)nc(N)n2)CC1 10.1016/j.bmc.2009.08.059
CHEMBL594721 198222 0 None 19 2 Human 7.8 pKi = 7.8 Binding
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 332 4 2 6 2.1 CN1CCN(c2cc(NCc3ccccc3Cl)nc(N)n2)CC1 10.1016/j.bmc.2009.08.059
24826165 67772 0 None - 1 Human 7.8 pKi = 7.8 Binding
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)nc3c2sc2cc(Cl)ccc23)CC1 10.1016/j.bmcl.2011.08.014
CHEMBL1914763 67772 0 None - 1 Human 7.8 pKi = 7.8 Binding
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)nc3c2sc2cc(Cl)ccc23)CC1 10.1016/j.bmcl.2011.08.014
1278 2119 79 None -3 8 Human 7.7 pKi = 7.7 Binding
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 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1016/j.bmcl.2011.09.001
1279 2119 79 None -3 8 Human 7.7 pKi = 7.7 Binding
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 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1016/j.bmcl.2011.09.001
4908365 2119 79 None -3 8 Human 7.7 pKi = 7.7 Binding
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 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1016/j.bmcl.2011.09.001
CHEMBL129198 2119 79 None -3 8 Human 7.7 pKi = 7.7 Binding
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 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1016/j.bmcl.2011.09.001
3032915 15321 20 None -1 6 Human 6.8 pKi = 6.8 Binding
Binding affinity to the human histamine H4 receptorBinding affinity to the human histamine H4 receptor
ChEMBL 212 5 3 2 1.2 C/N=C(\S)NCCCCc1c[nH]cn1 10.1021/jm0341047
CHEMBL12160 15321 20 None -1 6 Human 6.8 pKi = 6.8 Binding
Binding affinity to the human histamine H4 receptorBinding affinity to the human histamine H4 receptor
ChEMBL 212 5 3 2 1.2 C/N=C(\S)NCCCCc1c[nH]cn1 10.1021/jm0341047
127052294 139772 0 None 5 4 Human 6.8 pKi = 6.8 Binding
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
CHEMBL3806079 139772 0 None 5 4 Human 6.8 pKi = 6.8 Binding
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
57394550 67774 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 329 2 1 7 2.2 COc1ccc2c(c1)sc1c(N3CCN(C)CC3)nc(N)nc12 10.1016/j.bmcl.2011.08.014
CHEMBL1914765 67774 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 329 2 1 7 2.2 COc1ccc2c(c1)sc1c(N3CCN(C)CC3)nc(N)nc12 10.1016/j.bmcl.2011.08.014
51354009 58575 0 None -2 2 Human 6.7 pKi = 6.7 Binding
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 267 6 1 4 2.2 c1ccc(Cc2cn(CCCc3c[nH]cn3)nn2)cc1 10.1021/jm1013488
CHEMBL1688940 58575 0 None -2 2 Human 6.7 pKi = 6.7 Binding
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 267 6 1 4 2.2 c1ccc(Cc2cn(CCCc3c[nH]cn3)nn2)cc1 10.1021/jm1013488
156011119 176548 0 None -3 2 Human 5.7 pKi = 5.7 Binding
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 841 18 4 6 8.7 Cc1cc(OCCCNC(=O)CCCCCNC(=O)COc2ccc(/C=C/C3=[N+]4C(=Cc5ccc(-c6ccc[nH]6)n5[B-]4(F)F)C=C3)cc2)ccc1-c1nc2c(C)c(F)ccc2[nH]1 10.1021/acs.jmedchem.0c00160
CHEMBL4633688 176548 0 None -3 2 Human 5.7 pKi = 5.7 Binding
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 841 18 4 6 8.7 Cc1cc(OCCCNC(=O)CCCCCNC(=O)COc2ccc(/C=C/C3=[N+]4C(=Cc5ccc(-c6ccc[nH]6)n5[B-]4(F)F)C=C3)cc2)ccc1-c1nc2c(C)c(F)ccc2[nH]1 10.1021/acs.jmedchem.0c00160
51354296 58577 0 None -4 2 Human 5.7 pKi = 5.7 Binding
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 274 6 1 5 1.6 c1nc(CCCn2cc(CN3CCCCC3)nn2)c[nH]1 10.1021/jm1013488
CHEMBL1688942 58577 0 None -4 2 Human 5.7 pKi = 5.7 Binding
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 274 6 1 5 1.6 c1nc(CCCn2cc(CN3CCCCC3)nn2)c[nH]1 10.1021/jm1013488
1236 2036 23 None -204 7 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in SK-NM-C cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in SK-NM-C cells
ChEMBL 125 2 2 2 0.3 C[C@H](Cc1cnc[nH]1)N 10.1021/jm7014777
1237 2036 23 None -204 7 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in SK-NM-C cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in SK-NM-C cells
ChEMBL 125 2 2 2 0.3 C[C@H](Cc1cnc[nH]1)N 10.1021/jm7014777
156615 2036 23 None -204 7 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in SK-NM-C cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in SK-NM-C cells
ChEMBL 125 2 2 2 0.3 C[C@H](Cc1cnc[nH]1)N 10.1021/jm7014777
CHEMBL268229 2036 23 None -204 7 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in SK-NM-C cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in SK-NM-C cells
ChEMBL 125 2 2 2 0.3 C[C@H](Cc1cnc[nH]1)N 10.1021/jm7014777
756701 198135 29 None - 1 Human 4.7 pKi = 4.7 Binding
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 218 1 1 5 0.1 CN1CCN(c2ncnc3[nH]cnc23)CC1 10.1016/j.bmc.2009.08.059
CHEMBL594152 198135 29 None - 1 Human 4.7 pKi = 4.7 Binding
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 218 1 1 5 0.1 CN1CCN(c2ncnc3[nH]cnc23)CC1 10.1016/j.bmc.2009.08.059
63868328 173679 2 None - 1 Human 6.7 pKi = 6.7 Binding
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 236 3 1 6 0.2 CCCc1nc(N)nc(N2CCN(C)CC2)n1 10.1016/j.bmc.2019.02.020
CHEMBL4549015 173679 2 None - 1 Human 6.7 pKi = 6.7 Binding
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 236 3 1 6 0.2 CCCc1nc(N)nc(N2CCN(C)CC2)n1 10.1016/j.bmc.2019.02.020
58227381 176042 0 None - 1 Human 6.7 pKi = 6.7 Binding
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 249 3 2 5 1.3 CC(C)(C)CNc1nccc(N2CCNCC2)n1 10.1021/acs.jmedchem.9b01342
CHEMBL4513989 176042 0 None - 1 Human 6.7 pKi = 6.7 Binding
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 249 3 2 5 1.3 CC(C)(C)CNc1nccc(N2CCNCC2)n1 10.1021/acs.jmedchem.9b01342
CHEMBL4597817 176042 0 None - 1 Human 6.7 pKi = 6.7 Binding
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 249 3 2 5 1.3 CC(C)(C)CNc1nccc(N2CCNCC2)n1 10.1021/acs.jmedchem.9b01342
25128822 186898 0 None -10 5 Human 6.7 pKi = 6.7 Binding
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 295 1 1 5 1.6 CN1CCN(c2nc(N)nc3c2CCc2ccccc2-3)CC1 10.1016/j.bmcl.2015.12.035
CHEMBL494093 186898 0 None -10 5 Human 6.7 pKi = 6.7 Binding
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 295 1 1 5 1.6 CN1CCN(c2nc(N)nc3c2CCc2ccccc2-3)CC1 10.1016/j.bmcl.2015.12.035
25179124 173661 0 None - 1 Human 6.7 pKi = 6.7 Binding
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 371 4 1 6 3.5 Cc1cc(Cl)cc2c(NCc3ccco3)nc(N3CCN(C)CC3)nc12 10.1021/jm800876b
CHEMBL454883 173661 0 None - 1 Human 6.7 pKi = 6.7 Binding
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 371 4 1 6 3.5 Cc1cc(Cl)cc2c(NCc3ccco3)nc(N3CCN(C)CC3)nc12 10.1021/jm800876b
25179122 192670 0 None - 1 Human 6.7 pKi = 6.7 Binding
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 403 4 1 5 3.9 CN1CCN(c2nc(NCc3ccc(F)c(F)c3)c3cc(Cl)ccc3n2)CC1 10.1021/jm800876b
CHEMBL523941 192670 0 None - 1 Human 6.7 pKi = 6.7 Binding
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 403 4 1 5 3.9 CN1CCN(c2nc(NCc3ccc(F)c(F)c3)c3cc(Cl)ccc3n2)CC1 10.1021/jm800876b
25179124 173661 0 None - 1 Human 6.7 pKi = 6.7 Binding
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 371 4 1 6 3.5 Cc1cc(Cl)cc2c(NCc3ccco3)nc(N3CCN(C)CC3)nc12 10.1021/jm901379s
CHEMBL454883 173661 0 None - 1 Human 6.7 pKi = 6.7 Binding
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 371 4 1 6 3.5 Cc1cc(Cl)cc2c(NCc3ccco3)nc(N3CCN(C)CC3)nc12 10.1021/jm901379s
25179122 192670 0 None - 1 Human 6.7 pKi = 6.7 Binding
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 403 4 1 5 3.9 CN1CCN(c2nc(NCc3ccc(F)c(F)c3)c3cc(Cl)ccc3n2)CC1 10.1021/jm901379s
CHEMBL523941 192670 0 None - 1 Human 6.7 pKi = 6.7 Binding
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 403 4 1 5 3.9 CN1CCN(c2nc(NCc3ccc(F)c(F)c3)c3cc(Cl)ccc3n2)CC1 10.1021/jm901379s
1265 929 54 None -2290 8 Human 5.7 pKi = 5.7 Binding
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 270 7 1 3 3.0 O=C(c1ccc(cc1)OCCCc1[nH]cnc1)C1CC1 10.1021/jm8003625
6422124 929 54 None -2290 8 Human 5.7 pKi = 5.7 Binding
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 270 7 1 3 3.0 O=C(c1ccc(cc1)OCCCc1[nH]cnc1)C1CC1 10.1021/jm8003625
CHEMBL14638 929 54 None -2290 8 Human 5.7 pKi = 5.7 Binding
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 270 7 1 3 3.0 O=C(c1ccc(cc1)OCCCc1[nH]cnc1)C1CC1 10.1021/jm8003625
24994634 2111 26 None -21 7 Rat 6.7 pKi = 6.7 Binding
Displacement of [3H]histamine from rat histamine H4 receptor expressed in SK-N-MC cells after 45 mins by competition binding analysisDisplacement of [3H]histamine from rat 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 2111 26 None -21 7 Rat 6.7 pKi = 6.7 Binding
Displacement of [3H]histamine from rat histamine H4 receptor expressed in SK-N-MC cells after 45 mins by competition binding analysisDisplacement of [3H]histamine from rat 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 2111 26 None -21 7 Rat 6.7 pKi = 6.7 Binding
Displacement of [3H]histamine from rat histamine H4 receptor expressed in SK-N-MC cells after 45 mins by competition binding analysisDisplacement of [3H]histamine from rat 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
24994634 2111 26 None -21 7 Rat 6.7 pKi = 6.7 Binding
Displacement of [3H]histamine from rat recombinant histamine H4 receptorDisplacement of [3H]histamine from rat 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 2111 26 None -21 7 Rat 6.7 pKi = 6.7 Binding
Displacement of [3H]histamine from rat recombinant histamine H4 receptorDisplacement of [3H]histamine from rat 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 2111 26 None -21 7 Rat 6.7 pKi = 6.7 Binding
Displacement of [3H]histamine from rat recombinant histamine H4 receptorDisplacement of [3H]histamine from rat 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
CHEMBL4520788 212225 6 None -89 25 Human 5.7 pKi = 5.7 Binding
Selectivity interaction (GPCR panel (PDSP screen)) EUB0000743a HRH4Selectivity interaction (GPCR panel (PDSP screen)) EUB0000743a HRH4
ChEMBL None None None CNCc1ccccc1-c1csc([C@H](C)Nc2nc(C)nc3cc(OC)c(OC)cc23)c1 nan
54581937 61194 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]histamine from human histamine H4 receptorDisplacement of [3H]histamine from human histamine H4 receptor
ChEMBL 263 3 1 5 1.3 CC(C)N(C)c1cc(N2CCN(C)CC2)cc(N)n1 10.1016/j.bmcl.2011.03.017
CHEMBL1770963 61194 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]histamine from human histamine H4 receptorDisplacement of [3H]histamine from human histamine H4 receptor
ChEMBL 263 3 1 5 1.3 CC(C)N(C)c1cc(N2CCN(C)CC2)cc(N)n1 10.1016/j.bmcl.2011.03.017
137646939 157196 0 None - 1 Human 7.7 pKi = 7.7 Binding
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 335 5 3 4 3.6 CC(C)(CN=C(c1ccccc1O)c1ccccc1O)c1c[nH]cn1 10.1016/j.ejmech.2016.09.074
CHEMBL4082297 157196 0 None - 1 Human 7.7 pKi = 7.7 Binding
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 335 5 3 4 3.6 CC(C)(CN=C(c1ccccc1O)c1ccccc1O)c1c[nH]cn1 10.1016/j.ejmech.2016.09.074
9878733 116344 1 None - 1 Human 7.7 pKi = 7.7 Binding
Antagonist activity at Homo sapiens (human) histamine H4 receptorAntagonist activity at Homo sapiens (human) histamine H4 receptor
ChEMBL 277 1 1 2 2.2 CN1CCN(C(=O)c2cc3cccc(Cl)c3[nH]2)CC1 10.1007/s00044-004-0106-7
CHEMBL338051 116344 1 None - 1 Human 7.7 pKi = 7.7 Binding
Antagonist activity at Homo sapiens (human) histamine H4 receptorAntagonist activity at Homo sapiens (human) histamine H4 receptor
ChEMBL 277 1 1 2 2.2 CN1CCN(C(=O)c2cc3cccc(Cl)c3[nH]2)CC1 10.1007/s00044-004-0106-7
9878733 116344 1 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]- histamine from the recombinant human histamine H4 receptorDisplacement of [3H]- histamine from the recombinant human histamine H4 receptor
ChEMBL 277 1 1 2 2.2 CN1CCN(C(=O)c2cc3cccc(Cl)c3[nH]2)CC1 10.1021/jm0341047
CHEMBL338051 116344 1 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]- histamine from the recombinant human histamine H4 receptorDisplacement of [3H]- histamine from the recombinant human histamine H4 receptor
ChEMBL 277 1 1 2 2.2 CN1CCN(C(=O)c2cc3cccc(Cl)c3[nH]2)CC1 10.1021/jm0341047
49841610 69389 0 None - 1 Human 7.7 pKi = 7.7 Binding
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 319 2 1 5 2.6 CN1CCN(c2nc(N)nc3cc(-c4ccccc4)ccc23)CC1 10.1016/j.bmcl.2011.10.104
CHEMBL1935566 69389 0 None - 1 Human 7.7 pKi = 7.7 Binding
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 319 2 1 5 2.6 CN1CCN(c2nc(N)nc3cc(-c4ccccc4)ccc23)CC1 10.1016/j.bmcl.2011.10.104
44547127 115418 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 234 4 2 4 1.7 CN[C@@H]1CCN(c2ccnc(NC(C)C)c2)C1 10.1016/j.bmcl.2014.10.013
44547127 115418 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
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 115418 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 234 4 2 4 1.7 CN[C@@H]1CCN(c2ccnc(NC(C)C)c2)C1 10.1016/j.bmcl.2014.10.013
CHEMBL3354816 115418 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 234 4 2 4 1.7 CN[C@@H]1CCN(c2ccnc(NC(C)C)c2)C1 10.1016/j.bmcl.2014.12.027
24739219 67711 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 289 1 2 6 1.8 Nc1nc(N2CC(N)C2)c2oc3ccc(Cl)cc3c2n1 10.1016/j.bmcl.2011.08.014
CHEMBL1914546 67711 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 289 1 2 6 1.8 Nc1nc(N2CC(N)C2)c2oc3ccc(Cl)cc3c2n1 10.1016/j.bmcl.2011.08.014
24826265 67770 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 317 1 1 6 2.3 CN1CCN(c2nc(N)nc3c2sc2ccc(F)cc23)CC1 10.1016/j.bmcl.2011.08.014
CHEMBL1914761 67770 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 317 1 1 6 2.3 CN1CCN(c2nc(N)nc3c2sc2ccc(F)cc23)CC1 10.1016/j.bmcl.2011.08.014
9992865 113928 0 None - 1 Human 7.7 pKi = 7.7 Binding
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 262 1 1 3 1.1 CN1CCN(C(=O)c2nc3cc(F)ccc3[nH]2)CC1 10.1021/jm0502081
CHEMBL333220 113928 0 None - 1 Human 7.7 pKi = 7.7 Binding
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 262 1 1 3 1.1 CN1CCN(C(=O)c2nc3cc(F)ccc3[nH]2)CC1 10.1021/jm0502081
9878733 116344 1 None - 1 Human 7.7 pKi = 7.7 Binding
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 277 1 1 2 2.2 CN1CCN(C(=O)c2cc3cccc(Cl)c3[nH]2)CC1 10.1021/jm0502081
CHEMBL338051 116344 1 None - 1 Human 7.7 pKi = 7.7 Binding
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 277 1 1 2 2.2 CN1CCN(C(=O)c2cc3cccc(Cl)c3[nH]2)CC1 10.1021/jm0502081
2063135 8293 9 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]histamine human recombinant histamine H4 receptorDisplacement of [3H]histamine human recombinant histamine H4 receptor
ChEMBL 302 1 0 5 2.8 CN1CCN(c2ncnc3c2oc2ccc(Cl)cc23)CC1 10.1016/j.bmcl.2010.02.097
CHEMBL1093180 8293 9 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]histamine human recombinant histamine H4 receptorDisplacement of [3H]histamine human recombinant histamine H4 receptor
ChEMBL 302 1 0 5 2.8 CN1CCN(c2ncnc3c2oc2ccc(Cl)cc23)CC1 10.1016/j.bmcl.2010.02.097
44129213 197702 0 None - 1 Human 7.7 pKi = 7.7 Binding
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)c(Cl)cc3n2)CC1 10.1021/jm901379s
CHEMBL590995 197702 0 None - 1 Human 7.7 pKi = 7.7 Binding
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)c(Cl)cc3n2)CC1 10.1021/jm901379s
71525681 89298 0 None -2 6 Mouse 7.7 pKi = 7.7 Binding
Binding affinity to mouse histamine H4 receptorBinding affinity to mouse histamine H4 receptor
ChEMBL 298 3 2 6 1.7 CNC1CN(c2nc(N)nc3cc(C4CCCC4)cnc23)C1 10.1016/j.bmcl.2013.02.091
CHEMBL2376803 89298 0 None -2 6 Mouse 7.7 pKi = 7.7 Binding
Binding affinity to mouse histamine H4 receptorBinding affinity to mouse histamine H4 receptor
ChEMBL 298 3 2 6 1.7 CNC1CN(c2nc(N)nc3cc(C4CCCC4)cnc23)C1 10.1016/j.bmcl.2013.02.091
136141537 56187 1 None 2 3 Mouse 7.7 pKi = 7.7 Binding
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 271 2 2 3 3.0 Cc1ccc2[nH]c(/C(=N\O)C3CCN(C)CC3)cc2c1 10.1016/j.bmcl.2010.10.041
CHEMBL1632412 56187 1 None 2 3 Mouse 7.7 pKi = 7.7 Binding
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 271 2 2 3 3.0 Cc1ccc2[nH]c(/C(=N\O)C3CCN(C)CC3)cc2c1 10.1016/j.bmcl.2010.10.041
136030655 56188 0 None -2 3 Rat 7.7 pKi = 7.7 Binding
Binding affinity to rat histamine H4 receptor expressed in human SK-N-MC cells by radioligand displacement assayBinding affinity to rat histamine H4 receptor expressed in human SK-N-MC cells by radioligand displacement 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 56188 0 None -2 3 Rat 7.7 pKi = 7.7 Binding
Binding affinity to rat histamine H4 receptor expressed in human SK-N-MC cells by radioligand displacement assayBinding affinity to rat histamine H4 receptor expressed in human SK-N-MC cells by radioligand displacement 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
1278 2119 79 None -3 8 Human 7.7 pKi = 7.7 Binding
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 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1016/j.bmcl.2004.08.035
1279 2119 79 None -3 8 Human 7.7 pKi = 7.7 Binding
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 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1016/j.bmcl.2004.08.035
4908365 2119 79 None -3 8 Human 7.7 pKi = 7.7 Binding
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 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1016/j.bmcl.2004.08.035
CHEMBL129198 2119 79 None -3 8 Human 7.7 pKi = 7.7 Binding
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 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1016/j.bmcl.2004.08.035
1251 1983 34 None -100 5 Human 7.7 pKi = 7.7 Binding
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 165 2 2 2 1.0 N1CCC(CC1)Cc1[nH]cnc1 10.1016/j.bmcl.2010.10.041
3035842 1983 34 None -100 5 Human 7.7 pKi = 7.7 Binding
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 165 2 2 2 1.0 N1CCC(CC1)Cc1[nH]cnc1 10.1016/j.bmcl.2010.10.041
CHEMBL18661 1983 34 None -100 5 Human 7.7 pKi = 7.7 Binding
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 165 2 2 2 1.0 N1CCC(CC1)Cc1[nH]cnc1 10.1016/j.bmcl.2010.10.041
1251 1983 34 None -100 5 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]histamine binding to SK-N-MC cell membranes expressing human histamine H4 receptorDisplacement of [3H]histamine binding to SK-N-MC cell membranes expressing human histamine H4 receptor
ChEMBL 165 2 2 2 1.0 N1CCC(CC1)Cc1[nH]cnc1 10.1021/jm049475h
3035842 1983 34 None -100 5 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]histamine binding to SK-N-MC cell membranes expressing human histamine H4 receptorDisplacement of [3H]histamine binding to SK-N-MC cell membranes expressing human histamine H4 receptor
ChEMBL 165 2 2 2 1.0 N1CCC(CC1)Cc1[nH]cnc1 10.1021/jm049475h
CHEMBL18661 1983 34 None -100 5 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]histamine binding to SK-N-MC cell membranes expressing human histamine H4 receptorDisplacement of [3H]histamine binding to SK-N-MC cell membranes expressing human histamine H4 receptor
ChEMBL 165 2 2 2 1.0 N1CCC(CC1)Cc1[nH]cnc1 10.1021/jm049475h
1251 1983 34 None -100 5 Human 7.7 pKi = 7.7 Binding
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 165 2 2 2 1.0 N1CCC(CC1)Cc1[nH]cnc1 10.1021/jm201042n
3035842 1983 34 None -100 5 Human 7.7 pKi = 7.7 Binding
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 165 2 2 2 1.0 N1CCC(CC1)Cc1[nH]cnc1 10.1021/jm201042n
CHEMBL18661 1983 34 None -100 5 Human 7.7 pKi = 7.7 Binding
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 165 2 2 2 1.0 N1CCC(CC1)Cc1[nH]cnc1 10.1021/jm201042n
11673377 138732 0 None -1 2 Human 7.7 pKi = 7.7 Binding
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 263 7 2 2 3.2 Clc1ccc(CNCCCCc2c[nH]cn2)cc1 10.1021/jm0504353
CHEMBL379027 138732 0 None -1 2 Human 7.7 pKi = 7.7 Binding
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 263 7 2 2 3.2 Clc1ccc(CNCCCCc2c[nH]cn2)cc1 10.1021/jm0504353
25129523 186704 40 None 1 2 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]histamine from human histamine H4 receptor L175'5.39V mutant transfected in HEK293T cells after 1.5 hrs by liquid scintillation counting analysisDisplacement of [3H]histamine from human histamine H4 receptor L175'5.39V mutant transfected in HEK293T cells after 1.5 hrs by liquid scintillation counting analysis
ChEMBL 269 2 1 5 1.5 CN1CCN(c2cc(-c3ccccc3)nc(N)n2)CC1 10.1039/C2MD20212C
CHEMBL492884 186704 40 None 1 2 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]histamine from human histamine H4 receptor L175'5.39V mutant transfected in HEK293T cells after 1.5 hrs by liquid scintillation counting analysisDisplacement of [3H]histamine from human histamine H4 receptor L175'5.39V mutant transfected in HEK293T cells after 1.5 hrs by liquid scintillation counting analysis
ChEMBL 269 2 1 5 1.5 CN1CCN(c2cc(-c3ccccc3)nc(N)n2)CC1 10.1039/C2MD20212C
66572114 75298 0 None - 1 Human 7.7 pKi = 7.7 Binding
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 261 1 1 2 1.7 CN1CCN(C(=O)c2cc3cccc(F)c3[nH]2)CC1 10.1016/j.ejmech.2012.06.016
CHEMBL2047276 75298 0 None - 1 Human 7.7 pKi = 7.7 Binding
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 261 1 1 2 1.7 CN1CCN(C(=O)c2cc3cccc(F)c3[nH]2)CC1 10.1016/j.ejmech.2012.06.016
70690369 75338 0 None - 1 Human 7.7 pKi = 7.7 Binding
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 1 2 2 2.0 O=C(c1cc2cc(Cl)cc(F)c2[nH]1)N1CCNCC1 10.1016/j.ejmech.2012.06.016
CHEMBL2047473 75338 0 None - 1 Human 7.7 pKi = 7.7 Binding
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 1 2 2 2.0 O=C(c1cc2cc(Cl)cc(F)c2[nH]1)N1CCNCC1 10.1016/j.ejmech.2012.06.016
9878733 116344 1 None - 1 Human 7.7 pKi = 7.7 Binding
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 2 2.2 CN1CCN(C(=O)c2cc3cccc(Cl)c3[nH]2)CC1 10.1016/j.ejmech.2012.06.016
CHEMBL338051 116344 1 None - 1 Human 7.7 pKi = 7.7 Binding
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 2 2.2 CN1CCN(C(=O)c2cc3cccc(Cl)c3[nH]2)CC1 10.1016/j.ejmech.2012.06.016
1204 1901 114 None -3 23 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]histamine from wild type human histamine H4 receptor transfected in HEK293T cells after 1 hr by liquid scintillation counting analysisDisplacement of [3H]histamine from wild type human histamine H4 receptor transfected in HEK293T cells after 1 hr by liquid scintillation counting analysis
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1039/C2MD20212C
1247 1901 114 None -3 23 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]histamine from wild type human histamine H4 receptor transfected in HEK293T cells after 1 hr by liquid scintillation counting analysisDisplacement of [3H]histamine from wild type human histamine H4 receptor transfected in HEK293T cells after 1 hr by liquid scintillation counting analysis
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1039/C2MD20212C
1375 1901 114 None -3 23 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]histamine from wild type human histamine H4 receptor transfected in HEK293T cells after 1 hr by liquid scintillation counting analysisDisplacement of [3H]histamine from wild type human histamine H4 receptor transfected in HEK293T cells after 1 hr by liquid scintillation counting analysis
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1039/C2MD20212C
774 1901 114 None -3 23 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]histamine from wild type human histamine H4 receptor transfected in HEK293T cells after 1 hr by liquid scintillation counting analysisDisplacement of [3H]histamine from wild type human histamine H4 receptor transfected in HEK293T cells after 1 hr by liquid scintillation counting analysis
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1039/C2MD20212C
CHEMBL90 1901 114 None -3 23 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]histamine from wild type human histamine H4 receptor transfected in HEK293T cells after 1 hr by liquid scintillation counting analysisDisplacement of [3H]histamine from wild type human histamine H4 receptor transfected in HEK293T cells after 1 hr by liquid scintillation counting analysis
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1039/C2MD20212C
DB05381 1901 114 None -3 23 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]histamine from wild type human histamine H4 receptor transfected in HEK293T cells after 1 hr by liquid scintillation counting analysisDisplacement of [3H]histamine from wild type human histamine H4 receptor transfected in HEK293T cells after 1 hr by liquid scintillation counting analysis
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1039/C2MD20212C
1278 2119 79 None -3 8 Human 7.7 pKi = 7.7 Binding
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 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1039/C2MD20212C
1279 2119 79 None -3 8 Human 7.7 pKi = 7.7 Binding
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 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1039/C2MD20212C
4908365 2119 79 None -3 8 Human 7.7 pKi = 7.7 Binding
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 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1039/C2MD20212C
CHEMBL129198 2119 79 None -3 8 Human 7.7 pKi = 7.7 Binding
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 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1039/C2MD20212C
11846298 138751 0 None - 1 Human 6.7 pKi = 6.7 Binding
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 345 0 0 4 3.9 CN1CCN(C2=Nc3cc(Cl)ccc3Oc3ccc(F)cc32)CC1 10.1021/jm051008s
CHEMBL379102 138751 0 None - 1 Human 6.7 pKi = 6.7 Binding
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 345 0 0 4 3.9 CN1CCN(C2=Nc3cc(Cl)ccc3Oc3ccc(F)cc32)CC1 10.1021/jm051008s
155538989 175755 0 None 1 2 Human 5.7 pKi = 5.7 Binding
Displacement of 40 nM [3H]-histamine from human H4R expressed in Sf9 cell membranes co-expressing Gia2 and beta1gamma2 by competition binding assayDisplacement of 40 nM [3H]-histamine from human H4R expressed in Sf9 cell membranes co-expressing Gia2 and beta1gamma2 by competition binding assay
ChEMBL 263 4 3 5 2.1 CC(C)(C)CNc1nccc(NC2CCNCC2)n1 10.1021/acs.jmedchem.9b01342
CHEMBL4513421 175755 0 None 1 2 Human 5.7 pKi = 5.7 Binding
Displacement of 40 nM [3H]-histamine from human H4R expressed in Sf9 cell membranes co-expressing Gia2 and beta1gamma2 by competition binding assayDisplacement of 40 nM [3H]-histamine from human H4R expressed in Sf9 cell membranes co-expressing Gia2 and beta1gamma2 by competition binding assay
ChEMBL 263 4 3 5 2.1 CC(C)(C)CNc1nccc(NC2CCNCC2)n1 10.1021/acs.jmedchem.9b01342
CHEMBL4595438 175755 0 None 1 2 Human 5.7 pKi = 5.7 Binding
Displacement of 40 nM [3H]-histamine from human H4R expressed in Sf9 cell membranes co-expressing Gia2 and beta1gamma2 by competition binding assayDisplacement of 40 nM [3H]-histamine from human H4R expressed in Sf9 cell membranes co-expressing Gia2 and beta1gamma2 by competition binding assay
ChEMBL 263 4 3 5 2.1 CC(C)(C)CNc1nccc(NC2CCNCC2)n1 10.1021/acs.jmedchem.9b01342
164608815 183872 0 None -47 6 Human 5.7 pKi = 5.7 Binding
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 380 7 4 4 2.8 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCC(C)C1CCCCC1 10.1016/j.ejmech.2021.113190
CHEMBL4846638 183872 0 None -47 6 Human 5.7 pKi = 5.7 Binding
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 380 7 4 4 2.8 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCC(C)C1CCCCC1 10.1016/j.ejmech.2021.113190
164611342 184505 0 None -416 6 Human 4.7 pKi = 4.7 Binding
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 346 6 4 4 1.8 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCc1ccccc1 10.1016/j.ejmech.2021.113190
CHEMBL4856005 184505 0 None -416 6 Human 4.7 pKi = 4.7 Binding
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 346 6 4 4 1.8 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCc1ccccc1 10.1016/j.ejmech.2021.113190
155513612 175746 0 None -2 4 Rat 5.7 pKi = 5.7 Binding
Displacement of [3H]-UR-DEBa176 from rat H4R expressed in HEK293T-SF-His6-CRE-Luc cellsDisplacement of [3H]-UR-DEBa176 from rat H4R expressed in HEK293T-SF-His6-CRE-Luc cells
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 175746 0 None -2 4 Rat 5.7 pKi = 5.7 Binding
Displacement of [3H]-UR-DEBa176 from rat H4R expressed in HEK293T-SF-His6-CRE-Luc cellsDisplacement of [3H]-UR-DEBa176 from rat H4R expressed in HEK293T-SF-His6-CRE-Luc cells
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 175746 0 None -2 4 Rat 5.7 pKi = 5.7 Binding
Displacement of [3H]-UR-DEBa176 from rat H4R expressed in HEK293T-SF-His6-CRE-Luc cellsDisplacement of [3H]-UR-DEBa176 from rat H4R expressed in HEK293T-SF-His6-CRE-Luc cells
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 175746 0 None -2 4 Rat 5.7 pKi = 5.7 Binding
Displacement of [3H]-UR-DEBa176 from rat H4R expressed in HEK293T-SF-His6-CRE-Luc cellsDisplacement of [3H]-UR-DEBa176 from rat H4R expressed in HEK293T-SF-His6-CRE-Luc cells
ChEMBL 277 4 1 5 2.1 CN(C)[C@@H]1CCN(c2ccnc(NCC(C)(C)C)n2)C1 10.1021/acs.jmedchem.9b01342
156015838 177671 0 None -2 2 Human 5.7 pKi = 5.7 Binding
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 373 7 1 2 4.3 Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCc1c[nH]cn1 10.1021/acs.jmedchem.0c00160
CHEMBL4640263 177671 0 None -2 2 Human 5.7 pKi = 5.7 Binding
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 373 7 1 2 4.3 Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCc1c[nH]cn1 10.1021/acs.jmedchem.0c00160
CHEMBL4650622 177671 0 None -2 2 Human 5.7 pKi = 5.7 Binding
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 373 7 1 2 4.3 Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCc1c[nH]cn1 10.1021/acs.jmedchem.0c00160
127036982 136942 0 None -3 2 Human 4.7 pKi = 4.7 Binding
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 525 6 1 6 5.9 COc1ccc(CNc2nc(N3CCN(C)CC3)nc3c2CCc2ccccc2-3)cc1-c1ccc(Cl)cc1 10.1016/j.bmcl.2015.12.035
CHEMBL3753784 136942 0 None -3 2 Human 4.7 pKi = 4.7 Binding
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 525 6 1 6 5.9 COc1ccc(CNc2nc(N3CCN(C)CC3)nc3c2CCc2ccccc2-3)cc1-c1ccc(Cl)cc1 10.1016/j.bmcl.2015.12.035
57393769 67828 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 281 1 2 6 1.5 Nc1nc(N2C[C@@H]3C[C@H]2CN3)c2oc3ccccc3c2n1 10.1016/j.bmcl.2011.08.014
CHEMBL1915030 67828 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 281 1 2 6 1.5 Nc1nc(N2C[C@@H]3C[C@H]2CN3)c2oc3ccccc3c2n1 10.1016/j.bmcl.2011.08.014
11688307 69560 0 None - 1 Human 5.7 pKi = 5.7 Binding
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 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 69560 0 None - 1 Human 5.7 pKi = 5.7 Binding
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 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
136141537 56187 1 None -10 3 Rat 6.7 pKi = 6.7 Binding
Binding affinity to rat histamine H4 receptor expressed in human SK-N-MC cells by radioligand displacement assayBinding affinity to rat histamine H4 receptor expressed in human SK-N-MC cells by radioligand displacement 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 56187 1 None -10 3 Rat 6.7 pKi = 6.7 Binding
Binding affinity to rat histamine H4 receptor expressed in human SK-N-MC cells by radioligand displacement assayBinding affinity to rat histamine H4 receptor expressed in human SK-N-MC cells by radioligand displacement 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
44395364 66565 0 None 15 2 Human 6.7 pKi = 6.7 Binding
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 276 2 1 2 3.3 CN1CCC(C(=O)c2cc3cc(Cl)ccc3[nH]2)CC1 10.1016/j.bmcl.2004.08.035
CHEMBL186456 66565 0 None 15 2 Human 6.7 pKi = 6.7 Binding
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 276 2 1 2 3.3 CN1CCC(C(=O)c2cc3cc(Cl)ccc3[nH]2)CC1 10.1016/j.bmcl.2004.08.035
10037650 5138 0 None 31 2 Human 6.7 pKi = 6.7 Binding
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 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 5138 0 None 31 2 Human 6.7 pKi = 6.7 Binding
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 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
135398737 944 89 None -57 91 Human 6.7 pKi = 6.7 Binding
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 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm201042n
38 944 89 None -57 91 Human 6.7 pKi = 6.7 Binding
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 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm201042n
722 944 89 None -57 91 Human 6.7 pKi = 6.7 Binding
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 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm201042n
CHEMBL42 944 89 None -57 91 Human 6.7 pKi = 6.7 Binding
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 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm201042n
DB00363 944 89 None -57 91 Human 6.7 pKi = 6.7 Binding
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 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm201042n
11572015 74680 0 None -50 2 Human 6.7 pKi = 6.7 Binding
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 209 9 2 2 2.5 CCCCNCCCCCc1c[nH]cn1 10.1021/jm0504353
CHEMBL203441 74680 0 None -50 2 Human 6.7 pKi = 6.7 Binding
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 209 9 2 2 2.5 CCCCNCCCCCc1c[nH]cn1 10.1021/jm0504353
11600780 75696 0 None -2 2 Human 6.7 pKi = 6.7 Binding
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 181 6 2 2 1.7 CC(C)NCCCCc1c[nH]cn1 10.1021/jm0504353
CHEMBL205732 75696 0 None -2 2 Human 6.7 pKi = 6.7 Binding
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 181 6 2 2 1.7 CC(C)NCCCCc1c[nH]cn1 10.1021/jm0504353
1408942 64792 4 None - 1 Human 6.7 pKi = 6.7 Binding
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 254 2 0 4 1.9 CN1CCN(c2cc(-c3ccccc3)ncn2)CC1 10.1016/j.bmcl.2011.06.123
CHEMBL1824046 64792 4 None - 1 Human 6.7 pKi = 6.7 Binding
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 254 2 0 4 1.9 CN1CCN(c2cc(-c3ccccc3)ncn2)CC1 10.1016/j.bmcl.2011.06.123
4060730 19183 51 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]histamine from human histamine H4 receptor E182'5.46Q mutant transfected in HEK293T cells after 1.5 hrs by liquid scintillation counting analysisDisplacement of [3H]histamine from human histamine H4 receptor E182'5.46Q mutant transfected in HEK293T cells after 1.5 hrs by liquid scintillation counting analysis
ChEMBL 243 1 1 2 1.6 CN1CCN(C(=O)c2cc3ccccc3[nH]2)CC1 10.1039/C2MD20212C
CHEMBL129199 19183 51 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]histamine from human histamine H4 receptor E182'5.46Q mutant transfected in HEK293T cells after 1.5 hrs by liquid scintillation counting analysisDisplacement of [3H]histamine from human histamine H4 receptor E182'5.46Q mutant transfected in HEK293T cells after 1.5 hrs by liquid scintillation counting analysis
ChEMBL 243 1 1 2 1.6 CN1CCN(C(=O)c2cc3ccccc3[nH]2)CC1 10.1039/C2MD20212C
25129527 186831 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]histamine from human histamine H4 receptor E182'5.46Q mutant transfected in HEK293T cells after 1.5 hrs by liquid scintillation counting analysisDisplacement of [3H]histamine from human histamine H4 receptor E182'5.46Q mutant 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 186831 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]histamine from human histamine H4 receptor E182'5.46Q mutant transfected in HEK293T cells after 1.5 hrs by liquid scintillation counting analysisDisplacement of [3H]histamine from human histamine H4 receptor E182'5.46Q mutant 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
66573462 75318 0 None - 1 Human 6.7 pKi = 6.7 Binding
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 2 2 2 2.2 CNC1CN(C(=O)c2cc3cc(Cl)cc(C)c3[nH]2)C1 10.1016/j.ejmech.2012.06.016
CHEMBL2047453 75318 0 None - 1 Human 6.7 pKi = 6.7 Binding
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 2 2 2 2.2 CNC1CN(C(=O)c2cc3cc(Cl)cc(C)c3[nH]2)C1 10.1016/j.ejmech.2012.06.016
767246 95571 4 None - 1 Human 6.7 pKi = 6.7 Binding
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 242 1 0 4 1.7 Cc1nc2ccccc2nc1N1CCN(C)CC1 10.1021/jm7014217
CHEMBL259745 95571 4 None - 1 Human 6.7 pKi = 6.7 Binding
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 242 1 0 4 1.7 Cc1nc2ccccc2nc1N1CCN(C)CC1 10.1021/jm7014217
155550732 176055 0 None -794 3 Human 4.7 pKi = 4.7 Binding
Displacement of [3H]histamine from human recombinant H4R expressed in CHO cells incubated for 60 mins by microbeta scintillation counter methodDisplacement of [3H]histamine from human recombinant H4R expressed in CHO cells incubated for 60 mins by microbeta scintillation counter method
ChEMBL 323 8 0 2 5.4 c1ccc(-c2ccc(OCCCCCN3CCCCC3)cc2)cc1 10.1016/j.bmc.2017.07.058
CHEMBL4540849 176055 0 None -794 3 Human 4.7 pKi = 4.7 Binding
Displacement of [3H]histamine from human recombinant H4R expressed in CHO cells incubated for 60 mins by microbeta scintillation counter methodDisplacement of [3H]histamine from human recombinant H4R expressed in CHO cells incubated for 60 mins by microbeta scintillation counter method
ChEMBL 323 8 0 2 5.4 c1ccc(-c2ccc(OCCCCCN3CCCCC3)cc2)cc1 10.1016/j.bmc.2017.07.058
CHEMBL4597895 176055 0 None -794 3 Human 4.7 pKi = 4.7 Binding
Displacement of [3H]histamine from human recombinant H4R expressed in CHO cells incubated for 60 mins by microbeta scintillation counter methodDisplacement of [3H]histamine from human recombinant H4R expressed in CHO cells incubated for 60 mins by microbeta scintillation counter method
ChEMBL 323 8 0 2 5.4 c1ccc(-c2ccc(OCCCCCN3CCCCC3)cc2)cc1 10.1016/j.bmc.2017.07.058
11313837 2464 7 None -1995 2 Human 5.7 pKi = 5.7 Binding
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 179 2 1 2 1.3 CN1CCC(CC1)Cc1[nH]cnc1 10.1016/j.bmcl.2010.10.041
1254 2464 7 None -1995 2 Human 5.7 pKi = 5.7 Binding
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 179 2 1 2 1.3 CN1CCC(CC1)Cc1[nH]cnc1 10.1016/j.bmcl.2010.10.041
CHEMBL175782 2464 7 None -1995 2 Human 5.7 pKi = 5.7 Binding
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 179 2 1 2 1.3 CN1CCC(CC1)Cc1[nH]cnc1 10.1016/j.bmcl.2010.10.041
11313837 2464 7 None -1995 2 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]histamine binding to SK-N-MC cell membranes expressing human histamine H4 receptorDisplacement of [3H]histamine binding to SK-N-MC cell membranes expressing human histamine H4 receptor
ChEMBL 179 2 1 2 1.3 CN1CCC(CC1)Cc1[nH]cnc1 10.1021/jm049475h
1254 2464 7 None -1995 2 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]histamine binding to SK-N-MC cell membranes expressing human histamine H4 receptorDisplacement of [3H]histamine binding to SK-N-MC cell membranes expressing human histamine H4 receptor
ChEMBL 179 2 1 2 1.3 CN1CCC(CC1)Cc1[nH]cnc1 10.1021/jm049475h
CHEMBL175782 2464 7 None -1995 2 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]histamine binding to SK-N-MC cell membranes expressing human histamine H4 receptorDisplacement of [3H]histamine binding to SK-N-MC cell membranes expressing human histamine H4 receptor
ChEMBL 179 2 1 2 1.3 CN1CCC(CC1)Cc1[nH]cnc1 10.1021/jm049475h
71681480 89231 0 None - 1 Human 5.7 pKi = 5.7 Binding
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 307 6 3 7 2.0 Nc1nc(NCCNc2ccncn2)cc(-c2ccccc2)n1 10.1021/jm301886t
CHEMBL2375761 89231 0 None - 1 Human 5.7 pKi = 5.7 Binding
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 307 6 3 7 2.0 Nc1nc(NCCNc2ccncn2)cc(-c2ccccc2)n1 10.1021/jm301886t
57392460 69523 0 None 14 2 Human 5.7 pKi = 5.7 Binding
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 244 1 1 3 1.0 CN1CCN(C(=O)c2cc3cccnc3[nH]2)CC1 10.1016/j.ejmech.2012.06.016
CHEMBL1938843 69523 0 None 14 2 Human 5.7 pKi = 5.7 Binding
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 244 1 1 3 1.0 CN1CCN(C(=O)c2cc3cccnc3[nH]2)CC1 10.1016/j.ejmech.2012.06.016
66572104 75284 0 None - 1 Human 5.7 pKi = 5.7 Binding
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 244 1 1 3 1.0 CN1CCN(C(=O)c2cc3ccncc3[nH]2)CC1 10.1016/j.ejmech.2012.06.016
CHEMBL2047262 75284 0 None - 1 Human 5.7 pKi = 5.7 Binding
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 244 1 1 3 1.0 CN1CCN(C(=O)c2cc3ccncc3[nH]2)CC1 10.1016/j.ejmech.2012.06.016
66572112 75296 0 None - 1 Human 5.7 pKi = 5.7 Binding
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 288 2 1 4 1.5 CN1CCN(C(=O)c2cc3ccc([N+](=O)[O-])cc3[nH]2)CC1 10.1016/j.ejmech.2012.06.016
CHEMBL2047274 75296 0 None - 1 Human 5.7 pKi = 5.7 Binding
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 288 2 1 4 1.5 CN1CCN(C(=O)c2cc3ccc([N+](=O)[O-])cc3[nH]2)CC1 10.1016/j.ejmech.2012.06.016
44395361 66606 0 None - 1 Human 4.7 pKi = 4.7 Binding
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 293 1 2 3 2.0 CN1CCN(C(=O)Nc2nc3cc(Cl)ccc3[nH]2)CC1 10.1016/j.bmcl.2004.08.035
CHEMBL186640 66606 0 None - 1 Human 4.7 pKi = 4.7 Binding
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 293 1 2 3 2.0 CN1CCN(C(=O)Nc2nc3cc(Cl)ccc3[nH]2)CC1 10.1016/j.bmcl.2004.08.035
10879463 5218 0 None -1 2 Human 4.7 pKi = 4.7 Binding
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 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 5218 0 None -1 2 Human 4.7 pKi = 4.7 Binding
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 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
10945113 109141 1 None -1 2 Human 4.7 pKi = 4.7 Binding
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
CHEMBL322256 109141 1 None -1 2 Human 4.7 pKi = 4.7 Binding
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
127035836 136993 0 None -5 2 Human 4.7 pKi = 4.7 Binding
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 399 4 1 5 3.9 Cc1ccc(CNc2nc3c(c(N4CCN(C)CC4)n2)CCc2ccccc2-3)cc1 10.1016/j.bmcl.2015.12.035
CHEMBL3754176 136993 0 None -5 2 Human 4.7 pKi = 4.7 Binding
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 399 4 1 5 3.9 Cc1ccc(CNc2nc3c(c(N4CCN(C)CC4)n2)CCc2ccccc2-3)cc1 10.1016/j.bmcl.2015.12.035
164618283 183961 0 None -537 4 Human 4.7 pKi = 4.7 Binding
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 390 7 4 5 2.4 COc1ccc(C(C)NC(=O)/N=C(\N)NCCCc2sc(N)nc2C)cc1 10.1016/j.ejmech.2021.113190
CHEMBL4848026 183961 0 None -537 4 Human 4.7 pKi = 4.7 Binding
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 390 7 4 5 2.4 COc1ccc(C(C)NC(=O)/N=C(\N)NCCCc2sc(N)nc2C)cc1 10.1016/j.ejmech.2021.113190
53233805 61195 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]histamine from human histamine H4 receptorDisplacement of [3H]histamine from human histamine H4 receptor
ChEMBL 263 4 2 5 1.5 CC(C)CNc1cc(N2CCN(C)CC2)cc(N)n1 10.1016/j.bmcl.2011.03.017
CHEMBL1770964 61195 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]histamine from human histamine H4 receptorDisplacement of [3H]histamine from human histamine H4 receptor
ChEMBL 263 4 2 5 1.5 CC(C)CNc1cc(N2CCN(C)CC2)cc(N)n1 10.1016/j.bmcl.2011.03.017
54585781 61232 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]histamine from human histamine H4 receptorDisplacement of [3H]histamine from human histamine H4 receptor
ChEMBL 264 4 2 6 0.9 CC(C)CNc1cc(N2CCN(C)CC2)nc(N)n1 10.1016/j.bmcl.2011.03.017
CHEMBL1771000 61232 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]histamine from human histamine H4 receptorDisplacement of [3H]histamine from human histamine H4 receptor
ChEMBL 264 4 2 6 0.9 CC(C)CNc1cc(N2CCN(C)CC2)nc(N)n1 10.1016/j.bmcl.2011.03.017
118720442 115421 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 261 3 3 5 1.4 Nc1cc(N2CCNCC2)cc(NC2CCCC2)n1 10.1016/j.bmcl.2014.10.013
CHEMBL3354820 115421 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 261 3 3 5 1.4 Nc1cc(N2CCNCC2)cc(NC2CCCC2)n1 10.1016/j.bmcl.2014.10.013
44547268 116610 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
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 116610 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 248 5 2 4 1.9 CN[C@@H]1CCN(c2ccnc(NCC(C)C)c2)C1 10.1016/j.bmcl.2014.12.027
58227255 116623 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
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 116623 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 249 5 2 5 1.3 CN[C@@H]1CCN(c2ccnc(NCC(C)C)n2)C1 10.1016/j.bmcl.2014.12.027
58227252 116628 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 261 4 2 5 1.6 CN[C@@H]1CCN(c2ccnc(NC3CCCC3)n2)C1 10.1016/j.bmcl.2014.12.027
CHEMBL3393544 116628 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 261 4 2 5 1.6 CN[C@@H]1CCN(c2ccnc(NC3CCCC3)n2)C1 10.1016/j.bmcl.2014.12.027
25112105 8079 0 None - 1 Human 8.7 pKi = 8.7 Binding
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
CHEMBL1091875 8079 0 None - 1 Human 8.7 pKi = 8.7 Binding
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
24737949 67790 0 None - 1 Human 8.7 pKi = 8.7 Binding
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)nc3c2oc2ccc(F)cc23)C1 10.1016/j.bmcl.2011.08.014
CHEMBL1914782 67790 0 None - 1 Human 8.7 pKi = 8.7 Binding
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)nc3c2oc2ccc(F)cc23)C1 10.1016/j.bmcl.2011.08.014
24825996 67796 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 377 2 2 6 3.0 CN[C@@H]1CCN(c2nc(N)nc3c2sc2ccc(Br)cc23)C1 10.1016/j.bmcl.2011.08.014
CHEMBL1914788 67796 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 377 2 2 6 3.0 CN[C@@H]1CCN(c2nc(N)nc3c2sc2ccc(Br)cc23)C1 10.1016/j.bmcl.2011.08.014
59777341 109659 0 None - 1 Human 8.6 pKi = 8.6 Binding
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 275 3 2 5 1.9 CN[C@@H]1CCN(c2cc(C3CCCCC3)nc(N)n2)C1 10.1021/jm401727m
CHEMBL3236576 109659 0 None - 1 Human 8.6 pKi = 8.6 Binding
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 275 3 2 5 1.9 CN[C@@H]1CCN(c2cc(C3CCCCC3)nc(N)n2)C1 10.1021/jm401727m
1278 2119 79 None 3 8 Rat 8.6 pKi = 8.6 Binding
Binding affinity of compound towards rat histamine H4 receptorBinding affinity of compound towards rat histamine H4 receptor
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/jm0341047
1279 2119 79 None 3 8 Rat 8.6 pKi = 8.6 Binding
Binding affinity of compound towards rat histamine H4 receptorBinding affinity of compound towards rat histamine H4 receptor
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/jm0341047
4908365 2119 79 None 3 8 Rat 8.6 pKi = 8.6 Binding
Binding affinity of compound towards rat histamine H4 receptorBinding affinity of compound towards rat histamine H4 receptor
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/jm0341047
CHEMBL129198 2119 79 None 3 8 Rat 8.6 pKi = 8.6 Binding
Binding affinity of compound towards rat histamine H4 receptorBinding affinity of compound towards rat histamine H4 receptor
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/jm0341047
24745335 292 7 None 4 5 Human 8.6 pKi = 8.6 Binding
Binding affinity to human histamine H4 receptorBinding affinity to human histamine H4 receptor
ChEMBL 262 5 3 6 0.7 CN[C@@H]1CCN(C1)c1cc(NCC2CC2)nc(n1)N 10.1021/acs.jmedchem.5b00516
8985 292 7 None 4 5 Human 8.6 pKi = 8.6 Binding
Binding affinity to human histamine H4 receptorBinding affinity to human histamine H4 receptor
ChEMBL 262 5 3 6 0.7 CN[C@@H]1CCN(C1)c1cc(NCC2CC2)nc(n1)N 10.1021/acs.jmedchem.5b00516
CHEMBL1915540 292 7 None 4 5 Human 8.6 pKi = 8.6 Binding
Binding affinity to human histamine H4 receptorBinding affinity to human histamine H4 receptor
ChEMBL 262 5 3 6 0.7 CN[C@@H]1CCN(C1)c1cc(NCC2CC2)nc(n1)N 10.1021/acs.jmedchem.5b00516
DB15027 292 7 None 4 5 Human 8.6 pKi = 8.6 Binding
Binding affinity to human histamine H4 receptorBinding affinity to human histamine H4 receptor
ChEMBL 262 5 3 6 0.7 CN[C@@H]1CCN(C1)c1cc(NCC2CC2)nc(n1)N 10.1021/acs.jmedchem.5b00516
24745335 292 7 None 4 5 Human 8.6 pKi = 8.6 Binding
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 262 5 3 6 0.7 CN[C@@H]1CCN(C1)c1cc(NCC2CC2)nc(n1)N 10.1016/j.bmcl.2011.07.125
8985 292 7 None 4 5 Human 8.6 pKi = 8.6 Binding
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 262 5 3 6 0.7 CN[C@@H]1CCN(C1)c1cc(NCC2CC2)nc(n1)N 10.1016/j.bmcl.2011.07.125
CHEMBL1915540 292 7 None 4 5 Human 8.6 pKi = 8.6 Binding
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 262 5 3 6 0.7 CN[C@@H]1CCN(C1)c1cc(NCC2CC2)nc(n1)N 10.1016/j.bmcl.2011.07.125
DB15027 292 7 None 4 5 Human 8.6 pKi = 8.6 Binding
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 262 5 3 6 0.7 CN[C@@H]1CCN(C1)c1cc(NCC2CC2)nc(n1)N 10.1016/j.bmcl.2011.07.125
53257796 109658 0 None - 1 Human 8.6 pKi = 8.6 Binding
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 3 2 5 1.1 CN[C@@H]1CCN(c2cc(C3CCC3)nc(N)n2)C1 10.1021/jm401727m
CHEMBL3236575 109658 0 None - 1 Human 8.6 pKi = 8.6 Binding
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 3 2 5 1.1 CN[C@@H]1CCN(c2cc(C3CCC3)nc(N)n2)C1 10.1021/jm401727m
24738269 67708 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 303 1 2 6 2.1 Nc1nc(N2CC[C@@H](N)C2)c2oc3ccc(Cl)cc3c2n1 10.1016/j.bmcl.2011.08.014
CHEMBL1914543 67708 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 303 1 2 6 2.1 Nc1nc(N2CC[C@@H](N)C2)c2oc3ccc(Cl)cc3c2n1 10.1016/j.bmcl.2011.08.014
1223 940 32 None -60 11 Human 8.6 pKi = 8.6 Binding
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 308 6 2 3 3.2 Clc1ccc(cc1)CN=C(SCCCc1cnc[nH]1)N 10.1021/jm201042n
2790 940 32 None -60 11 Human 8.6 pKi = 8.6 Binding
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 308 6 2 3 3.2 Clc1ccc(cc1)CN=C(SCCCc1cnc[nH]1)N 10.1021/jm201042n
CHEMBL14690 940 32 None -60 11 Human 8.6 pKi = 8.6 Binding
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 308 6 2 3 3.2 Clc1ccc(cc1)CN=C(SCCCc1cnc[nH]1)N 10.1021/jm201042n
44231735 7703 0 None -1 4 Rat 8.6 pKi = 8.6 Binding
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 301 2 2 5 2.0 CN[C@@H]1CCN(c2nc(N)nc3c2CCCC32CCCC2)C1 10.1016/j.bmcl.2010.01.131
CHEMBL1089390 7703 0 None -1 4 Rat 8.6 pKi = 8.6 Binding
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 301 2 2 5 2.0 CN[C@@H]1CCN(c2nc(N)nc3c2CCCC32CCCC2)C1 10.1016/j.bmcl.2010.01.131
44462956 5523 0 None 2 2 Rat 8.6 pKi = 8.6 Binding
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 363 2 2 5 3.1 Nc1nc2c(c(N3CC4CCCNC4C3)n1)CCCCC2c1ccccc1 10.1016/j.bmcl.2010.01.131
CHEMBL1077276 5523 0 None 2 2 Rat 8.6 pKi = 8.6 Binding
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 363 2 2 5 3.1 Nc1nc2c(c(N3CC4CCCNC4C3)n1)CCCCC2c1ccccc1 10.1016/j.bmcl.2010.01.131
1278 2119 79 None 3 8 Rat 8.6 pKi = 8.6 Binding
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 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/jm8005959
1278 2119 79 None 3 8 Rat 8.6 pKi = 8.6 Binding
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 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/jm800670r
1279 2119 79 None 3 8 Rat 8.6 pKi = 8.6 Binding
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 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/jm8005959
1279 2119 79 None 3 8 Rat 8.6 pKi = 8.6 Binding
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 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/jm800670r
4908365 2119 79 None 3 8 Rat 8.6 pKi = 8.6 Binding
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 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/jm8005959
4908365 2119 79 None 3 8 Rat 8.6 pKi = 8.6 Binding
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 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/jm800670r
CHEMBL129198 2119 79 None 3 8 Rat 8.6 pKi = 8.6 Binding
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 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/jm8005959
CHEMBL129198 2119 79 None 3 8 Rat 8.6 pKi = 8.6 Binding
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 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/jm800670r
137657169 159040 0 None 3 2 Human 8.6 pKi = 8.6 Binding
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 337 8 1 4 4.1 O=[N+]([O-])c1cccc(C(OCCCc2c[nH]cn2)c2ccccc2)c1 10.1016/j.ejmech.2016.09.074
CHEMBL4102970 159040 0 None 3 2 Human 8.6 pKi = 8.6 Binding
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 337 8 1 4 4.1 O=[N+]([O-])c1cccc(C(OCCCc2c[nH]cn2)c2ccccc2)c1 10.1016/j.ejmech.2016.09.074
59777258 109644 0 None - 1 Human 8.5 pKi = 8.5 Binding
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 273 2 2 5 1.5 Nc1nc(C2CCCC2)cc(N2C[C@H]3CCN[C@H]3C2)n1 10.1021/jm401727m
CHEMBL3236561 109644 0 None - 1 Human 8.5 pKi = 8.5 Binding
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 273 2 2 5 1.5 Nc1nc(C2CCCC2)cc(N2C[C@H]3CCN[C@H]3C2)n1 10.1021/jm401727m
25130914 186671 0 None - 1 Human 7.7 pKi = 7.7 Binding
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(NCc3ccccc3)nc(N)n2)CC1 10.1016/j.bmcl.2011.03.017
CHEMBL492677 186671 0 None - 1 Human 7.7 pKi = 7.7 Binding
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(NCc3ccccc3)nc(N)n2)CC1 10.1016/j.bmcl.2011.03.017
46890547 6438 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
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 6438 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
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
10446295 2101 29 None 269 2 Human 7.7 pKi = 7.7 Binding
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 278 1 1 3 1.6 CN1CCN(CC1)C(=O)c1nc2c([nH]1)cc(cc2)Cl 10.1021/jm401727m
1277 2101 29 None 269 2 Human 7.7 pKi = 7.7 Binding
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 278 1 1 3 1.6 CN1CCN(CC1)C(=O)c1nc2c([nH]1)cc(cc2)Cl 10.1021/jm401727m
CHEMBL185951 2101 29 None 269 2 Human 7.7 pKi = 7.7 Binding
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 278 1 1 3 1.6 CN1CCN(CC1)C(=O)c1nc2c([nH]1)cc(cc2)Cl 10.1021/jm401727m
68081305 109633 0 None - 1 Human 7.7 pKi = 7.7 Binding
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 1 1 2 1.3 CN1CCN(C(=O)c2cc3c([nH]2)CCCC3)CC1 10.1021/jm401727m
CHEMBL3236550 109633 0 None - 1 Human 7.7 pKi = 7.7 Binding
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 1 1 2 1.3 CN1CCN(C(=O)c2cc3c([nH]2)CCCC3)CC1 10.1021/jm401727m
24798144 109636 2 None -19 3 Mouse 7.7 pKi = 7.7 Binding
Displacement of [3H]histamine from mouse histamine H4 receptor expressed in SK-N-MC cells after 45 mins by competition binding analysisDisplacement of [3H]histamine from mouse 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 109636 2 None -19 3 Mouse 7.7 pKi = 7.7 Binding
Displacement of [3H]histamine from mouse histamine H4 receptor expressed in SK-N-MC cells after 45 mins by competition binding analysisDisplacement of [3H]histamine from mouse 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
24738103 67788 0 None - 1 Human 7.7 pKi = 7.7 Binding
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)nc3c2oc2cccc(OC)c23)C1 10.1016/j.bmcl.2011.08.014
CHEMBL1914780 67788 0 None - 1 Human 7.7 pKi = 7.7 Binding
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)nc3c2oc2cccc(OC)c23)C1 10.1016/j.bmcl.2011.08.014
24745335 292 7 None -6 5 Mouse 7.7 pKi = 7.7 Binding
Displacement of [3H]-histamine from mouse H4R expressed in HEK293T cellsDisplacement of [3H]-histamine from mouse 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 292 7 None -6 5 Mouse 7.7 pKi = 7.7 Binding
Displacement of [3H]-histamine from mouse H4R expressed in HEK293T cellsDisplacement of [3H]-histamine from mouse 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 292 7 None -6 5 Mouse 7.7 pKi = 7.7 Binding
Displacement of [3H]-histamine from mouse H4R expressed in HEK293T cellsDisplacement of [3H]-histamine from mouse 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 292 7 None -6 5 Mouse 7.7 pKi = 7.7 Binding
Displacement of [3H]-histamine from mouse H4R expressed in HEK293T cellsDisplacement of [3H]-histamine from mouse 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 292 7 None -6 5 Mouse 7.7 pKi = 7.7 Binding
Displacement of [3H]histamine from mouse histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from mouse 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 292 7 None -6 5 Mouse 7.7 pKi = 7.7 Binding
Displacement of [3H]histamine from mouse histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from mouse 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 292 7 None -6 5 Mouse 7.7 pKi = 7.7 Binding
Displacement of [3H]histamine from mouse histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from mouse 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 292 7 None -6 5 Mouse 7.7 pKi = 7.7 Binding
Displacement of [3H]histamine from mouse histamine H4 receptor expressed in HEK293T cellsDisplacement of [3H]histamine from mouse 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
16362 3076 67 None -562 29 Human 5.7 pKi = 5.7 Binding
Antagonist activity at H4 receptor (unknown origin)Antagonist activity at H4 receptor (unknown origin)
ChEMBL 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 10.1016/j.ejmech.2016.09.074
2172 3076 67 None -562 29 Human 5.7 pKi = 5.7 Binding
Antagonist activity at H4 receptor (unknown origin)Antagonist activity at H4 receptor (unknown origin)
ChEMBL 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 10.1016/j.ejmech.2016.09.074
90 3076 67 None -562 29 Human 5.7 pKi = 5.7 Binding
Antagonist activity at H4 receptor (unknown origin)Antagonist activity at H4 receptor (unknown origin)
ChEMBL 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 10.1016/j.ejmech.2016.09.074
CHEMBL1423 3076 67 None -562 29 Human 5.7 pKi = 5.7 Binding
Antagonist activity at H4 receptor (unknown origin)Antagonist activity at H4 receptor (unknown origin)
ChEMBL 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 10.1016/j.ejmech.2016.09.074
DB01100 3076 67 None -562 29 Human 5.7 pKi = 5.7 Binding
Antagonist activity at H4 receptor (unknown origin)Antagonist activity at H4 receptor (unknown origin)
ChEMBL 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 10.1016/j.ejmech.2016.09.074
9904236 13962 16 None - 1 Human 5.7 pKi = 5.7 Binding
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 295 0 1 3 3.7 O=C1Cc2ccccc2C(=C2CCNCC2)c2ccsc21 nan
CHEMBL1197564 13962 16 None - 1 Human 5.7 pKi = 5.7 Binding
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 295 0 1 3 3.7 O=C1Cc2ccccc2C(=C2CCNCC2)c2ccsc21 nan
46890589 6944 0 None - 1 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 424 7 1 4 4.8 Cc1cc(OCCCN2CCCC(N(C)C)C2)ccc1-c1nc2c(C)c(F)ccc2[nH]1 10.1016/j.bmcl.2010.04.017
CHEMBL1084809 6944 0 None - 1 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 424 7 1 4 4.8 Cc1cc(OCCCN2CCCC(N(C)C)C2)ccc1-c1nc2c(C)c(F)ccc2[nH]1 10.1016/j.bmcl.2010.04.017
57396382 67977 0 None - 1 Human 4.7 pKi = 4.7 Binding
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 387 9 2 7 3.8 COCc1ccc(CN2CC[C@H](Nc3cc(NCCC(C)(C)C)ncn3)C2)o1 10.1016/j.bmcl.2011.07.114
CHEMBL1916495 67977 0 None - 1 Human 4.7 pKi = 4.7 Binding
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 387 9 2 7 3.8 COCc1ccc(CN2CC[C@H](Nc3cc(NCCC(C)(C)C)ncn3)C2)o1 10.1016/j.bmcl.2011.07.114
57391122 67978 0 None - 1 Human 4.7 pKi = 4.7 Binding
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 387 7 3 6 3.9 CC(C)(C)CCNc1cc(N[C@H]2CCN(Cc3cccc(F)c3O)C2)ncn1 10.1016/j.bmcl.2011.07.114
CHEMBL1916496 67978 0 None - 1 Human 4.7 pKi = 4.7 Binding
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 387 7 3 6 3.9 CC(C)(C)CCNc1cc(N[C@H]2CCN(Cc3cccc(F)c3O)C2)ncn1 10.1016/j.bmcl.2011.07.114
57394628 67983 1 None - 1 Human 6.7 pKi = 6.7 Binding
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 263 4 2 5 1.7 CC(C)(C)CCNc1cc(N2CCNCC2)ncn1 10.1016/j.bmcl.2011.07.114
CHEMBL1916500 67983 1 None - 1 Human 6.7 pKi = 6.7 Binding
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 263 4 2 5 1.7 CC(C)(C)CCNc1cc(N2CCNCC2)ncn1 10.1016/j.bmcl.2011.07.114
57397738 69521 0 None - 1 Human 4.7 pKi = 4.7 Binding
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 245 1 0 5 0.1 CN1CCN(C(=O)c2cn3ccncc3n2)CC1 10.1016/j.bmcl.2011.11.098
CHEMBL1938841 69521 0 None - 1 Human 4.7 pKi = 4.7 Binding
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 245 1 0 5 0.1 CN1CCN(C(=O)c2cn3ccncc3n2)CC1 10.1016/j.bmcl.2011.11.098
10399535 117937 3 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]- histamine from the recombinant human histamine H4 receptorDisplacement of [3H]- histamine from the recombinant human histamine H4 receptor
ChEMBL 243 1 2 2 1.6 CC1CN(C(=O)c2cc3ccccc3[nH]2)CCN1 10.1021/jm0341047
CHEMBL341087 117937 3 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]- histamine from the recombinant human histamine H4 receptorDisplacement of [3H]- histamine from the recombinant human histamine H4 receptor
ChEMBL 243 1 2 2 1.6 CC1CN(C(=O)c2cc3ccccc3[nH]2)CCN1 10.1021/jm0341047
90645147 111684 0 None 13 3 Human 6.7 pKi = 6.7 Binding
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 304 2 1 6 1.5 CN1CCN(c2nc(N)nc(-c3ccc(Cl)cc3)n2)CC1 10.1016/j.ejmech.2014.06.032
CHEMBL3290576 111684 0 None 13 3 Human 6.7 pKi = 6.7 Binding
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 304 2 1 6 1.5 CN1CCN(c2nc(N)nc(-c3ccc(Cl)cc3)n2)CC1 10.1016/j.ejmech.2014.06.032
155567108 176062 0 None 3 2 Human 6.7 pKi = 6.7 Binding
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 223 5 3 5 1.3 CC(C)(C)CNc1nccc(NCCN)n1 10.1021/acs.jmedchem.9b01342
CHEMBL4586599 176062 0 None 3 2 Human 6.7 pKi = 6.7 Binding
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 223 5 3 5 1.3 CC(C)(C)CNc1nccc(NCCN)n1 10.1021/acs.jmedchem.9b01342
CHEMBL4597946 176062 0 None 3 2 Human 6.7 pKi = 6.7 Binding
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 223 5 3 5 1.3 CC(C)(C)CNc1nccc(NCCN)n1 10.1021/acs.jmedchem.9b01342
155536509 175898 0 None -21 2 Human 6.7 pKi = 6.7 Binding
Displacement of 40 nM [3H]-histamine from human H4R expressed in Sf9 cell membranes co-expressing Gia2 and beta1gamma2 by competition binding assayDisplacement of 40 nM [3H]-histamine from human H4R expressed in Sf9 cell membranes co-expressing Gia2 and beta1gamma2 by competition binding assay
ChEMBL 274 6 3 5 2.3 CC(C)(C)CNc1nccc(NCCc2c[nH]cn2)n1 10.1021/acs.jmedchem.9b01342
CHEMBL4473753 175898 0 None -21 2 Human 6.7 pKi = 6.7 Binding
Displacement of 40 nM [3H]-histamine from human H4R expressed in Sf9 cell membranes co-expressing Gia2 and beta1gamma2 by competition binding assayDisplacement of 40 nM [3H]-histamine from human H4R expressed in Sf9 cell membranes co-expressing Gia2 and beta1gamma2 by competition binding assay
ChEMBL 274 6 3 5 2.3 CC(C)(C)CNc1nccc(NCCc2c[nH]cn2)n1 10.1021/acs.jmedchem.9b01342
CHEMBL4596582 175898 0 None -21 2 Human 6.7 pKi = 6.7 Binding
Displacement of 40 nM [3H]-histamine from human H4R expressed in Sf9 cell membranes co-expressing Gia2 and beta1gamma2 by competition binding assayDisplacement of 40 nM [3H]-histamine from human H4R expressed in Sf9 cell membranes co-expressing Gia2 and beta1gamma2 by competition binding assay
ChEMBL 274 6 3 5 2.3 CC(C)(C)CNc1nccc(NCCc2c[nH]cn2)n1 10.1021/acs.jmedchem.9b01342
4687476 95864 4 None - 1 Human 4.7 pKi = 4.7 Binding
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 227 1 0 3 2.0 CN1CCN(c2nccc3ccccc23)CC1 10.1016/j.bmcl.2011.10.104
CHEMBL261320 95864 4 None - 1 Human 4.7 pKi = 4.7 Binding
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 227 1 0 3 2.0 CN1CCN(c2nccc3ccccc23)CC1 10.1016/j.bmcl.2011.10.104
9928073 201954 0 None -67 3 Human 5.7 pKi = 5.7 Binding
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 343 0 0 4 4.1 CN1CCN(C2=Nc3cc(Cl)ccc3Sc3ccccc32)CC1 10.1021/jm051008s
CHEMBL67284 201954 0 None -67 3 Human 5.7 pKi = 5.7 Binding
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 343 0 0 4 4.1 CN1CCN(C2=Nc3cc(Cl)ccc3Sc3ccccc32)CC1 10.1021/jm051008s
90654501 109820 0 None -21877 3 Human 4.7 pKi = 4.7 Binding
Displacement of [3H]histamine from human H4 receptor expressed in Sf9 cell membrane co-transfected with Galphai2 and Gbeta1gamma2 after 60 mins by liquid scintillation counting analysisDisplacement of [3H]histamine from human H4 receptor expressed in Sf9 cell membrane co-transfected with Galphai2 and Gbeta1gamma2 after 60 mins by liquid scintillation counting analysis
ChEMBL 314 6 0 5 3.1 Cc1nnc(C)n1-c1ccc(OCCCN2CCCCC2)cc1 10.1016/j.ejmech.2014.03.014
CHEMBL3238444 109820 0 None -21877 3 Human 4.7 pKi = 4.7 Binding
Displacement of [3H]histamine from human H4 receptor expressed in Sf9 cell membrane co-transfected with Galphai2 and Gbeta1gamma2 after 60 mins by liquid scintillation counting analysisDisplacement of [3H]histamine from human H4 receptor expressed in Sf9 cell membrane co-transfected with Galphai2 and Gbeta1gamma2 after 60 mins by liquid scintillation counting analysis
ChEMBL 314 6 0 5 3.1 Cc1nnc(C)n1-c1ccc(OCCCN2CCCCC2)cc1 10.1016/j.ejmech.2014.03.014
4687476 95864 4 None - 1 Human 4.7 pKi = 4.7 Binding
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 227 1 0 3 2.0 CN1CCN(c2nccc3ccccc23)CC1 10.1021/jm7014217
CHEMBL261320 95864 4 None - 1 Human 4.7 pKi = 4.7 Binding
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 227 1 0 3 2.0 CN1CCN(c2nccc3ccccc23)CC1 10.1021/jm7014217
10879463 5218 0 None -1 2 Human 4.7 pKi = 4.7 Binding
Histamine H4 receptor competition binding using [3H]Na-methylhistamineHistamine H4 receptor competition binding using [3H]Na-methylhistamine
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 5218 0 None -1 2 Human 4.7 pKi = 4.7 Binding
Histamine H4 receptor competition binding using [3H]Na-methylhistamineHistamine H4 receptor competition binding using [3H]Na-methylhistamine
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
46228132 200459 0 None - 1 Human 6.7 pKi = 6.7 Binding
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 312 4 2 6 1.7 Cc1ccc(CNc2cc(N3CCN(C)CC3)nc(N)n2)cc1 10.1016/j.bmc.2009.08.059
CHEMBL609161 200459 0 None - 1 Human 6.7 pKi = 6.7 Binding
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 312 4 2 6 1.7 Cc1ccc(CNc2cc(N3CCN(C)CC3)nc(N)n2)cc1 10.1016/j.bmc.2009.08.059
46228071 198494 15 None - 1 Human 6.7 pKi = 6.7 Binding
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 283 4 1 5 1.8 CN1CCN(c2cc(NCc3ccccc3)ncn2)CC1 10.1016/j.bmcl.2011.07.114
CHEMBL596562 198494 15 None - 1 Human 6.7 pKi = 6.7 Binding
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 283 4 1 5 1.8 CN1CCN(c2cc(NCc3ccccc3)ncn2)CC1 10.1016/j.bmcl.2011.07.114
51354870 58596 0 None -26 2 Human 4.7 pKi = 4.7 Binding
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 305 6 0 5 2.0 CN1CCN(CCCn2cc(CC3CCCCC3)nn2)CC1 10.1021/jm1013488
CHEMBL1688981 58596 0 None -26 2 Human 4.7 pKi = 4.7 Binding
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 305 6 0 5 2.0 CN1CCN(CCCn2cc(CC3CCCCC3)nn2)CC1 10.1021/jm1013488
57391928 69566 0 None - 1 Human 5.7 pKi = 5.7 Binding
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 304 1 1 3 1.9 CN1C[C@H]2CN(C(=O)c3cc4ccc(Cl)nc4[nH]3)C[C@H]2C1 10.1016/j.bmcl.2011.11.098
CHEMBL1938973 69566 0 None - 1 Human 5.7 pKi = 5.7 Binding
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 304 1 1 3 1.9 CN1C[C@H]2CN(C(=O)c3cc4ccc(Cl)nc4[nH]3)C[C@H]2C1 10.1016/j.bmcl.2011.11.098
23650960 148597 0 None - 1 Human 7.7 pKi = 7.7 Binding
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 396 6 2 5 4.3 Cc1nc(NCCCC2CCN(C)CC2)ncc1-c1nc2c(C)c(F)ccc2[nH]1 nan
CHEMBL3943309 148597 0 None - 1 Human 7.7 pKi = 7.7 Binding
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 396 6 2 5 4.3 Cc1nc(NCCCC2CCN(C)CC2)ncc1-c1nc2c(C)c(F)ccc2[nH]1 nan
42624149 109651 1 None 3 3 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 221 3 2 5 0.4 CCc1cc(N2CC[C@@H](NC)C2)nc(N)n1 10.1016/j.bmcl.2014.10.013
CHEMBL3236568 109651 1 None 3 3 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 221 3 2 5 0.4 CCc1cc(N2CC[C@@H](NC)C2)nc(N)n1 10.1016/j.bmcl.2014.10.013
25218146 116605 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 259 2 0 4 2.6 CN1CCN(c2ccnc(-c3ccsc3)c2)CC1 10.1016/j.bmcl.2014.12.027
CHEMBL3393521 116605 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 259 2 0 4 2.6 CN1CCN(c2ccnc(-c3ccsc3)c2)CC1 10.1016/j.bmcl.2014.12.027
42624149 109651 1 None 3 3 Human 7.7 pKi = 7.7 Binding
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 3 2 5 0.4 CCc1cc(N2CC[C@@H](NC)C2)nc(N)n1 10.1021/jm401727m
CHEMBL3236568 109651 1 None 3 3 Human 7.7 pKi = 7.7 Binding
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 3 2 5 0.4 CCc1cc(N2CC[C@@H](NC)C2)nc(N)n1 10.1021/jm401727m
53258370 109652 1 None - 1 Human 7.7 pKi = 7.7 Binding
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 207 2 2 5 0.2 CCc1cc(N2CC[C@@H](N)C2)nc(N)n1 10.1021/jm401727m
CHEMBL3236569 109652 1 None - 1 Human 7.7 pKi = 7.7 Binding
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 207 2 2 5 0.2 CCc1cc(N2CC[C@@H](N)C2)nc(N)n1 10.1021/jm401727m
57394548 67756 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 343 1 2 6 2.8 Nc1nc(N2C[C@@H]3CCCN[C@@H]3C2)c2oc3ccc(Cl)cc3c2n1 10.1016/j.bmcl.2011.08.014
CHEMBL1914747 67756 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 343 1 2 6 2.8 Nc1nc(N2C[C@@H]3CCCN[C@@H]3C2)c2oc3ccc(Cl)cc3c2n1 10.1016/j.bmcl.2011.08.014
57396298 67761 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 301 1 1 6 1.8 CN1CCN(c2nc(N)nc3c2oc2cccc(F)c23)CC1 10.1016/j.bmcl.2011.08.014
CHEMBL1914752 67761 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 301 1 1 6 1.8 CN1CCN(c2nc(N)nc3c2oc2cccc(F)c23)CC1 10.1016/j.bmcl.2011.08.014
44628629 67776 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 269 1 2 6 1.4 Nc1nc(N2CCNCC2)c2oc3ccccc3c2n1 10.1016/j.bmcl.2011.08.014
CHEMBL1914767 67776 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 269 1 2 6 1.4 Nc1nc(N2CCNCC2)c2oc3ccccc3c2n1 10.1016/j.bmcl.2011.08.014
11630326 72226 0 None - 1 Human 7.7 pKi = 7.7 Binding
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 263 1 1 3 1.9 Cc1csc2cc(C(=O)N3CCN(C)CC3)[nH]c12 10.1021/jm0502081
CHEMBL199231 72226 0 None - 1 Human 7.7 pKi = 7.7 Binding
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 263 1 1 3 1.9 Cc1csc2cc(C(=O)N3CCN(C)CC3)[nH]c12 10.1021/jm0502081
51354582 58590 0 None 2 2 Human 7.7 pKi = 7.7 Binding
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 287 6 1 4 3.3 CC(c1cn(CCCc2c[nH]cn2)nn1)C1CCCCC1 10.1021/jm1013488
CHEMBL1688974 58590 0 None 2 2 Human 7.7 pKi = 7.7 Binding
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 287 6 1 4 3.3 CC(c1cn(CCCc2c[nH]cn2)nn1)C1CCCCC1 10.1021/jm1013488
71603195 89293 0 None 8 2 Human 7.7 pKi = 7.7 Binding
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 283 3 2 5 1.9 CN[C@@H]1CCN(c2nc(N)nc3cc(C4CC4)ccc23)C1 10.1016/j.bmcl.2013.02.091
CHEMBL2376798 89293 0 None 8 2 Human 7.7 pKi = 7.7 Binding
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 283 3 2 5 1.9 CN[C@@H]1CCN(c2nc(N)nc3cc(C4CC4)ccc23)C1 10.1016/j.bmcl.2013.02.091
1251 1983 34 None -100 5 Human 7.7 pKi = 7.7 Binding
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 165 2 2 2 1.0 N1CCC(CC1)Cc1[nH]cnc1 10.1021/jm049932u
3035842 1983 34 None -100 5 Human 7.7 pKi = 7.7 Binding
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 165 2 2 2 1.0 N1CCC(CC1)Cc1[nH]cnc1 10.1021/jm049932u
CHEMBL18661 1983 34 None -100 5 Human 7.7 pKi = 7.7 Binding
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 165 2 2 2 1.0 N1CCC(CC1)Cc1[nH]cnc1 10.1021/jm049932u
1530 2151 44 None -21379 20 Human 4.7 pKi = 4.7 Binding
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 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 nan
3827 2151 44 None -21379 20 Human 4.7 pKi = 4.7 Binding
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 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 nan
7206 2151 44 None -21379 20 Human 4.7 pKi = 4.7 Binding
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 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 nan
CHEMBL534 2151 44 None -21379 20 Human 4.7 pKi = 4.7 Binding
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 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 nan
DB00920 2151 44 None -21379 20 Human 4.7 pKi = 4.7 Binding
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 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 nan
57399107 67872 0 None - 1 Human 5.7 pKi = 5.7 Binding
Binding affinity to human histamine H4 receptorBinding affinity to human histamine H4 receptor
ChEMBL 373 8 3 7 3.1 CC(C)(C)CCNc1cc(NC2CCN(Cc3ccc(CO)o3)C2)ncn1 10.1021/acs.jmedchem.5b00516
CHEMBL1915532 67872 0 None - 1 Human 5.7 pKi = 5.7 Binding
Binding affinity to human histamine H4 receptorBinding affinity to human histamine H4 receptor
ChEMBL 373 8 3 7 3.1 CC(C)(C)CCNc1cc(NC2CCN(Cc3ccc(CO)o3)C2)ncn1 10.1021/acs.jmedchem.5b00516
57399107 67872 0 None - 1 Human 5.7 pKi = 5.7 Binding
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 373 8 3 7 3.1 CC(C)(C)CCNc1cc(NC2CCN(Cc3ccc(CO)o3)C2)ncn1 10.1016/j.bmcl.2011.07.125
CHEMBL1915532 67872 0 None - 1 Human 5.7 pKi = 5.7 Binding
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 373 8 3 7 3.1 CC(C)(C)CCNc1cc(NC2CCN(Cc3ccc(CO)o3)C2)ncn1 10.1016/j.bmcl.2011.07.125
57399107 67872 0 None - 1 Human 5.7 pKi = 5.7 Binding
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 373 8 3 7 3.1 CC(C)(C)CCNc1cc(NC2CCN(Cc3ccc(CO)o3)C2)ncn1 10.1016/j.bmcl.2011.07.114
CHEMBL1915532 67872 0 None - 1 Human 5.7 pKi = 5.7 Binding
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 373 8 3 7 3.1 CC(C)(C)CCNc1cc(NC2CCN(Cc3ccc(CO)o3)C2)ncn1 10.1016/j.bmcl.2011.07.114
57395619 67873 13 None - 1 Human 6.7 pKi = 6.7 Binding
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 309 3 1 5 1.8 CN1CCN(c2cc(NC3Cc4ccccc4C3)ncn2)CC1 10.1016/j.bmcl.2011.07.125
CHEMBL1915533 67873 13 None - 1 Human 6.7 pKi = 6.7 Binding
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 309 3 1 5 1.8 CN1CCN(c2cc(NC3Cc4ccccc4C3)ncn2)CC1 10.1016/j.bmcl.2011.07.125
57395619 67873 13 None - 1 Human 6.7 pKi = 6.7 Binding
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 309 3 1 5 1.8 CN1CCN(c2cc(NC3Cc4ccccc4C3)ncn2)CC1 10.1016/j.bmcl.2011.07.114
CHEMBL1915533 67873 13 None - 1 Human 6.7 pKi = 6.7 Binding
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 309 3 1 5 1.8 CN1CCN(c2cc(NC3Cc4ccccc4C3)ncn2)CC1 10.1016/j.bmcl.2011.07.114
168268680 192164 0 None -2 4 Human 5.7 pKi = 5.7 Binding
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 192164 0 None -2 4 Human 5.7 pKi = 5.7 Binding
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 192164 0 None -2 4 Human 5.7 pKi = 5.7 Binding
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
1403136 179927 7 None - 1 Human 5.7 pKi = 5.7 Binding
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 243 1 1 5 1.0 CN1CCN(c2nc(N)c3ccccc3n2)CC1 10.1021/jm800876b
CHEMBL475331 179927 7 None - 1 Human 5.7 pKi = 5.7 Binding
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 243 1 1 5 1.0 CN1CCN(c2nc(N)c3ccccc3n2)CC1 10.1021/jm800876b
1204 1901 114 None -15 23 Mouse 5.7 pKi = 5.7 Binding
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 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.0c00160
1247 1901 114 None -15 23 Mouse 5.7 pKi = 5.7 Binding
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 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.0c00160
1375 1901 114 None -15 23 Mouse 5.7 pKi = 5.7 Binding
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 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.0c00160
774 1901 114 None -15 23 Mouse 5.7 pKi = 5.7 Binding
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 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.0c00160
CHEMBL90 1901 114 None -15 23 Mouse 5.7 pKi = 5.7 Binding
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 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.0c00160
DB05381 1901 114 None -15 23 Mouse 5.7 pKi = 5.7 Binding
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 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.0c00160
164610824 184527 0 None -14 4 Human 4.7 pKi = 4.7 Binding
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 452 8 4 4 3.6 Cc1nc(N)sc1CCCN/C(N)=N/C(=S)NCC(c1ccccc1)c1ccccc1 10.1016/j.ejmech.2021.113190
CHEMBL4856200 184527 0 None -14 4 Human 4.7 pKi = 4.7 Binding
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 452 8 4 4 3.6 Cc1nc(N)sc1CCCN/C(N)=N/C(=S)NCC(c1ccccc1)c1ccccc1 10.1016/j.ejmech.2021.113190
10945113 109141 1 None -1 2 Human 4.7 pKi = 4.7 Binding
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
CHEMBL322256 109141 1 None -1 2 Human 4.7 pKi = 4.7 Binding
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
21896704 158979 0 None - 1 Human 6.7 pKi = 6.7 Binding
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 429 9 1 7 2.7 CC(=O)SCC(Cc1ccc2c(c1)OCO2)C(=O)NCC(=O)OCc1ccccc1 10.1016/j.ejmech.2016.09.074
CHEMBL4102243 158979 0 None - 1 Human 6.7 pKi = 6.7 Binding
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 429 9 1 7 2.7 CC(=O)SCC(Cc1ccc2c(c1)OCO2)C(=O)NCC(=O)OCc1ccccc1 10.1016/j.ejmech.2016.09.074
46912441 10801 0 None -117 2 Human 6.7 pKi = 6.7 Binding
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 309 3 1 2 3.9 FC(F)(F)c1ccc(N2CCC(Cc3c[nH]cn3)CC2)cc1 10.1016/j.bmc.2010.04.052
CHEMBL1172754 10801 0 None -117 2 Human 6.7 pKi = 6.7 Binding
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 309 3 1 2 3.9 FC(F)(F)c1ccc(N2CCC(Cc3c[nH]cn3)CC2)cc1 10.1016/j.bmc.2010.04.052
118725538 116606 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 259 3 1 4 2.6 CN[C@@H]1CCN(c2ccnc(-c3ccsc3)c2)C1 10.1016/j.bmcl.2014.12.027
CHEMBL3393522 116606 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 259 3 1 4 2.6 CN[C@@H]1CCN(c2ccnc(-c3ccsc3)c2)C1 10.1016/j.bmcl.2014.12.027
1204 1901 114 None -3 23 Human 6.7 pKi = 6.7 Binding
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 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.0c00160
1247 1901 114 None -3 23 Human 6.7 pKi = 6.7 Binding
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 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.0c00160
1375 1901 114 None -3 23 Human 6.7 pKi = 6.7 Binding
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 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.0c00160
774 1901 114 None -3 23 Human 6.7 pKi = 6.7 Binding
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 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.0c00160
CHEMBL90 1901 114 None -3 23 Human 6.7 pKi = 6.7 Binding
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 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.0c00160
DB05381 1901 114 None -3 23 Human 6.7 pKi = 6.7 Binding
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 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.0c00160
155567030 175843 0 None -645 4 Human 4.7 pKi = 4.7 Binding
Displacement of [3H]histamine from human recombinant H4R expressed in CHO cells incubated for 60 mins by microbeta scintillation counter methodDisplacement of [3H]histamine from human recombinant H4R expressed in CHO cells incubated for 60 mins by microbeta scintillation counter method
ChEMBL 337 8 0 2 5.8 c1ccc(-c2ccc(OCCCCCN3CCCCCC3)cc2)cc1 10.1016/j.bmc.2017.07.058
CHEMBL4586133 175843 0 None -645 4 Human 4.7 pKi = 4.7 Binding
Displacement of [3H]histamine from human recombinant H4R expressed in CHO cells incubated for 60 mins by microbeta scintillation counter methodDisplacement of [3H]histamine from human recombinant H4R expressed in CHO cells incubated for 60 mins by microbeta scintillation counter method
ChEMBL 337 8 0 2 5.8 c1ccc(-c2ccc(OCCCCCN3CCCCCC3)cc2)cc1 10.1016/j.bmc.2017.07.058
CHEMBL4596108 175843 0 None -645 4 Human 4.7 pKi = 4.7 Binding
Displacement of [3H]histamine from human recombinant H4R expressed in CHO cells incubated for 60 mins by microbeta scintillation counter methodDisplacement of [3H]histamine from human recombinant H4R expressed in CHO cells incubated for 60 mins by microbeta scintillation counter method
ChEMBL 337 8 0 2 5.8 c1ccc(-c2ccc(OCCCCCN3CCCCCC3)cc2)cc1 10.1016/j.bmc.2017.07.058
24854708 155182 0 None - 1 Human 5.7 pKi = 5.7 Binding
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 334 3 0 5 3.5 Cc1ccc(Oc2nc3ccccc3nc2N2CCN(C)CC2)cc1 10.1021/jm7014217
CHEMBL405416 155182 0 None - 1 Human 5.7 pKi = 5.7 Binding
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 334 3 0 5 3.5 Cc1ccc(Oc2nc3ccccc3nc2N2CCN(C)CC2)cc1 10.1021/jm7014217
51354587 58595 0 None -3 2 Human 4.7 pKi = 4.7 Binding
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 6 0 5 2.7 c1cn(CCCn2cc(CC3CCCCC3)nn2)cn1 10.1021/jm1013488
CHEMBL1688979 58595 0 None -3 2 Human 4.7 pKi = 4.7 Binding
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 6 0 5 2.7 c1cn(CCCn2cc(CC3CCCCC3)nn2)cn1 10.1021/jm1013488
10702196 108081 1 None -1 2 Human 4.7 pKi = 4.7 Binding
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
CHEMBL320279 108081 1 None -1 2 Human 4.7 pKi = 4.7 Binding
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
136016345 10286 2 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in SK-NM-C cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in SK-NM-C cells
ChEMBL 377 5 4 6 2.1 CCOC(=O)c1ccc(NC2=CC(=O)/C(=N\NC(=N)N)c3ccccc32)cc1 10.1021/jm7014777
CHEMBL1162352 10286 2 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in SK-NM-C cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in SK-NM-C cells
ChEMBL 377 5 4 6 2.1 CCOC(=O)c1ccc(NC2=CC(=O)/C(=N\NC(=N)N)c3ccccc32)cc1 10.1021/jm7014777
127052293 139708 1 None 34 4 Human 7.7 pKi = 7.7 Binding
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
CHEMBL3805361 139708 1 None 34 4 Human 7.7 pKi = 7.7 Binding
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
1251 1983 34 None -100 5 Human 7.7 pKi = 7.7 Binding
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 165 2 2 2 1.0 N1CCC(CC1)Cc1[nH]cnc1 10.1016/j.bmc.2010.04.052
3035842 1983 34 None -100 5 Human 7.7 pKi = 7.7 Binding
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 165 2 2 2 1.0 N1CCC(CC1)Cc1[nH]cnc1 10.1016/j.bmc.2010.04.052
CHEMBL18661 1983 34 None -100 5 Human 7.7 pKi = 7.7 Binding
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 165 2 2 2 1.0 N1CCC(CC1)Cc1[nH]cnc1 10.1016/j.bmc.2010.04.052
11258459 83814 0 None - 1 Human 7.7 pKi = 7.7 Binding
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 412 6 1 4 4.5 Cc1cc(C)c2nc(-c3ccc(OCCCN4CCN(C)CC4)cc3Cl)[nH]c2c1 10.1016/j.bmcl.2006.08.117
CHEMBL220933 83814 0 None - 1 Human 7.7 pKi = 7.7 Binding
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 412 6 1 4 4.5 Cc1cc(C)c2nc(-c3ccc(OCCCN4CCN(C)CC4)cc3Cl)[nH]c2c1 10.1016/j.bmcl.2006.08.117
46228082 200692 0 None - 1 Human 5.7 pKi = 5.7 Binding
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 340 5 2 6 2.5 CC(C)c1ccc(CNc2cc(N3CCN(C)CC3)nc(N)n2)cc1 10.1016/j.bmc.2009.08.059
CHEMBL610626 200692 0 None - 1 Human 5.7 pKi = 5.7 Binding
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 340 5 2 6 2.5 CC(C)c1ccc(CNc2cc(N3CCN(C)CC3)nc(N)n2)cc1 10.1016/j.bmc.2009.08.059
49841721 69381 0 None - 1 Human 6.7 pKi = 6.7 Binding
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 347 2 1 5 3.2 Cc1cccc(C)c1-c1cccc2c(N3CCN(C)CC3)nc(N)nc12 10.1016/j.bmcl.2011.10.104
CHEMBL1935558 69381 0 None - 1 Human 6.7 pKi = 6.7 Binding
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 347 2 1 5 3.2 Cc1cccc(C)c1-c1cccc2c(N3CCN(C)CC3)nc(N)nc12 10.1016/j.bmcl.2011.10.104
25178551 173659 0 None - 1 Human 6.7 pKi = 6.7 Binding
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 341 4 1 6 2.7 CN1CCN(c2nc(NCc3ccco3)c3cc(F)ccc3n2)CC1 10.1021/jm800876b
CHEMBL454882 173659 0 None - 1 Human 6.7 pKi = 6.7 Binding
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 341 4 1 6 2.7 CN1CCN(c2nc(NCc3ccco3)c3cc(F)ccc3n2)CC1 10.1021/jm800876b
25178551 173659 0 None - 1 Human 6.7 pKi = 6.7 Binding
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 341 4 1 6 2.7 CN1CCN(c2nc(NCc3ccco3)c3cc(F)ccc3n2)CC1 10.1021/jm901379s
CHEMBL454882 173659 0 None - 1 Human 6.7 pKi = 6.7 Binding
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 341 4 1 6 2.7 CN1CCN(c2nc(NCc3ccco3)c3cc(F)ccc3n2)CC1 10.1021/jm901379s
45379807 197828 0 None - 1 Human 6.7 pKi = 6.7 Binding
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 438 6 1 6 3.5 CN1CCN(c2nc(NCCC(=O)N(C)c3ccccc3)c3cc(Cl)ccc3n2)CC1 10.1021/jm901379s
CHEMBL591970 197828 0 None - 1 Human 6.7 pKi = 6.7 Binding
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 438 6 1 6 3.5 CN1CCN(c2nc(NCCC(=O)N(C)c3ccccc3)c3cc(Cl)ccc3n2)CC1 10.1021/jm901379s
10037650 5138 0 None 31 2 Human 6.7 pKi = 6.7 Binding
Histamine H4 receptor competition binding using [3H]Na-methylhistamineHistamine H4 receptor competition binding using [3H]Na-methylhistamine
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 5138 0 None 31 2 Human 6.7 pKi = 6.7 Binding
Histamine H4 receptor competition binding using [3H]Na-methylhistamineHistamine H4 receptor competition binding using [3H]Na-methylhistamine
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
122194624 123502 0 None - 1 Human 5.7 pKi = 5.7 Binding
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 310 3 1 6 1.7 Cc1ccccc1/C=C/c1nc(N)nc(N2CCN(C)CC2)n1 10.1016/j.ejmech.2015.08.014
CHEMBL3629827 123502 0 None - 1 Human 5.7 pKi = 5.7 Binding
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 310 3 1 6 1.7 Cc1ccccc1/C=C/c1nc(N)nc(N2CCN(C)CC2)n1 10.1016/j.ejmech.2015.08.014
57400700 67536 0 None -3090 3 Human 4.7 pKi = 4.7 Binding
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 470 8 1 6 3.4 COc1ccc(CN(CCN2CCN(C(=O)c3nc4ccccc4[nH]3)CC2)c2ccccn2)cc1 10.1016/j.bmcl.2011.09.001
CHEMBL1910380 67536 0 None -3090 3 Human 4.7 pKi = 4.7 Binding
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 470 8 1 6 3.4 COc1ccc(CN(CCN2CCN(C(=O)c3nc4ccccc4[nH]3)CC2)c2ccccn2)cc1 10.1016/j.bmcl.2011.09.001
164610421 184678 0 None -7 2 Human 4.7 pKi = 4.7 Binding
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 332 5 4 4 2.1 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)Nc1ccccc1 10.1016/j.ejmech.2021.113190
CHEMBL4858567 184678 0 None -7 2 Human 4.7 pKi = 4.7 Binding
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 332 5 4 4 2.1 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)Nc1ccccc1 10.1016/j.ejmech.2021.113190
46890120 6459 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 416 6 1 4 5.2 Cc1cc(OCCCN2Cc3cccnc3C2)ccc1-c1nc2c(C)c(F)ccc2[nH]1 10.1016/j.bmcl.2010.04.017
CHEMBL1082851 6459 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 416 6 1 4 5.2 Cc1cc(OCCCN2Cc3cccnc3C2)ccc1-c1nc2c(C)c(F)ccc2[nH]1 10.1016/j.bmcl.2010.04.017
56851604 71285 0 None -13 2 Human 6.6 pKi = 6.6 Binding
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 398 8 2 3 5.1 Clc1ccc(C/N=C(/NCc2ccccc2)SCCCc2c[nH]cn2)cc1 10.1021/jm201042n
CHEMBL1923028 71285 0 None -13 2 Human 6.6 pKi = 6.6 Binding
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 398 8 2 3 5.1 Clc1ccc(C/N=C(/NCc2ccccc2)SCCCc2c[nH]cn2)cc1 10.1021/jm201042n
CHEMBL1963460 71285 0 None -13 2 Human 6.6 pKi = 6.6 Binding
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 398 8 2 3 5.1 Clc1ccc(C/N=C(/NCc2ccccc2)SCCCc2c[nH]cn2)cc1 10.1021/jm201042n
24853663 95585 0 None - 1 Human 6.6 pKi = 6.6 Binding
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 272 3 0 5 1.8 CCOc1nc2ccccc2nc1N1CCN(C)CC1 10.1021/jm7014217
CHEMBL259839 95585 0 None - 1 Human 6.6 pKi = 6.6 Binding
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 272 3 0 5 1.8 CCOc1nc2ccccc2nc1N1CCN(C)CC1 10.1021/jm7014217
24278976 95804 56 None - 1 Human 6.6 pKi = 6.6 Binding
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 262 1 0 4 2.0 CN1CCN(c2nc3ccccc3nc2Cl)CC1 10.1021/jm7014217
CHEMBL261010 95804 56 None - 1 Human 6.6 pKi = 6.6 Binding
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 262 1 0 4 2.0 CN1CCN(c2nc3ccccc3nc2Cl)CC1 10.1021/jm7014217
24854704 95688 0 None - 1 Human 5.6 pKi = 5.6 Binding
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 368 4 0 5 3.6 CN1CCN(c2nc3ccccc3nc2OCc2ccc(Cl)cc2)CC1 10.1021/jm7014217
CHEMBL260456 95688 0 None - 1 Human 5.6 pKi = 5.6 Binding
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 368 4 0 5 3.6 CN1CCN(c2nc3ccccc3nc2OCc2ccc(Cl)cc2)CC1 10.1021/jm7014217
10923241 18972 1 None - 1 Human 7.6 pKi = 7.6 Binding
Antagonist activity at Homo sapiens (human) histamine H4 receptorAntagonist activity at Homo sapiens (human) histamine H4 receptor
ChEMBL 259 1 2 3 1.3 CN1CCN(C(=O)c2cc3cc(O)ccc3[nH]2)CC1 10.1007/s00044-004-0106-7
CHEMBL128958 18972 1 None - 1 Human 7.6 pKi = 7.6 Binding
Antagonist activity at Homo sapiens (human) histamine H4 receptorAntagonist activity at Homo sapiens (human) histamine H4 receptor
ChEMBL 259 1 2 3 1.3 CN1CCN(C(=O)c2cc3cc(O)ccc3[nH]2)CC1 10.1007/s00044-004-0106-7
10923241 18972 1 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]- histamine from the recombinant human histamine H4 receptorDisplacement of [3H]- histamine from the recombinant human histamine H4 receptor
ChEMBL 259 1 2 3 1.3 CN1CCN(C(=O)c2cc3cc(O)ccc3[nH]2)CC1 10.1021/jm0341047
CHEMBL128958 18972 1 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]- histamine from the recombinant human histamine H4 receptorDisplacement of [3H]- histamine from the recombinant human histamine H4 receptor
ChEMBL 259 1 2 3 1.3 CN1CCN(C(=O)c2cc3cc(O)ccc3[nH]2)CC1 10.1021/jm0341047
56835171 69397 0 None -1 9 Mouse 7.6 pKi = 7.6 Binding
Displacement of [3H]histamine from mouse H4RDisplacement of [3H]histamine from mouse H4R
ChEMBL 295 2 2 6 1.9 Nc1nc(N2CCNCC2)c2ccc(-c3ccco3)cc2n1 10.1016/j.bmcl.2011.10.104
CHEMBL1935574 69397 0 None -1 9 Mouse 7.6 pKi = 7.6 Binding
Displacement of [3H]histamine from mouse H4RDisplacement of [3H]histamine from mouse H4R
ChEMBL 295 2 2 6 1.9 Nc1nc(N2CCNCC2)c2ccc(-c3ccco3)cc2n1 10.1016/j.bmcl.2011.10.104
11687917 14796 0 None - 1 Human 7.6 pKi = 7.6 Binding
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 292 1 1 3 1.9 Cc1cc(Cl)c2nc(C(=O)N3CCN(C)CC3)[nH]c2c1 10.1021/jm0502081
CHEMBL120854 14796 0 None - 1 Human 7.6 pKi = 7.6 Binding
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 292 1 1 3 1.9 Cc1cc(Cl)c2nc(C(=O)N3CCN(C)CC3)[nH]c2c1 10.1021/jm0502081
10923241 18972 1 None - 1 Human 7.6 pKi = 7.6 Binding
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 259 1 2 3 1.3 CN1CCN(C(=O)c2cc3cc(O)ccc3[nH]2)CC1 10.1021/jm0502081
CHEMBL128958 18972 1 None - 1 Human 7.6 pKi = 7.6 Binding
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 259 1 2 3 1.3 CN1CCN(C(=O)c2cc3cc(O)ccc3[nH]2)CC1 10.1021/jm0502081
45257131 198226 0 None 18 2 Human 7.6 pKi = 7.6 Binding
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 312 4 2 6 1.7 Cc1ccccc1CNc1cc(N2CCN(C)CC2)nc(N)n1 10.1016/j.bmc.2009.08.059
CHEMBL594731 198226 0 None 18 2 Human 7.6 pKi = 7.6 Binding
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 312 4 2 6 1.7 Cc1ccccc1CNc1cc(N2CCN(C)CC2)nc(N)n1 10.1016/j.bmc.2009.08.059
57403350 67980 0 None 35 2 Human 7.6 pKi = 7.6 Binding
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 263 3 1 5 1.7 CN1CCN(c2cc(NCC(C)(C)C)ncn2)CC1 10.1016/j.bmcl.2011.07.114
CHEMBL1916498 67980 0 None 35 2 Human 7.6 pKi = 7.6 Binding
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 263 3 1 5 1.7 CN1CCN(c2cc(NCC(C)(C)C)ncn2)CC1 10.1016/j.bmcl.2011.07.114
24804058 143565 0 None - 1 Human 6.6 pKi = 6.6 Binding
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 424 7 2 5 5.1 Cc1c(F)ccc2[nH]c(-c3cnc(NCCCC4CCN(C)CC4)nc3C(C)C)nc12 nan
CHEMBL3903520 143565 0 None - 1 Human 6.6 pKi = 6.6 Binding
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 424 7 2 5 5.1 Cc1c(F)ccc2[nH]c(-c3cnc(NCCCC4CCN(C)CC4)nc3C(C)C)nc12 nan
126963284 144241 0 None - 1 Human 5.6 pKi = 5.6 Binding
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
CHEMBL3909134 144241 0 None - 1 Human 5.6 pKi = 5.6 Binding
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
46890675 7162 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 422 6 1 4 4.4 Cc1cc(OCCCN2CC3CCN(C)C3C2)ccc1-c1nc2c(C)c(F)ccc2[nH]1 10.1016/j.bmcl.2010.04.017
CHEMBL1085803 7162 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 422 6 1 4 4.4 Cc1cc(OCCCN2CC3CCN(C)C3C2)ccc1-c1nc2c(C)c(F)ccc2[nH]1 10.1016/j.bmcl.2010.04.017
49841722 69382 0 None - 1 Human 5.6 pKi = 5.6 Binding
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 344 2 1 6 2.5 CN1CCN(c2nc(N)nc3c(-c4ccc(C#N)cc4)cccc23)CC1 10.1016/j.bmcl.2011.10.104
CHEMBL1935559 69382 0 None - 1 Human 5.6 pKi = 5.6 Binding
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 344 2 1 6 2.5 CN1CCN(c2nc(N)nc3c(-c4ccc(C#N)cc4)cccc23)CC1 10.1016/j.bmcl.2011.10.104
168276867 192233 0 None -4 4 Human 5.6 pKi = 5.6 Binding
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 192233 0 None -4 4 Human 5.6 pKi = 5.6 Binding
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 192233 0 None -4 4 Human 5.6 pKi = 5.6 Binding
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
24853598 95776 0 None - 1 Human 5.6 pKi = 5.6 Binding
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 350 4 0 6 3.2 COc1ccc(Oc2nc3ccccc3nc2N2CCN(C)CC2)cc1 10.1021/jm7014217
CHEMBL260851 95776 0 None - 1 Human 5.6 pKi = 5.6 Binding
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 350 4 0 6 3.2 COc1ccc(Oc2nc3ccccc3nc2N2CCN(C)CC2)cc1 10.1021/jm7014217
24853596 95851 0 None - 1 Human 5.6 pKi = 5.6 Binding
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 354 3 0 5 3.8 CN1CCN(c2nc3ccccc3nc2Oc2ccc(Cl)cc2)CC1 10.1021/jm7014217
CHEMBL261225 95851 0 None - 1 Human 5.6 pKi = 5.6 Binding
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 354 3 0 5 3.8 CN1CCN(c2nc3ccccc3nc2Oc2ccc(Cl)cc2)CC1 10.1021/jm7014217
164610289 184550 0 None -38 4 Human 4.6 pKi = 4.6 Binding
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 438 7 4 4 3.5 Cc1nc(N)sc1CCCN/C(N)=N/C(=S)NC(c1ccccc1)c1ccccc1 10.1016/j.ejmech.2021.113190
CHEMBL4856602 184550 0 None -38 4 Human 4.6 pKi = 4.6 Binding
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 438 7 4 4 3.5 Cc1nc(N)sc1CCCN/C(N)=N/C(=S)NC(c1ccccc1)c1ccccc1 10.1016/j.ejmech.2021.113190
57399827 67984 0 None - 1 Human 6.6 pKi = 6.6 Binding
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 277 3 1 5 2.1 CN1CCCN(c2cc(NCC(C)(C)C)ncn2)CC1 10.1016/j.bmcl.2011.07.114
CHEMBL1916501 67984 0 None - 1 Human 6.6 pKi = 6.6 Binding
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 277 3 1 5 2.1 CN1CCCN(c2cc(NCC(C)(C)C)ncn2)CC1 10.1016/j.bmcl.2011.07.114
90645155 111690 0 None - 1 Human 5.6 pKi = 5.6 Binding
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 295 2 1 7 0.7 CN1CCN(c2nc(N)nc(-c3ccc(C#N)cc3)n2)CC1 10.1016/j.ejmech.2014.06.032
CHEMBL3290582 111690 0 None - 1 Human 5.6 pKi = 5.6 Binding
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 295 2 1 7 0.7 CN1CCN(c2nc(N)nc(-c3ccc(C#N)cc3)n2)CC1 10.1016/j.ejmech.2014.06.032
90645155 111690 0 None - 1 Human 5.6 pKi = 5.6 Binding
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 295 2 1 7 0.7 CN1CCN(c2nc(N)nc(-c3ccc(C#N)cc3)n2)CC1 10.1016/j.ejmech.2017.09.035
CHEMBL3290582 111690 0 None - 1 Human 5.6 pKi = 5.6 Binding
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 295 2 1 7 0.7 CN1CCN(c2nc(N)nc(-c3ccc(C#N)cc3)n2)CC1 10.1016/j.ejmech.2017.09.035
46228114 198492 0 None - 1 Human 6.6 pKi = 6.6 Binding
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 314 4 3 7 1.1 CN1CCN(c2cc(NCc3ccc(O)cc3)nc(N)n2)CC1 10.1016/j.bmc.2009.08.059
CHEMBL596551 198492 0 None - 1 Human 6.6 pKi = 6.6 Binding
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 314 4 3 7 1.1 CN1CCN(c2cc(NCc3ccc(O)cc3)nc(N)n2)CC1 10.1016/j.bmc.2009.08.059
25178131 186355 0 None - 1 Human 6.6 pKi = 6.6 Binding
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 381 5 1 5 3.7 CN1CCN(c2nc(NCCc3ccccc3)c3cc(Cl)ccc3n2)CC1 10.1021/jm800876b
CHEMBL490072 186355 0 None - 1 Human 6.6 pKi = 6.6 Binding
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 381 5 1 5 3.7 CN1CCN(c2nc(NCCc3ccccc3)c3cc(Cl)ccc3n2)CC1 10.1021/jm800876b
90645152 111687 0 None - 1 Human 5.6 pKi = 5.6 Binding
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 396 2 1 6 1.5 CN1CCN(c2nc(N)nc(-c3ccc(I)cc3)n2)CC1 10.1016/j.ejmech.2014.06.032
CHEMBL3290579 111687 0 None - 1 Human 5.6 pKi = 5.6 Binding
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 396 2 1 6 1.5 CN1CCN(c2nc(N)nc(-c3ccc(I)cc3)n2)CC1 10.1016/j.ejmech.2014.06.032
49818718 69387 0 None - 1 Human 7.6 pKi = 7.6 Binding
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 257 1 1 5 1.3 Cc1ccc2c(N3CCN(C)CC3)nc(N)nc2c1 10.1016/j.bmcl.2011.10.104
CHEMBL1935564 69387 0 None - 1 Human 7.6 pKi = 7.6 Binding
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 257 1 1 5 1.3 Cc1ccc2c(N3CCN(C)CC3)nc(N)nc2c1 10.1016/j.bmcl.2011.10.104
54582867 61230 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]histamine from human histamine H4 receptorDisplacement of [3H]histamine from human histamine H4 receptor
ChEMBL 264 3 1 6 0.7 CC(C)N(C)c1cc(N2CCN(C)CC2)nc(N)n1 10.1016/j.bmcl.2011.03.017
CHEMBL1770999 61230 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]histamine from human histamine H4 receptorDisplacement of [3H]histamine from human histamine H4 receptor
ChEMBL 264 3 1 6 0.7 CC(C)N(C)c1cc(N2CCN(C)CC2)nc(N)n1 10.1016/j.bmcl.2011.03.017
25147771 173666 0 None 1 3 Rat 7.6 pKi = 7.6 Binding
Binding affinity to rat histamine H4 receptorBinding affinity to rat histamine H4 receptor
ChEMBL 357 4 1 6 3.2 CN1CCN(c2nc(NCc3ccoc3)c3cc(Cl)ccc3n2)CC1 10.1021/jm800876b
CHEMBL454890 173666 0 None 1 3 Rat 7.6 pKi = 7.6 Binding
Binding affinity to rat histamine H4 receptorBinding affinity to rat histamine H4 receptor
ChEMBL 357 4 1 6 3.2 CN1CCN(c2nc(NCc3ccoc3)c3cc(Cl)ccc3n2)CC1 10.1021/jm800876b
11440060 205303 0 None - 1 Human 6.6 pKi = 6.6 Binding
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 368 8 1 2 5.4 c1ccc(C(OCCCc2c[nH]cn2)(c2ccccc2)c2ccccc2)cc1 10.1016/j.ejmech.2016.09.074
CHEMBL91576 205303 0 None - 1 Human 6.6 pKi = 6.6 Binding
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 368 8 1 2 5.4 c1ccc(C(OCCCc2c[nH]cn2)(c2ccccc2)c2ccccc2)cc1 10.1016/j.ejmech.2016.09.074
127051301 139670 0 None 5 2 Human 6.6 pKi = 6.6 Binding
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
CHEMBL3804906 139670 0 None 5 2 Human 6.6 pKi = 6.6 Binding
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
58227216 116638 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 261 4 2 5 1.6 CN[C@H]1CCN(c2cnnc(NC3CCCC3)c2)C1 10.1016/j.bmcl.2014.12.027
CHEMBL3393554 116638 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 261 4 2 5 1.6 CN[C@H]1CCN(c2cnnc(NC3CCCC3)c2)C1 10.1016/j.bmcl.2014.12.027
550981 68689 12 None 2 2 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation countingDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting
ChEMBL 280 5 2 3 2.9 OC(CNC1CC1)Cn1c2ccccc2c2ccccc21 10.1021/jm2011589
CHEMBL1923533 68689 12 None 2 2 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation countingDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting
ChEMBL 280 5 2 3 2.9 OC(CNC1CC1)Cn1c2ccccc2c2ccccc21 10.1021/jm2011589
24804056 150119 0 None - 1 Human 5.6 pKi = 5.6 Binding
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 420 8 2 5 5.1 CCCc1nc(NCCCC2CCN(C)CC2)ncc1-c1nc2c(C)c(C)ccc2[nH]1 nan
CHEMBL3955597 150119 0 None - 1 Human 5.6 pKi = 5.6 Binding
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 420 8 2 5 5.1 CCCc1nc(NCCCC2CCN(C)CC2)ncc1-c1nc2c(C)c(C)ccc2[nH]1 nan
71461658 78647 0 None - 1 Human 6.6 pKi = 6.6 Binding
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 259 1 2 4 0.5 CN1CCN(C(=O)c2nc3cc(N)ccc3[nH]2)CC1 10.1021/jm0502081
CHEMBL2113162 78647 0 None - 1 Human 6.6 pKi = 6.6 Binding
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 259 1 2 4 0.5 CN1CCN(C(=O)c2nc3cc(N)ccc3[nH]2)CC1 10.1021/jm0502081
4024 1984 14 None -301 2 Human 6.6 pKi = 6.6 Binding
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 159 2 1 2 1.4 n1ccc(cc1)Cc1c[nH]cn1 10.1021/jm049932u
9989505 1984 14 None -301 2 Human 6.6 pKi = 6.6 Binding
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 159 2 1 2 1.4 n1ccc(cc1)Cc1c[nH]cn1 10.1021/jm049932u
CHEMBL82298 1984 14 None -301 2 Human 6.6 pKi = 6.6 Binding
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 159 2 1 2 1.4 n1ccc(cc1)Cc1c[nH]cn1 10.1021/jm049932u
122193101 123402 0 None - 1 Human 5.6 pKi = 5.6 Binding
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 364 3 1 6 2.4 CN1CCN(c2nc(N)nc(/C=C/c3cccc(C(F)(F)F)c3)n2)CC1 10.1016/j.ejmech.2015.08.014
CHEMBL3628048 123402 0 None - 1 Human 5.6 pKi = 5.6 Binding
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 364 3 1 6 2.4 CN1CCN(c2nc(N)nc(/C=C/c3cccc(C(F)(F)F)c3)n2)CC1 10.1016/j.ejmech.2015.08.014
155546701 173083 0 None - 1 Human 6.6 pKi = 6.6 Binding
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 264 2 1 6 0.8 CN1CCN(c2nc(N)nc(CC(C)(C)C)n2)CC1 10.1016/j.bmc.2019.02.020
CHEMBL4534504 173083 0 None - 1 Human 6.6 pKi = 6.6 Binding
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 264 2 1 6 0.8 CN1CCN(c2nc(N)nc(CC(C)(C)C)n2)CC1 10.1016/j.bmc.2019.02.020
24798596 198185 2 None - 1 Human 6.6 pKi = 6.6 Binding
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 310 2 1 6 1.3 CN1CCN(c2cc(N3Cc4ccccc4C3)nc(N)n2)CC1 10.1016/j.bmc.2009.08.059
CHEMBL594491 198185 2 None - 1 Human 6.6 pKi = 6.6 Binding
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 310 2 1 6 1.3 CN1CCN(c2cc(N3Cc4ccccc4C3)nc(N)n2)CC1 10.1016/j.bmc.2009.08.059
21193534 11160 0 None -1 3 Human 7.6 pKi = 7.6 Binding
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 292 7 1 2 4.1 c1ccc(C(OCCCc2c[nH]cn2)c2ccccc2)cc1 10.1016/j.ejmech.2016.09.074
CHEMBL1179089 11160 0 None -1 3 Human 7.6 pKi = 7.6 Binding
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 292 7 1 2 4.1 c1ccc(C(OCCCc2c[nH]cn2)c2ccccc2)cc1 10.1016/j.ejmech.2016.09.074
CHEMBL59679 11160 0 None -1 3 Human 7.6 pKi = 7.6 Binding
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 292 7 1 2 4.1 c1ccc(C(OCCCc2c[nH]cn2)c2ccccc2)cc1 10.1016/j.ejmech.2016.09.074
54587789 61207 0 None - 1 Human 7.6 pKi = 7.6 Binding
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(NCCO)nc(N)n2)CC1 10.1016/j.bmcl.2011.03.017
CHEMBL1770976 61207 0 None - 1 Human 7.6 pKi = 7.6 Binding
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(NCCO)nc(N)n2)CC1 10.1016/j.bmcl.2011.03.017
45257131 198226 0 None 18 2 Human 7.6 pKi = 7.6 Binding
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 312 4 2 6 1.7 Cc1ccccc1CNc1cc(N2CCN(C)CC2)nc(N)n1 10.1016/j.bmc.2009.08.059
CHEMBL594731 198226 0 None 18 2 Human 7.6 pKi = 7.6 Binding
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 312 4 2 6 1.7 Cc1ccccc1CNc1cc(N2CCN(C)CC2)nc(N)n1 10.1016/j.bmc.2009.08.059
90655027 109638 0 None - 1 Human 7.6 pKi = 7.6 Binding
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
CHEMBL3236555 109638 0 None - 1 Human 7.6 pKi = 7.6 Binding
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
66740898 109645 0 None - 1 Human 7.6 pKi = 7.6 Binding
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 1 5 1.7 CN1C[C@H]2CN(c3cc(C4CCCC4)nc(N)n3)C[C@H]2C1 10.1021/jm401727m
CHEMBL3236562 109645 0 None - 1 Human 7.6 pKi = 7.6 Binding
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 1 5 1.7 CN1C[C@H]2CN(c3cc(C4CCCC4)nc(N)n3)C[C@H]2C1 10.1021/jm401727m
24826082 67799 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 377 2 2 6 3.0 CN[C@@H]1CCN(c2nc(N)nc3c2sc2cc(Br)ccc23)C1 10.1016/j.bmcl.2011.08.014
CHEMBL1914791 67799 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 377 2 2 6 3.0 CN[C@@H]1CCN(c2nc(N)nc3c2sc2cc(Br)ccc23)C1 10.1016/j.bmcl.2011.08.014
11587279 124531 3 None - 1 Human 7.6 pKi = 7.6 Binding
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 283 1 1 3 2.3 CN1CCN(C(=O)c2cc3cc(Cl)sc3[nH]2)CC1 10.1021/jm0502081
CHEMBL364400 124531 3 None - 1 Human 7.6 pKi = 7.6 Binding
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 283 1 1 3 2.3 CN1CCN(C(=O)c2cc3cc(Cl)sc3[nH]2)CC1 10.1021/jm0502081
1226 1988 16 None 2 6 Human 7.6 pKi = 7.6 Binding
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 321 9 4 4 1.2 NC(=NCCCc1cnc[nH]1)NCCSCc1nc[nH]c1C 10.1016/j.bmcl.2010.10.041
41376 1988 16 None 2 6 Human 7.6 pKi = 7.6 Binding
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 321 9 4 4 1.2 NC(=NCCCc1cnc[nH]1)NCCSCc1nc[nH]c1C 10.1016/j.bmcl.2010.10.041
CHEMBL12608 1988 16 None 2 6 Human 7.6 pKi = 7.6 Binding
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 321 9 4 4 1.2 NC(=NCCCc1cnc[nH]1)NCCSCc1nc[nH]c1C 10.1016/j.bmcl.2010.10.041
10105117 103718 0 None 1 2 Human 7.6 pKi = 7.6 Binding
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 226 6 3 2 1.6 CC/N=C(\S)NCCCCc1c[nH]cn1 10.1016/j.bmcl.2010.10.041
CHEMBL309819 103718 0 None 1 2 Human 7.6 pKi = 7.6 Binding
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 226 6 3 2 1.6 CC/N=C(\S)NCCCCc1c[nH]cn1 10.1016/j.bmcl.2010.10.041
10466840 202776 0 None -2 4 Human 7.6 pKi = 7.6 Binding
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 CC/N=C(\S)NCCCCCc1c[nH]cn1 10.1016/j.bmcl.2010.10.041
CHEMBL72424 202776 0 None -2 4 Human 7.6 pKi = 7.6 Binding
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 CC/N=C(\S)NCCCCCc1c[nH]cn1 10.1016/j.bmcl.2010.10.041
1204 1901 114 None -3 23 Human 7.6 pKi = 7.6 Binding
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 1901 114 None -3 23 Human 7.6 pKi = 7.6 Binding
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 1901 114 None -3 23 Human 7.6 pKi = 7.6 Binding
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 1901 114 None -3 23 Human 7.6 pKi = 7.6 Binding
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 1901 114 None -3 23 Human 7.6 pKi = 7.6 Binding
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 1901 114 None -3 23 Human 7.6 pKi = 7.6 Binding
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
71681476 89226 0 None - 1 Human 7.6 pKi = 7.6 Binding
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 316 8 4 8 1.5 CC(C)CCc1cc(NCCNc2ccnc(N)n2)nc(N)n1 10.1021/jm301886t
CHEMBL2375756 89226 0 None - 1 Human 7.6 pKi = 7.6 Binding
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 316 8 4 8 1.5 CC(C)CCc1cc(NCCNc2ccnc(N)n2)nc(N)n1 10.1021/jm301886t
4060730 19183 51 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]histamine displacement from human recombinant histamine H4 receptor expressed in SK-NM-C cells after 45 minsDisplacement of [3H]histamine displacement from human recombinant histamine H4 receptor expressed in SK-NM-C cells after 45 mins
ChEMBL 243 1 1 2 1.6 CN1CCN(C(=O)c2cc3ccccc3[nH]2)CC1 10.1021/jm301886t
CHEMBL129199 19183 51 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]histamine displacement from human recombinant histamine H4 receptor expressed in SK-NM-C cells after 45 minsDisplacement of [3H]histamine displacement from human recombinant histamine H4 receptor expressed in SK-NM-C cells after 45 mins
ChEMBL 243 1 1 2 1.6 CN1CCN(C(=O)c2cc3ccccc3[nH]2)CC1 10.1021/jm301886t
10923241 18972 1 None - 1 Human 7.6 pKi = 7.6 Binding
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 259 1 2 3 1.3 CN1CCN(C(=O)c2cc3cc(O)ccc3[nH]2)CC1 10.1016/j.ejmech.2012.06.016
CHEMBL128958 18972 1 None - 1 Human 7.6 pKi = 7.6 Binding
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 259 1 2 3 1.3 CN1CCN(C(=O)c2cc3cc(O)ccc3[nH]2)CC1 10.1016/j.ejmech.2012.06.016
4060730 19183 51 None - 1 Human 7.6 pKi = 7.6 Binding
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 243 1 1 2 1.6 CN1CCN(C(=O)c2cc3ccccc3[nH]2)CC1 10.1016/j.ejmech.2012.06.016
CHEMBL129199 19183 51 None - 1 Human 7.6 pKi = 7.6 Binding
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 243 1 1 2 1.6 CN1CCN(C(=O)c2cc3ccccc3[nH]2)CC1 10.1016/j.ejmech.2012.06.016
22660616 75295 0 None - 1 Human 7.6 pKi = 7.6 Binding
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 259 1 2 3 1.3 CN1CCN(C(=O)c2cc3ccc(O)cc3[nH]2)CC1 10.1016/j.ejmech.2012.06.016
CHEMBL2047273 75295 0 None - 1 Human 7.6 pKi = 7.6 Binding
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 259 1 2 3 1.3 CN1CCN(C(=O)c2cc3ccc(O)cc3[nH]2)CC1 10.1016/j.ejmech.2012.06.016
71525588 89300 0 None 33 2 Human 7.6 pKi = 7.6 Binding
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 272 3 2 6 1.1 CNC1CN(c2nc(N)nc3cc(C(C)C)cnc23)C1 10.1016/j.bmcl.2013.02.091
CHEMBL2376805 89300 0 None 33 2 Human 7.6 pKi = 7.6 Binding
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 272 3 2 6 1.1 CNC1CN(c2nc(N)nc3cc(C(C)C)cnc23)C1 10.1016/j.bmcl.2013.02.091
11846300 79856 3 None -2 4 Human 7.6 pKi = 7.6 Binding
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 327 0 0 4 3.8 CN1CCN(C2=Nc3ccc(Cl)cc3Oc3ccccc32)CC1 10.1021/jm7014217
CHEMBL213912 79856 3 None -2 4 Human 7.6 pKi = 7.6 Binding
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 327 0 0 4 3.8 CN1CCN(C2=Nc3ccc(Cl)cc3Oc3ccccc32)CC1 10.1021/jm7014217
45271470 193380 0 None -3 2 Human 7.6 pKi = 7.6 Binding
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 288 6 3 3 3.1 Cc1ccc(CNC(=N)SCCCc2c[nH]cn2)cc1 10.1016/j.bmc.2009.04.007
CHEMBL1202329 193380 0 None -3 2 Human 7.6 pKi = 7.6 Binding
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 288 6 3 3 3.1 Cc1ccc(CNC(=N)SCCCc2c[nH]cn2)cc1 10.1016/j.bmc.2009.04.007
CHEMBL549481 193380 0 None -3 2 Human 7.6 pKi = 7.6 Binding
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 288 6 3 3 3.1 Cc1ccc(CNC(=N)SCCCc2c[nH]cn2)cc1 10.1016/j.bmc.2009.04.007
45270644 193801 0 None 3 2 Human 7.6 pKi = 7.6 Binding
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 257 6 4 2 1.7 N=C(NCCCc1c[nH]cn1)NCc1ccccc1 10.1016/j.bmc.2009.04.007
CHEMBL552694 193801 0 None 3 2 Human 7.6 pKi = 7.6 Binding
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 257 6 4 2 1.7 N=C(NCCCc1c[nH]cn1)NCc1ccccc1 10.1016/j.bmc.2009.04.007
45271464 193831 0 None -5 2 Human 7.6 pKi = 7.6 Binding
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 292 6 3 3 2.9 N=C(NCc1ccc(F)cc1)SCCCc1c[nH]cn1 10.1016/j.bmc.2009.04.007
CHEMBL1202328 193831 0 None -5 2 Human 7.6 pKi = 7.6 Binding
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 292 6 3 3 2.9 N=C(NCc1ccc(F)cc1)SCCCc1c[nH]cn1 10.1016/j.bmc.2009.04.007
CHEMBL553455 193831 0 None -5 2 Human 7.6 pKi = 7.6 Binding
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 292 6 3 3 2.9 N=C(NCc1ccc(F)cc1)SCCCc1c[nH]cn1 10.1016/j.bmc.2009.04.007
10468601 193918 0 None -2 2 Human 7.6 pKi = 7.6 Binding
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 274 6 3 3 2.8 N=C(NCc1ccccc1)SCCCc1c[nH]cn1 10.1016/j.bmc.2009.04.007
CHEMBL1202324 193918 0 None -2 2 Human 7.6 pKi = 7.6 Binding
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 274 6 3 3 2.8 N=C(NCc1ccccc1)SCCCc1c[nH]cn1 10.1016/j.bmc.2009.04.007
CHEMBL555434 193918 0 None -2 2 Human 7.6 pKi = 7.6 Binding
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 274 6 3 3 2.8 N=C(NCc1ccccc1)SCCCc1c[nH]cn1 10.1016/j.bmc.2009.04.007
45268095 194366 0 None 1 2 Human 7.6 pKi = 7.6 Binding
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 378 9 3 3 4.8 N=C(NCCC(c1ccccc1)c1ccccc1)SCCCc1c[nH]cn1 10.1016/j.bmc.2009.04.007
CHEMBL1202323 194366 0 None 1 2 Human 7.6 pKi = 7.6 Binding
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 378 9 3 3 4.8 N=C(NCCC(c1ccccc1)c1ccccc1)SCCCc1c[nH]cn1 10.1016/j.bmc.2009.04.007
CHEMBL560313 194366 0 None 1 2 Human 7.6 pKi = 7.6 Binding
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 378 9 3 3 4.8 N=C(NCCC(c1ccccc1)c1ccccc1)SCCCc1c[nH]cn1 10.1016/j.bmc.2009.04.007
1204 1901 114 None -3 23 Human 7.6 pKi = 7.6 Binding
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 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.ejmech.2021.113190
1247 1901 114 None -3 23 Human 7.6 pKi = 7.6 Binding
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 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.ejmech.2021.113190
1375 1901 114 None -3 23 Human 7.6 pKi = 7.6 Binding
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 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.ejmech.2021.113190
774 1901 114 None -3 23 Human 7.6 pKi = 7.6 Binding
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 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.ejmech.2021.113190
CHEMBL90 1901 114 None -3 23 Human 7.6 pKi = 7.6 Binding
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 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.ejmech.2021.113190
DB05381 1901 114 None -3 23 Human 7.6 pKi = 7.6 Binding
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 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.ejmech.2021.113190
1274 4001 12 None 19 2 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]histamine from wild type human histamine H4 receptor transfected in HEK293T cells after 1 hr by liquid scintillation counting analysisDisplacement of [3H]histamine from wild type human histamine H4 receptor transfected in HEK293T cells after 1 hr by liquid scintillation counting analysis
ChEMBL 161 3 4 3 -1.1 NC(=N)SCCN=C(N)N 10.1039/C2MD20212C
3063228 4001 12 None 19 2 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]histamine from wild type human histamine H4 receptor transfected in HEK293T cells after 1 hr by liquid scintillation counting analysisDisplacement of [3H]histamine from wild type human histamine H4 receptor transfected in HEK293T cells after 1 hr by liquid scintillation counting analysis
ChEMBL 161 3 4 3 -1.1 NC(=N)SCCN=C(N)N 10.1039/C2MD20212C
CHEMBL1196470 4001 12 None 19 2 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]histamine from wild type human histamine H4 receptor transfected in HEK293T cells after 1 hr by liquid scintillation counting analysisDisplacement of [3H]histamine from wild type human histamine H4 receptor transfected in HEK293T cells after 1 hr by liquid scintillation counting analysis
ChEMBL 161 3 4 3 -1.1 NC(=N)SCCN=C(N)N 10.1039/C2MD20212C
10988959 117605 4 None - 1 Human 7.6 pKi = 7.6 Binding
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 258 1 2 3 1.1 CN1CCN(C(=O)c2cc3cc(N)ccc3[nH]2)CC1 10.1039/C2MD20212C
CHEMBL340740 117605 4 None - 1 Human 7.6 pKi = 7.6 Binding
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 258 1 2 3 1.1 CN1CCN(C(=O)c2cc3cc(N)ccc3[nH]2)CC1 10.1039/C2MD20212C
21638785 188073 4 None -4 2 Human 7.6 pKi = 7.6 Binding
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 263 1 2 2 1.9 O=C(c1cc2cc(Cl)ccc2[nH]1)N1CCNCC1 10.1021/jm800670r
CHEMBL503605 188073 4 None -4 2 Human 7.6 pKi = 7.6 Binding
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 263 1 2 2 1.9 O=C(c1cc2cc(Cl)ccc2[nH]1)N1CCNCC1 10.1021/jm800670r
127052294 139772 0 None 5 4 Human 6.6 pKi = 6.6 Binding
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
CHEMBL3806079 139772 0 None 5 4 Human 6.6 pKi = 6.6 Binding
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
11751419 137355 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 454 7 1 4 5.6 CN(C)C1CCN(CCCOc2ccc(-c3nc4cc(C(C)(C)C)ccc4[nH]3)cc2Cl)C1 10.1016/j.bmcl.2010.04.017
CHEMBL376268 137355 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 454 7 1 4 5.6 CN(C)C1CCN(CCCOc2ccc(-c3nc4cc(C(C)(C)C)ccc4[nH]3)cc2Cl)C1 10.1016/j.bmcl.2010.04.017
11751419 137355 0 None - 1 Human 6.6 pKi = 6.6 Binding
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 454 7 1 4 5.6 CN(C)C1CCN(CCCOc2ccc(-c3nc4cc(C(C)(C)C)ccc4[nH]3)cc2Cl)C1 10.1016/j.bmcl.2006.08.117
CHEMBL376268 137355 0 None - 1 Human 6.6 pKi = 6.6 Binding
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 454 7 1 4 5.6 CN(C)C1CCN(CCCOc2ccc(-c3nc4cc(C(C)(C)C)ccc4[nH]3)cc2Cl)C1 10.1016/j.bmcl.2006.08.117
57402512 67825 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 329 3 2 7 2.2 CN[C@H]1CCN(c2nc(N)nc3c2sc2cc(OC)ccc23)C1 10.1016/j.bmcl.2011.08.014
CHEMBL1915022 67825 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 329 3 2 7 2.2 CN[C@H]1CCN(c2nc(N)nc3c2sc2cc(OC)ccc23)C1 10.1016/j.bmcl.2011.08.014
46228092 198266 0 None - 1 Human 5.6 pKi = 5.6 Binding
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 299 4 1 6 1.4 CN1CCN(c2cc(OCc3ccccc3)nc(N)n2)CC1 10.1016/j.bmc.2009.08.059
CHEMBL594973 198266 0 None - 1 Human 5.6 pKi = 5.6 Binding
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 299 4 1 6 1.4 CN1CCN(c2cc(OCc3ccccc3)nc(N)n2)CC1 10.1016/j.bmc.2009.08.059
4024 1984 14 None -301 2 Human 6.6 pKi = 6.6 Binding
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 159 2 1 2 1.4 n1ccc(cc1)Cc1c[nH]cn1 10.1016/j.bmcl.2010.10.041
9989505 1984 14 None -301 2 Human 6.6 pKi = 6.6 Binding
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 159 2 1 2 1.4 n1ccc(cc1)Cc1c[nH]cn1 10.1016/j.bmcl.2010.10.041
CHEMBL82298 1984 14 None -301 2 Human 6.6 pKi = 6.6 Binding
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 159 2 1 2 1.4 n1ccc(cc1)Cc1c[nH]cn1 10.1016/j.bmcl.2010.10.041
1252 1986 16 None -100 4 Human 6.6 pKi = 6.6 Binding
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 153 5 2 2 1.1 NCCCCCc1cnc[nH]1 10.1016/j.bmcl.2010.10.041
9793868 1986 16 None -100 4 Human 6.6 pKi = 6.6 Binding
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 153 5 2 2 1.1 NCCCCCc1cnc[nH]1 10.1016/j.bmcl.2010.10.041
CHEMBL417096 1986 16 None -100 4 Human 6.6 pKi = 6.6 Binding
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 153 5 2 2 1.1 NCCCCCc1cnc[nH]1 10.1016/j.bmcl.2010.10.041
1236 2036 23 None -204 7 Human 6.6 pKi = 6.6 Binding
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 125 2 2 2 0.3 C[C@H](Cc1cnc[nH]1)N 10.1016/j.bmcl.2010.10.041
1237 2036 23 None -204 7 Human 6.6 pKi = 6.6 Binding
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 125 2 2 2 0.3 C[C@H](Cc1cnc[nH]1)N 10.1016/j.bmcl.2010.10.041
156615 2036 23 None -204 7 Human 6.6 pKi = 6.6 Binding
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 125 2 2 2 0.3 C[C@H](Cc1cnc[nH]1)N 10.1016/j.bmcl.2010.10.041
CHEMBL268229 2036 23 None -204 7 Human 6.6 pKi = 6.6 Binding
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 125 2 2 2 0.3 C[C@H](Cc1cnc[nH]1)N 10.1016/j.bmcl.2010.10.041
1252 1986 16 None -100 4 Human 6.6 pKi = 6.6 Binding
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 153 5 2 2 1.1 NCCCCCc1cnc[nH]1 10.1021/jm0504353
9793868 1986 16 None -100 4 Human 6.6 pKi = 6.6 Binding
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 153 5 2 2 1.1 NCCCCCc1cnc[nH]1 10.1021/jm0504353
CHEMBL417096 1986 16 None -100 4 Human 6.6 pKi = 6.6 Binding
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 153 5 2 2 1.1 NCCCCCc1cnc[nH]1 10.1021/jm0504353
81371 12661 11 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]histamine from human histamine H4 receptorDisplacement of [3H]histamine from human histamine H4 receptor
ChEMBL 178 3 4 4 0.2 N=C(N)SCCSC(=N)N 10.1021/jm060880d
CHEMBL1187946 12661 11 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]histamine from human histamine H4 receptorDisplacement of [3H]histamine from human histamine H4 receptor
ChEMBL 178 3 4 4 0.2 N=C(N)SCCSC(=N)N 10.1021/jm060880d
CHEMBL534494 12661 11 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]histamine from human histamine H4 receptorDisplacement of [3H]histamine from human histamine H4 receptor
ChEMBL 178 3 4 4 0.2 N=C(N)SCCSC(=N)N 10.1021/jm060880d
52128564 75281 2 None - 1 Human 6.6 pKi = 6.6 Binding
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 278 1 0 3 2.5 CN1CCN(C(=O)c2cc3cc(Cl)ccc3o2)CC1 10.1016/j.ejmech.2012.06.016
CHEMBL2047259 75281 2 None - 1 Human 6.6 pKi = 6.6 Binding
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 278 1 0 3 2.5 CN1CCN(C(=O)c2cc3cc(Cl)ccc3o2)CC1 10.1016/j.ejmech.2012.06.016
70684084 75317 0 None - 1 Human 6.6 pKi = 6.6 Binding
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 291 2 2 2 2.6 CN[C@@H]1CCN(C(=O)c2cc3cc(Cl)cc(C)c3[nH]2)C1 10.1016/j.ejmech.2012.06.016
CHEMBL2047452 75317 0 None - 1 Human 6.6 pKi = 6.6 Binding
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 291 2 2 2 2.6 CN[C@@H]1CCN(C(=O)c2cc3cc(Cl)cc(C)c3[nH]2)C1 10.1016/j.ejmech.2012.06.016
70692528 75323 2 None - 1 Human 6.6 pKi = 6.6 Binding
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 275 1 1 2 2.1 CN1CCCN(C(=O)c2cc3c(F)cccc3[nH]2)CC1 10.1016/j.ejmech.2012.06.016
CHEMBL2047458 75323 2 None - 1 Human 6.6 pKi = 6.6 Binding
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 275 1 1 2 2.1 CN1CCCN(C(=O)c2cc3c(F)cccc3[nH]2)CC1 10.1016/j.ejmech.2012.06.016
70686224 75337 0 None - 1 Human 6.6 pKi = 6.6 Binding
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 295 2 2 2 2.4 CN[C@@H]1CCN(C(=O)c2cc3cc(Cl)cc(F)c3[nH]2)C1 10.1016/j.ejmech.2012.06.016
CHEMBL2047472 75337 0 None - 1 Human 6.6 pKi = 6.6 Binding
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 295 2 2 2 2.4 CN[C@@H]1CCN(C(=O)c2cc3cc(Cl)cc(F)c3[nH]2)C1 10.1016/j.ejmech.2012.06.016
51355156 58602 0 None - 1 Human 6.6 pKi = 6.6 Binding
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 3.1 c1nc(CCCc2cn(C3CCCCCC3)nn2)c[nH]1 10.1021/jm1013488
CHEMBL1688989 58602 0 None - 1 Human 6.6 pKi = 6.6 Binding
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 3.1 c1nc(CCCc2cn(C3CCCCCC3)nn2)c[nH]1 10.1021/jm1013488
9990475 56183 0 None 3 3 Human 5.6 pKi = 5.6 Binding
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 205 2 2 3 -0.5 Cc1nc(N)[se]c1CCN 10.1016/j.bmcl.2010.10.041
CHEMBL1632408 56183 0 None 3 3 Human 5.6 pKi = 5.6 Binding
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 205 2 2 3 -0.5 Cc1nc(N)[se]c1CCN 10.1016/j.bmcl.2010.10.041
CHEMBL2448450 56183 0 None 3 3 Human 5.6 pKi = 5.6 Binding
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 205 2 2 3 -0.5 Cc1nc(N)[se]c1CCN 10.1016/j.bmcl.2010.10.041
10583206 108872 0 None -1 2 Human 5.6 pKi = 5.6 Binding
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 167 2 2 3 0.6 NC[C@@H]1CC[C@H](c2c[nH]cn2)O1 10.1016/j.bmcl.2010.10.041
CHEMBL321920 108872 0 None -1 2 Human 5.6 pKi = 5.6 Binding
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 167 2 2 3 0.6 NC[C@@H]1CC[C@H](c2c[nH]cn2)O1 10.1016/j.bmcl.2010.10.041
71681640 89233 0 None - 1 Human 5.6 pKi = 5.6 Binding
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 356 6 4 8 2.3 Nc1nc(Cl)cc(NCCNc2cc(-c3ccccc3)nc(N)n2)n1 10.1021/jm301886t
CHEMBL2375763 89233 0 None - 1 Human 5.6 pKi = 5.6 Binding
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 356 6 4 8 2.3 Nc1nc(Cl)cc(NCCNc2cc(-c3ccccc3)nc(N)n2)n1 10.1021/jm301886t
12438303 75280 2 None - 1 Human 5.6 pKi = 5.6 Binding
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 260 1 0 3 2.3 CN1CCN(C(=O)c2cc3ccccc3s2)CC1 10.1016/j.ejmech.2012.06.016
CHEMBL2047258 75280 2 None - 1 Human 5.6 pKi = 5.6 Binding
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 260 1 0 3 2.3 CN1CCN(C(=O)c2cc3ccccc3s2)CC1 10.1016/j.ejmech.2012.06.016
22660598 75305 1 None - 1 Human 5.6 pKi = 5.6 Binding
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 COc1cccc2cc(C(=O)N3CCN(C)CC3)[nH]c12 10.1016/j.ejmech.2012.06.016
CHEMBL2047440 75305 1 None - 1 Human 5.6 pKi = 5.6 Binding
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 COc1cccc2cc(C(=O)N3CCN(C)CC3)[nH]c12 10.1016/j.ejmech.2012.06.016
24854636 155776 0 None - 1 Human 5.6 pKi = 5.6 Binding
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 296 1 0 4 2.4 CN1CCN(c2nc3ccccc3nc2C(F)(F)F)CC1 10.1021/jm7014217
CHEMBL406558 155776 0 None - 1 Human 5.6 pKi = 5.6 Binding
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 296 1 0 4 2.4 CN1CCN(c2nc3ccccc3nc2C(F)(F)F)CC1 10.1021/jm7014217
10583206 108872 0 None -1 2 Human 5.6 pKi = 5.6 Binding
Histamine H4 receptor competition binding using [3H]Na-methylhistamineHistamine H4 receptor competition binding using [3H]Na-methylhistamine
ChEMBL 167 2 2 3 0.6 NC[C@@H]1CC[C@H](c2c[nH]cn2)O1 10.1021/jm0300025
CHEMBL321920 108872 0 None -1 2 Human 5.6 pKi = 5.6 Binding
Histamine H4 receptor competition binding using [3H]Na-methylhistamineHistamine H4 receptor competition binding using [3H]Na-methylhistamine
ChEMBL 167 2 2 3 0.6 NC[C@@H]1CC[C@H](c2c[nH]cn2)O1 10.1021/jm0300025
44395263 66370 0 None - 1 Human 4.6 pKi = 4.6 Binding
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 292 2 2 3 1.7 CN1CCN(NC(=O)c2cc3cc(Cl)ccc3[nH]2)CC1 10.1016/j.bmcl.2004.08.035
CHEMBL185546 66370 0 None - 1 Human 4.6 pKi = 4.6 Binding
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 292 2 2 3 1.7 CN1CCN(NC(=O)c2cc3cc(Cl)ccc3[nH]2)CC1 10.1016/j.bmcl.2004.08.035
44395336 66457 0 None - 1 Human 4.6 pKi = 4.6 Binding
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 280 4 1 3 1.9 CN(C)CCN(C)C(=O)c1nc2cc(Cl)ccc2[nH]1 10.1016/j.bmcl.2004.08.035
CHEMBL185948 66457 0 None - 1 Human 4.6 pKi = 4.6 Binding
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 280 4 1 3 1.9 CN(C)CCN(C)C(=O)c1nc2cc(Cl)ccc2[nH]1 10.1016/j.bmcl.2004.08.035
44395290 124997 0 None - 1 Human 4.6 pKi = 4.6 Binding
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 279 4 1 2 2.5 CN(C)CCN(C)C(=O)c1cc2cc(Cl)ccc2[nH]1 10.1016/j.bmcl.2004.08.035
CHEMBL364629 124997 0 None - 1 Human 4.6 pKi = 4.6 Binding
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 279 4 1 2 2.5 CN(C)CCN(C)C(=O)c1cc2cc(Cl)ccc2[nH]1 10.1016/j.bmcl.2004.08.035
15984057 139591 0 None -35481 3 Human 4.6 pKi = 4.6 Binding
Displacement of [3H]RAMHA from human histamine H4 receptor expressed in SK-N-MC cellsDisplacement of [3H]RAMHA from human histamine H4 receptor expressed in SK-N-MC cells
ChEMBL 348 5 0 2 5.3 c1cc(-c2ccc(CN3CCCCC3)cc2)ccc1CN1CCCCC1 10.1016/j.bmc.2008.10.029
CHEMBL380101 139591 0 None -35481 3 Human 4.6 pKi = 4.6 Binding
Displacement of [3H]RAMHA from human histamine H4 receptor expressed in SK-N-MC cellsDisplacement of [3H]RAMHA from human histamine H4 receptor expressed in SK-N-MC cells
ChEMBL 348 5 0 2 5.3 c1cc(-c2ccc(CN3CCCCC3)cc2)ccc1CN1CCCCC1 10.1016/j.bmc.2008.10.029
71519348 86063 0 None - 1 Human 4.6 pKi = 4.6 Binding
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 308 3 2 6 1.5 Nc1nc(N2CCNCC2)c2ccn(Cc3ccccc3)c2n1 10.1016/j.bmcl.2012.10.139
CHEMBL2314766 86063 0 None - 1 Human 4.6 pKi = 4.6 Binding
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 308 3 2 6 1.5 Nc1nc(N2CCNCC2)c2ccn(Cc3ccccc3)c2n1 10.1016/j.bmcl.2012.10.139
122193106 123406 0 None - 1 Human 5.6 pKi = 5.6 Binding
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 335 3 2 6 1.9 CN1CCN(c2nc(N)nc(/C=C/c3c[nH]c4ccccc34)n2)CC1 10.1016/j.ejmech.2015.08.014
CHEMBL3628052 123406 0 None - 1 Human 5.6 pKi = 5.6 Binding
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 335 3 2 6 1.9 CN1CCN(c2nc(N)nc(/C=C/c3c[nH]c4ccccc34)n2)CC1 10.1016/j.ejmech.2015.08.014
122193095 123396 0 None 3 2 Human 6.6 pKi = 6.6 Binding
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 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 123396 0 None 3 2 Human 6.6 pKi = 6.6 Binding
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 330 3 1 6 2.0 CN1CCN(c2nc(N)nc(/C=C/c3cccc(Cl)c3)n2)CC1 10.1016/j.ejmech.2015.08.014
54585776 61192 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]histamine from human histamine H4 receptorDisplacement of [3H]histamine from human histamine H4 receptor
ChEMBL 252 5 4 7 -0.7 CN[C@@H]1CCN(c2cc(N)nc(NCCO)n2)C1 10.1016/j.bmcl.2011.03.017
CHEMBL1770961 61192 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]histamine from human histamine H4 receptorDisplacement of [3H]histamine from human histamine H4 receptor
ChEMBL 252 5 4 7 -0.7 CN[C@@H]1CCN(c2cc(N)nc(NCCO)n2)C1 10.1016/j.bmcl.2011.03.017
24994630 109642 0 None - 1 Human 6.6 pKi = 6.6 Binding
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 2 5 1.6 Nc1nc(C2CCCC2)cc(N2CCC[C@@H](N)C2)n1 10.1021/jm401727m
CHEMBL3236559 109642 0 None - 1 Human 6.6 pKi = 6.6 Binding
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 2 5 1.6 Nc1nc(C2CCCC2)cc(N2CCC[C@@H](N)C2)n1 10.1021/jm401727m
25178933 186354 0 None - 1 Human 6.6 pKi = 6.6 Binding
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 367 4 1 5 3.6 CN1CCN(c2nc(NCc3ccccc3)c3cc(Cl)ccc3n2)CC1 10.1021/jm800876b
CHEMBL490071 186354 0 None - 1 Human 6.6 pKi = 6.6 Binding
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 367 4 1 5 3.6 CN1CCN(c2nc(NCc3ccccc3)c3cc(Cl)ccc3n2)CC1 10.1021/jm800876b
25178933 186354 0 None - 1 Human 6.6 pKi = 6.6 Binding
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 367 4 1 5 3.6 CN1CCN(c2nc(NCc3ccccc3)c3cc(Cl)ccc3n2)CC1 10.1021/jm901379s
CHEMBL490071 186354 0 None - 1 Human 6.6 pKi = 6.6 Binding
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 367 4 1 5 3.6 CN1CCN(c2nc(NCc3ccccc3)c3cc(Cl)ccc3n2)CC1 10.1021/jm901379s
122193103 123404 0 None - 1 Human 5.6 pKi = 5.6 Binding
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 341 4 1 8 1.3 CN1CCN(c2nc(N)nc(/C=C/c3cccc([N+](=O)[O-])c3)n2)CC1 10.1016/j.ejmech.2015.08.014
CHEMBL3628050 123404 0 None - 1 Human 5.6 pKi = 5.6 Binding
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 341 4 1 8 1.3 CN1CCN(c2nc(N)nc(/C=C/c3cccc([N+](=O)[O-])c3)n2)CC1 10.1016/j.ejmech.2015.08.014
10446295 2101 29 None 269 2 Human 7.6 pKi = 7.6 Binding
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 278 1 1 3 1.6 CN1CCN(CC1)C(=O)c1nc2c([nH]1)cc(cc2)Cl 10.1016/j.bmcl.2011.10.104
1277 2101 29 None 269 2 Human 7.6 pKi = 7.6 Binding
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 278 1 1 3 1.6 CN1CCN(CC1)C(=O)c1nc2c([nH]1)cc(cc2)Cl 10.1016/j.bmcl.2011.10.104
CHEMBL185951 2101 29 None 269 2 Human 7.6 pKi = 7.6 Binding
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 278 1 1 3 1.6 CN1CCN(CC1)C(=O)c1nc2c([nH]1)cc(cc2)Cl 10.1016/j.bmcl.2011.10.104
10446295 2101 29 None 269 2 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]histamine from human histamine H4 receptorDisplacement of [3H]histamine from human histamine H4 receptor
ChEMBL 278 1 1 3 1.6 CN1CCN(CC1)C(=O)c1nc2c([nH]1)cc(cc2)Cl 10.1016/j.bmcl.2011.03.017
1277 2101 29 None 269 2 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]histamine from human histamine H4 receptorDisplacement of [3H]histamine from human histamine H4 receptor
ChEMBL 278 1 1 3 1.6 CN1CCN(CC1)C(=O)c1nc2c([nH]1)cc(cc2)Cl 10.1016/j.bmcl.2011.03.017
CHEMBL185951 2101 29 None 269 2 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]histamine from human histamine H4 receptorDisplacement of [3H]histamine from human histamine H4 receptor
ChEMBL 278 1 1 3 1.6 CN1CCN(CC1)C(=O)c1nc2c([nH]1)cc(cc2)Cl 10.1016/j.bmcl.2011.03.017
46890627 6511 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
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 6511 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 408 6 2 4 4.0 Cc1cc(OCCCN2CC3CCNC3C2)ccc1-c1nc2c(C)c(F)ccc2[nH]1 10.1016/j.bmcl.2010.04.017
11340020 83847 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 454 6 1 4 5.6 CN1CCCN(CCCOc2ccc(-c3nc4cc(C(C)(C)C)ccc4[nH]3)cc2Cl)CC1 10.1016/j.bmcl.2010.04.017
CHEMBL221210 83847 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 454 6 1 4 5.6 CN1CCCN(CCCOc2ccc(-c3nc4cc(C(C)(C)C)ccc4[nH]3)cc2Cl)CC1 10.1016/j.bmcl.2010.04.017
136042265 69567 0 None - 1 Human 7.6 pKi = 7.6 Binding
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 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 69567 0 None - 1 Human 7.6 pKi = 7.6 Binding
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 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
11340020 83847 0 None - 1 Human 7.6 pKi = 7.6 Binding
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 454 6 1 4 5.6 CN1CCCN(CCCOc2ccc(-c3nc4cc(C(C)(C)C)ccc4[nH]3)cc2Cl)CC1 10.1016/j.bmcl.2006.08.117
CHEMBL221210 83847 0 None - 1 Human 7.6 pKi = 7.6 Binding
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 454 6 1 4 5.6 CN1CCCN(CCCOc2ccc(-c3nc4cc(C(C)(C)C)ccc4[nH]3)cc2Cl)CC1 10.1016/j.bmcl.2006.08.117
11189343 141445 0 None - 1 Human 7.6 pKi = 7.6 Binding
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 420 6 1 4 4.9 Cc1cc(-c2nc3cc(C(C)(C)C)ccc3[nH]2)ccc1OCCCN1CCN(C)CC1 10.1016/j.bmcl.2006.08.117
CHEMBL387342 141445 0 None - 1 Human 7.6 pKi = 7.6 Binding
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 420 6 1 4 4.9 Cc1cc(-c2nc3cc(C(C)(C)C)ccc3[nH]2)ccc1OCCCN1CCN(C)CC1 10.1016/j.bmcl.2006.08.117
57394549 67757 0 None - 1 Human 7.6 pKi = 7.6 Binding
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
CHEMBL1914748 67757 0 None - 1 Human 7.6 pKi = 7.6 Binding
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
10446295 2101 29 None 269 2 Human 7.6 pKi = 7.6 Binding
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 278 1 1 3 1.6 CN1CCN(CC1)C(=O)c1nc2c([nH]1)cc(cc2)Cl 10.1021/jm0502081
1277 2101 29 None 269 2 Human 7.6 pKi = 7.6 Binding
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 278 1 1 3 1.6 CN1CCN(CC1)C(=O)c1nc2c([nH]1)cc(cc2)Cl 10.1021/jm0502081
CHEMBL185951 2101 29 None 269 2 Human 7.6 pKi = 7.6 Binding
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 278 1 1 3 1.6 CN1CCN(CC1)C(=O)c1nc2c([nH]1)cc(cc2)Cl 10.1021/jm0502081
24759624 95686 0 None - 1 Human 7.6 pKi = 7.6 Binding
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 292 2 0 5 2.0 COc1nc2cc(Cl)ccc2nc1N1CCN(C)CC1 10.1021/jm7014217
CHEMBL260444 95686 0 None - 1 Human 7.6 pKi = 7.6 Binding
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 292 2 0 5 2.0 COc1nc2cc(Cl)ccc2nc1N1CCN(C)CC1 10.1021/jm7014217
25147771 173666 0 None -1 3 Human 7.6 pKi = 7.6 Binding
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 357 4 1 6 3.2 CN1CCN(c2nc(NCc3ccoc3)c3cc(Cl)ccc3n2)CC1 10.1021/jm800876b
CHEMBL454890 173666 0 None -1 3 Human 7.6 pKi = 7.6 Binding
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 357 4 1 6 3.2 CN1CCN(c2nc(NCc3ccoc3)c3cc(Cl)ccc3n2)CC1 10.1021/jm800876b
44129211 199290 0 None - 1 Human 7.6 pKi = 7.6 Binding
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 383 5 1 7 1.5 CN1CCN(c2nc(NCCS(C)(=O)=O)c3cc(Cl)ccc3n2)CC1 10.1021/jm901379s
CHEMBL601946 199290 0 None - 1 Human 7.6 pKi = 7.6 Binding
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 383 5 1 7 1.5 CN1CCN(c2nc(NCCS(C)(=O)=O)c3cc(Cl)ccc3n2)CC1 10.1021/jm901379s
11821243 18664 8 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]- histamine from the recombinant human histamine H4 receptorDisplacement of [3H]- histamine from the recombinant human histamine H4 receptor
ChEMBL 257 2 1 2 1.9 CCN1CCN(C(=O)c2cc3ccccc3[nH]2)CC1 10.1021/jm0341047
CHEMBL128134 18664 8 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]- histamine from the recombinant human histamine H4 receptorDisplacement of [3H]- histamine from the recombinant human histamine H4 receptor
ChEMBL 257 2 1 2 1.9 CCN1CCN(C(=O)c2cc3ccccc3[nH]2)CC1 10.1021/jm0341047
155549319 175750 0 None 1 2 Human 5.6 pKi = 5.6 Binding
Displacement of 40 nM [3H]-histamine from human H4R expressed in Sf9 cell membranes co-expressing Gia2 and beta1gamma2 by competition binding assayDisplacement of 40 nM [3H]-histamine from human H4R expressed in Sf9 cell membranes co-expressing Gia2 and beta1gamma2 by competition binding assay
ChEMBL 305 5 2 5 2.0 CCC(=O)N[C@@H]1CCN(c2ccnc(NCC(C)(C)C)n2)C1 10.1021/acs.jmedchem.9b01342
CHEMBL4538671 175750 0 None 1 2 Human 5.6 pKi = 5.6 Binding
Displacement of 40 nM [3H]-histamine from human H4R expressed in Sf9 cell membranes co-expressing Gia2 and beta1gamma2 by competition binding assayDisplacement of 40 nM [3H]-histamine from human H4R expressed in Sf9 cell membranes co-expressing Gia2 and beta1gamma2 by competition binding assay
ChEMBL 305 5 2 5 2.0 CCC(=O)N[C@@H]1CCN(c2ccnc(NCC(C)(C)C)n2)C1 10.1021/acs.jmedchem.9b01342
CHEMBL4595399 175750 0 None 1 2 Human 5.6 pKi = 5.6 Binding
Displacement of 40 nM [3H]-histamine from human H4R expressed in Sf9 cell membranes co-expressing Gia2 and beta1gamma2 by competition binding assayDisplacement of 40 nM [3H]-histamine from human H4R expressed in Sf9 cell membranes co-expressing Gia2 and beta1gamma2 by competition binding assay
ChEMBL 305 5 2 5 2.0 CCC(=O)N[C@@H]1CCN(c2ccnc(NCC(C)(C)C)n2)C1 10.1021/acs.jmedchem.9b01342
164620704 185501 0 None -17 4 Human 5.6 pKi = 5.6 Binding
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 416 8 4 4 3.5 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCC(C)c1ccc(C(C)C)cc1 10.1016/j.ejmech.2021.113190
CHEMBL4871482 185501 0 None -17 4 Human 5.6 pKi = 5.6 Binding
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 416 8 4 4 3.5 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCC(C)c1ccc(C(C)C)cc1 10.1016/j.ejmech.2021.113190
127026016 136964 0 None -13 2 Human 4.6 pKi = 4.6 Binding
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 385 4 1 5 3.6 CN1CCN(c2nc(NCc3ccccc3)nc3c2-c2ccccc2CC3)CC1 10.1016/j.bmcl.2015.12.035
CHEMBL3753967 136964 0 None -13 2 Human 4.6 pKi = 4.6 Binding
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 385 4 1 5 3.6 CN1CCN(c2nc(NCc3ccccc3)nc3c2-c2ccccc2CC3)CC1 10.1016/j.bmcl.2015.12.035
71518861 86070 0 None - 1 Human 5.6 pKi = 5.6 Binding
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 326 2 2 5 2.1 CN1CCN(c2nc(N)nc3[nH]c(-c4ccc(F)cc4)cc23)CC1 10.1016/j.bmcl.2012.10.139
CHEMBL2314774 86070 0 None - 1 Human 5.6 pKi = 5.6 Binding
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 326 2 2 5 2.1 CN1CCN(c2nc(N)nc3[nH]c(-c4ccc(F)cc4)cc23)CC1 10.1016/j.bmcl.2012.10.139
122193102 123403 0 None - 1 Human 5.6 pKi = 5.6 Binding
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 321 3 1 7 1.2 CN1CCN(c2nc(N)nc(/C=C/c3cccc(C#N)c3)n2)CC1 10.1016/j.ejmech.2015.08.014
CHEMBL3628049 123403 0 None - 1 Human 5.6 pKi = 5.6 Binding
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 321 3 1 7 1.2 CN1CCN(c2nc(N)nc(/C=C/c3cccc(C#N)c3)n2)CC1 10.1016/j.ejmech.2015.08.014
63868018 174804 2 None - 1 Human 5.6 pKi = 5.6 Binding
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 208 1 1 6 -0.5 Cc1nc(N)nc(N2CCN(C)CC2)n1 10.1016/j.bmc.2019.02.020
CHEMBL4574940 174804 2 None - 1 Human 5.6 pKi = 5.6 Binding
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 208 1 1 6 -0.5 Cc1nc(N)nc(N2CCN(C)CC2)n1 10.1016/j.bmc.2019.02.020
71518536 86067 0 None - 1 Human 5.6 pKi = 5.6 Binding
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 232 1 3 5 0.3 Cc1cc2c(N3CCNCC3)nc(N)nc2[nH]1 10.1016/j.bmcl.2012.10.139
CHEMBL2314771 86067 0 None - 1 Human 5.6 pKi = 5.6 Binding
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 232 1 3 5 0.3 Cc1cc2c(N3CCNCC3)nc(N)nc2[nH]1 10.1016/j.bmcl.2012.10.139
57391927 69561 0 None - 1 Human 5.6 pKi = 5.6 Binding
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 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 69561 0 None - 1 Human 5.6 pKi = 5.6 Binding
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 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
3991311 136338 9 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-histamine from human histamine H4 receptor expressed in HEK293T cells after 1 to 1.5 hrs by liquid scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor expressed in HEK293T cells after 1 to 1.5 hrs by liquid scintillation counting analysis
ChEMBL 296 2 0 5 2.7 CCc1nc(N2CCN(C)CC2)c2oc3ccccc3c2n1 10.1039/C5MD00022J
CHEMBL3741986 136338 9 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-histamine from human histamine H4 receptor expressed in HEK293T cells after 1 to 1.5 hrs by liquid scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor expressed in HEK293T cells after 1 to 1.5 hrs by liquid scintillation counting analysis
ChEMBL 296 2 0 5 2.7 CCc1nc(N2CCN(C)CC2)c2oc3ccccc3c2n1 10.1039/C5MD00022J
25178556 188496 0 None - 1 Human 6.6 pKi = 6.6 Binding
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 423 4 1 6 4.9 CN1CCN(c2nc(NCc3cc4ccccc4s3)c3cc(Cl)ccc3n2)CC1 10.1021/jm800876b
CHEMBL509961 188496 0 None - 1 Human 6.6 pKi = 6.6 Binding
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 423 4 1 6 4.9 CN1CCN(c2nc(NCc3cc4ccccc4s3)c3cc(Cl)ccc3n2)CC1 10.1021/jm800876b
44563707 200911 0 None - 1 Human 6.6 pKi = 6.6 Binding
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 368 4 0 5 3.6 CN1CCN(c2nc3ccc(Cl)cc3nc2OCc2ccccc2)CC1 10.1021/jm800876b
CHEMBL612059 200911 0 None - 1 Human 6.6 pKi = 6.6 Binding
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 368 4 0 5 3.6 CN1CCN(c2nc3ccc(Cl)cc3nc2OCc2ccccc2)CC1 10.1021/jm800876b
24853595 159624 0 None - 1 Human 6.6 pKi = 6.6 Binding
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 368 4 0 5 3.6 CN1CCN(c2nc3ccccc3nc2OCc2cccc(Cl)c2)CC1 10.1021/jm7014217
CHEMBL410925 159624 0 None - 1 Human 6.6 pKi = 6.6 Binding
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 368 4 0 5 3.6 CN1CCN(c2nc3ccccc3nc2OCc2cccc(Cl)c2)CC1 10.1021/jm7014217
155535098 175812 0 None - 1 Human 5.6 pKi = 5.6 Binding
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 305 3 3 5 1.3 CC(C)(C)CNc1nccc(N2CCCN(C(=N)N)CC2)n1 10.1021/acs.jmedchem.9b01342
CHEMBL4471442 175812 0 None - 1 Human 5.6 pKi = 5.6 Binding
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 305 3 3 5 1.3 CC(C)(C)CNc1nccc(N2CCCN(C(=N)N)CC2)n1 10.1021/acs.jmedchem.9b01342
CHEMBL4595908 175812 0 None - 1 Human 5.6 pKi = 5.6 Binding
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 305 3 3 5 1.3 CC(C)(C)CNc1nccc(N2CCCN(C(=N)N)CC2)n1 10.1021/acs.jmedchem.9b01342
10782821 95775 0 None - 1 Human 5.6 pKi = 5.6 Binding
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 332 4 0 4 3.4 CCN1CCN(c2nc3ccccc3nc2Cc2ccccc2)CC1 10.1021/jm7014217
CHEMBL260850 95775 0 None - 1 Human 5.6 pKi = 5.6 Binding
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 332 4 0 4 3.4 CCN1CCN(c2nc3ccccc3nc2Cc2ccccc2)CC1 10.1021/jm7014217
164616851 184367 0 None -446 5 Human 4.6 pKi = 4.6 Binding
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 376 6 4 4 2.5 Cc1nc(N)sc1CCCN/C(N)=N/C(=S)N[C@H](C)c1ccccc1 10.1016/j.ejmech.2021.113190
CHEMBL4853772 184367 0 None -446 5 Human 4.6 pKi = 4.6 Binding
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 376 6 4 4 2.5 Cc1nc(N)sc1CCCN/C(N)=N/C(=S)N[C@H](C)c1ccccc1 10.1016/j.ejmech.2021.113190
10591811 158806 0 None 4 2 Human 7.6 pKi = 7.6 Binding
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 320 9 1 2 4.7 c1ccc(-c2ccc(CCCOCCCc3c[nH]cn3)cc2)cc1 10.1016/j.ejmech.2016.09.074
CHEMBL4100315 158806 0 None 4 2 Human 7.6 pKi = 7.6 Binding
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 320 9 1 2 4.7 c1ccc(-c2ccc(CCCOCCCc3c[nH]cn3)cc2)cc1 10.1016/j.ejmech.2016.09.074
1267 3744 43 None -33 25 Human 7.6 pKi = 7.6 Binding
Binding affinity to the human histamine H4 receptorBinding affinity to the human histamine H4 receptor
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1021/jm0341047
3035905 3744 43 None -33 25 Human 7.6 pKi = 7.6 Binding
Binding affinity to the human histamine H4 receptorBinding affinity to the human histamine H4 receptor
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1021/jm0341047
CHEMBL260374 3744 43 None -33 25 Human 7.6 pKi = 7.6 Binding
Binding affinity to the human histamine H4 receptorBinding affinity to the human histamine H4 receptor
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1021/jm0341047
24804219 148031 0 None - 1 Human 7.6 pKi = 7.6 Binding
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 378 6 2 5 4.2 Cc1nc(NCCCC2CCN(C)CC2)ncc1-c1nc2c(C)cccc2[nH]1 nan
CHEMBL3938862 148031 0 None - 1 Human 7.6 pKi = 7.6 Binding
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 378 6 2 5 4.2 Cc1nc(NCCCC2CCN(C)CC2)ncc1-c1nc2c(C)cccc2[nH]1 nan
11565330 96771 0 None - 1 Human 7.6 pKi = 7.6 Binding
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 275 1 1 2 2.0 Cc1c(F)ccc2[nH]c(C(=O)N3CCN(C)CC3)cc12 10.1021/jm0502081
CHEMBL268525 96771 0 None - 1 Human 7.6 pKi = 7.6 Binding
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 275 1 1 2 2.0 Cc1c(F)ccc2[nH]c(C(=O)N3CCN(C)CC3)cc12 10.1021/jm0502081
1267 3744 43 None -33 25 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]histamine human recombinant histamine H4 receptorDisplacement of [3H]histamine human recombinant histamine H4 receptor
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1016/j.bmcl.2010.02.097
3035905 3744 43 None -33 25 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]histamine human recombinant histamine H4 receptorDisplacement of [3H]histamine human recombinant histamine H4 receptor
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1016/j.bmcl.2010.02.097
CHEMBL260374 3744 43 None -33 25 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]histamine human recombinant histamine H4 receptorDisplacement of [3H]histamine human recombinant histamine H4 receptor
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1016/j.bmcl.2010.02.097
71525681 89298 0 None -3 6 Rat 7.6 pKi = 7.6 Binding
Binding affinity to rat histamine H4 receptorBinding affinity to rat histamine H4 receptor
ChEMBL 298 3 2 6 1.7 CNC1CN(c2nc(N)nc3cc(C4CCCC4)cnc23)C1 10.1016/j.bmcl.2013.02.091
CHEMBL2376803 89298 0 None -3 6 Rat 7.6 pKi = 7.6 Binding
Binding affinity to rat histamine H4 receptorBinding affinity to rat histamine H4 receptor
ChEMBL 298 3 2 6 1.7 CNC1CN(c2nc(N)nc3cc(C4CCCC4)cnc23)C1 10.1016/j.bmcl.2013.02.091
11846634 77655 0 None - 1 Human 7.6 pKi = 7.6 Binding
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 345 0 0 4 3.9 CN1CCN(C2=Nc3cc(Cl)ccc3Oc3c(F)cccc32)CC1 10.1021/jm051008s
CHEMBL209758 77655 0 None - 1 Human 7.6 pKi = 7.6 Binding
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 345 0 0 4 3.9 CN1CCN(C2=Nc3cc(Cl)ccc3Oc3c(F)cccc32)CC1 10.1021/jm051008s
57395496 67831 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 349 1 2 6 2.5 Nc1nc(N2C[C@@H]3C[C@H]2CN3)c2oc3ccc(C(F)(F)F)cc3c2n1 10.1016/j.bmcl.2011.08.014
CHEMBL1915034 67831 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 349 1 2 6 2.5 Nc1nc(N2C[C@@H]3C[C@H]2CN3)c2oc3ccc(C(F)(F)F)cc3c2n1 10.1016/j.bmcl.2011.08.014
51354302 58586 0 None 1 2 Human 6.6 pKi = 6.6 Binding
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 287 7 1 4 3.1 c1nc(CCCCn2cc(CC3CCCCC3)nn2)c[nH]1 10.1021/jm1013488
CHEMBL1688970 58586 0 None 1 2 Human 6.6 pKi = 6.6 Binding
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 287 7 1 4 3.1 c1nc(CCCCn2cc(CC3CCCCC3)nn2)c[nH]1 10.1021/jm1013488
25130235 187004 1 None -7 11 Rat 6.6 pKi = 6.6 Binding
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 294 2 1 6 1.3 CN1CCN(c2cc(-c3ccc(C#N)cc3)nc(N)n2)CC1 10.1021/jm8005959
25130235 187004 1 None -7 11 Rat 6.6 pKi = 6.6 Binding
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 294 2 1 6 1.3 CN1CCN(c2cc(-c3ccc(C#N)cc3)nc(N)n2)CC1 10.1021/jm800670r
CHEMBL494678 187004 1 None -7 11 Rat 6.6 pKi = 6.6 Binding
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 294 2 1 6 1.3 CN1CCN(c2cc(-c3ccc(C#N)cc3)nc(N)n2)CC1 10.1021/jm8005959
CHEMBL494678 187004 1 None -7 11 Rat 6.6 pKi = 6.6 Binding
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 294 2 1 6 1.3 CN1CCN(c2cc(-c3ccc(C#N)cc3)nc(N)n2)CC1 10.1021/jm800670r
57390225 67540 0 None -3235 3 Human 4.6 pKi = 4.6 Binding
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 469 9 2 5 4.1 COc1ccc(CN(CCN[C@H]2CCN(C(=O)c3cc4ccccc4[nH]3)C2)c2ccccn2)cc1 10.1016/j.bmcl.2011.09.001
CHEMBL1910384 67540 0 None -3235 3 Human 4.6 pKi = 4.6 Binding
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 469 9 2 5 4.1 COc1ccc(CN(CCN[C@H]2CCN(C(=O)c3cc4ccccc4[nH]3)C2)c2ccccn2)cc1 10.1016/j.bmcl.2011.09.001
55251397 172693 2 None - 1 Human 6.6 pKi = 6.6 Binding
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 236 2 1 6 0.3 CC(C)c1nc(N)nc(N2CCN(C)CC2)n1 10.1016/j.bmc.2019.02.020
CHEMBL4525008 172693 2 None - 1 Human 6.6 pKi = 6.6 Binding
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 236 2 1 6 0.3 CC(C)c1nc(N)nc(N2CCN(C)CC2)n1 10.1016/j.bmc.2019.02.020
53233803 61193 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]histamine from human histamine H4 receptorDisplacement of [3H]histamine from human histamine H4 receptor
ChEMBL 249 3 2 5 1.2 CC(C)Nc1cc(N2CCN(C)CC2)cc(N)n1 10.1016/j.bmcl.2011.03.017
CHEMBL1770962 61193 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]histamine from human histamine H4 receptorDisplacement of [3H]histamine from human histamine H4 receptor
ChEMBL 249 3 2 5 1.2 CC(C)Nc1cc(N2CCN(C)CC2)cc(N)n1 10.1016/j.bmcl.2011.03.017
11293460 84419 0 None - 1 Human 7.6 pKi = 7.6 Binding
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 434 6 1 4 5.1 CN1CCN(CCCOc2ccc(-c3nc4c(ccc5ccccc54)[nH]3)c(Cl)c2)CC1 10.1016/j.bmcl.2006.08.117
CHEMBL223490 84419 0 None - 1 Human 7.6 pKi = 7.6 Binding
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 434 6 1 4 5.1 CN1CCN(CCCOc2ccc(-c3nc4c(ccc5ccccc54)[nH]3)c(Cl)c2)CC1 10.1016/j.bmcl.2006.08.117
42624148 109657 0 None - 1 Human 7.6 pKi = 7.6 Binding
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 233 3 2 5 0.7 CN[C@@H]1CCN(c2cc(C3CC3)nc(N)n2)C1 10.1021/jm401727m
CHEMBL3236574 109657 0 None - 1 Human 7.6 pKi = 7.6 Binding
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 233 3 2 5 0.7 CN[C@@H]1CCN(c2cc(C3CC3)nc(N)n2)C1 10.1021/jm401727m
11846300 79856 3 None -2 4 Human 7.6 pKi = 7.6 Binding
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 327 0 0 4 3.8 CN1CCN(C2=Nc3ccc(Cl)cc3Oc3ccccc32)CC1 10.1021/jm800876b
CHEMBL213912 79856 3 None -2 4 Human 7.6 pKi = 7.6 Binding
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 327 0 0 4 3.8 CN1CCN(C2=Nc3ccc(Cl)cc3Oc3ccccc32)CC1 10.1021/jm800876b
11846300 79856 3 None -2 4 Human 7.6 pKi = 7.6 Binding
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 79856 3 None -2 4 Human 7.6 pKi = 7.6 Binding
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
217674 178701 6 None - 1 Human 5.6 pKi = 5.6 Binding
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 320 3 0 5 3.2 CN1CCN(c2nc(Oc3ccccc3)c3ccccc3n2)CC1 10.1021/jm800876b
CHEMBL473098 178701 6 None - 1 Human 5.6 pKi = 5.6 Binding
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 320 3 0 5 3.2 CN1CCN(c2nc(Oc3ccccc3)c3ccccc3n2)CC1 10.1021/jm800876b
217674 178701 6 None - 1 Human 5.6 pKi = 5.6 Binding
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 320 3 0 5 3.2 CN1CCN(c2nc(Oc3ccccc3)c3ccccc3n2)CC1 10.1021/jm901379s
CHEMBL473098 178701 6 None - 1 Human 5.6 pKi = 5.6 Binding
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 320 3 0 5 3.2 CN1CCN(c2nc(Oc3ccccc3)c3ccccc3n2)CC1 10.1021/jm901379s
156009715 177745 0 None -1 2 Human 4.6 pKi = 4.6 Binding
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 601 8 1 3 8.2 Cc1cc(OCCC[n+]2c(C)cc(/C=C/c3cc4c5c(c3)CCCN5CCC4)cc2C)ccc1-c1nc2c(C)c(F)ccc2[nH]1 10.1021/acs.jmedchem.0c00160
CHEMBL4634631 177745 0 None -1 2 Human 4.6 pKi = 4.6 Binding
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 601 8 1 3 8.2 Cc1cc(OCCC[n+]2c(C)cc(/C=C/c3cc4c5c(c3)CCCN5CCC4)cc2C)ccc1-c1nc2c(C)c(F)ccc2[nH]1 10.1021/acs.jmedchem.0c00160
CHEMBL4651103 177745 0 None -1 2 Human 4.6 pKi = 4.6 Binding
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 601 8 1 3 8.2 Cc1cc(OCCC[n+]2c(C)cc(/C=C/c3cc4c5c(c3)CCCN5CCC4)cc2C)ccc1-c1nc2c(C)c(F)ccc2[nH]1 10.1021/acs.jmedchem.0c00160
45257134 198261 0 None - 1 Human 6.6 pKi = 6.6 Binding
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 312 4 2 6 1.7 Cc1cccc(CNc2cc(N3CCN(C)CC3)nc(N)n2)c1 10.1016/j.bmc.2009.08.059
CHEMBL594949 198261 0 None - 1 Human 6.6 pKi = 6.6 Binding
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 312 4 2 6 1.7 Cc1cccc(CNc2cc(N3CCN(C)CC3)nc(N)n2)c1 10.1016/j.bmc.2009.08.059
155539562 172274 0 None - 1 Human 5.6 pKi = 5.6 Binding
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 304 4 1 6 1.7 CN1CCN(c2nc(N)nc(CCC3CCCCC3)n2)CC1 10.1016/j.bmc.2019.02.020
CHEMBL4514667 172274 0 None - 1 Human 5.6 pKi = 5.6 Binding
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 304 4 1 6 1.7 CN1CCN(c2nc(N)nc(CCC3CCCCC3)n2)CC1 10.1016/j.bmc.2019.02.020
10083188 140403 3 None - 1 Human 6.5 pKi = 6.5 Binding
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 244 1 1 3 1.0 CN1CCN(C(=O)c2nc3ccccc3[nH]2)CC1 10.1016/j.bmcl.2011.09.001
CHEMBL382276 140403 3 None - 1 Human 6.5 pKi = 6.5 Binding
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 244 1 1 3 1.0 CN1CCN(C(=O)c2nc3ccccc3[nH]2)CC1 10.1016/j.bmcl.2011.09.001
9927983 79442 0 None - 1 Human 6.5 pKi = 6.5 Binding
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 341 1 0 4 4.2 CCN1CCN(C2=Nc3cc(Cl)ccc3Oc3ccccc32)CC1 10.1021/jm051008s
CHEMBL1795042 79442 0 None - 1 Human 6.5 pKi = 6.5 Binding
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 341 1 0 4 4.2 CCN1CCN(C2=Nc3cc(Cl)ccc3Oc3ccccc32)CC1 10.1021/jm051008s
CHEMBL212212 79442 0 None - 1 Human 6.5 pKi = 6.5 Binding
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 341 1 0 4 4.2 CCN1CCN(C2=Nc3cc(Cl)ccc3Oc3ccccc32)CC1 10.1021/jm051008s
49841612 69391 0 None - 1 Human 7.5 pKi = 7.5 Binding
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 344 2 1 6 2.5 CN1CCN(c2nc(N)nc3cc(-c4ccc(C#N)cc4)ccc23)CC1 10.1016/j.bmcl.2011.10.104
CHEMBL1935568 69391 0 None - 1 Human 7.5 pKi = 7.5 Binding
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 344 2 1 6 2.5 CN1CCN(c2nc(N)nc3cc(-c4ccc(C#N)cc4)ccc23)CC1 10.1016/j.bmcl.2011.10.104
54587786 61201 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]histamine from human histamine H4 receptorDisplacement of [3H]histamine from human histamine H4 receptor
ChEMBL 263 4 2 5 1.3 CN[C@@H]1CCN(c2cc(N)nc(N(C)C(C)C)c2)C1 10.1016/j.bmcl.2011.03.017
CHEMBL1770970 61201 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]histamine from human histamine H4 receptorDisplacement of [3H]histamine from human histamine H4 receptor
ChEMBL 263 4 2 5 1.3 CN[C@@H]1CCN(c2cc(N)nc(N(C)C(C)C)c2)C1 10.1016/j.bmcl.2011.03.017
24825897 67768 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 299 1 1 6 2.2 CN1CCN(c2nc(N)nc3c2sc2ccccc23)CC1 10.1016/j.bmcl.2011.08.014
CHEMBL1914759 67768 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 299 1 1 6 2.2 CN1CCN(c2nc(N)nc3c2sc2ccccc23)CC1 10.1016/j.bmcl.2011.08.014
71519674 89299 0 None -3 5 Rat 7.5 pKi = 7.5 Binding
Binding affinity to rat histamine H4 receptorBinding affinity to rat histamine H4 receptor
ChEMBL 270 3 2 6 0.9 CNC1CN(c2nc(N)nc3cc(C4CC4)cnc23)C1 10.1016/j.bmcl.2013.02.091
CHEMBL2376804 89299 0 None -3 5 Rat 7.5 pKi = 7.5 Binding
Binding affinity to rat histamine H4 receptorBinding affinity to rat histamine H4 receptor
ChEMBL 270 3 2 6 0.9 CNC1CN(c2nc(N)nc3cc(C4CC4)cnc23)C1 10.1016/j.bmcl.2013.02.091
56851610 71283 0 None 2 2 Human 7.5 pKi = 7.5 Binding
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 5 2 3 3.8 CC(C)(C)N/C(=N/C1CCCC1)SCCCc1c[nH]cn1 10.1021/jm201042n
CHEMBL1923031 71283 0 None 2 2 Human 7.5 pKi = 7.5 Binding
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 5 2 3 3.8 CC(C)(C)N/C(=N/C1CCCC1)SCCCc1c[nH]cn1 10.1021/jm201042n
CHEMBL1963448 71283 0 None 2 2 Human 7.5 pKi = 7.5 Binding
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 5 2 3 3.8 CC(C)(C)N/C(=N/C1CCCC1)SCCCc1c[nH]cn1 10.1021/jm201042n
127049856 139715 0 None 2 4 Human 6.5 pKi = 6.5 Binding
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
CHEMBL3805431 139715 0 None 2 4 Human 6.5 pKi = 6.5 Binding
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
10680721 5904 0 None -23 3 Human 6.5 pKi = 6.5 Binding
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 225 6 2 3 1.9 CC[C@@H](C)NC(=O)OCCCc1c[nH]cn1 10.1016/j.bmcl.2009.10.005
CHEMBL1080089 5904 0 None -23 3 Human 6.5 pKi = 6.5 Binding
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 225 6 2 3 1.9 CC[C@@H](C)NC(=O)OCCCc1c[nH]cn1 10.1016/j.bmcl.2009.10.005
CHEMBL158085 5904 0 None -23 3 Human 6.5 pKi = 6.5 Binding
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 225 6 2 3 1.9 CC[C@@H](C)NC(=O)OCCCc1c[nH]cn1 10.1016/j.bmcl.2009.10.005
753256 178770 10 None 2 2 Human 6.5 pKi = 6.5 Binding
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 208 1 2 6 -0.6 CN1CCN(c2cc(N)nc(N)n2)CC1 10.1016/j.bmc.2009.08.059
CHEMBL473662 178770 10 None 2 2 Human 6.5 pKi = 6.5 Binding
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 208 1 2 6 -0.6 CN1CCN(c2cc(N)nc(N)n2)CC1 10.1016/j.bmc.2009.08.059
46228133 198371 0 None - 1 Human 6.5 pKi = 6.5 Binding
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 332 4 2 6 2.1 CN1CCN(c2cc(NCc3cccc(Cl)c3)nc(N)n2)CC1 10.1016/j.bmc.2009.08.059
CHEMBL595639 198371 0 None - 1 Human 6.5 pKi = 6.5 Binding
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 332 4 2 6 2.1 CN1CCN(c2cc(NCc3cccc(Cl)c3)nc(N)n2)CC1 10.1016/j.bmc.2009.08.059
29136870 68679 7 None -46 2 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation countingDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting
ChEMBL 301 2 0 7 0.7 CN1CCN(c2nc(N3CCCC3)c3cnn(C)c3n2)CC1 10.1021/jm2011589
CHEMBL1923522 68679 7 None -46 2 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation countingDisplacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting
ChEMBL 301 2 0 7 0.7 CN1CCN(c2nc(N3CCCC3)c3cnn(C)c3n2)CC1 10.1021/jm2011589
71519176 86056 0 None - 1 Human 5.5 pKi = 5.5 Binding
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 340 2 2 5 2.5 CN1CCCN(c2nc(N)nc3[nH]c(-c4ccc(F)cc4)cc23)CC1 10.1016/j.bmcl.2012.10.139
CHEMBL2314759 86056 0 None - 1 Human 5.5 pKi = 5.5 Binding
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 340 2 2 5 2.5 CN1CCCN(c2nc(N)nc3[nH]c(-c4ccc(F)cc4)cc23)CC1 10.1016/j.bmcl.2012.10.139
155545717 172897 0 None -1 2 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptor expressed in CHO cell membranes after 30 mins by liquid scintillation analysisDisplacement of [3H]histamine from human recombinant histamine H4 receptor expressed in CHO cell membranes after 30 mins by liquid scintillation analysis
ChEMBL 238 3 2 2 2.6 c1ccc2[nH]c(C[C@@H]3C[C@H]3c3c[nH]cn3)nc2c1 10.1016/j.bmcl.2018.10.041
CHEMBL4529871 172897 0 None -1 2 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptor expressed in CHO cell membranes after 30 mins by liquid scintillation analysisDisplacement of [3H]histamine from human recombinant histamine H4 receptor expressed in CHO cell membranes after 30 mins by liquid scintillation analysis
ChEMBL 238 3 2 2 2.6 c1ccc2[nH]c(C[C@@H]3C[C@H]3c3c[nH]cn3)nc2c1 10.1016/j.bmcl.2018.10.041
156015791 177669 0 None 1 2 Human 6.5 pKi = 6.5 Binding
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 442 8 1 3 4.6 Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCCN1CCc2nc[nH]c2C1 10.1021/acs.jmedchem.0c00160
CHEMBL4646286 177669 0 None 1 2 Human 6.5 pKi = 6.5 Binding
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 442 8 1 3 4.6 Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCCN1CCc2nc[nH]c2C1 10.1021/acs.jmedchem.0c00160
CHEMBL4650609 177669 0 None 1 2 Human 6.5 pKi = 6.5 Binding
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 442 8 1 3 4.6 Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCCN1CCc2nc[nH]c2C1 10.1021/acs.jmedchem.0c00160
24854638 154656 0 None - 1 Human 6.5 pKi = 6.5 Binding
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 334 4 0 5 3.0 CN1CCN(c2nc3ccccc3nc2OCc2ccccc2)CC1 10.1021/jm7014217
CHEMBL402470 154656 0 None - 1 Human 6.5 pKi = 6.5 Binding
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 334 4 0 5 3.0 CN1CCN(c2nc3ccccc3nc2OCc2ccccc2)CC1 10.1021/jm7014217
24854702 95611 0 None - 1 Human 5.5 pKi = 5.5 Binding
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 335 4 0 6 2.4 CN1CCN(c2nc3ccccc3nc2OCc2cccnc2)CC1 10.1021/jm7014217
CHEMBL259955 95611 0 None - 1 Human 5.5 pKi = 5.5 Binding
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 335 4 0 6 2.4 CN1CCN(c2nc3ccccc3nc2OCc2cccnc2)CC1 10.1021/jm7014217
24853592 155616 0 None - 1 Human 5.5 pKi = 5.5 Binding
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 376 7 0 5 3.8 CN1CCN(c2nc3ccccc3nc2OCCCCc2ccccc2)CC1 10.1021/jm7014217
CHEMBL406380 155616 0 None - 1 Human 5.5 pKi = 5.5 Binding
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 376 7 0 5 3.8 CN1CCN(c2nc3ccccc3nc2OCCCCc2ccccc2)CC1 10.1021/jm7014217
122193104 123370 0 None - 1 Human 4.5 pKi = 4.5 Binding
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 346 3 1 6 2.5 CN1CCN(c2nc(N)nc(/C=C/c3cccc4ccccc34)n2)CC1 10.1016/j.ejmech.2015.08.014
CHEMBL3627724 123370 0 None - 1 Human 4.5 pKi = 4.5 Binding
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 346 3 1 6 2.5 CN1CCN(c2nc(N)nc(/C=C/c3cccc4ccccc34)n2)CC1 10.1016/j.ejmech.2015.08.014
137632569 155731 0 None 4 2 Human 8.5 pKi = 8.5 Binding
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 418 7 1 2 4.8 Ic1ccc(C(OCCCc2c[nH]cn2)c2ccccc2)cc1 10.1016/j.ejmech.2016.09.074
CHEMBL4065099 155731 0 None 4 2 Human 8.5 pKi = 8.5 Binding
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 418 7 1 2 4.8 Ic1ccc(C(OCCCc2c[nH]cn2)c2ccccc2)cc1 10.1016/j.ejmech.2016.09.074
53233804 61197 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]histamine from human histamine H4 receptorDisplacement of [3H]histamine from human histamine H4 receptor
ChEMBL 275 3 2 5 1.8 CN1CCN(c2cc(N)nc(NC3CCCC3)c2)CC1 10.1016/j.bmcl.2011.03.017
CHEMBL1770966 61197 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]histamine from human histamine H4 receptorDisplacement of [3H]histamine from human histamine H4 receptor
ChEMBL 275 3 2 5 1.8 CN1CCN(c2cc(N)nc(NC3CCCC3)c2)CC1 10.1016/j.bmcl.2011.03.017
54583873 61200 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]histamine from human histamine H4 receptorDisplacement of [3H]histamine from human histamine H4 receptor
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 61200 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]histamine from human histamine H4 receptorDisplacement of [3H]histamine from human histamine H4 receptor
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
54584824 61208 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]histamine from human histamine H4 receptorDisplacement of [3H]histamine from human histamine H4 receptor
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 61208 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]histamine from human histamine H4 receptorDisplacement of [3H]histamine from human histamine H4 receptor
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
54585780 61229 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]histamine from human histamine H4 receptorDisplacement of [3H]histamine from human histamine H4 receptor
ChEMBL 250 3 2 6 0.6 CC(C)Nc1cc(N2CCN(C)CC2)nc(N)n1 10.1016/j.bmcl.2011.03.017
CHEMBL1770998 61229 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]histamine from human histamine H4 receptorDisplacement of [3H]histamine from human histamine H4 receptor
ChEMBL 250 3 2 6 0.6 CC(C)Nc1cc(N2CCN(C)CC2)nc(N)n1 10.1016/j.bmcl.2011.03.017
58227326 116626 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 249 6 2 5 1.5 CCCCNc1nccc(N2CC[C@@H](NC)C2)n1 10.1016/j.bmcl.2014.12.027
CHEMBL3393542 116626 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 249 6 2 5 1.5 CCCCNc1nccc(N2CC[C@@H](NC)C2)n1 10.1016/j.bmcl.2014.12.027
9839217 72174 0 None - 1 Human 8.5 pKi = 8.5 Binding
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 297 1 1 3 2.6 Cc1c(Cl)sc2cc(C(=O)N3CCN(C)CC3)[nH]c12 10.1021/jm0502081
CHEMBL199062 72174 0 None - 1 Human 8.5 pKi = 8.5 Binding
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 297 1 1 3 2.6 Cc1c(Cl)sc2cc(C(=O)N3CCN(C)CC3)[nH]c12 10.1021/jm0502081
54583873 61200 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 249 4 3 5 1.3 CN[C@@H]1CCN(c2cc(N)nc(NC(C)C)c2)C1 10.1016/j.bmcl.2014.10.013
CHEMBL1770969 61200 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 249 4 3 5 1.3 CN[C@@H]1CCN(c2cc(N)nc(NC(C)C)c2)C1 10.1016/j.bmcl.2014.10.013
54585781 61232 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]histamine displacement from human recombinant histamine H4 receptor expressed in SK-NM-C cells after 45 minsDisplacement of [3H]histamine displacement from human recombinant histamine H4 receptor expressed in SK-NM-C cells after 45 mins
ChEMBL 264 4 2 6 0.9 CC(C)CNc1cc(N2CCN(C)CC2)nc(N)n1 10.1021/jm301886t
CHEMBL1771000 61232 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]histamine displacement from human recombinant histamine H4 receptor expressed in SK-NM-C cells after 45 minsDisplacement of [3H]histamine displacement from human recombinant histamine H4 receptor expressed in SK-NM-C cells after 45 mins
ChEMBL 264 4 2 6 0.9 CC(C)CNc1cc(N2CCN(C)CC2)nc(N)n1 10.1021/jm301886t
71551636 89243 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]histamine displacement from human recombinant histamine H4 receptor expressed in SK-NM-C cells after 45 minsDisplacement of [3H]histamine displacement from human recombinant histamine H4 receptor expressed in SK-NM-C cells after 45 mins
ChEMBL 263 4 1 5 1.4 CC(C)CCc1cc(N2CCN(C)CC2)nc(N)n1 10.1021/jm301886t
CHEMBL2375772 89243 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]histamine displacement from human recombinant histamine H4 receptor expressed in SK-NM-C cells after 45 minsDisplacement of [3H]histamine displacement from human recombinant histamine H4 receptor expressed in SK-NM-C cells after 45 mins
ChEMBL 263 4 1 5 1.4 CC(C)CCc1cc(N2CCN(C)CC2)nc(N)n1 10.1021/jm301886t
25129527 186831 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]histamine displacement from human recombinant histamine H4 receptor expressed in SK-NM-C cells after 45 minsDisplacement of [3H]histamine displacement from human recombinant histamine H4 receptor expressed in SK-NM-C cells after 45 mins
ChEMBL 303 2 1 5 2.1 CN1CCN(c2cc(-c3ccc(Cl)cc3)nc(N)n2)CC1 10.1021/jm301886t
CHEMBL493720 186831 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]histamine displacement from human recombinant histamine H4 receptor expressed in SK-NM-C cells after 45 minsDisplacement of [3H]histamine displacement from human recombinant histamine H4 receptor expressed in SK-NM-C cells after 45 mins
ChEMBL 303 2 1 5 2.1 CN1CCN(c2cc(-c3ccc(Cl)cc3)nc(N)n2)CC1 10.1021/jm301886t
46881855 7664 0 None 15 4 Rat 8.5 pKi = 8.5 Binding
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 337 3 2 5 2.5 CN[C@@H]1CCN(c2nc(N)nc3c2CCCC(c2ccccc2)C3)C1 10.1016/j.bmcl.2010.01.131
CHEMBL1089040 7664 0 None 15 4 Rat 8.5 pKi = 8.5 Binding
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 337 3 2 5 2.5 CN[C@@H]1CCN(c2nc(N)nc3c2CCCC(c2ccccc2)C3)C1 10.1016/j.bmcl.2010.01.131
10967174 19242 3 None 2 2 Rat 8.5 pKi = 8.5 Binding
Binding affinity of compound towards rat histamine H4 receptorBinding affinity of compound towards rat histamine H4 receptor
ChEMBL 258 1 2 3 1.1 CN1CCN(C(=O)c2cc3cccc(N)c3[nH]2)CC1 10.1021/jm0341047
CHEMBL129540 19242 3 None 2 2 Rat 8.5 pKi = 8.5 Binding
Binding affinity of compound towards rat histamine H4 receptorBinding affinity of compound towards rat histamine H4 receptor
ChEMBL 258 1 2 3 1.1 CN1CCN(C(=O)c2cc3cccc(N)c3[nH]2)CC1 10.1021/jm0341047
46890166 7235 0 None 4786 2 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human 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 7235 0 None 4786 2 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human 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
1278 2119 79 None -3 8 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]-histamine from human H4R expressed in HEK293T cellsDisplacement of [3H]-histamine from human 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 2119 79 None -3 8 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]-histamine from human H4R expressed in HEK293T cellsDisplacement of [3H]-histamine from human 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 2119 79 None -3 8 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]-histamine from human H4R expressed in HEK293T cellsDisplacement of [3H]-histamine from human 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 2119 79 None -3 8 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]-histamine from human H4R expressed in HEK293T cellsDisplacement of [3H]-histamine from human 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
71603136 89285 0 None 46 2 Human 8.5 pKi = 8.5 Binding
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 3 2 5 2.3 CNC1CN(c2nc(N)nc3cc(C4CCCC4)ccc23)C1 10.1016/j.bmcl.2013.02.091
CHEMBL2376790 89285 0 None 46 2 Human 8.5 pKi = 8.5 Binding
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 3 2 5 2.3 CNC1CN(c2nc(N)nc3cc(C4CCCC4)ccc23)C1 10.1016/j.bmcl.2013.02.091
25109291 190792 9 None -79 8 Rat 8.5 pKi = 8.5 Binding
Displacement of [3H]histamine from rat histamine H4 receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [3H]histamine from rat histamine H4 receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 327 1 2 6 1.7 Nc1nc2c(c(N3CCNCC3)n1)CCC1=C2[C@@H]2CCCC[C@@H]2O1 10.1021/jm8007618
CHEMBL519240 190792 9 None -79 8 Rat 8.5 pKi = 8.5 Binding
Displacement of [3H]histamine from rat histamine H4 receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [3H]histamine from rat histamine H4 receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 327 1 2 6 1.7 Nc1nc2c(c(N3CCNCC3)n1)CCC1=C2[C@@H]2CCCC[C@@H]2O1 10.1021/jm8007618
127050309 140318 0 None - 1 Human 8.5 pKi = 8.5 Binding
Inhibition of histamine H4 receptor (unknown origin)Inhibition of histamine H4 receptor (unknown origin)
ChEMBL 283 2 2 6 1.8 CN[C@H]1CCN(c2nc(N)nc3c2oc2ccccc23)C1 10.1039/C6MD00108D
CHEMBL3819470 140318 0 None - 1 Human 8.5 pKi = 8.5 Binding
Inhibition of histamine H4 receptor (unknown origin)Inhibition of histamine H4 receptor (unknown origin)
ChEMBL 283 2 2 6 1.8 CN[C@H]1CCN(c2nc(N)nc3c2oc2ccccc23)C1 10.1039/C6MD00108D
53476465 67712 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 303 2 2 6 2.0 NCC1CN(c2nc(N)nc3c2oc2ccc(Cl)cc23)C1 10.1016/j.bmcl.2011.08.014
CHEMBL1914547 67712 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 303 2 2 6 2.0 NCC1CN(c2nc(N)nc3c2oc2ccc(Cl)cc23)C1 10.1016/j.bmcl.2011.08.014
24737947 67785 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 283 2 2 6 1.8 CN[C@@H]1CCN(c2nc(N)nc3c2oc2ccccc23)C1 10.1016/j.bmcl.2011.08.014
CHEMBL1914776 67785 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 283 2 2 6 1.8 CN[C@@H]1CCN(c2nc(N)nc3c2oc2ccccc23)C1 10.1016/j.bmcl.2011.08.014
25071004 192116 0 None 1 2 Human 8.5 pKi = 8.5 Binding
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 309 2 2 5 2.0 CN[C@@H]1CCN(c2nc(N)nc3c2CCCc2ccccc2-3)C1 10.1021/jm800670r
CHEMBL521996 192116 0 None 1 2 Human 8.5 pKi = 8.5 Binding
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 309 2 2 5 2.0 CN[C@@H]1CCN(c2nc(N)nc3c2CCCc2ccccc2-3)C1 10.1021/jm800670r
25071004 192116 0 None 1 2 Human 8.5 pKi = 8.5 Binding
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 309 2 2 5 2.0 CN[C@@H]1CCN(c2nc(N)nc3c2CCCc2ccccc2-3)C1 10.1021/jm800670r
CHEMBL521996 192116 0 None 1 2 Human 8.5 pKi = 8.5 Binding
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 309 2 2 5 2.0 CN[C@@H]1CCN(c2nc(N)nc3c2CCCc2ccccc2-3)C1 10.1021/jm800670r
11957573 1979 29 None -40 6 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in SK-NM-C cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in SK-NM-C cells
ChEMBL 170 3 3 3 0.6 NC(=N)SCCc1cnc[nH]1 10.1021/jm7014777
1250 1979 29 None -40 6 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in SK-NM-C cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in SK-NM-C cells
ChEMBL 170 3 3 3 0.6 NC(=N)SCCc1cnc[nH]1 10.1021/jm7014777
3692 1979 29 None -40 6 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in SK-NM-C cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in SK-NM-C cells
ChEMBL 170 3 3 3 0.6 NC(=N)SCCc1cnc[nH]1 10.1021/jm7014777
CHEMBL19439 1979 29 None -40 6 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in SK-NM-C cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in SK-NM-C cells
ChEMBL 170 3 3 3 0.6 NC(=N)SCCc1cnc[nH]1 10.1021/jm7014777
24826358 67754 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 329 1 2 6 2.4 Nc1nc(N2CC3CCNC3C2)c2oc3ccc(Cl)cc3c2n1 10.1016/j.bmcl.2011.08.014
CHEMBL1914745 67754 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 329 1 2 6 2.4 Nc1nc(N2CC3CCNC3C2)c2oc3ccc(Cl)cc3c2n1 10.1016/j.bmcl.2011.08.014
25101945 192504 0 None 3 2 Rat 8.4 pKi = 8.4 Binding
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 295 2 2 5 1.6 CNC1CN(c2nc(N)nc3c2CCCc2ccccc2-3)C1 10.1021/jm800670r
CHEMBL522673 192504 0 None 3 2 Rat 8.4 pKi = 8.4 Binding
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 295 2 2 5 1.6 CNC1CN(c2nc(N)nc3c2CCCc2ccccc2-3)C1 10.1021/jm800670r
58227401 175877 0 None 7 2 Human 8.4 pKi = 8.4 Binding
Displacement of 40 nM [3H]-histamine from human H4R expressed in Sf9 cell membranes co-expressing Gia2 and beta1gamma2 by competition binding assayDisplacement of 40 nM [3H]-histamine from human H4R expressed in Sf9 cell membranes co-expressing Gia2 and beta1gamma2 by competition binding 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 175877 0 None 7 2 Human 8.4 pKi = 8.4 Binding
Displacement of 40 nM [3H]-histamine from human H4R expressed in Sf9 cell membranes co-expressing Gia2 and beta1gamma2 by competition binding assayDisplacement of 40 nM [3H]-histamine from human H4R expressed in Sf9 cell membranes co-expressing Gia2 and beta1gamma2 by competition binding 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 175877 0 None 7 2 Human 8.4 pKi = 8.4 Binding
Displacement of 40 nM [3H]-histamine from human H4R expressed in Sf9 cell membranes co-expressing Gia2 and beta1gamma2 by competition binding assayDisplacement of 40 nM [3H]-histamine from human H4R expressed in Sf9 cell membranes co-expressing Gia2 and beta1gamma2 by competition binding assay
ChEMBL 263 4 2 5 1.7 CN[C@@H]1CCN(c2ccnc(NCC(C)(C)C)n2)C1 10.1021/acs.jmedchem.9b01342
25068753 187854 15 None 1 2 Rat 8.4 pKi = 8.4 Binding
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 295 1 2 5 1.8 Nc1nc2c(c(N3CC[C@@H](N)C3)n1)CCCc1ccccc1-2 10.1021/jm800670r
CHEMBL502347 187854 15 None 1 2 Rat 8.4 pKi = 8.4 Binding
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 295 1 2 5 1.8 Nc1nc2c(c(N3CC[C@@H](N)C3)n1)CCCc1ccccc1-2 10.1021/jm800670r
1278 2119 79 None -4 8 Mouse 8.4 pKi = 8.4 Binding
Displacement of [3H]-histamine from mouse H4R expressed in HEK293T cellsDisplacement of [3H]-histamine from mouse 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 2119 79 None -4 8 Mouse 8.4 pKi = 8.4 Binding
Displacement of [3H]-histamine from mouse H4R expressed in HEK293T cellsDisplacement of [3H]-histamine from mouse 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 2119 79 None -4 8 Mouse 8.4 pKi = 8.4 Binding
Displacement of [3H]-histamine from mouse H4R expressed in HEK293T cellsDisplacement of [3H]-histamine from mouse 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 2119 79 None -4 8 Mouse 8.4 pKi = 8.4 Binding
Displacement of [3H]-histamine from mouse H4R expressed in HEK293T cellsDisplacement of [3H]-histamine from mouse 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
1267 3744 43 None -33 25 Human 8.4 pKi = 8.4 Binding
Binding affinity to histamine H4 receptorBinding affinity to histamine H4 receptor
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1016/j.bmc.2009.08.059
3035905 3744 43 None -33 25 Human 8.4 pKi = 8.4 Binding
Binding affinity to histamine H4 receptorBinding affinity to histamine H4 receptor
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1016/j.bmc.2009.08.059
CHEMBL260374 3744 43 None -33 25 Human 8.4 pKi = 8.4 Binding
Binding affinity to histamine H4 receptorBinding affinity to histamine H4 receptor
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1016/j.bmc.2009.08.059
21638785 188073 4 None 4 2 Rat 8.4 pKi = 8.4 Binding
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 263 1 2 2 1.9 O=C(c1cc2cc(Cl)ccc2[nH]1)N1CCNCC1 10.1021/jm800670r
CHEMBL503605 188073 4 None 4 2 Rat 8.4 pKi = 8.4 Binding
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 263 1 2 2 1.9 O=C(c1cc2cc(Cl)ccc2[nH]1)N1CCNCC1 10.1021/jm800670r
24994636 109648 0 None - 1 Human 7.5 pKi = 7.5 Binding
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 277 3 3 6 0.5 CN[C@H]1CN(c2cc(C3CCCC3)nc(N)n2)C[C@@H]1O 10.1021/jm401727m
CHEMBL3236565 109648 0 None - 1 Human 7.5 pKi = 7.5 Binding
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 277 3 3 6 0.5 CN[C@H]1CN(c2cc(C3CCCC3)nc(N)n2)C[C@@H]1O 10.1021/jm401727m
24826441 67763 0 None - 1 Human 7.5 pKi = 7.5 Binding
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 COc1cccc2oc3c(N4CCN(C)CC4)nc(N)nc3c12 10.1016/j.bmcl.2011.08.014
CHEMBL1914754 67763 0 None - 1 Human 7.5 pKi = 7.5 Binding
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 COc1cccc2oc3c(N4CCN(C)CC4)nc(N)nc3c12 10.1016/j.bmcl.2011.08.014
10244243 140782 3 None - 1 Human 7.5 pKi = 7.5 Binding
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 258 1 1 3 1.3 Cc1cccc2[nH]c(C(=O)N3CCN(C)CC3)nc12 10.1021/jm0502081
CHEMBL383384 140782 3 None - 1 Human 7.5 pKi = 7.5 Binding
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 258 1 1 3 1.3 Cc1cccc2[nH]c(C(=O)N3CCN(C)CC3)nc12 10.1021/jm0502081
73353369 89283 0 None - 1 Human 7.5 pKi = 7.5 Binding
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 244 1 1 6 0.4 CN1CCN(c2nc(N)nc3cccnc23)CC1 10.1016/j.bmcl.2013.02.091
CHEMBL2376788 89283 0 None - 1 Human 7.5 pKi = 7.5 Binding
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 244 1 1 6 0.4 CN1CCN(c2nc(N)nc3cccnc23)CC1 10.1016/j.bmcl.2013.02.091
11846636 77598 0 None - 1 Human 7.5 pKi = 7.5 Binding
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 345 0 0 4 3.9 CN1CCN(C2=Nc3ccc(Cl)cc3Oc3c(F)cccc32)CC1 10.1021/jm051008s
CHEMBL209628 77598 0 None - 1 Human 7.5 pKi = 7.5 Binding
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 345 0 0 4 3.9 CN1CCN(C2=Nc3ccc(Cl)cc3Oc3c(F)cccc32)CC1 10.1021/jm051008s
155513612 175746 0 None -1 4 Mouse 7.5 pKi = 7.5 Binding
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 4 1 5 2.1 CN(C)[C@@H]1CCN(c2ccnc(NCC(C)(C)C)n2)C1 10.1021/acs.jmedchem.0c00160
CHEMBL4439142 175746 0 None -1 4 Mouse 7.5 pKi = 7.5 Binding
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 4 1 5 2.1 CN(C)[C@@H]1CCN(c2ccnc(NCC(C)(C)C)n2)C1 10.1021/acs.jmedchem.0c00160
CHEMBL4515149 175746 0 None -1 4 Mouse 7.5 pKi = 7.5 Binding
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 4 1 5 2.1 CN(C)[C@@H]1CCN(c2ccnc(NCC(C)(C)C)n2)C1 10.1021/acs.jmedchem.0c00160
CHEMBL4595327 175746 0 None -1 4 Mouse 7.5 pKi = 7.5 Binding
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 4 1 5 2.1 CN(C)[C@@H]1CCN(c2ccnc(NCC(C)(C)C)n2)C1 10.1021/acs.jmedchem.0c00160
206876 18756 7 None - 1 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]- histamine from the recombinant human histamine H4 receptorDisplacement of [3H]- histamine from the recombinant human histamine H4 receptor
ChEMBL 273 2 1 3 1.6 COc1ccc2[nH]c(C(=O)N3CCN(C)CC3)cc2c1 10.1021/jm0341047
CHEMBL128637 18756 7 None - 1 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]- histamine from the recombinant human histamine H4 receptorDisplacement of [3H]- histamine from the recombinant human histamine H4 receptor
ChEMBL 273 2 1 3 1.6 COc1ccc2[nH]c(C(=O)N3CCN(C)CC3)cc2c1 10.1021/jm0341047
206876 18756 7 None - 1 Human 5.5 pKi = 5.5 Binding
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 273 2 1 3 1.6 COc1ccc2[nH]c(C(=O)N3CCN(C)CC3)cc2c1 10.1021/jm0502081
CHEMBL128637 18756 7 None - 1 Human 5.5 pKi = 5.5 Binding
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 273 2 1 3 1.6 COc1ccc2[nH]c(C(=O)N3CCN(C)CC3)cc2c1 10.1021/jm0502081
11249610 157424 0 None -6309 2 Human 4.5 pKi = 4.5 Binding
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 354 9 2 5 3.6 Nc1ccc(NCCc2ccc(OCCCN3CCCCC3)cc2)nc1 10.1016/j.ejmech.2016.09.074
CHEMBL4084820 157424 0 None -6309 2 Human 4.5 pKi = 4.5 Binding
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 354 9 2 5 3.6 Nc1ccc(NCCc2ccc(OCCCN3CCCCC3)cc2)nc1 10.1016/j.ejmech.2016.09.074
137634777 155435 0 None - 1 Human 5.5 pKi = 5.5 Binding
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 453 8 3 6 1.0 CCOC(=O)CN1Cc2ccccc2C[C@@H](NC(=O)C(Cc2ccccc2)C(=O)NO)C1=O 10.1016/j.ejmech.2016.09.074
CHEMBL4061504 155435 0 None - 1 Human 5.5 pKi = 5.5 Binding
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 453 8 3 6 1.0 CCOC(=O)CN1Cc2ccccc2C[C@@H](NC(=O)C(Cc2ccccc2)C(=O)NO)C1=O 10.1016/j.ejmech.2016.09.074
164611474 184870 0 None -478 4 Human 4.5 pKi = 4.5 Binding
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 366 6 4 5 2.4 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NC(C)c1cccs1 10.1016/j.ejmech.2021.113190
CHEMBL4861704 184870 0 None -478 4 Human 4.5 pKi = 4.5 Binding
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 366 6 4 5 2.4 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NC(C)c1cccs1 10.1016/j.ejmech.2021.113190
164619427 185487 0 None -7 2 Human 4.5 pKi = 4.5 Binding
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 380 5 4 4 3.1 N/C(=N\C(=O)NCCc1ccccc1)Nc1cccc(-c2csc(N)n2)c1 10.1016/j.ejmech.2021.113190
CHEMBL4871221 185487 0 None -7 2 Human 4.5 pKi = 4.5 Binding
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 380 5 4 4 3.1 N/C(=N\C(=O)NCCc1ccccc1)Nc1cccc(-c2csc(N)n2)c1 10.1016/j.ejmech.2021.113190
164627774 185983 0 None -58 6 Human 4.5 pKi = 4.5 Binding
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 344 3 4 4 1.4 N/C(=N\C(=O)NCc1ccccc1)NC1CCc2nc(N)sc2C1 10.1016/j.ejmech.2021.113190
CHEMBL4878215 185983 0 None -58 6 Human 4.5 pKi = 4.5 Binding
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 344 3 4 4 1.4 N/C(=N\C(=O)NCc1ccccc1)NC1CCc2nc(N)sc2C1 10.1016/j.ejmech.2021.113190
24994634 2111 26 None -60 7 Guinea pig 6.5 pKi = 6.5 Binding
Binding affinity to guinea pig histamine H4 receptorBinding affinity to guinea pig histamine H4 receptor
ChEMBL 221 2 2 5 0.7 N[C@@H]1CCN(C1)c1cc(nc(n1)N)C(C)C 10.1021/jm401727m
8984 2111 26 None -60 7 Guinea pig 6.5 pKi = 6.5 Binding
Binding affinity to guinea pig histamine H4 receptorBinding affinity to guinea pig histamine H4 receptor
ChEMBL 221 2 2 5 0.7 N[C@@H]1CCN(C1)c1cc(nc(n1)N)C(C)C 10.1021/jm401727m
CHEMBL3236549 2111 26 None -60 7 Guinea pig 6.5 pKi = 6.5 Binding
Binding affinity to guinea pig histamine H4 receptorBinding affinity to guinea pig histamine H4 receptor
ChEMBL 221 2 2 5 0.7 N[C@@H]1CCN(C1)c1cc(nc(n1)N)C(C)C 10.1021/jm401727m
24994634 2111 26 None -60 7 Guinea pig 6.5 pKi = 6.5 Binding
Displacement of [3H]histamine from guinea pig recombinant histamine H4 receptorDisplacement of [3H]histamine from guinea pig 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 2111 26 None -60 7 Guinea pig 6.5 pKi = 6.5 Binding
Displacement of [3H]histamine from guinea pig recombinant histamine H4 receptorDisplacement of [3H]histamine from guinea pig 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 2111 26 None -60 7 Guinea pig 6.5 pKi = 6.5 Binding
Displacement of [3H]histamine from guinea pig recombinant histamine H4 receptorDisplacement of [3H]histamine from guinea pig 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
155552341 175810 0 None -1 2 Human 6.5 pKi = 6.5 Binding
Displacement of 40 nM [3H]-histamine from human H4R expressed in Sf9 cell membranes co-expressing Gia2 and beta1gamma2 by competition binding assayDisplacement of 40 nM [3H]-histamine from human H4R expressed in Sf9 cell membranes co-expressing Gia2 and beta1gamma2 by competition binding assay
ChEMBL 249 4 3 5 1.7 CC(C)(C)CNc1nccc(NC2CCNC2)n1 10.1021/acs.jmedchem.9b01342
CHEMBL4543928 175810 0 None -1 2 Human 6.5 pKi = 6.5 Binding
Displacement of 40 nM [3H]-histamine from human H4R expressed in Sf9 cell membranes co-expressing Gia2 and beta1gamma2 by competition binding assayDisplacement of 40 nM [3H]-histamine from human H4R expressed in Sf9 cell membranes co-expressing Gia2 and beta1gamma2 by competition binding assay
ChEMBL 249 4 3 5 1.7 CC(C)(C)CNc1nccc(NC2CCNC2)n1 10.1021/acs.jmedchem.9b01342
CHEMBL4595906 175810 0 None -1 2 Human 6.5 pKi = 6.5 Binding
Displacement of 40 nM [3H]-histamine from human H4R expressed in Sf9 cell membranes co-expressing Gia2 and beta1gamma2 by competition binding assayDisplacement of 40 nM [3H]-histamine from human H4R expressed in Sf9 cell membranes co-expressing Gia2 and beta1gamma2 by competition binding assay
ChEMBL 249 4 3 5 1.7 CC(C)(C)CNc1nccc(NC2CCNC2)n1 10.1021/acs.jmedchem.9b01342
44129283 199342 0 None - 1 Human 6.5 pKi = 6.5 Binding
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)c3ccc(Cl)c(Cl)c3n2)CC1 10.1021/jm901379s
CHEMBL602330 199342 0 None - 1 Human 6.5 pKi = 6.5 Binding
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)c3ccc(Cl)c(Cl)c3n2)CC1 10.1021/jm901379s
11846299 138690 0 None - 1 Human 6.5 pKi = 6.5 Binding
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 361 0 0 4 4.4 CN1CCN(C2=Nc3cc(Cl)ccc3Oc3cc(Cl)ccc32)CC1 10.1021/jm051008s
CHEMBL378788 138690 0 None - 1 Human 6.5 pKi = 6.5 Binding
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 361 0 0 4 4.4 CN1CCN(C2=Nc3cc(Cl)ccc3Oc3cc(Cl)ccc32)CC1 10.1021/jm051008s
10934567 19062 1 None - 1 Human 7.5 pKi = 7.5 Binding
Antagonist activity at Homo sapiens (human) histamine H4 receptorAntagonist activity at Homo sapiens (human) histamine H4 receptor
ChEMBL 271 1 1 2 2.2 Cc1cc(C)c2[nH]c(C(=O)N3CCN(C)CC3)cc2c1 10.1007/s00044-004-0106-7
CHEMBL129026 19062 1 None - 1 Human 7.5 pKi = 7.5 Binding
Antagonist activity at Homo sapiens (human) histamine H4 receptorAntagonist activity at Homo sapiens (human) histamine H4 receptor
ChEMBL 271 1 1 2 2.2 Cc1cc(C)c2[nH]c(C(=O)N3CCN(C)CC3)cc2c1 10.1007/s00044-004-0106-7
10934567 19062 1 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]- histamine from the recombinant human histamine H4 receptorDisplacement of [3H]- histamine from the recombinant human histamine H4 receptor
ChEMBL 271 1 1 2 2.2 Cc1cc(C)c2[nH]c(C(=O)N3CCN(C)CC3)cc2c1 10.1021/jm0341047
CHEMBL129026 19062 1 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]- histamine from the recombinant human histamine H4 receptorDisplacement of [3H]- histamine from the recombinant human histamine H4 receptor
ChEMBL 271 1 1 2 2.2 Cc1cc(C)c2[nH]c(C(=O)N3CCN(C)CC3)cc2c1 10.1021/jm0341047
25128833 187818 30 None -4 3 Human 7.5 pKi = 7.5 Binding
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 193 1 1 5 -0.2 CN1CCN(c2ccnc(N)n2)CC1 10.1016/j.bmcl.2011.10.104
CHEMBL501882 187818 30 None -4 3 Human 7.5 pKi = 7.5 Binding
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 193 1 1 5 -0.2 CN1CCN(c2ccnc(N)n2)CC1 10.1016/j.bmcl.2011.10.104
24826354 67798 0 None - 1 Human 7.5 pKi = 7.5 Binding
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)nc3c2sc2ccc(F)cc23)C1 10.1016/j.bmcl.2011.08.014
CHEMBL1914790 67798 0 None - 1 Human 7.5 pKi = 7.5 Binding
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)nc3c2sc2ccc(F)cc23)C1 10.1016/j.bmcl.2011.08.014
10934567 19062 1 None - 1 Human 7.5 pKi = 7.5 Binding
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 271 1 1 2 2.2 Cc1cc(C)c2[nH]c(C(=O)N3CCN(C)CC3)cc2c1 10.1021/jm0502081
CHEMBL129026 19062 1 None - 1 Human 7.5 pKi = 7.5 Binding
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 271 1 1 2 2.2 Cc1cc(C)c2[nH]c(C(=O)N3CCN(C)CC3)cc2c1 10.1021/jm0502081
16006947 138528 0 None 1 2 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]histamine form human H4 receptorDisplacement of [3H]histamine form human H4 receptor
ChEMBL 247 6 2 2 3.1 c1nc([C@@H]2C[C@H]2CCNCC2CCCCC2)c[nH]1 10.1021/jm0603318
CHEMBL378619 138528 0 None 1 2 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]histamine form human H4 receptorDisplacement of [3H]histamine form human H4 receptor
ChEMBL 247 6 2 2 3.1 c1nc([C@@H]2C[C@H]2CCNCC2CCCCC2)c[nH]1 10.1021/jm0603318
136030655 56188 0 None -3 3 Human 7.5 pKi = 7.5 Binding
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 292 1 2 3 2.2 CN1CCN(/C(=N\O)c2cc3cc(Cl)ccc3[nH]2)CC1 10.1016/j.bmcl.2010.10.041
CHEMBL1632413 56188 0 None -3 3 Human 7.5 pKi = 7.5 Binding
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 292 1 2 3 2.2 CN1CCN(/C(=N\O)c2cc3cc(Cl)ccc3[nH]2)CC1 10.1016/j.bmcl.2010.10.041
9923162 18751 5 None 199 2 Human 7.5 pKi = 7.5 Binding
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 321 1 1 2 2.3 CN1CCN(C(=O)c2cc3cc(Br)ccc3[nH]2)CC1 10.1016/j.bmcl.2004.08.035
CHEMBL128613 18751 5 None 199 2 Human 7.5 pKi = 7.5 Binding
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 321 1 1 2 2.3 CN1CCN(C(=O)c2cc3cc(Br)ccc3[nH]2)CC1 10.1016/j.bmcl.2004.08.035
170389 205253 31 None 1 3 Human 7.5 pKi = 7.5 Binding
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 125 3 2 2 0.3 NCCCc1c[nH]cn1 10.1021/acs.jmedchem.0c00160
CHEMBL4634086 205253 31 None 1 3 Human 7.5 pKi = 7.5 Binding
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 125 3 2 2 0.3 NCCCc1c[nH]cn1 10.1021/acs.jmedchem.0c00160
CHEMBL91353 205253 31 None 1 3 Human 7.5 pKi = 7.5 Binding
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 125 3 2 2 0.3 NCCCc1c[nH]cn1 10.1021/acs.jmedchem.0c00160
1274 4001 12 None 19 2 Human 7.5 pKi = 7.5 Binding
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 161 3 4 3 -1.1 NC(=N)SCCN=C(N)N 10.1016/j.bmcl.2010.10.041
3063228 4001 12 None 19 2 Human 7.5 pKi = 7.5 Binding
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 161 3 4 3 -1.1 NC(=N)SCCN=C(N)N 10.1016/j.bmcl.2010.10.041
CHEMBL1196470 4001 12 None 19 2 Human 7.5 pKi = 7.5 Binding
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 161 3 4 3 -1.1 NC(=N)SCCN=C(N)N 10.1016/j.bmcl.2010.10.041
170389 205253 31 None 1 3 Human 7.5 pKi = 7.5 Binding
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 125 3 2 2 0.3 NCCCc1c[nH]cn1 10.1016/j.bmcl.2010.10.041
CHEMBL4634086 205253 31 None 1 3 Human 7.5 pKi = 7.5 Binding
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 125 3 2 2 0.3 NCCCc1c[nH]cn1 10.1016/j.bmcl.2010.10.041
CHEMBL91353 205253 31 None 1 3 Human 7.5 pKi = 7.5 Binding
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 125 3 2 2 0.3 NCCCc1c[nH]cn1 10.1016/j.bmcl.2010.10.041
71681808 89218 0 None - 1 Human 7.5 pKi = 7.5 Binding
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 392 9 3 8 3.1 CC(C)CNc1nccc(NCCN(C)c2cc(-c3ccccc3)nc(N)n2)n1 10.1021/jm301886t
CHEMBL2375748 89218 0 None - 1 Human 7.5 pKi = 7.5 Binding
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 392 9 3 8 3.1 CC(C)CNc1nccc(NCCN(C)c2cc(-c3ccccc3)nc(N)n2)n1 10.1021/jm301886t
1274 4001 12 None 19 2 Human 7.5 pKi = 7.5 Binding
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 161 3 4 3 -1.1 NC(=N)SCCN=C(N)N 10.1021/jm201042n
3063228 4001 12 None 19 2 Human 7.5 pKi = 7.5 Binding
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 161 3 4 3 -1.1 NC(=N)SCCN=C(N)N 10.1021/jm201042n
CHEMBL1196470 4001 12 None 19 2 Human 7.5 pKi = 7.5 Binding
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 161 3 4 3 -1.1 NC(=N)SCCN=C(N)N 10.1021/jm201042n
56851608 71286 0 None -1 2 Human 7.5 pKi = 7.5 Binding
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 334 6 2 3 4.3 c1nc(CCCS/C(=N\C2CCCC2)NC2CCCCC2)c[nH]1 10.1021/jm201042n
CHEMBL1923030 71286 0 None -1 2 Human 7.5 pKi = 7.5 Binding
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 334 6 2 3 4.3 c1nc(CCCS/C(=N\C2CCCC2)NC2CCCCC2)c[nH]1 10.1021/jm201042n
CHEMBL1963461 71286 0 None -1 2 Human 7.5 pKi = 7.5 Binding
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 334 6 2 3 4.3 c1nc(CCCS/C(=N\C2CCCC2)NC2CCCCC2)c[nH]1 10.1021/jm201042n
1274 4001 12 None 19 2 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]histamine from human histamine H4 receptorDisplacement of [3H]histamine from human histamine H4 receptor
ChEMBL 161 3 4 3 -1.1 NC(=N)SCCN=C(N)N 10.1021/jm060880d
3063228 4001 12 None 19 2 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]histamine from human histamine H4 receptorDisplacement of [3H]histamine from human histamine H4 receptor
ChEMBL 161 3 4 3 -1.1 NC(=N)SCCN=C(N)N 10.1021/jm060880d
CHEMBL1196470 4001 12 None 19 2 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]histamine from human histamine H4 receptorDisplacement of [3H]histamine from human histamine H4 receptor
ChEMBL 161 3 4 3 -1.1 NC(=N)SCCN=C(N)N 10.1021/jm060880d
1278 2119 79 None -3 8 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]histamine from human histamine H4 receptor E182'5.46Q mutant transfected in HEK293T cells after 1.5 hrs by liquid scintillation counting analysisDisplacement of [3H]histamine from human histamine H4 receptor E182'5.46Q mutant transfected in HEK293T cells after 1.5 hrs by liquid scintillation counting analysis
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1039/C2MD20212C
1279 2119 79 None -3 8 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]histamine from human histamine H4 receptor E182'5.46Q mutant transfected in HEK293T cells after 1.5 hrs by liquid scintillation counting analysisDisplacement of [3H]histamine from human histamine H4 receptor E182'5.46Q mutant transfected in HEK293T cells after 1.5 hrs by liquid scintillation counting analysis
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1039/C2MD20212C
4908365 2119 79 None -3 8 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]histamine from human histamine H4 receptor E182'5.46Q mutant transfected in HEK293T cells after 1.5 hrs by liquid scintillation counting analysisDisplacement of [3H]histamine from human histamine H4 receptor E182'5.46Q mutant transfected in HEK293T cells after 1.5 hrs by liquid scintillation counting analysis
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1039/C2MD20212C
CHEMBL129198 2119 79 None -3 8 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]histamine from human histamine H4 receptor E182'5.46Q mutant transfected in HEK293T cells after 1.5 hrs by liquid scintillation counting analysisDisplacement of [3H]histamine from human histamine H4 receptor E182'5.46Q mutant transfected in HEK293T cells after 1.5 hrs by liquid scintillation counting analysis
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1039/C2MD20212C
66572105 75285 2 None - 1 Human 7.5 pKi = 7.5 Binding
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 261 1 1 2 1.7 CN1CCN(C(=O)c2cc3c(F)cccc3[nH]2)CC1 10.1016/j.ejmech.2012.06.016
CHEMBL2047263 75285 2 None - 1 Human 7.5 pKi = 7.5 Binding
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 261 1 1 2 1.7 CN1CCN(C(=O)c2cc3c(F)cccc3[nH]2)CC1 10.1016/j.ejmech.2012.06.016
66572106 75286 1 None - 1 Human 7.5 pKi = 7.5 Binding
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 2 2.2 CN1CCN(C(=O)c2cc3c(Cl)cccc3[nH]2)CC1 10.1016/j.ejmech.2012.06.016
CHEMBL2047264 75286 1 None - 1 Human 7.5 pKi = 7.5 Binding
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 2 2.2 CN1CCN(C(=O)c2cc3c(Cl)cccc3[nH]2)CC1 10.1016/j.ejmech.2012.06.016
66573463 75319 0 None - 1 Human 7.5 pKi = 7.5 Binding
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 317 2 1 2 3.1 Cc1cc(Cl)cc2cc(C(=O)N3CC(N4CCCC4)C3)[nH]c12 10.1016/j.ejmech.2012.06.016
CHEMBL2047454 75319 0 None - 1 Human 7.5 pKi = 7.5 Binding
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 317 2 1 2 3.1 Cc1cc(Cl)cc2cc(C(=O)N3CC(N4CCCC4)C3)[nH]c12 10.1016/j.ejmech.2012.06.016
70696622 75334 0 None - 1 Human 7.5 pKi = 7.5 Binding
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 309 1 1 2 2.7 CN1CCCN(C(=O)c2cc3c(F)c(Cl)ccc3[nH]2)CC1 10.1016/j.ejmech.2012.06.016
CHEMBL2047469 75334 0 None - 1 Human 7.5 pKi = 7.5 Binding
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 309 1 1 2 2.7 CN1CCCN(C(=O)c2cc3c(F)c(Cl)ccc3[nH]2)CC1 10.1016/j.ejmech.2012.06.016
10988959 117605 4 None - 1 Human 7.5 pKi = 7.5 Binding
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 1 2 3 1.1 CN1CCN(C(=O)c2cc3cc(N)ccc3[nH]2)CC1 10.1016/j.ejmech.2012.06.016
CHEMBL340740 117605 4 None - 1 Human 7.5 pKi = 7.5 Binding
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 1 2 3 1.1 CN1CCN(C(=O)c2cc3cc(N)ccc3[nH]2)CC1 10.1016/j.ejmech.2012.06.016
10087533 194336 0 None -3 2 Human 7.5 pKi = 7.5 Binding
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 322 7 3 3 3.5 N=C(NCCc1ccc(Cl)cc1)SCCCc1c[nH]cn1 10.1016/j.bmc.2009.04.007
CHEMBL1202322 194336 0 None -3 2 Human 7.5 pKi = 7.5 Binding
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 322 7 3 3 3.5 N=C(NCCc1ccc(Cl)cc1)SCCCc1c[nH]cn1 10.1016/j.bmc.2009.04.007
CHEMBL560068 194336 0 None -3 2 Human 7.5 pKi = 7.5 Binding
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 322 7 3 3 3.5 N=C(NCCc1ccc(Cl)cc1)SCCCc1c[nH]cn1 10.1016/j.bmc.2009.04.007
46929648 16580 0 None -6 3 Human 6.5 pKi = 6.5 Binding
Binding affinity to human histamine H4 receptorBinding affinity to human histamine H4 receptor
ChEMBL 355 5 2 3 4.3 FC(F)(F)c1ccc(SC[C@@H](c2c[nH]cn2)C2CCNCC2)cc1 10.1021/jm100643t
CHEMBL1243395 16580 0 None -6 3 Human 6.5 pKi = 6.5 Binding
Binding affinity to human histamine H4 receptorBinding affinity to human histamine H4 receptor
ChEMBL 355 5 2 3 4.3 FC(F)(F)c1ccc(SC[C@@H](c2c[nH]cn2)C2CCNCC2)cc1 10.1021/jm100643t
137650793 156900 0 None -1096 2 Human 5.5 pKi = 5.5 Binding
Antagonist activity at human H4 receptor assessed as inhibition of imetit-induced GTPgamma[35S] binding after 30 mins by microbeta scintillation counting methodAntagonist activity at human H4 receptor assessed as inhibition of imetit-induced GTPgamma[35S] binding after 30 mins by microbeta scintillation counting method
ChEMBL 484 7 1 4 4.5 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cncc(Br)c1 10.1016/j.ejmech.2016.09.074
CHEMBL4078910 156900 0 None -1096 2 Human 5.5 pKi = 5.5 Binding
Antagonist activity at human H4 receptor assessed as inhibition of imetit-induced GTPgamma[35S] binding after 30 mins by microbeta scintillation counting methodAntagonist activity at human H4 receptor assessed as inhibition of imetit-induced GTPgamma[35S] binding after 30 mins by microbeta scintillation counting method
ChEMBL 484 7 1 4 4.5 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cncc(Br)c1 10.1016/j.ejmech.2016.09.074
46912442 10803 0 None -575 2 Human 5.5 pKi = 5.5 Binding
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 271 4 1 3 2.9 COc1ccc(N2CCC(Cc3c[nH]cn3)CC2)cc1 10.1016/j.bmc.2010.04.052
CHEMBL1172775 10803 0 None -575 2 Human 5.5 pKi = 5.5 Binding
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 271 4 1 3 2.9 COc1ccc(N2CCC(Cc3c[nH]cn3)CC2)cc1 10.1016/j.bmc.2010.04.052
57392460 69523 0 None 14 2 Human 5.5 pKi = 5.5 Binding
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 244 1 1 3 1.0 CN1CCN(C(=O)c2cc3cccnc3[nH]2)CC1 10.1016/j.bmcl.2011.11.098
CHEMBL1938843 69523 0 None 14 2 Human 5.5 pKi = 5.5 Binding
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 244 1 1 3 1.0 CN1CCN(C(=O)c2cc3cccnc3[nH]2)CC1 10.1016/j.bmcl.2011.11.098
136192886 56186 0 None -6 4 Rat 6.5 pKi = 6.5 Binding
Binding affinity to rat histamine H4 receptor expressed in human SK-N-MC cells by radioligand displacement assayBinding affinity to rat 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 56186 0 None -6 4 Rat 6.5 pKi = 6.5 Binding
Binding affinity to rat histamine H4 receptor expressed in human SK-N-MC cells by radioligand displacement assayBinding affinity to rat 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
1248 1396 27 None -15 6 Human 6.5 pKi = 6.5 Binding
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 161 4 2 3 0.6 CN(CCCSC(=N)N)C 10.1016/j.bmcl.2010.10.041
3077 1396 27 None -15 6 Human 6.5 pKi = 6.5 Binding
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 161 4 2 3 0.6 CN(CCCSC(=N)N)C 10.1016/j.bmcl.2010.10.041
90045 1396 27 None -15 6 Human 6.5 pKi = 6.5 Binding
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 161 4 2 3 0.6 CN(CCCSC(=N)N)C 10.1016/j.bmcl.2010.10.041
CHEMBL12344 1396 27 None -15 6 Human 6.5 pKi = 6.5 Binding
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 161 4 2 3 0.6 CN(CCCSC(=N)N)C 10.1016/j.bmcl.2010.10.041
1239 2002 23 None -154 5 Human 6.5 pKi = 6.5 Binding
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 125 3 2 2 0.2 CNCCc1cnc[nH]1 10.1016/j.bmcl.2010.10.041
1240 2002 23 None -154 5 Human 6.5 pKi = 6.5 Binding
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 125 3 2 2 0.2 CNCCc1cnc[nH]1 10.1016/j.bmcl.2010.10.041
912 2002 23 None -154 5 Human 6.5 pKi = 6.5 Binding
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 125 3 2 2 0.2 CNCCc1cnc[nH]1 10.1016/j.bmcl.2010.10.041
CHEMBL268490 2002 23 None -154 5 Human 6.5 pKi = 6.5 Binding
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 125 3 2 2 0.2 CNCCc1cnc[nH]1 10.1016/j.bmcl.2010.10.041
71681976 89221 0 None - 1 Human 6.5 pKi = 6.5 Binding
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 5 4 5 2.0 Nc1nccc(NCCNC(=O)c2cc3cc(Cl)ccc3[nH]2)n1 10.1021/jm301886t
CHEMBL2375751 89221 0 None - 1 Human 6.5 pKi = 6.5 Binding
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 5 4 5 2.0 Nc1nccc(NCCNC(=O)c2cc3cc(Cl)ccc3[nH]2)n1 10.1021/jm301886t
10023327 168450 0 None -144 3 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]histamine from human H4 receptor N4.57Y mutant expressed in HEK293 cells after 1 to 1.5 hrs by scintillation countingDisplacement of [3H]histamine from human H4 receptor N4.57Y 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 168450 0 None -144 3 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]histamine from human H4 receptor N4.57Y mutant expressed in HEK293 cells after 1 to 1.5 hrs by scintillation countingDisplacement of [3H]histamine from human H4 receptor N4.57Y 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
11622672 74669 2 None -39 2 Human 6.5 pKi = 6.5 Binding
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 1 2 2.6 c1nc(CCCCCN2CCCCC2)c[nH]1 10.1021/jm0504353
CHEMBL203389 74669 2 None -39 2 Human 6.5 pKi = 6.5 Binding
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 1 2 2.6 c1nc(CCCCCN2CCCCC2)c[nH]1 10.1021/jm0504353
11679919 75190 0 None -39 2 Human 6.5 pKi = 6.5 Binding
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 181 7 2 2 1.7 CCNCCCCCc1c[nH]cn1 10.1021/jm0504353
CHEMBL204413 75190 0 None -39 2 Human 6.5 pKi = 6.5 Binding
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 181 7 2 2 1.7 CCNCCCCCc1c[nH]cn1 10.1021/jm0504353
11701199 75221 0 None -3 2 Human 6.5 pKi = 6.5 Binding
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 195 7 1 2 2.1 CCN(CC)CCCCc1c[nH]cn1 10.1021/jm0504353
CHEMBL204615 75221 0 None -3 2 Human 6.5 pKi = 6.5 Binding
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 195 7 1 2 2.1 CCN(CC)CCCCc1c[nH]cn1 10.1021/jm0504353
1248 1396 27 None -15 6 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]histamine from human histamine H4 receptorDisplacement of [3H]histamine from human histamine H4 receptor
ChEMBL 161 4 2 3 0.6 CN(CCCSC(=N)N)C 10.1021/jm060880d
3077 1396 27 None -15 6 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]histamine from human histamine H4 receptorDisplacement of [3H]histamine from human histamine H4 receptor
ChEMBL 161 4 2 3 0.6 CN(CCCSC(=N)N)C 10.1021/jm060880d
90045 1396 27 None -15 6 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]histamine from human histamine H4 receptorDisplacement of [3H]histamine from human histamine H4 receptor
ChEMBL 161 4 2 3 0.6 CN(CCCSC(=N)N)C 10.1021/jm060880d
CHEMBL12344 1396 27 None -15 6 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]histamine from human histamine H4 receptorDisplacement of [3H]histamine from human histamine H4 receptor
ChEMBL 161 4 2 3 0.6 CN(CCCSC(=N)N)C 10.1021/jm060880d
4060730 19183 51 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]histamine from human histamine H4 receptor L175'5.39V mutant transfected in HEK293T cells after 1.5 hrs by liquid scintillation counting analysisDisplacement of [3H]histamine from human histamine H4 receptor L175'5.39V mutant transfected in HEK293T cells after 1.5 hrs by liquid scintillation counting analysis
ChEMBL 243 1 1 2 1.6 CN1CCN(C(=O)c2cc3ccccc3[nH]2)CC1 10.1039/C2MD20212C
CHEMBL129199 19183 51 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]histamine from human histamine H4 receptor L175'5.39V mutant transfected in HEK293T cells after 1.5 hrs by liquid scintillation counting analysisDisplacement of [3H]histamine from human histamine H4 receptor L175'5.39V mutant transfected in HEK293T cells after 1.5 hrs by liquid scintillation counting analysis
ChEMBL 243 1 1 2 1.6 CN1CCN(C(=O)c2cc3ccccc3[nH]2)CC1 10.1039/C2MD20212C
10377814 75290 0 None - 1 Human 6.5 pKi = 6.5 Binding
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 1 2 3 1.1 CN1CCN(C(=O)c2cc3c(N)cccc3[nH]2)CC1 10.1016/j.ejmech.2012.06.016
CHEMBL2047268 75290 0 None - 1 Human 6.5 pKi = 6.5 Binding
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 1 2 3 1.1 CN1CCN(C(=O)c2cc3c(N)cccc3[nH]2)CC1 10.1016/j.ejmech.2012.06.016
1248 1396 27 None -15 6 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in human SK-N-MC cells after 1 hrDisplacement of [3H]histamine from human histamine H4 receptor expressed in human SK-N-MC cells after 1 hr
ChEMBL 161 4 2 3 0.6 CN(CCCSC(=N)N)C 10.1039/C2MD20212C
3077 1396 27 None -15 6 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in human SK-N-MC cells after 1 hrDisplacement of [3H]histamine from human histamine H4 receptor expressed in human SK-N-MC cells after 1 hr
ChEMBL 161 4 2 3 0.6 CN(CCCSC(=N)N)C 10.1039/C2MD20212C
90045 1396 27 None -15 6 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in human SK-N-MC cells after 1 hrDisplacement of [3H]histamine from human histamine H4 receptor expressed in human SK-N-MC cells after 1 hr
ChEMBL 161 4 2 3 0.6 CN(CCCSC(=N)N)C 10.1039/C2MD20212C
CHEMBL12344 1396 27 None -15 6 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in human SK-N-MC cells after 1 hrDisplacement of [3H]histamine from human histamine H4 receptor expressed in human SK-N-MC cells after 1 hr
ChEMBL 161 4 2 3 0.6 CN(CCCSC(=N)N)C 10.1039/C2MD20212C
4563101 66425 11 None 1 2 Human 5.5 pKi = 5.5 Binding
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 265 4 2 2 2.1 CN(C)CCNC(=O)c1cc2cc(Cl)ccc2[nH]1 10.1016/j.bmcl.2004.08.035
CHEMBL185842 66425 11 None 1 2 Human 5.5 pKi = 5.5 Binding
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 265 4 2 2 2.1 CN(C)CCNC(=O)c1cc2cc(Cl)ccc2[nH]1 10.1016/j.bmcl.2004.08.035
71681977 89222 0 None - 1 Human 5.5 pKi = 5.5 Binding
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 344 5 3 5 2.4 CN(CCNc1ccnc(N)n1)C(=O)c1cc2cc(Cl)ccc2[nH]1 10.1021/jm301886t
CHEMBL2375752 89222 0 None - 1 Human 5.5 pKi = 5.5 Binding
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 344 5 3 5 2.4 CN(CCNc1ccnc(N)n1)C(=O)c1cc2cc(Cl)ccc2[nH]1 10.1021/jm301886t
71681479 89230 0 None - 1 Human 5.5 pKi = 5.5 Binding
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 393 9 5 9 2.7 CC(C)CNc1cc(NCCNc2cc(-c3ccccc3)nc(N)n2)nc(N)n1 10.1021/jm301886t
CHEMBL2375760 89230 0 None - 1 Human 5.5 pKi = 5.5 Binding
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 393 9 5 9 2.7 CC(C)CNc1cc(NCCNc2cc(-c3ccccc3)nc(N)n2)nc(N)n1 10.1021/jm301886t
3063453 12663 1 None - 1 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]histamine from human histamine H4 receptorDisplacement of [3H]histamine from human histamine H4 receptor
ChEMBL 189 5 5 3 -0.1 N=C(N)NCCCCSC(=N)N 10.1021/jm060880d
CHEMBL1187950 12663 1 None - 1 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]histamine from human histamine H4 receptorDisplacement of [3H]histamine from human histamine H4 receptor
ChEMBL 189 5 5 3 -0.1 N=C(N)NCCCCSC(=N)N 10.1021/jm060880d
CHEMBL534498 12663 1 None - 1 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]histamine from human histamine H4 receptorDisplacement of [3H]histamine from human histamine H4 receptor
ChEMBL 189 5 5 3 -0.1 N=C(N)NCCCCSC(=N)N 10.1021/jm060880d
112936341 136949 1 None -12 2 Human 4.5 pKi = 4.5 Binding
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 359 5 1 5 3.5 CN1CCN(c2nc(NCc3ccccc3)cc(-c3ccccc3)n2)CC1 10.1016/j.bmcl.2015.12.035
CHEMBL3753849 136949 1 None -12 2 Human 4.5 pKi = 4.5 Binding
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 359 5 1 5 3.5 CN1CCN(c2nc(NCc3ccccc3)cc(-c3ccccc3)n2)CC1 10.1016/j.bmcl.2015.12.035
164628701 185885 0 None -186 3 Human 4.5 pKi = 4.5 Binding
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 338 5 4 4 1.9 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NC1CCCCC1 10.1016/j.ejmech.2021.113190
CHEMBL4876743 185885 0 None -186 3 Human 4.5 pKi = 4.5 Binding
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 338 5 4 4 1.9 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NC1CCCCC1 10.1016/j.ejmech.2021.113190
57402928 69522 0 None 9 2 Human 5.5 pKi = 5.5 Binding
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 278 1 0 4 1.4 CN1CCN(C(=O)c2cn3cc(Cl)ccc3n2)CC1 10.1016/j.bmcl.2011.11.098
CHEMBL1938842 69522 0 None 9 2 Human 5.5 pKi = 5.5 Binding
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 278 1 0 4 1.4 CN1CCN(C(=O)c2cn3cc(Cl)ccc3n2)CC1 10.1016/j.bmcl.2011.11.098
121238071 166687 0 None - 1 Human 5.5 pKi = 5.5 Binding
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 271 2 1 7 0.3 CN1CCN(c2nc(N)nc(-c3ccncc3)n2)CC1 10.1016/j.ejmech.2017.09.035
CHEMBL4292486 166687 0 None - 1 Human 5.5 pKi = 5.5 Binding
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 271 2 1 7 0.3 CN1CCN(c2nc(N)nc(-c3ccncc3)n2)CC1 10.1016/j.ejmech.2017.09.035
11120826 18730 1 None - 1 Human 7.5 pKi = 7.5 Binding
Antagonist activity at Homo sapiens (human) histamine H4 receptorAntagonist activity at Homo sapiens (human) histamine H4 receptor
ChEMBL 321 1 1 2 2.3 CN1CCN(C(=O)c2cc3c(Br)cccc3[nH]2)CC1 10.1007/s00044-004-0106-7
CHEMBL128505 18730 1 None - 1 Human 7.5 pKi = 7.5 Binding
Antagonist activity at Homo sapiens (human) histamine H4 receptorAntagonist activity at Homo sapiens (human) histamine H4 receptor
ChEMBL 321 1 1 2 2.3 CN1CCN(C(=O)c2cc3c(Br)cccc3[nH]2)CC1 10.1007/s00044-004-0106-7
11120826 18730 1 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]- histamine from the recombinant human histamine H4 receptorDisplacement of [3H]- histamine from the recombinant human histamine H4 receptor
ChEMBL 321 1 1 2 2.3 CN1CCN(C(=O)c2cc3c(Br)cccc3[nH]2)CC1 10.1021/jm0341047
CHEMBL128505 18730 1 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]- histamine from the recombinant human histamine H4 receptorDisplacement of [3H]- histamine from the recombinant human histamine H4 receptor
ChEMBL 321 1 1 2 2.3 CN1CCN(C(=O)c2cc3c(Br)cccc3[nH]2)CC1 10.1021/jm0341047
49841720 69380 0 None - 1 Human 7.5 pKi = 7.5 Binding
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 319 2 1 5 2.6 CN1CCN(c2nc(N)nc3c(-c4ccccc4)cccc23)CC1 10.1016/j.bmcl.2011.10.104
CHEMBL1935557 69380 0 None - 1 Human 7.5 pKi = 7.5 Binding
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 319 2 1 5 2.6 CN1CCN(c2nc(N)nc3c(-c4ccccc4)cccc23)CC1 10.1016/j.bmcl.2011.10.104
44275465 98764 2 None - 1 Human 7.5 pKi = 7.5 Binding
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 243 1 1 5 1.0 CN1CCN(c2nc(N)nc3ccccc23)CC1 10.1016/j.bmcl.2011.10.104
CHEMBL281590 98764 2 None - 1 Human 7.5 pKi = 7.5 Binding
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 243 1 1 5 1.0 CN1CCN(c2nc(N)nc3ccccc23)CC1 10.1016/j.bmcl.2011.10.104
46890545 7304 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
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 7304 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
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
11120826 18730 1 None - 1 Human 7.5 pKi = 7.5 Binding
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 321 1 1 2 2.3 CN1CCN(C(=O)c2cc3c(Br)cccc3[nH]2)CC1 10.1021/jm0502081
CHEMBL128505 18730 1 None - 1 Human 7.5 pKi = 7.5 Binding
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 321 1 1 2 2.3 CN1CCN(C(=O)c2cc3c(Br)cccc3[nH]2)CC1 10.1021/jm0502081
57399829 67988 1 None - 1 Human 7.5 pKi = 7.5 Binding
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 235 7 2 5 1.3 CN(C)CCNc1cc(NCC2CC2)ncn1 10.1016/j.bmcl.2011.07.114
CHEMBL1916505 67988 1 None - 1 Human 7.5 pKi = 7.5 Binding
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 235 7 2 5 1.3 CN(C)CCNc1cc(NCC2CC2)ncn1 10.1016/j.bmcl.2011.07.114
44126357 115415 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 235 3 2 5 1.0 CN[C@@H]1CCN(c2cc(N)nc(C(C)C)n2)C1 10.1016/j.bmcl.2014.10.013
CHEMBL3354813 115415 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 235 3 2 5 1.0 CN[C@@H]1CCN(c2cc(N)nc(C(C)C)n2)C1 10.1016/j.bmcl.2014.10.013
57393772 67835 0 None - 1 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 375 1 2 6 2.7 Nc1nc(N2C[C@@H]3C[C@H]2CN3)c2sc3cc(Br)ccc3c2n1 10.1016/j.bmcl.2011.08.014
CHEMBL1915041 67835 0 None - 1 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 375 1 2 6 2.7 Nc1nc(N2C[C@@H]3C[C@H]2CN3)c2sc3cc(Br)ccc3c2n1 10.1016/j.bmcl.2011.08.014
24854637 95872 0 None - 1 Human 6.5 pKi = 6.5 Binding
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 320 3 0 5 3.2 CN1CCN(c2nc3ccccc3nc2Oc2ccccc2)CC1 10.1021/jm7014217
CHEMBL261363 95872 0 None - 1 Human 6.5 pKi = 6.5 Binding
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 320 3 0 5 3.2 CN1CCN(c2nc3ccccc3nc2Oc2ccccc2)CC1 10.1021/jm7014217
11738520 138736 0 None - 1 Human 6.5 pKi = 6.5 Binding
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 313 0 1 4 3.4 Clc1ccc2c(c1)N=C(N1CCNCC1)c1ccccc1O2 10.1021/jm051008s
CHEMBL1794919 138736 0 None - 1 Human 6.5 pKi = 6.5 Binding
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 313 0 1 4 3.4 Clc1ccc2c(c1)N=C(N1CCNCC1)c1ccccc1O2 10.1021/jm051008s
CHEMBL379044 138736 0 None - 1 Human 6.5 pKi = 6.5 Binding
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 313 0 1 4 3.4 Clc1ccc2c(c1)N=C(N1CCNCC1)c1ccccc1O2 10.1021/jm051008s
60150162 173294 0 None -524 5 Human 5.5 pKi = 5.5 Binding
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 479 16 2 4 4.8 N=C(N)N(CCCCN1CCN(CCCCCCCOc2ccccc2)CC1)Cc1ccccc1 10.1039/C8MD00527C
CHEMBL4539444 173294 0 None -524 5 Human 5.5 pKi = 5.5 Binding
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 479 16 2 4 4.8 N=C(N)N(CCCCN1CCN(CCCCCCCOc2ccccc2)CC1)Cc1ccccc1 10.1039/C8MD00527C
164624107 185140 0 None -70 6 Human 5.5 pKi = 5.5 Binding
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 402 9 4 4 2.8 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCC(C)CCc1ccccc1 10.1016/j.ejmech.2021.113190
CHEMBL4865765 185140 0 None -70 6 Human 5.5 pKi = 5.5 Binding
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 402 9 4 4 2.8 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCC(C)CCc1ccccc1 10.1016/j.ejmech.2021.113190
164608941 183801 0 None -75 4 Human 4.5 pKi = 4.5 Binding
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 390 7 4 4 2.5 Cc1nc(N)sc1CCCN/C(N)=N/C(=S)NC[C@@H](C)c1ccccc1 10.1016/j.ejmech.2021.113190
CHEMBL4845733 183801 0 None -75 4 Human 4.5 pKi = 4.5 Binding
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 390 7 4 4 2.5 Cc1nc(N)sc1CCCN/C(N)=N/C(=S)NC[C@@H](C)c1ccccc1 10.1016/j.ejmech.2021.113190
57392890 67974 0 None -1 2 Human 5.5 pKi = 5.5 Binding
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 370 7 1 5 2.5 COc1cccc(C(O)(COc2ccccc2C)CN2CCN(C)CC2)c1 10.1016/j.bmcl.2011.07.114
CHEMBL1916492 67974 0 None -1 2 Human 5.5 pKi = 5.5 Binding
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 370 7 1 5 2.5 COc1cccc(C(O)(COc2ccccc2C)CN2CCN(C)CC2)c1 10.1016/j.bmcl.2011.07.114
21029584 188279 4 None - 1 Human 6.5 pKi = 6.5 Binding
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 228 1 0 4 1.4 CN1CCN(c2ncnc3ccccc23)CC1 10.1016/j.bmcl.2011.10.104
CHEMBL506969 188279 4 None - 1 Human 6.5 pKi = 6.5 Binding
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 228 1 0 4 1.4 CN1CCN(c2ncnc3ccccc23)CC1 10.1016/j.bmcl.2011.10.104
1267 3744 43 None -33 25 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in SK-NM-C cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in SK-NM-C cells
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1021/jm7014777
3035905 3744 43 None -33 25 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in SK-NM-C cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in SK-NM-C cells
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1021/jm7014777
CHEMBL260374 3744 43 None -33 25 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in SK-NM-C cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in SK-NM-C cells
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1021/jm7014777
90655029 109646 0 None - 1 Human 6.5 pKi = 6.5 Binding
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 273 2 2 5 1.4 Nc1nc(C2CCCC2)cc(N2C[C@@H]3CNC[C@@H]3C2)n1 10.1021/jm401727m
CHEMBL3236563 109646 0 None - 1 Human 6.5 pKi = 6.5 Binding
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 273 2 2 5 1.4 Nc1nc(C2CCCC2)cc(N2C[C@@H]3CNC[C@@H]3C2)n1 10.1021/jm401727m
71518862 86071 0 None - 1 Human 5.5 pKi = 5.5 Binding
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 342 2 2 5 2.6 CN1CCN(c2nc(N)nc3[nH]c(-c4ccc(Cl)cc4)cc23)CC1 10.1016/j.bmcl.2012.10.139
CHEMBL2314775 86071 0 None - 1 Human 5.5 pKi = 5.5 Binding
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 342 2 2 5 2.6 CN1CCN(c2nc(N)nc3[nH]c(-c4ccc(Cl)cc4)cc23)CC1 10.1016/j.bmcl.2012.10.139
44547567 116617 2 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 260 4 2 4 2.2 CN[C@H]1CCN(c2ccnc(NC3CCCC3)c2)C1 10.1016/j.bmcl.2014.12.027
CHEMBL3393533 116617 2 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 260 4 2 4 2.2 CN[C@H]1CCN(c2ccnc(NC3CCCC3)c2)C1 10.1016/j.bmcl.2014.12.027
24826163 67824 0 None - 1 Human 7.5 pKi = 7.5 Binding
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)nc3c2sc2cc(Cl)ccc23)C1 10.1016/j.bmcl.2011.08.014
CHEMBL1915020 67824 0 None - 1 Human 7.5 pKi = 7.5 Binding
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)nc3c2sc2cc(Cl)ccc23)C1 10.1016/j.bmcl.2011.08.014
57393773 67837 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 318 1 1 7 1.8 CN1CCN(c2nc(N)nc3c2oc2ncc(Cl)cc23)CC1 10.1016/j.bmcl.2011.08.014
CHEMBL1915044 67837 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 318 1 1 7 1.8 CN1CCN(c2nc(N)nc3c2oc2ncc(Cl)cc23)CC1 10.1016/j.bmcl.2011.08.014
11572877 66745 0 None - 1 Human 7.5 pKi = 7.5 Binding
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 291 1 1 2 2.5 Cc1cc(Cl)c2[nH]c(C(=O)N3CCN(C)CC3)cc2c1 10.1021/jm0502081
CHEMBL187285 66745 0 None - 1 Human 7.5 pKi = 7.5 Binding
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 291 1 1 2 2.5 Cc1cc(Cl)c2[nH]c(C(=O)N3CCN(C)CC3)cc2c1 10.1021/jm0502081
44129210 197804 0 None - 1 Human 7.5 pKi = 7.5 Binding
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 7 2 7 1.4 CNS(=O)(=O)CCCNc1nc(N2CCN(C)CC2)nc2ccc(Cl)cc12 10.1021/jm901379s
CHEMBL591711 197804 0 None - 1 Human 7.5 pKi = 7.5 Binding
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 7 2 7 1.4 CNS(=O)(=O)CCCNc1nc(N2CCN(C)CC2)nc2ccc(Cl)cc12 10.1021/jm901379s
156015638 177697 0 None -58 4 Human 7.5 pKi = 7.5 Binding
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 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 177697 0 None -58 4 Human 7.5 pKi = 7.5 Binding
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 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 177697 0 None -58 4 Human 7.5 pKi = 7.5 Binding
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 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
25179127 188491 0 None - 1 Human 7.5 pKi = 7.5 Binding
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 387 4 1 6 4.0 Cc1ccsc1CNc1nc(N2CCN(C)CC2)nc2ccc(Cl)cc12 10.1021/jm800876b
CHEMBL509852 188491 0 None - 1 Human 7.5 pKi = 7.5 Binding
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 387 4 1 6 4.0 Cc1ccsc1CNc1nc(N2CCN(C)CC2)nc2ccc(Cl)cc12 10.1021/jm800876b
25179127 188491 0 None - 1 Human 7.5 pKi = 7.5 Binding
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 387 4 1 6 4.0 Cc1ccsc1CNc1nc(N2CCN(C)CC2)nc2ccc(Cl)cc12 10.1021/jm901379s
CHEMBL509852 188491 0 None - 1 Human 7.5 pKi = 7.5 Binding
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 387 4 1 6 4.0 Cc1ccsc1CNc1nc(N2CCN(C)CC2)nc2ccc(Cl)cc12 10.1021/jm901379s
71518863 86072 0 None - 1 Human 5.5 pKi = 5.5 Binding
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 338 3 2 6 2.0 COc1ccc(-c2cc3c(N4CCN(C)CC4)nc(N)nc3[nH]2)cc1 10.1016/j.bmcl.2012.10.139
CHEMBL2314776 86072 0 None - 1 Human 5.5 pKi = 5.5 Binding
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 338 3 2 6 2.0 COc1ccc(-c2cc3c(N4CCN(C)CC4)nc(N)nc3[nH]2)cc1 10.1016/j.bmcl.2012.10.139
8070960 155151 10 None - 1 Human 6.5 pKi = 6.5 Binding
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 258 2 0 5 1.4 COc1nc2ccccc2nc1N1CCN(C)CC1 10.1021/jm7014217
CHEMBL405044 155151 10 None - 1 Human 6.5 pKi = 6.5 Binding
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 258 2 0 5 1.4 COc1nc2ccccc2nc1N1CCN(C)CC1 10.1021/jm7014217
25130576 187043 1 None -8 4 Rat 6.5 pKi = 6.5 Binding
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 280 2 2 6 1.0 N#Cc1ccc(-c2cc(N3CCNCC3)nc(N)n2)cc1 10.1021/jm8005959
25130576 187043 1 None -8 4 Rat 6.5 pKi = 6.5 Binding
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 280 2 2 6 1.0 N#Cc1ccc(-c2cc(N3CCNCC3)nc(N)n2)cc1 10.1021/jm800670r
CHEMBL494890 187043 1 None -8 4 Rat 6.5 pKi = 6.5 Binding
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 280 2 2 6 1.0 N#Cc1ccc(-c2cc(N3CCNCC3)nc(N)n2)cc1 10.1021/jm8005959
CHEMBL494890 187043 1 None -8 4 Rat 6.5 pKi = 6.5 Binding
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 280 2 2 6 1.0 N#Cc1ccc(-c2cc(N3CCNCC3)nc(N)n2)cc1 10.1021/jm800670r
86277887 123294 22 None - 1 Human 5.5 pKi = 5.5 Binding
GPCRScan assay: inhibition of H4GPCRScan assay: inhibition of H4
ChEMBL 802 18 0 11 7.4 COc1ccc(CC[C@@H](OC(=O)[C@@H]2CCCCN2C(=O)[C@H](c2cc(OC)c(OC)c(OC)c2)C2CCCCC2)c2cccc(OCCN3CCOCC3)c2)cc1OC 10.6019/CHEMBL5058648
CHEMBL3623630 123294 22 None - 1 Human 5.5 pKi = 5.5 Binding
GPCRScan assay: inhibition of H4GPCRScan assay: inhibition of H4
ChEMBL 802 18 0 11 7.4 COc1ccc(CC[C@@H](OC(=O)[C@@H]2CCCCN2C(=O)[C@H](c2cc(OC)c(OC)c(OC)c2)C2CCCCC2)c2cccc(OCCN3CCOCC3)c2)cc1OC 10.6019/CHEMBL5058648
168294445 192408 0 None -8 4 Human 5.5 pKi = 5.5 Binding
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 192408 0 None -8 4 Human 5.5 pKi = 5.5 Binding
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 192408 0 None -8 4 Human 5.5 pKi = 5.5 Binding
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
25130235 187004 1 None 1 11 Human 7.5 pKi = 7.5 Binding
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 294 2 1 6 1.3 CN1CCN(c2cc(-c3ccc(C#N)cc3)nc(N)n2)CC1 10.1021/jm8005959
25130235 187004 1 None 1 11 Human 7.5 pKi = 7.5 Binding
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 294 2 1 6 1.3 CN1CCN(c2cc(-c3ccc(C#N)cc3)nc(N)n2)CC1 10.1021/jm800670r
CHEMBL494678 187004 1 None 1 11 Human 7.5 pKi = 7.5 Binding
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 294 2 1 6 1.3 CN1CCN(c2cc(-c3ccc(C#N)cc3)nc(N)n2)CC1 10.1021/jm8005959
CHEMBL494678 187004 1 None 1 11 Human 7.5 pKi = 7.5 Binding
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 294 2 1 6 1.3 CN1CCN(c2cc(-c3ccc(C#N)cc3)nc(N)n2)CC1 10.1021/jm800670r
46228076 200415 0 None - 1 Human 5.5 pKi = 5.5 Binding
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 354 4 2 6 2.7 CN1CCN(c2cc(NCc3ccc(C(C)(C)C)cc3)nc(N)n2)CC1 10.1016/j.bmc.2009.08.059
CHEMBL608864 200415 0 None - 1 Human 5.5 pKi = 5.5 Binding
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 354 4 2 6 2.7 CN1CCN(c2cc(NCc3ccc(C(C)(C)C)cc3)nc(N)n2)CC1 10.1016/j.bmc.2009.08.059
46228158 200472 0 None - 1 Human 6.5 pKi = 6.5 Binding
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 323 4 2 7 1.3 CN1CCN(c2cc(NCc3ccc(C#N)cc3)nc(N)n2)CC1 10.1016/j.bmc.2009.08.059
CHEMBL609289 200472 0 None - 1 Human 6.5 pKi = 6.5 Binding
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 323 4 2 7 1.3 CN1CCN(c2cc(NCc3ccc(C#N)cc3)nc(N)n2)CC1 10.1016/j.bmc.2009.08.059
57402514 67833 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 375 1 2 6 2.7 Nc1nc(N2C[C@@H]3C[C@H]2CN3)c2sc3ccc(Br)cc3c2n1 10.1016/j.bmcl.2011.08.014
CHEMBL1915039 67833 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 375 1 2 6 2.7 Nc1nc(N2C[C@@H]3C[C@H]2CN3)c2sc3ccc(Br)cc3c2n1 10.1016/j.bmcl.2011.08.014
164619039 185566 0 None -17 2 Human 4.5 pKi = 4.5 Binding
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 366 4 4 4 3.0 N/C(=N\C(=O)NCc1ccccc1)Nc1cccc(-c2csc(N)n2)c1 10.1016/j.ejmech.2021.113190
CHEMBL4872277 185566 0 None -17 2 Human 4.5 pKi = 4.5 Binding
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 366 4 4 4 3.0 N/C(=N\C(=O)NCc1ccccc1)Nc1cccc(-c2csc(N)n2)c1 10.1016/j.ejmech.2021.113190
57392889 67973 0 None - 1 Human 4.5 pKi = 4.5 Binding
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 379 4 1 5 2.2 CN1CCN(c2cc(C(=O)NCc3cccc(C(F)(F)F)c3)ncn2)CC1 10.1016/j.bmcl.2011.07.114
CHEMBL1916491 67973 0 None - 1 Human 4.5 pKi = 4.5 Binding
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 379 4 1 5 2.2 CN1CCN(c2cc(C(=O)NCc3cccc(C(F)(F)F)c3)ncn2)CC1 10.1016/j.bmcl.2011.07.114
25130235 187004 1 None 1 11 Human 7.5 pKi = 7.5 Binding
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 294 2 1 6 1.3 CN1CCN(c2cc(-c3ccc(C#N)cc3)nc(N)n2)CC1 10.1021/jm800670r
CHEMBL494678 187004 1 None 1 11 Human 7.5 pKi = 7.5 Binding
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 294 2 1 6 1.3 CN1CCN(c2cc(-c3ccc(C#N)cc3)nc(N)n2)CC1 10.1021/jm800670r
57393774 67838 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 304 1 2 7 1.4 Nc1nc(N2CCNCC2)c2oc3ncc(Cl)cc3c2n1 10.1016/j.bmcl.2011.08.014
CHEMBL1915045 67838 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 304 1 2 7 1.4 Nc1nc(N2CCNCC2)c2oc3ncc(Cl)cc3c2n1 10.1016/j.bmcl.2011.08.014
10083188 140403 3 None - 1 Human 7.5 pKi = 7.5 Binding
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 244 1 1 3 1.0 CN1CCN(C(=O)c2nc3ccccc3[nH]2)CC1 10.1021/jm0502081
CHEMBL382276 140403 3 None - 1 Human 7.5 pKi = 7.5 Binding
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 244 1 1 3 1.0 CN1CCN(C(=O)c2nc3ccccc3[nH]2)CC1 10.1021/jm0502081
1278 2119 79 None -3 8 Human 7.5 pKi = 7.5 Binding
Binding affinity to histamine 4 receptor (unknown origin)Binding affinity to histamine 4 receptor (unknown origin)
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1016/j.bmcl.2015.12.035
1279 2119 79 None -3 8 Human 7.5 pKi = 7.5 Binding
Binding affinity to histamine 4 receptor (unknown origin)Binding affinity to histamine 4 receptor (unknown origin)
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1016/j.bmcl.2015.12.035
4908365 2119 79 None -3 8 Human 7.5 pKi = 7.5 Binding
Binding affinity to histamine 4 receptor (unknown origin)Binding affinity to histamine 4 receptor (unknown origin)
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1016/j.bmcl.2015.12.035
CHEMBL129198 2119 79 None -3 8 Human 7.5 pKi = 7.5 Binding
Binding affinity to histamine 4 receptor (unknown origin)Binding affinity to histamine 4 receptor (unknown origin)
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1016/j.bmcl.2015.12.035
71603137 89286 0 None 23 2 Human 7.5 pKi = 7.5 Binding
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 285 1 2 5 1.9 CC(C)(C)c1ccc2c(N3CCNCC3)nc(N)nc2c1 10.1016/j.bmcl.2013.02.091
CHEMBL2376791 89286 0 None 23 2 Human 7.5 pKi = 7.5 Binding
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 285 1 2 5 1.9 CC(C)(C)c1ccc2c(N3CCNCC3)nc(N)nc2c1 10.1016/j.bmcl.2013.02.091
25179125 188437 0 None - 1 Human 7.5 pKi = 7.5 Binding
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 373 4 1 6 3.7 CN1CCN(c2nc(NCc3ccsc3)c3cc(Cl)ccc3n2)CC1 10.1021/jm800876b
CHEMBL509142 188437 0 None - 1 Human 7.5 pKi = 7.5 Binding
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 373 4 1 6 3.7 CN1CCN(c2nc(NCc3ccsc3)c3cc(Cl)ccc3n2)CC1 10.1021/jm800876b
25179125 188437 0 None - 1 Human 7.5 pKi = 7.5 Binding
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 373 4 1 6 3.7 CN1CCN(c2nc(NCc3ccsc3)c3cc(Cl)ccc3n2)CC1 10.1021/jm901379s
CHEMBL509142 188437 0 None - 1 Human 7.5 pKi = 7.5 Binding
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 373 4 1 6 3.7 CN1CCN(c2nc(NCc3ccsc3)c3cc(Cl)ccc3n2)CC1 10.1021/jm901379s
127051047 139781 0 None 2 2 Human 5.5 pKi = 5.5 Binding
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
CHEMBL3806162 139781 0 None 2 2 Human 5.5 pKi = 5.5 Binding
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
7015108 198224 8 None - 1 Human 5.5 pKi = 5.5 Binding
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 343 3 0 7 1.7 CN1CCN(c2ncnc3c2nnn3Cc2ccc(Cl)cc2)CC1 10.1016/j.bmc.2009.08.059
CHEMBL594729 198224 8 None - 1 Human 5.5 pKi = 5.5 Binding
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 343 3 0 7 1.7 CN1CCN(c2ncnc3c2nnn3Cc2ccc(Cl)cc2)CC1 10.1016/j.bmc.2009.08.059
46228070 198043 0 None - 1 Human 4.5 pKi = 4.5 Binding
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 271 4 0 5 1.1 CN1CCN(Cc2cn(Cc3ccccc3)nn2)CC1 10.1016/j.bmc.2009.08.059
CHEMBL593448 198043 0 None - 1 Human 4.5 pKi = 4.5 Binding
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 271 4 0 5 1.1 CN1CCN(Cc2cn(Cc3ccccc3)nn2)CC1 10.1016/j.bmc.2009.08.059
122193100 123401 0 None - 1 Human 5.5 pKi = 5.5 Binding
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 314 3 1 6 1.5 CN1CCN(c2nc(N)nc(/C=C/c3cccc(F)c3)n2)CC1 10.1016/j.ejmech.2015.08.014
CHEMBL3628047 123401 0 None - 1 Human 5.5 pKi = 5.5 Binding
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 314 3 1 6 1.5 CN1CCN(c2nc(N)nc(/C=C/c3cccc(F)c3)n2)CC1 10.1016/j.ejmech.2015.08.014
155513612 175746 0 None 1 4 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-UR-DEBa176 from human H4R expressed in HEK293T-SF-His6-CRE-Luc cellsDisplacement of [3H]-UR-DEBa176 from human H4R expressed in HEK293T-SF-His6-CRE-Luc cells
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 175746 0 None 1 4 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-UR-DEBa176 from human H4R expressed in HEK293T-SF-His6-CRE-Luc cellsDisplacement of [3H]-UR-DEBa176 from human H4R expressed in HEK293T-SF-His6-CRE-Luc cells
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 175746 0 None 1 4 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-UR-DEBa176 from human H4R expressed in HEK293T-SF-His6-CRE-Luc cellsDisplacement of [3H]-UR-DEBa176 from human H4R expressed in HEK293T-SF-His6-CRE-Luc cells
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 175746 0 None 1 4 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-UR-DEBa176 from human H4R expressed in HEK293T-SF-His6-CRE-Luc cellsDisplacement of [3H]-UR-DEBa176 from human H4R expressed in HEK293T-SF-His6-CRE-Luc cells
ChEMBL 277 4 1 5 2.1 CN(C)[C@@H]1CCN(c2ccnc(NCC(C)(C)C)n2)C1 10.1021/acs.jmedchem.9b01342
127050018 140237 0 None - 1 Human 6.5 pKi = 6.5 Binding
Inhibition of histamine H4 receptor (unknown origin)Inhibition of histamine H4 receptor (unknown origin)
ChEMBL 221 2 2 5 0.5 CN[C@H]1CCN(c2nc(N)nc(C)c2C)C1 10.1039/C6MD00108D
CHEMBL3818402 140237 0 None - 1 Human 6.5 pKi = 6.5 Binding
Inhibition of histamine H4 receptor (unknown origin)Inhibition of histamine H4 receptor (unknown origin)
ChEMBL 221 2 2 5 0.5 CN[C@H]1CCN(c2nc(N)nc(C)c2C)C1 10.1039/C6MD00108D
24994950 109664 0 None - 1 Human 6.5 pKi = 6.5 Binding
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 0.5 CN[C@@H]1CCN(c2nc(N)nc(C)c2C)C1 10.1021/jm401727m
CHEMBL3236580 109664 0 None - 1 Human 6.5 pKi = 6.5 Binding
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 0.5 CN[C@@H]1CCN(c2nc(N)nc(C)c2C)C1 10.1021/jm401727m
54583875 61226 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]histamine from human histamine H4 receptorDisplacement of [3H]histamine from human histamine H4 receptor
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 61226 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]histamine from human histamine H4 receptorDisplacement of [3H]histamine from human histamine H4 receptor
ChEMBL 262 3 2 6 0.5 CN[C@@H]1CCN(c2cc(N3CCCC3)nc(N)n2)C1 10.1016/j.bmcl.2011.03.017
90655028 109640 0 None - 1 Human 7.4 pKi = 7.4 Binding
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
CHEMBL3236557 109640 0 None - 1 Human 7.4 pKi = 7.4 Binding
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
59777262 109655 0 None - 1 Human 7.4 pKi = 7.4 Binding
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 283 4 2 5 1.4 CN[C@@H]1CCN(c2cc(Cc3ccccc3)nc(N)n2)C1 10.1021/jm401727m
CHEMBL3236572 109655 0 None - 1 Human 7.4 pKi = 7.4 Binding
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 283 4 2 5 1.4 CN[C@@H]1CCN(c2cc(Cc3ccccc3)nc(N)n2)C1 10.1021/jm401727m
155512725 175667 0 None 154 2 Human 7.4 pKi = 7.4 Binding
Displacement of 40 nM [3H]-histamine from human H4R expressed in Sf9 cell membranes co-expressing Gia2 and beta1gamma2 by competition binding assayDisplacement of 40 nM [3H]-histamine from human H4R expressed in Sf9 cell membranes co-expressing Gia2 and beta1gamma2 by competition binding assay
ChEMBL 237 6 3 5 1.7 CC(C)(C)CNc1nccc(NCCCN)n1 10.1021/acs.jmedchem.9b01342
CHEMBL4437371 175667 0 None 154 2 Human 7.4 pKi = 7.4 Binding
Displacement of 40 nM [3H]-histamine from human H4R expressed in Sf9 cell membranes co-expressing Gia2 and beta1gamma2 by competition binding assayDisplacement of 40 nM [3H]-histamine from human H4R expressed in Sf9 cell membranes co-expressing Gia2 and beta1gamma2 by competition binding assay
ChEMBL 237 6 3 5 1.7 CC(C)(C)CNc1nccc(NCCCN)n1 10.1021/acs.jmedchem.9b01342
CHEMBL4594753 175667 0 None 154 2 Human 7.4 pKi = 7.4 Binding
Displacement of 40 nM [3H]-histamine from human H4R expressed in Sf9 cell membranes co-expressing Gia2 and beta1gamma2 by competition binding assayDisplacement of 40 nM [3H]-histamine from human H4R expressed in Sf9 cell membranes co-expressing Gia2 and beta1gamma2 by competition binding assay
ChEMBL 237 6 3 5 1.7 CC(C)(C)CNc1nccc(NCCCN)n1 10.1021/acs.jmedchem.9b01342
46929553 16574 0 None -5 2 Human 6.4 pKi = 6.4 Binding
Binding affinity to human histamine H4 receptorBinding affinity to human histamine H4 receptor
ChEMBL 337 5 1 3 5.0 CC(C)(C)c1ccc(SCC(c2cccnc2)c2c[nH]cn2)cc1 10.1021/jm100643t
CHEMBL1243366 16574 0 None -5 2 Human 6.4 pKi = 6.4 Binding
Binding affinity to human histamine H4 receptorBinding affinity to human histamine H4 receptor
ChEMBL 337 5 1 3 5.0 CC(C)(C)c1ccc(SCC(c2cccnc2)c2c[nH]cn2)cc1 10.1021/jm100643t
71519011 86037 0 None - 1 Human 4.4 pKi = 4.4 Binding
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 376 2 2 5 3.3 CN1CCN(c2nc(N)nc3[nH]c(-c4ccc(Cl)c(Cl)c4)cc23)CC1 10.1016/j.bmcl.2012.10.139
CHEMBL2314496 86037 0 None - 1 Human 4.4 pKi = 4.4 Binding
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 376 2 2 5 3.3 CN1CCN(c2nc(N)nc3[nH]c(-c4ccc(Cl)c(Cl)c4)cc23)CC1 10.1016/j.bmcl.2012.10.139
24826598 67827 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 313 2 2 7 1.9 COc1ccc2oc3c(N4CCC[C@H](N)C4)nc(N)nc3c2c1 10.1016/j.bmcl.2011.08.014
CHEMBL1915027 67827 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 313 2 2 7 1.9 COc1ccc2oc3c(N4CCC[C@H](N)C4)nc(N)nc3c2c1 10.1016/j.bmcl.2011.08.014
25178939 186267 0 None - 1 Human 6.4 pKi = 6.4 Binding
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 397 5 1 6 3.7 COc1ccc(CNc2nc(N3CCN(C)CC3)nc3ccc(Cl)cc23)cc1 10.1021/jm800876b
CHEMBL489464 186267 0 None - 1 Human 6.4 pKi = 6.4 Binding
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 397 5 1 6 3.7 COc1ccc(CNc2nc(N3CCN(C)CC3)nc3ccc(Cl)cc23)cc1 10.1021/jm800876b
24853529 95677 0 None - 1 Human 6.4 pKi = 6.4 Binding
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 336 3 0 5 3.5 CN1CCN(c2nc3ccccc3nc2Sc2ccccc2)CC1 10.1021/jm7014217
CHEMBL260388 95677 0 None - 1 Human 6.4 pKi = 6.4 Binding
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 336 3 0 5 3.5 CN1CCN(c2nc3ccccc3nc2Sc2ccccc2)CC1 10.1021/jm7014217
25178939 186267 0 None - 1 Human 6.4 pKi = 6.4 Binding
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 397 5 1 6 3.7 COc1ccc(CNc2nc(N3CCN(C)CC3)nc3ccc(Cl)cc23)cc1 10.1021/jm901379s
CHEMBL489464 186267 0 None - 1 Human 6.4 pKi = 6.4 Binding
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 397 5 1 6 3.7 COc1ccc(CNc2nc(N3CCN(C)CC3)nc3ccc(Cl)cc23)cc1 10.1021/jm901379s
164611757 184320 0 None -50 6 Human 5.4 pKi = 5.4 Binding
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 402 8 4 4 2.8 Cc1ccc(CC(C)CNC(=O)/N=C(\N)NCCCc2sc(N)nc2C)cc1 10.1016/j.ejmech.2021.113190
CHEMBL4853107 184320 0 None -50 6 Human 5.4 pKi = 5.4 Binding
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 402 8 4 4 2.8 Cc1ccc(CC(C)CNC(=O)/N=C(\N)NCCCc2sc(N)nc2C)cc1 10.1016/j.ejmech.2021.113190
112936357 136834 1 None -18 2 Human 4.4 pKi = 4.4 Binding
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 373 6 1 5 3.6 CN1CCN(c2nc(NCCc3ccccc3)cc(-c3ccccc3)n2)CC1 10.1016/j.bmcl.2015.12.035
CHEMBL3752978 136834 1 None -18 2 Human 4.4 pKi = 4.4 Binding
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 373 6 1 5 3.6 CN1CCN(c2nc(NCCc3ccccc3)cc(-c3ccccc3)n2)CC1 10.1016/j.bmcl.2015.12.035
71519346 86061 0 None - 1 Human 4.4 pKi = 4.4 Binding
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 232 1 2 6 -0.0 Cn1ccc2c(N3CCNCC3)nc(N)nc21 10.1016/j.bmcl.2012.10.139
CHEMBL2314764 86061 0 None - 1 Human 4.4 pKi = 4.4 Binding
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 232 1 2 6 -0.0 Cn1ccc2c(N3CCNCC3)nc(N)nc21 10.1016/j.bmcl.2012.10.139
58227144 116639 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 287 3 1 5 1.8 CN1CCN(c2cnnc(NC3CC4CCC3C4)c2)CC1 10.1016/j.bmcl.2014.12.027
CHEMBL3393555 116639 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 287 3 1 5 1.8 CN1CCN(c2cnnc(NC3CC4CCC3C4)c2)CC1 10.1016/j.bmcl.2014.12.027
57399018 67840 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 332 1 1 7 2.1 CN1CCCN(c2nc(N)nc3c2oc2ncc(Cl)cc23)CC1 10.1016/j.bmcl.2011.08.014
CHEMBL1915047 67840 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 332 1 1 7 2.1 CN1CCCN(c2nc(N)nc3c2oc2ncc(Cl)cc23)CC1 10.1016/j.bmcl.2011.08.014
16082831 79936 0 None -10 2 Human 7.4 pKi = 7.4 Binding
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
CHEMBL214311 79936 0 None -10 2 Human 7.4 pKi = 7.4 Binding
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
25178554 172855 0 None - 1 Human 6.4 pKi = 6.4 Binding
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 373 4 1 8 2.3 Cc1noc(CNc2nc(N3CCN(C)CC3)nc3ccc(Cl)cc23)n1 10.1021/jm800876b
CHEMBL452870 172855 0 None - 1 Human 6.4 pKi = 6.4 Binding
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 373 4 1 8 2.3 Cc1noc(CNc2nc(N3CCN(C)CC3)nc3ccc(Cl)cc23)n1 10.1021/jm800876b
25178554 172855 0 None - 1 Human 6.4 pKi = 6.4 Binding
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 373 4 1 8 2.3 Cc1noc(CNc2nc(N3CCN(C)CC3)nc3ccc(Cl)cc23)n1 10.1021/jm901379s
CHEMBL452870 172855 0 None - 1 Human 6.4 pKi = 6.4 Binding
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 373 4 1 8 2.3 Cc1noc(CNc2nc(N3CCN(C)CC3)nc3ccc(Cl)cc23)n1 10.1021/jm901379s
164610892 184615 0 None -52 6 Human 5.4 pKi = 5.4 Binding
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 394 8 4 4 3.2 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCC(C)CC1CCCCC1 10.1016/j.ejmech.2021.113190
CHEMBL4857560 184615 0 None -52 6 Human 5.4 pKi = 5.4 Binding
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 394 8 4 4 3.2 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCC(C)CC1CCCCC1 10.1016/j.ejmech.2021.113190
71518864 86073 0 None - 1 Human 5.4 pKi = 5.4 Binding
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 322 2 2 5 2.3 Cc1ccc(-c2cc3c(N4CCN(C)CC4)nc(N)nc3[nH]2)cc1 10.1016/j.bmcl.2012.10.139
CHEMBL2314777 86073 0 None - 1 Human 5.4 pKi = 5.4 Binding
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 322 2 2 5 2.3 Cc1ccc(-c2cc3c(N4CCN(C)CC4)nc(N)nc3[nH]2)cc1 10.1016/j.bmcl.2012.10.139
122194626 123504 0 None - 1 Human 4.4 pKi = 4.4 Binding
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 310 3 1 6 1.7 Cc1ccc(/C=C/c2nc(N)nc(N3CCN(C)CC3)n2)cc1 10.1016/j.ejmech.2015.08.014
CHEMBL3629829 123504 0 None - 1 Human 4.4 pKi = 4.4 Binding
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 310 3 1 6 1.7 Cc1ccc(/C=C/c2nc(N)nc(N3CCN(C)CC3)n2)cc1 10.1016/j.ejmech.2015.08.014
57399019 67844 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 304 2 2 7 1.4 NCC1CN(c2nc(N)nc3c2oc2ncc(Cl)cc23)C1 10.1016/j.bmcl.2011.08.014
CHEMBL1915051 67844 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 304 2 2 7 1.4 NCC1CN(c2nc(N)nc3c2oc2ncc(Cl)cc23)C1 10.1016/j.bmcl.2011.08.014
90645146 111685 0 None - 1 Human 6.4 pKi = 6.4 Binding
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 288 2 1 6 1.0 CN1CCN(c2nc(N)nc(-c3ccc(F)cc3)n2)CC1 10.1016/j.ejmech.2014.06.032
CHEMBL3290577 111685 0 None - 1 Human 6.4 pKi = 6.4 Binding
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 288 2 1 6 1.0 CN1CCN(c2nc(N)nc(-c3ccc(F)cc3)n2)CC1 10.1016/j.ejmech.2014.06.032
54584374 62794 0 None -6 2 Human 6.4 pKi = 6.4 Binding
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 7 2 3 1.6 C=CCCNC(=O)OCCCc1c[nH]cn1 10.1016/j.bmc.2011.03.046
CHEMBL1774590 62794 0 None -6 2 Human 6.4 pKi = 6.4 Binding
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 7 2 3 1.6 C=CCCNC(=O)OCCCc1c[nH]cn1 10.1016/j.bmc.2011.03.046
CHEMBL1789360 62794 0 None -6 2 Human 6.4 pKi = 6.4 Binding
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 7 2 3 1.6 C=CCCNC(=O)OCCCc1c[nH]cn1 10.1016/j.bmc.2011.03.046
122193105 123405 0 None - 1 Human 5.4 pKi = 5.4 Binding
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 346 3 1 6 2.5 CN1CCN(c2nc(N)nc(/C=C/c3ccc4ccccc4c3)n2)CC1 10.1016/j.ejmech.2015.08.014
CHEMBL3628051 123405 0 None - 1 Human 5.4 pKi = 5.4 Binding
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 346 3 1 6 2.5 CN1CCN(c2nc(N)nc(/C=C/c3ccc4ccccc4c3)n2)CC1 10.1016/j.ejmech.2015.08.014
921599 19255 44 None 234 2 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]- histamine from the recombinant human histamine H4 receptorDisplacement of [3H]- histamine from the recombinant human histamine H4 receptor
ChEMBL 229 1 2 2 1.2 O=C(c1cc2ccccc2[nH]1)N1CCNCC1 10.1021/jm0341047
CHEMBL129660 19255 44 None 234 2 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]- histamine from the recombinant human histamine H4 receptorDisplacement of [3H]- histamine from the recombinant human histamine H4 receptor
ChEMBL 229 1 2 2 1.2 O=C(c1cc2ccccc2[nH]1)N1CCNCC1 10.1021/jm0341047
921599 19255 44 None 234 2 Human 7.4 pKi = 7.4 Binding
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 229 1 2 2 1.2 O=C(c1cc2ccccc2[nH]1)N1CCNCC1 10.1021/jm0502081
CHEMBL129660 19255 44 None 234 2 Human 7.4 pKi = 7.4 Binding
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 229 1 2 2 1.2 O=C(c1cc2ccccc2[nH]1)N1CCNCC1 10.1021/jm0502081
4060730 19183 51 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]histamine human recombinant histamine H4 receptorDisplacement of [3H]histamine human recombinant histamine H4 receptor
ChEMBL 243 1 1 2 1.6 CN1CCN(C(=O)c2cc3ccccc3[nH]2)CC1 10.1016/j.bmcl.2010.02.097
CHEMBL129199 19183 51 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]histamine human recombinant histamine H4 receptorDisplacement of [3H]histamine human recombinant histamine H4 receptor
ChEMBL 243 1 1 2 1.6 CN1CCN(C(=O)c2cc3ccccc3[nH]2)CC1 10.1016/j.bmcl.2010.02.097
25178553 172854 0 None - 1 Human 7.4 pKi = 7.4 Binding
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 387 4 1 6 4.0 Cc1csc(CNc2nc(N3CCN(C)CC3)nc3ccc(Cl)cc23)c1 10.1021/jm800876b
CHEMBL452869 172854 0 None - 1 Human 7.4 pKi = 7.4 Binding
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 387 4 1 6 4.0 Cc1csc(CNc2nc(N3CCN(C)CC3)nc3ccc(Cl)cc23)c1 10.1021/jm800876b
25178553 172854 0 None - 1 Human 7.4 pKi = 7.4 Binding
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 387 4 1 6 4.0 Cc1csc(CNc2nc(N3CCN(C)CC3)nc3ccc(Cl)cc23)c1 10.1021/jm901379s
CHEMBL452869 172854 0 None - 1 Human 7.4 pKi = 7.4 Binding
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 387 4 1 6 4.0 Cc1csc(CNc2nc(N3CCN(C)CC3)nc3ccc(Cl)cc23)c1 10.1021/jm901379s
11846465 141400 0 None - 1 Human 7.4 pKi = 7.4 Binding
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 345 0 0 4 3.9 CN1CCN(C2=Nc3ccc(Cl)cc3Oc3cc(F)ccc32)CC1 10.1021/jm051008s
CHEMBL387054 141400 0 None - 1 Human 7.4 pKi = 7.4 Binding
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 345 0 0 4 3.9 CN1CCN(C2=Nc3ccc(Cl)cc3Oc3cc(F)ccc32)CC1 10.1021/jm051008s
56851606 71256 0 None -11 2 Human 6.4 pKi = 6.4 Binding
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 432 8 2 3 5.7 Clc1ccc(C/N=C(/NCc2ccccc2)SCCCc2c[nH]cn2)cc1Cl 10.1021/jm201042n
CHEMBL1923029 71256 0 None -11 2 Human 6.4 pKi = 6.4 Binding
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 432 8 2 3 5.7 Clc1ccc(C/N=C(/NCc2ccccc2)SCCCc2c[nH]cn2)cc1Cl 10.1021/jm201042n
CHEMBL1963244 71256 0 None -11 2 Human 6.4 pKi = 6.4 Binding
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 432 8 2 3 5.7 Clc1ccc(C/N=C(/NCc2ccccc2)SCCCc2c[nH]cn2)cc1Cl 10.1021/jm201042n
51354877 58601 0 None - 1 Human 6.4 pKi = 6.4 Binding
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 287 7 1 4 3.1 c1nc(CCCc2cn(CCC3CCCCC3)nn2)c[nH]1 10.1021/jm1013488
CHEMBL1688988 58601 0 None - 1 Human 6.4 pKi = 6.4 Binding
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 287 7 1 4 3.1 c1nc(CCCc2cn(CCC3CCCCC3)nn2)c[nH]1 10.1021/jm1013488
137658819 158763 0 None -7585 2 Human 5.4 pKi = 5.4 Binding
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 467 9 1 5 3.9 COc1cc2c(cc1OC)C(C)=C(C(=O)NCCCCN1CCN(c3ccccc3F)CC1)C2 10.1016/j.ejmech.2016.09.074
CHEMBL4099779 158763 0 None -7585 2 Human 5.4 pKi = 5.4 Binding
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 467 9 1 5 3.9 COc1cc2c(cc1OC)C(C)=C(C(=O)NCCCCN1CCN(c3ccccc3F)CC1)C2 10.1016/j.ejmech.2016.09.074
54584374 62794 0 None -6 2 Human 5.4 pKi = 5.4 Binding
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 223 7 2 3 1.6 C=CCCNC(=O)OCCCc1c[nH]cn1 10.1016/j.bmcl.2013.06.075
CHEMBL1774590 62794 0 None -6 2 Human 5.4 pKi = 5.4 Binding
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 223 7 2 3 1.6 C=CCCNC(=O)OCCCc1c[nH]cn1 10.1016/j.bmcl.2013.06.075
CHEMBL1789360 62794 0 None -6 2 Human 5.4 pKi = 5.4 Binding
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 223 7 2 3 1.6 C=CCCNC(=O)OCCCc1c[nH]cn1 10.1016/j.bmcl.2013.06.075
58227207 116635 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 249 5 2 5 1.3 CN[C@H]1CCN(c2cnnc(NCC(C)C)c2)C1 10.1016/j.bmcl.2014.12.027
CHEMBL3393551 116635 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 249 5 2 5 1.3 CN[C@H]1CCN(c2cnnc(NCC(C)C)c2)C1 10.1016/j.bmcl.2014.12.027
51354872 59883 0 None -323 2 Human 4.4 pKi = 4.4 Binding
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 291 6 0 5 2.1 c1c(CN2CCCCC2)nnn1CCCN1CCCCC1 10.1021/jm1013488
CHEMBL1688983 59883 0 None -323 2 Human 4.4 pKi = 4.4 Binding
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 291 6 0 5 2.1 c1c(CN2CCCCC2)nnn1CCCN1CCCCC1 10.1021/jm1013488
CHEMBL1739923 59883 0 None -323 2 Human 4.4 pKi = 4.4 Binding
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 291 6 0 5 2.1 c1c(CN2CCCCC2)nnn1CCCN1CCCCC1 10.1021/jm1013488
68081433 109634 0 None - 1 Human 7.4 pKi = 7.4 Binding
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 248 1 1 3 0.7 CN1CCN(C(=O)c2nc3c([nH]2)CCCC3)CC1 10.1021/jm401727m
CHEMBL3236551 109634 0 None - 1 Human 7.4 pKi = 7.4 Binding
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 248 1 1 3 0.7 CN1CCN(C(=O)c2nc3c([nH]2)CCCC3)CC1 10.1021/jm401727m
57399747 67795 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 319 2 2 6 2.0 CN[C@@H]1CCN(c2nc(N)nc3c2oc2ccc(F)c(F)c23)C1 10.1016/j.bmcl.2011.08.014
CHEMBL1914787 67795 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 319 2 2 6 2.0 CN[C@@H]1CCN(c2nc(N)nc3c2oc2ccc(F)c(F)c23)C1 10.1016/j.bmcl.2011.08.014
25129169 186598 0 None -8 4 Human 7.4 pKi = 7.4 Binding
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 323 2 2 5 2.3 Nc1nc2c(c(N3CCNCC3)n1)CCCCC2c1ccccc1 10.1021/jm800670r
CHEMBL492231 186598 0 None -8 4 Human 7.4 pKi = 7.4 Binding
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 323 2 2 5 2.3 Nc1nc2c(c(N3CCNCC3)n1)CCCCC2c1ccccc1 10.1021/jm800670r
25129169 186598 0 None -8 4 Human 7.4 pKi = 7.4 Binding
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 323 2 2 5 2.3 Nc1nc2c(c(N3CCNCC3)n1)CCCCC2c1ccccc1 10.1016/j.bmcl.2010.01.131
CHEMBL492231 186598 0 None -8 4 Human 7.4 pKi = 7.4 Binding
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 323 2 2 5 2.3 Nc1nc2c(c(N3CCNCC3)n1)CCCCC2c1ccccc1 10.1016/j.bmcl.2010.01.131
3032915 15321 20 None -1 6 Human 7.4 pKi = 7.4 Binding
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 212 5 3 2 1.2 C/N=C(\S)NCCCCc1c[nH]cn1 10.1016/j.bmcl.2010.10.041
CHEMBL12160 15321 20 None -1 6 Human 7.4 pKi = 7.4 Binding
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 212 5 3 2 1.2 C/N=C(\S)NCCCCc1c[nH]cn1 10.1016/j.bmcl.2010.10.041
71681806 89215 0 None - 1 Human 7.4 pKi = 7.4 Binding
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 331 8 4 9 1.0 CC(C)CNc1cc(N(C)CCNc2ccnc(N)n2)nc(N)n1 10.1021/jm301886t
CHEMBL2375667 89215 0 None - 1 Human 7.4 pKi = 7.4 Binding
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 331 8 4 9 1.0 CC(C)CNc1cc(N(C)CCNc2ccnc(N)n2)nc(N)n1 10.1021/jm301886t
71681639 89232 0 None - 1 Human 7.4 pKi = 7.4 Binding
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 321 6 3 7 2.3 Cc1nccc(NCCNc2cc(-c3ccccc3)nc(N)n2)n1 10.1021/jm301886t
CHEMBL2375762 89232 0 None - 1 Human 7.4 pKi = 7.4 Binding
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 321 6 3 7 2.3 Cc1nccc(NCCNc2cc(-c3ccccc3)nc(N)n2)n1 10.1021/jm301886t
11492393 3997 4 None -3 2 Human 7.4 pKi = 7.4 Binding
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 235 7 2 2 3.0 C(CCc1cnc[nH]1)CCNC1CCCCC1 10.1021/jm0504353
1263 3997 4 None -3 2 Human 7.4 pKi = 7.4 Binding
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 235 7 2 2 3.0 C(CCc1cnc[nH]1)CCNC1CCCCC1 10.1021/jm0504353
CHEMBL206346 3997 4 None -3 2 Human 7.4 pKi = 7.4 Binding
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 235 7 2 2 3.0 C(CCc1cnc[nH]1)CCNC1CCCCC1 10.1021/jm0504353
11557610 74098 0 None -10 2 Human 7.4 pKi = 7.4 Binding
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 7 2 2 2.7 c1nc(CCCCCNC2CCCC2)c[nH]1 10.1021/jm0504353
CHEMBL202744 74098 0 None -10 2 Human 7.4 pKi = 7.4 Binding
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 7 2 2 2.7 c1nc(CCCCCNC2CCCC2)c[nH]1 10.1021/jm0504353
11615406 138962 0 None -1 2 Human 7.4 pKi = 7.4 Binding
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 207 6 2 2 2.3 c1nc(CCCCNC2CCCC2)c[nH]1 10.1021/jm0504353
CHEMBL379447 138962 0 None -1 2 Human 7.4 pKi = 7.4 Binding
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 207 6 2 2 2.3 c1nc(CCCCNC2CCCC2)c[nH]1 10.1021/jm0504353
66572116 75308 1 None - 1 Human 7.4 pKi = 7.4 Binding
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 243 1 2 2 1.5 Cc1cccc2cc(C(=O)N3CCNCC3)[nH]c12 10.1016/j.ejmech.2012.06.016
CHEMBL2047443 75308 1 None - 1 Human 7.4 pKi = 7.4 Binding
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 243 1 2 2 1.5 Cc1cccc2cc(C(=O)N3CCNCC3)[nH]c12 10.1016/j.ejmech.2012.06.016
70681961 75320 2 None - 1 Human 7.4 pKi = 7.4 Binding
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 291 1 1 2 2.6 CN1CCCN(C(=O)c2cc3cc(Cl)ccc3[nH]2)CC1 10.1016/j.ejmech.2012.06.016
CHEMBL2047455 75320 2 None - 1 Human 7.4 pKi = 7.4 Binding
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 291 1 1 2 2.6 CN1CCCN(C(=O)c2cc3cc(Cl)ccc3[nH]2)CC1 10.1016/j.ejmech.2012.06.016
70696621 75327 0 None - 1 Human 7.4 pKi = 7.4 Binding
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 287 2 1 2 2.2 O=C(c1cc2cccc(F)c2[nH]1)N1CC(N2CCCC2)C1 10.1016/j.ejmech.2012.06.016
CHEMBL2047462 75327 0 None - 1 Human 7.4 pKi = 7.4 Binding
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 287 2 1 2 2.2 O=C(c1cc2cccc(F)c2[nH]1)N1CC(N2CCCC2)C1 10.1016/j.ejmech.2012.06.016
70692531 75340 0 None - 1 Human 7.4 pKi = 7.4 Binding
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 275 1 1 2 2.0 Cc1ccc(F)c2cc(C(=O)N3CCN(C)CC3)[nH]c12 10.1016/j.ejmech.2012.06.016
CHEMBL2047475 75340 0 None - 1 Human 7.4 pKi = 7.4 Binding
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 275 1 1 2 2.0 Cc1ccc(F)c2cc(C(=O)N3CCN(C)CC3)[nH]c12 10.1016/j.ejmech.2012.06.016
24759623 95902 16 None 18 2 Human 7.4 pKi = 7.4 Binding
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 318 3 0 4 3.0 CN1CCN(c2nc3ccccc3nc2Cc2ccccc2)CC1 10.1021/jm800876b
CHEMBL261551 95902 16 None 18 2 Human 7.4 pKi = 7.4 Binding
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 318 3 0 4 3.0 CN1CCN(c2nc3ccccc3nc2Cc2ccccc2)CC1 10.1021/jm800876b
25129169 186598 0 None -8 4 Human 7.4 pKi = 7.4 Binding
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 323 2 2 5 2.3 Nc1nc2c(c(N3CCNCC3)n1)CCCCC2c1ccccc1 10.1021/jm800670r
CHEMBL492231 186598 0 None -8 4 Human 7.4 pKi = 7.4 Binding
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 323 2 2 5 2.3 Nc1nc2c(c(N3CCNCC3)n1)CCCCC2c1ccccc1 10.1021/jm800670r
24759623 95902 16 None 18 2 Human 7.4 pKi = 7.4 Binding
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 318 3 0 4 3.0 CN1CCN(c2nc3ccccc3nc2Cc2ccccc2)CC1 10.1021/jm7014217
CHEMBL261551 95902 16 None 18 2 Human 7.4 pKi = 7.4 Binding
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 318 3 0 4 3.0 CN1CCN(c2nc3ccccc3nc2Cc2ccccc2)CC1 10.1021/jm7014217
10429016 194486 0 None -5 2 Human 7.4 pKi = 7.4 Binding
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 366 7 3 3 3.6 N=C(NCCc1ccc(Br)cc1)SCCCc1c[nH]cn1 10.1016/j.bmc.2009.04.007
CHEMBL561250 194486 0 None -5 2 Human 7.4 pKi = 7.4 Binding
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 366 7 3 3 3.6 N=C(NCCc1ccc(Br)cc1)SCCCc1c[nH]cn1 10.1016/j.bmc.2009.04.007
1223 940 32 None -60 11 Human 7.4 pKi = 7.4 Binding
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 308 6 2 3 3.2 Clc1ccc(cc1)CN=C(SCCCc1cnc[nH]1)N 10.1021/acs.jmedchem.0c00160
2790 940 32 None -60 11 Human 7.4 pKi = 7.4 Binding
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 308 6 2 3 3.2 Clc1ccc(cc1)CN=C(SCCCc1cnc[nH]1)N 10.1021/acs.jmedchem.0c00160
CHEMBL14690 940 32 None -60 11 Human 7.4 pKi = 7.4 Binding
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 308 6 2 3 3.2 Clc1ccc(cc1)CN=C(SCCCc1cnc[nH]1)N 10.1021/acs.jmedchem.0c00160
71519012 86038 0 None 218 2 Human 6.4 pKi = 6.4 Binding
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 312 2 3 5 1.8 Nc1nc(N2CCNCC2)c2cc(-c3ccc(F)cc3)[nH]c2n1 10.1016/j.bmcl.2012.10.139
CHEMBL2314497 86038 0 None 218 2 Human 6.4 pKi = 6.4 Binding
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 312 2 3 5 1.8 Nc1nc(N2CCNCC2)c2cc(-c3ccc(F)cc3)[nH]c2n1 10.1016/j.bmcl.2012.10.139
10934158 108090 1 None -1 2 Human 6.4 pKi = 6.4 Binding
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
CHEMBL320331 108090 1 None -1 2 Human 6.4 pKi = 6.4 Binding
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
71681478 89229 0 None - 1 Human 6.4 pKi = 6.4 Binding
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 392 9 4 8 3.2 CC(C)CCc1cc(NCCNc2cc(-c3ccccc3)nc(N)n2)nc(N)n1 10.1021/jm301886t
CHEMBL2375759 89229 0 None - 1 Human 6.4 pKi = 6.4 Binding
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 392 9 4 8 3.2 CC(C)CCc1cc(NCCNc2cc(-c3ccccc3)nc(N)n2)nc(N)n1 10.1021/jm301886t
11629829 75669 0 None -19 2 Human 6.4 pKi = 6.4 Binding
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 207 5 1 2 2.2 c1nc(CCCCN2CCCCC2)c[nH]1 10.1021/jm0504353
CHEMBL205583 75669 0 None -19 2 Human 6.4 pKi = 6.4 Binding
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 207 5 1 2 2.2 c1nc(CCCCN2CCCCC2)c[nH]1 10.1021/jm0504353
25831 12898 26 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]histamine from human histamine H4 receptorDisplacement of [3H]histamine from human histamine H4 receptor
ChEMBL 144 3 6 2 -2.0 N=C(N)NCCNC(=N)N 10.1021/jm060880d
CHEMBL1189742 12898 26 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]histamine from human histamine H4 receptorDisplacement of [3H]histamine from human histamine H4 receptor
ChEMBL 144 3 6 2 -2.0 N=C(N)NCCNC(=N)N 10.1021/jm060880d
CHEMBL539343 12898 26 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]histamine from human histamine H4 receptorDisplacement of [3H]histamine from human histamine H4 receptor
ChEMBL 144 3 6 2 -2.0 N=C(N)NCCNC(=N)N 10.1021/jm060880d
1278 2119 79 None -3 8 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]histamine from human histamine H4 receptor L175'5.39V mutant transfected in HEK293T cells after 1.5 hrs by liquid scintillation counting analysisDisplacement of [3H]histamine from human histamine H4 receptor L175'5.39V mutant transfected in HEK293T cells after 1.5 hrs by liquid scintillation counting analysis
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1039/C2MD20212C
1279 2119 79 None -3 8 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]histamine from human histamine H4 receptor L175'5.39V mutant transfected in HEK293T cells after 1.5 hrs by liquid scintillation counting analysisDisplacement of [3H]histamine from human histamine H4 receptor L175'5.39V mutant transfected in HEK293T cells after 1.5 hrs by liquid scintillation counting analysis
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1039/C2MD20212C
4908365 2119 79 None -3 8 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]histamine from human histamine H4 receptor L175'5.39V mutant transfected in HEK293T cells after 1.5 hrs by liquid scintillation counting analysisDisplacement of [3H]histamine from human histamine H4 receptor L175'5.39V mutant transfected in HEK293T cells after 1.5 hrs by liquid scintillation counting analysis
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1039/C2MD20212C
CHEMBL129198 2119 79 None -3 8 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]histamine from human histamine H4 receptor L175'5.39V mutant transfected in HEK293T cells after 1.5 hrs by liquid scintillation counting analysisDisplacement of [3H]histamine from human histamine H4 receptor L175'5.39V mutant transfected in HEK293T cells after 1.5 hrs by liquid scintillation counting analysis
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1039/C2MD20212C
66573456 75310 0 None - 1 Human 6.4 pKi = 6.4 Binding
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 243 2 2 2 1.5 CNC1CN(C(=O)c2cc3cccc(C)c3[nH]2)C1 10.1016/j.ejmech.2012.06.016
CHEMBL2047445 75310 0 None - 1 Human 6.4 pKi = 6.4 Binding
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 243 2 2 2 1.5 CNC1CN(C(=O)c2cc3cccc(C)c3[nH]2)C1 10.1016/j.ejmech.2012.06.016
43398194 75321 21 None - 1 Human 6.4 pKi = 6.4 Binding
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 CN1CCCN(C(=O)c2cc3ccccc3[nH]2)CC1 10.1016/j.ejmech.2012.06.016
CHEMBL2047456 75321 21 None - 1 Human 6.4 pKi = 6.4 Binding
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 CN1CCCN(C(=O)c2cc3ccccc3[nH]2)CC1 10.1016/j.ejmech.2012.06.016
70694582 75325 0 None - 1 Human 6.4 pKi = 6.4 Binding
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 275 1 1 2 2.1 CN1CCCN(C(=O)c2cc3cccc(F)c3[nH]2)CC1 10.1016/j.ejmech.2012.06.016
CHEMBL2047460 75325 0 None - 1 Human 6.4 pKi = 6.4 Binding
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 275 1 1 2 2.1 CN1CCCN(C(=O)c2cc3cccc(F)c3[nH]2)CC1 10.1016/j.ejmech.2012.06.016
70686223 75330 0 None - 1 Human 6.4 pKi = 6.4 Binding
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 2 2 2 1.4 CNC1CN(C(=O)c2cc3cccc(F)c3[nH]2)C1 10.1016/j.ejmech.2012.06.016
CHEMBL2047465 75330 0 None - 1 Human 6.4 pKi = 6.4 Binding
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 2 2 2 1.4 CNC1CN(C(=O)c2cc3cccc(F)c3[nH]2)C1 10.1016/j.ejmech.2012.06.016
70692530 75339 0 None - 1 Human 6.4 pKi = 6.4 Binding
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 322 2 1 4 2.1 CN1CCN(C(=O)c2cc3cc(Cl)cc([N+](=O)[O-])c3[nH]2)CC1 10.1016/j.ejmech.2012.06.016
CHEMBL2047474 75339 0 None - 1 Human 6.4 pKi = 6.4 Binding
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 322 2 1 4 2.1 CN1CCN(C(=O)c2cc3cc(Cl)cc([N+](=O)[O-])c3[nH]2)CC1 10.1016/j.ejmech.2012.06.016
1238 2051 11 None -19 3 Human 5.4 pKi = 5.4 Binding
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 125 2 2 2 0.3 C[C@@H](Cc1cnc[nH]1)N 10.1016/j.bmcl.2010.10.041
6603865 2051 11 None -19 3 Human 5.4 pKi = 5.4 Binding
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 125 2 2 2 0.3 C[C@@H](Cc1cnc[nH]1)N 10.1016/j.bmcl.2010.10.041
CHEMBL11919 2051 11 None -19 3 Human 5.4 pKi = 5.4 Binding
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 125 2 2 2 0.3 C[C@@H](Cc1cnc[nH]1)N 10.1016/j.bmcl.2010.10.041
44417445 12693 0 None - 1 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]histamine from human histamine H4 receptorDisplacement of [3H]histamine from human histamine H4 receptor
ChEMBL 217 7 5 3 0.7 N=C(N)NCCCCCCSC(=N)N 10.1021/jm060880d
CHEMBL1188154 12693 0 None - 1 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]histamine from human histamine H4 receptorDisplacement of [3H]histamine from human histamine H4 receptor
ChEMBL 217 7 5 3 0.7 N=C(N)NCCCCCCSC(=N)N 10.1021/jm060880d
CHEMBL535387 12693 0 None - 1 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]histamine from human histamine H4 receptorDisplacement of [3H]histamine from human histamine H4 receptor
ChEMBL 217 7 5 3 0.7 N=C(N)NCCCCCCSC(=N)N 10.1021/jm060880d
66572102 75282 1 None - 1 Human 5.4 pKi = 5.4 Binding
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 244 1 1 3 1.0 CN1CCN(C(=O)c2cc3ncccc3[nH]2)CC1 10.1016/j.ejmech.2012.06.016
CHEMBL2047260 75282 1 None - 1 Human 5.4 pKi = 5.4 Binding
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 244 1 1 3 1.0 CN1CCN(C(=O)c2cc3ncccc3[nH]2)CC1 10.1016/j.ejmech.2012.06.016
24854634 155615 0 None - 1 Human 5.4 pKi = 5.4 Binding
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 400 4 0 4 4.5 CN1CCN(c2nc3cc(Cl)c(Cl)cc3nc2CCc2ccccc2)CC1 10.1021/jm7014217
CHEMBL406379 155615 0 None - 1 Human 5.4 pKi = 5.4 Binding
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 400 4 0 4 4.5 CN1CCN(c2nc3cc(Cl)c(Cl)cc3nc2CCc2ccccc2)CC1 10.1021/jm7014217
24853528 166529 0 None - 1 Human 5.4 pKi = 5.4 Binding
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 329 6 0 6 1.7 CN(C)CCCOc1nc2ccccc2nc1N1CCN(C)CC1 10.1021/jm7014217
CHEMBL428964 166529 0 None - 1 Human 5.4 pKi = 5.4 Binding
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 329 6 0 6 1.7 CN(C)CCCOc1nc2ccccc2nc1N1CCN(C)CC1 10.1021/jm7014217
137659490 158650 0 None 11 2 Human 8.4 pKi = 8.4 Binding
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 420 7 1 2 6.1 Brc1ccc(C(OCCCc2c[nH]cn2)c2ccc3ccccc3c2)cc1 10.1016/j.ejmech.2016.09.074
CHEMBL4098585 158650 0 None 11 2 Human 8.4 pKi = 8.4 Binding
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 420 7 1 2 6.1 Brc1ccc(C(OCCCc2c[nH]cn2)c2ccc3ccccc3c2)cc1 10.1016/j.ejmech.2016.09.074
1278 2119 79 None -3 8 Human 8.4 pKi = 8.4 Binding
Antagonist activity at Homo sapiens (human) histamine H4 receptorAntagonist activity at Homo sapiens (human) histamine H4 receptor
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1007/s00044-004-0106-7
1279 2119 79 None -3 8 Human 8.4 pKi = 8.4 Binding
Antagonist activity at Homo sapiens (human) histamine H4 receptorAntagonist activity at Homo sapiens (human) histamine H4 receptor
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1007/s00044-004-0106-7
4908365 2119 79 None -3 8 Human 8.4 pKi = 8.4 Binding
Antagonist activity at Homo sapiens (human) histamine H4 receptorAntagonist activity at Homo sapiens (human) histamine H4 receptor
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1007/s00044-004-0106-7
CHEMBL129198 2119 79 None -3 8 Human 8.4 pKi = 8.4 Binding
Antagonist activity at Homo sapiens (human) histamine H4 receptorAntagonist activity at Homo sapiens (human) histamine H4 receptor
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1007/s00044-004-0106-7
1278 2119 79 None -3 8 Human 8.4 pKi = 8.4 Binding
Binding affinity to human histamine H4 receptorBinding affinity to human histamine H4 receptor
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 2119 79 None -3 8 Human 8.4 pKi = 8.4 Binding
Binding affinity to human histamine H4 receptorBinding affinity to human histamine H4 receptor
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 2119 79 None -3 8 Human 8.4 pKi = 8.4 Binding
Binding affinity to human histamine H4 receptorBinding affinity to human histamine H4 receptor
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 2119 79 None -3 8 Human 8.4 pKi = 8.4 Binding
Binding affinity to human histamine H4 receptorBinding affinity to human histamine H4 receptor
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1016/j.bmcl.2011.11.098
1278 2119 79 None -3 8 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]- histamine from the recombinant human histamine H4 receptorDisplacement of [3H]- histamine from the recombinant human histamine H4 receptor
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/jm0341047
1279 2119 79 None -3 8 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]- histamine from the recombinant human histamine H4 receptorDisplacement of [3H]- histamine from the recombinant human histamine H4 receptor
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/jm0341047
4908365 2119 79 None -3 8 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]- histamine from the recombinant human histamine H4 receptorDisplacement of [3H]- histamine from the recombinant human histamine H4 receptor
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/jm0341047
CHEMBL129198 2119 79 None -3 8 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]- histamine from the recombinant human histamine H4 receptorDisplacement of [3H]- histamine from the recombinant human histamine H4 receptor
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/jm0341047
24803709 145397 0 None - 1 Human 8.4 pKi = 8.4 Binding
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 396 6 2 5 4.3 Cc1nc(NCCCC2CCN(C)CC2)ncc1-c1nc2c(C)cc(F)cc2[nH]1 nan
CHEMBL3917992 145397 0 None - 1 Human 8.4 pKi = 8.4 Binding
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 396 6 2 5 4.3 Cc1nc(NCCCC2CCN(C)CC2)ncc1-c1nc2c(C)cc(F)cc2[nH]1 nan
1278 2119 79 None -3 8 Human 8.4 pKi = 8.4 Binding
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 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1016/j.bmcl.2011.10.104
1279 2119 79 None -3 8 Human 8.4 pKi = 8.4 Binding
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 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1016/j.bmcl.2011.10.104
4908365 2119 79 None -3 8 Human 8.4 pKi = 8.4 Binding
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 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1016/j.bmcl.2011.10.104
CHEMBL129198 2119 79 None -3 8 Human 8.4 pKi = 8.4 Binding
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 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1016/j.bmcl.2011.10.104
49841846 69395 0 None 18 3 Human 8.4 pKi = 8.4 Binding
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 325 2 1 6 2.7 CN1CCN(c2nc(N)nc3cc(-c4ccsc4)ccc23)CC1 10.1016/j.bmcl.2011.10.104
CHEMBL1935572 69395 0 None 18 3 Human 8.4 pKi = 8.4 Binding
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 325 2 1 6 2.7 CN1CCN(c2nc(N)nc3cc(-c4ccsc4)ccc23)CC1 10.1016/j.bmcl.2011.10.104
44129130 197875 0 None -2 2 Human 8.4 pKi = 8.4 Binding
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 460 7 2 7 2.9 CN1CCN(c2nc(NCCS(=O)(=O)Nc3ccccc3)c3cc(Cl)ccc3n2)CC1 10.1016/j.bmcl.2011.10.104
CHEMBL592379 197875 0 None -2 2 Human 8.4 pKi = 8.4 Binding
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 460 7 2 7 2.9 CN1CCN(c2nc(NCCS(=O)(=O)Nc3ccccc3)c3cc(Cl)ccc3n2)CC1 10.1016/j.bmcl.2011.10.104
1278 2119 79 None -3 8 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]histamine from human histamine H4 receptorDisplacement of [3H]histamine from human histamine H4 receptor
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1016/j.bmcl.2011.03.017
1279 2119 79 None -3 8 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]histamine from human histamine H4 receptorDisplacement of [3H]histamine from human histamine H4 receptor
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1016/j.bmcl.2011.03.017
4908365 2119 79 None -3 8 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]histamine from human histamine H4 receptorDisplacement of [3H]histamine from human histamine H4 receptor
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1016/j.bmcl.2011.03.017
CHEMBL129198 2119 79 None -3 8 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]histamine from human histamine H4 receptorDisplacement of [3H]histamine from human histamine H4 receptor
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1016/j.bmcl.2011.03.017
24745337 61210 0 None - 1 Human 8.4 pKi = 8.4 Binding
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(NCC(C)C)nc(N)n2)C1 10.1016/j.bmcl.2011.03.017
CHEMBL1770979 61210 0 None - 1 Human 8.4 pKi = 8.4 Binding
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(NCC(C)C)nc(N)n2)C1 10.1016/j.bmcl.2011.03.017
58227340 116616 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 260 4 2 4 2.2 CN[C@@H]1CCN(c2ccnc(NC3CCCC3)c2)C1 10.1016/j.bmcl.2014.12.027
CHEMBL3393532 116616 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 260 4 2 4 2.2 CN[C@@H]1CCN(c2ccnc(NC3CCCC3)c2)C1 10.1016/j.bmcl.2014.12.027
1278 2119 79 None -3 8 Human 8.4 pKi = 8.4 Binding
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 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/jm0502081
1279 2119 79 None -3 8 Human 8.4 pKi = 8.4 Binding
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 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/jm0502081
4908365 2119 79 None -3 8 Human 8.4 pKi = 8.4 Binding
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 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/jm0502081
CHEMBL129198 2119 79 None -3 8 Human 8.4 pKi = 8.4 Binding
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 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/jm0502081
1278 2119 79 None -3 8 Human 8.4 pKi = 8.4 Binding
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 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/jm800876b
1279 2119 79 None -3 8 Human 8.4 pKi = 8.4 Binding
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 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/jm800876b
4908365 2119 79 None -3 8 Human 8.4 pKi = 8.4 Binding
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 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/jm800876b
CHEMBL129198 2119 79 None -3 8 Human 8.4 pKi = 8.4 Binding
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 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/jm800876b
1278 2119 79 None -3 8 Human 8.4 pKi = 8.4 Binding
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 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/acs.jmedchem.0c00160
1279 2119 79 None -3 8 Human 8.4 pKi = 8.4 Binding
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 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/acs.jmedchem.0c00160
4908365 2119 79 None -3 8 Human 8.4 pKi = 8.4 Binding
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 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/acs.jmedchem.0c00160
CHEMBL129198 2119 79 None -3 8 Human 8.4 pKi = 8.4 Binding
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 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/acs.jmedchem.0c00160
1278 2119 79 None 3 8 Rat 8.4 pKi = 8.4 Binding
Displacement of [3H]-histamine from rat H4R expressed in HEK293T cellsDisplacement of [3H]-histamine from rat 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 2119 79 None 3 8 Rat 8.4 pKi = 8.4 Binding
Displacement of [3H]-histamine from rat H4R expressed in HEK293T cellsDisplacement of [3H]-histamine from rat 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 2119 79 None 3 8 Rat 8.4 pKi = 8.4 Binding
Displacement of [3H]-histamine from rat H4R expressed in HEK293T cellsDisplacement of [3H]-histamine from rat 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 2119 79 None 3 8 Rat 8.4 pKi = 8.4 Binding
Displacement of [3H]-histamine from rat H4R expressed in HEK293T cellsDisplacement of [3H]-histamine from rat 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
44129133 197704 0 None - 1 Human 8.4 pKi = 8.4 Binding
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 398 6 2 7 1.0 CNS(=O)(=O)CCNc1nc(N2CCN(C)CC2)nc2ccc(Cl)cc12 10.1021/jm901379s
CHEMBL591011 197704 0 None - 1 Human 8.4 pKi = 8.4 Binding
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 398 6 2 7 1.0 CNS(=O)(=O)CCNc1nc(N2CCN(C)CC2)nc2ccc(Cl)cc12 10.1021/jm901379s
1223 940 32 None -60 11 Human 8.4 pKi = 8.4 Binding
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 308 6 2 3 3.2 Clc1ccc(cc1)CN=C(SCCCc1cnc[nH]1)N 10.1016/j.bmc.2011.03.046
2790 940 32 None -60 11 Human 8.4 pKi = 8.4 Binding
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 308 6 2 3 3.2 Clc1ccc(cc1)CN=C(SCCCc1cnc[nH]1)N 10.1016/j.bmc.2011.03.046
CHEMBL14690 940 32 None -60 11 Human 8.4 pKi = 8.4 Binding
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 308 6 2 3 3.2 Clc1ccc(cc1)CN=C(SCCCc1cnc[nH]1)N 10.1016/j.bmc.2011.03.046
1223 940 32 None -60 11 Human 8.4 pKi = 8.4 Binding
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 308 6 2 3 3.2 Clc1ccc(cc1)CN=C(SCCCc1cnc[nH]1)N 10.1016/j.bmcl.2009.10.005
2790 940 32 None -60 11 Human 8.4 pKi = 8.4 Binding
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 308 6 2 3 3.2 Clc1ccc(cc1)CN=C(SCCCc1cnc[nH]1)N 10.1016/j.bmcl.2009.10.005
CHEMBL14690 940 32 None -60 11 Human 8.4 pKi = 8.4 Binding
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 308 6 2 3 3.2 Clc1ccc(cc1)CN=C(SCCCc1cnc[nH]1)N 10.1016/j.bmcl.2009.10.005
25129169 186598 0 None 8 4 Rat 8.4 pKi = 8.4 Binding
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 323 2 2 5 2.3 Nc1nc2c(c(N3CCNCC3)n1)CCCCC2c1ccccc1 10.1016/j.bmcl.2010.01.131
CHEMBL492231 186598 0 None 8 4 Rat 8.4 pKi = 8.4 Binding
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 323 2 2 5 2.3 Nc1nc2c(c(N3CCNCC3)n1)CCCCC2c1ccccc1 10.1016/j.bmcl.2010.01.131
44129134 197827 0 None 22 2 Human 8.4 pKi = 8.4 Binding
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 384 5 2 7 0.7 CN1CCN(c2nc(NCCS(N)(=O)=O)c3cc(Cl)ccc3n2)CC1 10.1021/jm901379s
CHEMBL591969 197827 0 None 22 2 Human 8.4 pKi = 8.4 Binding
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 384 5 2 7 0.7 CN1CCN(c2nc(NCCS(N)(=O)=O)c3cc(Cl)ccc3n2)CC1 10.1021/jm901379s
25129169 186598 0 None 8 4 Rat 8.4 pKi = 8.4 Binding
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 323 2 2 5 2.3 Nc1nc2c(c(N3CCNCC3)n1)CCCCC2c1ccccc1 10.1021/jm800670r
CHEMBL492231 186598 0 None 8 4 Rat 8.4 pKi = 8.4 Binding
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 323 2 2 5 2.3 Nc1nc2c(c(N3CCNCC3)n1)CCCCC2c1ccccc1 10.1021/jm800670r
1278 2119 79 None -3 8 Human 8.4 pKi = 8.4 Binding
Binding affinity to human histamine H4 receptorBinding affinity to human histamine H4 receptor
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/acs.jmedchem.5b00516
1279 2119 79 None -3 8 Human 8.4 pKi = 8.4 Binding
Binding affinity to human histamine H4 receptorBinding affinity to human histamine H4 receptor
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/acs.jmedchem.5b00516
4908365 2119 79 None -3 8 Human 8.4 pKi = 8.4 Binding
Binding affinity to human histamine H4 receptorBinding affinity to human histamine H4 receptor
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/acs.jmedchem.5b00516
CHEMBL129198 2119 79 None -3 8 Human 8.4 pKi = 8.4 Binding
Binding affinity to human histamine H4 receptorBinding affinity to human histamine H4 receptor
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/acs.jmedchem.5b00516
24745506 67877 0 None - 1 Human 8.3 pKi = 8.3 Binding
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 278 5 3 6 1.3 CNC1CN(c2cc(NCCC(C)(C)C)nc(N)n2)C1 10.1016/j.bmcl.2011.07.125
CHEMBL1915537 67877 0 None - 1 Human 8.3 pKi = 8.3 Binding
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 278 5 3 6 1.3 CNC1CN(c2cc(NCCC(C)(C)C)nc(N)n2)C1 10.1016/j.bmcl.2011.07.125
136042266 69568 0 None - 1 Human 8.3 pKi = 8.3 Binding
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 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 69568 0 None - 1 Human 8.3 pKi = 8.3 Binding
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 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
136042268 69570 0 None 186 2 Human 8.3 pKi = 8.3 Binding
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 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 69570 0 None 186 2 Human 8.3 pKi = 8.3 Binding
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 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
25068753 187854 15 None -1 2 Human 8.3 pKi = 8.3 Binding
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 1 2 5 1.8 Nc1nc2c(c(N3CC[C@@H](N)C3)n1)CCCc1ccccc1-2 10.1021/jm800670r
CHEMBL502347 187854 15 None -1 2 Human 8.3 pKi = 8.3 Binding
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 1 2 5 1.8 Nc1nc2c(c(N3CC[C@@H](N)C3)n1)CCCc1ccccc1-2 10.1021/jm800670r
1278 2119 79 None 3 8 Rat 8.3 pKi = 8.3 Binding
Displacement of [3H]histamine from rat histamine H4 receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [3H]histamine from rat 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 2119 79 None 3 8 Rat 8.3 pKi = 8.3 Binding
Displacement of [3H]histamine from rat histamine H4 receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [3H]histamine from rat 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 2119 79 None 3 8 Rat 8.3 pKi = 8.3 Binding
Displacement of [3H]histamine from rat histamine H4 receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [3H]histamine from rat 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 2119 79 None 3 8 Rat 8.3 pKi = 8.3 Binding
Displacement of [3H]histamine from rat histamine H4 receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [3H]histamine from rat 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
25068753 187854 15 None -1 2 Human 8.3 pKi = 8.3 Binding
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 1 2 5 1.8 Nc1nc2c(c(N3CC[C@@H](N)C3)n1)CCCc1ccccc1-2 10.1021/jm800670r
CHEMBL502347 187854 15 None -1 2 Human 8.3 pKi = 8.3 Binding
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 1 2 5 1.8 Nc1nc2c(c(N3CC[C@@H](N)C3)n1)CCCc1ccccc1-2 10.1021/jm800670r
2063135 8293 9 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from 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 8293 9 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 302 1 0 5 2.8 CN1CCN(c2ncnc3c2oc2ccc(Cl)cc23)CC1 10.1016/j.bmcl.2011.08.014
24826437 67755 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 343 1 2 6 2.8 Nc1nc(N2C[C@H]3CCCN[C@H]3C2)c2oc3ccc(Cl)cc3c2n1 10.1016/j.bmcl.2011.08.014
CHEMBL1914746 67755 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 343 1 2 6 2.8 Nc1nc(N2C[C@H]3CCCN[C@H]3C2)c2oc3ccc(Cl)cc3c2n1 10.1016/j.bmcl.2011.08.014
25128823 192115 0 None 2 2 Rat 8.3 pKi = 8.3 Binding
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 267 1 2 5 1.0 Nc1nc2c(c(N3CCNCC3)n1)Cc1ccccc1-2 10.1021/jm800670r
CHEMBL521995 192115 0 None 2 2 Rat 8.3 pKi = 8.3 Binding
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 267 1 2 5 1.0 Nc1nc2c(c(N3CCNCC3)n1)Cc1ccccc1-2 10.1021/jm800670r
1204 1901 114 None -3 23 Human 8.3 pKi = 8.3 Binding
Binding affinity to human histamine H4 receptorBinding affinity to human histamine H4 receptor
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.5b00516
1247 1901 114 None -3 23 Human 8.3 pKi = 8.3 Binding
Binding affinity to human histamine H4 receptorBinding affinity to human histamine H4 receptor
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.5b00516
1375 1901 114 None -3 23 Human 8.3 pKi = 8.3 Binding
Binding affinity to human histamine H4 receptorBinding affinity to human histamine H4 receptor
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.5b00516
774 1901 114 None -3 23 Human 8.3 pKi = 8.3 Binding
Binding affinity to human histamine H4 receptorBinding affinity to human histamine H4 receptor
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.5b00516
CHEMBL90 1901 114 None -3 23 Human 8.3 pKi = 8.3 Binding
Binding affinity to human histamine H4 receptorBinding affinity to human histamine H4 receptor
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.5b00516
DB05381 1901 114 None -3 23 Human 8.3 pKi = 8.3 Binding
Binding affinity to human histamine H4 receptorBinding affinity to human histamine H4 receptor
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.5b00516
1278 2119 79 None -3 8 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]histamine from human histamine 4 receptor expressed in HEK293T cell membranes incubated for 1 hr by radioligand binding assayDisplacement of [3H]histamine from human histamine 4 receptor expressed in HEK293T cell membranes incubated for 1 hr by radioligand binding assay
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1016/j.bmcl.2015.12.035
1279 2119 79 None -3 8 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]histamine from human histamine 4 receptor expressed in HEK293T cell membranes incubated for 1 hr by radioligand binding assayDisplacement of [3H]histamine from human histamine 4 receptor expressed in HEK293T cell membranes incubated for 1 hr by radioligand binding assay
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1016/j.bmcl.2015.12.035
4908365 2119 79 None -3 8 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]histamine from human histamine 4 receptor expressed in HEK293T cell membranes incubated for 1 hr by radioligand binding assayDisplacement of [3H]histamine from human histamine 4 receptor expressed in HEK293T cell membranes incubated for 1 hr by radioligand binding assay
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1016/j.bmcl.2015.12.035
CHEMBL129198 2119 79 None -3 8 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]histamine from human histamine 4 receptor expressed in HEK293T cell membranes incubated for 1 hr by radioligand binding assayDisplacement of [3H]histamine from human histamine 4 receptor expressed in HEK293T cell membranes incubated for 1 hr by radioligand binding assay
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1016/j.bmcl.2015.12.035
44129130 197875 0 None -2 2 Human 8.3 pKi = 8.3 Binding
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 460 7 2 7 2.9 CN1CCN(c2nc(NCCS(=O)(=O)Nc3ccccc3)c3cc(Cl)ccc3n2)CC1 10.1021/jm901379s
CHEMBL592379 197875 0 None -2 2 Human 8.3 pKi = 8.3 Binding
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 460 7 2 7 2.9 CN1CCN(c2nc(NCCS(=O)(=O)Nc3ccccc3)c3cc(Cl)ccc3n2)CC1 10.1021/jm901379s
54581941 61228 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]histamine from human histamine H4 receptorDisplacement of [3H]histamine from human histamine H4 receptor
ChEMBL 288 2 2 6 0.8 Nc1nc(N2CCCC2)cc(N2CC3CCCNC3C2)n1 10.1016/j.bmcl.2011.03.017
CHEMBL1770997 61228 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]histamine from human histamine H4 receptorDisplacement of [3H]histamine from human histamine H4 receptor
ChEMBL 288 2 2 6 0.8 Nc1nc(N2CCCC2)cc(N2CC3CCCNC3C2)n1 10.1016/j.bmcl.2011.03.017
24826680 67786 0 None - 1 Human 7.4 pKi = 7.4 Binding
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)nc3c2oc2cccc(Cl)c23)C1 10.1016/j.bmcl.2011.08.014
CHEMBL1914777 67786 0 None - 1 Human 7.4 pKi = 7.4 Binding
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)nc3c2oc2cccc(Cl)c23)C1 10.1016/j.bmcl.2011.08.014
11601630 132296 0 None - 1 Human 7.4 pKi = 7.4 Binding
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 283 1 1 3 2.3 CN1CCN(C(=O)c2cc3sc(Cl)cc3[nH]2)CC1 10.1021/jm0502081
CHEMBL370135 132296 0 None - 1 Human 7.4 pKi = 7.4 Binding
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 283 1 1 3 2.3 CN1CCN(C(=O)c2cc3sc(Cl)cc3[nH]2)CC1 10.1021/jm0502081
137640214 156425 0 None - 1 Human 6.4 pKi = 6.4 Binding
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 394 6 1 2 5.5 O=C(NCCCCN1Cc2cccc3cccc(c23)C1)c1ccc2ccccc2c1 10.1016/j.ejmech.2016.09.074
CHEMBL4072893 156425 0 None - 1 Human 6.4 pKi = 6.4 Binding
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 394 6 1 2 5.5 O=C(NCCCCN1Cc2cccc3cccc(c23)C1)c1ccc2ccccc2c1 10.1016/j.ejmech.2016.09.074
71519013 86039 0 None - 1 Human 5.4 pKi = 5.4 Binding
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 340 3 2 5 2.5 CCN1CCN(c2nc(N)nc3[nH]c(-c4ccc(F)cc4)cc23)CC1 10.1016/j.bmcl.2012.10.139
CHEMBL2314498 86039 0 None - 1 Human 5.4 pKi = 5.4 Binding
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 340 3 2 5 2.5 CCN1CCN(c2nc(N)nc3[nH]c(-c4ccc(F)cc4)cc23)CC1 10.1016/j.bmcl.2012.10.139
168284289 192304 0 None -7 4 Human 5.4 pKi = 5.4 Binding
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 192304 0 None -7 4 Human 5.4 pKi = 5.4 Binding
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 192304 0 None -7 4 Human 5.4 pKi = 5.4 Binding
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
3076002 178702 2 None - 1 Human 5.4 pKi = 5.4 Binding
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 334 4 0 5 3.0 CN1CCN(c2nc(OCc3ccccc3)c3ccccc3n2)CC1 10.1021/jm800876b
CHEMBL473099 178702 2 None - 1 Human 5.4 pKi = 5.4 Binding
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 334 4 0 5 3.0 CN1CCN(c2nc(OCc3ccccc3)c3ccccc3n2)CC1 10.1021/jm800876b
3076002 178702 2 None - 1 Human 5.4 pKi = 5.4 Binding
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 334 4 0 5 3.0 CN1CCN(c2nc(OCc3ccccc3)c3ccccc3n2)CC1 10.1021/jm901379s
CHEMBL473099 178702 2 None - 1 Human 5.4 pKi = 5.4 Binding
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 334 4 0 5 3.0 CN1CCN(c2nc(OCc3ccccc3)c3ccccc3n2)CC1 10.1021/jm901379s
90645150 111681 0 None - 1 Human 6.4 pKi = 6.4 Binding
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 304 2 1 6 1.5 CN1CCN(c2nc(N)nc(-c3cccc(Cl)c3)n2)CC1 10.1016/j.ejmech.2014.06.032
CHEMBL3290573 111681 0 None - 1 Human 6.4 pKi = 6.4 Binding
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 304 2 1 6 1.5 CN1CCN(c2nc(N)nc(-c3cccc(Cl)c3)n2)CC1 10.1016/j.ejmech.2014.06.032
25130576 187043 1 None 2 4 Human 7.4 pKi = 7.4 Binding
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 280 2 2 6 1.0 N#Cc1ccc(-c2cc(N3CCNCC3)nc(N)n2)cc1 10.1021/jm8005959
25130576 187043 1 None 2 4 Human 7.4 pKi = 7.4 Binding
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 280 2 2 6 1.0 N#Cc1ccc(-c2cc(N3CCNCC3)nc(N)n2)cc1 10.1021/jm800670r
CHEMBL494890 187043 1 None 2 4 Human 7.4 pKi = 7.4 Binding
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 280 2 2 6 1.0 N#Cc1ccc(-c2cc(N3CCNCC3)nc(N)n2)cc1 10.1021/jm8005959
CHEMBL494890 187043 1 None 2 4 Human 7.4 pKi = 7.4 Binding
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 280 2 2 6 1.0 N#Cc1ccc(-c2cc(N3CCNCC3)nc(N)n2)cc1 10.1021/jm800670r
10018335 71668 0 None - 1 Human 6.4 pKi = 6.4 Binding
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 2.6 CN1CCN(C(=O)c2cc3cc(C(F)(F)F)ccc3[nH]2)CC1 10.1021/jm0502081
CHEMBL197477 71668 0 None - 1 Human 6.4 pKi = 6.4 Binding
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 2.6 CN1CCN(C(=O)c2cc3cc(C(F)(F)F)ccc3[nH]2)CC1 10.1021/jm0502081
57393771 67832 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 311 2 2 7 1.5 COc1ccc2oc3c(N4C[C@@H]5C[C@H]4CN5)nc(N)nc3c2c1 10.1016/j.bmcl.2011.08.014
CHEMBL1915035 67832 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 311 2 2 7 1.5 COc1ccc2oc3c(N4C[C@@H]5C[C@H]4CN5)nc(N)nc3c2c1 10.1016/j.bmcl.2011.08.014
10545988 62817 0 None -93 2 Human 4.4 pKi = 4.4 Binding
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 237 8 2 3 2.0 C=CCCCNC(=O)OCCCc1c[nH]cn1 10.1016/j.bmcl.2013.06.075
CHEMBL1774593 62817 0 None -93 2 Human 4.4 pKi = 4.4 Binding
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 237 8 2 3 2.0 C=CCCCNC(=O)OCCCc1c[nH]cn1 10.1016/j.bmcl.2013.06.075
CHEMBL1789558 62817 0 None -93 2 Human 4.4 pKi = 4.4 Binding
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 237 8 2 3 2.0 C=CCCCNC(=O)OCCCc1c[nH]cn1 10.1016/j.bmcl.2013.06.075
46228071 198494 15 None - 1 Human 6.4 pKi = 6.4 Binding
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 283 4 1 5 1.8 CN1CCN(c2cc(NCc3ccccc3)ncn2)CC1 10.1016/j.bmc.2009.08.059
CHEMBL596562 198494 15 None - 1 Human 6.4 pKi = 6.4 Binding
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 283 4 1 5 1.8 CN1CCN(c2cc(NCc3ccccc3)ncn2)CC1 10.1016/j.bmc.2009.08.059
1204 1901 114 None -15 23 Mouse 7.4 pKi = 7.4 Binding
Binding affinity to mouse histamine H4 receptorBinding affinity to mouse histamine H4 receptor
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.5b00516
1247 1901 114 None -15 23 Mouse 7.4 pKi = 7.4 Binding
Binding affinity to mouse histamine H4 receptorBinding affinity to mouse histamine H4 receptor
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.5b00516
1375 1901 114 None -15 23 Mouse 7.4 pKi = 7.4 Binding
Binding affinity to mouse histamine H4 receptorBinding affinity to mouse histamine H4 receptor
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.5b00516
774 1901 114 None -15 23 Mouse 7.4 pKi = 7.4 Binding
Binding affinity to mouse histamine H4 receptorBinding affinity to mouse histamine H4 receptor
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.5b00516
CHEMBL90 1901 114 None -15 23 Mouse 7.4 pKi = 7.4 Binding
Binding affinity to mouse histamine H4 receptorBinding affinity to mouse histamine H4 receptor
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.5b00516
DB05381 1901 114 None -15 23 Mouse 7.4 pKi = 7.4 Binding
Binding affinity to mouse histamine H4 receptorBinding affinity to mouse histamine H4 receptor
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.5b00516
46890590 6946 0 None 1 2 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
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 6946 0 None 1 2 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 422 6 2 4 4.4 Cc1cc(OCCCN2CC3CCCNC3C2)ccc1-c1nc2c(C)c(F)ccc2[nH]1 10.1016/j.bmcl.2010.04.017
57400735 67826 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 351 1 2 6 2.9 Nc1nc(N2CCC[C@H](N)C2)c2oc3ccc(C(F)(F)F)cc3c2n1 10.1016/j.bmcl.2011.08.014
CHEMBL1915026 67826 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 351 1 2 6 2.9 Nc1nc(N2CCC[C@H](N)C2)c2oc3ccc(C(F)(F)F)cc3c2n1 10.1016/j.bmcl.2011.08.014
56851441 71255 0 None -1 2 Human 7.4 pKi = 7.4 Binding
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 7 2 3 4.2 c1ccc(CN/C(=N/C2CCCC2)SCCCc2c[nH]cn2)cc1 10.1021/jm201042n
CHEMBL1923023 71255 0 None -1 2 Human 7.4 pKi = 7.4 Binding
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 7 2 3 4.2 c1ccc(CN/C(=N/C2CCCC2)SCCCc2c[nH]cn2)cc1 10.1021/jm201042n
CHEMBL1963243 71255 0 None -1 2 Human 7.4 pKi = 7.4 Binding
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 7 2 3 4.2 c1ccc(CN/C(=N/C2CCCC2)SCCCc2c[nH]cn2)cc1 10.1021/jm201042n
25147772 172837 4 None -1 3 Human 7.4 pKi = 7.4 Binding
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 373 4 1 6 3.7 CN1CCN(c2nc(NCc3cccs3)c3cc(Cl)ccc3n2)CC1 10.1016/j.bmcl.2015.12.035
CHEMBL452847 172837 4 None -1 3 Human 7.4 pKi = 7.4 Binding
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 373 4 1 6 3.7 CN1CCN(c2nc(NCc3cccs3)c3cc(Cl)ccc3n2)CC1 10.1016/j.bmcl.2015.12.035
16061961 197997 0 None 7 2 Human 7.4 pKi = 7.4 Binding
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 316 4 2 6 1.6 CN1CCN(c2cc(NCc3ccc(F)cc3)nc(N)n2)CC1 10.1016/j.bmc.2009.08.059
CHEMBL593103 197997 0 None 7 2 Human 7.4 pKi = 7.4 Binding
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 316 4 2 6 1.6 CN1CCN(c2cc(NCc3ccc(F)cc3)nc(N)n2)CC1 10.1016/j.bmc.2009.08.059
10381810 203463 0 None -2 5 Human 7.4 pKi = 7.4 Binding
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=Nc3cc(Cl)ccc3Oc3ccccc32)CC1 10.1021/jm051008s
CHEMBL7828 203463 0 None -2 5 Human 7.4 pKi = 7.4 Binding
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=Nc3cc(Cl)ccc3Oc3ccccc32)CC1 10.1021/jm051008s
137647794 157438 0 None - 1 Human 5.4 pKi = 5.4 Binding
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 464 8 1 6 4.2 COc1ccc2c(c1)c(CC(=O)NCCCn1ccnc1)c(C)n2C(=O)c1ccc(Cl)cc1 10.1016/j.ejmech.2016.09.074
CHEMBL4085023 157438 0 None - 1 Human 5.4 pKi = 5.4 Binding
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 464 8 1 6 4.2 COc1ccc2c(c1)c(CC(=O)NCCCn1ccnc1)c(C)n2C(=O)c1ccc(Cl)cc1 10.1016/j.ejmech.2016.09.074
10545988 62817 0 None -93 2 Human 6.4 pKi = 6.4 Binding
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 237 8 2 3 2.0 C=CCCCNC(=O)OCCCc1c[nH]cn1 10.1016/j.bmc.2011.03.046
CHEMBL1774593 62817 0 None -93 2 Human 6.4 pKi = 6.4 Binding
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 237 8 2 3 2.0 C=CCCCNC(=O)OCCCc1c[nH]cn1 10.1016/j.bmc.2011.03.046
CHEMBL1789558 62817 0 None -93 2 Human 6.4 pKi = 6.4 Binding
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 237 8 2 3 2.0 C=CCCCNC(=O)OCCCc1c[nH]cn1 10.1016/j.bmc.2011.03.046
122193096 123397 0 None - 1 Human 5.4 pKi = 5.4 Binding
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 330 3 1 6 2.0 CN1CCN(c2nc(N)nc(/C=C/c3ccc(Cl)cc3)n2)CC1 10.1016/j.ejmech.2015.08.014
CHEMBL3628043 123397 0 None - 1 Human 5.4 pKi = 5.4 Binding
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 330 3 1 6 2.0 CN1CCN(c2nc(N)nc(/C=C/c3ccc(Cl)cc3)n2)CC1 10.1016/j.ejmech.2015.08.014
90645154 111689 0 None - 1 Human 5.4 pKi = 5.4 Binding
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 338 2 1 6 1.9 CN1CCN(c2nc(N)nc(-c3ccc(C(F)(F)F)cc3)n2)CC1 10.1016/j.ejmech.2014.06.032
CHEMBL3290581 111689 0 None - 1 Human 5.4 pKi = 5.4 Binding
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 338 2 1 6 1.9 CN1CCN(c2nc(N)nc(-c3ccc(C(F)(F)F)cc3)n2)CC1 10.1016/j.ejmech.2014.06.032
10777275 5818 1 None -22 3 Human 6.4 pKi = 6.4 Binding
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 2.6 CCCC[C@@H](C)NC(=O)OCCCc1c[nH]cn1 10.1016/j.bmcl.2009.10.005
CHEMBL1079553 5818 1 None -22 3 Human 6.4 pKi = 6.4 Binding
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 2.6 CCCC[C@@H](C)NC(=O)OCCCc1c[nH]cn1 10.1016/j.bmcl.2009.10.005
CHEMBL156005 5818 1 None -22 3 Human 6.4 pKi = 6.4 Binding
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 2.6 CCCC[C@@H](C)NC(=O)OCCCc1c[nH]cn1 10.1016/j.bmcl.2009.10.005
1267 3744 43 None -33 25 Human 6.4 pKi = 6.4 Binding
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 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1016/j.bmcl.2013.06.075
3035905 3744 43 None -33 25 Human 6.4 pKi = 6.4 Binding
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 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1016/j.bmcl.2013.06.075
CHEMBL260374 3744 43 None -33 25 Human 6.4 pKi = 6.4 Binding
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 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1016/j.bmcl.2013.06.075
127036978 136757 0 None 1 2 Human 5.4 pKi = 5.4 Binding
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 415 5 1 6 3.6 COc1ccc(CNc2nc3c(c(N4CCN(C)CC4)n2)CCc2ccccc2-3)cc1 10.1016/j.bmcl.2015.12.035
CHEMBL3752225 136757 0 None 1 2 Human 5.4 pKi = 5.4 Binding
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 415 5 1 6 3.6 COc1ccc(CNc2nc3c(c(N4CCN(C)CC4)n2)CCc2ccccc2-3)cc1 10.1016/j.bmcl.2015.12.035
164612037 184795 0 None -81283 20 Human 5.4 pKi = 5.4 Binding
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 326 8 4 4 1.8 CCCCCNC(=O)/N=C(\N)NCCCc1sc(N)nc1C 10.1016/j.ejmech.2021.113190
CHEMBL4860528 184795 0 None -81283 20 Human 5.4 pKi = 5.4 Binding
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 326 8 4 4 1.8 CCCCCNC(=O)/N=C(\N)NCCCc1sc(N)nc1C 10.1016/j.ejmech.2021.113190
1224 1404 79 None -194 13 Human 4.4 pKi = 4.4 Binding
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 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C 10.1016/j.bmcl.2011.09.001
3100 1404 79 None -194 13 Human 4.4 pKi = 4.4 Binding
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 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C 10.1016/j.bmcl.2011.09.001
8980 1404 79 None -194 13 Human 4.4 pKi = 4.4 Binding
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 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C 10.1016/j.bmcl.2011.09.001
916 1404 79 None -194 13 Human 4.4 pKi = 4.4 Binding
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 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C 10.1016/j.bmcl.2011.09.001
CHEMBL657 1404 79 None -194 13 Human 4.4 pKi = 4.4 Binding
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 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C 10.1016/j.bmcl.2011.09.001
DB01075 1404 79 None -194 13 Human 4.4 pKi = 4.4 Binding
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 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C 10.1016/j.bmcl.2011.09.001
9883231 112887 0 None - 1 Human 6.4 pKi = 6.4 Binding
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 312 1 1 3 2.0 CN1CCN(C(=O)c2nc3cc(C(F)(F)F)ccc3[nH]2)CC1 10.1021/jm0502081
CHEMBL331773 112887 0 None - 1 Human 6.4 pKi = 6.4 Binding
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 312 1 1 3 2.0 CN1CCN(C(=O)c2nc3cc(C(F)(F)F)ccc3[nH]2)CC1 10.1021/jm0502081
1267 3744 43 None -33 25 Human 7.4 pKi = 7.4 Binding
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 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1016/j.bmc.2011.03.046
3035905 3744 43 None -33 25 Human 7.4 pKi = 7.4 Binding
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 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1016/j.bmc.2011.03.046
CHEMBL260374 3744 43 None -33 25 Human 7.4 pKi = 7.4 Binding
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 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1016/j.bmc.2011.03.046
1267 3744 43 None -33 25 Human 7.4 pKi = 7.4 Binding
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 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1016/j.bmcl.2009.10.005
3035905 3744 43 None -33 25 Human 7.4 pKi = 7.4 Binding
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 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1016/j.bmcl.2009.10.005
CHEMBL260374 3744 43 None -33 25 Human 7.4 pKi = 7.4 Binding
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 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1016/j.bmcl.2009.10.005
24992735 109666 0 None - 1 Human 7.4 pKi = 7.4 Binding
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 0.7 CN[C@@H]1CCN(c2nc(N)nc3c2CCCC3)C1 10.1021/jm401727m
CHEMBL3236582 109666 0 None - 1 Human 7.4 pKi = 7.4 Binding
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 0.7 CN[C@@H]1CCN(c2nc(N)nc3c2CCCC3)C1 10.1021/jm401727m
24826081 67771 0 None - 1 Human 7.4 pKi = 7.4 Binding
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)nc3c2sc2cc(Br)ccc23)CC1 10.1016/j.bmcl.2011.08.014
CHEMBL1914762 67771 0 None - 1 Human 7.4 pKi = 7.4 Binding
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)nc3c2sc2cc(Br)ccc23)CC1 10.1016/j.bmcl.2011.08.014
90645153 111688 0 None - 1 Human 6.4 pKi = 6.4 Binding
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 284 2 1 6 1.2 Cc1ccc(-c2nc(N)nc(N3CCN(C)CC3)n2)cc1 10.1016/j.ejmech.2014.06.032
CHEMBL3290580 111688 0 None - 1 Human 6.4 pKi = 6.4 Binding
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 284 2 1 6 1.2 Cc1ccc(-c2nc(N)nc(N3CCN(C)CC3)n2)cc1 10.1016/j.ejmech.2014.06.032
25178344 186303 0 None - 1 Human 6.4 pKi = 6.4 Binding
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 321 4 2 6 1.4 CN1CCN(c2nc(NCCO)c3cc(Cl)ccc3n2)CC1 10.1021/jm901379s
CHEMBL489664 186303 0 None - 1 Human 6.4 pKi = 6.4 Binding
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 321 4 2 6 1.4 CN1CCN(c2nc(NCCO)c3cc(Cl)ccc3n2)CC1 10.1021/jm901379s
10934158 108090 1 None -1 2 Human 6.4 pKi = 6.4 Binding
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
CHEMBL320331 108090 1 None -1 2 Human 6.4 pKi = 6.4 Binding
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
24853593 95612 0 None - 1 Human 5.4 pKi = 5.4 Binding
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 335 4 0 6 2.4 CN1CCN(c2nc3ccccc3nc2OCc2ccncc2)CC1 10.1021/jm7014217
CHEMBL259956 95612 0 None - 1 Human 5.4 pKi = 5.4 Binding
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 335 4 0 6 2.4 CN1CCN(c2nc3ccccc3nc2OCc2ccncc2)CC1 10.1021/jm7014217
54586765 61213 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]histamine from human histamine H4 receptorDisplacement of [3H]histamine from human histamine H4 receptor
ChEMBL 252 5 4 7 -0.7 CN[C@@H]1CCN(c2cc(NCCO)nc(N)n2)C1 10.1016/j.bmcl.2011.03.017
CHEMBL1770982 61213 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]histamine from human histamine H4 receptorDisplacement of [3H]histamine from human histamine H4 receptor
ChEMBL 252 5 4 7 -0.7 CN[C@@H]1CCN(c2cc(NCCO)nc(N)n2)C1 10.1016/j.bmcl.2011.03.017
44275465 98764 2 None - 1 Human 7.4 pKi = 7.4 Binding
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 243 1 1 5 1.0 CN1CCN(c2nc(N)nc3ccccc23)CC1 10.1016/j.bmcl.2013.02.091
CHEMBL281590 98764 2 None - 1 Human 7.4 pKi = 7.4 Binding
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 243 1 1 5 1.0 CN1CCN(c2nc(N)nc3ccccc23)CC1 10.1016/j.bmcl.2013.02.091
24826080 67773 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 367 1 1 6 3.2 CN1CCN(c2nc(N)nc3c2sc2cc(C(F)(F)F)ccc23)CC1 10.1016/j.bmcl.2011.08.014
CHEMBL1914764 67773 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 367 1 1 6 3.2 CN1CCN(c2nc(N)nc3c2sc2cc(C(F)(F)F)ccc23)CC1 10.1016/j.bmcl.2011.08.014
71519349 86064 0 None - 1 Human 4.4 pKi = 4.4 Binding
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 326 2 2 6 1.8 Cn1c(-c2ccc(F)cc2)cc2c(N3CCNCC3)nc(N)nc21 10.1016/j.bmcl.2012.10.139
CHEMBL2314767 86064 0 None - 1 Human 4.4 pKi = 4.4 Binding
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 326 2 2 6 1.8 Cn1c(-c2ccc(F)cc2)cc2c(N3CCNCC3)nc(N)nc21 10.1016/j.bmcl.2012.10.139
57393770 67829 0 None - 1 Human 6.4 pKi = 6.4 Binding
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)c2oc3cccc(Cl)c3c2n1 10.1016/j.bmcl.2011.08.014
CHEMBL1915031 67829 0 None - 1 Human 6.4 pKi = 6.4 Binding
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)c2oc3cccc(Cl)c3c2n1 10.1016/j.bmcl.2011.08.014
155534519 175909 0 None -47 2 Human 6.4 pKi = 6.4 Binding
Displacement of 40 nM [3H]-histamine from human H4R expressed in Sf9 cell membranes co-expressing Gia2 and beta1gamma2 by competition binding assayDisplacement of 40 nM [3H]-histamine from human H4R expressed in Sf9 cell membranes co-expressing Gia2 and beta1gamma2 by competition binding assay
ChEMBL 288 7 3 5 2.7 CC(C)(C)CNc1nccc(NCCCc2c[nH]cn2)n1 10.1021/acs.jmedchem.9b01342
CHEMBL4470527 175909 0 None -47 2 Human 6.4 pKi = 6.4 Binding
Displacement of 40 nM [3H]-histamine from human H4R expressed in Sf9 cell membranes co-expressing Gia2 and beta1gamma2 by competition binding assayDisplacement of 40 nM [3H]-histamine from human H4R expressed in Sf9 cell membranes co-expressing Gia2 and beta1gamma2 by competition binding assay
ChEMBL 288 7 3 5 2.7 CC(C)(C)CNc1nccc(NCCCc2c[nH]cn2)n1 10.1021/acs.jmedchem.9b01342
CHEMBL4596640 175909 0 None -47 2 Human 6.4 pKi = 6.4 Binding
Displacement of 40 nM [3H]-histamine from human H4R expressed in Sf9 cell membranes co-expressing Gia2 and beta1gamma2 by competition binding assayDisplacement of 40 nM [3H]-histamine from human H4R expressed in Sf9 cell membranes co-expressing Gia2 and beta1gamma2 by competition binding assay
ChEMBL 288 7 3 5 2.7 CC(C)(C)CNc1nccc(NCCCc2c[nH]cn2)n1 10.1021/acs.jmedchem.9b01342
51354873 58598 0 None - 1 Human 6.4 pKi = 6.4 Binding
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 267 6 1 4 2.2 c1ccc(Cn2cc(CCCc3c[nH]cn3)nn2)cc1 10.1021/jm1013488
CHEMBL1688984 58598 0 None - 1 Human 6.4 pKi = 6.4 Binding
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 267 6 1 4 2.2 c1ccc(Cn2cc(CCCc3c[nH]cn3)nn2)cc1 10.1021/jm1013488
51354874 58599 0 None - 1 Human 6.4 pKi = 6.4 Binding
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 335 6 1 4 3.5 Clc1ccc(Cn2cc(CCCc3c[nH]cn3)nn2)cc1Cl 10.1021/jm1013488
CHEMBL1688985 58599 0 None - 1 Human 6.4 pKi = 6.4 Binding
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 335 6 1 4 3.5 Clc1ccc(Cn2cc(CCCc3c[nH]cn3)nn2)cc1Cl 10.1021/jm1013488
168292954 192395 0 None -112 6 Human 5.4 pKi = 5.4 Binding
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 192395 0 None -112 6 Human 5.4 pKi = 5.4 Binding
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 192395 0 None -112 6 Human 5.4 pKi = 5.4 Binding
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
11779175 62836 0 None -5 3 Human 5.4 pKi = 5.4 Binding
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 293 8 2 3 3.4 O=C(NCCCC1CCCCC1)OCCCc1c[nH]cn1 10.1016/j.bmcl.2013.06.075
CHEMBL1774600 62836 0 None -5 3 Human 5.4 pKi = 5.4 Binding
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 293 8 2 3 3.4 O=C(NCCCC1CCCCC1)OCCCc1c[nH]cn1 10.1016/j.bmcl.2013.06.075
CHEMBL1789801 62836 0 None -5 3 Human 5.4 pKi = 5.4 Binding
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 293 8 2 3 3.4 O=C(NCCCC1CCCCC1)OCCCc1c[nH]cn1 10.1016/j.bmcl.2013.06.075
164612760 184135 0 None -38 4 Human 4.4 pKi = 4.4 Binding
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 390 7 4 4 2.5 Cc1nc(N)sc1CCCN/C(N)=N/C(=S)NC[C@H](C)c1ccccc1 10.1016/j.ejmech.2021.113190
CHEMBL4850490 184135 0 None -38 4 Human 4.4 pKi = 4.4 Binding
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 390 7 4 4 2.5 Cc1nc(N)sc1CCCN/C(N)=N/C(=S)NC[C@H](C)c1ccccc1 10.1016/j.ejmech.2021.113190
11779175 62836 0 None -5 3 Human 6.4 pKi = 6.4 Binding
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 293 8 2 3 3.4 O=C(NCCCC1CCCCC1)OCCCc1c[nH]cn1 10.1016/j.bmc.2011.03.046
CHEMBL1774600 62836 0 None -5 3 Human 6.4 pKi = 6.4 Binding
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 293 8 2 3 3.4 O=C(NCCCC1CCCCC1)OCCCc1c[nH]cn1 10.1016/j.bmc.2011.03.046
CHEMBL1789801 62836 0 None -5 3 Human 6.4 pKi = 6.4 Binding
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 293 8 2 3 3.4 O=C(NCCCC1CCCCC1)OCCCc1c[nH]cn1 10.1016/j.bmc.2011.03.046
58227085 116629 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 261 4 2 5 1.6 CN[C@H]1CCN(c2ccnc(NC3CCCC3)n2)C1 10.1016/j.bmcl.2014.12.027
CHEMBL3393545 116629 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 261 4 2 5 1.6 CN[C@H]1CCN(c2ccnc(NC3CCCC3)n2)C1 10.1016/j.bmcl.2014.12.027
1267 3744 43 None -33 25 Human 7.3 pKi = 7.3 Binding
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 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1039/C8MD00527C
3035905 3744 43 None -33 25 Human 7.3 pKi = 7.3 Binding
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 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1039/C8MD00527C
CHEMBL260374 3744 43 None -33 25 Human 7.3 pKi = 7.3 Binding
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 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1039/C8MD00527C
11846464 78051 0 None - 1 Human 7.3 pKi = 7.3 Binding
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 361 0 0 4 4.4 CN1CCN(C2=Nc3ccc(Cl)cc3Oc3c(Cl)cccc32)CC1 10.1021/jm051008s
CHEMBL211170 78051 0 None - 1 Human 7.3 pKi = 7.3 Binding
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 361 0 0 4 4.4 CN1CCN(C2=Nc3ccc(Cl)cc3Oc3c(Cl)cccc32)CC1 10.1021/jm051008s
118720433 115410 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 206 3 1 4 0.8 CCc1cc(N2CC[C@@H](NC)C2)ncn1 10.1016/j.bmcl.2014.10.013
CHEMBL3354807 115410 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 206 3 1 4 0.8 CCc1cc(N2CC[C@@H](NC)C2)ncn1 10.1016/j.bmcl.2014.10.013
51354581 58589 0 None -4 2 Human 6.3 pKi = 6.3 Binding
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 275 10 1 4 3.1 CCCCCCCc1cn(CCCc2c[nH]cn2)nn1 10.1021/jm1013488
CHEMBL1688973 58589 0 None -4 2 Human 6.3 pKi = 6.3 Binding
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 275 10 1 4 3.1 CCCCCCCc1cn(CCCc2c[nH]cn2)nn1 10.1021/jm1013488
9877454 203901 1 None -4 2 Human 5.3 pKi = 5.3 Binding
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 159 2 1 2 1.4 c1ccc(Cc2c[nH]cn2)nc1 10.1021/jm049932u
CHEMBL81644 203901 1 None -4 2 Human 5.3 pKi = 5.3 Binding
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 159 2 1 2 1.4 c1ccc(Cc2c[nH]cn2)nc1 10.1021/jm049932u
1613 2316 44 None -112 44 Human 5.3 pKi = 5.3 Binding
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(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 10.1021/jm051008s
205 2316 44 None -112 44 Human 5.3 pKi = 5.3 Binding
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(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 10.1021/jm051008s
3964 2316 44 None -112 44 Human 5.3 pKi = 5.3 Binding
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(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 10.1021/jm051008s
CHEMBL831 2316 44 None -112 44 Human 5.3 pKi = 5.3 Binding
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(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 10.1021/jm051008s
DB00408 2316 44 None -112 44 Human 5.3 pKi = 5.3 Binding
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(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 10.1021/jm051008s
164609493 183854 0 None -2630 6 Human 4.3 pKi = 4.3 Binding
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 350 6 4 5 1.9 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NC(C)c1ccco1 10.1016/j.ejmech.2021.113190
CHEMBL4846380 183854 0 None -2630 6 Human 4.3 pKi = 4.3 Binding
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 350 6 4 5 1.9 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NC(C)c1ccco1 10.1016/j.ejmech.2021.113190
71518698 86066 2 None - 1 Human 4.3 pKi = 4.3 Binding
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 218 1 3 5 -0.1 Nc1nc(N2CCNCC2)c2cc[nH]c2n1 10.1016/j.bmcl.2012.10.139
CHEMBL2314770 86066 2 None - 1 Human 4.3 pKi = 4.3 Binding
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 218 1 3 5 -0.1 Nc1nc(N2CCNCC2)c2cc[nH]c2n1 10.1016/j.bmcl.2012.10.139
4242975 18654 9 None - 1 Human 7.3 pKi = 7.3 Binding
Antagonist activity at Homo sapiens (human) histamine H4 receptorAntagonist activity at Homo sapiens (human) histamine H4 receptor
ChEMBL 257 1 1 2 1.9 Cc1ccc2[nH]c(C(=O)N3CCN(C)CC3)cc2c1 10.1007/s00044-004-0106-7
CHEMBL128088 18654 9 None - 1 Human 7.3 pKi = 7.3 Binding
Antagonist activity at Homo sapiens (human) histamine H4 receptorAntagonist activity at Homo sapiens (human) histamine H4 receptor
ChEMBL 257 1 1 2 1.9 Cc1ccc2[nH]c(C(=O)N3CCN(C)CC3)cc2c1 10.1007/s00044-004-0106-7
4242975 18654 9 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]- histamine from the recombinant human histamine H4 receptorDisplacement of [3H]- histamine from the recombinant human histamine H4 receptor
ChEMBL 257 1 1 2 1.9 Cc1ccc2[nH]c(C(=O)N3CCN(C)CC3)cc2c1 10.1021/jm0341047
CHEMBL128088 18654 9 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]- histamine from the recombinant human histamine H4 receptorDisplacement of [3H]- histamine from the recombinant human histamine H4 receptor
ChEMBL 257 1 1 2 1.9 Cc1ccc2[nH]c(C(=O)N3CCN(C)CC3)cc2c1 10.1021/jm0341047
16061961 197997 0 None 7 2 Human 7.3 pKi = 7.3 Binding
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 316 4 2 6 1.6 CN1CCN(c2cc(NCc3ccc(F)cc3)nc(N)n2)CC1 10.1016/j.bmc.2009.08.059
CHEMBL593103 197997 0 None 7 2 Human 7.3 pKi = 7.3 Binding
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 316 4 2 6 1.6 CN1CCN(c2cc(NCc3ccc(F)cc3)nc(N)n2)CC1 10.1016/j.bmc.2009.08.059
11258458 83040 0 None - 1 Human 7.3 pKi = 7.3 Binding
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 412 6 1 4 4.5 Cc1ccc2[nH]c(-c3ccc(OCCCN4CCN(C)CC4)cc3Cl)nc2c1C 10.1016/j.bmcl.2006.08.117
CHEMBL219930 83040 0 None - 1 Human 7.3 pKi = 7.3 Binding
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 412 6 1 4 4.5 Cc1ccc2[nH]c(-c3ccc(OCCCN4CCN(C)CC4)cc3Cl)nc2c1C 10.1016/j.bmcl.2006.08.117
57398183 67710 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 347 4 3 7 1.8 Nc1nc(N2CC[C@@H](NCCO)C2)c2oc3ccc(Cl)cc3c2n1 10.1016/j.bmcl.2011.08.014
CHEMBL1914545 67710 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 347 4 3 7 1.8 Nc1nc(N2CC[C@@H](NCCO)C2)c2oc3ccc(Cl)cc3c2n1 10.1016/j.bmcl.2011.08.014
4242975 18654 9 None - 1 Human 7.3 pKi = 7.3 Binding
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 257 1 1 2 1.9 Cc1ccc2[nH]c(C(=O)N3CCN(C)CC3)cc2c1 10.1021/jm0502081
CHEMBL128088 18654 9 None - 1 Human 7.3 pKi = 7.3 Binding
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 257 1 1 2 1.9 Cc1ccc2[nH]c(C(=O)N3CCN(C)CC3)cc2c1 10.1021/jm0502081
118720438 115416 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 220 3 1 4 1.4 CN[C@@H]1CCN(c2ccnc(C(C)C)n2)C1 10.1016/j.bmcl.2014.10.013
CHEMBL3354814 115416 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 220 3 1 4 1.4 CN[C@@H]1CCN(c2ccnc(C(C)C)n2)C1 10.1016/j.bmcl.2014.10.013
24854640 95613 0 None - 1 Human 6.3 pKi = 6.3 Binding
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 335 4 0 6 2.4 CN1CCN(c2nc3ccccc3nc2OCc2ccccn2)CC1 10.1021/jm7014217
CHEMBL259957 95613 0 None - 1 Human 6.3 pKi = 6.3 Binding
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 335 4 0 6 2.4 CN1CCN(c2nc3ccccc3nc2OCc2ccccn2)CC1 10.1021/jm7014217
135589846 141288 3 None - 1 Human 5.3 pKi = 5.3 Binding
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 356 2 2 5 3.1 OCCN1CCN(C2=Nc3cc(Cl)ccc3Nc3ccccc32)CC1 10.1021/jm051008s
CHEMBL386333 141288 3 None - 1 Human 5.3 pKi = 5.3 Binding
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 356 2 2 5 3.1 OCCN1CCN(C2=Nc3cc(Cl)ccc3Nc3ccccc32)CC1 10.1021/jm051008s
24826439 67780 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 299 2 2 7 1.4 COc1cccc2oc3c(N4CCNCC4)nc(N)nc3c12 10.1016/j.bmcl.2011.08.014
CHEMBL1914771 67780 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 299 2 2 7 1.4 COc1cccc2oc3c(N4CCNCC4)nc(N)nc3c12 10.1016/j.bmcl.2011.08.014
10446295 2101 29 None 269 2 Human 7.3 pKi = 7.3 Binding
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 278 1 1 3 1.6 CN1CCN(CC1)C(=O)c1nc2c([nH]1)cc(cc2)Cl 10.1016/j.bmcl.2011.07.114
1277 2101 29 None 269 2 Human 7.3 pKi = 7.3 Binding
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 278 1 1 3 1.6 CN1CCN(CC1)C(=O)c1nc2c([nH]1)cc(cc2)Cl 10.1016/j.bmcl.2011.07.114
CHEMBL185951 2101 29 None 269 2 Human 7.3 pKi = 7.3 Binding
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 278 1 1 3 1.6 CN1CCN(CC1)C(=O)c1nc2c([nH]1)cc(cc2)Cl 10.1016/j.bmcl.2011.07.114
10446295 2101 29 None 269 2 Human 7.3 pKi = 7.3 Binding
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 278 1 1 3 1.6 CN1CCN(CC1)C(=O)c1nc2c([nH]1)cc(cc2)Cl 10.1016/j.bmcl.2011.11.098
1277 2101 29 None 269 2 Human 7.3 pKi = 7.3 Binding
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 278 1 1 3 1.6 CN1CCN(CC1)C(=O)c1nc2c([nH]1)cc(cc2)Cl 10.1016/j.bmcl.2011.11.098
CHEMBL185951 2101 29 None 269 2 Human 7.3 pKi = 7.3 Binding
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 278 1 1 3 1.6 CN1CCN(CC1)C(=O)c1nc2c([nH]1)cc(cc2)Cl 10.1016/j.bmcl.2011.11.098
10023327 168450 0 None -144 3 Human 7.3 pKi = 7.3 Binding
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 390 7 2 3 5.2 Clc1ccc(CN/C(=N\C2CCCCC2)SCCCc2c[nH]cn2)cc1 10.1021/jm201042n
CHEMBL43934 168450 0 None -144 3 Human 7.3 pKi = 7.3 Binding
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 390 7 2 3 5.2 Clc1ccc(CN/C(=N\C2CCCCC2)SCCCc2c[nH]cn2)cc1 10.1021/jm201042n
1267 3744 43 None -33 25 Human 7.3 pKi = 7.3 Binding
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 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1021/jm8003625
3035905 3744 43 None -33 25 Human 7.3 pKi = 7.3 Binding
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 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1021/jm8003625
CHEMBL260374 3744 43 None -33 25 Human 7.3 pKi = 7.3 Binding
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 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1021/jm8003625
155556721 173982 0 None - 1 Human 6.3 pKi = 6.3 Binding
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 248 2 1 6 0.6 CC(C)=Cc1nc(N)nc(N2CCN(C)CC2)n1 10.1016/j.bmc.2019.02.020
CHEMBL4556243 173982 0 None - 1 Human 6.3 pKi = 6.3 Binding
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 248 2 1 6 0.6 CC(C)=Cc1nc(N)nc(N2CCN(C)CC2)n1 10.1016/j.bmc.2019.02.020
24854639 95689 0 None - 1 Human 6.3 pKi = 6.3 Binding
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 348 5 0 5 3.0 CN1CCN(c2nc3ccccc3nc2OCCc2ccccc2)CC1 10.1021/jm7014217
CHEMBL260458 95689 0 None - 1 Human 6.3 pKi = 6.3 Binding
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 348 5 0 5 3.0 CN1CCN(c2nc3ccccc3nc2OCCc2ccccc2)CC1 10.1021/jm7014217
11344458 203487 2 None -14 2 Human 6.3 pKi = 6.3 Binding
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 c1cncc(CCCc2c[nH]cn2)c1 10.1021/jm049932u
CHEMBL78497 203487 2 None -14 2 Human 6.3 pKi = 6.3 Binding
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 c1cncc(CCCc2c[nH]cn2)c1 10.1021/jm049932u
51354588 59855 0 None 3 2 Human 5.3 pKi = 5.3 Binding
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 292 6 0 5 2.1 c1c(CC2CCCCC2)nnn1CCCN1CCOCC1 10.1021/jm1013488
CHEMBL1688980 59855 0 None 3 2 Human 5.3 pKi = 5.3 Binding
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 292 6 0 5 2.1 c1c(CC2CCCCC2)nnn1CCCN1CCOCC1 10.1021/jm1013488
CHEMBL1739759 59855 0 None 3 2 Human 5.3 pKi = 5.3 Binding
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 292 6 0 5 2.1 c1c(CC2CCCCC2)nnn1CCCN1CCOCC1 10.1021/jm1013488
16106 117643 28 None -20 11 Human 5.3 pKi = 5.3 Binding
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 291 0 0 3 2.9 CN1CCN(C2=Nc3ccccc3Cc3ccccc32)CC1 10.1021/jm051008s
CHEMBL340801 117643 28 None -20 11 Human 5.3 pKi = 5.3 Binding
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 291 0 0 3 2.9 CN1CCN(C2=Nc3ccccc3Cc3ccccc32)CC1 10.1021/jm051008s
46881855 7664 0 None -15 4 Human 7.3 pKi = 7.3 Binding
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 337 3 2 5 2.5 CN[C@@H]1CCN(c2nc(N)nc3c2CCCC(c2ccccc2)C3)C1 10.1016/j.bmcl.2010.01.131
CHEMBL1089040 7664 0 None -15 4 Human 7.3 pKi = 7.3 Binding
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 337 3 2 5 2.5 CN[C@@H]1CCN(c2nc(N)nc3c2CCCC(c2ccccc2)C3)C1 10.1016/j.bmcl.2010.01.131
71519014 86040 0 None - 1 Human 4.3 pKi = 4.3 Binding
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 2 5 2.9 CC(C)N1CCN(c2nc(N)nc3[nH]c(-c4ccc(F)cc4)cc23)CC1 10.1016/j.bmcl.2012.10.139
CHEMBL2314499 86040 0 None - 1 Human 4.3 pKi = 4.3 Binding
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 2 5 2.9 CC(C)N1CCN(c2nc(N)nc3[nH]c(-c4ccc(F)cc4)cc23)CC1 10.1016/j.bmcl.2012.10.139
122193094 123395 0 None - 1 Human 5.3 pKi = 5.3 Binding
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 330 3 1 6 2.0 CN1CCN(c2nc(N)nc(/C=C/c3ccccc3Cl)n2)CC1 10.1016/j.ejmech.2015.08.014
CHEMBL3628041 123395 0 None - 1 Human 5.3 pKi = 5.3 Binding
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 330 3 1 6 2.0 CN1CCN(c2nc(N)nc(/C=C/c3ccccc3Cl)n2)CC1 10.1016/j.ejmech.2015.08.014
155513612 175746 0 None -1 4 Mouse 6.3 pKi = 6.3 Binding
Displacement of [3H]-UR-DEBa176 from mouse H4R expressed in HEK293T-SF-His6-CRE-Luc cellsDisplacement of [3H]-UR-DEBa176 from mouse H4R expressed in HEK293T-SF-His6-CRE-Luc cells
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 175746 0 None -1 4 Mouse 6.3 pKi = 6.3 Binding
Displacement of [3H]-UR-DEBa176 from mouse H4R expressed in HEK293T-SF-His6-CRE-Luc cellsDisplacement of [3H]-UR-DEBa176 from mouse H4R expressed in HEK293T-SF-His6-CRE-Luc cells
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 175746 0 None -1 4 Mouse 6.3 pKi = 6.3 Binding
Displacement of [3H]-UR-DEBa176 from mouse H4R expressed in HEK293T-SF-His6-CRE-Luc cellsDisplacement of [3H]-UR-DEBa176 from mouse H4R expressed in HEK293T-SF-His6-CRE-Luc cells
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 175746 0 None -1 4 Mouse 6.3 pKi = 6.3 Binding
Displacement of [3H]-UR-DEBa176 from mouse H4R expressed in HEK293T-SF-His6-CRE-Luc cellsDisplacement of [3H]-UR-DEBa176 from mouse H4R expressed in HEK293T-SF-His6-CRE-Luc cells
ChEMBL 277 4 1 5 2.1 CN(C)[C@@H]1CCN(c2ccnc(NCC(C)(C)C)n2)C1 10.1021/acs.jmedchem.9b01342
45379808 199534 0 None - 1 Human 6.3 pKi = 6.3 Binding
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 362 5 2 6 1.6 CC(=O)NCCNc1nc(N2CCN(C)CC2)nc2ccc(Cl)cc12 10.1021/jm901379s
CHEMBL603621 199534 0 None - 1 Human 6.3 pKi = 6.3 Binding
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 362 5 2 6 1.6 CC(=O)NCCNc1nc(N2CCN(C)CC2)nc2ccc(Cl)cc12 10.1021/jm901379s
168286426 192324 0 None -109 6 Human 5.3 pKi = 5.3 Binding
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 192324 0 None -109 6 Human 5.3 pKi = 5.3 Binding
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 192324 0 None -109 6 Human 5.3 pKi = 5.3 Binding
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
164620139 185206 0 None -56 4 Human 5.3 pKi = 5.3 Binding
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 436 8 4 4 3.4 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCC(c1ccccc1)c1ccccc1 10.1016/j.ejmech.2021.113190
CHEMBL4866734 185206 0 None -56 4 Human 5.3 pKi = 5.3 Binding
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 436 8 4 4 3.4 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCC(c1ccccc1)c1ccccc1 10.1016/j.ejmech.2021.113190
136042267 69569 0 None - 1 Human 7.3 pKi = 7.3 Binding
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 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 69569 0 None - 1 Human 7.3 pKi = 7.3 Binding
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 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
11623296 116522 0 None - 1 Human 7.3 pKi = 7.3 Binding
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 280 1 1 3 1.2 CN1CCN(C(=O)c2nc3c(F)c(F)ccc3[nH]2)CC1 10.1021/jm0502081
CHEMBL338972 116522 0 None - 1 Human 7.3 pKi = 7.3 Binding
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 280 1 1 3 1.2 CN1CCN(C(=O)c2nc3c(F)c(F)ccc3[nH]2)CC1 10.1021/jm0502081
11066922 19225 1 None - 1 Human 8.3 pKi = 8.3 Binding
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)c2cc3c(Cl)c(Cl)ccc3[nH]2)CC1 10.1007/s00044-004-0106-7
CHEMBL129436 19225 1 None - 1 Human 8.3 pKi = 8.3 Binding
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)c2cc3c(Cl)c(Cl)ccc3[nH]2)CC1 10.1007/s00044-004-0106-7
11066922 19225 1 None - 1 Human 8.3 pKi = 8.3 Binding
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)c2cc3c(Cl)c(Cl)ccc3[nH]2)CC1 10.1021/jm0341047
CHEMBL129436 19225 1 None - 1 Human 8.3 pKi = 8.3 Binding
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)c2cc3c(Cl)c(Cl)ccc3[nH]2)CC1 10.1021/jm0341047
49841845 69396 0 None 19 3 Human 8.3 pKi = 8.3 Binding
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)nc3cc(-c4ccco4)ccc23)CC1 10.1016/j.bmcl.2011.10.104
CHEMBL1935573 69396 0 None 19 3 Human 8.3 pKi = 8.3 Binding
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)nc3cc(-c4ccco4)ccc23)CC1 10.1016/j.bmcl.2011.10.104
25068753 187854 15 None -1 2 Human 8.3 pKi = 8.3 Binding
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 295 1 2 5 1.8 Nc1nc2c(c(N3CC[C@@H](N)C3)n1)CCCc1ccccc1-2 10.1016/j.bmcl.2011.10.104
CHEMBL502347 187854 15 None -1 2 Human 8.3 pKi = 8.3 Binding
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 295 1 2 5 1.8 Nc1nc2c(c(N3CC[C@@H](N)C3)n1)CCCc1ccccc1-2 10.1016/j.bmcl.2011.10.104
1223 940 32 None -60 11 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in SK-NM-C cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in SK-NM-C cells
ChEMBL 308 6 2 3 3.2 Clc1ccc(cc1)CN=C(SCCCc1cnc[nH]1)N 10.1021/jm7014777
2790 940 32 None -60 11 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in SK-NM-C cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in SK-NM-C cells
ChEMBL 308 6 2 3 3.2 Clc1ccc(cc1)CN=C(SCCCc1cnc[nH]1)N 10.1021/jm7014777
CHEMBL14690 940 32 None -60 11 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in SK-NM-C cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in SK-NM-C cells
ChEMBL 308 6 2 3 3.2 Clc1ccc(cc1)CN=C(SCCCc1cnc[nH]1)N 10.1021/jm7014777
1278 2119 79 None -3 8 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1016/j.bmcl.2014.10.013
1278 2119 79 None -3 8 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1016/j.bmcl.2014.12.027
1279 2119 79 None -3 8 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1016/j.bmcl.2014.10.013
1279 2119 79 None -3 8 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1016/j.bmcl.2014.12.027
4908365 2119 79 None -3 8 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1016/j.bmcl.2014.10.013
4908365 2119 79 None -3 8 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1016/j.bmcl.2014.12.027
CHEMBL129198 2119 79 None -3 8 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1016/j.bmcl.2014.10.013
CHEMBL129198 2119 79 None -3 8 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1016/j.bmcl.2014.12.027
58227086 116641 0 None - 1 Human 8.3 pKi = 8.3 Binding
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(c2cnnc(NC3CC4CCC3C4)c2)C1 10.1016/j.bmcl.2014.12.027
CHEMBL3393557 116641 0 None - 1 Human 8.3 pKi = 8.3 Binding
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(c2cnnc(NC3CC4CCC3C4)c2)C1 10.1016/j.bmcl.2014.12.027
1278 2119 79 None -3 8 Human 8.3 pKi = 8.3 Binding
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 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/jm401727m
1279 2119 79 None -3 8 Human 8.3 pKi = 8.3 Binding
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 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/jm401727m
4908365 2119 79 None -3 8 Human 8.3 pKi = 8.3 Binding
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 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/jm401727m
CHEMBL129198 2119 79 None -3 8 Human 8.3 pKi = 8.3 Binding
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 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/jm401727m
2063135 8293 9 None - 1 Human 8.3 pKi = 8.3 Binding
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 302 1 0 5 2.8 CN1CCN(c2ncnc3c2oc2ccc(Cl)cc23)CC1 10.1021/jm401727m
CHEMBL1093180 8293 9 None - 1 Human 8.3 pKi = 8.3 Binding
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 302 1 0 5 2.8 CN1CCN(c2ncnc3c2oc2ccc(Cl)cc23)CC1 10.1021/jm401727m
23650959 109632 0 None - 1 Human 8.3 pKi = 8.3 Binding
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 410 7 1 4 5.3 Cc1cnc(OCCCCC2CCN(C)CC2)cc1-c1nc2c(C)c(F)ccc2[nH]1 10.1021/jm401727m
CHEMBL3236548 109632 0 None - 1 Human 8.3 pKi = 8.3 Binding
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 410 7 1 4 5.3 Cc1cnc(OCCCCC2CCN(C)CC2)cc1-c1nc2c(C)c(F)ccc2[nH]1 10.1021/jm401727m
11066922 19225 1 None - 1 Human 8.3 pKi = 8.3 Binding
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)c2cc3c(Cl)c(Cl)ccc3[nH]2)CC1 10.1021/jm0502081
CHEMBL129436 19225 1 None - 1 Human 8.3 pKi = 8.3 Binding
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)c2cc3c(Cl)c(Cl)ccc3[nH]2)CC1 10.1021/jm0502081
155524115 175973 0 None -2 3 Human 8.3 pKi = 8.3 Binding
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 286 3 2 5 2.2 CC(C)(C)CNc1nccc(N2CCc3nc[nH]c3C2)n1 10.1021/acs.jmedchem.0c00160
CHEMBL4454158 175973 0 None -2 3 Human 8.3 pKi = 8.3 Binding
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 286 3 2 5 2.2 CC(C)(C)CNc1nccc(N2CCc3nc[nH]c3C2)n1 10.1021/acs.jmedchem.0c00160
CHEMBL4597218 175973 0 None -2 3 Human 8.3 pKi = 8.3 Binding
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 286 3 2 5 2.2 CC(C)(C)CNc1nccc(N2CCc3nc[nH]c3C2)n1 10.1021/acs.jmedchem.0c00160
70696620 75315 0 None - 1 Human 8.3 pKi = 8.3 Binding
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 292 1 2 3 1.8 CN1CCN(C(=O)c2cc3cc(Cl)cc(N)c3[nH]2)CC1 10.1016/j.ejmech.2012.06.016
CHEMBL2047450 75315 0 None - 1 Human 8.3 pKi = 8.3 Binding
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 292 1 2 3 1.8 CN1CCN(C(=O)c2cc3cc(Cl)cc(N)c3[nH]2)CC1 10.1016/j.ejmech.2012.06.016
25129523 186704 40 None 1 2 Human 8.3 pKi = 8.3 Binding
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 269 2 1 5 1.5 CN1CCN(c2cc(-c3ccccc3)nc(N)n2)CC1 10.1021/jm800670r
CHEMBL492884 186704 40 None 1 2 Human 8.3 pKi = 8.3 Binding
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 269 2 1 5 1.5 CN1CCN(c2cc(-c3ccccc3)nc(N)n2)CC1 10.1021/jm800670r
76311195 105571 0 None - 1 Human 8.3 pKi = 8.3 Binding
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 284 2 2 6 1.1 CN1CCN(c2cc(-c3ccc(N)cc3)nc(N)n2)CC1 10.1039/C2MD20212C
CHEMBL3133130 105571 0 None - 1 Human 8.3 pKi = 8.3 Binding
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 284 2 2 6 1.1 CN1CCN(c2cc(-c3ccc(N)cc3)nc(N)n2)CC1 10.1039/C2MD20212C
25129523 186704 40 None 1 2 Human 8.3 pKi = 8.3 Binding
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 269 2 1 5 1.5 CN1CCN(c2cc(-c3ccccc3)nc(N)n2)CC1 10.1039/C2MD20212C
CHEMBL492884 186704 40 None 1 2 Human 8.3 pKi = 8.3 Binding
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 269 2 1 5 1.5 CN1CCN(c2cc(-c3ccccc3)nc(N)n2)CC1 10.1039/C2MD20212C
25128824 192575 0 None -3 2 Human 8.3 pKi = 8.3 Binding
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 313 1 2 5 1.8 Nc1nc2c(c(N3CCNCC3)n1)CCCc1ccc(F)cc1-2 10.1021/jm800670r
CHEMBL523225 192575 0 None -3 2 Human 8.3 pKi = 8.3 Binding
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 313 1 2 5 1.8 Nc1nc2c(c(N3CCNCC3)n1)CCCc1ccc(F)cc1-2 10.1021/jm800670r
155524115 175973 0 None -2 3 Human 8.3 pKi = 8.3 Binding
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 286 3 2 5 2.2 CC(C)(C)CNc1nccc(N2CCc3nc[nH]c3C2)n1 10.1021/acs.jmedchem.9b01342
CHEMBL4454158 175973 0 None -2 3 Human 8.3 pKi = 8.3 Binding
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 286 3 2 5 2.2 CC(C)(C)CNc1nccc(N2CCc3nc[nH]c3C2)n1 10.1021/acs.jmedchem.9b01342
CHEMBL4597218 175973 0 None -2 3 Human 8.3 pKi = 8.3 Binding
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 286 3 2 5 2.2 CC(C)(C)CNc1nccc(N2CCc3nc[nH]c3C2)n1 10.1021/acs.jmedchem.9b01342
25128824 192575 0 None -3 2 Human 8.3 pKi = 8.3 Binding
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 313 1 2 5 1.8 Nc1nc2c(c(N3CCNCC3)n1)CCCc1ccc(F)cc1-2 10.1021/jm800670r
CHEMBL523225 192575 0 None -3 2 Human 8.3 pKi = 8.3 Binding
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 313 1 2 5 1.8 Nc1nc2c(c(N3CCNCC3)n1)CCCc1ccc(F)cc1-2 10.1021/jm800670r
25071004 192116 0 None -1 2 Rat 8.3 pKi = 8.3 Binding
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 309 2 2 5 2.0 CN[C@@H]1CCN(c2nc(N)nc3c2CCCc2ccccc2-3)C1 10.1021/jm800670r
CHEMBL521996 192116 0 None -1 2 Rat 8.3 pKi = 8.3 Binding
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 309 2 2 5 2.0 CN[C@@H]1CCN(c2nc(N)nc3c2CCCc2ccccc2-3)C1 10.1021/jm800670r
11705395 15876 0 None -1 4 Human 8.3 pKi = 8.3 Binding
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 428 7 1 4 5.6 Clc1cccc(N2CCN(CCCCNc3nccc4ccccc34)CC2)c1Cl 10.1016/j.ejmech.2016.09.074
CHEMBL1223749 15876 0 None -1 4 Human 8.3 pKi = 8.3 Binding
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 428 7 1 4 5.6 Clc1cccc(N2CCN(CCCCNc3nccc4ccccc34)CC2)c1Cl 10.1016/j.ejmech.2016.09.074
24826162 67800 0 None - 1 Human 8.3 pKi = 8.3 Binding
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)nc3c2sc2cc(Cl)ccc23)C1 10.1016/j.bmcl.2011.08.014
CHEMBL1914792 67800 0 None - 1 Human 8.3 pKi = 8.3 Binding
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)nc3c2sc2cc(Cl)ccc23)C1 10.1016/j.bmcl.2011.08.014
71519674 89299 0 None 1 5 Human 8.3 pKi = 8.3 Binding
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 270 3 2 6 0.9 CNC1CN(c2nc(N)nc3cc(C4CC4)cnc23)C1 10.1016/j.bmcl.2013.02.091
CHEMBL2376804 89299 0 None 1 5 Human 8.3 pKi = 8.3 Binding
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 270 3 2 6 0.9 CNC1CN(c2nc(N)nc3cc(C4CC4)cnc23)C1 10.1016/j.bmcl.2013.02.091
46890072 6832 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
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 6832 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 404 8 2 4 4.9 Cc1cc(OCCCNCc2cccnc2)ccc1-c1nc2c(C)c(F)ccc2[nH]1 10.1016/j.bmcl.2010.04.017
24994634 2111 26 None 2 7 Mouse 8.3 pKi = 8.3 Binding
Displacement of [3H]histamine from mouse histamine H4 receptor expressed in SK-N-MC cells after 45 mins by competition binding analysisDisplacement of [3H]histamine from mouse 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 2111 26 None 2 7 Mouse 8.3 pKi = 8.3 Binding
Displacement of [3H]histamine from mouse histamine H4 receptor expressed in SK-N-MC cells after 45 mins by competition binding analysisDisplacement of [3H]histamine from mouse 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 2111 26 None 2 7 Mouse 8.3 pKi = 8.3 Binding
Displacement of [3H]histamine from mouse histamine H4 receptor expressed in SK-N-MC cells after 45 mins by competition binding analysisDisplacement of [3H]histamine from mouse 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
24994634 2111 26 None 2 7 Mouse 8.3 pKi = 8.3 Binding
Displacement of [3H]histamine from mouse recombinant histamine H4 receptorDisplacement of [3H]histamine from mouse 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 2111 26 None 2 7 Mouse 8.3 pKi = 8.3 Binding
Displacement of [3H]histamine from mouse recombinant histamine H4 receptorDisplacement of [3H]histamine from mouse 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 2111 26 None 2 7 Mouse 8.3 pKi = 8.3 Binding
Displacement of [3H]histamine from mouse recombinant histamine H4 receptorDisplacement of [3H]histamine from mouse 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
44129056 197919 0 None - 1 Human 8.3 pKi = 8.3 Binding
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 474 7 1 7 2.9 CN1CCN(c2nc(NCCS(=O)(=O)N(C)c3ccccc3)c3cc(Cl)ccc3n2)CC1 10.1021/jm901379s
CHEMBL592663 197919 0 None - 1 Human 8.3 pKi = 8.3 Binding
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 474 7 1 7 2.9 CN1CCN(c2nc(NCCS(=O)(=O)N(C)c3ccccc3)c3cc(Cl)ccc3n2)CC1 10.1021/jm901379s
25128822 186898 0 None 10 5 Rat 8.3 pKi = 8.3 Binding
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 295 1 1 5 1.6 CN1CCN(c2nc(N)nc3c2CCc2ccccc2-3)CC1 10.1021/jm800670r
CHEMBL494093 186898 0 None 10 5 Rat 8.3 pKi = 8.3 Binding
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 295 1 1 5 1.6 CN1CCN(c2nc(N)nc3c2CCc2ccccc2-3)CC1 10.1021/jm800670r
11554490 15877 0 None -5 4 Human 8.3 pKi = 8.3 Binding
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 428 7 1 4 5.3 FC(F)(F)c1cccc(N2CCN(CCCCNc3nccc4ccccc34)CC2)c1 10.1016/j.ejmech.2016.09.074
CHEMBL1223750 15877 0 None -5 4 Human 8.3 pKi = 8.3 Binding
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 428 7 1 4 5.3 FC(F)(F)c1cccc(N2CCN(CCCCNc3nccc4ccccc34)CC2)c1 10.1016/j.ejmech.2016.09.074
24797956 109641 3 None - 1 Human 8.3 pKi = 8.3 Binding
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 233 2 2 5 0.9 Nc1nc(C2CCCC2)cc(N2CC(N)C2)n1 10.1021/jm401727m
CHEMBL3236558 109641 3 None - 1 Human 8.3 pKi = 8.3 Binding
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 233 2 2 5 0.9 Nc1nc(C2CCCC2)cc(N2CC(N)C2)n1 10.1021/jm401727m
24825514 186272 0 None 5 3 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in CHO cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in CHO cells
ChEMBL 256 4 1 2 3.6 CC(C)(C)CC(=O)c1cccc(Cc2c[nH]cn2)c1 10.1021/jm7014149
CHEMBL489493 186272 0 None 5 3 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in CHO cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in CHO cells
ChEMBL 256 4 1 2 3.6 CC(C)(C)CC(=O)c1cccc(Cc2c[nH]cn2)c1 10.1021/jm7014149
24825515 186734 0 None -1 3 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in CHO cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in CHO cells
ChEMBL 238 2 1 1 3.4 CC(C)(C)C#Cc1cccc(Cc2c[nH]cn2)c1 10.1021/jm7014149
CHEMBL493014 186734 0 None -1 3 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in CHO cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in CHO cells
ChEMBL 238 2 1 1 3.4 CC(C)(C)C#Cc1cccc(Cc2c[nH]cn2)c1 10.1021/jm7014149
11301441 95707 6 None - 1 Human 8.3 pKi = 8.3 Binding
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 312 1 1 4 2.0 CN1CCN(c2nc3cc(Cl)c(Cl)cc3[nH]c2=O)CC1 10.1021/jm800876b
CHEMBL260549 95707 6 None - 1 Human 8.3 pKi = 8.3 Binding
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 312 1 1 4 2.0 CN1CCN(c2nc3cc(Cl)c(Cl)cc3[nH]c2=O)CC1 10.1021/jm800876b
11301441 95707 6 None - 1 Human 8.3 pKi = 8.3 Binding
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 312 1 1 4 2.0 CN1CCN(c2nc3cc(Cl)c(Cl)cc3[nH]c2=O)CC1 10.1021/jm7014217
CHEMBL260549 95707 6 None - 1 Human 8.3 pKi = 8.3 Binding
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 312 1 1 4 2.0 CN1CCN(c2nc3cc(Cl)c(Cl)cc3[nH]c2=O)CC1 10.1021/jm7014217
24825791 67713 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 317 1 2 6 2.5 Nc1nc(N2CCC[C@H](N)C2)c2oc3ccc(Cl)cc3c2n1 10.1016/j.bmcl.2011.08.014
CHEMBL1914548 67713 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 317 1 2 6 2.5 Nc1nc(N2CCC[C@H](N)C2)c2oc3ccc(Cl)cc3c2n1 10.1016/j.bmcl.2011.08.014
25109291 190792 9 None -501 8 Human 8.2 pKi = 8.2 Binding
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 327 1 2 6 1.7 Nc1nc2c(c(N3CCNCC3)n1)CCC1=C2[C@@H]2CCCC[C@@H]2O1 10.1021/jm8007618
CHEMBL519240 190792 9 None -501 8 Human 8.2 pKi = 8.2 Binding
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 327 1 2 6 1.7 Nc1nc2c(c(N3CCNCC3)n1)CCC1=C2[C@@H]2CCCC[C@@H]2O1 10.1021/jm8007618
45379922 197882 0 None - 1 Human 8.2 pKi = 8.2 Binding
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 552 7 2 7 2.8 CN1CCN(c2nc(NCCS(=O)(=O)Nc3ccccc3)c3cc(I)ccc3n2)CC1 10.1021/jm901379s
CHEMBL592434 197882 0 None - 1 Human 8.2 pKi = 8.2 Binding
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 552 7 2 7 2.8 CN1CCN(c2nc(NCCS(=O)(=O)Nc3ccccc3)c3cc(I)ccc3n2)CC1 10.1021/jm901379s
54585777 61205 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]histamine from human histamine H4 receptorDisplacement of [3H]histamine from human histamine H4 receptor
ChEMBL 297 5 3 5 2.1 CN[C@@H]1CCN(c2cc(N)nc(NCc3ccccc3)c2)C1 10.1016/j.bmcl.2011.03.017
CHEMBL1770974 61205 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]histamine from human histamine H4 receptorDisplacement of [3H]histamine from human histamine H4 receptor
ChEMBL 297 5 3 5 2.1 CN[C@@H]1CCN(c2cc(N)nc(NCc3ccccc3)c2)C1 10.1016/j.bmcl.2011.03.017
118720441 115420 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 260 3 3 4 2.5 Nc1cc(C2CCNCC2)cc(NC2CCCC2)n1 10.1016/j.bmcl.2014.10.013
CHEMBL3354819 115420 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 260 3 3 4 2.5 Nc1cc(C2CCNCC2)cc(NC2CCCC2)n1 10.1016/j.bmcl.2014.10.013
24826518 67762 0 None - 1 Human 7.3 pKi = 7.3 Binding
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)nc3c2oc2cccc(C(F)(F)F)c23)CC1 10.1016/j.bmcl.2011.08.014
CHEMBL1914753 67762 0 None - 1 Human 7.3 pKi = 7.3 Binding
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)nc3c2oc2cccc(C(F)(F)F)c23)CC1 10.1016/j.bmcl.2011.08.014
1278 2119 79 None -3 8 Human 7.3 pKi = 7.3 Binding
Binding affinity to histamine H4 receptorBinding affinity to histamine H4 receptor
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 2119 79 None -3 8 Human 7.3 pKi = 7.3 Binding
Binding affinity to histamine H4 receptorBinding affinity to histamine H4 receptor
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 2119 79 None -3 8 Human 7.3 pKi = 7.3 Binding
Binding affinity to histamine H4 receptorBinding affinity to histamine H4 receptor
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 2119 79 None -3 8 Human 7.3 pKi = 7.3 Binding
Binding affinity to histamine H4 receptorBinding affinity to histamine H4 receptor
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1016/j.bmc.2009.08.059
136192886 56186 0 None 1 4 Human 7.3 pKi = 7.3 Binding
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 257 2 2 3 2.7 CN1CCC(/C(=N/O)c2cc3ccccc3[nH]2)CC1 10.1016/j.bmcl.2010.10.041
CHEMBL1632411 56186 0 None 1 4 Human 7.3 pKi = 7.3 Binding
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 257 2 2 3 2.7 CN1CCC(/C(=N/O)c2cc3ccccc3[nH]2)CC1 10.1016/j.bmcl.2010.10.041
136141537 56187 1 None -2 3 Human 7.3 pKi = 7.3 Binding
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 271 2 2 3 3.0 Cc1ccc2[nH]c(/C(=N\O)C3CCN(C)CC3)cc2c1 10.1016/j.bmcl.2010.10.041
CHEMBL1632412 56187 1 None -2 3 Human 7.3 pKi = 7.3 Binding
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 271 2 2 3 3.0 Cc1ccc2[nH]c(/C(=N\O)C3CCN(C)CC3)cc2c1 10.1016/j.bmcl.2010.10.041
71525678 89295 0 None -5 6 Mouse 7.3 pKi = 7.3 Binding
Binding affinity to mouse histamine H4 receptorBinding affinity to mouse histamine H4 receptor
ChEMBL 258 3 2 6 0.6 CCc1cnc2c(N3CC(NC)C3)nc(N)nc2c1 10.1016/j.bmcl.2013.02.091
CHEMBL2376800 89295 0 None -5 6 Mouse 7.3 pKi = 7.3 Binding
Binding affinity to mouse histamine H4 receptorBinding affinity to mouse histamine H4 receptor
ChEMBL 258 3 2 6 0.6 CCc1cnc2c(N3CC(NC)C3)nc(N)nc2c1 10.1016/j.bmcl.2013.02.091
1267 3744 43 None -14 25 Rat 7.3 pKi = 7.3 Binding
Binding affinity to rat histamine H4 receptorBinding affinity to rat histamine H4 receptor
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1021/jm100064d
3035905 3744 43 None -14 25 Rat 7.3 pKi = 7.3 Binding
Binding affinity to rat histamine H4 receptorBinding affinity to rat histamine H4 receptor
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1021/jm100064d
CHEMBL260374 3744 43 None -14 25 Rat 7.3 pKi = 7.3 Binding
Binding affinity to rat histamine H4 receptorBinding affinity to rat histamine H4 receptor
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1021/jm100064d
1223 940 32 None -60 11 Human 7.3 pKi = 7.3 Binding
Displacement of UR-DEBa176 from human recombinant H4R expressed in HEK293T-SF-His6-CRE-Luc cellsDisplacement of UR-DEBa176 from human recombinant H4R expressed in HEK293T-SF-His6-CRE-Luc cells
ChEMBL 308 6 2 3 3.2 Clc1ccc(cc1)CN=C(SCCCc1cnc[nH]1)N 10.1021/acs.jmedchem.0c00160
2790 940 32 None -60 11 Human 7.3 pKi = 7.3 Binding
Displacement of UR-DEBa176 from human recombinant H4R expressed in HEK293T-SF-His6-CRE-Luc cellsDisplacement of UR-DEBa176 from human recombinant H4R expressed in HEK293T-SF-His6-CRE-Luc cells
ChEMBL 308 6 2 3 3.2 Clc1ccc(cc1)CN=C(SCCCc1cnc[nH]1)N 10.1021/acs.jmedchem.0c00160
CHEMBL14690 940 32 None -60 11 Human 7.3 pKi = 7.3 Binding
Displacement of UR-DEBa176 from human recombinant H4R expressed in HEK293T-SF-His6-CRE-Luc cellsDisplacement of UR-DEBa176 from human recombinant H4R expressed in HEK293T-SF-His6-CRE-Luc cells
ChEMBL 308 6 2 3 3.2 Clc1ccc(cc1)CN=C(SCCCc1cnc[nH]1)N 10.1021/acs.jmedchem.0c00160
1223 940 32 None -60 11 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]-UR-PI294 from Galphai2/Gbeta1gamma2-coupled human recombinant H4R expressed in baculovirus infected Sf9 insect cell membranes co-expressing RGS19 measured after 60 mins by microbeta scintillation counting methodDisplacement of [3H]-UR-PI294 from Galphai2/Gbeta1gamma2-coupled human recombinant H4R expressed in baculovirus infected Sf9 insect cell membranes co-expressing RGS19 measured after 60 mins by microbeta scintillation counting method
ChEMBL 308 6 2 3 3.2 Clc1ccc(cc1)CN=C(SCCCc1cnc[nH]1)N 10.1021/acs.jmedchem.0c00160
2790 940 32 None -60 11 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]-UR-PI294 from Galphai2/Gbeta1gamma2-coupled human recombinant H4R expressed in baculovirus infected Sf9 insect cell membranes co-expressing RGS19 measured after 60 mins by microbeta scintillation counting methodDisplacement of [3H]-UR-PI294 from Galphai2/Gbeta1gamma2-coupled human recombinant H4R expressed in baculovirus infected Sf9 insect cell membranes co-expressing RGS19 measured after 60 mins by microbeta scintillation counting method
ChEMBL 308 6 2 3 3.2 Clc1ccc(cc1)CN=C(SCCCc1cnc[nH]1)N 10.1021/acs.jmedchem.0c00160
CHEMBL14690 940 32 None -60 11 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]-UR-PI294 from Galphai2/Gbeta1gamma2-coupled human recombinant H4R expressed in baculovirus infected Sf9 insect cell membranes co-expressing RGS19 measured after 60 mins by microbeta scintillation counting methodDisplacement of [3H]-UR-PI294 from Galphai2/Gbeta1gamma2-coupled human recombinant H4R expressed in baculovirus infected Sf9 insect cell membranes co-expressing RGS19 measured after 60 mins by microbeta scintillation counting method
ChEMBL 308 6 2 3 3.2 Clc1ccc(cc1)CN=C(SCCCc1cnc[nH]1)N 10.1021/acs.jmedchem.0c00160
1269 121 33 None 213 3 Human 7.3 pKi = 7.3 Binding
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 125 2 2 2 0.2 Cc1c(CCN)nc[nH]1 10.1016/j.bmcl.2010.10.041
37463 121 33 None 213 3 Human 7.3 pKi = 7.3 Binding
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 125 2 2 2 0.2 Cc1c(CCN)nc[nH]1 10.1016/j.bmcl.2010.10.041
CHEMBL275443 121 33 None 213 3 Human 7.3 pKi = 7.3 Binding
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 125 2 2 2 0.2 Cc1c(CCN)nc[nH]1 10.1016/j.bmcl.2010.10.041
1255 3146 11 None -12 4 Human 7.3 pKi = 7.3 Binding
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 216 6 1 2 2.6 C(CCc1cnc[nH]1)OCc1ccccc1 10.1016/j.bmcl.2010.10.041
6421522 3146 11 None -12 4 Human 7.3 pKi = 7.3 Binding
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 216 6 1 2 2.6 C(CCc1cnc[nH]1)OCc1ccccc1 10.1016/j.bmcl.2010.10.041
CHEMBL19173 3146 11 None -12 4 Human 7.3 pKi = 7.3 Binding
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 216 6 1 2 2.6 C(CCc1cnc[nH]1)OCc1ccccc1 10.1016/j.bmcl.2010.10.041
10017000 202780 0 None 1 2 Human 7.3 pKi = 7.3 Binding
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 288 7 3 2 2.4 S=C(NCCCCc1c[nH]cn1)NCc1ccccc1 10.1016/j.bmcl.2010.10.041
CHEMBL72431 202780 0 None 1 2 Human 7.3 pKi = 7.3 Binding
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 288 7 3 2 2.4 S=C(NCCCCc1c[nH]cn1)NCc1ccccc1 10.1016/j.bmcl.2010.10.041
1223 940 32 None -60 11 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]-histamine from human recombinant H4R expressed in HEK293T cell homogenatesDisplacement of [3H]-histamine from human recombinant H4R expressed in HEK293T cell homogenates
ChEMBL 308 6 2 3 3.2 Clc1ccc(cc1)CN=C(SCCCc1cnc[nH]1)N 10.1021/acs.jmedchem.0c00160
2790 940 32 None -60 11 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]-histamine from human recombinant H4R expressed in HEK293T cell homogenatesDisplacement of [3H]-histamine from human recombinant H4R expressed in HEK293T cell homogenates
ChEMBL 308 6 2 3 3.2 Clc1ccc(cc1)CN=C(SCCCc1cnc[nH]1)N 10.1021/acs.jmedchem.0c00160
CHEMBL14690 940 32 None -60 11 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]-histamine from human recombinant H4R expressed in HEK293T cell homogenatesDisplacement of [3H]-histamine from human recombinant H4R expressed in HEK293T cell homogenates
ChEMBL 308 6 2 3 3.2 Clc1ccc(cc1)CN=C(SCCCc1cnc[nH]1)N 10.1021/acs.jmedchem.0c00160
1223 940 32 None -60 11 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]-histamine from human recombinant H4R stably expressed in human SK-N-MC cell homogenatesDisplacement of [3H]-histamine from human recombinant H4R stably expressed in human SK-N-MC cell homogenates
ChEMBL 308 6 2 3 3.2 Clc1ccc(cc1)CN=C(SCCCc1cnc[nH]1)N 10.1021/acs.jmedchem.0c00160
2790 940 32 None -60 11 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]-histamine from human recombinant H4R stably expressed in human SK-N-MC cell homogenatesDisplacement of [3H]-histamine from human recombinant H4R stably expressed in human SK-N-MC cell homogenates
ChEMBL 308 6 2 3 3.2 Clc1ccc(cc1)CN=C(SCCCc1cnc[nH]1)N 10.1021/acs.jmedchem.0c00160
CHEMBL14690 940 32 None -60 11 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]-histamine from human recombinant H4R stably expressed in human SK-N-MC cell homogenatesDisplacement of [3H]-histamine from human recombinant H4R stably expressed in human SK-N-MC cell homogenates
ChEMBL 308 6 2 3 3.2 Clc1ccc(cc1)CN=C(SCCCc1cnc[nH]1)N 10.1021/acs.jmedchem.0c00160
1223 940 32 None -60 11 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]-histamine from human recombinant H4R stably expressed in human SK-N-MC cell membranesDisplacement of [3H]-histamine from human recombinant H4R stably expressed in human SK-N-MC cell membranes
ChEMBL 308 6 2 3 3.2 Clc1ccc(cc1)CN=C(SCCCc1cnc[nH]1)N 10.1021/acs.jmedchem.0c00160
2790 940 32 None -60 11 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]-histamine from human recombinant H4R stably expressed in human SK-N-MC cell membranesDisplacement of [3H]-histamine from human recombinant H4R stably expressed in human SK-N-MC cell membranes
ChEMBL 308 6 2 3 3.2 Clc1ccc(cc1)CN=C(SCCCc1cnc[nH]1)N 10.1021/acs.jmedchem.0c00160
CHEMBL14690 940 32 None -60 11 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]-histamine from human recombinant H4R stably expressed in human SK-N-MC cell membranesDisplacement of [3H]-histamine from human recombinant H4R stably expressed in human SK-N-MC cell membranes
ChEMBL 308 6 2 3 3.2 Clc1ccc(cc1)CN=C(SCCCc1cnc[nH]1)N 10.1021/acs.jmedchem.0c00160
1223 940 32 None -60 11 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]JNJ7777120 from human H4 receptor E5.46Q mutant expressed in HEK293 cells after 1 to 1.5 hrs by scintillation countingDisplacement of [3H]JNJ7777120 from human H4 receptor E5.46Q 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 940 32 None -60 11 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]JNJ7777120 from human H4 receptor E5.46Q mutant expressed in HEK293 cells after 1 to 1.5 hrs by scintillation countingDisplacement of [3H]JNJ7777120 from human H4 receptor E5.46Q 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 940 32 None -60 11 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]JNJ7777120 from human H4 receptor E5.46Q mutant expressed in HEK293 cells after 1 to 1.5 hrs by scintillation countingDisplacement of [3H]JNJ7777120 from human H4 receptor E5.46Q 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
71681644 89237 0 None - 1 Human 7.3 pKi = 7.3 Binding
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 412 9 4 8 3.8 CC(C)CNc1nccc(NCCNc2cc(-c3cccc(Cl)c3)nc(N)n2)n1 10.1021/jm301886t
CHEMBL2375767 89237 0 None - 1 Human 7.3 pKi = 7.3 Binding
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 412 9 4 8 3.8 CC(C)CNc1nccc(NCCNc2cc(-c3cccc(Cl)c3)nc(N)n2)n1 10.1021/jm301886t
71681805 89242 0 None - 1 Human 7.3 pKi = 7.3 Binding
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 426 9 3 8 3.8 CC(C)CNc1nccc(NCCN(C)c2cc(-c3cccc(Cl)c3)nc(N)n2)n1 10.1021/jm301886t
CHEMBL2375771 89242 0 None - 1 Human 7.3 pKi = 7.3 Binding
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 426 9 3 8 3.8 CC(C)CNc1nccc(NCCN(C)c2cc(-c3cccc(Cl)c3)nc(N)n2)n1 10.1021/jm301886t
11506928 74093 0 None -1 2 Human 7.3 pKi = 7.3 Binding
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 235 6 2 2 3.0 c1nc(CCCCNC2CCCCCC2)c[nH]1 10.1021/jm0504353
CHEMBL202728 74093 0 None -1 2 Human 7.3 pKi = 7.3 Binding
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 235 6 2 2 3.0 c1nc(CCCCNC2CCCCCC2)c[nH]1 10.1021/jm0504353
11600779 75695 0 None -6 2 Human 7.3 pKi = 7.3 Binding
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 181 7 2 2 1.7 CCCNCCCCc1c[nH]cn1 10.1021/jm0504353
CHEMBL205731 75695 0 None -6 2 Human 7.3 pKi = 7.3 Binding
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 181 7 2 2 1.7 CCCNCCCCc1c[nH]cn1 10.1021/jm0504353
11536119 138178 0 None -15 2 Human 7.3 pKi = 7.3 Binding
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 249 7 2 2 3.4 c1nc(CCCCCNC2CCCCCC2)c[nH]1 10.1021/jm0504353
CHEMBL377954 138178 0 None -15 2 Human 7.3 pKi = 7.3 Binding
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 249 7 2 2 3.4 c1nc(CCCCCNC2CCCCCC2)c[nH]1 10.1021/jm0504353
4242975 18654 9 None - 1 Human 7.3 pKi = 7.3 Binding
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 Cc1ccc2[nH]c(C(=O)N3CCN(C)CC3)cc2c1 10.1016/j.ejmech.2012.06.016
CHEMBL128088 18654 9 None - 1 Human 7.3 pKi = 7.3 Binding
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 Cc1ccc2[nH]c(C(=O)N3CCN(C)CC3)cc2c1 10.1016/j.ejmech.2012.06.016
45379921 197524 0 None - 1 Human 7.3 pKi = 7.3 Binding
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 426 6 1 7 3.6 CN1CCN(c2nc(NCCc3ccc([N+](=O)[O-])cc3)c3cc(Cl)ccc3n2)CC1 10.1021/jm901379s
CHEMBL589800 197524 0 None - 1 Human 7.3 pKi = 7.3 Binding
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 426 6 1 7 3.6 CN1CCN(c2nc(NCCc3ccc([N+](=O)[O-])cc3)c3cc(Cl)ccc3n2)CC1 10.1021/jm901379s
9972181 193547 0 None -5 2 Human 7.3 pKi = 7.3 Binding
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 8 3 3 3.2 N=C(NCCCc1ccccc1)SCCCc1c[nH]cn1 10.1016/j.bmc.2009.04.007
CHEMBL1202331 193547 0 None -5 2 Human 7.3 pKi = 7.3 Binding
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 8 3 3 3.2 N=C(NCCCc1ccccc1)SCCCc1c[nH]cn1 10.1016/j.bmc.2009.04.007
CHEMBL550757 193547 0 None -5 2 Human 7.3 pKi = 7.3 Binding
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 8 3 3 3.2 N=C(NCCCc1ccccc1)SCCCc1c[nH]cn1 10.1016/j.bmc.2009.04.007
10063835 62793 0 None -2 2 Human 6.3 pKi = 6.3 Binding
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 307 9 2 3 3.8 O=C(NCCCCC1CCCCC1)OCCCc1c[nH]cn1 10.1016/j.bmc.2011.03.046
CHEMBL1774601 62793 0 None -2 2 Human 6.3 pKi = 6.3 Binding
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 307 9 2 3 3.8 O=C(NCCCCC1CCCCC1)OCCCc1c[nH]cn1 10.1016/j.bmc.2011.03.046
CHEMBL1789356 62793 0 None -2 2 Human 6.3 pKi = 6.3 Binding
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 307 9 2 3 3.8 O=C(NCCCCC1CCCCC1)OCCCc1c[nH]cn1 10.1016/j.bmc.2011.03.046
46890200 7081 0 None - 1 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 442 9 1 4 5.4 CN(C)CCN(C)CCCOc1ccc(-c2nc3cc(C(C)(C)C)ccc3[nH]2)cc1Cl 10.1016/j.bmcl.2010.04.017
CHEMBL1085403 7081 0 None - 1 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 442 9 1 4 5.4 CN(C)CCN(C)CCCOc1ccc(-c2nc3cc(C(C)(C)C)ccc3[nH]2)cc1Cl 10.1016/j.bmcl.2010.04.017
1267 3744 43 None -33 25 Human 6.3 pKi = 6.3 Binding
Displacement of UR-DEBa176 from human recombinant H4R expressed in HEK293T-SF-His6-CRE-Luc cellsDisplacement of UR-DEBa176 from human recombinant H4R expressed in HEK293T-SF-His6-CRE-Luc cells
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1021/acs.jmedchem.0c00160
3035905 3744 43 None -33 25 Human 6.3 pKi = 6.3 Binding
Displacement of UR-DEBa176 from human recombinant H4R expressed in HEK293T-SF-His6-CRE-Luc cellsDisplacement of UR-DEBa176 from human recombinant H4R expressed in HEK293T-SF-His6-CRE-Luc cells
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1021/acs.jmedchem.0c00160
CHEMBL260374 3744 43 None -33 25 Human 6.3 pKi = 6.3 Binding
Displacement of UR-DEBa176 from human recombinant H4R expressed in HEK293T-SF-His6-CRE-Luc cellsDisplacement of UR-DEBa176 from human recombinant H4R expressed in HEK293T-SF-His6-CRE-Luc cells
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1021/acs.jmedchem.0c00160
1204 1901 114 None -15 23 Mouse 6.3 pKi = 6.3 Binding
Displacement of UR-DEBa176 from mouse recombinant H4R expressed in HEK293T-SF-His6-CRE-Luc cellsDisplacement of UR-DEBa176 from mouse recombinant H4R expressed in HEK293T-SF-His6-CRE-Luc cells
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.0c00160
1247 1901 114 None -15 23 Mouse 6.3 pKi = 6.3 Binding
Displacement of UR-DEBa176 from mouse recombinant H4R expressed in HEK293T-SF-His6-CRE-Luc cellsDisplacement of UR-DEBa176 from mouse recombinant H4R expressed in HEK293T-SF-His6-CRE-Luc cells
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.0c00160
1375 1901 114 None -15 23 Mouse 6.3 pKi = 6.3 Binding
Displacement of UR-DEBa176 from mouse recombinant H4R expressed in HEK293T-SF-His6-CRE-Luc cellsDisplacement of UR-DEBa176 from mouse recombinant H4R expressed in HEK293T-SF-His6-CRE-Luc cells
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.0c00160
774 1901 114 None -15 23 Mouse 6.3 pKi = 6.3 Binding
Displacement of UR-DEBa176 from mouse recombinant H4R expressed in HEK293T-SF-His6-CRE-Luc cellsDisplacement of UR-DEBa176 from mouse recombinant H4R expressed in HEK293T-SF-His6-CRE-Luc cells
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.0c00160
CHEMBL90 1901 114 None -15 23 Mouse 6.3 pKi = 6.3 Binding
Displacement of UR-DEBa176 from mouse recombinant H4R expressed in HEK293T-SF-His6-CRE-Luc cellsDisplacement of UR-DEBa176 from mouse recombinant H4R expressed in HEK293T-SF-His6-CRE-Luc cells
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.0c00160
DB05381 1901 114 None -15 23 Mouse 6.3 pKi = 6.3 Binding
Displacement of UR-DEBa176 from mouse recombinant H4R expressed in HEK293T-SF-His6-CRE-Luc cellsDisplacement of UR-DEBa176 from mouse recombinant H4R expressed in HEK293T-SF-His6-CRE-Luc cells
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.0c00160
1267 3744 43 None -33 25 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-UR-PI294 from Galphai2/Gbeta1gamma2-coupled human recombinant H4R expressed in baculovirus infected Sf9 insect cell membranes co-expressing RGS19 measured after 60 mins by microbeta scintillation counting methodDisplacement of [3H]-UR-PI294 from Galphai2/Gbeta1gamma2-coupled human recombinant H4R expressed in baculovirus infected Sf9 insect cell membranes co-expressing RGS19 measured after 60 mins by microbeta scintillation counting method
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1021/acs.jmedchem.0c00160
3035905 3744 43 None -33 25 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-UR-PI294 from Galphai2/Gbeta1gamma2-coupled human recombinant H4R expressed in baculovirus infected Sf9 insect cell membranes co-expressing RGS19 measured after 60 mins by microbeta scintillation counting methodDisplacement of [3H]-UR-PI294 from Galphai2/Gbeta1gamma2-coupled human recombinant H4R expressed in baculovirus infected Sf9 insect cell membranes co-expressing RGS19 measured after 60 mins by microbeta scintillation counting method
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1021/acs.jmedchem.0c00160
CHEMBL260374 3744 43 None -33 25 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-UR-PI294 from Galphai2/Gbeta1gamma2-coupled human recombinant H4R expressed in baculovirus infected Sf9 insect cell membranes co-expressing RGS19 measured after 60 mins by microbeta scintillation counting methodDisplacement of [3H]-UR-PI294 from Galphai2/Gbeta1gamma2-coupled human recombinant H4R expressed in baculovirus infected Sf9 insect cell membranes co-expressing RGS19 measured after 60 mins by microbeta scintillation counting method
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1021/acs.jmedchem.0c00160
1267 3744 43 None -33 25 Human 6.3 pKi = 6.3 Binding
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 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1021/acs.jmedchem.0c00160
3035905 3744 43 None -33 25 Human 6.3 pKi = 6.3 Binding
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 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1021/acs.jmedchem.0c00160
CHEMBL260374 3744 43 None -33 25 Human 6.3 pKi = 6.3 Binding
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 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1021/acs.jmedchem.0c00160
1267 3744 43 None -33 25 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-histamine from Galphai2/Gbeta1gamma2-coupled human recombinant H4R expressed in baculovirus infected Sf9 insect cell membranes co-expressing RGS19Displacement of [3H]-histamine from Galphai2/Gbeta1gamma2-coupled human recombinant H4R expressed in baculovirus infected Sf9 insect cell membranes co-expressing RGS19
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1021/acs.jmedchem.0c00160
3035905 3744 43 None -33 25 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-histamine from Galphai2/Gbeta1gamma2-coupled human recombinant H4R expressed in baculovirus infected Sf9 insect cell membranes co-expressing RGS19Displacement of [3H]-histamine from Galphai2/Gbeta1gamma2-coupled human recombinant H4R expressed in baculovirus infected Sf9 insect cell membranes co-expressing RGS19
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1021/acs.jmedchem.0c00160
CHEMBL260374 3744 43 None -33 25 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-histamine from Galphai2/Gbeta1gamma2-coupled human recombinant H4R expressed in baculovirus infected Sf9 insect cell membranes co-expressing RGS19Displacement of [3H]-histamine from Galphai2/Gbeta1gamma2-coupled human recombinant H4R expressed in baculovirus infected Sf9 insect cell membranes co-expressing RGS19
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1021/acs.jmedchem.0c00160
1267 3744 43 None -33 25 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-histamine from human recombinant H4R expressed in HEK293T cell homogenatesDisplacement of [3H]-histamine from human recombinant H4R expressed in HEK293T cell homogenates
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1021/acs.jmedchem.0c00160
3035905 3744 43 None -33 25 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-histamine from human recombinant H4R expressed in HEK293T cell homogenatesDisplacement of [3H]-histamine from human recombinant H4R expressed in HEK293T cell homogenates
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1021/acs.jmedchem.0c00160
CHEMBL260374 3744 43 None -33 25 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-histamine from human recombinant H4R expressed in HEK293T cell homogenatesDisplacement of [3H]-histamine from human recombinant H4R expressed in HEK293T cell homogenates
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1021/acs.jmedchem.0c00160
1267 3744 43 None -33 25 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-histamine from human recombinant H4R stably expressed in human SK-N-MC cell homogenatesDisplacement of [3H]-histamine from human recombinant H4R stably expressed in human SK-N-MC cell homogenates
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1021/acs.jmedchem.0c00160
3035905 3744 43 None -33 25 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-histamine from human recombinant H4R stably expressed in human SK-N-MC cell homogenatesDisplacement of [3H]-histamine from human recombinant H4R stably expressed in human SK-N-MC cell homogenates
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1021/acs.jmedchem.0c00160
CHEMBL260374 3744 43 None -33 25 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-histamine from human recombinant H4R stably expressed in human SK-N-MC cell homogenatesDisplacement of [3H]-histamine from human recombinant H4R stably expressed in human SK-N-MC cell homogenates
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1021/acs.jmedchem.0c00160
1267 3744 43 None -33 25 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-histamine from human recombinant H4R stably expressed in human SK-N-MC cell membranesDisplacement of [3H]-histamine from human recombinant H4R stably expressed in human SK-N-MC cell membranes
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1021/acs.jmedchem.0c00160
3035905 3744 43 None -33 25 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-histamine from human recombinant H4R stably expressed in human SK-N-MC cell membranesDisplacement of [3H]-histamine from human recombinant H4R stably expressed in human SK-N-MC cell membranes
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1021/acs.jmedchem.0c00160
CHEMBL260374 3744 43 None -33 25 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-histamine from human recombinant H4R stably expressed in human SK-N-MC cell membranesDisplacement of [3H]-histamine from human recombinant H4R stably expressed in human SK-N-MC cell membranes
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1021/acs.jmedchem.0c00160
71681803 89186 0 None - 1 Human 6.3 pKi = 6.3 Binding
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 378 9 4 8 3.1 CC(C)CNc1cc(NCCNc2cc(-c3ccccc3)nc(N)n2)ncn1 10.1021/jm301886t
CHEMBL2375363 89186 0 None - 1 Human 6.3 pKi = 6.3 Binding
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 378 9 4 8 3.1 CC(C)CNc1cc(NCCNc2cc(-c3ccccc3)nc(N)n2)ncn1 10.1021/jm301886t
11672774 3998 6 None -31 2 Human 6.3 pKi = 6.3 Binding
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 181 6 1 2 1.7 CN(CCCCCc1[nH]cnc1)C 10.1021/jm0504353
1245 3998 6 None -31 2 Human 6.3 pKi = 6.3 Binding
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 181 6 1 2 1.7 CN(CCCCCc1[nH]cnc1)C 10.1021/jm0504353
CHEMBL206548 3998 6 None -31 2 Human 6.3 pKi = 6.3 Binding
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 181 6 1 2 1.7 CN(CCCCCc1[nH]cnc1)C 10.1021/jm0504353
11564628 75180 0 None -12 2 Human 6.3 pKi = 6.3 Binding
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 193 5 1 2 1.8 c1nc(CCCCN2CCCC2)c[nH]1 10.1021/jm0504353
CHEMBL204360 75180 0 None -12 2 Human 6.3 pKi = 6.3 Binding
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 193 5 1 2 1.8 c1nc(CCCCN2CCCC2)c[nH]1 10.1021/jm0504353
11629931 75958 0 None -12 2 Human 6.3 pKi = 6.3 Binding
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 5 1 2 2.6 c1nc(CCCCN2CCCCCC2)c[nH]1 10.1021/jm0504353
CHEMBL205868 75958 0 None -12 2 Human 6.3 pKi = 6.3 Binding
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 5 1 2 2.6 c1nc(CCCCN2CCCCCC2)c[nH]1 10.1021/jm0504353
70686222 75329 0 None - 1 Human 6.3 pKi = 6.3 Binding
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 261 2 2 2 1.7 CN[C@@H]1CCN(C(=O)c2cc3cccc(F)c3[nH]2)C1 10.1016/j.ejmech.2012.06.016
CHEMBL2047464 75329 0 None - 1 Human 6.3 pKi = 6.3 Binding
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 261 2 2 2 1.7 CN[C@@H]1CCN(C(=O)c2cc3cccc(F)c3[nH]2)C1 10.1016/j.ejmech.2012.06.016
135398737 944 89 None -57 91 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]histamine from wild type human histamine H4 receptor transfected in HEK293T cells after 1 hr by liquid scintillation counting analysisDisplacement of [3H]histamine from wild type human histamine H4 receptor transfected in HEK293T cells after 1 hr by liquid scintillation counting analysis
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1039/C2MD20212C
38 944 89 None -57 91 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]histamine from wild type human histamine H4 receptor transfected in HEK293T cells after 1 hr by liquid scintillation counting analysisDisplacement of [3H]histamine from wild type human histamine H4 receptor transfected in HEK293T cells after 1 hr by liquid scintillation counting analysis
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1039/C2MD20212C
722 944 89 None -57 91 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]histamine from wild type human histamine H4 receptor transfected in HEK293T cells after 1 hr by liquid scintillation counting analysisDisplacement of [3H]histamine from wild type human histamine H4 receptor transfected in HEK293T cells after 1 hr by liquid scintillation counting analysis
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1039/C2MD20212C
CHEMBL42 944 89 None -57 91 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]histamine from wild type human histamine H4 receptor transfected in HEK293T cells after 1 hr by liquid scintillation counting analysisDisplacement of [3H]histamine from wild type human histamine H4 receptor transfected in HEK293T cells after 1 hr by liquid scintillation counting analysis
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1039/C2MD20212C
DB00363 944 89 None -57 91 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]histamine from wild type human histamine H4 receptor transfected in HEK293T cells after 1 hr by liquid scintillation counting analysisDisplacement of [3H]histamine from wild type human histamine H4 receptor transfected in HEK293T cells after 1 hr by liquid scintillation counting analysis
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1039/C2MD20212C
44395314 123169 0 None -3 2 Human 5.3 pKi = 5.3 Binding
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 278 2 2 2 3.2 CN1CCC(C(O)c2cc3cc(Cl)ccc3[nH]2)CC1 10.1016/j.bmcl.2004.08.035
CHEMBL362163 123169 0 None -3 2 Human 5.3 pKi = 5.3 Binding
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 278 2 2 2 3.2 CN1CCC(C(O)c2cc3cc(Cl)ccc3[nH]2)CC1 10.1016/j.bmcl.2004.08.035
126688 400 28 None 1 3 Human 5.3 pKi = 5.3 Binding
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 157 2 2 4 0.5 NCCc1sc(nc1C)N 10.1016/j.bmcl.2010.10.041
4025 400 28 None 1 3 Human 5.3 pKi = 5.3 Binding
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 157 2 2 4 0.5 NCCc1sc(nc1C)N 10.1016/j.bmcl.2010.10.041
CHEMBL293762 400 28 None 1 3 Human 5.3 pKi = 5.3 Binding
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 157 2 2 4 0.5 NCCc1sc(nc1C)N 10.1016/j.bmcl.2010.10.041
66572110 75291 0 None - 1 Human 5.3 pKi = 5.3 Binding
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 285 2 1 3 1.8 CC(=O)c1cccc2[nH]c(C(=O)N3CCN(C)CC3)cc12 10.1016/j.ejmech.2012.06.016
CHEMBL2047269 75291 0 None - 1 Human 5.3 pKi = 5.3 Binding
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 285 2 1 3 1.8 CC(=O)c1cccc2[nH]c(C(=O)N3CCN(C)CC3)cc12 10.1016/j.ejmech.2012.06.016
70684085 75322 0 None - 1 Human 5.3 pKi = 5.3 Binding
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 325 1 1 2 3.0 CN1CCCN(C(=O)c2cc3cccc(C(F)(F)F)c3[nH]2)CC1 10.1016/j.ejmech.2012.06.016
CHEMBL2047457 75322 0 None - 1 Human 5.3 pKi = 5.3 Binding
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 325 1 1 2 3.0 CN1CCCN(C(=O)c2cc3cccc(C(F)(F)F)c3[nH]2)CC1 10.1016/j.ejmech.2012.06.016
10063835 62793 0 None -2 2 Human 5.3 pKi = 5.3 Binding
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 307 9 2 3 3.8 O=C(NCCCCC1CCCCC1)OCCCc1c[nH]cn1 10.1016/j.bmcl.2013.06.075
CHEMBL1774601 62793 0 None -2 2 Human 5.3 pKi = 5.3 Binding
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 307 9 2 3 3.8 O=C(NCCCCC1CCCCC1)OCCCc1c[nH]cn1 10.1016/j.bmcl.2013.06.075
CHEMBL1789356 62793 0 None -2 2 Human 5.3 pKi = 5.3 Binding
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 307 9 2 3 3.8 O=C(NCCCCC1CCCCC1)OCCCc1c[nH]cn1 10.1016/j.bmcl.2013.06.075
206876 18756 7 None - 1 Human 5.3 pKi = 5.3 Binding
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 273 2 1 3 1.6 COc1ccc2[nH]c(C(=O)N3CCN(C)CC3)cc2c1 10.1039/C2MD20212C
CHEMBL128637 18756 7 None - 1 Human 5.3 pKi = 5.3 Binding
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 273 2 1 3 1.6 COc1ccc2[nH]c(C(=O)N3CCN(C)CC3)cc2c1 10.1039/C2MD20212C
57395620 67874 0 None 15 3 Human 6.3 pKi = 6.3 Binding
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 263 5 3 5 2.1 CC(C)(C)CCNc1cc(N[C@H]2CCNC2)ncn1 10.1016/j.bmcl.2011.07.125
CHEMBL1915534 67874 0 None 15 3 Human 6.3 pKi = 6.3 Binding
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 263 5 3 5 2.1 CC(C)(C)CCNc1cc(N[C@H]2CCNC2)ncn1 10.1016/j.bmcl.2011.07.125
57395620 67874 0 None 15 3 Human 6.3 pKi = 6.3 Binding
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 263 5 3 5 2.1 CC(C)(C)CCNc1cc(N[C@H]2CCNC2)ncn1 10.1016/j.bmcl.2011.07.114
CHEMBL1915534 67874 0 None 15 3 Human 6.3 pKi = 6.3 Binding
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 263 5 3 5 2.1 CC(C)(C)CCNc1cc(N[C@H]2CCNC2)ncn1 10.1016/j.bmcl.2011.07.114
90645160 111695 0 None - 1 Human 5.3 pKi = 5.3 Binding
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(-c3c(F)cccc3F)n2)CC1 10.1016/j.ejmech.2014.06.032
CHEMBL3290587 111695 0 None - 1 Human 5.3 pKi = 5.3 Binding
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(-c3c(F)cccc3F)n2)CC1 10.1016/j.ejmech.2014.06.032
57390145 69563 0 None - 1 Human 5.3 pKi = 5.3 Binding
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 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 69563 0 None - 1 Human 5.3 pKi = 5.3 Binding
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 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
49865668 15875 0 None -51 4 Human 7.3 pKi = 7.3 Binding
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 390 8 1 5 4.3 COc1ccccc1N1CCN(CCCCNc2nccc3ccccc23)CC1 10.1016/j.ejmech.2016.09.074
CHEMBL1223748 15875 0 None -51 4 Human 7.3 pKi = 7.3 Binding
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 390 8 1 5 4.3 COc1ccccc1N1CCN(CCCCNc2nccc3ccccc23)CC1 10.1016/j.ejmech.2016.09.074
54586764 61209 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]histamine from human histamine H4 receptorDisplacement of [3H]histamine from human histamine H4 receptor
ChEMBL 264 4 2 6 0.7 CN[C@@H]1CCN(c2cc(N(C)C(C)C)nc(N)n2)C1 10.1016/j.bmcl.2011.03.017
CHEMBL1770978 61209 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]histamine from human histamine H4 receptorDisplacement of [3H]histamine from human histamine H4 receptor
ChEMBL 264 4 2 6 0.7 CN[C@@H]1CCN(c2cc(N(C)C(C)C)nc(N)n2)C1 10.1016/j.bmcl.2011.03.017
44546966 116609 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 248 4 1 4 1.9 CC(C)CNc1cc(N2CCN(C)CC2)ccn1 10.1016/j.bmcl.2014.12.027
CHEMBL3393525 116609 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 248 4 1 4 1.9 CC(C)CNc1cc(N2CCN(C)CC2)ccn1 10.1016/j.bmcl.2014.12.027
9964223 203974 11 None -36 2 Human 5.3 pKi = 5.3 Binding
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 173 3 1 2 1.6 c1cncc(CCc2c[nH]cn2)c1 10.1021/jm049932u
CHEMBL82244 203974 11 None -36 2 Human 5.3 pKi = 5.3 Binding
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 173 3 1 2 1.6 c1cncc(CCc2c[nH]cn2)c1 10.1021/jm049932u
90645148 111683 0 None - 1 Human 5.3 pKi = 5.3 Binding
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 295 2 1 7 0.7 CN1CCN(c2nc(N)nc(-c3cccc(C#N)c3)n2)CC1 10.1016/j.ejmech.2014.06.032
CHEMBL3290575 111683 0 None - 1 Human 5.3 pKi = 5.3 Binding
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 295 2 1 7 0.7 CN1CCN(c2nc(N)nc(-c3cccc(C#N)c3)n2)CC1 10.1016/j.ejmech.2014.06.032
56950378 69525 0 None - 1 Human 7.3 pKi = 7.3 Binding
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 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 69525 0 None - 1 Human 7.3 pKi = 7.3 Binding
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 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
25071940 186771 0 None -5 2 Human 7.3 pKi = 7.3 Binding
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 281 1 2 5 1.2 Nc1nc2c(c(N3CCNCC3)n1)CCc1ccccc1-2 10.1021/jm800670r
CHEMBL493281 186771 0 None -5 2 Human 7.3 pKi = 7.3 Binding
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 281 1 2 5 1.2 Nc1nc2c(c(N3CCNCC3)n1)CCc1ccccc1-2 10.1021/jm800670r
90645145 111686 0 None 28 2 Human 6.3 pKi = 6.3 Binding
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 348 2 1 6 1.6 CN1CCN(c2nc(N)nc(-c3ccc(Br)cc3)n2)CC1 10.1016/j.ejmech.2017.09.035
CHEMBL3290578 111686 0 None 28 2 Human 6.3 pKi = 6.3 Binding
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 348 2 1 6 1.6 CN1CCN(c2nc(N)nc(-c3ccc(Br)cc3)n2)CC1 10.1016/j.ejmech.2017.09.035
66741667 109649 0 None - 1 Human 6.3 pKi = 6.3 Binding
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 289 2 2 6 0.9 Nc1nc(C2CCCC2)cc(N2C[C@@H]3NCCO[C@@H]3C2)n1 10.1021/jm401727m
CHEMBL3236566 109649 0 None - 1 Human 6.3 pKi = 6.3 Binding
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 289 2 2 6 0.9 Nc1nc(C2CCCC2)cc(N2C[C@@H]3NCCO[C@@H]3C2)n1 10.1021/jm401727m
122194623 123501 0 None - 1 Human 5.3 pKi = 5.3 Binding
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 296 3 1 6 1.4 CN1CCN(c2nc(N)nc(/C=C/c3ccccc3)n2)CC1 10.1016/j.ejmech.2015.08.014
CHEMBL3629826 123501 0 None - 1 Human 5.3 pKi = 5.3 Binding
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 296 3 1 6 1.4 CN1CCN(c2nc(N)nc(/C=C/c3ccccc3)n2)CC1 10.1016/j.ejmech.2015.08.014
90645145 111686 0 None 28 2 Human 6.3 pKi = 6.3 Binding
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 348 2 1 6 1.6 CN1CCN(c2nc(N)nc(-c3ccc(Br)cc3)n2)CC1 10.1016/j.ejmech.2014.06.032
CHEMBL3290578 111686 0 None 28 2 Human 6.3 pKi = 6.3 Binding
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 348 2 1 6 1.6 CN1CCN(c2nc(N)nc(-c3ccc(Br)cc3)n2)CC1 10.1016/j.ejmech.2014.06.032
10083861 15332 0 None - 1 Human 6.3 pKi = 6.3 Binding
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 258 1 1 3 1.3 Cc1ccc2[nH]c(C(=O)N3CCN(C)CC3)nc2c1 10.1021/jm0502081
CHEMBL121679 15332 0 None - 1 Human 6.3 pKi = 6.3 Binding
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 258 1 1 3 1.3 Cc1ccc2[nH]c(C(=O)N3CCN(C)CC3)nc2c1 10.1021/jm0502081
121238067 166558 0 None - 1 Human 6.3 pKi = 6.3 Binding
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 3 1 6 0.4 CC(C)Cc1nc(N)nc(N2CCN(C)CC2)n1 10.1016/j.bmc.2019.02.020
CHEMBL4290148 166558 0 None - 1 Human 6.3 pKi = 6.3 Binding
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 3 1 6 0.4 CC(C)Cc1nc(N)nc(N2CCN(C)CC2)n1 10.1016/j.bmc.2019.02.020
57394636 67704 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 284 1 0 5 2.6 CN1CCN(c2ncnc3c2sc2ccccc23)CC1 10.1016/j.bmcl.2011.08.014
CHEMBL1914534 67704 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 284 1 0 5 2.6 CN1CCN(c2ncnc3c2sc2ccccc23)CC1 10.1016/j.bmcl.2011.08.014
71525587 89297 0 None 177 2 Human 7.3 pKi = 7.3 Binding
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 255 2 2 7 -0.1 CNC1CN(c2nc(N)nc3cc(C#N)cnc23)C1 10.1016/j.bmcl.2013.02.091
CHEMBL2376802 89297 0 None 177 2 Human 7.3 pKi = 7.3 Binding
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 255 2 2 7 -0.1 CNC1CN(c2nc(N)nc3cc(C#N)cnc23)C1 10.1016/j.bmcl.2013.02.091
753256 178770 10 None 2 2 Human 6.3 pKi = 6.3 Binding
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 208 1 2 6 -0.6 CN1CCN(c2cc(N)nc(N)n2)CC1 10.1016/j.bmcl.2012.10.139
CHEMBL473662 178770 10 None 2 2 Human 6.3 pKi = 6.3 Binding
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 208 1 2 6 -0.6 CN1CCN(c2cc(N)nc(N)n2)CC1 10.1016/j.bmcl.2012.10.139
46228143 198400 0 None - 1 Human 6.3 pKi = 6.3 Binding
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 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 198400 0 None - 1 Human 6.3 pKi = 6.3 Binding
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 343 5 2 8 1.3 CN1CCN(c2cc(NCc3cccc([N+](=O)[O-])c3)nc(N)n2)CC1 10.1016/j.bmc.2009.08.059
24745335 292 7 None -6 5 Mouse 7.3 pKi = 7.3 Binding
Binding affinity to mouse histamine H4 receptorBinding affinity to mouse histamine H4 receptor
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 292 7 None -6 5 Mouse 7.3 pKi = 7.3 Binding
Binding affinity to mouse histamine H4 receptorBinding affinity to mouse histamine H4 receptor
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 292 7 None -6 5 Mouse 7.3 pKi = 7.3 Binding
Binding affinity to mouse histamine H4 receptorBinding affinity to mouse histamine H4 receptor
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 292 7 None -6 5 Mouse 7.3 pKi = 7.3 Binding
Binding affinity to mouse histamine H4 receptorBinding affinity to mouse histamine H4 receptor
ChEMBL 262 5 3 6 0.7 CN[C@@H]1CCN(C1)c1cc(NCC2CC2)nc(n1)N 10.1016/j.bmcl.2013.02.091
24745335 292 7 None -4 5 Rat 7.3 pKi = 7.3 Binding
Binding affinity to rat histamine H4 receptorBinding affinity to rat histamine H4 receptor
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 292 7 None -4 5 Rat 7.3 pKi = 7.3 Binding
Binding affinity to rat histamine H4 receptorBinding affinity to rat histamine H4 receptor
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 292 7 None -4 5 Rat 7.3 pKi = 7.3 Binding
Binding affinity to rat histamine H4 receptorBinding affinity to rat histamine H4 receptor
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 292 7 None -4 5 Rat 7.3 pKi = 7.3 Binding
Binding affinity to rat histamine H4 receptorBinding affinity to rat histamine H4 receptor
ChEMBL 262 5 3 6 0.7 CN[C@@H]1CCN(C1)c1cc(NCC2CC2)nc(n1)N 10.1016/j.bmcl.2013.02.091
51354583 58591 0 None 2 2 Human 7.3 pKi = 7.3 Binding
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 287 6 1 4 3.1 c1nc(CCCn2cc(CC3CCCCCC3)nn2)c[nH]1 10.1021/jm1013488
CHEMBL1688975 58591 0 None 2 2 Human 7.3 pKi = 7.3 Binding
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 287 6 1 4 3.1 c1nc(CCCn2cc(CC3CCCCCC3)nn2)c[nH]1 10.1021/jm1013488
71518860 86069 0 None - 1 Human 5.3 pKi = 5.3 Binding
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 308 2 2 5 2.0 CN1CCN(c2nc(N)nc3[nH]c(-c4ccccc4)cc23)CC1 10.1016/j.bmcl.2012.10.139
CHEMBL2314773 86069 0 None - 1 Human 5.3 pKi = 5.3 Binding
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 308 2 2 5 2.0 CN1CCN(c2nc(N)nc3[nH]c(-c4ccccc4)cc23)CC1 10.1016/j.bmcl.2012.10.139
46228113 200388 0 None - 1 Human 6.3 pKi = 6.3 Binding
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 328 5 2 7 1.4 COc1ccc(CNc2cc(N3CCN(C)CC3)nc(N)n2)cc1 10.1016/j.bmc.2009.08.059
CHEMBL608717 200388 0 None - 1 Human 6.3 pKi = 6.3 Binding
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 328 5 2 7 1.4 COc1ccc(CNc2cc(N3CCN(C)CC3)nc(N)n2)cc1 10.1016/j.bmc.2009.08.059
164611807 184401 0 None -162 4 Human 4.3 pKi = 4.3 Binding
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 376 6 4 4 2.5 Cc1nc(N)sc1CCCN/C(N)=N/C(=S)N[C@@H](C)c1ccccc1 10.1016/j.ejmech.2021.113190
CHEMBL4854278 184401 0 None -162 4 Human 4.3 pKi = 4.3 Binding
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 376 6 4 4 2.5 Cc1nc(N)sc1CCCN/C(N)=N/C(=S)N[C@@H](C)c1ccccc1 10.1016/j.ejmech.2021.113190
49841718 69392 0 None - 1 Human 7.3 pKi = 7.3 Binding
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 349 3 1 6 2.6 COc1ccc(-c2ccc3c(N4CCN(C)CC4)nc(N)nc3c2)cc1 10.1016/j.bmcl.2011.10.104
CHEMBL1935569 69392 0 None - 1 Human 7.3 pKi = 7.3 Binding
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 349 3 1 6 2.6 COc1ccc(-c2ccc3c(N4CCN(C)CC4)nc(N)nc3c2)cc1 10.1016/j.bmcl.2011.10.104
58227143 116625 1 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 249 5 1 5 1.4 CCCCNc1nccc(N2CCN(C)CC2)n1 10.1016/j.bmcl.2014.12.027
CHEMBL3393541 116625 1 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 249 5 1 5 1.4 CCCCNc1nccc(N2CCN(C)CC2)n1 10.1016/j.bmcl.2014.12.027
67087450 116634 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
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 116634 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 249 5 2 5 1.3 CN[C@@H]1CCN(c2cnnc(NCC(C)C)c2)C1 10.1016/j.bmcl.2014.12.027
46890071 6831 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 424 8 2 4 4.7 Cc1cc(OCCCNCC2CCCN(C)C2)ccc1-c1nc2c(C)c(F)ccc2[nH]1 10.1016/j.bmcl.2010.04.017
CHEMBL1084354 6831 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 424 8 2 4 4.7 Cc1cc(OCCCNCC2CCCN(C)C2)ccc1-c1nc2c(C)c(F)ccc2[nH]1 10.1016/j.bmcl.2010.04.017
66740470 109310 0 None - 1 Human 7.3 pKi = 7.3 Binding
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 289 2 2 6 0.9 Nc1nc(C2CCCC2)cc(N2C[C@H]3NCCO[C@@H]3C2)n1 10.1021/jm401727m
CHEMBL3233048 109310 0 None - 1 Human 7.3 pKi = 7.3 Binding
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 289 2 2 6 0.9 Nc1nc(C2CCCC2)cc(N2C[C@H]3NCCO[C@@H]3C2)n1 10.1021/jm401727m
2306318 86580 12 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 268 1 0 5 2.1 CN1CCN(c2ncnc3c2oc2ccccc23)CC1 10.1016/j.bmcl.2011.08.014
CHEMBL232421 86580 12 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 268 1 0 5 2.1 CN1CCN(c2ncnc3c2oc2ccccc23)CC1 10.1016/j.bmcl.2011.08.014
121238068 156668 0 None -281 2 Human 5.3 pKi = 5.3 Binding
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 3 1 6 2.0 CN1CCN(c2nc(N)nc(Cc3cccc4ccccc34)n2)CC1 10.1016/j.ejmech.2017.09.035
CHEMBL4076046 156668 0 None -281 2 Human 5.3 pKi = 5.3 Binding
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 3 1 6 2.0 CN1CCN(c2nc(N)nc(Cc3cccc4ccccc34)n2)CC1 10.1016/j.ejmech.2017.09.035
25178341 186227 0 None - 1 Human 6.3 pKi = 6.3 Binding
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 382 4 2 6 3.2 CN1CCN(c2nc(NCc3ccc(N)cc3)c3cc(Cl)ccc3n2)CC1 10.1021/jm800876b
CHEMBL489271 186227 0 None - 1 Human 6.3 pKi = 6.3 Binding
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 382 4 2 6 3.2 CN1CCN(c2nc(NCc3ccc(N)cc3)c3cc(Cl)ccc3n2)CC1 10.1021/jm800876b
25178341 186227 0 None - 1 Human 6.3 pKi = 6.3 Binding
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 382 4 2 6 3.2 CN1CCN(c2nc(NCc3ccc(N)cc3)c3cc(Cl)ccc3n2)CC1 10.1021/jm901379s
CHEMBL489271 186227 0 None - 1 Human 6.3 pKi = 6.3 Binding
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 382 4 2 6 3.2 CN1CCN(c2nc(NCc3ccc(N)cc3)c3cc(Cl)ccc3n2)CC1 10.1021/jm901379s
25178556 188496 0 None - 1 Human 6.3 pKi = 6.3 Binding
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 423 4 1 6 4.9 CN1CCN(c2nc(NCc3cc4ccccc4s3)c3cc(Cl)ccc3n2)CC1 10.1021/jm901379s
CHEMBL509961 188496 0 None - 1 Human 6.3 pKi = 6.3 Binding
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 423 4 1 6 4.9 CN1CCN(c2nc(NCc3cc4ccccc4s3)c3cc(Cl)ccc3n2)CC1 10.1021/jm901379s
23649429 95850 0 None - 1 Human 7.2 pKi = 7.2 Binding
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 326 2 0 5 2.7 COc1nc2cc(Cl)c(Cl)cc2nc1N1CCN(C)CC1 10.1021/jm7014217
CHEMBL261224 95850 0 None - 1 Human 7.2 pKi = 7.2 Binding
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 326 2 0 5 2.7 COc1nc2cc(Cl)c(Cl)cc2nc1N1CCN(C)CC1 10.1021/jm7014217
44478385 5699 2 None 9 4 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cells
ChEMBL 342 9 3 4 2.5 N#C/N=C(/NCCCCc1c[nH]cn1)NCCSc1ccccc1 10.1021/jm900526h
CHEMBL1078642 5699 2 None 9 4 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cells
ChEMBL 342 9 3 4 2.5 N#C/N=C(/NCCCCc1c[nH]cn1)NCCSc1ccccc1 10.1021/jm900526h
25178344 186303 0 None - 1 Human 6.2 pKi = 6.2 Binding
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 321 4 2 6 1.4 CN1CCN(c2nc(NCCO)c3cc(Cl)ccc3n2)CC1 10.1021/jm800876b
CHEMBL489664 186303 0 None - 1 Human 6.2 pKi = 6.2 Binding
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 321 4 2 6 1.4 CN1CCN(c2nc(NCCO)c3cc(Cl)ccc3n2)CC1 10.1021/jm800876b
24853597 95849 0 None - 1 Human 6.2 pKi = 6.2 Binding
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 334 3 0 5 3.5 Cc1cccc(Oc2nc3ccccc3nc2N2CCN(C)CC2)c1 10.1021/jm7014217
CHEMBL261223 95849 0 None - 1 Human 6.2 pKi = 6.2 Binding
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 334 3 0 5 3.5 Cc1cccc(Oc2nc3ccccc3nc2N2CCN(C)CC2)c1 10.1021/jm7014217
8070044 155411 10 None - 1 Human 5.2 pKi = 5.2 Binding
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 300 4 0 5 2.4 CC(C)COc1nc2ccccc2nc1N1CCN(C)CC1 10.1021/jm7014217
CHEMBL406123 155411 10 None - 1 Human 5.2 pKi = 5.2 Binding
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 300 4 0 5 2.4 CC(C)COc1nc2ccccc2nc1N1CCN(C)CC1 10.1021/jm7014217
16061844 61212 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]histamine from human histamine H4 receptorDisplacement of [3H]histamine from human histamine H4 receptor
ChEMBL 298 5 3 6 1.5 CN[C@@H]1CCN(c2cc(NCc3ccccc3)nc(N)n2)C1 10.1016/j.bmcl.2011.03.017
CHEMBL1770981 61212 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]histamine from human histamine H4 receptorDisplacement of [3H]histamine from human histamine H4 receptor
ChEMBL 298 5 3 6 1.5 CN[C@@H]1CCN(c2cc(NCc3ccccc3)nc(N)n2)C1 10.1016/j.bmcl.2011.03.017
57403351 67981 0 None -1 2 Human 7.2 pKi = 7.2 Binding
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 277 4 1 5 2.1 CN(C)[C@@H]1CCN(c2cc(NCC(C)(C)C)ncn2)C1 10.1016/j.bmcl.2011.07.114
CHEMBL1916499 67981 0 None -1 2 Human 7.2 pKi = 7.2 Binding
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 277 4 1 5 2.1 CN(C)[C@@H]1CCN(c2cc(NCC(C)(C)C)ncn2)C1 10.1016/j.bmcl.2011.07.114
156011443 177766 0 None -50 2 Human 6.2 pKi = 6.2 Binding
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 387 8 1 2 4.7 Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCCc1c[nH]cn1 10.1021/acs.jmedchem.0c00160
CHEMBL4636487 177766 0 None -50 2 Human 6.2 pKi = 6.2 Binding
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 387 8 1 2 4.7 Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCCc1c[nH]cn1 10.1021/acs.jmedchem.0c00160
CHEMBL4651225 177766 0 None -50 2 Human 6.2 pKi = 6.2 Binding
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 387 8 1 2 4.7 Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCCc1c[nH]cn1 10.1021/acs.jmedchem.0c00160
25178339 186201 0 None - 1 Human 6.2 pKi = 6.2 Binding
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 373 4 1 5 4.0 CN1CCN(c2nc(NCC3CCCCC3)c3cc(Cl)ccc3n2)CC1 10.1021/jm800876b
CHEMBL489061 186201 0 None - 1 Human 6.2 pKi = 6.2 Binding
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 373 4 1 5 4.0 CN1CCN(c2nc(NCC3CCCCC3)c3cc(Cl)ccc3n2)CC1 10.1021/jm800876b
51354585 58593 0 None -5 2 Human 6.2 pKi = 6.2 Binding
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 245 5 1 4 2.0 c1nc(CCn2cc(CC3CCCC3)nn2)c[nH]1 10.1021/jm1013488
CHEMBL1688977 58593 0 None -5 2 Human 6.2 pKi = 6.2 Binding
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 245 5 1 4 2.0 c1nc(CCn2cc(CC3CCCC3)nn2)c[nH]1 10.1021/jm1013488
51354876 59884 0 None - 1 Human 6.2 pKi = 6.2 Binding
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 259 5 1 4 2.4 c1nc(CCc2cn(CC3CCCCC3)nn2)c[nH]1 10.1021/jm1013488
CHEMBL1739924 59884 0 None - 1 Human 6.2 pKi = 6.2 Binding
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 259 5 1 4 2.4 c1nc(CCc2cn(CC3CCCCC3)nn2)c[nH]1 10.1021/jm1013488
CHEMBL3216267 59884 0 None - 1 Human 6.2 pKi = 6.2 Binding
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 259 5 1 4 2.4 c1nc(CCc2cn(CC3CCCCC3)nn2)c[nH]1 10.1021/jm1013488
12741697 95713 2 None - 1 Human 6.2 pKi = 6.2 Binding
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 261 1 0 3 2.6 CN1CCN(c2ccc3cc(Cl)ccc3n2)CC1 10.1021/jm7014217
CHEMBL260565 95713 2 None - 1 Human 6.2 pKi = 6.2 Binding
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 261 1 0 3 2.6 CN1CCN(c2ccc3cc(Cl)ccc3n2)CC1 10.1021/jm7014217
25178339 186201 0 None - 1 Human 6.2 pKi = 6.2 Binding
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 373 4 1 5 4.0 CN1CCN(c2nc(NCC3CCCCC3)c3cc(Cl)ccc3n2)CC1 10.1021/jm901379s
CHEMBL489061 186201 0 None - 1 Human 6.2 pKi = 6.2 Binding
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 373 4 1 5 4.0 CN1CCN(c2nc(NCC3CCCCC3)c3cc(Cl)ccc3n2)CC1 10.1021/jm901379s
919019 136209 7 None - 1 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]-histamine from human histamine H4 receptor expressed in HEK293T cells after 1 to 1.5 hrs by liquid scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor expressed in HEK293T cells after 1 to 1.5 hrs by liquid scintillation counting analysis
ChEMBL 297 2 1 5 1.9 COc1ccc2[nH]c3c(N4CCN(C)CC4)ncnc3c2c1 10.1039/C5MD00022J
CHEMBL3740837 136209 7 None - 1 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]-histamine from human histamine H4 receptor expressed in HEK293T cells after 1 to 1.5 hrs by liquid scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor expressed in HEK293T cells after 1 to 1.5 hrs by liquid scintillation counting analysis
ChEMBL 297 2 1 5 1.9 COc1ccc2[nH]c3c(N4CCN(C)CC4)ncnc3c2c1 10.1039/C5MD00022J
929854 197407 8 None - 1 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]-histamine from human histamine H4 receptor expressed in HEK293T cells after 1 to 1.5 hrs by liquid scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor expressed in HEK293T cells after 1 to 1.5 hrs by liquid scintillation counting analysis
ChEMBL 289 4 2 4 2.7 CN(C)CCNc1ncnc2c1[nH]c1ccc(Cl)cc12 10.1039/C5MD00022J
CHEMBL588176 197407 8 None - 1 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]-histamine from human histamine H4 receptor expressed in HEK293T cells after 1 to 1.5 hrs by liquid scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor expressed in HEK293T cells after 1 to 1.5 hrs by liquid scintillation counting analysis
ChEMBL 289 4 2 4 2.7 CN(C)CCNc1ncnc2c1[nH]c1ccc(Cl)cc12 10.1039/C5MD00022J
168278543 192249 0 None -4 4 Human 5.2 pKi = 5.2 Binding
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 192249 0 None -4 4 Human 5.2 pKi = 5.2 Binding
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 192249 0 None -4 4 Human 5.2 pKi = 5.2 Binding
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
168295803 192443 0 None -6 4 Human 5.2 pKi = 5.2 Binding
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 192443 0 None -6 4 Human 5.2 pKi = 5.2 Binding
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 192443 0 None -6 4 Human 5.2 pKi = 5.2 Binding
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
57402471 67534 0 None -549 3 Human 5.2 pKi = 5.2 Binding
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 469 8 1 5 4.0 COc1ccc(CN(CCN2CCN(C(=O)c3cc4ccccc4[nH]3)CC2)c2ccccn2)cc1 10.1016/j.bmcl.2011.09.001
CHEMBL1910378 67534 0 None -549 3 Human 5.2 pKi = 5.2 Binding
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 469 8 1 5 4.0 COc1ccc(CN(CCN2CCN(C(=O)c3cc4ccccc4[nH]3)CC2)c2ccccn2)cc1 10.1016/j.bmcl.2011.09.001
164614645 184549 0 None -57 4 Human 5.2 pKi = 5.2 Binding
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 402 8 4 4 3.0 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCC(c1ccccc1)C(C)C 10.1016/j.ejmech.2021.113190
CHEMBL4856572 184549 0 None -57 4 Human 5.2 pKi = 5.2 Binding
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 402 8 4 4 3.0 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCC(c1ccccc1)C(C)C 10.1016/j.ejmech.2021.113190
57394627 67979 0 None - 1 Human 6.2 pKi = 6.2 Binding
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 277 5 2 5 2.4 CN1CC[C@H](Nc2cc(NCCC(C)(C)C)ncn2)C1 10.1016/j.bmcl.2011.07.114
CHEMBL1916497 67979 0 None - 1 Human 6.2 pKi = 6.2 Binding
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 277 5 2 5 2.4 CN1CC[C@H](Nc2cc(NCCC(C)(C)C)ncn2)C1 10.1016/j.bmcl.2011.07.114
71519179 86059 0 None - 1 Human 5.2 pKi = 5.2 Binding
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 312 3 4 5 2.1 Nc1nc(N[C@H]2CCNC2)c2cc(-c3ccc(F)cc3)[nH]c2n1 10.1016/j.bmcl.2012.10.139
CHEMBL2314762 86059 0 None - 1 Human 5.2 pKi = 5.2 Binding
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 312 3 4 5 2.1 Nc1nc(N[C@H]2CCNC2)c2cc(-c3ccc(F)cc3)[nH]c2n1 10.1016/j.bmcl.2012.10.139
1204 1901 114 None 1 23 Guinea pig 8.2 pKi = 8.2 Binding
Binding affinity to guinea pig histamine H4 receptorBinding affinity to guinea pig histamine H4 receptor
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.5b00516
1247 1901 114 None 1 23 Guinea pig 8.2 pKi = 8.2 Binding
Binding affinity to guinea pig histamine H4 receptorBinding affinity to guinea pig histamine H4 receptor
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.5b00516
1375 1901 114 None 1 23 Guinea pig 8.2 pKi = 8.2 Binding
Binding affinity to guinea pig histamine H4 receptorBinding affinity to guinea pig histamine H4 receptor
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.5b00516
774 1901 114 None 1 23 Guinea pig 8.2 pKi = 8.2 Binding
Binding affinity to guinea pig histamine H4 receptorBinding affinity to guinea pig histamine H4 receptor
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.5b00516
CHEMBL90 1901 114 None 1 23 Guinea pig 8.2 pKi = 8.2 Binding
Binding affinity to guinea pig histamine H4 receptorBinding affinity to guinea pig histamine H4 receptor
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.5b00516
DB05381 1901 114 None 1 23 Guinea pig 8.2 pKi = 8.2 Binding
Binding affinity to guinea pig histamine H4 receptorBinding affinity to guinea pig histamine H4 receptor
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.5b00516
1278 2119 79 None -3 8 Human 8.2 pKi = 8.2 Binding
Binding affinity to human histamine H4 receptorBinding affinity to human histamine H4 receptor
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1016/j.bmcl.2011.10.104
1279 2119 79 None -3 8 Human 8.2 pKi = 8.2 Binding
Binding affinity to human histamine H4 receptorBinding affinity to human histamine H4 receptor
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1016/j.bmcl.2011.10.104
4908365 2119 79 None -3 8 Human 8.2 pKi = 8.2 Binding
Binding affinity to human histamine H4 receptorBinding affinity to human histamine H4 receptor
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1016/j.bmcl.2011.10.104
CHEMBL129198 2119 79 None -3 8 Human 8.2 pKi = 8.2 Binding
Binding affinity to human histamine H4 receptorBinding affinity to human histamine H4 receptor
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1016/j.bmcl.2011.10.104
1278 2119 79 None 3 8 Rat 8.2 pKi = 8.2 Binding
Binding affinity to rat histamine H4 receptorBinding affinity to rat histamine H4 receptor
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1016/j.bmcl.2011.10.104
1279 2119 79 None 3 8 Rat 8.2 pKi = 8.2 Binding
Binding affinity to rat histamine H4 receptorBinding affinity to rat histamine H4 receptor
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1016/j.bmcl.2011.10.104
4908365 2119 79 None 3 8 Rat 8.2 pKi = 8.2 Binding
Binding affinity to rat histamine H4 receptorBinding affinity to rat histamine H4 receptor
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1016/j.bmcl.2011.10.104
CHEMBL129198 2119 79 None 3 8 Rat 8.2 pKi = 8.2 Binding
Binding affinity to rat histamine H4 receptorBinding affinity to rat histamine H4 receptor
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1016/j.bmcl.2011.10.104
44538833 69376 21 None - 1 Human 8.2 pKi = 8.2 Binding
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 327 1 2 6 1.7 Nc1nc2c(c(N3CCNCC3)n1)CCC1=C2[C@H]2CCCC[C@H]2O1 10.1016/j.bmcl.2011.10.104
CHEMBL1935450 69376 21 None - 1 Human 8.2 pKi = 8.2 Binding
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 327 1 2 6 1.7 Nc1nc2c(c(N3CCNCC3)n1)CCC1=C2[C@H]2CCCC[C@H]2O1 10.1016/j.bmcl.2011.10.104
49841719 69394 0 None 38 3 Human 8.2 pKi = 8.2 Binding
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)nc3cc(-c4ccoc4)ccc23)CC1 10.1016/j.bmcl.2011.10.104
CHEMBL1935571 69394 0 None 38 3 Human 8.2 pKi = 8.2 Binding
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)nc3cc(-c4ccoc4)ccc23)CC1 10.1016/j.bmcl.2011.10.104
11846300 79856 3 None -2 4 Human 8.2 pKi = 8.2 Binding
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 327 0 0 4 3.8 CN1CCN(C2=Nc3ccc(Cl)cc3Oc3ccccc32)CC1 10.1016/j.bmcl.2011.10.104
CHEMBL213912 79856 3 None -2 4 Human 8.2 pKi = 8.2 Binding
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 327 0 0 4 3.8 CN1CCN(C2=Nc3ccc(Cl)cc3Oc3ccccc32)CC1 10.1016/j.bmcl.2011.10.104
11301441 95707 6 None - 1 Human 8.2 pKi = 8.2 Binding
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 312 1 1 4 2.0 CN1CCN(c2nc3cc(Cl)c(Cl)cc3[nH]c2=O)CC1 10.1016/j.bmcl.2011.10.104
CHEMBL260549 95707 6 None - 1 Human 8.2 pKi = 8.2 Binding
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 312 1 1 4 2.0 CN1CCN(c2nc3cc(Cl)c(Cl)cc3[nH]c2=O)CC1 10.1016/j.bmcl.2011.10.104
54582865 61190 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]histamine from human histamine H4 receptorDisplacement of [3H]histamine from human histamine H4 receptor
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 61190 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]histamine from human histamine H4 receptorDisplacement of [3H]histamine from human histamine H4 receptor
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 61221 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]histamine from human histamine H4 receptorDisplacement of [3H]histamine from human histamine H4 receptor
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 61221 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]histamine from human histamine H4 receptorDisplacement of [3H]histamine from human histamine H4 receptor
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
25130912 188153 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]histamine from human histamine H4 receptorDisplacement of [3H]histamine from human histamine H4 receptor
ChEMBL 262 2 1 6 0.4 CN1CCN(c2cc(N3CCCC3)nc(N)n2)CC1 10.1016/j.bmcl.2011.03.017
CHEMBL505061 188153 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]histamine from human histamine H4 receptorDisplacement of [3H]histamine from human histamine H4 receptor
ChEMBL 262 2 1 6 0.4 CN1CCN(c2cc(N3CCCC3)nc(N)n2)CC1 10.1016/j.bmcl.2011.03.017
54584825 61221 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 250 4 3 6 0.7 CN[C@@H]1CCN(c2cc(N)nc(NC(C)C)n2)C1 10.1016/j.bmcl.2014.10.013
CHEMBL1770990 61221 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 250 4 3 6 0.7 CN[C@@H]1CCN(c2cc(N)nc(NC(C)C)n2)C1 10.1016/j.bmcl.2014.10.013
58227157 115417 0 None - 1 Human 8.2 pKi = 8.2 Binding
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.2014.10.013
CHEMBL3354815 115417 0 None - 1 Human 8.2 pKi = 8.2 Binding
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.2014.10.013
58227200 116619 0 None - 1 Human 8.2 pKi = 8.2 Binding
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
CHEMBL3393535 116619 0 None - 1 Human 8.2 pKi = 8.2 Binding
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
58227337 116637 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 261 4 2 5 1.6 CN[C@@H]1CCN(c2cnnc(NC3CCCC3)c2)C1 10.1016/j.bmcl.2014.12.027
CHEMBL3393553 116637 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 261 4 2 5 1.6 CN[C@@H]1CCN(c2cnnc(NC3CCCC3)c2)C1 10.1016/j.bmcl.2014.12.027
24745335 292 7 None 4 5 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-histamine from human H4R expressed in HEK293T cellsDisplacement of [3H]-histamine from human 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 292 7 None 4 5 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-histamine from human H4R expressed in HEK293T cellsDisplacement of [3H]-histamine from human 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 292 7 None 4 5 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-histamine from human H4R expressed in HEK293T cellsDisplacement of [3H]-histamine from human 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 292 7 None 4 5 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-histamine from human H4R expressed in HEK293T cellsDisplacement of [3H]-histamine from human 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 292 7 None 4 5 Human 8.2 pKi = 8.2 Binding
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 262 5 3 6 0.7 CN[C@@H]1CCN(C1)c1cc(NCC2CC2)nc(n1)N 10.1021/acs.jmedchem.5b00516
8985 292 7 None 4 5 Human 8.2 pKi = 8.2 Binding
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 262 5 3 6 0.7 CN[C@@H]1CCN(C1)c1cc(NCC2CC2)nc(n1)N 10.1021/acs.jmedchem.5b00516
CHEMBL1915540 292 7 None 4 5 Human 8.2 pKi = 8.2 Binding
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 262 5 3 6 0.7 CN[C@@H]1CCN(C1)c1cc(NCC2CC2)nc(n1)N 10.1021/acs.jmedchem.5b00516
DB15027 292 7 None 4 5 Human 8.2 pKi = 8.2 Binding
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 262 5 3 6 0.7 CN[C@@H]1CCN(C1)c1cc(NCC2CC2)nc(n1)N 10.1021/acs.jmedchem.5b00516
11957573 1979 29 None -40 6 Human 8.2 pKi = 8.2 Binding
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 170 3 3 3 0.6 NC(=N)SCCc1cnc[nH]1 10.1016/j.bmcl.2010.10.041
1250 1979 29 None -40 6 Human 8.2 pKi = 8.2 Binding
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 170 3 3 3 0.6 NC(=N)SCCc1cnc[nH]1 10.1016/j.bmcl.2010.10.041
3692 1979 29 None -40 6 Human 8.2 pKi = 8.2 Binding
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 170 3 3 3 0.6 NC(=N)SCCc1cnc[nH]1 10.1016/j.bmcl.2010.10.041
CHEMBL19439 1979 29 None -40 6 Human 8.2 pKi = 8.2 Binding
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 170 3 3 3 0.6 NC(=N)SCCc1cnc[nH]1 10.1016/j.bmcl.2010.10.041
44595856 89227 0 None - 1 Human 8.2 pKi = 8.2 Binding
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 356 6 4 8 2.3 Nc1nccc(NCCNc2cc(-c3cccc(Cl)c3)nc(N)n2)n1 10.1021/jm301886t
CHEMBL2375757 89227 0 None - 1 Human 8.2 pKi = 8.2 Binding
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 356 6 4 8 2.3 Nc1nccc(NCCNc2cc(-c3cccc(Cl)c3)nc(N)n2)n1 10.1021/jm301886t
1278 2119 79 None -3 8 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]histamine displacement from human recombinant histamine H4 receptor expressed in SK-NM-C cells after 45 minsDisplacement of [3H]histamine displacement from human recombinant histamine H4 receptor expressed in SK-NM-C cells after 45 mins
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/jm301886t
1279 2119 79 None -3 8 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]histamine displacement from human recombinant histamine H4 receptor expressed in SK-NM-C cells after 45 minsDisplacement of [3H]histamine displacement from human recombinant histamine H4 receptor expressed in SK-NM-C cells after 45 mins
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/jm301886t
4908365 2119 79 None -3 8 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]histamine displacement from human recombinant histamine H4 receptor expressed in SK-NM-C cells after 45 minsDisplacement of [3H]histamine displacement from human recombinant histamine H4 receptor expressed in SK-NM-C cells after 45 mins
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/jm301886t
CHEMBL129198 2119 79 None -3 8 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]histamine displacement from human recombinant histamine H4 receptor expressed in SK-NM-C cells after 45 minsDisplacement of [3H]histamine displacement from human recombinant histamine H4 receptor expressed in SK-NM-C cells after 45 mins
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/jm301886t
11957573 1979 29 None -40 6 Human 8.2 pKi = 8.2 Binding
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 170 3 3 3 0.6 NC(=N)SCCc1cnc[nH]1 10.1021/jm201042n
1250 1979 29 None -40 6 Human 8.2 pKi = 8.2 Binding
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 170 3 3 3 0.6 NC(=N)SCCc1cnc[nH]1 10.1021/jm201042n
3692 1979 29 None -40 6 Human 8.2 pKi = 8.2 Binding
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 170 3 3 3 0.6 NC(=N)SCCc1cnc[nH]1 10.1021/jm201042n
CHEMBL19439 1979 29 None -40 6 Human 8.2 pKi = 8.2 Binding
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 170 3 3 3 0.6 NC(=N)SCCc1cnc[nH]1 10.1021/jm201042n
25129523 186704 40 None 1 2 Human 8.2 pKi = 8.2 Binding
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 269 2 1 5 1.5 CN1CCN(c2cc(-c3ccccc3)nc(N)n2)CC1 10.1016/j.bmcl.2011.06.123
CHEMBL492884 186704 40 None 1 2 Human 8.2 pKi = 8.2 Binding
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 269 2 1 5 1.5 CN1CCN(c2cc(-c3ccccc3)nc(N)n2)CC1 10.1016/j.bmcl.2011.06.123
1278 2119 79 None -3 8 Human 8.2 pKi = 8.2 Binding
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 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1016/j.ejmech.2012.06.016
1279 2119 79 None -3 8 Human 8.2 pKi = 8.2 Binding
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 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1016/j.ejmech.2012.06.016
4908365 2119 79 None -3 8 Human 8.2 pKi = 8.2 Binding
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 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1016/j.ejmech.2012.06.016
CHEMBL129198 2119 79 None -3 8 Human 8.2 pKi = 8.2 Binding
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 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1016/j.ejmech.2012.06.016
11066922 19225 1 None - 1 Human 8.2 pKi = 8.2 Binding
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 2.9 CN1CCN(C(=O)c2cc3c(Cl)c(Cl)ccc3[nH]2)CC1 10.1016/j.ejmech.2012.06.016
CHEMBL129436 19225 1 None - 1 Human 8.2 pKi = 8.2 Binding
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 2.9 CN1CCN(C(=O)c2cc3c(Cl)c(Cl)ccc3[nH]2)CC1 10.1016/j.ejmech.2012.06.016
66573458 75312 0 None - 1 Human 8.2 pKi = 8.2 Binding
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 295 1 1 2 2.3 CN1CCN(C(=O)c2cc3c(F)c(Cl)ccc3[nH]2)CC1 10.1016/j.ejmech.2012.06.016
CHEMBL2047447 75312 0 None - 1 Human 8.2 pKi = 8.2 Binding
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 295 1 1 2 2.3 CN1CCN(C(=O)c2cc3c(F)c(Cl)ccc3[nH]2)CC1 10.1016/j.ejmech.2012.06.016
66573459 75313 0 None - 1 Human 8.2 pKi = 8.2 Binding
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 295 1 1 2 2.3 CN1CCN(C(=O)c2cc3cc(Cl)cc(F)c3[nH]2)CC1 10.1016/j.ejmech.2012.06.016
CHEMBL2047448 75313 0 None - 1 Human 8.2 pKi = 8.2 Binding
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 295 1 1 2 2.3 CN1CCN(C(=O)c2cc3cc(Cl)cc(F)c3[nH]2)CC1 10.1016/j.ejmech.2012.06.016
9860842 75314 0 None - 1 Human 8.2 pKi = 8.2 Binding
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 291 1 1 2 2.5 Cc1cc(Cl)cc2cc(C(=O)N3CCN(C)CC3)[nH]c12 10.1016/j.ejmech.2012.06.016
CHEMBL2047449 75314 0 None - 1 Human 8.2 pKi = 8.2 Binding
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 291 1 1 2 2.5 Cc1cc(Cl)cc2cc(C(=O)N3CCN(C)CC3)[nH]c12 10.1016/j.ejmech.2012.06.016
11957573 1979 29 None -40 6 Human 8.2 pKi = 8.2 Binding
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 170 3 3 3 0.6 NC(=N)SCCc1cnc[nH]1 10.1016/j.bmc.2009.04.007
1250 1979 29 None -40 6 Human 8.2 pKi = 8.2 Binding
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 170 3 3 3 0.6 NC(=N)SCCc1cnc[nH]1 10.1016/j.bmc.2009.04.007
3692 1979 29 None -40 6 Human 8.2 pKi = 8.2 Binding
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 170 3 3 3 0.6 NC(=N)SCCc1cnc[nH]1 10.1016/j.bmc.2009.04.007
CHEMBL19439 1979 29 None -40 6 Human 8.2 pKi = 8.2 Binding
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 170 3 3 3 0.6 NC(=N)SCCc1cnc[nH]1 10.1016/j.bmc.2009.04.007
71525681 89298 0 None 2 6 Human 8.2 pKi = 8.2 Binding
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 298 3 2 6 1.7 CNC1CN(c2nc(N)nc3cc(C4CCCC4)cnc23)C1 10.1016/j.bmcl.2013.02.091
CHEMBL2376803 89298 0 None 2 6 Human 8.2 pKi = 8.2 Binding
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 298 3 2 6 1.7 CNC1CN(c2nc(N)nc3cc(C4CCCC4)cnc23)C1 10.1016/j.bmcl.2013.02.091
136042270 69572 0 None 426 2 Human 8.2 pKi = 8.2 Binding
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 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 69572 0 None 426 2 Human 8.2 pKi = 8.2 Binding
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 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
1204 1901 114 None -3 23 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmcl.2010.04.017
1247 1901 114 None -3 23 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmcl.2010.04.017
1375 1901 114 None -3 23 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmcl.2010.04.017
774 1901 114 None -3 23 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmcl.2010.04.017
CHEMBL90 1901 114 None -3 23 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmcl.2010.04.017
DB05381 1901 114 None -3 23 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmcl.2010.04.017
25178552 172839 0 None - 1 Human 7.2 pKi = 7.2 Binding
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 387 5 1 6 3.8 CN1CCN(c2nc(NCCc3cccs3)c3cc(Cl)ccc3n2)CC1 10.1021/jm800876b
CHEMBL452848 172839 0 None - 1 Human 7.2 pKi = 7.2 Binding
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 387 5 1 6 3.8 CN1CCN(c2nc(NCCc3cccs3)c3cc(Cl)ccc3n2)CC1 10.1021/jm800876b
25178552 172839 0 None - 1 Human 7.2 pKi = 7.2 Binding
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 387 5 1 6 3.8 CN1CCN(c2nc(NCCc3cccs3)c3cc(Cl)ccc3n2)CC1 10.1021/jm901379s
CHEMBL452848 172839 0 None - 1 Human 7.2 pKi = 7.2 Binding
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 387 5 1 6 3.8 CN1CCN(c2nc(NCCc3cccs3)c3cc(Cl)ccc3n2)CC1 10.1021/jm901379s
90645158 111693 0 None - 1 Human 5.2 pKi = 5.2 Binding
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 334 3 1 7 1.5 COc1ccc(Cl)cc1-c1nc(N)nc(N2CCN(C)CC2)n1 10.1016/j.ejmech.2014.06.032
CHEMBL3290585 111693 0 None - 1 Human 5.2 pKi = 5.2 Binding
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 334 3 1 7 1.5 COc1ccc(Cl)cc1-c1nc(N)nc(N2CCN(C)CC2)n1 10.1016/j.ejmech.2014.06.032
57399828 67985 0 None - 1 Human 6.2 pKi = 6.2 Binding
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 345 5 1 5 3.8 CC(C)(C)CCNc1cc(N2CCN(C3CCCCC3)CC2)ncn1 10.1016/j.bmcl.2011.07.114
CHEMBL1916502 67985 0 None - 1 Human 6.2 pKi = 6.2 Binding
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 345 5 1 5 3.8 CC(C)(C)CCNc1cc(N2CCN(C3CCCCC3)CC2)ncn1 10.1016/j.bmcl.2011.07.114
805994 173783 7 None - 1 Human 6.2 pKi = 6.2 Binding
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 323 4 1 6 2.6 CN1CCN(c2nc(NCc3ccco3)c3ccccc3n2)CC1 10.1021/jm800876b
CHEMBL455133 173783 7 None - 1 Human 6.2 pKi = 6.2 Binding
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 323 4 1 6 2.6 CN1CCN(c2nc(NCc3ccco3)c3ccccc3n2)CC1 10.1021/jm800876b
805994 173783 7 None - 1 Human 6.2 pKi = 6.2 Binding
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 323 4 1 6 2.6 CN1CCN(c2nc(NCc3ccco3)c3ccccc3n2)CC1 10.1021/jm901379s
CHEMBL455133 173783 7 None - 1 Human 6.2 pKi = 6.2 Binding
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 323 4 1 6 2.6 CN1CCN(c2nc(NCc3ccco3)c3ccccc3n2)CC1 10.1021/jm901379s
168286141 192322 0 None -5 4 Human 5.2 pKi = 5.2 Binding
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 192322 0 None -5 4 Human 5.2 pKi = 5.2 Binding
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 192322 0 None -5 4 Human 5.2 pKi = 5.2 Binding
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
46890167 7178 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 454 7 1 4 5.6 CN1CCC(N(C)CCCOc2ccc(-c3nc4cc(C(C)(C)C)ccc4[nH]3)cc2Cl)C1 10.1016/j.bmcl.2010.04.017
CHEMBL1085872 7178 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 454 7 1 4 5.6 CN1CCC(N(C)CCCOc2ccc(-c3nc4cc(C(C)(C)C)ccc4[nH]3)cc2Cl)C1 10.1016/j.bmcl.2010.04.017
9966927 18687 4 None - 1 Human 7.2 pKi = 7.2 Binding
Antagonist activity at Homo sapiens (human) histamine H4 receptorAntagonist activity at Homo sapiens (human) histamine H4 receptor
ChEMBL 321 1 1 2 2.3 CN1CCN(C(=O)c2cc3cccc(Br)c3[nH]2)CC1 10.1007/s00044-004-0106-7
CHEMBL128252 18687 4 None - 1 Human 7.2 pKi = 7.2 Binding
Antagonist activity at Homo sapiens (human) histamine H4 receptorAntagonist activity at Homo sapiens (human) histamine H4 receptor
ChEMBL 321 1 1 2 2.3 CN1CCN(C(=O)c2cc3cccc(Br)c3[nH]2)CC1 10.1007/s00044-004-0106-7
9966927 18687 4 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]- histamine from the recombinant human histamine H4 receptorDisplacement of [3H]- histamine from the recombinant human histamine H4 receptor
ChEMBL 321 1 1 2 2.3 CN1CCN(C(=O)c2cc3cccc(Br)c3[nH]2)CC1 10.1021/jm0341047
CHEMBL128252 18687 4 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]- histamine from the recombinant human histamine H4 receptorDisplacement of [3H]- histamine from the recombinant human histamine H4 receptor
ChEMBL 321 1 1 2 2.3 CN1CCN(C(=O)c2cc3cccc(Br)c3[nH]2)CC1 10.1021/jm0341047
9966927 18687 4 None - 1 Human 7.2 pKi = 7.2 Binding
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 321 1 1 2 2.3 CN1CCN(C(=O)c2cc3cccc(Br)c3[nH]2)CC1 10.1021/jm0502081
CHEMBL128252 18687 4 None - 1 Human 7.2 pKi = 7.2 Binding
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 321 1 1 2 2.3 CN1CCN(C(=O)c2cc3cccc(Br)c3[nH]2)CC1 10.1021/jm0502081
12686479 161246 2 None - 1 Human 7.2 pKi = 7.2 Binding
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 244 1 1 5 1.1 CN1CCN(c2nc3ccccc3nc2O)CC1 10.1021/jm7014217
CHEMBL414183 161246 2 None - 1 Human 7.2 pKi = 7.2 Binding
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 244 1 1 5 1.1 CN1CCN(c2nc3ccccc3nc2O)CC1 10.1021/jm7014217
1265 929 54 None -2290 8 Human 6.2 pKi = 6.2 Binding
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 270 7 1 3 3.0 O=C(c1ccc(cc1)OCCCc1[nH]cnc1)C1CC1 10.1016/j.bmc.2011.03.046
6422124 929 54 None -2290 8 Human 6.2 pKi = 6.2 Binding
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 270 7 1 3 3.0 O=C(c1ccc(cc1)OCCCc1[nH]cnc1)C1CC1 10.1016/j.bmc.2011.03.046
CHEMBL14638 929 54 None -2290 8 Human 6.2 pKi = 6.2 Binding
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 270 7 1 3 3.0 O=C(c1ccc(cc1)OCCCc1[nH]cnc1)C1CC1 10.1016/j.bmc.2011.03.046
1265 929 54 None -2290 8 Human 6.2 pKi = 6.2 Binding
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 270 7 1 3 3.0 O=C(c1ccc(cc1)OCCCc1[nH]cnc1)C1CC1 10.1016/j.bmcl.2009.10.005
6422124 929 54 None -2290 8 Human 6.2 pKi = 6.2 Binding
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 270 7 1 3 3.0 O=C(c1ccc(cc1)OCCCc1[nH]cnc1)C1CC1 10.1016/j.bmcl.2009.10.005
CHEMBL14638 929 54 None -2290 8 Human 6.2 pKi = 6.2 Binding
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 270 7 1 3 3.0 O=C(c1ccc(cc1)OCCCc1[nH]cnc1)C1CC1 10.1016/j.bmcl.2009.10.005
57390262 67843 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 290 1 2 7 1.2 Nc1nc(N2CC(N)C2)c2oc3ncc(Cl)cc3c2n1 10.1016/j.bmcl.2011.08.014
CHEMBL1915050 67843 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 290 1 2 7 1.2 Nc1nc(N2CC(N)C2)c2oc3ncc(Cl)cc3c2n1 10.1016/j.bmcl.2011.08.014
155552102 175989 0 None 9 2 Human 6.2 pKi = 6.2 Binding
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 291 3 3 5 1.0 CC(C)(C)CNc1nccc(N2CCN(C(=N)N)CC2)n1 10.1021/acs.jmedchem.9b01342
CHEMBL4576393 175989 0 None 9 2 Human 6.2 pKi = 6.2 Binding
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 291 3 3 5 1.0 CC(C)(C)CNc1nccc(N2CCN(C(=N)N)CC2)n1 10.1021/acs.jmedchem.9b01342
CHEMBL4597352 175989 0 None 9 2 Human 6.2 pKi = 6.2 Binding
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 291 3 3 5 1.0 CC(C)(C)CNc1nccc(N2CCN(C(=N)N)CC2)n1 10.1021/acs.jmedchem.9b01342
25178936 186200 0 None - 1 Human 6.2 pKi = 6.2 Binding
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 305 2 0 5 2.1 CN1CCN(c2nc(N(C)C)c3cc(Cl)ccc3n2)CC1 10.1021/jm800876b
CHEMBL489060 186200 0 None - 1 Human 6.2 pKi = 6.2 Binding
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 305 2 0 5 2.1 CN1CCN(c2nc(N(C)C)c3cc(Cl)ccc3n2)CC1 10.1021/jm800876b
25178936 186200 0 None - 1 Human 6.2 pKi = 6.2 Binding
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 305 2 0 5 2.1 CN1CCN(c2nc(N(C)C)c3cc(Cl)ccc3n2)CC1 10.1021/jm901379s
CHEMBL489060 186200 0 None - 1 Human 6.2 pKi = 6.2 Binding
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 305 2 0 5 2.1 CN1CCN(c2nc(N(C)C)c3cc(Cl)ccc3n2)CC1 10.1021/jm901379s
137646103 157364 0 None - 1 Human 7.2 pKi = 7.2 Binding
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 393 8 3 3 3.7 O=C(O)C(Cc1cccc2ccccc12)NC(=O)[C@@H](CS)Cc1ccccc1 10.1016/j.ejmech.2016.09.074
CHEMBL4084275 157364 0 None - 1 Human 7.2 pKi = 7.2 Binding
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 393 8 3 3 3.7 O=C(O)C(Cc1cccc2ccccc12)NC(=O)[C@@H](CS)Cc1ccccc1 10.1016/j.ejmech.2016.09.074
42624149 109651 1 None -3 3 Mouse 7.2 pKi = 7.2 Binding
Displacement of [3H]histamine from mouse histamine H4 receptor expressed in SK-N-MC cells after 45 mins by competition binding analysisDisplacement of [3H]histamine from mouse histamine H4 receptor expressed in SK-N-MC cells after 45 mins by competition binding analysis
ChEMBL 221 3 2 5 0.4 CCc1cc(N2CC[C@@H](NC)C2)nc(N)n1 10.1021/jm401727m
CHEMBL3236568 109651 1 None -3 3 Mouse 7.2 pKi = 7.2 Binding
Displacement of [3H]histamine from mouse histamine H4 receptor expressed in SK-N-MC cells after 45 mins by competition binding analysisDisplacement of [3H]histamine from mouse histamine H4 receptor expressed in SK-N-MC cells after 45 mins by competition binding analysis
ChEMBL 221 3 2 5 0.4 CCc1cc(N2CC[C@@H](NC)C2)nc(N)n1 10.1021/jm401727m
58227127 116627 1 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 261 3 1 5 1.6 CN1CCN(c2ccnc(NC3CCCC3)n2)CC1 10.1016/j.bmcl.2014.12.027
CHEMBL3393543 116627 1 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 261 3 1 5 1.6 CN1CCN(c2ccnc(NC3CCCC3)n2)CC1 10.1016/j.bmcl.2014.12.027
1204 1901 114 None -12 23 Rat 7.2 pKi = 7.2 Binding
Binding affinity to rat histamine H4 receptor expressed in human SK-N-MC cells by radioligand displacement assayBinding affinity to rat 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 1901 114 None -12 23 Rat 7.2 pKi = 7.2 Binding
Binding affinity to rat histamine H4 receptor expressed in human SK-N-MC cells by radioligand displacement assayBinding affinity to rat 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 1901 114 None -12 23 Rat 7.2 pKi = 7.2 Binding
Binding affinity to rat histamine H4 receptor expressed in human SK-N-MC cells by radioligand displacement assayBinding affinity to rat 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 1901 114 None -12 23 Rat 7.2 pKi = 7.2 Binding
Binding affinity to rat histamine H4 receptor expressed in human SK-N-MC cells by radioligand displacement assayBinding affinity to rat 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 1901 114 None -12 23 Rat 7.2 pKi = 7.2 Binding
Binding affinity to rat histamine H4 receptor expressed in human SK-N-MC cells by radioligand displacement assayBinding affinity to rat 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 1901 114 None -12 23 Rat 7.2 pKi = 7.2 Binding
Binding affinity to rat histamine H4 receptor expressed in human SK-N-MC cells by radioligand displacement assayBinding affinity to rat 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
44395308 66494 0 None 39 2 Human 7.2 pKi = 7.2 Binding
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 369 1 1 2 2.2 CN1CCN(C(=O)c2cc3cc(I)ccc3[nH]2)CC1 10.1016/j.bmcl.2004.08.035
CHEMBL186108 66494 0 None 39 2 Human 7.2 pKi = 7.2 Binding
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 369 1 1 2 2.2 CN1CCN(C(=O)c2cc3cc(I)ccc3[nH]2)CC1 10.1016/j.bmcl.2004.08.035
155552061 175904 0 None 38 2 Human 7.2 pKi = 7.2 Binding
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 3 1 5 2.1 CN1CCCN(c2ccnc(NCC(C)(C)C)n2)CC1 10.1021/acs.jmedchem.9b01342
CHEMBL4543119 175904 0 None 38 2 Human 7.2 pKi = 7.2 Binding
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 3 1 5 2.1 CN1CCCN(c2ccnc(NCC(C)(C)C)n2)CC1 10.1021/acs.jmedchem.9b01342
CHEMBL4596606 175904 0 None 38 2 Human 7.2 pKi = 7.2 Binding
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 3 1 5 2.1 CN1CCCN(c2ccnc(NCC(C)(C)C)n2)CC1 10.1021/acs.jmedchem.9b01342
1204 1901 114 None -3 23 Human 7.2 pKi = 7.2 Binding
Displacement of UR-DEBa176 from human recombinant H4R expressed in HEK293T-SF-His6-CRE-Luc cellsDisplacement of UR-DEBa176 from human recombinant H4R expressed in HEK293T-SF-His6-CRE-Luc cells
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.0c00160
1247 1901 114 None -3 23 Human 7.2 pKi = 7.2 Binding
Displacement of UR-DEBa176 from human recombinant H4R expressed in HEK293T-SF-His6-CRE-Luc cellsDisplacement of UR-DEBa176 from human recombinant H4R expressed in HEK293T-SF-His6-CRE-Luc cells
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.0c00160
1375 1901 114 None -3 23 Human 7.2 pKi = 7.2 Binding
Displacement of UR-DEBa176 from human recombinant H4R expressed in HEK293T-SF-His6-CRE-Luc cellsDisplacement of UR-DEBa176 from human recombinant H4R expressed in HEK293T-SF-His6-CRE-Luc cells
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.0c00160
774 1901 114 None -3 23 Human 7.2 pKi = 7.2 Binding
Displacement of UR-DEBa176 from human recombinant H4R expressed in HEK293T-SF-His6-CRE-Luc cellsDisplacement of UR-DEBa176 from human recombinant H4R expressed in HEK293T-SF-His6-CRE-Luc cells
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.0c00160
CHEMBL90 1901 114 None -3 23 Human 7.2 pKi = 7.2 Binding
Displacement of UR-DEBa176 from human recombinant H4R expressed in HEK293T-SF-His6-CRE-Luc cellsDisplacement of UR-DEBa176 from human recombinant H4R expressed in HEK293T-SF-His6-CRE-Luc cells
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.0c00160
DB05381 1901 114 None -3 23 Human 7.2 pKi = 7.2 Binding
Displacement of UR-DEBa176 from human recombinant H4R expressed in HEK293T-SF-His6-CRE-Luc cellsDisplacement of UR-DEBa176 from human recombinant H4R expressed in HEK293T-SF-His6-CRE-Luc cells
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.0c00160
1278 2119 79 None -3 8 Human 7.2 pKi = 7.2 Binding
Displacement of UR-DEBa176 from human recombinant H4R expressed in HEK293T-SF-His6-CRE-Luc cellsDisplacement of UR-DEBa176 from human recombinant H4R expressed in HEK293T-SF-His6-CRE-Luc cells
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/acs.jmedchem.0c00160
1279 2119 79 None -3 8 Human 7.2 pKi = 7.2 Binding
Displacement of UR-DEBa176 from human recombinant H4R expressed in HEK293T-SF-His6-CRE-Luc cellsDisplacement of UR-DEBa176 from human recombinant H4R expressed in HEK293T-SF-His6-CRE-Luc cells
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/acs.jmedchem.0c00160
4908365 2119 79 None -3 8 Human 7.2 pKi = 7.2 Binding
Displacement of UR-DEBa176 from human recombinant H4R expressed in HEK293T-SF-His6-CRE-Luc cellsDisplacement of UR-DEBa176 from human recombinant H4R expressed in HEK293T-SF-His6-CRE-Luc cells
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/acs.jmedchem.0c00160
CHEMBL129198 2119 79 None -3 8 Human 7.2 pKi = 7.2 Binding
Displacement of UR-DEBa176 from human recombinant H4R expressed in HEK293T-SF-His6-CRE-Luc cellsDisplacement of UR-DEBa176 from human recombinant H4R expressed in HEK293T-SF-His6-CRE-Luc cells
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/acs.jmedchem.0c00160
1204 1901 114 None -3 23 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-UR-PI294 from Galphai2/Gbeta1gamma2-coupled human recombinant H4R expressed in baculovirus infected Sf9 insect cell membranes co-expressing RGS19 measured after 60 mins by microbeta scintillation counting methodDisplacement of [3H]-UR-PI294 from Galphai2/Gbeta1gamma2-coupled human recombinant H4R expressed in baculovirus infected Sf9 insect cell membranes co-expressing RGS19 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 1901 114 None -3 23 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-UR-PI294 from Galphai2/Gbeta1gamma2-coupled human recombinant H4R expressed in baculovirus infected Sf9 insect cell membranes co-expressing RGS19 measured after 60 mins by microbeta scintillation counting methodDisplacement of [3H]-UR-PI294 from Galphai2/Gbeta1gamma2-coupled human recombinant H4R expressed in baculovirus infected Sf9 insect cell membranes co-expressing RGS19 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 1901 114 None -3 23 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-UR-PI294 from Galphai2/Gbeta1gamma2-coupled human recombinant H4R expressed in baculovirus infected Sf9 insect cell membranes co-expressing RGS19 measured after 60 mins by microbeta scintillation counting methodDisplacement of [3H]-UR-PI294 from Galphai2/Gbeta1gamma2-coupled human recombinant H4R expressed in baculovirus infected Sf9 insect cell membranes co-expressing RGS19 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 1901 114 None -3 23 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-UR-PI294 from Galphai2/Gbeta1gamma2-coupled human recombinant H4R expressed in baculovirus infected Sf9 insect cell membranes co-expressing RGS19 measured after 60 mins by microbeta scintillation counting methodDisplacement of [3H]-UR-PI294 from Galphai2/Gbeta1gamma2-coupled human recombinant H4R expressed in baculovirus infected Sf9 insect cell membranes co-expressing RGS19 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 1901 114 None -3 23 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-UR-PI294 from Galphai2/Gbeta1gamma2-coupled human recombinant H4R expressed in baculovirus infected Sf9 insect cell membranes co-expressing RGS19 measured after 60 mins by microbeta scintillation counting methodDisplacement of [3H]-UR-PI294 from Galphai2/Gbeta1gamma2-coupled human recombinant H4R expressed in baculovirus infected Sf9 insect cell membranes co-expressing RGS19 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 1901 114 None -3 23 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-UR-PI294 from Galphai2/Gbeta1gamma2-coupled human recombinant H4R expressed in baculovirus infected Sf9 insect cell membranes co-expressing RGS19 measured after 60 mins by microbeta scintillation counting methodDisplacement of [3H]-UR-PI294 from Galphai2/Gbeta1gamma2-coupled human recombinant H4R expressed in baculovirus infected Sf9 insect cell membranes co-expressing RGS19 measured after 60 mins by microbeta scintillation counting method
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.0c00160
1278 2119 79 None -3 8 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-UR-PI294 from Galphai2/Gbeta1gamma2-coupled human recombinant H4R expressed in baculovirus infected Sf9 insect cell membranes co-expressing RGS19 measured after 60 mins by microbeta scintillation counting methodDisplacement of [3H]-UR-PI294 from Galphai2/Gbeta1gamma2-coupled human recombinant H4R expressed in baculovirus infected Sf9 insect cell membranes co-expressing RGS19 measured after 60 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.0c00160
1279 2119 79 None -3 8 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-UR-PI294 from Galphai2/Gbeta1gamma2-coupled human recombinant H4R expressed in baculovirus infected Sf9 insect cell membranes co-expressing RGS19 measured after 60 mins by microbeta scintillation counting methodDisplacement of [3H]-UR-PI294 from Galphai2/Gbeta1gamma2-coupled human recombinant H4R expressed in baculovirus infected Sf9 insect cell membranes co-expressing RGS19 measured after 60 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.0c00160
4908365 2119 79 None -3 8 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-UR-PI294 from Galphai2/Gbeta1gamma2-coupled human recombinant H4R expressed in baculovirus infected Sf9 insect cell membranes co-expressing RGS19 measured after 60 mins by microbeta scintillation counting methodDisplacement of [3H]-UR-PI294 from Galphai2/Gbeta1gamma2-coupled human recombinant H4R expressed in baculovirus infected Sf9 insect cell membranes co-expressing RGS19 measured after 60 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.0c00160
CHEMBL129198 2119 79 None -3 8 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-UR-PI294 from Galphai2/Gbeta1gamma2-coupled human recombinant H4R expressed in baculovirus infected Sf9 insect cell membranes co-expressing RGS19 measured after 60 mins by microbeta scintillation counting methodDisplacement of [3H]-UR-PI294 from Galphai2/Gbeta1gamma2-coupled human recombinant H4R expressed in baculovirus infected Sf9 insect cell membranes co-expressing RGS19 measured after 60 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.0c00160
1204 1901 114 None -3 23 Human 7.2 pKi = 7.2 Binding
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 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.0c00160
1247 1901 114 None -3 23 Human 7.2 pKi = 7.2 Binding
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 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.0c00160
1375 1901 114 None -3 23 Human 7.2 pKi = 7.2 Binding
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 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.0c00160
774 1901 114 None -3 23 Human 7.2 pKi = 7.2 Binding
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 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.0c00160
CHEMBL90 1901 114 None -3 23 Human 7.2 pKi = 7.2 Binding
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 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.0c00160
DB05381 1901 114 None -3 23 Human 7.2 pKi = 7.2 Binding
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 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.0c00160
1278 2119 79 None -3 8 Human 7.2 pKi = 7.2 Binding
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 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/acs.jmedchem.0c00160
1279 2119 79 None -3 8 Human 7.2 pKi = 7.2 Binding
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 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/acs.jmedchem.0c00160
4908365 2119 79 None -3 8 Human 7.2 pKi = 7.2 Binding
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 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/acs.jmedchem.0c00160
CHEMBL129198 2119 79 None -3 8 Human 7.2 pKi = 7.2 Binding
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 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/acs.jmedchem.0c00160
1278 2119 79 None -3 8 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-histamine from Galphai2/Gbeta1gamma2-coupled human recombinant H4R expressed in baculovirus infected Sf9 insect cell membranes co-expressing RGS19Displacement of [3H]-histamine from Galphai2/Gbeta1gamma2-coupled human recombinant H4R expressed in baculovirus infected Sf9 insect cell membranes co-expressing RGS19
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/acs.jmedchem.0c00160
1279 2119 79 None -3 8 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-histamine from Galphai2/Gbeta1gamma2-coupled human recombinant H4R expressed in baculovirus infected Sf9 insect cell membranes co-expressing RGS19Displacement of [3H]-histamine from Galphai2/Gbeta1gamma2-coupled human recombinant H4R expressed in baculovirus infected Sf9 insect cell membranes co-expressing RGS19
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/acs.jmedchem.0c00160
4908365 2119 79 None -3 8 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-histamine from Galphai2/Gbeta1gamma2-coupled human recombinant H4R expressed in baculovirus infected Sf9 insect cell membranes co-expressing RGS19Displacement of [3H]-histamine from Galphai2/Gbeta1gamma2-coupled human recombinant H4R expressed in baculovirus infected Sf9 insect cell membranes co-expressing RGS19
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/acs.jmedchem.0c00160
CHEMBL129198 2119 79 None -3 8 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-histamine from Galphai2/Gbeta1gamma2-coupled human recombinant H4R expressed in baculovirus infected Sf9 insect cell membranes co-expressing RGS19Displacement of [3H]-histamine from Galphai2/Gbeta1gamma2-coupled human recombinant H4R expressed in baculovirus infected Sf9 insect cell membranes co-expressing RGS19
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/acs.jmedchem.0c00160
10017821 103310 0 None 1 2 Human 7.2 pKi = 7.2 Binding
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 302 8 3 2 2.4 S=C(NCCCCc1c[nH]cn1)NCCc1ccccc1 10.1016/j.bmcl.2010.10.041
CHEMBL308913 103310 0 None 1 2 Human 7.2 pKi = 7.2 Binding
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 302 8 3 2 2.4 S=C(NCCCCc1c[nH]cn1)NCCc1ccccc1 10.1016/j.bmcl.2010.10.041
1204 1901 114 None -3 23 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-histamine from human recombinant H4R expressed in HEK293T cell homogenatesDisplacement of [3H]-histamine from human recombinant H4R expressed in HEK293T cell homogenates
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.0c00160
1247 1901 114 None -3 23 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-histamine from human recombinant H4R expressed in HEK293T cell homogenatesDisplacement of [3H]-histamine from human recombinant H4R expressed in HEK293T cell homogenates
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.0c00160
1375 1901 114 None -3 23 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-histamine from human recombinant H4R expressed in HEK293T cell homogenatesDisplacement of [3H]-histamine from human recombinant H4R expressed in HEK293T cell homogenates
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.0c00160
774 1901 114 None -3 23 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-histamine from human recombinant H4R expressed in HEK293T cell homogenatesDisplacement of [3H]-histamine from human recombinant H4R expressed in HEK293T cell homogenates
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.0c00160
CHEMBL90 1901 114 None -3 23 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-histamine from human recombinant H4R expressed in HEK293T cell homogenatesDisplacement of [3H]-histamine from human recombinant H4R expressed in HEK293T cell homogenates
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.0c00160
DB05381 1901 114 None -3 23 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-histamine from human recombinant H4R expressed in HEK293T cell homogenatesDisplacement of [3H]-histamine from human recombinant H4R expressed in HEK293T cell homogenates
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.0c00160
1278 2119 79 None -3 8 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-histamine from human recombinant H4R expressed in HEK293T cell homogenatesDisplacement of [3H]-histamine from human recombinant H4R expressed in HEK293T cell homogenates
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/acs.jmedchem.0c00160
1279 2119 79 None -3 8 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-histamine from human recombinant H4R expressed in HEK293T cell homogenatesDisplacement of [3H]-histamine from human recombinant H4R expressed in HEK293T cell homogenates
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/acs.jmedchem.0c00160
4908365 2119 79 None -3 8 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-histamine from human recombinant H4R expressed in HEK293T cell homogenatesDisplacement of [3H]-histamine from human recombinant H4R expressed in HEK293T cell homogenates
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/acs.jmedchem.0c00160
CHEMBL129198 2119 79 None -3 8 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-histamine from human recombinant H4R expressed in HEK293T cell homogenatesDisplacement of [3H]-histamine from human recombinant H4R expressed in HEK293T cell homogenates
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/acs.jmedchem.0c00160
1204 1901 114 None -3 23 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-histamine from human recombinant H4R stably expressed in human SK-N-MC cell homogenatesDisplacement of [3H]-histamine from human recombinant H4R stably expressed in human SK-N-MC cell homogenates
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.0c00160
1247 1901 114 None -3 23 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-histamine from human recombinant H4R stably expressed in human SK-N-MC cell homogenatesDisplacement of [3H]-histamine from human recombinant H4R stably expressed in human SK-N-MC cell homogenates
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.0c00160
1375 1901 114 None -3 23 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-histamine from human recombinant H4R stably expressed in human SK-N-MC cell homogenatesDisplacement of [3H]-histamine from human recombinant H4R stably expressed in human SK-N-MC cell homogenates
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.0c00160
774 1901 114 None -3 23 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-histamine from human recombinant H4R stably expressed in human SK-N-MC cell homogenatesDisplacement of [3H]-histamine from human recombinant H4R stably expressed in human SK-N-MC cell homogenates
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.0c00160
CHEMBL90 1901 114 None -3 23 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-histamine from human recombinant H4R stably expressed in human SK-N-MC cell homogenatesDisplacement of [3H]-histamine from human recombinant H4R stably expressed in human SK-N-MC cell homogenates
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.0c00160
DB05381 1901 114 None -3 23 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-histamine from human recombinant H4R stably expressed in human SK-N-MC cell homogenatesDisplacement of [3H]-histamine from human recombinant H4R stably expressed in human SK-N-MC cell homogenates
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.0c00160
1278 2119 79 None -3 8 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-histamine from human recombinant H4R stably expressed in human SK-N-MC cell homogenatesDisplacement of [3H]-histamine from human recombinant H4R stably expressed in human SK-N-MC cell homogenates
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/acs.jmedchem.0c00160
1279 2119 79 None -3 8 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-histamine from human recombinant H4R stably expressed in human SK-N-MC cell homogenatesDisplacement of [3H]-histamine from human recombinant H4R stably expressed in human SK-N-MC cell homogenates
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/acs.jmedchem.0c00160
4908365 2119 79 None -3 8 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-histamine from human recombinant H4R stably expressed in human SK-N-MC cell homogenatesDisplacement of [3H]-histamine from human recombinant H4R stably expressed in human SK-N-MC cell homogenates
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/acs.jmedchem.0c00160
CHEMBL129198 2119 79 None -3 8 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-histamine from human recombinant H4R stably expressed in human SK-N-MC cell homogenatesDisplacement of [3H]-histamine from human recombinant H4R stably expressed in human SK-N-MC cell homogenates
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/acs.jmedchem.0c00160
1204 1901 114 None -3 23 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-histamine from human recombinant H4R stably expressed in human SK-N-MC cell membranesDisplacement of [3H]-histamine from human recombinant H4R stably expressed in human SK-N-MC cell membranes
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.0c00160
1247 1901 114 None -3 23 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-histamine from human recombinant H4R stably expressed in human SK-N-MC cell membranesDisplacement of [3H]-histamine from human recombinant H4R stably expressed in human SK-N-MC cell membranes
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.0c00160
1375 1901 114 None -3 23 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-histamine from human recombinant H4R stably expressed in human SK-N-MC cell membranesDisplacement of [3H]-histamine from human recombinant H4R stably expressed in human SK-N-MC cell membranes
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.0c00160
774 1901 114 None -3 23 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-histamine from human recombinant H4R stably expressed in human SK-N-MC cell membranesDisplacement of [3H]-histamine from human recombinant H4R stably expressed in human SK-N-MC cell membranes
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.0c00160
CHEMBL90 1901 114 None -3 23 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-histamine from human recombinant H4R stably expressed in human SK-N-MC cell membranesDisplacement of [3H]-histamine from human recombinant H4R stably expressed in human SK-N-MC cell membranes
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.0c00160
DB05381 1901 114 None -3 23 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-histamine from human recombinant H4R stably expressed in human SK-N-MC cell membranesDisplacement of [3H]-histamine from human recombinant H4R stably expressed in human SK-N-MC cell membranes
ChEMBL 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1021/acs.jmedchem.0c00160
1278 2119 79 None -3 8 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-histamine from human recombinant H4R stably expressed in human SK-N-MC cell membranesDisplacement of [3H]-histamine from human recombinant H4R stably expressed in human SK-N-MC cell membranes
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/acs.jmedchem.0c00160
1279 2119 79 None -3 8 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-histamine from human recombinant H4R stably expressed in human SK-N-MC cell membranesDisplacement of [3H]-histamine from human recombinant H4R stably expressed in human SK-N-MC cell membranes
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/acs.jmedchem.0c00160
4908365 2119 79 None -3 8 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-histamine from human recombinant H4R stably expressed in human SK-N-MC cell membranesDisplacement of [3H]-histamine from human recombinant H4R stably expressed in human SK-N-MC cell membranes
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/acs.jmedchem.0c00160
CHEMBL129198 2119 79 None -3 8 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-histamine from human recombinant H4R stably expressed in human SK-N-MC cell membranesDisplacement of [3H]-histamine from human recombinant H4R stably expressed in human SK-N-MC cell membranes
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/acs.jmedchem.0c00160
10023327 168450 0 None -144 3 Human 7.2 pKi = 7.2 Binding
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 390 7 2 3 5.2 Clc1ccc(CN/C(=N\C2CCCCC2)SCCCc2c[nH]cn2)cc1 10.1021/jm201042n
CHEMBL43934 168450 0 None -144 3 Human 7.2 pKi = 7.2 Binding
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 390 7 2 3 5.2 Clc1ccc(CN/C(=N\C2CCCCC2)SCCCc2c[nH]cn2)cc1 10.1021/jm201042n
11499454 74071 0 None -1 2 Human 7.2 pKi = 7.2 Binding
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 209 6 2 2 2.5 CC(C)(C)NCCCCCc1c[nH]cn1 10.1021/jm0504353
CHEMBL202638 74071 0 None -1 2 Human 7.2 pKi = 7.2 Binding
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 209 6 2 2 2.5 CC(C)(C)NCCCCCc1c[nH]cn1 10.1021/jm0504353
10446240 74649 1 None -50 3 Human 7.2 pKi = 7.2 Binding
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 277 8 2 2 3.6 Clc1ccc(CNCCCCCc2c[nH]cn2)cc1 10.1021/jm0504353
CHEMBL203263 74649 1 None -50 3 Human 7.2 pKi = 7.2 Binding
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 277 8 2 2 3.6 Clc1ccc(CNCCCCCc2c[nH]cn2)cc1 10.1021/jm0504353
11622495 76224 0 None -9 2 Human 7.2 pKi = 7.2 Binding
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 195 8 2 2 2.1 CCCCNCCCCc1c[nH]cn1 10.1021/jm0504353
CHEMBL206303 76224 0 None -9 2 Human 7.2 pKi = 7.2 Binding
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 195 8 2 2 2.1 CCCCNCCCCc1c[nH]cn1 10.1021/jm0504353
1267 3744 43 None -33 25 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]histamine from human H4 receptor expressed in Sf9 cell membrane co-transfected with Galphai2 and Gbeta1gamma2 after 60 mins by liquid scintillation counting analysisDisplacement of [3H]histamine from human H4 receptor expressed in Sf9 cell membrane co-transfected with Galphai2 and Gbeta1gamma2 after 60 mins by liquid scintillation counting analysis
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1016/j.ejmech.2014.03.014
3035905 3744 43 None -33 25 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]histamine from human H4 receptor expressed in Sf9 cell membrane co-transfected with Galphai2 and Gbeta1gamma2 after 60 mins by liquid scintillation counting analysisDisplacement of [3H]histamine from human H4 receptor expressed in Sf9 cell membrane co-transfected with Galphai2 and Gbeta1gamma2 after 60 mins by liquid scintillation counting analysis
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1016/j.ejmech.2014.03.014
CHEMBL260374 3744 43 None -33 25 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]histamine from human H4 receptor expressed in Sf9 cell membrane co-transfected with Galphai2 and Gbeta1gamma2 after 60 mins by liquid scintillation counting analysisDisplacement of [3H]histamine from human H4 receptor expressed in Sf9 cell membrane co-transfected with Galphai2 and Gbeta1gamma2 after 60 mins by liquid scintillation counting analysis
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1016/j.ejmech.2014.03.014
12686479 161246 2 None - 1 Human 7.2 pKi = 7.2 Binding
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 244 1 1 5 1.1 CN1CCN(c2nc3ccccc3nc2O)CC1 10.1016/j.bmcl.2011.06.123
CHEMBL414183 161246 2 None - 1 Human 7.2 pKi = 7.2 Binding
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 244 1 1 5 1.1 CN1CCN(c2nc3ccccc3nc2O)CC1 10.1016/j.bmcl.2011.06.123
25129523 186704 40 None 1 2 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]histamine from human histamine H4 receptor E182'5.46Q mutant transfected in HEK293T cells after 1.5 hrs by liquid scintillation counting analysisDisplacement of [3H]histamine from human histamine H4 receptor E182'5.46Q mutant transfected in HEK293T cells after 1.5 hrs by liquid scintillation counting analysis
ChEMBL 269 2 1 5 1.5 CN1CCN(c2cc(-c3ccccc3)nc(N)n2)CC1 10.1039/C2MD20212C
CHEMBL492884 186704 40 None 1 2 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]histamine from human histamine H4 receptor E182'5.46Q mutant transfected in HEK293T cells after 1.5 hrs by liquid scintillation counting analysisDisplacement of [3H]histamine from human histamine H4 receptor E182'5.46Q mutant transfected in HEK293T cells after 1.5 hrs by liquid scintillation counting analysis
ChEMBL 269 2 1 5 1.5 CN1CCN(c2cc(-c3ccccc3)nc(N)n2)CC1 10.1039/C2MD20212C
25129527 186831 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]histamine from human histamine H4 receptor L175'5.39V mutant transfected in HEK293T cells after 1.5 hrs by liquid scintillation counting analysisDisplacement of [3H]histamine from human histamine H4 receptor L175'5.39V mutant 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 186831 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]histamine from human histamine H4 receptor L175'5.39V mutant transfected in HEK293T cells after 1.5 hrs by liquid scintillation counting analysisDisplacement of [3H]histamine from human histamine H4 receptor L175'5.39V mutant 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
70681962 75332 1 None - 1 Human 7.2 pKi = 7.2 Binding
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 2.3 O=C(c1cc2cc(Cl)ccc2[nH]1)N1CCCNCC1 10.1016/j.ejmech.2012.06.016
CHEMBL2047467 75332 1 None - 1 Human 7.2 pKi = 7.2 Binding
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 2.3 O=C(c1cc2cc(Cl)ccc2[nH]1)N1CCCNCC1 10.1016/j.ejmech.2012.06.016
70688339 75333 0 None - 1 Human 7.2 pKi = 7.2 Binding
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 309 1 1 2 2.7 CN1CCCN(C(=O)c2cc3cc(Cl)cc(F)c3[nH]2)CC1 10.1016/j.ejmech.2012.06.016
CHEMBL2047468 75333 0 None - 1 Human 7.2 pKi = 7.2 Binding
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 309 1 1 2 2.7 CN1CCCN(C(=O)c2cc3cc(Cl)cc(F)c3[nH]2)CC1 10.1016/j.ejmech.2012.06.016
1267 3744 43 None -33 25 Human 7.2 pKi = 7.2 Binding
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 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1021/jm1013488
3035905 3744 43 None -33 25 Human 7.2 pKi = 7.2 Binding
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 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1021/jm1013488
CHEMBL260374 3744 43 None -33 25 Human 7.2 pKi = 7.2 Binding
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 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1021/jm1013488
1267 3744 43 None -33 25 Human 7.2 pKi = 7.2 Binding
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 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1021/jm7014217
1267 3744 43 None -33 25 Human 7.2 pKi = 7.2 Binding
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 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1021/jm901379s
3035905 3744 43 None -33 25 Human 7.2 pKi = 7.2 Binding
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 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1021/jm7014217
3035905 3744 43 None -33 25 Human 7.2 pKi = 7.2 Binding
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 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1021/jm901379s
CHEMBL260374 3744 43 None -33 25 Human 7.2 pKi = 7.2 Binding
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 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1021/jm7014217
CHEMBL260374 3744 43 None -33 25 Human 7.2 pKi = 7.2 Binding
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 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1021/jm901379s
24854635 95895 0 None - 1 Human 7.2 pKi = 7.2 Binding
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 310 1 0 4 3.0 Cc1nc2cc(Cl)c(Cl)cc2nc1N1CCN(C)CC1 10.1021/jm7014217
CHEMBL261519 95895 0 None - 1 Human 7.2 pKi = 7.2 Binding
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 310 1 0 4 3.0 Cc1nc2cc(Cl)c(Cl)cc2nc1N1CCN(C)CC1 10.1021/jm7014217
10085528 193524 0 None -3 2 Human 7.2 pKi = 7.2 Binding
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 288 7 3 3 2.8 N=C(NCCc1ccccc1)SCCCc1c[nH]cn1 10.1016/j.bmc.2009.04.007
CHEMBL1202330 193524 0 None -3 2 Human 7.2 pKi = 7.2 Binding
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 288 7 3 3 2.8 N=C(NCCc1ccccc1)SCCCc1c[nH]cn1 10.1016/j.bmc.2009.04.007
CHEMBL550570 193524 0 None -3 2 Human 7.2 pKi = 7.2 Binding
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 288 7 3 3 2.8 N=C(NCCc1ccccc1)SCCCc1c[nH]cn1 10.1016/j.bmc.2009.04.007
10041484 193580 0 None -3 2 Human 7.2 pKi = 7.2 Binding
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 316 9 3 3 3.6 N=C(NCCCCc1ccccc1)SCCCc1c[nH]cn1 10.1016/j.bmc.2009.04.007
CHEMBL551047 193580 0 None -3 2 Human 7.2 pKi = 7.2 Binding
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 316 9 3 3 3.6 N=C(NCCCCc1ccccc1)SCCCc1c[nH]cn1 10.1016/j.bmc.2009.04.007
1267 3744 43 None -33 25 Human 7.2 pKi = 7.2 Binding
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 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1021/acs.jmedchem.0c00160
3035905 3744 43 None -33 25 Human 7.2 pKi = 7.2 Binding
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 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1021/acs.jmedchem.0c00160
CHEMBL260374 3744 43 None -33 25 Human 7.2 pKi = 7.2 Binding
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 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1021/acs.jmedchem.0c00160
1252 1986 16 None -100 4 Human 6.2 pKi = 6.2 Binding
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 153 5 2 2 1.1 NCCCCCc1cnc[nH]1 10.1021/acs.jmedchem.0c00160
9793868 1986 16 None -100 4 Human 6.2 pKi = 6.2 Binding
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 153 5 2 2 1.1 NCCCCCc1cnc[nH]1 10.1021/acs.jmedchem.0c00160
CHEMBL417096 1986 16 None -100 4 Human 6.2 pKi = 6.2 Binding
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 153 5 2 2 1.1 NCCCCCc1cnc[nH]1 10.1021/acs.jmedchem.0c00160
71681641 89234 0 None - 1 Human 6.2 pKi = 6.2 Binding
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 350 8 4 8 2.2 CC(C)CCc1cc(NCCNc2cc(Cl)nc(N)n2)nc(N)n1 10.1021/jm301886t
CHEMBL2375764 89234 0 None - 1 Human 6.2 pKi = 6.2 Binding
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 350 8 4 8 2.2 CC(C)CCc1cc(NCCNc2cc(Cl)nc(N)n2)nc(N)n1 10.1021/jm301886t
11492189 75653 0 None -10 2 Human 6.2 pKi = 6.2 Binding
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 209 8 1 2 2.5 CCN(CC)CCCCCc1c[nH]cn1 10.1021/jm0504353
CHEMBL205511 75653 0 None -10 2 Human 6.2 pKi = 6.2 Binding
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 209 8 1 2 2.5 CCN(CC)CCCCCc1c[nH]cn1 10.1021/jm0504353
14712103 61556 7 None - 1 Human 6.2 pKi = 6.2 Binding
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 201 5 2 2 1.7 c1ccc(CNCCc2c[nH]cn2)cc1 10.1016/j.bmcl.2011.06.123
CHEMBL17740 61556 7 None - 1 Human 6.2 pKi = 6.2 Binding
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 201 5 2 2 1.7 c1ccc(CNCCc2c[nH]cn2)cc1 10.1016/j.bmcl.2011.06.123
12741697 95713 2 None - 1 Human 6.2 pKi = 6.2 Binding
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 261 1 0 3 2.6 CN1CCN(c2ccc3cc(Cl)ccc3n2)CC1 10.1016/j.bmcl.2011.06.123
CHEMBL260565 95713 2 None - 1 Human 6.2 pKi = 6.2 Binding
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 261 1 0 3 2.6 CN1CCN(c2ccc3cc(Cl)ccc3n2)CC1 10.1016/j.bmcl.2011.06.123
9793921 64797 7 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]histamine from human H4R receptor expressed in SK-N-MC cells at 10 uM after 1.5 hrs by liquid scintillation countingDisplacement of [3H]histamine from human H4R receptor expressed in SK-N-MC cells at 10 uM after 1.5 hrs by liquid scintillation counting
ChEMBL 164 2 1 1 2.5 c1nc(CC2CCCCC2)c[nH]1 10.1016/j.bmcl.2011.06.123
CHEMBL1824228 64797 7 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]histamine from human H4R receptor expressed in SK-N-MC cells at 10 uM after 1.5 hrs by liquid scintillation countingDisplacement of [3H]histamine from human H4R receptor expressed in SK-N-MC cells at 10 uM after 1.5 hrs by liquid scintillation counting
ChEMBL 164 2 1 1 2.5 c1nc(CC2CCCCC2)c[nH]1 10.1016/j.bmcl.2011.06.123
24764570 75309 0 None - 1 Human 6.2 pKi = 6.2 Binding
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 2 2 2 1.9 CN[C@@H]1CCN(C(=O)c2cc3cccc(C)c3[nH]2)C1 10.1016/j.ejmech.2012.06.016
CHEMBL2047444 75309 0 None - 1 Human 6.2 pKi = 6.2 Binding
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 2 2 2 1.9 CN[C@@H]1CCN(C(=O)c2cc3cccc(C)c3[nH]2)C1 10.1016/j.ejmech.2012.06.016
25178938 186177 0 None - 1 Human 6.2 pKi = 6.2 Binding
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 271 2 1 5 1.7 CNc1nc(N2CCN(C)CC2)nc2cccc(C)c12 10.1021/jm901379s
CHEMBL488885 186177 0 None - 1 Human 6.2 pKi = 6.2 Binding
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 271 2 1 5 1.7 CNc1nc(N2CCN(C)CC2)nc2cccc(C)c12 10.1021/jm901379s
933006 136050 9 None - 1 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]-histamine from human histamine H4 receptor expressed in HEK293T cells after 1 to 1.5 hrs by liquid scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor expressed in HEK293T cells after 1 to 1.5 hrs by liquid scintillation counting analysis
ChEMBL 297 2 1 5 1.9 COc1ccc2c(c1)[nH]c1c(N3CCN(C)CC3)ncnc12 10.1039/C5MD00022J
CHEMBL3739430 136050 9 None - 1 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]-histamine from human histamine H4 receptor expressed in HEK293T cells after 1 to 1.5 hrs by liquid scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor expressed in HEK293T cells after 1 to 1.5 hrs by liquid scintillation counting analysis
ChEMBL 297 2 1 5 1.9 COc1ccc2c(c1)[nH]c1c(N3CCN(C)CC3)ncnc12 10.1039/C5MD00022J
10419556 5286 0 None -3 2 Human 5.2 pKi = 5.2 Binding
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 167 2 2 3 0.6 NC[C@H]1CC[C@@H](c2c[nH]cn2)O1 10.1016/j.bmcl.2010.10.041
CHEMBL106913 5286 0 None -3 2 Human 5.2 pKi = 5.2 Binding
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 167 2 2 3 0.6 NC[C@H]1CC[C@@H](c2c[nH]cn2)O1 10.1016/j.bmcl.2010.10.041
168273549 192201 0 None -5 4 Human 5.2 pKi = 5.2 Binding
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 192201 0 None -5 4 Human 5.2 pKi = 5.2 Binding
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 192201 0 None -5 4 Human 5.2 pKi = 5.2 Binding
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
66572103 75283 0 None - 1 Human 5.2 pKi = 5.2 Binding
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 244 1 1 3 1.0 CN1CCN(C(=O)c2cc3cnccc3[nH]2)CC1 10.1016/j.ejmech.2012.06.016
CHEMBL2047261 75283 0 None - 1 Human 5.2 pKi = 5.2 Binding
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 244 1 1 3 1.0 CN1CCN(C(=O)c2cc3cnccc3[nH]2)CC1 10.1016/j.ejmech.2012.06.016
164627020 185826 0 None -144 4 Human 5.2 pKi = 5.2 Binding
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 422 7 4 4 3.4 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NC(c1ccccc1)c1ccccc1 10.1016/j.ejmech.2021.113190
CHEMBL4876025 185826 0 None -144 4 Human 5.2 pKi = 5.2 Binding
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 422 7 4 4 3.4 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NC(c1ccccc1)c1ccccc1 10.1016/j.ejmech.2021.113190
10515993 5884 1 None -27 3 Human 6.2 pKi = 6.2 Binding
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 267 9 2 3 3.0 CCCCC[C@@H](C)NC(=O)OCCCc1c[nH]cn1 10.1016/j.bmcl.2009.10.005
CHEMBL1079918 5884 1 None -27 3 Human 6.2 pKi = 6.2 Binding
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 267 9 2 3 3.0 CCCCC[C@@H](C)NC(=O)OCCCc1c[nH]cn1 10.1016/j.bmcl.2009.10.005
CHEMBL154944 5884 1 None -27 3 Human 6.2 pKi = 6.2 Binding
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 267 9 2 3 3.0 CCCCC[C@@H](C)NC(=O)OCCCc1c[nH]cn1 10.1016/j.bmcl.2009.10.005
54587792 61225 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]histamine from human histamine H4 receptorDisplacement of [3H]histamine from human histamine H4 receptor
ChEMBL 248 2 2 6 0.2 Nc1nc(N2CCCC2)cc(N2CC[C@@H](N)C2)n1 10.1016/j.bmcl.2011.03.017
CHEMBL1770994 61225 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]histamine from human histamine H4 receptorDisplacement of [3H]histamine from human histamine H4 receptor
ChEMBL 248 2 2 6 0.2 Nc1nc(N2CCCC2)cc(N2CC[C@@H](N)C2)n1 10.1016/j.bmcl.2011.03.017
90645156 111691 0 None - 1 Human 4.2 pKi = 4.2 Binding
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 313 3 1 7 0.9 CN1CCN(c2nc(N)nc(-c3ccc(N(C)C)cc3)n2)CC1 10.1016/j.ejmech.2014.06.032
CHEMBL3290583 111691 0 None - 1 Human 4.2 pKi = 4.2 Binding
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 313 3 1 7 0.9 CN1CCN(c2nc(N)nc(-c3ccc(N(C)C)cc3)n2)CC1 10.1016/j.ejmech.2014.06.032
763018 136211 10 None - 1 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]-histamine from human histamine H4 receptor expressed in HEK293T cells after 1 to 1.5 hrs by liquid scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor expressed in HEK293T cells after 1 to 1.5 hrs by liquid scintillation counting analysis
ChEMBL 282 1 0 6 1.3 Cc1nnc2c(N3CCN(C)CC3)nc3ccccc3n12 10.1039/C5MD00022J
CHEMBL3740846 136211 10 None - 1 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]-histamine from human histamine H4 receptor expressed in HEK293T cells after 1 to 1.5 hrs by liquid scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor expressed in HEK293T cells after 1 to 1.5 hrs by liquid scintillation counting analysis
ChEMBL 282 1 0 6 1.3 Cc1nnc2c(N3CCN(C)CC3)nc3ccccc3n12 10.1039/C5MD00022J
44414498 79586 0 None -173 3 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]RAMHA from human histamine H4 receptor expressed in SK-N-MC cellsDisplacement of [3H]RAMHA from human histamine H4 receptor expressed in SK-N-MC cells
ChEMBL 404 7 0 2 6.9 CN(Cc1ccc(-c2ccc(CN(C)C3CCCCC3)cc2)cc1)C1CCCCC1 10.1016/j.bmc.2008.10.029
CHEMBL212775 79586 0 None -173 3 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]RAMHA from human histamine H4 receptor expressed in SK-N-MC cellsDisplacement of [3H]RAMHA from human histamine H4 receptor expressed in SK-N-MC cells
ChEMBL 404 7 0 2 6.9 CN(Cc1ccc(-c2ccc(CN(C)C3CCCCC3)cc2)cc1)C1CCCCC1 10.1016/j.bmc.2008.10.029
44414433 138999 0 None -8 3 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]RAMHA from human histamine H4 receptor expressed in SK-N-MC cellsDisplacement of [3H]RAMHA from human histamine H4 receptor expressed in SK-N-MC cells
ChEMBL 352 13 2 2 5.9 CCCCCNCc1ccc(-c2ccc(CNCCCCC)cc2)cc1 10.1016/j.bmc.2008.10.029
CHEMBL379545 138999 0 None -8 3 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]RAMHA from human histamine H4 receptor expressed in SK-N-MC cellsDisplacement of [3H]RAMHA from human histamine H4 receptor expressed in SK-N-MC cells
ChEMBL 352 13 2 2 5.9 CCCCCNCc1ccc(-c2ccc(CNCCCCC)cc2)cc1 10.1016/j.bmc.2008.10.029
10419556 5286 0 None -3 2 Human 5.2 pKi = 5.2 Binding
Histamine H4 receptor competition binding using [3H]Na-methylhistamineHistamine H4 receptor competition binding using [3H]Na-methylhistamine
ChEMBL 167 2 2 3 0.6 NC[C@H]1CC[C@@H](c2c[nH]cn2)O1 10.1021/jm0300025
CHEMBL106913 5286 0 None -3 2 Human 5.2 pKi = 5.2 Binding
Histamine H4 receptor competition binding using [3H]Na-methylhistamineHistamine H4 receptor competition binding using [3H]Na-methylhistamine
ChEMBL 167 2 2 3 0.6 NC[C@H]1CC[C@@H](c2c[nH]cn2)O1 10.1021/jm0300025
164623155 184993 0 None - 1 Human 4.2 pKi = 4.2 Binding
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 352 3 4 4 3.4 N/C(=N\C(=O)Nc1ccccc1)Nc1cccc(-c2csc(N)n2)c1 10.1016/j.ejmech.2021.113190
CHEMBL4863393 184993 0 None - 1 Human 4.2 pKi = 4.2 Binding
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 352 3 4 4 3.4 N/C(=N\C(=O)Nc1ccccc1)Nc1cccc(-c2csc(N)n2)c1 10.1016/j.ejmech.2021.113190
57395260 69386 0 None - 1 Human 6.2 pKi = 6.2 Binding
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 257 1 1 5 1.3 Cc1ccc2nc(N)nc(N3CCN(C)CC3)c2c1 10.1016/j.bmcl.2011.10.104
CHEMBL1935563 69386 0 None - 1 Human 6.2 pKi = 6.2 Binding
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 257 1 1 5 1.3 Cc1ccc2nc(N)nc(N3CCN(C)CC3)c2c1 10.1016/j.bmcl.2011.10.104
11408069 83848 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 440 6 1 4 5.2 CN1CCN(CCCOc2ccc(-c3nc4cc(C(C)(C)C)ccc4[nH]3)cc2Cl)CC1 10.1016/j.bmcl.2010.04.017
CHEMBL221211 83848 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 440 6 1 4 5.2 CN1CCN(CCCOc2ccc(-c3nc4cc(C(C)(C)C)ccc4[nH]3)cc2Cl)CC1 10.1016/j.bmcl.2010.04.017
11408069 83848 0 None - 1 Human 7.2 pKi = 7.2 Binding
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 440 6 1 4 5.2 CN1CCN(CCCOc2ccc(-c3nc4cc(C(C)(C)C)ccc4[nH]3)cc2Cl)CC1 10.1016/j.bmcl.2006.08.117
CHEMBL221211 83848 0 None - 1 Human 7.2 pKi = 7.2 Binding
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 440 6 1 4 5.2 CN1CCN(CCCOc2ccc(-c3nc4cc(C(C)(C)C)ccc4[nH]3)cc2Cl)CC1 10.1016/j.bmcl.2006.08.117
24825995 67803 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 377 2 2 6 3.0 CN[C@H]1CCN(c2nc(N)nc3c2sc2ccc(Br)cc23)C1 10.1016/j.bmcl.2011.08.014
CHEMBL1914795 67803 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 377 2 2 6 3.0 CN[C@H]1CCN(c2nc(N)nc3c2sc2ccc(Br)cc23)C1 10.1016/j.bmcl.2011.08.014
1267 3744 43 None -21 25 Mouse 7.2 pKi = 7.2 Binding
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 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1021/acs.jmedchem.0c00160
3035905 3744 43 None -21 25 Mouse 7.2 pKi = 7.2 Binding
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 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1021/acs.jmedchem.0c00160
CHEMBL260374 3744 43 None -21 25 Mouse 7.2 pKi = 7.2 Binding
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 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1021/acs.jmedchem.0c00160
762810 198225 11 None - 1 Human 5.2 pKi = 5.2 Binding
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 262 2 0 5 2.0 CCc1cc2c(N3CCN(C)CC3)ncnc2s1 10.1016/j.bmc.2009.08.059
CHEMBL594730 198225 11 None - 1 Human 5.2 pKi = 5.2 Binding
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 262 2 0 5 2.0 CCc1cc2c(N3CCN(C)CC3)ncnc2s1 10.1016/j.bmc.2009.08.059
51354299 58580 0 None 1 2 Human 7.2 pKi = 7.2 Binding
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 247 8 1 4 2.4 CCCCCc1cn(CCCc2c[nH]cn2)nn1 10.1021/jm1013488
CHEMBL1688945 58580 0 None 1 2 Human 7.2 pKi = 7.2 Binding
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 247 8 1 4 2.4 CCCCCc1cn(CCCc2c[nH]cn2)nn1 10.1021/jm1013488
136773074 156823 0 None - 1 Human 5.2 pKi = 5.2 Binding
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 156823 0 None - 1 Human 5.2 pKi = 5.2 Binding
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
57400473 69384 0 None - 1 Human 6.2 pKi = 6.2 Binding
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 361 3 1 6 2.8 CC(=O)c1cccc(-c2cccc3c(N4CCN(C)CC4)nc(N)nc23)c1 10.1016/j.bmcl.2011.10.104
CHEMBL1935561 69384 0 None - 1 Human 6.2 pKi = 6.2 Binding
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 361 3 1 6 2.8 CC(=O)c1cccc(-c2cccc3c(N4CCN(C)CC4)nc(N)nc23)c1 10.1016/j.bmcl.2011.10.104
57397301 67538 0 None -891 3 Human 5.2 pKi = 5.2 Binding
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 560 11 1 6 4.6 COc1ccc(CN(CCN(C)CCN2CCN(C(=O)c3cc4cc(Cl)ccc4[nH]3)CC2)c2ccccn2)cc1 10.1016/j.bmcl.2011.09.001
CHEMBL1910382 67538 0 None -891 3 Human 5.2 pKi = 5.2 Binding
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 560 11 1 6 4.6 COc1ccc(CN(CCN(C)CCN2CCN(C(=O)c3cc4cc(Cl)ccc4[nH]3)CC2)c2ccccn2)cc1 10.1016/j.bmcl.2011.09.001
127026018 136967 0 None -3 2 Human 5.2 pKi = 5.2 Binding
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 399 5 1 5 3.6 CN1CCN(c2nc(NCCc3ccccc3)nc3c2-c2ccccc2CC3)CC1 10.1016/j.bmcl.2015.12.035
CHEMBL3753985 136967 0 None -3 2 Human 5.2 pKi = 5.2 Binding
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 399 5 1 5 3.6 CN1CCN(c2nc(NCCc3ccccc3)nc3c2-c2ccccc2CC3)CC1 10.1016/j.bmcl.2015.12.035
73346048 91435 0 None -15 2 Human 5.2 pKi = 5.2 Binding
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 307 7 2 3 3.0 O=C(NCCc1ccc(Cl)cc1)OCCCc1c[nH]cn1 10.1016/j.bmcl.2013.06.075
CHEMBL2413359 91435 0 None -15 2 Human 5.2 pKi = 5.2 Binding
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 307 7 2 3 3.0 O=C(NCCc1ccc(Cl)cc1)OCCCc1c[nH]cn1 10.1016/j.bmcl.2013.06.075
164617783 184007 0 None -104 6 Human 5.2 pKi = 5.2 Binding
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 388 8 4 4 2.8 CCC(CNC(=O)/N=C(\N)NCCCc1sc(N)nc1C)c1ccccc1 10.1016/j.ejmech.2021.113190
CHEMBL4848815 184007 0 None -104 6 Human 5.2 pKi = 5.2 Binding
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 388 8 4 4 2.8 CCC(CNC(=O)/N=C(\N)NCCCc1sc(N)nc1C)c1ccccc1 10.1016/j.ejmech.2021.113190
71519499 86065 0 None - 1 Human 4.2 pKi = 4.2 Binding
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 340 2 1 6 2.1 CN1CCN(c2nc(N)nc3c2cc(-c2ccc(F)cc2)n3C)CC1 10.1016/j.bmcl.2012.10.139
CHEMBL2314768 86065 0 None - 1 Human 4.2 pKi = 4.2 Binding
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 340 2 1 6 2.1 CN1CCN(c2nc(N)nc3c2cc(-c2ccc(F)cc2)n3C)CC1 10.1016/j.bmcl.2012.10.139
54583872 61191 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]histamine from human histamine H4 receptorDisplacement of [3H]histamine from human histamine H4 receptor
ChEMBL 298 5 3 6 1.5 CN[C@@H]1CCN(c2cc(N)nc(NCc3ccccc3)n2)C1 10.1016/j.bmcl.2011.03.017
CHEMBL1770960 61191 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]histamine from human histamine H4 receptorDisplacement of [3H]histamine from human histamine H4 receptor
ChEMBL 298 5 3 6 1.5 CN[C@@H]1CCN(c2cc(N)nc(NCc3ccccc3)n2)C1 10.1016/j.bmcl.2011.03.017
1278 2119 79 None -3 8 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in sf9 cells co-expressing mammalian Galphai2 and Gbeta1gamma2Displacement of [3H]histamine from human histamine H4 receptor expressed in sf9 cells co-expressing mammalian Galphai2 and Gbeta1gamma2
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/acs.jmedchem.6b00120
1279 2119 79 None -3 8 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in sf9 cells co-expressing mammalian Galphai2 and Gbeta1gamma2Displacement of [3H]histamine from human histamine H4 receptor expressed in sf9 cells co-expressing mammalian Galphai2 and Gbeta1gamma2
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/acs.jmedchem.6b00120
4908365 2119 79 None -3 8 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in sf9 cells co-expressing mammalian Galphai2 and Gbeta1gamma2Displacement of [3H]histamine from human histamine H4 receptor expressed in sf9 cells co-expressing mammalian Galphai2 and Gbeta1gamma2
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/acs.jmedchem.6b00120
CHEMBL129198 2119 79 None -3 8 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in sf9 cells co-expressing mammalian Galphai2 and Gbeta1gamma2Displacement of [3H]histamine from human histamine H4 receptor expressed in sf9 cells co-expressing mammalian Galphai2 and Gbeta1gamma2
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/acs.jmedchem.6b00120
58227388 116622 1 None - 1 Human 7.2 pKi = 7.2 Binding
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)CNc1nccc(N2CCN(C)CC2)n1 10.1016/j.bmcl.2014.12.027
CHEMBL3393538 116622 1 None - 1 Human 7.2 pKi = 7.2 Binding
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)CNc1nccc(N2CCN(C)CC2)n1 10.1016/j.bmcl.2014.12.027
155517880 176093 0 None 16 2 Human 7.2 pKi = 7.2 Binding
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 291 4 4 5 1.0 CC(C)(C)CNc1nccc(N2CC[C@@H](NC(=N)N)C2)n1 10.1021/acs.jmedchem.9b01342
CHEMBL4445423 176093 0 None 16 2 Human 7.2 pKi = 7.2 Binding
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 291 4 4 5 1.0 CC(C)(C)CNc1nccc(N2CC[C@@H](NC(=N)N)C2)n1 10.1021/acs.jmedchem.9b01342
CHEMBL4598198 176093 0 None 16 2 Human 7.2 pKi = 7.2 Binding
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 291 4 4 5 1.0 CC(C)(C)CNc1nccc(N2CC[C@@H](NC(=N)N)C2)n1 10.1021/acs.jmedchem.9b01342
155517880 176093 0 None 16 2 Human 7.2 pKi = 7.2 Binding
Displacement of 40 nM [3H]-histamine from human H4R expressed in Sf9 cell membranes co-expressing Gia2 and beta1gamma2 by competition binding assayDisplacement of 40 nM [3H]-histamine from human H4R expressed in Sf9 cell membranes co-expressing Gia2 and beta1gamma2 by competition binding 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 176093 0 None 16 2 Human 7.2 pKi = 7.2 Binding
Displacement of 40 nM [3H]-histamine from human H4R expressed in Sf9 cell membranes co-expressing Gia2 and beta1gamma2 by competition binding assayDisplacement of 40 nM [3H]-histamine from human H4R expressed in Sf9 cell membranes co-expressing Gia2 and beta1gamma2 by competition binding 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 176093 0 None 16 2 Human 7.2 pKi = 7.2 Binding
Displacement of 40 nM [3H]-histamine from human H4R expressed in Sf9 cell membranes co-expressing Gia2 and beta1gamma2 by competition binding assayDisplacement of 40 nM [3H]-histamine from human H4R expressed in Sf9 cell membranes co-expressing Gia2 and beta1gamma2 by competition binding 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
46890626 6510 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human 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
CHEMBL1083097 6510 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human 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
25178938 186177 0 None - 1 Human 6.2 pKi = 6.2 Binding
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 271 2 1 5 1.7 CNc1nc(N2CCN(C)CC2)nc2cccc(C)c12 10.1021/jm800876b
CHEMBL488885 186177 0 None - 1 Human 6.2 pKi = 6.2 Binding
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 271 2 1 5 1.7 CNc1nc(N2CCN(C)CC2)nc2cccc(C)c12 10.1021/jm800876b
9812843 203533 1 None -4 2 Human 6.2 pKi = 6.2 Binding
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 159 2 1 2 1.4 c1cncc(Cc2c[nH]cn2)c1 10.1021/jm049932u
CHEMBL78838 203533 1 None -4 2 Human 6.2 pKi = 6.2 Binding
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 159 2 1 2 1.4 c1cncc(Cc2c[nH]cn2)c1 10.1021/jm049932u
647957 28864 12 None - 1 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]-histamine from human histamine H4 receptor expressed in HEK293T cells after 1 to 1.5 hrs by liquid scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor expressed in HEK293T cells after 1 to 1.5 hrs by liquid scintillation counting analysis
ChEMBL 277 2 0 6 0.4 Cc1cc(N2CCN(C)CC2)nc(N2CCOCC2)n1 10.1039/C5MD00022J
CHEMBL1381010 28864 12 None - 1 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]-histamine from human histamine H4 receptor expressed in HEK293T cells after 1 to 1.5 hrs by liquid scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor expressed in HEK293T cells after 1 to 1.5 hrs by liquid scintillation counting analysis
ChEMBL 277 2 0 6 0.4 Cc1cc(N2CCN(C)CC2)nc(N2CCOCC2)n1 10.1039/C5MD00022J
747187 136115 9 None - 1 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]-histamine from human histamine H4 receptor expressed in HEK293T cells after 1 to 1.5 hrs by liquid scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor expressed in HEK293T cells after 1 to 1.5 hrs by liquid scintillation counting analysis
ChEMBL 249 4 1 3 2.8 Cc1cc2nc(SCCN(C)C)[nH]c2cc1C 10.1039/C5MD00022J
CHEMBL3739949 136115 9 None - 1 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]-histamine from human histamine H4 receptor expressed in HEK293T cells after 1 to 1.5 hrs by liquid scintillation counting analysisDisplacement of [3H]-histamine from human histamine H4 receptor expressed in HEK293T cells after 1 to 1.5 hrs by liquid scintillation counting analysis
ChEMBL 249 4 1 3 2.8 Cc1cc2nc(SCCN(C)C)[nH]c2cc1C 10.1039/C5MD00022J
168268716 192160 0 None -3 4 Human 5.2 pKi = 5.2 Binding
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 192160 0 None -3 4 Human 5.2 pKi = 5.2 Binding
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 192160 0 None -3 4 Human 5.2 pKi = 5.2 Binding
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
168268853 192183 0 None -83 6 Human 5.2 pKi = 5.2 Binding
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 192183 0 None -83 6 Human 5.2 pKi = 5.2 Binding
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 192183 0 None -83 6 Human 5.2 pKi = 5.2 Binding
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
5013 99773 28 None -16 2 Human 5.2 pKi = 5.2 Binding
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 227 1 0 3 2.0 CN1CCN(c2ccc3ccccc3n2)CC1 10.1021/jm7014217
CHEMBL288591 99773 28 None -16 2 Human 5.2 pKi = 5.2 Binding
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 227 1 0 3 2.0 CN1CCN(c2ccc3ccccc3n2)CC1 10.1021/jm7014217
10243990 5817 0 None -79 3 Human 6.2 pKi = 6.2 Binding
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 2.6 CCCCC(C)NC(=O)OCCCc1c[nH]cn1 10.1016/j.bmcl.2009.10.005
CHEMBL1079552 5817 0 None -79 3 Human 6.2 pKi = 6.2 Binding
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 2.6 CCCCC(C)NC(=O)OCCCc1c[nH]cn1 10.1016/j.bmcl.2009.10.005
CHEMBL155830 5817 0 None -79 3 Human 6.2 pKi = 6.2 Binding
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 2.6 CCCCC(C)NC(=O)OCCCc1c[nH]cn1 10.1016/j.bmcl.2009.10.005
11065080 19236 2 None - 1 Human 8.2 pKi = 8.2 Binding
Antagonist activity at Homo sapiens (human) histamine H4 receptorAntagonist activity at Homo sapiens (human) histamine H4 receptor
ChEMBL 257 1 1 2 1.9 Cc1cccc2cc(C(=O)N3CCN(C)CC3)[nH]c12 10.1007/s00044-004-0106-7
CHEMBL129488 19236 2 None - 1 Human 8.2 pKi = 8.2 Binding
Antagonist activity at Homo sapiens (human) histamine H4 receptorAntagonist activity at Homo sapiens (human) histamine H4 receptor
ChEMBL 257 1 1 2 1.9 Cc1cccc2cc(C(=O)N3CCN(C)CC3)[nH]c12 10.1007/s00044-004-0106-7
11065080 19236 2 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]- histamine from the recombinant human histamine H4 receptorDisplacement of [3H]- histamine from the recombinant human histamine H4 receptor
ChEMBL 257 1 1 2 1.9 Cc1cccc2cc(C(=O)N3CCN(C)CC3)[nH]c12 10.1021/jm0341047
CHEMBL129488 19236 2 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]- histamine from the recombinant human histamine H4 receptorDisplacement of [3H]- histamine from the recombinant human histamine H4 receptor
ChEMBL 257 1 1 2 1.9 Cc1cccc2cc(C(=O)N3CCN(C)CC3)[nH]c12 10.1021/jm0341047
117724523 116613 2 None - 1 Human 8.2 pKi = 8.2 Binding
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
CHEMBL3393529 116613 2 None - 1 Human 8.2 pKi = 8.2 Binding
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
11594278 14521 0 None - 1 Human 8.2 pKi = 8.2 Binding
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 276 1 1 3 1.4 Cc1c(F)ccc2[nH]c(C(=O)N3CCN(C)CC3)nc12 10.1021/jm0502081
CHEMBL120591 14521 0 None - 1 Human 8.2 pKi = 8.2 Binding
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 276 1 1 3 1.4 Cc1c(F)ccc2[nH]c(C(=O)N3CCN(C)CC3)nc12 10.1021/jm0502081
11065080 19236 2 None - 1 Human 8.2 pKi = 8.2 Binding
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 257 1 1 2 1.9 Cc1cccc2cc(C(=O)N3CCN(C)CC3)[nH]c12 10.1021/jm0502081
CHEMBL129488 19236 2 None - 1 Human 8.2 pKi = 8.2 Binding
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 257 1 1 2 1.9 Cc1cccc2cc(C(=O)N3CCN(C)CC3)[nH]c12 10.1021/jm0502081
44462956 5523 0 None -2 2 Human 8.2 pKi = 8.2 Binding
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 363 2 2 5 3.1 Nc1nc2c(c(N3CC4CCCNC4C3)n1)CCCCC2c1ccccc1 10.1016/j.bmcl.2010.01.131
CHEMBL1077276 5523 0 None -2 2 Human 8.2 pKi = 8.2 Binding
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 363 2 2 5 3.1 Nc1nc2c(c(N3CC4CCCNC4C3)n1)CCCCC2c1ccccc1 10.1016/j.bmcl.2010.01.131
71603140 89289 0 None 97 2 Human 8.2 pKi = 8.2 Binding
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 3 2 5 1.5 CNC1CN(c2nc(N)nc3cc(C4CC4)ccc23)C1 10.1016/j.bmcl.2013.02.091
CHEMBL2376794 89289 0 None 97 2 Human 8.2 pKi = 8.2 Binding
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 3 2 5 1.5 CNC1CN(c2nc(N)nc3cc(C4CC4)ccc23)C1 10.1016/j.bmcl.2013.02.091
25147772 172837 4 None -1 3 Human 8.1 pKi = 8.1 Binding
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 373 4 1 6 3.7 CN1CCN(c2nc(NCc3cccs3)c3cc(Cl)ccc3n2)CC1 10.1021/jm800876b
CHEMBL452847 172837 4 None -1 3 Human 8.1 pKi = 8.1 Binding
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 373 4 1 6 3.7 CN1CCN(c2nc(NCc3cccs3)c3cc(Cl)ccc3n2)CC1 10.1021/jm800876b
25147772 172837 4 None -1 3 Human 8.1 pKi = 8.1 Binding
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 373 4 1 6 3.7 CN1CCN(c2nc(NCc3cccs3)c3cc(Cl)ccc3n2)CC1 10.1021/jm901379s
CHEMBL452847 172837 4 None -1 3 Human 8.1 pKi = 8.1 Binding
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 373 4 1 6 3.7 CN1CCN(c2nc(NCc3cccs3)c3cc(Cl)ccc3n2)CC1 10.1021/jm901379s
44129131 197773 0 None - 1 Human 8.1 pKi = 8.1 Binding
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 440 8 1 7 2.1 CCN(CC)S(=O)(=O)CCNc1nc(N2CCN(C)CC2)nc2ccc(Cl)cc12 10.1021/jm901379s
CHEMBL591500 197773 0 None - 1 Human 8.1 pKi = 8.1 Binding
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 440 8 1 7 2.1 CCN(CC)S(=O)(=O)CCNc1nc(N2CCN(C)CC2)nc2ccc(Cl)cc12 10.1021/jm901379s
25071319 188474 8 None 9 2 Rat 8.1 pKi = 8.1 Binding
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 295 1 2 5 1.6 Nc1nc2c(c(N3CCNCC3)n1)CCCc1ccccc1-2 10.1021/jm800670r
CHEMBL509540 188474 8 None 9 2 Rat 8.1 pKi = 8.1 Binding
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 295 1 2 5 1.6 Nc1nc2c(c(N3CCNCC3)n1)CCCc1ccccc1-2 10.1021/jm800670r
16082828 79850 0 None 1 2 Human 8.1 pKi = 8.1 Binding
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
CHEMBL213886 79850 0 None 1 2 Human 8.1 pKi = 8.1 Binding
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
57398091 67766 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 351 1 1 6 3.0 CN1CCN(c2nc(N)nc3c2oc2ccc(Cl)c(Cl)c23)CC1 10.1016/j.bmcl.2011.08.014
CHEMBL1914757 67766 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 351 1 1 6 3.0 CN1CCN(c2nc(N)nc3c2oc2ccc(Cl)c(Cl)c23)CC1 10.1016/j.bmcl.2011.08.014
57401517 67783 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 337 1 2 6 2.7 Nc1nc(N2CCNCC2)c2oc3ccc(Cl)c(Cl)c3c2n1 10.1016/j.bmcl.2011.08.014
CHEMBL1914774 67783 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 337 1 2 6 2.7 Nc1nc(N2CCNCC2)c2oc3ccc(Cl)c(Cl)c3c2n1 10.1016/j.bmcl.2011.08.014
3035746 187597 6 None -1 2 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in SK-NM-C cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in SK-NM-C cells
ChEMBL 414 7 2 3 3.2 N/C(=N/CCc1ccc(I)cc1)SCCCc1cnc[nH]1 10.1021/jm7014777
CHEMBL1237146 187597 6 None -1 2 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in SK-NM-C cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in SK-NM-C cells
ChEMBL 414 7 2 3 3.2 N/C(=N/CCc1ccc(I)cc1)SCCCc1cnc[nH]1 10.1021/jm7014777
CHEMBL498770 187597 6 None -1 2 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in SK-NM-C cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in SK-NM-C cells
ChEMBL 414 7 2 3 3.2 N/C(=N/CCc1ccc(I)cc1)SCCCc1cnc[nH]1 10.1021/jm7014777
136030655 56188 0 None 2 3 Mouse 8.1 pKi = 8.1 Binding
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 292 1 2 3 2.2 CN1CCN(/C(=N\O)c2cc3cc(Cl)ccc3[nH]2)CC1 10.1016/j.bmcl.2010.10.041
CHEMBL1632413 56188 0 None 2 3 Mouse 8.1 pKi = 8.1 Binding
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 292 1 2 3 2.2 CN1CCN(/C(=N\O)c2cc3cc(Cl)ccc3[nH]2)CC1 10.1016/j.bmcl.2010.10.041
136192874 56189 0 None 1 3 Mouse 8.1 pKi = 8.1 Binding
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 292 2 2 4 2.7 CN1CCC(/C(=N/O)c2nc3cc(Cl)ccc3[nH]2)CC1 10.1016/j.bmcl.2010.10.041
CHEMBL1632414 56189 0 None 1 3 Mouse 8.1 pKi = 8.1 Binding
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 292 2 2 4 2.7 CN1CCC(/C(=N/O)c2nc3cc(Cl)ccc3[nH]2)CC1 10.1016/j.bmcl.2010.10.041
1204 1901 114 None -3 23 Human 8.1 pKi = 8.1 Binding
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 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmcl.2004.08.035
1247 1901 114 None -3 23 Human 8.1 pKi = 8.1 Binding
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 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmcl.2004.08.035
1375 1901 114 None -3 23 Human 8.1 pKi = 8.1 Binding
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 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmcl.2004.08.035
774 1901 114 None -3 23 Human 8.1 pKi = 8.1 Binding
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 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmcl.2004.08.035
CHEMBL90 1901 114 None -3 23 Human 8.1 pKi = 8.1 Binding
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 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmcl.2004.08.035
DB05381 1901 114 None -3 23 Human 8.1 pKi = 8.1 Binding
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 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmcl.2004.08.035
1204 1901 114 None -3 23 Human 8.1 pKi = 8.1 Binding
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 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmcl.2010.10.041
1247 1901 114 None -3 23 Human 8.1 pKi = 8.1 Binding
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 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmcl.2010.10.041
1375 1901 114 None -3 23 Human 8.1 pKi = 8.1 Binding
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 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmcl.2010.10.041
774 1901 114 None -3 23 Human 8.1 pKi = 8.1 Binding
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 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmcl.2010.10.041
CHEMBL90 1901 114 None -3 23 Human 8.1 pKi = 8.1 Binding
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 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmcl.2010.10.041
DB05381 1901 114 None -3 23 Human 8.1 pKi = 8.1 Binding
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 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmcl.2010.10.041
53321919 56184 0 None -3 2 Human 8.1 pKi = 8.1 Binding
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 322 7 3 3 3.8 N=C(NCc1ccc(Cl)cc1)SCCCCc1c[nH]cn1 10.1016/j.bmcl.2010.10.041
CHEMBL1632409 56184 0 None -3 2 Human 8.1 pKi = 8.1 Binding
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 322 7 3 3 3.8 N=C(NCc1ccc(Cl)cc1)SCCCCc1c[nH]cn1 10.1016/j.bmcl.2010.10.041
10060213 102438 1 None 3 2 Human 8.1 pKi = 8.1 Binding
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 6 3 2 2.0 CC(C)/N=C(\S)NCCCCc1c[nH]cn1 10.1016/j.bmcl.2010.10.041
CHEMBL306077 102438 1 None 3 2 Human 8.1 pKi = 8.1 Binding
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 6 3 2 2.0 CC(C)/N=C(\S)NCCCCc1c[nH]cn1 10.1016/j.bmcl.2010.10.041
155491015 175921 3 None -7 4 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]NAMH from human H4R expressed in HEK293T cells incubated for 2 hrs by microbeta scintillation counting analysisDisplacement of [3H]NAMH from human H4R expressed in HEK293T cells incubated for 2 hrs by microbeta scintillation counting analysis
ChEMBL 207 4 2 5 0.2 CCCNC1CN(c2ccnc(N)n2)C1 10.1021/acs.jmedchem.9b01462
CHEMBL4441731 175921 3 None -7 4 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]NAMH from human H4R expressed in HEK293T cells incubated for 2 hrs by microbeta scintillation counting analysisDisplacement of [3H]NAMH from human H4R expressed in HEK293T cells incubated for 2 hrs by microbeta scintillation counting analysis
ChEMBL 207 4 2 5 0.2 CCCNC1CN(c2ccnc(N)n2)C1 10.1021/acs.jmedchem.9b01462
CHEMBL4596734 175921 3 None -7 4 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]NAMH from human H4R expressed in HEK293T cells incubated for 2 hrs by microbeta scintillation counting analysisDisplacement of [3H]NAMH from human H4R expressed in HEK293T cells incubated for 2 hrs by microbeta scintillation counting analysis
ChEMBL 207 4 2 5 0.2 CCCNC1CN(c2ccnc(N)n2)C1 10.1021/acs.jmedchem.9b01462
44609412 89244 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]histamine displacement from human recombinant histamine H4 receptor expressed in SK-NM-C cells after 45 minsDisplacement of [3H]histamine displacement from human recombinant histamine H4 receptor expressed in SK-NM-C cells after 45 mins
ChEMBL 322 6 4 8 1.6 Nc1nccc(NCCNc2cc(-c3ccccc3)nc(N)n2)n1 10.1021/jm301886t
CHEMBL2375773 89244 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]histamine displacement from human recombinant histamine H4 receptor expressed in SK-NM-C cells after 45 minsDisplacement of [3H]histamine displacement from human recombinant histamine H4 receptor expressed in SK-NM-C cells after 45 mins
ChEMBL 322 6 4 8 1.6 Nc1nccc(NCCNc2cc(-c3ccccc3)nc(N)n2)n1 10.1021/jm301886t
25129523 186704 40 None 1 2 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]histamine displacement from human recombinant histamine H4 receptor expressed in SK-NM-C cells after 45 minsDisplacement of [3H]histamine displacement from human recombinant histamine H4 receptor expressed in SK-NM-C cells after 45 mins
ChEMBL 269 2 1 5 1.5 CN1CCN(c2cc(-c3ccccc3)nc(N)n2)CC1 10.1021/jm301886t
CHEMBL492884 186704 40 None 1 2 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]histamine displacement from human recombinant histamine H4 receptor expressed in SK-NM-C cells after 45 minsDisplacement of [3H]histamine displacement from human recombinant histamine H4 receptor expressed in SK-NM-C cells after 45 mins
ChEMBL 269 2 1 5 1.5 CN1CCN(c2cc(-c3ccccc3)nc(N)n2)CC1 10.1021/jm301886t
51354584 58592 0 None 11 2 Human 8.1 pKi = 8.1 Binding
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 259 6 1 4 2.4 c1nc(CCCn2cc(CC3CCCC3)nn2)c[nH]1 10.1021/jm1013488
CHEMBL1688976 58592 0 None 11 2 Human 8.1 pKi = 8.1 Binding
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 259 6 1 4 2.4 c1nc(CCCn2cc(CC3CCCC3)nn2)c[nH]1 10.1021/jm1013488
76314798 105572 0 None - 1 Human 8.1 pKi = 8.1 Binding
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 314 3 1 7 1.4 CN1CCN(c2cc(-c3ccc([N+](=O)[O-])cc3)nc(N)n2)CC1 10.1039/C2MD20212C
CHEMBL3133131 105572 0 None - 1 Human 8.1 pKi = 8.1 Binding
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 314 3 1 7 1.4 CN1CCN(c2cc(-c3ccc([N+](=O)[O-])cc3)nc(N)n2)CC1 10.1039/C2MD20212C
136042269 69571 0 None - 1 Human 7.2 pKi = 7.2 Binding
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 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 69571 0 None - 1 Human 7.2 pKi = 7.2 Binding
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 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
71525678 89295 0 None -7 6 Rat 7.2 pKi = 7.2 Binding
Binding affinity to rat histamine H4 receptorBinding affinity to rat histamine H4 receptor
ChEMBL 258 3 2 6 0.6 CCc1cnc2c(N3CC(NC)C3)nc(N)nc2c1 10.1016/j.bmcl.2013.02.091
CHEMBL2376800 89295 0 None -7 6 Rat 7.2 pKi = 7.2 Binding
Binding affinity to rat histamine H4 receptorBinding affinity to rat histamine H4 receptor
ChEMBL 258 3 2 6 0.6 CCc1cnc2c(N3CC(NC)C3)nc(N)nc2c1 10.1016/j.bmcl.2013.02.091
25178937 186202 0 None - 1 Human 7.2 pKi = 7.2 Binding
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 291 2 1 5 2.1 CNc1nc(N2CCN(C)CC2)nc2ccc(Cl)cc12 10.1021/jm800876b
CHEMBL489062 186202 0 None - 1 Human 7.2 pKi = 7.2 Binding
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 291 2 1 5 2.1 CNc1nc(N2CCN(C)CC2)nc2ccc(Cl)cc12 10.1021/jm800876b
25071319 188474 8 None -9 2 Human 7.2 pKi = 7.2 Binding
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 1 2 5 1.6 Nc1nc2c(c(N3CCNCC3)n1)CCCc1ccccc1-2 10.1021/jm800670r
CHEMBL509540 188474 8 None -9 2 Human 7.2 pKi = 7.2 Binding
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 1 2 5 1.6 Nc1nc2c(c(N3CCNCC3)n1)CCCc1ccccc1-2 10.1021/jm800670r
44129209 200344 0 None - 1 Human 7.2 pKi = 7.2 Binding
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 586 7 2 7 3.5 CN1CCN(c2nc(NCCS(=O)(=O)Nc3ccc(I)cc3)c3cc(Cl)ccc3n2)CC1 10.1021/jm901379s
CHEMBL608373 200344 0 None - 1 Human 7.2 pKi = 7.2 Binding
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 586 7 2 7 3.5 CN1CCN(c2nc(NCCS(=O)(=O)Nc3ccc(I)cc3)c3cc(Cl)ccc3n2)CC1 10.1021/jm901379s
11013044 18722 1 None - 1 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]- histamine from the recombinant human histamine H4 receptorDisplacement of [3H]- histamine from the recombinant human histamine H4 receptor
ChEMBL 333 4 1 2 3.2 O=C(c1cc2ccccc2[nH]1)N1CCN(CCc2ccccc2)CC1 10.1021/jm0341047
CHEMBL128470 18722 1 None - 1 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]- histamine from the recombinant human histamine H4 receptorDisplacement of [3H]- histamine from the recombinant human histamine H4 receptor
ChEMBL 333 4 1 2 3.2 O=C(c1cc2ccccc2[nH]1)N1CCN(CCc2ccccc2)CC1 10.1021/jm0341047
122194625 123503 0 None - 1 Human 6.2 pKi = 6.2 Binding
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 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 123503 0 None - 1 Human 6.2 pKi = 6.2 Binding
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 310 3 1 6 1.7 Cc1cccc(/C=C/c2nc(N)nc(N3CCN(C)CC3)n2)c1 10.1016/j.ejmech.2015.08.014
52952957 62833 0 None -29 2 Human 6.2 pKi = 6.2 Binding
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 251 8 2 3 2.4 CCC/C=C/CNC(=O)OCCCc1c[nH]cn1 10.1016/j.bmc.2011.03.046
CHEMBL1774594 62833 0 None -29 2 Human 6.2 pKi = 6.2 Binding
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 251 8 2 3 2.4 CCC/C=C/CNC(=O)OCCCc1c[nH]cn1 10.1016/j.bmc.2011.03.046
CHEMBL1789799 62833 0 None -29 2 Human 6.2 pKi = 6.2 Binding
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 251 8 2 3 2.4 CCC/C=C/CNC(=O)OCCCc1c[nH]cn1 10.1016/j.bmc.2011.03.046
24854703 166334 0 None - 1 Human 6.2 pKi = 6.2 Binding
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 364 5 0 6 3.0 COc1ccc(COc2nc3ccccc3nc2N2CCN(C)CC2)cc1 10.1021/jm7014217
CHEMBL428606 166334 0 None - 1 Human 6.2 pKi = 6.2 Binding
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 364 5 0 6 3.0 COc1ccc(COc2nc3ccccc3nc2N2CCN(C)CC2)cc1 10.1021/jm7014217
156013005 176925 0 None -2 2 Human 5.2 pKi = 5.2 Binding
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 899 20 2 7 10.6 Cc1cc(OCCCNC(=O)CCCCCN2/C(=C\C=C\C=C\C3=[N+](CCCCS(=O)(=O)[O-])c4ccccc4C3(C)C)C(C)(C)c3ccccc32)ccc1-c1nc2c(C)c(F)ccc2[nH]1 10.1021/acs.jmedchem.0c00160
CHEMBL4639472 176925 0 None -2 2 Human 5.2 pKi = 5.2 Binding
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 899 20 2 7 10.6 Cc1cc(OCCCNC(=O)CCCCCN2/C(=C\C=C\C=C\C3=[N+](CCCCS(=O)(=O)[O-])c4ccccc4C3(C)C)C(C)(C)c3ccccc32)ccc1-c1nc2c(C)c(F)ccc2[nH]1 10.1021/acs.jmedchem.0c00160
168268827 192177 0 None -6 4 Human 5.2 pKi = 5.2 Binding
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 192177 0 None -6 4 Human 5.2 pKi = 5.2 Binding
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 192177 0 None -6 4 Human 5.2 pKi = 5.2 Binding
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
52952957 62833 0 None -29 2 Human 5.2 pKi = 5.2 Binding
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 251 8 2 3 2.4 CCC/C=C/CNC(=O)OCCCc1c[nH]cn1 10.1016/j.bmcl.2013.06.075
CHEMBL1774594 62833 0 None -29 2 Human 5.2 pKi = 5.2 Binding
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 251 8 2 3 2.4 CCC/C=C/CNC(=O)OCCCc1c[nH]cn1 10.1016/j.bmcl.2013.06.075
CHEMBL1789799 62833 0 None -29 2 Human 5.2 pKi = 5.2 Binding
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 251 8 2 3 2.4 CCC/C=C/CNC(=O)OCCCc1c[nH]cn1 10.1016/j.bmcl.2013.06.075
25071319 188474 8 None -9 2 Human 7.2 pKi = 7.2 Binding
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 1 2 5 1.6 Nc1nc2c(c(N3CCNCC3)n1)CCCc1ccccc1-2 10.1021/jm800670r
CHEMBL509540 188474 8 None -9 2 Human 7.2 pKi = 7.2 Binding
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 1 2 5 1.6 Nc1nc2c(c(N3CCNCC3)n1)CCCc1ccccc1-2 10.1021/jm800670r
46228101 198116 0 None - 1 Human 7.2 pKi = 7.2 Binding
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 332 4 2 6 2.1 CN1CCN(c2cc(NCc3ccc(Cl)cc3)nc(N)n2)CC1 10.1016/j.bmc.2009.08.059
CHEMBL594022 198116 0 None - 1 Human 7.2 pKi = 7.2 Binding
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 332 4 2 6 2.1 CN1CCN(c2cc(NCc3ccc(Cl)cc3)nc(N)n2)CC1 10.1016/j.bmc.2009.08.059
46228083 198059 0 None - 1 Human 6.1 pKi = 6.1 Binding
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 374 5 2 6 3.1 CN1CCN(c2cc(NCc3ccc(-c4ccccc4)cc3)nc(N)n2)CC1 10.1016/j.bmc.2009.08.059
CHEMBL593551 198059 0 None - 1 Human 6.1 pKi = 6.1 Binding
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 374 5 2 6 3.1 CN1CCN(c2cc(NCc3ccc(-c4ccccc4)cc3)nc(N)n2)CC1 10.1016/j.bmc.2009.08.059
46890549 6507 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
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 6507 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
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
112936352 136969 1 None -17 2 Human 4.1 pKi = 4.1 Binding
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 389 6 1 6 3.5 COc1ccc(CNc2cc(-c3ccccc3)nc(N3CCN(C)CC3)n2)cc1 10.1016/j.bmcl.2015.12.035
CHEMBL3754008 136969 1 None -17 2 Human 4.1 pKi = 4.1 Binding
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 389 6 1 6 3.5 COc1ccc(CNc2cc(-c3ccccc3)nc(N3CCN(C)CC3)n2)cc1 10.1016/j.bmcl.2015.12.035
155563489 174757 0 None - 1 Human 6.1 pKi = 6.1 Binding
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 3 1 6 0.7 CCC(C)c1nc(N)nc(N2CCN(C)CC2)n1 10.1016/j.bmc.2019.02.020
CHEMBL4573929 174757 0 None - 1 Human 6.1 pKi = 6.1 Binding
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 3 1 6 0.7 CCC(C)c1nc(N)nc(N2CCN(C)CC2)n1 10.1016/j.bmc.2019.02.020
71518865 86035 0 None - 1 Human 5.1 pKi = 5.1 Binding
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 333 2 2 6 1.8 CN1CCN(c2nc(N)nc3[nH]c(-c4ccc(C#N)cc4)cc23)CC1 10.1016/j.bmcl.2012.10.139
CHEMBL2314494 86035 0 None - 1 Human 5.1 pKi = 5.1 Binding
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 333 2 2 6 1.8 CN1CCN(c2nc(N)nc3[nH]c(-c4ccc(C#N)cc4)cc23)CC1 10.1016/j.bmcl.2012.10.139
57401167 69526 0 None - 1 Human 7.1 pKi = 7.1 Binding
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 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 69526 0 None - 1 Human 7.1 pKi = 7.1 Binding
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 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
24826679 67760 0 None - 1 Human 7.1 pKi = 7.1 Binding
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)nc3c2oc2cccc(Cl)c23)CC1 10.1016/j.bmcl.2011.08.014
CHEMBL1914751 67760 0 None - 1 Human 7.1 pKi = 7.1 Binding
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)nc3c2oc2cccc(Cl)c23)CC1 10.1016/j.bmcl.2011.08.014
168294161 192404 0 None -7 4 Human 5.1 pKi = 5.1 Binding
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 192404 0 None -7 4 Human 5.1 pKi = 5.1 Binding
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 192404 0 None -7 4 Human 5.1 pKi = 5.1 Binding
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
168294770 192418 0 None -6 4 Human 5.1 pKi = 5.1 Binding
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 192418 0 None -6 4 Human 5.1 pKi = 5.1 Binding
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 192418 0 None -6 4 Human 5.1 pKi = 5.1 Binding
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
44450438 95675 0 None - 1 Human 5.1 pKi = 5.1 Binding
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(c2nc3ccccc3nc2NCc2ccccc2)CC1 10.1021/jm7014217
CHEMBL260371 95675 0 None - 1 Human 5.1 pKi = 5.1 Binding
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(c2nc3ccccc3nc2NCc2ccccc2)CC1 10.1021/jm7014217
71528209 86544 0 None -1148 7 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cells
ChEMBL 465 6 0 3 5.8 CC1=CC(C)=[N+]2C1=C(c1ccc(OCCCN3CCCCC3)cc1)c1c(C)cc(C)n1[B-]2(F)F 10.1021/ml300383n
CHEMBL2323582 86544 0 None -1148 7 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cells
ChEMBL 465 6 0 3 5.8 CC1=CC(C)=[N+]2C1=C(c1ccc(OCCCN3CCCCC3)cc1)c1c(C)cc(C)n1[B-]2(F)F 10.1021/ml300383n
121238069 158580 0 None -79 2 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]-histamine from human histamine H4R expressed in insect Sf9 cell membranes co-expressing Galphai2 and Gbeta1gamma2 after 60 mins by liquid scintillation counting methodDisplacement of [3H]-histamine from human histamine H4R expressed in insect Sf9 cell membranes co-expressing Galphai2 and Gbeta1gamma2 after 60 mins by liquid scintillation counting method
ChEMBL 284 3 1 6 0.8 CN1CCN(c2nc(N)nc(Cc3ccccc3)n2)CC1 10.1016/j.ejmech.2017.04.033
CHEMBL4097856 158580 0 None -79 2 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]-histamine from human histamine H4R expressed in insect Sf9 cell membranes co-expressing Galphai2 and Gbeta1gamma2 after 60 mins by liquid scintillation counting methodDisplacement of [3H]-histamine from human histamine H4R expressed in insect Sf9 cell membranes co-expressing Galphai2 and Gbeta1gamma2 after 60 mins by liquid scintillation counting method
ChEMBL 284 3 1 6 0.8 CN1CCN(c2nc(N)nc(Cc3ccccc3)n2)CC1 10.1016/j.ejmech.2017.04.033
24826268 67709 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 331 3 2 6 2.8 CCN[C@@H]1CCN(c2nc(N)nc3c2oc2ccc(Cl)cc23)C1 10.1016/j.bmcl.2011.08.014
CHEMBL1914544 67709 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 331 3 2 6 2.8 CCN[C@@H]1CCN(c2nc(N)nc3c2oc2ccc(Cl)cc23)C1 10.1016/j.bmcl.2011.08.014
56851443 71284 0 None -7 2 Human 7.1 pKi = 7.1 Binding
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 356 7 2 3 4.6 c1ccc(CN/C(=N/C2CCCCC2)SCCCc2c[nH]cn2)cc1 10.1021/jm201042n
CHEMBL1923024 71284 0 None -7 2 Human 7.1 pKi = 7.1 Binding
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 356 7 2 3 4.6 c1ccc(CN/C(=N/C2CCCCC2)SCCCc2c[nH]cn2)cc1 10.1021/jm201042n
CHEMBL1963459 71284 0 None -7 2 Human 7.1 pKi = 7.1 Binding
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 356 7 2 3 4.6 c1ccc(CN/C(=N/C2CCCCC2)SCCCc2c[nH]cn2)cc1 10.1021/jm201042n
121238069 158580 0 None -79 2 Human 5.1 pKi = 5.1 Binding
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 284 3 1 6 0.8 CN1CCN(c2nc(N)nc(Cc3ccccc3)n2)CC1 10.1016/j.ejmech.2017.09.035
CHEMBL4097856 158580 0 None -79 2 Human 5.1 pKi = 5.1 Binding
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 284 3 1 6 0.8 CN1CCN(c2nc(N)nc(Cc3ccccc3)n2)CC1 10.1016/j.ejmech.2017.09.035
25178132 186356 0 None - 1 Human 6.1 pKi = 6.1 Binding
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 319 3 1 5 2.9 CC(C)Nc1nc(N2CCN(C)CC2)nc2ccc(Cl)cc12 10.1021/jm800876b
CHEMBL490073 186356 0 None - 1 Human 6.1 pKi = 6.1 Binding
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 319 3 1 5 2.9 CC(C)Nc1nc(N2CCN(C)CC2)nc2ccc(Cl)cc12 10.1021/jm800876b
25178132 186356 0 None - 1 Human 6.1 pKi = 6.1 Binding
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 319 3 1 5 2.9 CC(C)Nc1nc(N2CCN(C)CC2)nc2ccc(Cl)cc12 10.1021/jm901379s
CHEMBL490073 186356 0 None - 1 Human 6.1 pKi = 6.1 Binding
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 319 3 1 5 2.9 CC(C)Nc1nc(N2CCN(C)CC2)nc2ccc(Cl)cc12 10.1021/jm901379s
168283321 192293 0 None -6 4 Human 5.1 pKi = 5.1 Binding
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 192293 0 None -6 4 Human 5.1 pKi = 5.1 Binding
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 192293 0 None -6 4 Human 5.1 pKi = 5.1 Binding
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
24759622 169112 1 None - 1 Human 5.1 pKi = 5.1 Binding
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 228 1 0 4 1.4 CN1CCN(c2ncc3ccccc3n2)CC1 10.1021/jm800876b
CHEMBL443764 169112 1 None - 1 Human 5.1 pKi = 5.1 Binding
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 228 1 0 4 1.4 CN1CCN(c2ncc3ccccc3n2)CC1 10.1021/jm800876b
24759622 169112 1 None - 1 Human 5.1 pKi = 5.1 Binding
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 228 1 0 4 1.4 CN1CCN(c2ncc3ccccc3n2)CC1 10.1021/jm7014217
24759622 169112 1 None - 1 Human 5.1 pKi = 5.1 Binding
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 228 1 0 4 1.4 CN1CCN(c2ncc3ccccc3n2)CC1 10.1021/jm901379s
CHEMBL443764 169112 1 None - 1 Human 5.1 pKi = 5.1 Binding
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 228 1 0 4 1.4 CN1CCN(c2ncc3ccccc3n2)CC1 10.1021/jm7014217
CHEMBL443764 169112 1 None - 1 Human 5.1 pKi = 5.1 Binding
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 228 1 0 4 1.4 CN1CCN(c2ncc3ccccc3n2)CC1 10.1021/jm901379s
164622259 185148 0 None -7244 4 Human 4.1 pKi = 4.1 Binding
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 336 6 4 5 1.4 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCc1ccco1 10.1016/j.ejmech.2021.113190
CHEMBL4865965 185148 0 None -7244 4 Human 4.1 pKi = 4.1 Binding
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 336 6 4 5 1.4 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCc1ccco1 10.1016/j.ejmech.2021.113190
24826167 67804 0 None - 1 Human 7.1 pKi = 7.1 Binding
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
CHEMBL1914796 67804 0 None - 1 Human 7.1 pKi = 7.1 Binding
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
54581938 61203 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]histamine from human histamine H4 receptorDisplacement of [3H]histamine from human histamine H4 receptor
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 61203 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]histamine from human histamine H4 receptorDisplacement of [3H]histamine from human histamine H4 receptor
ChEMBL 261 3 2 5 1.1 CN[C@@H]1CCN(c2cc(N)nc(N3CCCC3)c2)C1 10.1016/j.bmcl.2011.03.017
46890019 7231 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
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 7231 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
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
24994945 109650 1 None - 1 Human 7.1 pKi = 7.1 Binding
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 207 2 2 5 0.2 CN[C@@H]1CCN(c2cc(C)nc(N)n2)C1 10.1021/jm401727m
CHEMBL3236567 109650 1 None - 1 Human 7.1 pKi = 7.1 Binding
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 207 2 2 5 0.2 CN[C@@H]1CCN(c2cc(C)nc(N)n2)C1 10.1021/jm401727m
1223 940 32 None -60 11 Human 7.1 pKi = 7.1 Binding
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 308 6 2 3 3.2 Clc1ccc(cc1)CN=C(SCCCc1cnc[nH]1)N 10.1021/acs.jmedchem.0c00160
2790 940 32 None -60 11 Human 7.1 pKi = 7.1 Binding
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 308 6 2 3 3.2 Clc1ccc(cc1)CN=C(SCCCc1cnc[nH]1)N 10.1021/acs.jmedchem.0c00160
CHEMBL14690 940 32 None -60 11 Human 7.1 pKi = 7.1 Binding
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 308 6 2 3 3.2 Clc1ccc(cc1)CN=C(SCCCc1cnc[nH]1)N 10.1021/acs.jmedchem.0c00160
51354301 58584 0 None -10 2 Human 6.1 pKi = 6.1 Binding
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 259 5 1 4 2.4 c1nc(CCn2cc(CC3CCCCC3)nn2)c[nH]1 10.1021/jm1013488
CHEMBL1688969 58584 0 None -10 2 Human 6.1 pKi = 6.1 Binding
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 259 5 1 4 2.4 c1nc(CCn2cc(CC3CCCCC3)nn2)c[nH]1 10.1021/jm1013488
164609017 183843 0 None -13 6 Human 6.1 pKi = 6.1 Binding
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 416 10 4 4 3.2 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCC(C)CCCc1ccccc1 10.1016/j.ejmech.2021.113190
CHEMBL4846201 183843 0 None -13 6 Human 6.1 pKi = 6.1 Binding
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 416 10 4 4 3.2 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCC(C)CCCc1ccccc1 10.1016/j.ejmech.2021.113190
168294166 192412 0 None -4 4 Human 5.1 pKi = 5.1 Binding
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 192412 0 None -4 4 Human 5.1 pKi = 5.1 Binding
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 192412 0 None -4 4 Human 5.1 pKi = 5.1 Binding
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
168294178 192433 0 None -5 4 Human 5.1 pKi = 5.1 Binding
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 192433 0 None -5 4 Human 5.1 pKi = 5.1 Binding
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 192433 0 None -5 4 Human 5.1 pKi = 5.1 Binding
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
127026019 136935 0 None -6 2 Human 5.1 pKi = 5.1 Binding
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 378 2 0 6 1.7 CN1CCN(c2nc3c(c(N4CCN(C)CC4)n2)-c2ccccc2CC3)CC1 10.1016/j.bmcl.2015.12.035
CHEMBL3753705 136935 0 None -6 2 Human 5.1 pKi = 5.1 Binding
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 378 2 0 6 1.7 CN1CCN(c2nc3c(c(N4CCN(C)CC4)n2)-c2ccccc2CC3)CC1 10.1016/j.bmcl.2015.12.035
11546127 95040 2 None - 1 Human 5.1 pKi = 5.1 Binding
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 95040 2 None - 1 Human 5.1 pKi = 5.1 Binding
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
10715823 5853 0 None -20 2 Human 6.1 pKi = 6.1 Binding
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 281 10 2 3 3.3 CCCCC(CC)CNC(=O)OCCCc1c[nH]cn1 10.1016/j.bmcl.2009.10.005
CHEMBL1079747 5853 0 None -20 2 Human 6.1 pKi = 6.1 Binding
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 281 10 2 3 3.3 CCCCC(CC)CNC(=O)OCCCc1c[nH]cn1 10.1016/j.bmcl.2009.10.005
1267 3744 43 None -33 25 Human 7.1 pKi = 7.1 Binding
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 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1016/j.bmcl.2011.10.104
3035905 3744 43 None -33 25 Human 7.1 pKi = 7.1 Binding
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 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1016/j.bmcl.2011.10.104
CHEMBL260374 3744 43 None -33 25 Human 7.1 pKi = 7.1 Binding
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 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1016/j.bmcl.2011.10.104
25071319 188474 8 None -9 2 Human 7.1 pKi = 7.1 Binding
Binding affinity to H4R receptorBinding affinity to H4R receptor
ChEMBL 295 1 2 5 1.6 Nc1nc2c(c(N3CCNCC3)n1)CCCc1ccccc1-2 10.1016/j.bmcl.2011.06.123
CHEMBL509540 188474 8 None -9 2 Human 7.1 pKi = 7.1 Binding
Binding affinity to H4R receptorBinding affinity to H4R receptor
ChEMBL 295 1 2 5 1.6 Nc1nc2c(c(N3CCNCC3)n1)CCCc1ccccc1-2 10.1016/j.bmcl.2011.06.123
25109291 190792 9 None -501 8 Human 7.1 pKi = 7.1 Binding
Binding affinity to H4R receptorBinding affinity to H4R receptor
ChEMBL 327 1 2 6 1.7 Nc1nc2c(c(N3CCNCC3)n1)CCC1=C2[C@@H]2CCCC[C@@H]2O1 10.1016/j.bmcl.2011.06.123
CHEMBL519240 190792 9 None -501 8 Human 7.1 pKi = 7.1 Binding
Binding affinity to H4R receptorBinding affinity to H4R receptor
ChEMBL 327 1 2 6 1.7 Nc1nc2c(c(N3CCNCC3)n1)CCC1=C2[C@@H]2CCCC[C@@H]2O1 10.1016/j.bmcl.2011.06.123
1204 1901 114 None -15 23 Mouse 7.1 pKi = 7.1 Binding
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 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmcl.2010.10.041
1247 1901 114 None -15 23 Mouse 7.1 pKi = 7.1 Binding
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 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmcl.2010.10.041
1375 1901 114 None -15 23 Mouse 7.1 pKi = 7.1 Binding
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 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmcl.2010.10.041
774 1901 114 None -15 23 Mouse 7.1 pKi = 7.1 Binding
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 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmcl.2010.10.041
CHEMBL90 1901 114 None -15 23 Mouse 7.1 pKi = 7.1 Binding
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 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmcl.2010.10.041
DB05381 1901 114 None -15 23 Mouse 7.1 pKi = 7.1 Binding
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 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmcl.2010.10.041
10446295 2101 29 None 269 2 Human 7.1 pKi = 7.1 Binding
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 278 1 1 3 1.6 CN1CCN(CC1)C(=O)c1nc2c([nH]1)cc(cc2)Cl 10.1016/j.bmcl.2004.08.035
1277 2101 29 None 269 2 Human 7.1 pKi = 7.1 Binding
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 278 1 1 3 1.6 CN1CCN(CC1)C(=O)c1nc2c([nH]1)cc(cc2)Cl 10.1016/j.bmcl.2004.08.035
CHEMBL185951 2101 29 None 269 2 Human 7.1 pKi = 7.1 Binding
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 278 1 1 3 1.6 CN1CCN(CC1)C(=O)c1nc2c([nH]1)cc(cc2)Cl 10.1016/j.bmcl.2004.08.035
1267 3744 43 None -21 25 Mouse 7.1 pKi = 7.1 Binding
Displacement of UR-DEBa176 from mouse recombinant H4R expressed in HEK293T-SF-His6-CRE-Luc cellsDisplacement of UR-DEBa176 from mouse recombinant H4R expressed in HEK293T-SF-His6-CRE-Luc cells
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1021/acs.jmedchem.0c00160
3035905 3744 43 None -21 25 Mouse 7.1 pKi = 7.1 Binding
Displacement of UR-DEBa176 from mouse recombinant H4R expressed in HEK293T-SF-His6-CRE-Luc cellsDisplacement of UR-DEBa176 from mouse recombinant H4R expressed in HEK293T-SF-His6-CRE-Luc cells
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1021/acs.jmedchem.0c00160
CHEMBL260374 3744 43 None -21 25 Mouse 7.1 pKi = 7.1 Binding
Displacement of UR-DEBa176 from mouse recombinant H4R expressed in HEK293T-SF-His6-CRE-Luc cellsDisplacement of UR-DEBa176 from mouse recombinant H4R expressed in HEK293T-SF-His6-CRE-Luc cells
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1021/acs.jmedchem.0c00160
937120 174529 8 None - 1 Human 7.1 pKi = 7.1 Binding
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 244 1 0 3 1.8 CN1CCN(C(=O)c2cc3ccccc3o2)CC1 10.1016/j.bmc.2020.115924
CHEMBL4568949 174529 8 None - 1 Human 7.1 pKi = 7.1 Binding
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 244 1 0 3 1.8 CN1CCN(C(=O)c2cc3ccccc3o2)CC1 10.1016/j.bmc.2020.115924
71681974 89219 0 None - 1 Human 7.1 pKi = 7.1 Binding
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(CCNc1cc(-c2ccccc2)nc(N)n1)c1ccnc(N)n1 10.1021/jm301886t
CHEMBL2375749 89219 0 None - 1 Human 7.1 pKi = 7.1 Binding
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(CCNc1cc(-c2ccccc2)nc(N)n1)c1ccnc(N)n1 10.1021/jm301886t
71681475 89225 0 None - 1 Human 7.1 pKi = 7.1 Binding
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 317 8 5 9 1.0 CC(C)CNc1cc(NCCNc2ccnc(N)n2)nc(N)n1 10.1021/jm301886t
CHEMBL2375755 89225 0 None - 1 Human 7.1 pKi = 7.1 Binding
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 317 8 5 9 1.0 CC(C)CNc1cc(NCCNc2ccnc(N)n2)nc(N)n1 10.1021/jm301886t
71681643 89236 0 None - 1 Human 7.1 pKi = 7.1 Binding
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 378 9 4 8 3.1 CC(C)CNc1nccc(NCCNc2cc(-c3ccccc3)nc(N)n2)n1 10.1021/jm301886t
CHEMBL2375766 89236 0 None - 1 Human 7.1 pKi = 7.1 Binding
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 378 9 4 8 3.1 CC(C)CNc1nccc(NCCNc2cc(-c3ccccc3)nc(N)n2)n1 10.1021/jm301886t
71681645 89238 0 None - 1 Human 7.1 pKi = 7.1 Binding
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)CNc1nccc(NCCNc2ccnc(N)n2)n1 10.1021/jm301886t
CHEMBL2375768 89238 0 None - 1 Human 7.1 pKi = 7.1 Binding
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)CNc1nccc(NCCNc2ccnc(N)n2)n1 10.1021/jm301886t
11679993 75664 0 None -25 2 Human 7.1 pKi = 7.1 Binding
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 195 7 2 2 2.0 CC(C)CNCCCCc1c[nH]cn1 10.1021/jm0504353
CHEMBL205559 75664 0 None -25 2 Human 7.1 pKi = 7.1 Binding
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 195 7 2 2 2.0 CC(C)CNCCCCc1c[nH]cn1 10.1021/jm0504353
11087453 75292 0 None - 1 Human 7.1 pKi = 7.1 Binding
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 288 2 1 4 1.5 CN1CCN(C(=O)c2cc3cc([N+](=O)[O-])ccc3[nH]2)CC1 10.1016/j.ejmech.2012.06.016
CHEMBL2047270 75292 0 None - 1 Human 7.1 pKi = 7.1 Binding
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 288 2 1 4 1.5 CN1CCN(C(=O)c2cc3cc([N+](=O)[O-])ccc3[nH]2)CC1 10.1016/j.ejmech.2012.06.016
66572113 75297 0 None - 1 Human 7.1 pKi = 7.1 Binding
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 1 2 3 1.1 CN1CCN(C(=O)c2cc3ccc(N)cc3[nH]2)CC1 10.1016/j.ejmech.2012.06.016
CHEMBL2047275 75297 0 None - 1 Human 7.1 pKi = 7.1 Binding
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 1 2 3 1.1 CN1CCN(C(=O)c2cc3ccc(N)cc3[nH]2)CC1 10.1016/j.ejmech.2012.06.016
66573457 75311 0 None - 1 Human 7.1 pKi = 7.1 Binding
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 283 2 1 2 2.4 Cc1cccc2cc(C(=O)N3CC(N4CCCC4)C3)[nH]c12 10.1016/j.ejmech.2012.06.016
CHEMBL2047446 75311 0 None - 1 Human 7.1 pKi = 7.1 Binding
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 283 2 1 2 2.4 Cc1cccc2cc(C(=O)N3CC(N4CCCC4)C3)[nH]c12 10.1016/j.ejmech.2012.06.016
70688340 75341 0 None - 1 Human 7.1 pKi = 7.1 Binding
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 279 1 1 2 1.8 CN1CCN(C(=O)c2cc3c(F)ccc(F)c3[nH]2)CC1 10.1016/j.ejmech.2012.06.016
CHEMBL2047476 75341 0 None - 1 Human 7.1 pKi = 7.1 Binding
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 279 1 1 2 1.8 CN1CCN(C(=O)c2cc3c(F)ccc(F)c3[nH]2)CC1 10.1016/j.ejmech.2012.06.016
51354875 58600 0 None - 1 Human 7.1 pKi = 7.1 Binding
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 6 1 4 2.8 c1nc(CCCc2cn(CC3CCCCC3)nn2)c[nH]1 10.1021/jm1013488
CHEMBL1688986 58600 0 None - 1 Human 7.1 pKi = 7.1 Binding
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 6 1 4 2.8 c1nc(CCCc2cn(CC3CCCCC3)nn2)c[nH]1 10.1021/jm1013488
25178937 186202 0 None - 1 Human 7.1 pKi = 7.1 Binding
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 291 2 1 5 2.1 CNc1nc(N2CCN(C)CC2)nc2ccc(Cl)cc12 10.1021/jm901379s
CHEMBL489062 186202 0 None - 1 Human 7.1 pKi = 7.1 Binding
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 291 2 1 5 2.1 CNc1nc(N2CCN(C)CC2)nc2ccc(Cl)cc12 10.1021/jm901379s
11846635 78270 0 None - 1 Human 7.1 pKi = 7.1 Binding
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 307 0 0 4 3.4 Cc1ccc2c(c1)Oc1ccccc1C(N1CCN(C)CC1)=N2 10.1021/jm051008s
CHEMBL211242 78270 0 None - 1 Human 7.1 pKi = 7.1 Binding
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 307 0 0 4 3.4 Cc1ccc2c(c1)Oc1ccccc1C(N1CCN(C)CC1)=N2 10.1021/jm051008s
4060730 19183 51 None - 1 Human 7.1 pKi = 7.1 Binding
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 243 1 1 2 1.6 CN1CCN(C(=O)c2cc3ccccc3[nH]2)CC1 10.1039/C2MD20212C
CHEMBL129199 19183 51 None - 1 Human 7.1 pKi = 7.1 Binding
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 243 1 1 2 1.6 CN1CCN(C(=O)c2cc3ccccc3[nH]2)CC1 10.1039/C2MD20212C
90645159 111694 0 None - 1 Human 6.1 pKi = 6.1 Binding
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 338 2 1 6 2.2 CN1CCN(c2nc(N)nc(-c3ccc(Cl)c(Cl)c3)n2)CC1 10.1016/j.ejmech.2014.06.032
CHEMBL3290586 111694 0 None - 1 Human 6.1 pKi = 6.1 Binding
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 338 2 1 6 2.2 CN1CCN(c2nc(N)nc(-c3ccc(Cl)c(Cl)c3)n2)CC1 10.1016/j.ejmech.2014.06.032
162671115 182365 0 None -1 2 Human 6.1 pKi = 6.1 Binding
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 266 2 0 3 1.9 CN1CCN(CC2Cc3cc(Cl)ccc3O2)CC1 10.1016/j.bmc.2020.115924
CHEMBL4792753 182365 0 None -1 2 Human 6.1 pKi = 6.1 Binding
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 266 2 0 3 1.9 CN1CCN(CC2Cc3cc(Cl)ccc3O2)CC1 10.1016/j.bmc.2020.115924
10197870 5229 0 None -3 2 Human 6.1 pKi = 6.1 Binding
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 167 2 2 3 0.6 NC[C@H]1CC[C@H](c2c[nH]cn2)O1 10.1016/j.bmcl.2010.10.041
CHEMBL106612 5229 0 None -3 2 Human 6.1 pKi = 6.1 Binding
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 167 2 2 3 0.6 NC[C@H]1CC[C@H](c2c[nH]cn2)O1 10.1016/j.bmcl.2010.10.041
91613 17804 31 None - 1 Human 6.1 pKi = 6.1 Binding
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 125 2 2 2 0.2 Cc1ncc(CCN)[nH]1 10.1016/j.bmcl.2010.10.041
CHEMBL12620 17804 31 None - 1 Human 6.1 pKi = 6.1 Binding
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 125 2 2 2 0.2 Cc1ncc(CCN)[nH]1 10.1016/j.bmcl.2010.10.041
71681474 89224 0 None - 1 Human 6.1 pKi = 6.1 Binding
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 246 5 4 8 -0.0 Nc1nccc(NCCNc2ccnc(N)n2)n1 10.1021/jm301886t
CHEMBL2375754 89224 0 None - 1 Human 6.1 pKi = 6.1 Binding
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 246 5 4 8 -0.0 Nc1nccc(NCCNc2ccnc(N)n2)n1 10.1021/jm301886t
11637064 74605 0 None -25 2 Human 6.1 pKi = 6.1 Binding
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 207 6 1 2 2.2 c1nc(CCCCCN2CCCC2)c[nH]1 10.1021/jm0504353
CHEMBL203228 74605 0 None -25 2 Human 6.1 pKi = 6.1 Binding
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 207 6 1 2 2.2 c1nc(CCCCCN2CCCC2)c[nH]1 10.1021/jm0504353
11708125 76166 3 None -251 2 Human 6.1 pKi = 6.1 Binding
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 5 1 2 1.3 CN(C)CCCCc1c[nH]cn1 10.1021/jm0504353
CHEMBL206000 76166 3 None -251 2 Human 6.1 pKi = 6.1 Binding
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 5 1 2 1.3 CN(C)CCCCc1c[nH]cn1 10.1021/jm0504353
11499376 137974 0 None -1 2 Human 6.1 pKi = 6.1 Binding
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 195 5 2 2 2.1 CC(C)(C)NCCCCc1c[nH]cn1 10.1021/jm0504353
CHEMBL377491 137974 0 None -1 2 Human 6.1 pKi = 6.1 Binding
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 195 5 2 2 2.1 CC(C)(C)NCCCCc1c[nH]cn1 10.1021/jm0504353
56672434 64793 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]histamine from human H4R receptor expressed in SK-N-MC cells at 10 uM after 1.5 hrs by liquid scintillation countingDisplacement of [3H]histamine from human H4R receptor expressed in SK-N-MC cells at 10 uM after 1.5 hrs by liquid scintillation counting
ChEMBL 261 1 1 2 3.3 CN1CCC(=Cc2nc3cc(Cl)ccc3[nH]2)CC1 10.1016/j.bmcl.2011.06.123
CHEMBL1824048 64793 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]histamine from human H4R receptor expressed in SK-N-MC cells at 10 uM after 1.5 hrs by liquid scintillation countingDisplacement of [3H]histamine from human H4R receptor expressed in SK-N-MC cells at 10 uM after 1.5 hrs by liquid scintillation counting
ChEMBL 261 1 1 2 3.3 CN1CCC(=Cc2nc3cc(Cl)ccc3[nH]2)CC1 10.1016/j.bmcl.2011.06.123
66572109 75289 0 None - 1 Human 6.1 pKi = 6.1 Binding
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 288 2 1 4 1.5 CN1CCN(C(=O)c2cc3c([N+](=O)[O-])cccc3[nH]2)CC1 10.1016/j.ejmech.2012.06.016
CHEMBL2047267 75289 0 None - 1 Human 6.1 pKi = 6.1 Binding
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 288 2 1 4 1.5 CN1CCN(C(=O)c2cc3c([N+](=O)[O-])cccc3[nH]2)CC1 10.1016/j.ejmech.2012.06.016
10957150 75306 0 None - 1 Human 6.1 pKi = 6.1 Binding
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 288 2 1 4 1.5 CN1CCN(C(=O)c2cc3cccc([N+](=O)[O-])c3[nH]2)CC1 10.1016/j.ejmech.2012.06.016
CHEMBL2047441 75306 0 None - 1 Human 6.1 pKi = 6.1 Binding
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 288 2 1 4 1.5 CN1CCN(C(=O)c2cc3cccc([N+](=O)[O-])c3[nH]2)CC1 10.1016/j.ejmech.2012.06.016
3939214 126124 7 None -1 2 Human 5.1 pKi = 5.1 Binding
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 262 1 1 1 3.4 O=C(c1cc2cc(Cl)ccc2[nH]1)N1CCCCC1 10.1016/j.bmcl.2004.08.035
CHEMBL365257 126124 7 None -1 2 Human 5.1 pKi = 5.1 Binding
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 262 1 1 1 3.4 O=C(c1cc2cc(Cl)ccc2[nH]1)N1CCCCC1 10.1016/j.bmcl.2004.08.035
11086114 7313 0 None -1 2 Human 5.1 pKi = 5.1 Binding
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 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 7313 0 None -1 2 Human 5.1 pKi = 5.1 Binding
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 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
2247 502 77 None -117 41 Human 5.1 pKi = 5.1 Binding
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 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 10.1016/j.bmcl.2011.09.001
249 502 77 None -117 41 Human 5.1 pKi = 5.1 Binding
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 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 10.1016/j.bmcl.2011.09.001
2603 502 77 None -117 41 Human 5.1 pKi = 5.1 Binding
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 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 10.1016/j.bmcl.2011.09.001
CHEMBL296419 502 77 None -117 41 Human 5.1 pKi = 5.1 Binding
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 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 10.1016/j.bmcl.2011.09.001
DB00637 502 77 None -117 41 Human 5.1 pKi = 5.1 Binding
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 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 10.1016/j.bmcl.2011.09.001
44417471 12662 0 None - 1 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]histamine from human histamine H4 receptorDisplacement of [3H]histamine from human histamine H4 receptor
ChEMBL 175 4 5 3 -0.5 N=C(N)NCCCSC(=N)N 10.1021/jm060880d
CHEMBL1187948 12662 0 None - 1 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]histamine from human histamine H4 receptorDisplacement of [3H]histamine from human histamine H4 receptor
ChEMBL 175 4 5 3 -0.5 N=C(N)NCCCSC(=N)N 10.1021/jm060880d
CHEMBL534496 12662 0 None - 1 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]histamine from human histamine H4 receptorDisplacement of [3H]histamine from human histamine H4 receptor
ChEMBL 175 4 5 3 -0.5 N=C(N)NCCCSC(=N)N 10.1021/jm060880d
164614841 184692 0 None -223 4 Human 5.1 pKi = 5.1 Binding
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 388 7 4 4 3.0 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NC(c1ccccc1)C(C)C 10.1016/j.ejmech.2021.113190
CHEMBL4858849 184692 0 None -223 4 Human 5.1 pKi = 5.1 Binding
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 388 7 4 4 3.0 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NC(c1ccccc1)C(C)C 10.1016/j.ejmech.2021.113190
9923162 18751 5 None 199 2 Human 8.1 pKi = 8.1 Binding
Antagonist activity at Homo sapiens (human) histamine H4 receptorAntagonist activity at Homo sapiens (human) histamine H4 receptor
ChEMBL 321 1 1 2 2.3 CN1CCN(C(=O)c2cc3cc(Br)ccc3[nH]2)CC1 10.1007/s00044-004-0106-7
CHEMBL128613 18751 5 None 199 2 Human 8.1 pKi = 8.1 Binding
Antagonist activity at Homo sapiens (human) histamine H4 receptorAntagonist activity at Homo sapiens (human) histamine H4 receptor
ChEMBL 321 1 1 2 2.3 CN1CCN(C(=O)c2cc3cc(Br)ccc3[nH]2)CC1 10.1007/s00044-004-0106-7
10967174 19242 3 None -2 2 Human 8.1 pKi = 8.1 Binding
Antagonist activity at Homo sapiens (human) histamine H4 receptorAntagonist activity at Homo sapiens (human) histamine H4 receptor
ChEMBL 258 1 2 3 1.1 CN1CCN(C(=O)c2cc3cccc(N)c3[nH]2)CC1 10.1007/s00044-004-0106-7
CHEMBL129540 19242 3 None -2 2 Human 8.1 pKi = 8.1 Binding
Antagonist activity at Homo sapiens (human) histamine H4 receptorAntagonist activity at Homo sapiens (human) histamine H4 receptor
ChEMBL 258 1 2 3 1.1 CN1CCN(C(=O)c2cc3cccc(N)c3[nH]2)CC1 10.1007/s00044-004-0106-7
1204 1901 114 None -3 23 Human 8.1 pKi = 8.1 Binding
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 10.1021/acs.jmedchem.5b00516
1247 1901 114 None -3 23 Human 8.1 pKi = 8.1 Binding
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 10.1021/acs.jmedchem.5b00516
1375 1901 114 None -3 23 Human 8.1 pKi = 8.1 Binding
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 10.1021/acs.jmedchem.5b00516
774 1901 114 None -3 23 Human 8.1 pKi = 8.1 Binding
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 10.1021/acs.jmedchem.5b00516
CHEMBL90 1901 114 None -3 23 Human 8.1 pKi = 8.1 Binding
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 10.1021/acs.jmedchem.5b00516
DB05381 1901 114 None -3 23 Human 8.1 pKi = 8.1 Binding
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 10.1021/acs.jmedchem.5b00516
9923162 18751 5 None 199 2 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]- histamine from the recombinant human histamine H4 receptorDisplacement of [3H]- histamine from the recombinant human histamine H4 receptor
ChEMBL 321 1 1 2 2.3 CN1CCN(C(=O)c2cc3cc(Br)ccc3[nH]2)CC1 10.1021/jm0341047
CHEMBL128613 18751 5 None 199 2 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]- histamine from the recombinant human histamine H4 receptorDisplacement of [3H]- histamine from the recombinant human histamine H4 receptor
ChEMBL 321 1 1 2 2.3 CN1CCN(C(=O)c2cc3cc(Br)ccc3[nH]2)CC1 10.1021/jm0341047
10967174 19242 3 None -2 2 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]- histamine from the recombinant human histamine H4 receptorDisplacement of [3H]- histamine from the recombinant human histamine H4 receptor
ChEMBL 258 1 2 3 1.1 CN1CCN(C(=O)c2cc3cccc(N)c3[nH]2)CC1 10.1021/jm0341047
CHEMBL129540 19242 3 None -2 2 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]- histamine from the recombinant human histamine H4 receptorDisplacement of [3H]- histamine from the recombinant human histamine H4 receptor
ChEMBL 258 1 2 3 1.1 CN1CCN(C(=O)c2cc3cccc(N)c3[nH]2)CC1 10.1021/jm0341047
1278 2119 79 None -3 8 Human 8.1 pKi = 8.1 Binding
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 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1016/j.bmcl.2011.07.125
1279 2119 79 None -3 8 Human 8.1 pKi = 8.1 Binding
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 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1016/j.bmcl.2011.07.125
4908365 2119 79 None -3 8 Human 8.1 pKi = 8.1 Binding
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 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1016/j.bmcl.2011.07.125
CHEMBL129198 2119 79 None -3 8 Human 8.1 pKi = 8.1 Binding
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 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1016/j.bmcl.2011.07.125
54580746 61062 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]histamine from human histamine H4 receptorDisplacement of [3H]histamine from human histamine H4 receptor
ChEMBL 248 2 2 6 0.1 Nc1nc(N2CCCC2)cc(N2CCNCC2)n1 10.1016/j.bmcl.2011.03.017
CHEMBL1770160 61062 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]histamine from human histamine H4 receptorDisplacement of [3H]histamine from human histamine H4 receptor
ChEMBL 248 2 2 6 0.1 Nc1nc(N2CCCC2)cc(N2CCNCC2)n1 10.1016/j.bmcl.2011.03.017
1278 2119 79 None -3 8 Human 8.1 pKi = 8.1 Binding
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 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1016/j.bmcl.2011.07.114
1279 2119 79 None -3 8 Human 8.1 pKi = 8.1 Binding
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 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1016/j.bmcl.2011.07.114
4908365 2119 79 None -3 8 Human 8.1 pKi = 8.1 Binding
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 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1016/j.bmcl.2011.07.114
CHEMBL129198 2119 79 None -3 8 Human 8.1 pKi = 8.1 Binding
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 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1016/j.bmcl.2011.07.114
58227157 115417 0 None - 1 Human 8.1 pKi = 8.1 Binding
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
CHEMBL3354815 115417 0 None - 1 Human 8.1 pKi = 8.1 Binding
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
58227179 116632 0 None - 1 Human 8.1 pKi = 8.1 Binding
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
CHEMBL3393548 116632 0 None - 1 Human 8.1 pKi = 8.1 Binding
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
58227259 116640 0 None - 1 Human 8.1 pKi = 8.1 Binding
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(c2cnnc(NC3CC4CCC3C4)c2)C1 10.1016/j.bmcl.2014.12.027
CHEMBL3393556 116640 0 None - 1 Human 8.1 pKi = 8.1 Binding
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(c2cnnc(NC3CC4CCC3C4)c2)C1 10.1016/j.bmcl.2014.12.027
1278 2119 79 None -3 8 Human 8.1 pKi = 8.1 Binding
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 2119 79 None -3 8 Human 8.1 pKi = 8.1 Binding
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 2119 79 None -3 8 Human 8.1 pKi = 8.1 Binding
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 2119 79 None -3 8 Human 8.1 pKi = 8.1 Binding
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
42624150 109660 0 None - 1 Human 8.1 pKi = 8.1 Binding
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 2 2 5 1.2 CN[C@@H]1CCN(c2cc(C(C)(C)C)nc(N)n2)C1 10.1021/jm401727m
CHEMBL3236577 109660 0 None - 1 Human 8.1 pKi = 8.1 Binding
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 2 2 5 1.2 CN[C@@H]1CCN(c2cc(C(C)(C)C)nc(N)n2)C1 10.1021/jm401727m
24827129 67793 0 None - 1 Human 8.1 pKi = 8.1 Binding
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)nc3c2oc2c(Cl)cc(Cl)cc23)C1 10.1016/j.bmcl.2011.08.014
CHEMBL1914785 67793 0 None - 1 Human 8.1 pKi = 8.1 Binding
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)nc3c2oc2c(Cl)cc(Cl)cc23)C1 10.1016/j.bmcl.2011.08.014
9923162 18751 5 None 199 2 Human 8.1 pKi = 8.1 Binding
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 321 1 1 2 2.3 CN1CCN(C(=O)c2cc3cc(Br)ccc3[nH]2)CC1 10.1021/jm0502081
CHEMBL128613 18751 5 None 199 2 Human 8.1 pKi = 8.1 Binding
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 321 1 1 2 2.3 CN1CCN(C(=O)c2cc3cc(Br)ccc3[nH]2)CC1 10.1021/jm0502081
10967174 19242 3 None -2 2 Human 8.1 pKi = 8.1 Binding
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 258 1 2 3 1.1 CN1CCN(C(=O)c2cc3cccc(N)c3[nH]2)CC1 10.1021/jm0502081
CHEMBL129540 19242 3 None -2 2 Human 8.1 pKi = 8.1 Binding
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 258 1 2 3 1.1 CN1CCN(C(=O)c2cc3cccc(N)c3[nH]2)CC1 10.1021/jm0502081
44129212 197772 0 None - 1 Human 8.1 pKi = 8.1 Binding
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 3.3 CN1CCN(c2nc(NCCS(=O)(=O)Nc3ccccc3)c3c(C(F)(F)F)cccc3n2)CC1 10.1021/jm901379s
CHEMBL591496 197772 0 None - 1 Human 8.1 pKi = 8.1 Binding
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 3.3 CN1CCN(c2nc(NCCS(=O)(=O)Nc3ccccc3)c3c(C(F)(F)F)cccc3n2)CC1 10.1021/jm901379s
24825522 187060 0 None -6 3 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in CHO cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in CHO cells
ChEMBL 283 3 1 3 3.3 CC1CC(C)(C)N=C(c2cccc(Cc3c[nH]cn3)c2)O1 10.1021/jm7014149
CHEMBL494982 187060 0 None -6 3 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in CHO cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in CHO cells
ChEMBL 283 3 1 3 3.3 CC1CC(C)(C)N=C(c2cccc(Cc3c[nH]cn3)c2)O1 10.1021/jm7014149
51354300 58581 0 None 15 2 Human 8.1 pKi = 8.1 Binding
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 6 1 4 2.8 c1nc(CCCn2cc(CC3CCCCC3)nn2)c[nH]1 10.1021/jm1013488
CHEMBL1688946 58581 0 None 15 2 Human 8.1 pKi = 8.1 Binding
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 6 1 4 2.8 c1nc(CCCn2cc(CC3CCCCC3)nn2)c[nH]1 10.1021/jm1013488
58227373 175934 0 None 1 2 Human 8.1 pKi = 8.1 Binding
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 249 3 2 5 1.5 CC(C)(C)CNc1nccc(N2CC[C@@H](N)C2)n1 10.1021/acs.jmedchem.9b01342
CHEMBL4455324 175934 0 None 1 2 Human 8.1 pKi = 8.1 Binding
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 249 3 2 5 1.5 CC(C)(C)CNc1nccc(N2CC[C@@H](N)C2)n1 10.1021/acs.jmedchem.9b01342
CHEMBL4596881 175934 0 None 1 2 Human 8.1 pKi = 8.1 Binding
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 249 3 2 5 1.5 CC(C)(C)CNc1nccc(N2CC[C@@H](N)C2)n1 10.1021/acs.jmedchem.9b01342
168294182 192446 0 None -5 4 Human 8.1 pKi = 8.1 Binding
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 192446 0 None -5 4 Human 8.1 pKi = 8.1 Binding
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 192446 0 None -5 4 Human 8.1 pKi = 8.1 Binding
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
46890546 6437 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
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 6437 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
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
46228069 198466 0 None - 1 Human 5.1 pKi = 5.1 Binding
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 323 3 1 7 1.2 CN1CCN(c2nc(N)nc3c2ncn3Cc2ccccc2)CC1 10.1016/j.bmc.2009.08.059
CHEMBL596348 198466 0 None - 1 Human 5.1 pKi = 5.1 Binding
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 323 3 1 7 1.2 CN1CCN(c2nc(N)nc3c2ncn3Cc2ccccc2)CC1 10.1016/j.bmc.2009.08.059
63868172 175482 2 None - 1 Human 6.1 pKi = 6.1 Binding
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 222 2 1 6 -0.2 CCc1nc(N)nc(N2CCN(C)CC2)n1 10.1016/j.bmc.2019.02.020
CHEMBL4590628 175482 2 None - 1 Human 6.1 pKi = 6.1 Binding
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 222 2 1 6 -0.2 CCc1nc(N)nc(N2CCN(C)CC2)n1 10.1016/j.bmc.2019.02.020
164614549 184360 0 None -575 6 Human 5.1 pKi = 5.1 Binding
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 340 9 4 4 2.2 CCCCCCNC(=O)/N=C(\N)NCCCc1sc(N)nc1C 10.1016/j.ejmech.2021.113190
CHEMBL4853668 184360 0 None -575 6 Human 5.1 pKi = 5.1 Binding
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 340 9 4 4 2.2 CCCCCCNC(=O)/N=C(\N)NCCCc1sc(N)nc1C 10.1016/j.ejmech.2021.113190
164621681 184998 0 None -64 4 Human 5.1 pKi = 5.1 Binding
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 444 7 4 5 3.2 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NC(C)c1ccc(OC(F)(F)F)cc1 10.1016/j.ejmech.2021.113190
CHEMBL4863523 184998 0 None -64 4 Human 5.1 pKi = 5.1 Binding
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 444 7 4 5 3.2 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NC(C)c1ccc(OC(F)(F)F)cc1 10.1016/j.ejmech.2021.113190
164627241 185847 0 None -269 4 Human 5.1 pKi = 5.1 Binding
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 438 6 4 4 3.1 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NC(C)c1ccc(Br)cc1 10.1016/j.ejmech.2021.113190
CHEMBL4876267 185847 0 None -269 4 Human 5.1 pKi = 5.1 Binding
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 438 6 4 4 3.1 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NC(C)c1ccc(Br)cc1 10.1016/j.ejmech.2021.113190
11086114 7313 0 None -1 2 Human 5.1 pKi = 5.1 Binding
Histamine H4 receptor competition binding using [3H]Na-methylhistamineHistamine H4 receptor competition binding using [3H]Na-methylhistamine
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 7313 0 None -1 2 Human 5.1 pKi = 5.1 Binding
Histamine H4 receptor competition binding using [3H]Na-methylhistamineHistamine H4 receptor competition binding using [3H]Na-methylhistamine
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
71519347 86062 0 None - 1 Human 5.1 pKi = 5.1 Binding
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 274 4 2 6 1.2 CCCCn1ccc2c(N3CCNCC3)nc(N)nc21 10.1016/j.bmcl.2012.10.139
CHEMBL2314765 86062 0 None - 1 Human 5.1 pKi = 5.1 Binding
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 274 4 2 6 1.2 CCCCn1ccc2c(N3CCNCC3)nc(N)nc21 10.1016/j.bmcl.2012.10.139
54754351 67875 0 None 10 3 Human 7.1 pKi = 7.1 Binding
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 277 4 1 5 2.1 CN1CCN(c2cc(NCCC(C)(C)C)ncn2)CC1 10.1016/j.bmcl.2011.07.125
CHEMBL1915535 67875 0 None 10 3 Human 7.1 pKi = 7.1 Binding
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 277 4 1 5 2.1 CN1CCN(c2cc(NCCC(C)(C)C)ncn2)CC1 10.1016/j.bmcl.2011.07.125
54754351 67875 0 None 10 3 Human 7.1 pKi = 7.1 Binding
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 277 4 1 5 2.1 CN1CCN(c2cc(NCCC(C)(C)C)ncn2)CC1 10.1016/j.bmcl.2011.07.114
CHEMBL1915535 67875 0 None 10 3 Human 7.1 pKi = 7.1 Binding
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 277 4 1 5 2.1 CN1CCN(c2cc(NCCC(C)(C)C)ncn2)CC1 10.1016/j.bmcl.2011.07.114
58227242 116636 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 261 3 1 5 1.6 CN1CCN(c2cnnc(NC3CCCC3)c2)CC1 10.1016/j.bmcl.2014.12.027
CHEMBL3393552 116636 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 261 3 1 5 1.6 CN1CCN(c2cnnc(NC3CCCC3)c2)CC1 10.1016/j.bmcl.2014.12.027
121238067 166558 0 None - 1 Human 5.1 pKi = 5.1 Binding
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 250 3 1 6 0.4 CC(C)Cc1nc(N)nc(N2CCN(C)CC2)n1 10.1016/j.ejmech.2017.09.035
CHEMBL4290148 166558 0 None - 1 Human 5.1 pKi = 5.1 Binding
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 250 3 1 6 0.4 CC(C)Cc1nc(N)nc(N2CCN(C)CC2)n1 10.1016/j.ejmech.2017.09.035
57400778 67868 0 None 199 2 Human 7.1 pKi = 7.1 Binding
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 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 67868 0 None 199 2 Human 7.1 pKi = 7.1 Binding
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 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
54584827 61227 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]histamine from human histamine H4 receptorDisplacement of [3H]histamine from human histamine H4 receptor
ChEMBL 262 3 2 6 0.5 CN[C@H]1CCN(c2cc(N3CCCC3)nc(N)n2)C1 10.1016/j.bmcl.2011.03.017
CHEMBL1770996 61227 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]histamine from human histamine H4 receptorDisplacement of [3H]histamine from human histamine H4 receptor
ChEMBL 262 3 2 6 0.5 CN[C@H]1CCN(c2cc(N3CCCC3)nc(N)n2)C1 10.1016/j.bmcl.2011.03.017
57400778 67868 0 None 199 2 Human 7.1 pKi = 7.1 Binding
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 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 67868 0 None 199 2 Human 7.1 pKi = 7.1 Binding
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 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
57400589 69565 0 None - 1 Human 7.1 pKi = 7.1 Binding
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 304 1 1 3 1.9 CN1C[C@H]2CN(C(=O)c3cc4cc(Cl)cnc4[nH]3)C[C@H]2C1 10.1016/j.bmcl.2011.11.098
CHEMBL1938972 69565 0 None - 1 Human 7.1 pKi = 7.1 Binding
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 304 1 1 3 1.9 CN1C[C@H]2CN(C(=O)c3cc4cc(Cl)cnc4[nH]3)C[C@H]2C1 10.1016/j.bmcl.2011.11.098
90645164 111699 0 None - 1 Human 6.1 pKi = 6.1 Binding
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 Cc1ccc(-c2nc(N)nc(N3CCN(C)CC3)n2)cc1C 10.1016/j.ejmech.2014.06.032
CHEMBL3290591 111699 0 None - 1 Human 6.1 pKi = 6.1 Binding
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 Cc1ccc(-c2nc(N)nc(N3CCN(C)CC3)n2)cc1C 10.1016/j.ejmech.2014.06.032
57399016 67834 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 331 1 2 6 2.6 Nc1nc(N2C[C@@H]3C[C@H]2CN3)c2sc3ccc(Cl)cc3c2n1 10.1016/j.bmcl.2011.08.014
CHEMBL1915040 67834 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 331 1 2 6 2.6 Nc1nc(N2C[C@@H]3C[C@H]2CN3)c2sc3ccc(Cl)cc3c2n1 10.1016/j.bmcl.2011.08.014
46890548 6506 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
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 6506 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
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
46929551 16565 0 None -52 2 Human 6.1 pKi = 6.1 Binding
Binding affinity to human histamine H4 receptorBinding affinity to human histamine H4 receptor
ChEMBL 337 5 1 3 5.0 CC(C)(C)c1ccc(SCC(c2ccccn2)c2c[nH]cn2)cc1 10.1021/jm100643t
CHEMBL1243335 16565 0 None -52 2 Human 6.1 pKi = 6.1 Binding
Binding affinity to human histamine H4 receptorBinding affinity to human histamine H4 receptor
ChEMBL 337 5 1 3 5.0 CC(C)(C)c1ccc(SCC(c2ccccn2)c2c[nH]cn2)cc1 10.1021/jm100643t
5159263 10285 11 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in SK-NM-C cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in SK-NM-C cells
ChEMBL 259 4 3 4 0.8 Cc1cc(C)nc(N/C(N)=N/CCc2c[nH]cn2)n1 10.1021/jm7014777
CHEMBL1162351 10285 11 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in SK-NM-C cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in SK-NM-C cells
ChEMBL 259 4 3 4 0.8 Cc1cc(C)nc(N/C(N)=N/CCc2c[nH]cn2)n1 10.1021/jm7014777
71525679 89296 0 None -6 6 Mouse 7.1 pKi = 7.1 Binding
Binding affinity to mouse histamine H4 receptorBinding affinity to mouse histamine H4 receptor
ChEMBL 272 3 2 6 1.0 CCc1cnc2c(N3CC[C@@H](NC)C3)nc(N)nc2c1 10.1016/j.bmcl.2013.02.091
CHEMBL2376801 89296 0 None -6 6 Mouse 7.1 pKi = 7.1 Binding
Binding affinity to mouse histamine H4 receptorBinding affinity to mouse histamine H4 receptor
ChEMBL 272 3 2 6 1.0 CCc1cnc2c(N3CC[C@@H](NC)C3)nc(N)nc2c1 10.1016/j.bmcl.2013.02.091
25178130 189153 2 None - 1 Human 5.1 pKi = 5.1 Binding
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 319 3 1 5 3.1 CN1CCN(c2nc(Nc3ccccc3)c3ccccc3n2)CC1 10.1021/jm800876b
CHEMBL515870 189153 2 None - 1 Human 5.1 pKi = 5.1 Binding
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 319 3 1 5 3.1 CN1CCN(c2nc(Nc3ccccc3)c3ccccc3n2)CC1 10.1021/jm800876b
25178130 189153 2 None - 1 Human 5.1 pKi = 5.1 Binding
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 319 3 1 5 3.1 CN1CCN(c2nc(Nc3ccccc3)c3ccccc3n2)CC1 10.1021/jm901379s
CHEMBL515870 189153 2 None - 1 Human 5.1 pKi = 5.1 Binding
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 319 3 1 5 3.1 CN1CCN(c2nc(Nc3ccccc3)c3ccccc3n2)CC1 10.1021/jm901379s
164622153 184986 0 None -181 4 Human 5.1 pKi = 5.1 Binding
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 394 6 4 4 3.0 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NC(C)c1ccc(Cl)cc1 10.1016/j.ejmech.2021.113190
CHEMBL4863347 184986 0 None -181 4 Human 5.1 pKi = 5.1 Binding
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 394 6 4 4 3.0 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NC(C)c1ccc(Cl)cc1 10.1016/j.ejmech.2021.113190
54581939 61215 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]histamine from human histamine H4 receptorDisplacement of [3H]histamine from human histamine H4 receptor
ChEMBL 264 3 1 6 0.7 CC(C)N(C)c1nc(N)cc(N2CCN(C)CC2)n1 10.1016/j.bmcl.2011.03.017
CHEMBL1770984 61215 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]histamine from human histamine H4 receptorDisplacement of [3H]histamine from human histamine H4 receptor
ChEMBL 264 3 1 6 0.7 CC(C)N(C)c1nc(N)cc(N2CCN(C)CC2)n1 10.1016/j.bmcl.2011.03.017
122193095 123396 0 None -3 2 Mouse 6.1 pKi = 6.1 Binding
Displacement of [3H]histamine from mouse H4 receptor expressed in HEK293 cell membranes co-expressing Galphai2 and Gbeta1gamma2 after 1 hr by liquid scintillation counting assayDisplacement of [3H]histamine from mouse H4 receptor expressed in HEK293 cell membranes co-expressing Galphai2 and Gbeta1gamma2 after 1 hr by liquid scintillation counting assay
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 123396 0 None -3 2 Mouse 6.1 pKi = 6.1 Binding
Displacement of [3H]histamine from mouse H4 receptor expressed in HEK293 cell membranes co-expressing Galphai2 and Gbeta1gamma2 after 1 hr by liquid scintillation counting assayDisplacement of [3H]histamine from mouse H4 receptor expressed in HEK293 cell membranes co-expressing Galphai2 and Gbeta1gamma2 after 1 hr by liquid scintillation counting assay
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
58227260 116630 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 287 3 1 5 1.8 CN1CCN(c2ccnc(NC3CC4CCC3C4)n2)CC1 10.1016/j.bmcl.2014.12.027
CHEMBL3393546 116630 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 287 3 1 5 1.8 CN1CCN(c2ccnc(NC3CC4CCC3C4)n2)CC1 10.1016/j.bmcl.2014.12.027
57398176 67986 0 None - 1 Human 6.1 pKi = 6.1 Binding
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 273 2 0 5 1.4 CN1CCN(c2cc(N3[C@@H]4CCC[C@@H]3C4)ncn2)CC1 10.1016/j.bmcl.2011.07.114
CHEMBL1916503 67986 0 None - 1 Human 6.1 pKi = 6.1 Binding
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 273 2 0 5 1.4 CN1CCN(c2cc(N3[C@@H]4CCC[C@@H]3C4)ncn2)CC1 10.1016/j.bmcl.2011.07.114
127050776 139717 0 None 6 2 Human 6.1 pKi = 6.1 Binding
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
CHEMBL3805437 139717 0 None 6 2 Human 6.1 pKi = 6.1 Binding
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
164627189 185739 0 None -831 4 Human 4.1 pKi = 4.1 Binding
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 298 6 4 4 1.0 CCCNC(=O)/N=C(\N)NCCCc1sc(N)nc1C 10.1016/j.ejmech.2021.113190
CHEMBL4874758 185739 0 None -831 4 Human 4.1 pKi = 4.1 Binding
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 298 6 4 4 1.0 CCCNC(=O)/N=C(\N)NCCCc1sc(N)nc1C 10.1016/j.ejmech.2021.113190
71519015 86041 0 None - 1 Human 5.1 pKi = 5.1 Binding
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 246 1 2 5 0.7 CN1CCCN(c2nc(N)nc3[nH]ccc23)CC1 10.1016/j.bmcl.2012.10.139
CHEMBL2314500 86041 0 None - 1 Human 5.1 pKi = 5.1 Binding
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 246 1 2 5 0.7 CN1CCCN(c2nc(N)nc3[nH]ccc23)CC1 10.1016/j.bmcl.2012.10.139
57400737 67836 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 331 1 2 6 2.6 Nc1nc(N2C[C@@H]3C[C@H]2CN3)c2sc3cc(Cl)ccc3c2n1 10.1016/j.bmcl.2011.08.014
CHEMBL1915042 67836 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 331 1 2 6 2.6 Nc1nc(N2C[C@@H]3C[C@H]2CN3)c2sc3cc(Cl)ccc3c2n1 10.1016/j.bmcl.2011.08.014
57395494 67830 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 349 1 2 6 2.5 Nc1nc(N2C[C@@H]3C[C@H]2CN3)c2oc3cccc(C(F)(F)F)c3c2n1 10.1016/j.bmcl.2011.08.014
CHEMBL1915032 67830 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 349 1 2 6 2.5 Nc1nc(N2C[C@@H]3C[C@H]2CN3)c2oc3cccc(C(F)(F)F)c3c2n1 10.1016/j.bmcl.2011.08.014
57395499 67839 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 318 1 2 7 1.8 C[C@H]1CN(c2nc(N)nc3c2oc2ncc(Cl)cc23)CCN1 10.1016/j.bmcl.2011.08.014
CHEMBL1915046 67839 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 318 1 2 7 1.8 C[C@H]1CN(c2nc(N)nc3c2oc2ncc(Cl)cc23)CCN1 10.1016/j.bmcl.2011.08.014
46890677 7210 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
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 7210 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
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
56851612 71257 0 None -19 2 Human 7.1 pKi = 7.1 Binding
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 398 9 2 3 5.3 CCCCN/C(=N/Cc1ccc(Cl)c(Cl)c1)SCCCc1c[nH]cn1 10.1021/jm201042n
CHEMBL1923032 71257 0 None -19 2 Human 7.1 pKi = 7.1 Binding
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 398 9 2 3 5.3 CCCCN/C(=N/Cc1ccc(Cl)c(Cl)c1)SCCCc1c[nH]cn1 10.1021/jm201042n
CHEMBL1963245 71257 0 None -19 2 Human 7.1 pKi = 7.1 Binding
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 398 9 2 3 5.3 CCCCN/C(=N/Cc1ccc(Cl)c(Cl)c1)SCCCc1c[nH]cn1 10.1021/jm201042n
56851602 71259 0 None -18 2 Human 7.1 pKi = 7.1 Binding
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 364 9 2 3 4.7 CCCCN/C(=N/Cc1ccc(Cl)cc1)SCCCc1c[nH]cn1 10.1021/jm201042n
CHEMBL1923027 71259 0 None -18 2 Human 7.1 pKi = 7.1 Binding
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 364 9 2 3 4.7 CCCCN/C(=N/Cc1ccc(Cl)cc1)SCCCc1c[nH]cn1 10.1021/jm201042n
CHEMBL1963260 71259 0 None -18 2 Human 7.1 pKi = 7.1 Binding
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 364 9 2 3 4.7 CCCCN/C(=N/Cc1ccc(Cl)cc1)SCCCc1c[nH]cn1 10.1021/jm201042n
25178345 172874 0 None - 1 Human 7.1 pKi = 7.1 Binding
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 357 4 1 6 3.2 CN1CCN(c2nc(NCc3ccco3)c3cc(Cl)ccc3n2)CC1 10.1021/jm800876b
CHEMBL452925 172874 0 None - 1 Human 7.1 pKi = 7.1 Binding
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 357 4 1 6 3.2 CN1CCN(c2nc(NCc3ccco3)c3cc(Cl)ccc3n2)CC1 10.1021/jm800876b
51354303 58587 0 None -1 2 Human 7.1 pKi = 7.1 Binding
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 259 5 1 4 2.7 c1nc(CCCn2cc(C3CCCCC3)nn2)c[nH]1 10.1021/jm1013488
CHEMBL1688971 58587 0 None -1 2 Human 7.1 pKi = 7.1 Binding
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 259 5 1 4 2.7 c1nc(CCCn2cc(C3CCCCC3)nn2)c[nH]1 10.1021/jm1013488
25147771 173666 0 None -1 3 Human 7.1 pKi = 7.1 Binding
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 357 4 1 6 3.2 CN1CCN(c2nc(NCc3ccoc3)c3cc(Cl)ccc3n2)CC1 10.1021/jm901379s
CHEMBL454890 173666 0 None -1 3 Human 7.1 pKi = 7.1 Binding
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 357 4 1 6 3.2 CN1CCN(c2nc(NCc3ccoc3)c3cc(Cl)ccc3n2)CC1 10.1021/jm901379s
10656971 16244 4 None - 1 Human 6.1 pKi = 6.1 Binding
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 228 1 0 4 1.4 CN1CCN(c2cnc3ccccc3n2)CC1 10.1021/jm7014217
CHEMBL123137 16244 4 None - 1 Human 6.1 pKi = 6.1 Binding
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 228 1 0 4 1.4 CN1CCN(c2cnc3ccccc3n2)CC1 10.1021/jm7014217
25179123 188511 0 None - 1 Human 6.1 pKi = 6.1 Binding
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 363 5 1 7 2.0 CCOC(=O)CNc1nc(N2CCN(C)CC2)nc2ccc(Cl)cc12 10.1021/jm901379s
CHEMBL510181 188511 0 None - 1 Human 6.1 pKi = 6.1 Binding
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 363 5 1 7 2.0 CCOC(=O)CNc1nc(N2CCN(C)CC2)nc2ccc(Cl)cc12 10.1021/jm901379s
10197870 5229 0 None -3 2 Human 6.1 pKi = 6.1 Binding
Histamine H4 receptor competition binding using [3H]Na-methylhistamineHistamine H4 receptor competition binding using [3H]Na-methylhistamine
ChEMBL 167 2 2 3 0.6 NC[C@H]1CC[C@H](c2c[nH]cn2)O1 10.1021/jm0300025
CHEMBL106612 5229 0 None -3 2 Human 6.1 pKi = 6.1 Binding
Histamine H4 receptor competition binding using [3H]Na-methylhistamineHistamine H4 receptor competition binding using [3H]Na-methylhistamine
ChEMBL 167 2 2 3 0.6 NC[C@H]1CC[C@H](c2c[nH]cn2)O1 10.1021/jm0300025
168273471 192199 0 None -50 4 Human 5.1 pKi = 5.1 Binding
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 192199 0 None -50 4 Human 5.1 pKi = 5.1 Binding
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 192199 0 None -50 4 Human 5.1 pKi = 5.1 Binding
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
57402472 67537 0 None -1819 3 Human 5.1 pKi = 5.1 Binding
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 526 11 1 6 4.0 COc1ccc(CN(CCN(C)CCN2CCN(C(=O)c3cc4ccccc4[nH]3)CC2)c2ccccn2)cc1 10.1016/j.bmcl.2011.09.001
CHEMBL1910381 67537 0 None -1819 3 Human 5.1 pKi = 5.1 Binding
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 526 11 1 6 4.0 COc1ccc(CN(CCN(C)CCN2CCN(C(=O)c3cc4ccccc4[nH]3)CC2)c2ccccn2)cc1 10.1016/j.bmcl.2011.09.001
44576985 10284 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in SK-NM-C cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in SK-NM-C cells
ChEMBL 212 4 7 4 -1.3 CC(/C=C(\C)NNC(=N)N)=N/NC(=N)N 10.1021/jm7014777
CHEMBL1162347 10284 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in SK-NM-C cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in SK-NM-C cells
ChEMBL 212 4 7 4 -1.3 CC(/C=C(\C)NNC(=N)N)=N/NC(=N)N 10.1021/jm7014777
71519010 86036 0 None - 1 Human 5.1 pKi = 5.1 Binding
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 386 2 2 5 2.7 CN1CCN(c2nc(N)nc3[nH]c(-c4ccc(Br)cc4)cc23)CC1 10.1016/j.bmcl.2012.10.139
CHEMBL2314495 86036 0 None - 1 Human 5.1 pKi = 5.1 Binding
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 386 2 2 5 2.7 CN1CCN(c2nc(N)nc3[nH]c(-c4ccc(Br)cc4)cc23)CC1 10.1016/j.bmcl.2012.10.139
1204 1901 114 None -3 23 Human 8.1 pKi = 8.1 Binding
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 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmcl.2011.10.104
1247 1901 114 None -3 23 Human 8.1 pKi = 8.1 Binding
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 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmcl.2011.10.104
1375 1901 114 None -3 23 Human 8.1 pKi = 8.1 Binding
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 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmcl.2011.10.104
774 1901 114 None -3 23 Human 8.1 pKi = 8.1 Binding
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 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmcl.2011.10.104
CHEMBL90 1901 114 None -3 23 Human 8.1 pKi = 8.1 Binding
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 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmcl.2011.10.104
DB05381 1901 114 None -3 23 Human 8.1 pKi = 8.1 Binding
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 111 2 2 2 -0.1 NCCc1cnc[nH]1 10.1016/j.bmcl.2011.10.104
54587790 61211 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]histamine from human histamine H4 receptorDisplacement of [3H]histamine from human histamine H4 receptor
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 61211 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]histamine from human histamine H4 receptorDisplacement of [3H]histamine from human histamine H4 receptor
ChEMBL 276 4 3 6 1.2 CN[C@@H]1CCN(c2cc(NC3CCCC3)nc(N)n2)C1 10.1016/j.bmcl.2011.03.017
54753437 67841 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 318 2 2 7 1.8 CN[C@@H]1CCN(c2nc(N)nc3c2oc2ncc(Cl)cc23)C1 10.1016/j.bmcl.2014.12.027
CHEMBL1915048 67841 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 318 2 2 7 1.8 CN[C@@H]1CCN(c2nc(N)nc3c2oc2ncc(Cl)cc23)C1 10.1016/j.bmcl.2014.12.027
11750684 83047 0 None - 1 Human 8.1 pKi = 8.1 Binding
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 Cc1ccc2[nH]c(-c3ccc(OCCCN4CCCN(C)CC4)cc3Cl)nc2c1C 10.1016/j.bmcl.2006.08.117
CHEMBL219982 83047 0 None - 1 Human 8.1 pKi = 8.1 Binding
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 Cc1ccc2[nH]c(-c3ccc(OCCCN4CCCN(C)CC4)cc3Cl)nc2c1C 10.1016/j.bmcl.2006.08.117
54753437 67841 0 None - 1 Human 8.1 pKi = 8.1 Binding
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 318 2 2 7 1.8 CN[C@@H]1CCN(c2nc(N)nc3c2oc2ncc(Cl)cc23)C1 10.1021/jm401727m
CHEMBL1915048 67841 0 None - 1 Human 8.1 pKi = 8.1 Binding
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 318 2 2 7 1.8 CN[C@@H]1CCN(c2nc(N)nc3c2oc2ncc(Cl)cc23)C1 10.1021/jm401727m
24825794 67714 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 317 1 2 6 2.5 Nc1nc(N2CCC[C@@H](N)C2)c2oc3ccc(Cl)cc3c2n1 10.1016/j.bmcl.2011.08.014
CHEMBL1914549 67714 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from recombinant human histamine H4 receptor
ChEMBL 317 1 2 6 2.5 Nc1nc(N2CCC[C@@H](N)C2)c2oc3ccc(Cl)cc3c2n1 10.1016/j.bmcl.2011.08.014
71525679 89296 0 None 6 6 Human 8.0 pKi = 8.0 Binding
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 272 3 2 6 1.0 CCc1cnc2c(N3CC[C@@H](NC)C3)nc(N)nc2c1 10.1016/j.bmcl.2013.02.091
CHEMBL2376801 89296 0 None 6 6 Human 8.0 pKi = 8.0 Binding
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 272 3 2 6 1.0 CCc1cnc2c(N3CC[C@@H](NC)C3)nc(N)nc2c1 10.1016/j.bmcl.2013.02.091
25071940 186771 0 None 5 2 Rat 8.0 pKi = 8.0 Binding
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 281 1 2 5 1.2 Nc1nc2c(c(N3CCNCC3)n1)CCc1ccccc1-2 10.1021/jm800670r
CHEMBL493281 186771 0 None 5 2 Rat 8.0 pKi = 8.0 Binding
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 281 1 2 5 1.2 Nc1nc2c(c(N3CCNCC3)n1)CCc1ccccc1-2 10.1021/jm800670r
71525586 89294 0 None 22 2 Human 8.0 pKi = 8.0 Binding
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 272 2 1 6 0.9 CCc1cnc2c(N3CCN(C)CC3)nc(N)nc2c1 10.1016/j.bmcl.2013.02.091
CHEMBL2376799 89294 0 None 22 2 Human 8.0 pKi = 8.0 Binding
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 272 2 1 6 0.9 CCc1cnc2c(N3CCN(C)CC3)nc(N)nc2c1 10.1016/j.bmcl.2013.02.091
44129135 197749 0 None - 1 Human 8.0 pKi = 8.0 Binding
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 454 6 1 8 1.1 CN1CCN(c2nc(NCCS(=O)(=O)N3CCOCC3)c3cc(Cl)ccc3n2)CC1 10.1021/jm901379s
CHEMBL591250 197749 0 None - 1 Human 8.0 pKi = 8.0 Binding
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 454 6 1 8 1.1 CN1CCN(c2nc(NCCS(=O)(=O)N3CCOCC3)c3cc(Cl)ccc3n2)CC1 10.1021/jm901379s
53378711 109661 0 None - 1 Human 8.0 pKi = 8.0 Binding
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 1 2 5 0.9 CC(C)(C)c1cc(N2CC[C@@H](N)C2)nc(N)n1 10.1021/jm401727m
CHEMBL3236578 109661 0 None - 1 Human 8.0 pKi = 8.0 Binding
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 1 2 5 0.9 CC(C)(C)c1cc(N2CC[C@@H](N)C2)nc(N)n1 10.1021/jm401727m
54753437 67841 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from 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 67841 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]histamine from recombinant human histamine H4 receptorDisplacement of [3H]histamine from 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
135525668 67870 0 None 263 2 Human 8.0 pKi = 8.0 Binding
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 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 67870 0 None 263 2 Human 8.0 pKi = 8.0 Binding
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 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
49841611 69390 0 None - 1 Human 7.1 pKi = 7.1 Binding
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 347 2 1 5 3.2 Cc1cccc(C)c1-c1ccc2c(N3CCN(C)CC3)nc(N)nc2c1 10.1016/j.bmcl.2011.10.104
CHEMBL1935567 69390 0 None - 1 Human 7.1 pKi = 7.1 Binding
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 347 2 1 5 3.2 Cc1cccc(C)c1-c1ccc2c(N3CCN(C)CC3)nc(N)nc2c1 10.1016/j.bmcl.2011.10.104
1248 1396 27 None -15 6 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in SK-NM-C cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in SK-NM-C cells
ChEMBL 161 4 2 3 0.6 CN(CCCSC(=N)N)C 10.1021/jm7014777
3077 1396 27 None -15 6 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in SK-NM-C cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in SK-NM-C cells
ChEMBL 161 4 2 3 0.6 CN(CCCSC(=N)N)C 10.1021/jm7014777
90045 1396 27 None -15 6 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in SK-NM-C cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in SK-NM-C cells
ChEMBL 161 4 2 3 0.6 CN(CCCSC(=N)N)C 10.1021/jm7014777
CHEMBL12344 1396 27 None -15 6 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in SK-NM-C cellsDisplacement of [3H]histamine from human histamine H4 receptor expressed in SK-NM-C cells
ChEMBL 161 4 2 3 0.6 CN(CCCSC(=N)N)C 10.1021/jm7014777
11615753 72593 6 None - 1 Human 7.1 pKi = 7.1 Binding
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 249 1 1 3 1.6 CN1CCN(C(=O)c2cc3sccc3[nH]2)CC1 10.1021/jm0502081
CHEMBL200546 72593 6 None - 1 Human 7.1 pKi = 7.1 Binding
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 249 1 1 3 1.6 CN1CCN(C(=O)c2cc3sccc3[nH]2)CC1 10.1021/jm0502081
10444761 123320 0 None - 1 Human 7.1 pKi = 7.1 Binding
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 249 1 1 3 1.6 CN1CCN(C(=O)c2cc3ccsc3[nH]2)CC1 10.1021/jm0502081
CHEMBL362495 123320 0 None - 1 Human 7.1 pKi = 7.1 Binding
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 249 1 1 3 1.6 CN1CCN(C(=O)c2cc3ccsc3[nH]2)CC1 10.1021/jm0502081
16082826 79903 0 None 3 2 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]histamine form human H4 receptorDisplacement of [3H]histamine form human H4 receptor
ChEMBL 233 5 2 2 2.7 c1nc([C@H]2C[C@@H]2CNCC2CCCCC2)c[nH]1 10.1021/jm0603318
CHEMBL214156 79903 0 None 3 2 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]histamine form human H4 receptorDisplacement of [3H]histamine form human H4 receptor
ChEMBL 233 5 2 2 2.7 c1nc([C@H]2C[C@@H]2CNCC2CCCCC2)c[nH]1 10.1021/jm0603318
122193097 123398 0 None - 1 Human 5.0 pKi = 5.0 Binding
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 364 3 1 6 2.7 CN1CCN(c2nc(N)nc(/C=C/c3ccc(Cl)cc3Cl)n2)CC1 10.1016/j.ejmech.2015.08.014
CHEMBL3628044 123398 0 None - 1 Human 5.0 pKi = 5.0 Binding
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 364 3 1 6 2.7 CN1CCN(c2nc(N)nc(/C=C/c3ccc(Cl)cc3Cl)n2)CC1 10.1016/j.ejmech.2015.08.014
57390344 67879 0 None - 1 Human 5.0 pKi = 5.0 Binding
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 248 5 3 6 0.3 CNC1CN(c2cc(N)nc(NCC3CC3)n2)C1 10.1016/j.bmcl.2011.07.125
CHEMBL1915539 67879 0 None - 1 Human 5.0 pKi = 5.0 Binding
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 248 5 3 6 0.3 CNC1CN(c2cc(N)nc(NCC3CC3)n2)C1 10.1016/j.bmcl.2011.07.125
49841607 69378 0 None - 1 Human 7.0 pKi = 7.0 Binding
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 257 1 1 5 1.3 Cc1cccc2c(N3CCN(C)CC3)nc(N)nc12 10.1016/j.bmcl.2011.10.104
CHEMBL1935555 69378 0 None - 1 Human 7.0 pKi = 7.0 Binding
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 257 1 1 5 1.3 Cc1cccc2c(N3CCN(C)CC3)nc(N)nc12 10.1016/j.bmcl.2011.10.104
12686451 202351 2 None - 1 Human 7.0 pKi = 7.0 Binding
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 262 1 0 4 2.0 CN1CCN(c2cnc3cc(Cl)ccc3n2)CC1 10.1021/jm7014217
CHEMBL1743969 202351 2 None - 1 Human 7.0 pKi = 7.0 Binding
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 262 1 0 4 2.0 CN1CCN(c2cnc3cc(Cl)ccc3n2)CC1 10.1021/jm7014217
CHEMBL6992 202351 2 None - 1 Human 7.0 pKi = 7.0 Binding
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 262 1 0 4 2.0 CN1CCN(c2cnc3cc(Cl)ccc3n2)CC1 10.1021/jm7014217
51354010 58576 0 None -1 2 Human 6.0 pKi = 6.0 Binding
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 281 7 1 4 2.6 c1ccc(Cc2cn(CCCCc3c[nH]cn3)nn2)cc1 10.1021/jm1013488
CHEMBL1688941 58576 0 None -1 2 Human 6.0 pKi = 6.0 Binding
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 281 7 1 4 2.6 c1ccc(Cc2cn(CCCCc3c[nH]cn3)nn2)cc1 10.1021/jm1013488
127036979 136963 0 None 1 2 Human 5.0 pKi = 5.0 Binding
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 399 5 1 5 3.6 CN1CCN(c2nc(NCCc3ccccc3)nc3c2CCc2ccccc2-3)CC1 10.1016/j.bmcl.2015.12.035
CHEMBL3753962 136963 0 None 1 2 Human 5.0 pKi = 5.0 Binding
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 399 5 1 5 3.6 CN1CCN(c2nc(NCCc3ccccc3)nc3c2CCc2ccccc2-3)CC1 10.1016/j.bmcl.2015.12.035
118720434 115411 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 241 3 2 5 0.6 CN[C@@H]1CCN(c2cc(CCl)nc(N)n2)C1 10.1016/j.bmcl.2014.10.013
CHEMBL3354808 115411 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 241 3 2 5 0.6 CN[C@@H]1CCN(c2cc(CCl)nc(N)n2)C1 10.1016/j.bmcl.2014.10.013
11212855 83815 0 None - 1 Human 7.0 pKi = 7.0 Binding
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 440 6 1 4 5.2 CN1CCN(CCCOc2ccc(-c3nc4cc(C(C)(C)C)ccc4[nH]3)c(Cl)c2)CC1 10.1016/j.bmcl.2006.08.117
CHEMBL220934 83815 0 None - 1 Human 7.0 pKi = 7.0 Binding
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 440 6 1 4 5.2 CN1CCN(CCCOc2ccc(-c3nc4cc(C(C)(C)C)ccc4[nH]3)c(Cl)c2)CC1 10.1016/j.bmcl.2006.08.117
57401602 67987 0 None - 1 Human 6.0 pKi = 6.0 Binding
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 242 1 0 4 1.3 Cc1ccc(C#N)c(N2CC3CN(C)CC3C2)n1 10.1016/j.bmcl.2011.07.114
CHEMBL1916504 67987 0 None - 1 Human 6.0 pKi = 6.0 Binding
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 242 1 0 4 1.3 Cc1ccc(C#N)c(N2CC3CN(C)CC3C2)n1 10.1016/j.bmcl.2011.07.114
156010537 177734 0 None -69 2 Human 6.0 pKi = 6.0 Binding
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 430 11 2 3 4.3 Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCCNCCc1c[nH]cn1 10.1021/acs.jmedchem.0c00160
CHEMBL4634235 177734 0 None -69 2 Human 6.0 pKi = 6.0 Binding
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 430 11 2 3 4.3 Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCCNCCc1c[nH]cn1 10.1021/acs.jmedchem.0c00160
CHEMBL4651053 177734 0 None -69 2 Human 6.0 pKi = 6.0 Binding
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 430 11 2 3 4.3 Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCCNCCc1c[nH]cn1 10.1021/acs.jmedchem.0c00160
90654503 109823 0 None -123 3 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]histamine from human H4 receptor expressed in Sf9 cell membrane co-transfected with Galphai2 and Gbeta1gamma2 after 60 mins by liquid scintillation counting analysisDisplacement of [3H]histamine from human H4 receptor expressed in Sf9 cell membrane co-transfected with Galphai2 and Gbeta1gamma2 after 60 mins by liquid scintillation counting analysis
ChEMBL 483 9 1 4 4.9 O=C1NC(c2ccccc2)(c2ccccc2)C(=O)N1Cc1ccc(OCCCN2CCCCC2)cc1 10.1016/j.ejmech.2014.03.014
CHEMBL3238447 109823 0 None -123 3 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]histamine from human H4 receptor expressed in Sf9 cell membrane co-transfected with Galphai2 and Gbeta1gamma2 after 60 mins by liquid scintillation counting analysisDisplacement of [3H]histamine from human H4 receptor expressed in Sf9 cell membrane co-transfected with Galphai2 and Gbeta1gamma2 after 60 mins by liquid scintillation counting analysis
ChEMBL 483 9 1 4 4.9 O=C1NC(c2ccccc2)(c2ccccc2)C(=O)N1Cc1ccc(OCCCN2CCCCC2)cc1 10.1016/j.ejmech.2014.03.014
57394626 67976 0 None 14 2 Human 6.0 pKi = 6.0 Binding
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 263 5 3 5 2.1 CC(C)(C)CCNc1cc(N[C@@H]2CCNC2)ncn1 10.1016/j.bmcl.2011.07.114
CHEMBL1916494 67976 0 None 14 2 Human 6.0 pKi = 6.0 Binding
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 263 5 3 5 2.1 CC(C)(C)CCNc1cc(N[C@@H]2CCNC2)ncn1 10.1016/j.bmcl.2011.07.114
49841723 69383 0 None - 1 Human 6.0 pKi = 6.0 Binding
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 349 3 1 6 2.6 COc1ccc(-c2cccc3c(N4CCN(C)CC4)nc(N)nc23)cc1 10.1016/j.bmcl.2011.10.104
CHEMBL1935560 69383 0 None - 1 Human 6.0 pKi = 6.0 Binding
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 349 3 1 6 2.6 COc1ccc(-c2cccc3c(N4CCN(C)CC4)nc(N)nc23)cc1 10.1016/j.bmcl.2011.10.104
112936251 136742 1 None 1 4 Human 6.0 pKi = 6.0 Binding
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 359 5 1 5 3.5 CN1CCN(c2cc(-c3ccccc3)nc(NCc3ccccc3)n2)CC1 10.1016/j.bmcl.2015.12.035
CHEMBL3752085 136742 1 None 1 4 Human 6.0 pKi = 6.0 Binding
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 359 5 1 5 3.5 CN1CCN(c2cc(-c3ccccc3)nc(NCc3ccccc3)n2)CC1 10.1016/j.bmcl.2015.12.035
25178340 186203 0 None - 1 Human 6.0 pKi = 6.0 Binding
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 291 2 1 5 2.1 CNc1nc(N2CCN(C)CC2)nc2cc(Cl)ccc12 10.1021/jm800876b
CHEMBL489069 186203 0 None - 1 Human 6.0 pKi = 6.0 Binding
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 291 2 1 5 2.1 CNc1nc(N2CCN(C)CC2)nc2cc(Cl)ccc12 10.1021/jm800876b
25179123 188511 0 None - 1 Human 6.0 pKi = 6.0 Binding
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 363 5 1 7 2.0 CCOC(=O)CNc1nc(N2CCN(C)CC2)nc2ccc(Cl)cc12 10.1021/jm800876b
CHEMBL510181 188511 0 None - 1 Human 6.0 pKi = 6.0 Binding
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 363 5 1 7 2.0 CCOC(=O)CNc1nc(N2CCN(C)CC2)nc2ccc(Cl)cc12 10.1021/jm800876b
25178340 186203 0 None - 1 Human 6.0 pKi = 6.0 Binding
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 291 2 1 5 2.1 CNc1nc(N2CCN(C)CC2)nc2cc(Cl)ccc12 10.1021/jm901379s
CHEMBL489069 186203 0 None - 1 Human 6.0 pKi = 6.0 Binding
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 291 2 1 5 2.1 CNc1nc(N2CCN(C)CC2)nc2cc(Cl)ccc12 10.1021/jm901379s
164618690 185574 0 None -13 5 Human 5.0 pKi = 5.0 Binding
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 360 7 4 4 3.4 CCCCCCNC(=O)/N=C(\N)Nc1cccc(-c2csc(N)n2)c1 10.1016/j.ejmech.2021.113190
CHEMBL4872375 185574 0 None -13 5 Human 5.0 pKi = 5.0 Binding
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 360 7 4 4 3.4 CCCCCCNC(=O)/N=C(\N)Nc1cccc(-c2csc(N)n2)c1 10.1016/j.ejmech.2021.113190
44547126 116611 1 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 248 5 2 4 1.9 CN[C@H]1CCN(c2ccnc(NCC(C)C)c2)C1 10.1016/j.bmcl.2014.12.027
CHEMBL3393527 116611 1 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 248 5 2 4 1.9 CN[C@H]1CCN(c2ccnc(NCC(C)C)c2)C1 10.1016/j.bmcl.2014.12.027
118725540 116608 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 260 3 1 4 1.9 CN[C@@H]1CCN(c2ccnc(N3CCCCC3)c2)C1 10.1016/j.bmcl.2014.12.027
CHEMBL3393524 116608 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 260 3 1 4 1.9 CN[C@@H]1CCN(c2ccnc(N3CCCCC3)c2)C1 10.1016/j.bmcl.2014.12.027
46890676 7163 0 None - 1 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 408 6 1 4 4.0 Cc1cc(OCCCN2CC3CN(C)C3C2)ccc1-c1nc2c(C)c(F)ccc2[nH]1 10.1016/j.bmcl.2010.04.017
CHEMBL1085804 7163 0 None - 1 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptorDisplacement of [3H]histamine from human recombinant histamine H4 receptor
ChEMBL 408 6 1 4 4.0 Cc1cc(OCCCN2CC3CN(C)C3C2)ccc1-c1nc2c(C)c(F)ccc2[nH]1 10.1016/j.bmcl.2010.04.017
57393651 69564 0 None - 1 Human 6.0 pKi = 6.0 Binding
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)c3cc4cccnc4[nH]3)C[C@H]2C1 10.1016/j.bmcl.2011.11.098
CHEMBL1938971 69564 0 None - 1 Human 6.0 pKi = 6.0 Binding
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)c3cc4cccnc4[nH]3)C[C@H]2C1 10.1016/j.bmcl.2011.11.098
24853666 155577 0 None - 1 Human 6.0 pKi = 6.0 Binding
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 292 1 1 4 1.7 CN1CCCN(c2nc3cc(Cl)ccc3[nH]c2=O)CC1 10.1021/jm7014217
CHEMBL406327 155577 0 None - 1 Human 6.0 pKi = 6.0 Binding
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 292 1 1 4 1.7 CN1CCCN(c2nc3cc(Cl)ccc3[nH]c2=O)CC1 10.1021/jm7014217
112936267 136771 1 None -2 2 Human 5.0 pKi = 5.0 Binding
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 373 6 1 5 3.6 CN1CCN(c2cc(-c3ccccc3)nc(NCCc3ccccc3)n2)CC1 10.1016/j.bmcl.2015.12.035
CHEMBL3752383 136771 1 None -2 2 Human 5.0 pKi = 5.0 Binding
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 373 6 1 5 3.6 CN1CCN(c2cc(-c3ccccc3)nc(NCCc3ccccc3)n2)CC1 10.1016/j.bmcl.2015.12.035
127051301 139670 0 None 5 2 Human 7.0 pKi = 7.0 Binding
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
CHEMBL3804906 139670 0 None 5 2 Human 7.0 pKi = 7.0 Binding
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
25130914 186671 0 None - 1 Human 7.0 pKi = 7.0 Binding
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 298 4 2 6 1.4 CN1CCN(c2cc(NCc3ccccc3)nc(N)n2)CC1 10.1016/j.bmc.2009.08.059
CHEMBL492677 186671 0 None - 1 Human 7.0 pKi = 7.0 Binding
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 298 4 2 6 1.4 CN1CCN(c2cc(NCc3ccccc3)nc(N)n2)CC1 10.1016/j.bmc.2009.08.059
71519178 86058 0 None - 1 Human 6.0 pKi = 6.0 Binding
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 312 2 3 5 1.9 Nc1nc(N2CC[C@H](N)C2)c2cc(-c3ccc(F)cc3)[nH]c2n1 10.1016/j.bmcl.2012.10.139
CHEMBL2314761 86058 0 None - 1 Human 6.0 pKi = 6.0 Binding
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 312 2 3 5 1.9 Nc1nc(N2CC[C@H](N)C2)c2cc(-c3ccc(F)cc3)[nH]c2n1 10.1016/j.bmcl.2012.10.139
127052293 139708 1 None 34 4 Human 7.0 pKi = 7 Binding
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
CHEMBL3805361 139708 1 None 34 4 Human 7.0 pKi = 7 Binding
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
1530 2151 44 None -21379 20 Human 8.3 pIC50 = 8.3 Binding
Histamine H-4 Receptor Binding Assay: Histamine H-4 Receptor Binding AssayHistamine H-4 Receptor Binding Assay: Histamine H-4 Receptor Binding Assay
Drug Central 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 None
3827 2151 44 None -21379 20 Human 8.3 pIC50 = 8.3 Binding
Histamine H-4 Receptor Binding Assay: Histamine H-4 Receptor Binding AssayHistamine H-4 Receptor Binding Assay: Histamine H-4 Receptor Binding Assay
Drug Central 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 None
7206 2151 44 None -21379 20 Human 8.3 pIC50 = 8.3 Binding
Histamine H-4 Receptor Binding Assay: Histamine H-4 Receptor Binding AssayHistamine H-4 Receptor Binding Assay: Histamine H-4 Receptor Binding Assay
Drug Central 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 None
CHEMBL534 2151 44 None -21379 20 Human 8.3 pIC50 = 8.3 Binding
Histamine H-4 Receptor Binding Assay: Histamine H-4 Receptor Binding AssayHistamine H-4 Receptor Binding Assay: Histamine H-4 Receptor Binding Assay
Drug Central 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 None
DB00920 2151 44 None -21379 20 Human 8.3 pIC50 = 8.3 Binding
Histamine H-4 Receptor Binding Assay: Histamine H-4 Receptor Binding AssayHistamine H-4 Receptor Binding Assay: Histamine H-4 Receptor Binding Assay
Drug Central 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 None
124087 1362 106 None -5888 15 Human 8.3 pIC50 = 8.3 Binding
Histamine H-4 Receptor Binding Assay: Histamine H-4 Receptor Binding AssayHistamine H-4 Receptor Binding Assay: Histamine H-4 Receptor Binding Assay
Drug Central 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 None
7157 1362 106 None -5888 15 Human 8.3 pIC50 = 8.3 Binding
Histamine H-4 Receptor Binding Assay: Histamine H-4 Receptor Binding AssayHistamine H-4 Receptor Binding Assay: Histamine H-4 Receptor Binding Assay
Drug Central 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 None
814 1362 106 None -5888 15 Human 8.3 pIC50 = 8.3 Binding
Histamine H-4 Receptor Binding Assay: Histamine H-4 Receptor Binding AssayHistamine H-4 Receptor Binding Assay: Histamine H-4 Receptor Binding Assay
Drug Central 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 None
CHEMBL1172 1362 106 None -5888 15 Human 8.3 pIC50 = 8.3 Binding
Histamine H-4 Receptor Binding Assay: Histamine H-4 Receptor Binding AssayHistamine H-4 Receptor Binding Assay: Histamine H-4 Receptor Binding Assay
Drug Central 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 None
DB00967 1362 106 None -5888 15 Human 8.3 pIC50 = 8.3 Binding
Histamine H-4 Receptor Binding Assay: Histamine H-4 Receptor Binding AssayHistamine H-4 Receptor Binding Assay: Histamine H-4 Receptor Binding Assay
Drug Central 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 None
71548412 1878 14 None - 0 Mouse 6.5 pIC50 = 6.5 Binding
Radioligand competitive binding assay using [<sup>3</sup>H]Histamine as tracer, and membrane preparations from CHO-K1 cells expressing mouse H<sub>4</sub> receptor.Radioligand competitive binding assay using [<sup>3</sup>H]Histamine as tracer, and membrane preparations from CHO-K1 cells expressing mouse H<sub>4</sub> receptor.
Guide to Pharmacology 334 2 1 8 0.2 CNC1CN(C1)c1nc2ncc(cc2n2c1nnn2)Br 29579390
9879 1878 14 None - 0 Mouse 6.5 pIC50 = 6.5 Binding
Radioligand competitive binding assay using [<sup>3</sup>H]Histamine as tracer, and membrane preparations from CHO-K1 cells expressing mouse H<sub>4</sub> receptor.Radioligand competitive binding assay using [<sup>3</sup>H]Histamine as tracer, and membrane preparations from CHO-K1 cells expressing mouse H<sub>4</sub> receptor.
Guide to Pharmacology 334 2 1 8 0.2 CNC1CN(C1)c1nc2ncc(cc2n2c1nnn2)Br 29579390
CHEMBL4790724 1878 14 None - 0 Mouse 6.5 pIC50 = 6.5 Binding
Radioligand competitive binding assay using [<sup>3</sup>H]Histamine as tracer, and membrane preparations from CHO-K1 cells expressing mouse H<sub>4</sub> receptor.Radioligand competitive binding assay using [<sup>3</sup>H]Histamine as tracer, and membrane preparations from CHO-K1 cells expressing mouse H<sub>4</sub> receptor.
Guide to Pharmacology 334 2 1 8 0.2 CNC1CN(C1)c1nc2ncc(cc2n2c1nnn2)Br 29579390
71548412 1878 14 None - 0 Human 7.6 pIC50 = 7.6 Binding
Radioligand competitive binding assay using [<sup>3</sup>H]Histamine as tracer, and membrane preparations from CHO-K1 cells expressing human H<sub>4</sub> receptor.Radioligand competitive binding assay using [<sup>3</sup>H]Histamine as tracer, and membrane preparations from CHO-K1 cells expressing human H<sub>4</sub> receptor.
Guide to Pharmacology 334 2 1 8 0.2 CNC1CN(C1)c1nc2ncc(cc2n2c1nnn2)Br 29579390
9879 1878 14 None - 0 Human 7.6 pIC50 = 7.6 Binding
Radioligand competitive binding assay using [<sup>3</sup>H]Histamine as tracer, and membrane preparations from CHO-K1 cells expressing human H<sub>4</sub> receptor.Radioligand competitive binding assay using [<sup>3</sup>H]Histamine as tracer, and membrane preparations from CHO-K1 cells expressing human H<sub>4</sub> receptor.
Guide to Pharmacology 334 2 1 8 0.2 CNC1CN(C1)c1nc2ncc(cc2n2c1nnn2)Br 29579390
CHEMBL4790724 1878 14 None - 0 Human 7.6 pIC50 = 7.6 Binding
Radioligand competitive binding assay using [<sup>3</sup>H]Histamine as tracer, and membrane preparations from CHO-K1 cells expressing human H<sub>4</sub> receptor.Radioligand competitive binding assay using [<sup>3</sup>H]Histamine as tracer, and membrane preparations from CHO-K1 cells expressing human H<sub>4</sub> receptor.
Guide to Pharmacology 334 2 1 8 0.2 CNC1CN(C1)c1nc2ncc(cc2n2c1nnn2)Br 29579390
1278 2119 79 None -3 8 Human 8.4 pKd = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 14722321
1279 2119 79 None -3 8 Human 8.4 pKd = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 14722321
4908365 2119 79 None -3 8 Human 8.4 pKd = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 14722321
CHEMBL129198 2119 79 None -3 8 Human 8.4 pKd = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 14722321
1204 1901 114 None -12 23 Rat 6.9 pKd None 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 11561071
1247 1901 114 None -12 23 Rat 6.9 pKd None 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 11561071
1375 1901 114 None -12 23 Rat 6.9 pKd None 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 11561071
774 1901 114 None -12 23 Rat 6.9 pKd None 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 11561071
CHEMBL90 1901 114 None -12 23 Rat 6.9 pKd None 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 11561071
DB05381 1901 114 None -12 23 Rat 6.9 pKd None 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 11561071
1236 2036 23 None -204 7 Human 7.2 pKd None 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 125 2 2 2 0.3 C[C@H](Cc1cnc[nH]1)N 11179434
1237 2036 23 None -204 7 Human 7.2 pKd None 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 125 2 2 2 0.3 C[C@H](Cc1cnc[nH]1)N 11179434
156615 2036 23 None -204 7 Human 7.2 pKd None 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 125 2 2 2 0.3 C[C@H](Cc1cnc[nH]1)N 11179434
CHEMBL268229 2036 23 None -204 7 Human 7.2 pKd None 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 125 2 2 2 0.3 C[C@H](Cc1cnc[nH]1)N 11179434
1204 1901 114 None -15 23 Mouse 7.4 pKd None 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 11561071
1247 1901 114 None -15 23 Mouse 7.4 pKd None 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 11561071
1375 1901 114 None -15 23 Mouse 7.4 pKd None 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 11561071
774 1901 114 None -15 23 Mouse 7.4 pKd None 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 11561071
CHEMBL90 1901 114 None -15 23 Mouse 7.4 pKd None 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 11561071
DB05381 1901 114 None -15 23 Mouse 7.4 pKd None 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 11561071
1241 2006 46 None -89 5 Human 7.8 pKd None 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 125 2 1 3 -0.1 Cn1cc(nc1)CCN 11179434
1242 2006 46 None -89 5 Human 7.8 pKd None 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 125 2 1 3 -0.1 Cn1cc(nc1)CCN 11179434
3614 2006 46 None -89 5 Human 7.8 pKd None 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 125 2 1 3 -0.1 Cn1cc(nc1)CCN 11179434
CHEMBL507 2006 46 None -89 5 Human 7.8 pKd None 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 125 2 1 3 -0.1 Cn1cc(nc1)CCN 11179434
1204 1901 114 None -3 23 Human 7.9 pKd None 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 10973974
1204 1901 114 None -3 23 Human 7.9 pKd None 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 11179434
1204 1901 114 None -3 23 Human 7.9 pKd None 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 11179435
1204 1901 114 None -3 23 Human 7.9 pKd None 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 11181941
1204 1901 114 None -3 23 Human 7.9 pKd None 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 11561071
1204 1901 114 None -3 23 Human 7.9 pKd None 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 16432504
1247 1901 114 None -3 23 Human 7.9 pKd None 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 10973974
1247 1901 114 None -3 23 Human 7.9 pKd None 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 11179434
1247 1901 114 None -3 23 Human 7.9 pKd None 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 11179435
1247 1901 114 None -3 23 Human 7.9 pKd None 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 11181941
1247 1901 114 None -3 23 Human 7.9 pKd None 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 11561071
1247 1901 114 None -3 23 Human 7.9 pKd None 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 16432504
1375 1901 114 None -3 23 Human 7.9 pKd None 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 10973974
1375 1901 114 None -3 23 Human 7.9 pKd None 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 11179434
1375 1901 114 None -3 23 Human 7.9 pKd None 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 11179435
1375 1901 114 None -3 23 Human 7.9 pKd None 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 11181941
1375 1901 114 None -3 23 Human 7.9 pKd None 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 11561071
1375 1901 114 None -3 23 Human 7.9 pKd None 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 16432504
774 1901 114 None -3 23 Human 7.9 pKd None 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 10973974
774 1901 114 None -3 23 Human 7.9 pKd None 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 11179434
774 1901 114 None -3 23 Human 7.9 pKd None 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 11179435
774 1901 114 None -3 23 Human 7.9 pKd None 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 11181941
774 1901 114 None -3 23 Human 7.9 pKd None 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 11561071
774 1901 114 None -3 23 Human 7.9 pKd None 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 16432504
CHEMBL90 1901 114 None -3 23 Human 7.9 pKd None 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 10973974
CHEMBL90 1901 114 None -3 23 Human 7.9 pKd None 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 11179434
CHEMBL90 1901 114 None -3 23 Human 7.9 pKd None 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 11179435
CHEMBL90 1901 114 None -3 23 Human 7.9 pKd None 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 11181941
CHEMBL90 1901 114 None -3 23 Human 7.9 pKd None 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 11561071
CHEMBL90 1901 114 None -3 23 Human 7.9 pKd None 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 16432504
DB05381 1901 114 None -3 23 Human 7.9 pKd None 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 10973974
DB05381 1901 114 None -3 23 Human 7.9 pKd None 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 11179434
DB05381 1901 114 None -3 23 Human 7.9 pKd None 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 11179435
DB05381 1901 114 None -3 23 Human 7.9 pKd None 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 11181941
DB05381 1901 114 None -3 23 Human 7.9 pKd None 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 11561071
DB05381 1901 114 None -3 23 Human 7.9 pKd None 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 16432504
None 214372 0 3H-Histamine 4 6 Guinea pig 10.0 pKi = 10 Binding
NoneNone
PDSP KiDatabase 125 2 2 2 0.3 CC(CC1=CN=CN1)N None
1204 1901 114 3H-Histamine 1 23 Guinea pig 9.9 pKi = 9.9 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
1247 1901 114 3H-Histamine 1 23 Guinea pig 9.9 pKi = 9.9 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
1375 1901 114 3H-Histamine 1 23 Guinea pig 9.9 pKi = 9.9 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
774 1901 114 3H-Histamine 1 23 Guinea pig 9.9 pKi = 9.9 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
CHEMBL90 1901 114 3H-Histamine 1 23 Guinea pig 9.9 pKi = 9.9 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
DB05381 1901 114 3H-Histamine 1 23 Guinea pig 9.9 pKi = 9.9 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
None 214372 0 3H-Histamine 4 6 Guinea pig 9.8 pKi = 9.8 Binding
NoneNone
PDSP KiDatabase 125 2 2 2 0.3 CC(CC1=CN=CN1)N None
179 396 107 3H-Histamine -4365 50 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 369 7 2 6 1.3 CCN1CCCC1CNC(=O)c1cc(c(cc1OC)N)S(=O)(=O)CC None
2159 396 107 3H-Histamine -4365 50 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 369 7 2 6 1.3 CCN1CCCC1CNC(=O)c1cc(c(cc1OC)N)S(=O)(=O)CC None
963 396 107 3H-Histamine -4365 50 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 369 7 2 6 1.3 CCN1CCCC1CNC(=O)c1cc(c(cc1OC)N)S(=O)(=O)CC None
CHEMBL243712 396 107 3H-Histamine -4365 50 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 369 7 2 6 1.3 CCN1CCCC1CNC(=O)c1cc(c(cc1OC)N)S(=O)(=O)CC None
DB06288 396 107 3H-Histamine -4365 50 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 369 7 2 6 1.3 CCN1CCCC1CNC(=O)c1cc(c(cc1OC)N)S(=O)(=O)CC None
242 467 117 3H-Histamine -7244 51 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
34 467 117 3H-Histamine -7244 51 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
60795 467 117 3H-Histamine -7244 51 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
CHEMBL1112 467 117 3H-Histamine -7244 51 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
DB01238 467 117 3H-Histamine -7244 51 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
1231 924 112 3H-Histamine -81 7 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 252 5 3 4 0.6 N#CNC(=NC)NCCSCc1nc[nH]c1C None
1231 924 112 3H-PYRILAMINE -81 7 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 252 5 3 4 0.6 N#CNC(=NC)NCCSCc1nc[nH]c1C None
2756 924 112 3H-Histamine -81 7 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 252 5 3 4 0.6 N#CNC(=NC)NCCSCc1nc[nH]c1C None
2756 924 112 3H-PYRILAMINE -81 7 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 252 5 3 4 0.6 N#CNC(=NC)NCCSCc1nc[nH]c1C None
645 924 112 3H-Histamine -81 7 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 252 5 3 4 0.6 N#CNC(=NC)NCCSCc1nc[nH]c1C None
645 924 112 3H-PYRILAMINE -81 7 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 252 5 3 4 0.6 N#CNC(=NC)NCCSCc1nc[nH]c1C None
CHEMBL30 924 112 3H-Histamine -81 7 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 252 5 3 4 0.6 N#CNC(=NC)NCCSCc1nc[nH]c1C None
CHEMBL30 924 112 3H-PYRILAMINE -81 7 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 252 5 3 4 0.6 N#CNC(=NC)NCCSCc1nc[nH]c1C None
DB00501 924 112 3H-Histamine -81 7 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 252 5 3 4 0.6 N#CNC(=NC)NCCSCc1nc[nH]c1C None
DB00501 924 112 3H-PYRILAMINE -81 7 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 252 5 3 4 0.6 N#CNC(=NC)NCCSCc1nc[nH]c1C None
277 1274 55 3H-Histamine -301 45 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
2913 1274 55 3H-Histamine -301 45 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
765 1274 55 3H-Histamine -301 45 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
CHEMBL516 1274 55 3H-Histamine -301 45 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
DB00434 1274 55 3H-Histamine -301 45 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
1248 1396 27 3H-PYRILAMINE -15 6 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 161 4 2 3 0.6 CN(CCCSC(=N)N)C None
3077 1396 27 3H-PYRILAMINE -15 6 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 161 4 2 3 0.6 CN(CCCSC(=N)N)C None
90045 1396 27 3H-PYRILAMINE -15 6 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 161 4 2 3 0.6 CN(CCCSC(=N)N)C None
CHEMBL12344 1396 27 3H-PYRILAMINE -15 6 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 161 4 2 3 0.6 CN(CCCSC(=N)N)C None
1224 1404 79 3H-Histamine -194 13 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C None
3100 1404 79 3H-Histamine -194 13 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C None
8980 1404 79 3H-Histamine -194 13 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C None
916 1404 79 3H-Histamine -194 13 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C None
CHEMBL657 1404 79 3H-Histamine -194 13 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C None
DB01075 1404 79 3H-Histamine -194 13 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C None
1212 1632 45 3H-Histamine -19952 65 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
204 1632 45 3H-Histamine -19952 65 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
3372 1632 45 3H-Histamine -19952 65 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
CHEMBL726 1632 45 3H-Histamine -19952 65 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
DB00623 1632 45 3H-Histamine -19952 65 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
1353 1880 85 3H-Histamine -6918 85 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
3559 1880 85 3H-Histamine -6918 85 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
86 1880 85 3H-Histamine -6918 85 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
CHEMBL54 1880 85 3H-Histamine -6918 85 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
DB00502 1880 85 3H-Histamine -6918 85 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
135398745 2869 108 3H-Histamine -5128 65 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
47 2869 108 3H-Histamine -5128 65 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
CHEMBL715 2869 108 3H-Histamine -5128 65 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
DB00334 2869 108 3H-Histamine -5128 65 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
119570 3110 90 3H-Histamine -301 40 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N None
2233 3110 90 3H-Histamine -301 40 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N None
953 3110 90 3H-Histamine -301 40 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N None
CHEMBL301265 3110 90 3H-Histamine -301 40 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N None
DB00413 3110 90 3H-Histamine -301 40 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N None
2337 3205 72 3H-Histamine -1122 62 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
50 3205 72 3H-Histamine -1122 62 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
5002 3205 72 3H-Histamine -1122 62 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
CHEMBL716 3205 72 3H-Histamine -1122 62 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
DB01224 3205 72 3H-Histamine -1122 62 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
1234 3239 0 3H-Histamine -162 6 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 314 10 2 7 1.5 CN/C(=C\[N+](=O)[O-])/NCCSCc1ccc(o1)CN(C)C None
3001055 3239 0 3H-Histamine -162 6 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 314 10 2 7 1.5 CN/C(=C\[N+](=O)[O-])/NCCSCc1ccc(o1)CN(C)C None
CHEMBL512 3239 0 3H-Histamine -162 6 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 314 10 2 7 1.5 CN/C(=C\[N+](=O)[O-])/NCCSCc1ccc(o1)CN(C)C None
DB00863 3239 0 3H-Histamine -162 6 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 314 10 2 7 1.5 CN/C(=C\[N+](=O)[O-])/NCCSCc1ccc(o1)CN(C)C None
2389 3279 114 3H-Histamine -25703 67 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
5073 3279 114 3H-Histamine -25703 67 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
96 3279 114 3H-Histamine -25703 67 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
CHEMBL85 3279 114 3H-Histamine -25703 67 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
DB00734 3279 114 3H-Histamine -25703 67 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
6917970 3635 54 3H-Histamine -2290 34 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 327 2 2 5 2.8 COc1cc2CCN3[C@H](c2cc1O)Cc1c(C3)c(OC)c(cc1)O None
8370 3635 54 3H-Histamine -2290 34 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 327 2 2 5 2.8 COc1cc2CCN3[C@H](c2cc1O)Cc1c(C3)c(OC)c(cc1)O None
CHEMBL487387 3635 54 3H-Histamine -2290 34 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 327 2 2 5 2.8 COc1cc2CCN3[C@H](c2cc1O)Cc1c(C3)c(OC)c(cc1)O None
213 3792 50 3H-Histamine -549 43 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 None
2717 3792 50 3H-Histamine -549 43 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 None
5533 3792 50 3H-Histamine -549 43 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 None
CHEMBL621 3792 50 3H-Histamine -549 43 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 None
DB00656 3792 50 3H-Histamine -549 43 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 None
185 3943 54 3H-Histamine -30902 37 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 373 7 1 4 3.8 COc1cccc(c1OC)[C@@H](C1CCN(CC1)CCc1ccc(cc1)F)O None
5311271 3943 54 3H-Histamine -30902 37 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 373 7 1 4 3.8 COc1cccc(c1OC)[C@@H](C1CCN(CC1)CCc1ccc(cc1)F)O None
CHEMBL74355 3943 54 3H-Histamine -30902 37 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 373 7 1 4 3.8 COc1cccc(c1OC)[C@@H](C1CCN(CC1)CCc1ccc(cc1)F)O None
DB16351 3943 54 3H-Histamine -30902 37 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 373 7 1 4 3.8 COc1cccc(c1OC)[C@@H](C1CCN(CC1)CCc1ccc(cc1)F)O None
2865 4079 67 3H-Histamine -20417 53 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
59 4079 67 3H-Histamine -20417 53 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
60854 4079 67 3H-Histamine -20417 53 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
CHEMBL708 4079 67 3H-Histamine -20417 53 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
DB00246 4079 67 3H-Histamine -20417 53 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
10297 26905 29 3H-Histamine -38 43 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 151 2 2 2 1.1 C[C@H](N)[C@H](O)c1ccccc1 None
CHEMBL136560 26905 29 3H-Histamine -38 43 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 151 2 2 2 1.1 C[C@H](N)[C@H](O)c1ccccc1 None
156391 46537 95 3H-Histamine -1 30 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 230 3 1 2 3.0 COc1ccc2cc([C@H](C)C(=O)O)ccc2c1 None
CHEMBL1200806 46537 95 3H-Histamine -1 30 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 230 3 1 2 3.0 COc1ccc2cc([C@H](C)C(=O)O)ccc2c1 None
CHEMBL154 46537 95 3H-Histamine -1 30 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 230 3 1 2 3.0 COc1ccc2cc([C@H](C)C(=O)O)ccc2c1 None
10624 69957 17 3H-Histamine -102 32 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 284 5 3 3 1.7 CN(C)CCc1c[nH]c2cccc(OP(=O)(O)O)c12 None
138543650 69957 17 3H-Histamine -102 32 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 284 5 3 3 1.7 CN(C)CCc1c[nH]c2cccc(OP(=O)(O)O)c12 None
CHEMBL194378 69957 17 3H-Histamine -102 32 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 284 5 3 3 1.7 CN(C)CCc1c[nH]c2cccc(OP(=O)(O)O)c12 None
21830793 91403 5 3H-8-OH-DPAT -66069 46 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 373 7 0 8 0.6 COc1ccccc1N1CCN(CCCCn2ncc(=O)n(C)c2=O)CC1 None
CHEMBL2413154 91403 5 3H-8-OH-DPAT -66069 46 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 373 7 0 8 0.6 COc1ccccc1N1CCN(CCCCn2ncc(=O)n(C)c2=O)CC1 None
46780481 107045 18 3H-Histamine -58884 53 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
9903970 107045 18 3H-Histamine -58884 53 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
CHEMBL3187365 107045 18 3H-Histamine -58884 53 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
CHEMBL3544974 107045 18 3H-Histamine -58884 53 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
446220 132998 13 3H-Histamine -1778 45 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 303 3 0 5 1.9 COC(=O)[C@H]1[C@@H](OC(=O)c2ccccc2)C[C@@H]2CC[C@H]1N2C None
CHEMBL370805 132998 13 3H-Histamine -1778 45 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 303 3 0 5 1.9 COC(=O)[C@H]1[C@@H](OC(=O)c2ccccc2)C[C@@H]2CC[C@H]1N2C None
4495 194860 87 3H-Histamine -1 30 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 308 5 1 5 2.8 CS(=O)(=O)Nc1ccc([N+](=O)[O-])cc1Oc1ccccc1 None
CHEMBL56367 194860 87 3H-Histamine -1 30 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 308 5 1 5 2.8 CS(=O)(=O)Nc1ccc([N+](=O)[O-])cc1Oc1ccccc1 None
54677470 198867 110 3H-Histamine -1 30 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 351 2 2 6 2.0 Cc1cnc(NC(=O)C2=C(O)c3ccccc3S(=O)(=O)N2C)s1 None
CHEMBL1256873 198867 110 3H-Histamine -1 30 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 351 2 2 6 2.0 Cc1cnc(NC(=O)C2=C(O)c3ccccc3S(=O)(=O)N2C)s1 None
CHEMBL599 198867 110 3H-Histamine -1 30 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 351 2 2 6 2.0 Cc1cnc(NC(=O)C2=C(O)c3ccccc3S(=O)(=O)N2C)s1 None
162265 200587 19 3H-Histamine -239 44 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 151 2 2 2 1.1 CC(N)C(O)c1ccccc1 None
4786 200587 19 3H-Histamine -239 44 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 151 2 2 2 1.1 CC(N)C(O)c1ccccc1 None
CHEMBL61006 200587 19 3H-Histamine -239 44 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 151 2 2 2 1.1 CC(N)C(O)c1ccccc1 None
4054 203790 64 3H-Histamine -1 37 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 179 0 1 1 2.7 CC12CC3CC(C)(C1)CC(N)(C3)C2 None
CHEMBL1699 203790 64 3H-Histamine -1 37 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 179 0 1 1 2.7 CC12CC3CC(C)(C1)CC(N)(C3)C2 None
CHEMBL807 203790 64 3H-Histamine -1 37 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 179 0 1 1 2.7 CC12CC3CC(C)(C1)CC(N)(C3)C2 None
11954259 214201 0 3H-Histamine -33113 43 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 443 5 0 5 3.5 CN1CCN(CC1)CCC=C2C3=CC=CC=C3SC4=C2C=C(C=C4)S(=O)(=O)N(C)C None
None 214217 0 3H-Histamine -1 27 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 329 2 0 4 3.6 CC1=NC=CN1CC2CCC3=C(C2=O)C4=CC=CC=C4N3C.Cl None
104911 214249 0 3H-Histamine -41686 36 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 530 7 0 5 5.1 COC1=CC=CC=C1N2CCN(CC2)CCN(C3=CC=CC=N3)C(=O)C4CCCCC4.Cl.Cl.Cl None
None 214372 0 3H-PYRILAMINE -7585 6 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 125 2 2 2 0.3 CC(CC1=CN=CN1)N None
25137849 214425 0 3H-Histamine -4 40 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 165 3 2 2 1.3 CC(C(C1=CC=CC=C1)O)NC None
71290 214425 0 3H-Histamine -4 40 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 165 3 2 2 1.3 CC(C(C1=CC=CC=C1)O)NC None
None 214560 0 3H-Histamine -1 33 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 240 7 4 6 -0.8 C(C(C(=O)O)N)SSCC(C(=O)O)N None
None 214561 0 3H-Histamine -1 33 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 149 4 2 3 0.2 CSCCC(C(=O)O)N None
None 214562 0 3H-Histamine -1 33 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 135 3 3 3 -0.3 C(CS)C(C(=O)O)N None
None 214563 0 3H-Histamine -1 33 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 121 2 3 3 -0.7 C(C(C(=O)O)N)S None
None 214564 0 3H-Histamine -1 28 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 117 0 1 3 -0.0 C1CSC(=O)C1N None
None 214565 0 3H-Histamine -1 39 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 153 3 3 3 -1.4 C(C(C(=O)O)N)S(=O)O None
None 214566 0 3H-Histamine -1 38 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 169 3 3 4 -1.7 C(C(C(=O)O)N)S(=O)(=O)O None
None 214574 0 3H-Histamine -13 40 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 149 2 1 2 1.2 CC(C(=O)C1=CC=CC=C1)N None
1576 214575 0 3H-Histamine -16 40 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 163 3 1 2 1.5 CC(C(=O)C1=CC=CC=C1)NC None
135269 214639 0 3H-Histamine -1 30 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 222 5 1 3 2.5 CCCCC(=O)OC1=CC=CC=C1C(=O)O None
23681059 214640 0 3H-Histamine -1 29 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 230 3 1 2 3.0 CC(C1=CC2=C(C=C1)C=C(C=C2)OC)C(=O)O None
123619 214644 0 3H-Histamine -1412 27 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 358 3 0 4 4.2 CC1=NC=C(C=C1)C2=NC=C(C=C2C3=CC=C(C=C3)S(=O)(=O)C)Cl None
119828 214645 0 3H-Histamine -1 30 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 370 5 1 5 3.5 CCC(=O)NS(=O)(=O)C1=CC=C(C=C1)C2=C(ON=C2C3=CC=CC=C3)C None
None 214648 0 3H-Histamine -7 29 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 517 8 2 5 5.2 CC1=C(C2=C(N1C(=O)C3=CC=C(C=C3)Cl)C=CC(=C2)OC)CC(=O)NCCC4=CC=C(C=C4)NC(=O)C None
None 214747 0 3H-Histamine -4570 27 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 347 6 0 3 5.0 CC(=O)N(CC1=CC=CC=C1OC)C2=CC=CC=C2OC3=CC=CC=C3 None
135409468 2004 63 3H-Histamine -363 40 Human 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 312 1 2 4 1.7 Clc1ccc2c(c1)NC(=c1c(=N2)cccc1)N1CCNCC1 None
333 2004 63 3H-Histamine -363 40 Human 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 312 1 2 4 1.7 Clc1ccc2c(c1)NC(=c1c(=N2)cccc1)N1CCNCC1 None
CHEMBL845 2004 63 3H-Histamine -363 40 Human 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 312 1 2 4 1.7 Clc1ccc2c(c1)NC(=c1c(=N2)cccc1)N1CCNCC1 None
1204 1901 114 3H-Histamine 1 23 Guinea pig 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
1247 1901 114 3H-Histamine 1 23 Guinea pig 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
1375 1901 114 3H-Histamine 1 23 Guinea pig 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
774 1901 114 3H-Histamine 1 23 Guinea pig 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
CHEMBL90 1901 114 3H-Histamine 1 23 Guinea pig 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
DB05381 1901 114 3H-Histamine 1 23 Guinea pig 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
1225 1443 24 3H-PYRILAMINE -371 21 Human 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 279 3 0 2 4.0 CN(CC/C=C\1/c2ccccc2OCc2c1cccc2)C None
3958 1443 24 3H-PYRILAMINE -371 21 Human 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 279 3 0 2 4.0 CN(CC/C=C\1/c2ccccc2OCc2c1cccc2)C None
667477 1443 24 3H-PYRILAMINE -371 21 Human 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 279 3 0 2 4.0 CN(CC/C=C\1/c2ccccc2OCc2c1cccc2)C None
CHEMBL860 1443 24 3H-PYRILAMINE -371 21 Human 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 279 3 0 2 4.0 CN(CC/C=C\1/c2ccccc2OCc2c1cccc2)C None
DB01142 1443 24 3H-PYRILAMINE -371 21 Human 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 279 3 0 2 4.0 CN(CC/C=C\1/c2ccccc2OCc2c1cccc2)C None
1226 1988 16 3H-Histamine 2 6 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 321 9 4 4 1.2 NC(=NCCCc1cnc[nH]1)NCCSCc1nc[nH]c1C None
41376 1988 16 3H-Histamine 2 6 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 321 9 4 4 1.2 NC(=NCCCc1cnc[nH]1)NCCSCc1nc[nH]c1C None
CHEMBL12608 1988 16 3H-Histamine 2 6 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 321 9 4 4 1.2 NC(=NCCCc1cnc[nH]1)NCCSCc1nc[nH]c1C None
1223 940 32 3H-JNJ 7777120 -60 11 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 308 6 2 3 3.2 Clc1ccc(cc1)CN=C(SCCCc1cnc[nH]1)N None
2790 940 32 3H-JNJ 7777120 -60 11 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 308 6 2 3 3.2 Clc1ccc(cc1)CN=C(SCCCc1cnc[nH]1)N None
CHEMBL14690 940 32 3H-JNJ 7777120 -60 11 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 308 6 2 3 3.2 Clc1ccc(cc1)CN=C(SCCCc1cnc[nH]1)N None
1251 1983 34 3H-JNJ 7777120 -100 5 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 165 2 2 2 1.0 N1CCC(CC1)Cc1[nH]cnc1 None
3035842 1983 34 3H-JNJ 7777120 -100 5 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 165 2 2 2 1.0 N1CCC(CC1)Cc1[nH]cnc1 None
CHEMBL18661 1983 34 3H-JNJ 7777120 -100 5 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 165 2 2 2 1.0 N1CCC(CC1)Cc1[nH]cnc1 None
1253 2027 7 3H-N-alpha-methylhistamine -11 4 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 342 6 1 2 3.2 Ic1ccc(cc1)COCCCc1cnc[nH]1 None
132937 2027 7 3H-N-alpha-methylhistamine -11 4 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 342 6 1 2 3.2 Ic1ccc(cc1)COCCCc1cnc[nH]1 None
CHEMBL19010 2027 7 3H-N-alpha-methylhistamine -11 4 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 342 6 1 2 3.2 Ic1ccc(cc1)COCCCc1cnc[nH]1 None
None 214502 0 3H-Histamine -13 18 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 416 9 3 4 2.8 C1=CC(=CC=C1CCNC(N)SCCCC2=CN=CN2)I None
None 214502 0 3H-N-alpha-methylhistamine -13 18 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 416 9 3 4 2.8 C1=CC(=CC=C1CCNC(N)SCCCC2=CN=CN2)I None
1223 940 32 3H-Histamine -60 11 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 308 6 2 3 3.2 Clc1ccc(cc1)CN=C(SCCCc1cnc[nH]1)N None
2790 940 32 3H-Histamine -60 11 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 308 6 2 3 3.2 Clc1ccc(cc1)CN=C(SCCCc1cnc[nH]1)N None
CHEMBL14690 940 32 3H-Histamine -60 11 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 308 6 2 3 3.2 Clc1ccc(cc1)CN=C(SCCCc1cnc[nH]1)N None
1267 3744 43 3H-Histamine -33 25 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 None
1267 3744 43 3H-N-alpha-methylhistamine -33 25 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 None
3035905 3744 43 3H-Histamine -33 25 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 None
3035905 3744 43 3H-N-alpha-methylhistamine -33 25 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 None
CHEMBL260374 3744 43 3H-Histamine -33 25 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 None
CHEMBL260374 3744 43 3H-N-alpha-methylhistamine -33 25 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 None
1547484 927 70 3H-PYRILAMINE -5 20 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 368 6 0 2 5.1 c1ccc(cc1)/C=C/CN1CCN(CC1)C(c1ccccc1)c1ccccc1 None
654 927 70 3H-PYRILAMINE -5 20 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 368 6 0 2 5.1 c1ccc(cc1)/C=C/CN1CCN(CC1)C(c1ccccc1)c1ccccc1 None
9072 927 70 3H-PYRILAMINE -5 20 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 368 6 0 2 5.1 c1ccc(cc1)/C=C/CN1CCN(CC1)C(c1ccccc1)c1ccccc1 None
CHEMBL43064 927 70 3H-PYRILAMINE -5 20 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 368 6 0 2 5.1 c1ccc(cc1)/C=C/CN1CCN(CC1)C(c1ccccc1)c1ccccc1 None
DB00568 927 70 3H-PYRILAMINE -5 20 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 368 6 0 2 5.1 c1ccc(cc1)/C=C/CN1CCN(CC1)C(c1ccccc1)c1ccccc1 None
45037031 214395 0 3H-Histamine -70 4 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 285 2 2 2 1.5 C[C@H](CC1=CN=CN1)N.Br.Br None
1223 940 32 125I-iodophenpropit -60 11 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 308 6 2 3 3.2 Clc1ccc(cc1)CN=C(SCCCc1cnc[nH]1)N None
2790 940 32 125I-iodophenpropit -60 11 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 308 6 2 3 3.2 Clc1ccc(cc1)CN=C(SCCCc1cnc[nH]1)N None
CHEMBL14690 940 32 125I-iodophenpropit -60 11 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 308 6 2 3 3.2 Clc1ccc(cc1)CN=C(SCCCc1cnc[nH]1)N None
1204 1901 114 3H-Histamine -3 23 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
1204 1901 114 3H-N-alpha-methylhistamine -3 23 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
1247 1901 114 3H-Histamine -3 23 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
1247 1901 114 3H-N-alpha-methylhistamine -3 23 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
1375 1901 114 3H-Histamine -3 23 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
1375 1901 114 3H-N-alpha-methylhistamine -3 23 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
774 1901 114 3H-Histamine -3 23 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
774 1901 114 3H-N-alpha-methylhistamine -3 23 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
CHEMBL90 1901 114 3H-Histamine -3 23 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
CHEMBL90 1901 114 3H-N-alpha-methylhistamine -3 23 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
DB05381 1901 114 3H-Histamine -3 23 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
DB05381 1901 114 3H-N-alpha-methylhistamine -3 23 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
2286 3134 48 3H-PYRILAMINE -10 29 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C None
4927 3134 48 3H-PYRILAMINE -10 29 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C None
7282 3134 48 3H-PYRILAMINE -10 29 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C None
CHEMBL643 3134 48 3H-PYRILAMINE -10 29 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C None
DB01069 3134 48 3H-PYRILAMINE -10 29 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C None
1204 1901 114 3H-Histamine -3 23 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
1247 1901 114 3H-Histamine -3 23 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
1375 1901 114 3H-Histamine -3 23 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
774 1901 114 3H-Histamine -3 23 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
CHEMBL90 1901 114 3H-Histamine -3 23 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
DB05381 1901 114 3H-Histamine -3 23 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
3032915 15321 20 3H-Histamine -1 6 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 212 5 3 2 1.2 C/N=C(\S)NCCCCc1c[nH]cn1 None
CHEMBL12160 15321 20 3H-Histamine -1 6 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 212 5 3 2 1.2 C/N=C(\S)NCCCCc1c[nH]cn1 None
1204 1901 114 3H-JNJ 7777120 -3 23 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
1247 1901 114 3H-JNJ 7777120 -3 23 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
1375 1901 114 3H-JNJ 7777120 -3 23 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
774 1901 114 3H-JNJ 7777120 -3 23 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
CHEMBL90 1901 114 3H-JNJ 7777120 -3 23 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
DB05381 1901 114 3H-JNJ 7777120 -3 23 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
1251 1983 34 125I-iodophenpropit -100 5 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 165 2 2 2 1.0 N1CCC(CC1)Cc1[nH]cnc1 None
1251 1983 34 3H-Histamine -100 5 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 165 2 2 2 1.0 N1CCC(CC1)Cc1[nH]cnc1 None
1251 1983 34 3H-N-alpha-methylhistamine -100 5 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 165 2 2 2 1.0 N1CCC(CC1)Cc1[nH]cnc1 None
3035842 1983 34 125I-iodophenpropit -100 5 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 165 2 2 2 1.0 N1CCC(CC1)Cc1[nH]cnc1 None
3035842 1983 34 3H-Histamine -100 5 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 165 2 2 2 1.0 N1CCC(CC1)Cc1[nH]cnc1 None
3035842 1983 34 3H-N-alpha-methylhistamine -100 5 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 165 2 2 2 1.0 N1CCC(CC1)Cc1[nH]cnc1 None
CHEMBL18661 1983 34 125I-iodophenpropit -100 5 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 165 2 2 2 1.0 N1CCC(CC1)Cc1[nH]cnc1 None
CHEMBL18661 1983 34 3H-Histamine -100 5 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 165 2 2 2 1.0 N1CCC(CC1)Cc1[nH]cnc1 None
CHEMBL18661 1983 34 3H-N-alpha-methylhistamine -100 5 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 165 2 2 2 1.0 N1CCC(CC1)Cc1[nH]cnc1 None
None 214502 0 125I-iodophenpropit -13 18 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 416 9 3 4 2.8 C1=CC(=CC=C1CCNC(N)SCCCC2=CN=CN2)I None
None 214502 0 3H-JNJ 7777120 -13 18 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 416 9 3 4 2.8 C1=CC(=CC=C1CCNC(N)SCCCC2=CN=CN2)I None
103 4089 56 3H-Histamine -89 53 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
2875 4089 56 3H-Histamine -89 53 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
5736 4089 56 3H-Histamine -89 53 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
CHEMBL285802 4089 56 3H-Histamine -89 53 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
DB09225 4089 56 3H-Histamine -89 53 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
135398737 944 89 3H-Histamine -57 91 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 944 89 3H-Histamine -57 91 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 944 89 3H-Histamine -57 91 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 944 89 3H-Histamine -57 91 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 944 89 3H-Histamine -57 91 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
1204 1901 114 3H-Histamine -3 23 Human 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
1247 1901 114 3H-Histamine -3 23 Human 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
1375 1901 114 3H-Histamine -3 23 Human 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
774 1901 114 3H-Histamine -3 23 Human 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
CHEMBL90 1901 114 3H-Histamine -3 23 Human 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
DB05381 1901 114 3H-Histamine -3 23 Human 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
11957573 1979 29 3H-Histamine -40 6 Human 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 170 3 3 3 0.6 NC(=N)SCCc1cnc[nH]1 None
1250 1979 29 3H-Histamine -40 6 Human 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 170 3 3 3 0.6 NC(=N)SCCc1cnc[nH]1 None
3692 1979 29 3H-Histamine -40 6 Human 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 170 3 3 3 0.6 NC(=N)SCCc1cnc[nH]1 None
CHEMBL19439 1979 29 3H-Histamine -40 6 Human 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 170 3 3 3 0.6 NC(=N)SCCc1cnc[nH]1 None
277 1274 55 3H-PYRILAMINE -301 45 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
2913 1274 55 3H-PYRILAMINE -301 45 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
765 1274 55 3H-PYRILAMINE -301 45 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
CHEMBL516 1274 55 3H-PYRILAMINE -301 45 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
DB00434 1274 55 3H-PYRILAMINE -301 45 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
1241 2006 46 3H-Histamine -89 5 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 125 2 1 3 -0.1 Cn1cc(nc1)CCN None
1242 2006 46 3H-Histamine -89 5 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 125 2 1 3 -0.1 Cn1cc(nc1)CCN None
3614 2006 46 3H-Histamine -89 5 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 125 2 1 3 -0.1 Cn1cc(nc1)CCN None
CHEMBL507 2006 46 3H-Histamine -89 5 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 125 2 1 3 -0.1 Cn1cc(nc1)CCN None
None 214372 0 3H-Histamine -7585 6 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 125 2 2 2 0.3 CC(CC1=CN=CN1)N None
100 3745 52 3H-Histamine -56 55 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
2637 3745 52 3H-Histamine -56 55 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
5452 3745 52 3H-Histamine -56 55 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
CHEMBL479 3745 52 3H-Histamine -56 55 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
DB00679 3745 52 3H-Histamine -56 55 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
1204 1901 114 125I-iodophenpropit -3 23 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
1247 1901 114 125I-iodophenpropit -3 23 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
1375 1901 114 125I-iodophenpropit -3 23 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
774 1901 114 125I-iodophenpropit -3 23 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
CHEMBL90 1901 114 125I-iodophenpropit -3 23 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
DB05381 1901 114 125I-iodophenpropit -3 23 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
1226 1988 16 3H-N-alpha-methylhistamine 2 6 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 321 9 4 4 1.2 NC(=NCCCc1cnc[nH]1)NCCSCc1nc[nH]c1C None
41376 1988 16 3H-N-alpha-methylhistamine 2 6 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 321 9 4 4 1.2 NC(=NCCCc1cnc[nH]1)NCCSCc1nc[nH]c1C None
CHEMBL12608 1988 16 3H-N-alpha-methylhistamine 2 6 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 321 9 4 4 1.2 NC(=NCCCc1cnc[nH]1)NCCSCc1nc[nH]c1C None
45037031 214395 0 3H-N-alpha-methylhistamine -70 4 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 285 2 2 2 1.5 C[C@H](CC1=CN=CN1)N.Br.Br None
1267 3744 43 3H-Histamine -33 25 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 None
3035905 3744 43 3H-Histamine -33 25 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 None
CHEMBL260374 3744 43 3H-Histamine -33 25 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 None
1210 905 45 3H-PYRILAMINE -186 20 Human 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C None
1213 905 45 3H-PYRILAMINE -186 20 Human 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C None
2725 905 45 3H-PYRILAMINE -186 20 Human 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C None
33036 905 45 3H-PYRILAMINE -186 20 Human 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C None
4411 905 45 3H-PYRILAMINE -186 20 Human 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C None
616 905 45 3H-PYRILAMINE -186 20 Human 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C None
6976 905 45 3H-PYRILAMINE -186 20 Human 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C None
716121 905 45 3H-PYRILAMINE -186 20 Human 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C None
90475904 905 45 3H-PYRILAMINE -186 20 Human 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C None
CHEMBL1201353 905 45 3H-PYRILAMINE -186 20 Human 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C None
CHEMBL1554789 905 45 3H-PYRILAMINE -186 20 Human 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C None
CHEMBL505 905 45 3H-PYRILAMINE -186 20 Human 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C None
DB01114 905 45 3H-PYRILAMINE -186 20 Human 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C None
DB13679 905 45 3H-PYRILAMINE -186 20 Human 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C None
135398737 944 89 125I-iodophenpropit -57 91 Human 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 944 89 125I-iodophenpropit -57 91 Human 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 944 89 125I-iodophenpropit -57 91 Human 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 944 89 125I-iodophenpropit -57 91 Human 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 944 89 125I-iodophenpropit -57 91 Human 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
1239 2002 23 3H-N-alpha-methylhistamine -154 5 Human 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 125 3 2 2 0.2 CNCCc1cnc[nH]1 None
1240 2002 23 3H-N-alpha-methylhistamine -154 5 Human 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 125 3 2 2 0.2 CNCCc1cnc[nH]1 None
912 2002 23 3H-N-alpha-methylhistamine -154 5 Human 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 125 3 2 2 0.2 CNCCc1cnc[nH]1 None
CHEMBL268490 2002 23 3H-N-alpha-methylhistamine -154 5 Human 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 125 3 2 2 0.2 CNCCc1cnc[nH]1 None
180 397 50 3H-PYRILAMINE -32 38 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
200 397 50 3H-PYRILAMINE -32 38 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
2160 397 50 3H-PYRILAMINE -32 38 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
CHEMBL629 397 50 3H-PYRILAMINE -32 38 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
DB00321 397 50 3H-PYRILAMINE -32 38 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
1204 1901 114 3H-PYRILAMINE -3 23 Human 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
1247 1901 114 3H-PYRILAMINE -3 23 Human 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
1375 1901 114 3H-PYRILAMINE -3 23 Human 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
774 1901 114 3H-PYRILAMINE -3 23 Human 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
CHEMBL90 1901 114 3H-PYRILAMINE -3 23 Human 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
DB05381 1901 114 3H-PYRILAMINE -3 23 Human 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
None 214372 0 3H-Histamine -7585 6 Human 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 125 2 2 2 0.3 CC(CC1=CN=CN1)N None
1248 1396 27 3H-Histamine -15 6 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 161 4 2 3 0.6 CN(CCCSC(=N)N)C None
3077 1396 27 3H-Histamine -15 6 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 161 4 2 3 0.6 CN(CCCSC(=N)N)C None
90045 1396 27 3H-Histamine -15 6 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 161 4 2 3 0.6 CN(CCCSC(=N)N)C None
CHEMBL12344 1396 27 3H-Histamine -15 6 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 161 4 2 3 0.6 CN(CCCSC(=N)N)C None
11957573 1979 29 3H-PYRILAMINE -40 6 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 170 3 3 3 0.6 NC(=N)SCCc1cnc[nH]1 None
1250 1979 29 3H-PYRILAMINE -40 6 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 170 3 3 3 0.6 NC(=N)SCCc1cnc[nH]1 None
3692 1979 29 3H-PYRILAMINE -40 6 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 170 3 3 3 0.6 NC(=N)SCCc1cnc[nH]1 None
CHEMBL19439 1979 29 3H-PYRILAMINE -40 6 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 170 3 3 3 0.6 NC(=N)SCCc1cnc[nH]1 None
921599 19255 44 3H-Histamine 234 2 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 229 1 2 2 1.2 O=C(c1cc2ccccc2[nH]1)N1CCNCC1 None
CHEMBL129660 19255 44 3H-Histamine 234 2 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 229 1 2 2 1.2 O=C(c1cc2ccccc2[nH]1)N1CCNCC1 None
1204 1901 114 3H-Histamine -3 23 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
1247 1901 114 3H-Histamine -3 23 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
1375 1901 114 3H-Histamine -3 23 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
774 1901 114 3H-Histamine -3 23 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
CHEMBL90 1901 114 3H-Histamine -3 23 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
DB05381 1901 114 3H-Histamine -3 23 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
1267 3744 43 125I-iodophenpropit -33 25 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 None
3035905 3744 43 125I-iodophenpropit -33 25 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 None
CHEMBL260374 3744 43 125I-iodophenpropit -33 25 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 None
3032915 15321 20 3H-Histamine -1 6 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 212 5 3 2 1.2 C/N=C(\S)NCCCCc1c[nH]cn1 None
3032915 15321 20 3H-N-alpha-methylhistamine -1 6 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 212 5 3 2 1.2 C/N=C(\S)NCCCCc1c[nH]cn1 None
CHEMBL12160 15321 20 3H-Histamine -1 6 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 212 5 3 2 1.2 C/N=C(\S)NCCCCc1c[nH]cn1 None
CHEMBL12160 15321 20 3H-N-alpha-methylhistamine -1 6 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 212 5 3 2 1.2 C/N=C(\S)NCCCCc1c[nH]cn1 None
135398737 944 89 3H-JNJ 7777120 -57 91 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 944 89 3H-JNJ 7777120 -57 91 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 944 89 3H-JNJ 7777120 -57 91 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 944 89 3H-JNJ 7777120 -57 91 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 944 89 3H-JNJ 7777120 -57 91 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
45073439 214396 0 3H-N-alpha-methylhistamine -75 4 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 285 2 2 2 1.5 C[C@@H](CC1=CN=CN1)N.Br.Br None
1224 1404 79 None -194 13 Human 8.4 pKi = 8.4 Binding
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
Drug Central 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C None
3100 1404 79 None -194 13 Human 8.4 pKi = 8.4 Binding
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
Drug Central 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C None
8980 1404 79 None -194 13 Human 8.4 pKi = 8.4 Binding
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
Drug Central 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C None
916 1404 79 None -194 13 Human 8.4 pKi = 8.4 Binding
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
Drug Central 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C None
CHEMBL657 1404 79 None -194 13 Human 8.4 pKi = 8.4 Binding
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
Drug Central 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C None
DB01075 1404 79 None -194 13 Human 8.4 pKi = 8.4 Binding
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
Drug Central 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C None
2782 31784 62 3H-PYRILAMINE - 1 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 325 4 0 3 4.3 Clc1ccc(Cn2c(CN3CCCC3)nc3ccccc32)cc1 None
CHEMBL1407943 31784 62 3H-PYRILAMINE - 1 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 325 4 0 3 4.3 Clc1ccc(Cn2c(CN3CCCC3)nc3ccccc32)cc1 None
CHEMBL3216363 31784 62 3H-PYRILAMINE - 1 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 325 4 0 3 4.3 Clc1ccc(Cn2c(CN3CCCC3)nc3ccccc32)cc1 None
1223 940 32 3H-Histamine -60 11 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 308 6 2 3 3.2 Clc1ccc(cc1)CN=C(SCCCc1cnc[nH]1)N None
2790 940 32 3H-Histamine -60 11 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 308 6 2 3 3.2 Clc1ccc(cc1)CN=C(SCCCc1cnc[nH]1)N None
CHEMBL14690 940 32 3H-Histamine -60 11 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 308 6 2 3 3.2 Clc1ccc(cc1)CN=C(SCCCc1cnc[nH]1)N None
4761 13330 39 3H-PYRILAMINE - 1 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 240 5 0 2 3.2 CN(C)CCC(c1ccccc1)c1ccccn1 None
CHEMBL1193 13330 39 3H-PYRILAMINE - 1 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 240 5 0 2 3.2 CN(C)CCC(c1ccccc1)c1ccccn1 None
CHEMBL1580221 13330 39 3H-PYRILAMINE - 1 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 240 5 0 2 3.2 CN(C)CCC(c1ccccc1)c1ccccn1 None
1267 3744 43 3H-Histamine -33 25 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 None
3035905 3744 43 3H-Histamine -33 25 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 None
CHEMBL260374 3744 43 3H-Histamine -33 25 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 None
1267 3744 43 3H-Histamine -33 25 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 None
3035905 3744 43 3H-Histamine -33 25 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 None
CHEMBL260374 3744 43 3H-Histamine -33 25 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 None
115237 55296 113 None -162 54 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 426 4 1 7 3.1 Cc1nc2n(c(=O)c1CCN1CCC(c3noc4cc(F)ccc34)CC1)CCCC2O None
CHEMBL1621 55296 113 None -162 54 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 426 4 1 7 3.1 Cc1nc2n(c(=O)c1CCN1CCC(c3noc4cc(F)ccc34)CC1)CCCC2O None
2247 502 77 None -117 41 Human 8.3 pKi = 8.3 Binding
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
Drug Central 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 None
249 502 77 None -117 41 Human 8.3 pKi = 8.3 Binding
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
Drug Central 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 None
2603 502 77 None -117 41 Human 8.3 pKi = 8.3 Binding
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
Drug Central 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 None
CHEMBL296419 502 77 None -117 41 Human 8.3 pKi = 8.3 Binding
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
Drug Central 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 None
DB00637 502 77 None -117 41 Human 8.3 pKi = 8.3 Binding
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
Drug Central 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 None
5625 215971 0 None - 1 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 456 6 3 6 2.7 CC(C)NC1=C(N=CC=C1)N1CCN(CC1)C(=O)C1=CC2=C(N1)C=CC(NS(C)(=O)=O)=C2 None
1613 2316 44 None -112 44 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
205 2316 44 None -112 44 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
3964 2316 44 None -112 44 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
CHEMBL831 2316 44 None -112 44 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
DB00408 2316 44 None -112 44 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
16106 117643 28 None -20 11 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 291 0 0 3 2.9 CN1CCN(C2=Nc3ccccc3Cc3ccccc32)CC1 None
CHEMBL340801 117643 28 None -20 11 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 291 0 0 3 2.9 CN1CCN(C2=Nc3ccccc3Cc3ccccc32)CC1 None
4761 13330 39 None - 1 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 240 5 0 2 3.2 CN(C)CCC(c1ccccc1)c1ccccn1 None
CHEMBL1193 13330 39 None - 1 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 240 5 0 2 3.2 CN(C)CCC(c1ccccc1)c1ccccn1 None
CHEMBL1580221 13330 39 None - 1 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 240 5 0 2 3.2 CN(C)CCC(c1ccccc1)c1ccccn1 None
135398737 944 89 None -54 91 Mouse 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 944 89 None -54 91 Mouse 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 944 89 None -54 91 Mouse 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 944 89 None -54 91 Mouse 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 944 89 None -54 91 Mouse 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
100 3745 52 None -56 55 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
2637 3745 52 None -56 55 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
5452 3745 52 None -56 55 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
CHEMBL479 3745 52 None -56 55 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
DB00679 3745 52 None -56 55 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
16362 3076 67 None -562 29 Human 8.2 pKi = 8.2 Binding
Antagonist activity at H4 receptor (unknown origin)Antagonist activity at H4 receptor (unknown origin)
Drug Central 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 None
2172 3076 67 None -562 29 Human 8.2 pKi = 8.2 Binding
Antagonist activity at H4 receptor (unknown origin)Antagonist activity at H4 receptor (unknown origin)
Drug Central 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 None
90 3076 67 None -562 29 Human 8.2 pKi = 8.2 Binding
Antagonist activity at H4 receptor (unknown origin)Antagonist activity at H4 receptor (unknown origin)
Drug Central 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 None
CHEMBL1423 3076 67 None -562 29 Human 8.2 pKi = 8.2 Binding
Antagonist activity at H4 receptor (unknown origin)Antagonist activity at H4 receptor (unknown origin)
Drug Central 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 None
DB01100 3076 67 None -562 29 Human 8.2 pKi = 8.2 Binding
Antagonist activity at H4 receptor (unknown origin)Antagonist activity at H4 receptor (unknown origin)
Drug Central 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 None
135398737 944 89 None -44 91 Rat 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 944 89 None -44 91 Rat 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 944 89 None -44 91 Rat 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 944 89 None -44 91 Rat 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 944 89 None -44 91 Rat 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
103 4089 56 None -89 53 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
2875 4089 56 None -89 53 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
5736 4089 56 None -89 53 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
CHEMBL285802 4089 56 None -89 53 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
DB09225 4089 56 None -89 53 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
2726 906 64 3H-PYRILAMINE -70 72 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
621 906 64 3H-PYRILAMINE -70 72 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
83 906 64 3H-PYRILAMINE -70 72 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
CHEMBL71 906 64 3H-PYRILAMINE -70 72 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
DB00477 906 64 3H-PYRILAMINE -70 72 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
2726 906 64 3H-Histamine -70 72 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
621 906 64 3H-Histamine -70 72 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
83 906 64 3H-Histamine -70 72 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
CHEMBL71 906 64 3H-Histamine -70 72 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
DB00477 906 64 3H-Histamine -70 72 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
1613 2316 44 3H-Histamine -112 44 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
205 2316 44 3H-Histamine -112 44 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
3964 2316 44 3H-Histamine -112 44 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
CHEMBL831 2316 44 3H-Histamine -112 44 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
DB00408 2316 44 3H-Histamine -112 44 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
135398737 944 89 3H-Histamine -57 91 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 944 89 3H-Histamine -57 91 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 944 89 3H-Histamine -57 91 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 944 89 3H-Histamine -57 91 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 944 89 3H-Histamine -57 91 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
11957573 1979 29 3H-N-alpha-methylhistamine -40 6 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 170 3 3 3 0.6 NC(=N)SCCc1cnc[nH]1 None
1250 1979 29 3H-N-alpha-methylhistamine -40 6 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 170 3 3 3 0.6 NC(=N)SCCc1cnc[nH]1 None
3692 1979 29 3H-N-alpha-methylhistamine -40 6 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 170 3 3 3 0.6 NC(=N)SCCc1cnc[nH]1 None
CHEMBL19439 1979 29 3H-N-alpha-methylhistamine -40 6 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 170 3 3 3 0.6 NC(=N)SCCc1cnc[nH]1 None
2782 31784 62 None - 1 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 325 4 0 3 4.3 Clc1ccc(Cn2c(CN3CCCC3)nc3ccccc32)cc1 None
CHEMBL1407943 31784 62 None - 1 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 325 4 0 3 4.3 Clc1ccc(Cn2c(CN3CCCC3)nc3ccccc32)cc1 None
CHEMBL3216363 31784 62 None - 1 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 325 4 0 3 4.3 Clc1ccc(Cn2c(CN3CCCC3)nc3ccccc32)cc1 None
1210 905 45 None -186 20 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C None
1213 905 45 None -186 20 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C None
2725 905 45 None -186 20 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C None
33036 905 45 None -186 20 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C None
4411 905 45 None -186 20 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C None
616 905 45 None -186 20 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C None
6976 905 45 None -186 20 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C None
716121 905 45 None -186 20 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C None
90475904 905 45 None -186 20 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C None
CHEMBL1201353 905 45 None -186 20 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C None
CHEMBL1554789 905 45 None -186 20 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C None
CHEMBL505 905 45 None -186 20 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C None
DB01114 905 45 None -186 20 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C None
DB13679 905 45 None -186 20 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C None
2286 3134 48 None -10 29 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C None
4927 3134 48 None -10 29 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C None
7282 3134 48 None -10 29 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C None
CHEMBL643 3134 48 None -10 29 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C None
DB01069 3134 48 None -10 29 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C None
2726 906 64 None -70 72 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
621 906 64 None -70 72 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
83 906 64 None -70 72 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
CHEMBL71 906 64 None -70 72 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
DB00477 906 64 None -70 72 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
1204 1901 114 None -15 23 Mouse 8.2 pKi = 8.2 Binding
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
Drug Central 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
1247 1901 114 None -15 23 Mouse 8.2 pKi = 8.2 Binding
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
Drug Central 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
1375 1901 114 None -15 23 Mouse 8.2 pKi = 8.2 Binding
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
Drug Central 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
774 1901 114 None -15 23 Mouse 8.2 pKi = 8.2 Binding
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
Drug Central 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
CHEMBL90 1901 114 None -15 23 Mouse 8.2 pKi = 8.2 Binding
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
Drug Central 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
DB05381 1901 114 None -15 23 Mouse 8.2 pKi = 8.2 Binding
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
Drug Central 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
1204 1901 114 None -12 23 Rat 8.1 pKi = 8.1 Binding
Binding affinity to rat histamine H4 receptor expressed in human SK-N-MC cells by radioligand displacement assayBinding affinity to rat histamine H4 receptor expressed in human SK-N-MC cells by radioligand displacement assay
Drug Central 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
1247 1901 114 None -12 23 Rat 8.1 pKi = 8.1 Binding
Binding affinity to rat histamine H4 receptor expressed in human SK-N-MC cells by radioligand displacement assayBinding affinity to rat histamine H4 receptor expressed in human SK-N-MC cells by radioligand displacement assay
Drug Central 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
1375 1901 114 None -12 23 Rat 8.1 pKi = 8.1 Binding
Binding affinity to rat histamine H4 receptor expressed in human SK-N-MC cells by radioligand displacement assayBinding affinity to rat histamine H4 receptor expressed in human SK-N-MC cells by radioligand displacement assay
Drug Central 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
774 1901 114 None -12 23 Rat 8.1 pKi = 8.1 Binding
Binding affinity to rat histamine H4 receptor expressed in human SK-N-MC cells by radioligand displacement assayBinding affinity to rat histamine H4 receptor expressed in human SK-N-MC cells by radioligand displacement assay
Drug Central 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
CHEMBL90 1901 114 None -12 23 Rat 8.1 pKi = 8.1 Binding
Binding affinity to rat histamine H4 receptor expressed in human SK-N-MC cells by radioligand displacement assayBinding affinity to rat histamine H4 receptor expressed in human SK-N-MC cells by radioligand displacement assay
Drug Central 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
DB05381 1901 114 None -12 23 Rat 8.1 pKi = 8.1 Binding
Binding affinity to rat histamine H4 receptor expressed in human SK-N-MC cells by radioligand displacement assayBinding affinity to rat histamine H4 receptor expressed in human SK-N-MC cells by radioligand displacement assay
Drug Central 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
1223 940 32 3H-Histamine -60 11 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 308 6 2 3 3.2 Clc1ccc(cc1)CN=C(SCCCc1cnc[nH]1)N None
1223 940 32 3H-N-alpha-methylhistamine -60 11 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 308 6 2 3 3.2 Clc1ccc(cc1)CN=C(SCCCc1cnc[nH]1)N None
2790 940 32 3H-Histamine -60 11 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 308 6 2 3 3.2 Clc1ccc(cc1)CN=C(SCCCc1cnc[nH]1)N None
2790 940 32 3H-N-alpha-methylhistamine -60 11 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 308 6 2 3 3.2 Clc1ccc(cc1)CN=C(SCCCc1cnc[nH]1)N None
CHEMBL14690 940 32 3H-Histamine -60 11 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 308 6 2 3 3.2 Clc1ccc(cc1)CN=C(SCCCc1cnc[nH]1)N None
CHEMBL14690 940 32 3H-N-alpha-methylhistamine -60 11 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 308 6 2 3 3.2 Clc1ccc(cc1)CN=C(SCCCc1cnc[nH]1)N None
135 2496 38 3H-PYRILAMINE -389 57 Human 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
1796 2496 38 3H-PYRILAMINE -389 57 Human 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
4184 2496 38 3H-PYRILAMINE -389 57 Human 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
CHEMBL6437 2496 38 3H-PYRILAMINE -389 57 Human 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
DB06148 2496 38 3H-PYRILAMINE -389 57 Human 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
1267 3744 43 3H-JNJ 7777120 -33 25 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 None
1267 3744 43 3H-JNJ-5207852 -33 25 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 None
3035905 3744 43 3H-JNJ 7777120 -33 25 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 None
3035905 3744 43 3H-JNJ-5207852 -33 25 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 None
CHEMBL260374 3744 43 3H-JNJ 7777120 -33 25 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 None
CHEMBL260374 3744 43 3H-JNJ-5207852 -33 25 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 None
1204 1901 114 None -3 23 Human 8.1 pKi = 8.1 Binding
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
Drug Central 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
1247 1901 114 None -3 23 Human 8.1 pKi = 8.1 Binding
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
Drug Central 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
1375 1901 114 None -3 23 Human 8.1 pKi = 8.1 Binding
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
Drug Central 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
774 1901 114 None -3 23 Human 8.1 pKi = 8.1 Binding
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
Drug Central 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
CHEMBL90 1901 114 None -3 23 Human 8.1 pKi = 8.1 Binding
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
Drug Central 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
DB05381 1901 114 None -3 23 Human 8.1 pKi = 8.1 Binding
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
Drug Central 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
1204 1901 114 3H-Histamine -3 23 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
1247 1901 114 3H-Histamine -3 23 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
1375 1901 114 3H-Histamine -3 23 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
774 1901 114 3H-Histamine -3 23 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
CHEMBL90 1901 114 3H-Histamine -3 23 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
DB05381 1901 114 3H-Histamine -3 23 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
180 397 50 None -32 38 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
200 397 50 None -32 38 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
2160 397 50 None -32 38 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
CHEMBL629 397 50 None -32 38 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
DB00321 397 50 None -32 38 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
277 1274 55 None -301 45 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
2913 1274 55 None -301 45 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
765 1274 55 None -301 45 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
CHEMBL516 1274 55 None -301 45 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
DB00434 1274 55 None -301 45 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
1204 1901 114 None 1 23 Guinea pig 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
1247 1901 114 None 1 23 Guinea pig 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
1375 1901 114 None 1 23 Guinea pig 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
774 1901 114 None 1 23 Guinea pig 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
CHEMBL90 1901 114 None 1 23 Guinea pig 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
DB05381 1901 114 None 1 23 Guinea pig 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
135398737 944 89 None -57 91 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 944 89 None -57 91 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 944 89 None -57 91 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 944 89 None -57 91 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 944 89 None -57 91 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
135398737 944 89 3H-Histamine -57 91 Human 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 944 89 3H-Histamine -57 91 Human 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 944 89 3H-Histamine -57 91 Human 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 944 89 3H-Histamine -57 91 Human 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 944 89 3H-Histamine -57 91 Human 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
135398737 944 89 3H-PYRILAMINE -57 91 Human 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 944 89 3H-PYRILAMINE -57 91 Human 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 944 89 3H-PYRILAMINE -57 91 Human 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 944 89 3H-PYRILAMINE -57 91 Human 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 944 89 3H-PYRILAMINE -57 91 Human 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
115237 55296 113 3H-Histamine -162 54 Human 5.1 pKi = 5.1 Binding
NoneNone
PDSP KiDatabase 426 4 1 7 3.1 Cc1nc2n(c(=O)c1CCN1CCC(c3noc4cc(F)ccc34)CC1)CCCC2O None
CHEMBL1621 55296 113 3H-Histamine -162 54 Human 5.1 pKi = 5.1 Binding
NoneNone
PDSP KiDatabase 426 4 1 7 3.1 Cc1nc2n(c(=O)c1CCN1CCC(c3noc4cc(F)ccc34)CC1)CCCC2O None
1251 1983 34 3H-Histamine -100 5 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 165 2 2 2 1.0 N1CCC(CC1)Cc1[nH]cnc1 None
3035842 1983 34 3H-Histamine -100 5 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 165 2 2 2 1.0 N1CCC(CC1)Cc1[nH]cnc1 None
CHEMBL18661 1983 34 3H-Histamine -100 5 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 165 2 2 2 1.0 N1CCC(CC1)Cc1[nH]cnc1 None
23650961 3785 18 None - 1 Human 7.1 pKi = 7.1 Binding
Displacament of histamine from human H4 recepotor expressed in mammalian cells.Displacament of histamine from human H4 recepotor expressed in mammalian cells.
Guide to Pharmacology 392 6 2 5 4.5 CN1CCC(CC1)CCCNc1ncc(c(n1)C)c1nc2c([nH]1)cc(cc2C)C None
9276 3785 18 None - 1 Human 7.1 pKi = 7.1 Binding
Displacament of histamine from human H4 recepotor expressed in mammalian cells.Displacament of histamine from human H4 recepotor expressed in mammalian cells.
Guide to Pharmacology 392 6 2 5 4.5 CN1CCC(CC1)CCCNc1ncc(c(n1)C)c1nc2c([nH]1)cc(cc2C)C None
CHEMBL3301609 3785 18 None - 1 Human 7.1 pKi = 7.1 Binding
Displacament of histamine from human H4 recepotor expressed in mammalian cells.Displacament of histamine from human H4 recepotor expressed in mammalian cells.
Guide to Pharmacology 392 6 2 5 4.5 CN1CCC(CC1)CCCNc1ncc(c(n1)C)c1nc2c([nH]1)cc(cc2C)C None
DB12522 3785 18 None - 1 Human 7.1 pKi = 7.1 Binding
Displacament of histamine from human H4 recepotor expressed in mammalian cells.Displacament of histamine from human H4 recepotor expressed in mammalian cells.
Guide to Pharmacology 392 6 2 5 4.5 CN1CCC(CC1)CCCNc1ncc(c(n1)C)c1nc2c([nH]1)cc(cc2C)C None
1265 929 54 None -2290 8 Human 5.7 pKi = 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 270 7 1 3 3.0 O=C(c1ccc(cc1)OCCCc1[nH]cnc1)C1CC1 12606603
1265 929 54 None -2290 8 Human 5.7 pKi = 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 270 7 1 3 3.0 O=C(c1ccc(cc1)OCCCc1[nH]cnc1)C1CC1 15294456
1265 929 54 None -2290 8 Human 5.7 pKi = 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 270 7 1 3 3.0 O=C(c1ccc(cc1)OCCCc1[nH]cnc1)C1CC1 26084539
6422124 929 54 None -2290 8 Human 5.7 pKi = 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 270 7 1 3 3.0 O=C(c1ccc(cc1)OCCCc1[nH]cnc1)C1CC1 12606603
6422124 929 54 None -2290 8 Human 5.7 pKi = 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 270 7 1 3 3.0 O=C(c1ccc(cc1)OCCCc1[nH]cnc1)C1CC1 15294456
6422124 929 54 None -2290 8 Human 5.7 pKi = 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 270 7 1 3 3.0 O=C(c1ccc(cc1)OCCCc1[nH]cnc1)C1CC1 26084539
CHEMBL14638 929 54 None -2290 8 Human 5.7 pKi = 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 270 7 1 3 3.0 O=C(c1ccc(cc1)OCCCc1[nH]cnc1)C1CC1 12606603
CHEMBL14638 929 54 None -2290 8 Human 5.7 pKi = 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 270 7 1 3 3.0 O=C(c1ccc(cc1)OCCCc1[nH]cnc1)C1CC1 15294456
CHEMBL14638 929 54 None -2290 8 Human 5.7 pKi = 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 270 7 1 3 3.0 O=C(c1ccc(cc1)OCCCc1[nH]cnc1)C1CC1 26084539
1267 3744 43 None -33 25 Human 7.0 pKi = 7.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 11179434
1267 3744 43 None -33 25 Human 7.0 pKi = 7.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 11179436
1267 3744 43 None -33 25 Human 7.0 pKi = 7.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 11181941
1267 3744 43 None -33 25 Human 7.0 pKi = 7.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 11561071
1267 3744 43 None -33 25 Human 7.0 pKi = 7.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 12606603
1267 3744 43 None -33 25 Human 7.0 pKi = 7.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 15294456
3035905 3744 43 None -33 25 Human 7.0 pKi = 7.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 11179434
3035905 3744 43 None -33 25 Human 7.0 pKi = 7.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 11179436
3035905 3744 43 None -33 25 Human 7.0 pKi = 7.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 11181941
3035905 3744 43 None -33 25 Human 7.0 pKi = 7.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 11561071
3035905 3744 43 None -33 25 Human 7.0 pKi = 7.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 12606603
3035905 3744 43 None -33 25 Human 7.0 pKi = 7.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 15294456
CHEMBL260374 3744 43 None -33 25 Human 7.0 pKi = 7.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 11179434
CHEMBL260374 3744 43 None -33 25 Human 7.0 pKi = 7.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 11179436
CHEMBL260374 3744 43 None -33 25 Human 7.0 pKi = 7.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 11181941
CHEMBL260374 3744 43 None -33 25 Human 7.0 pKi = 7.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 11561071
CHEMBL260374 3744 43 None -33 25 Human 7.0 pKi = 7.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 12606603
CHEMBL260374 3744 43 None -33 25 Human 7.0 pKi = 7.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 15294456
10446295 2101 29 None 269 2 Human 7.1 pKi = 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 278 1 1 3 1.6 CN1CCN(CC1)C(=O)c1nc2c([nH]1)cc(cc2)Cl 15454206
1277 2101 29 None 269 2 Human 7.1 pKi = 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 278 1 1 3 1.6 CN1CCN(CC1)C(=O)c1nc2c([nH]1)cc(cc2)Cl 15454206
CHEMBL185951 2101 29 None 269 2 Human 7.1 pKi = 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 278 1 1 3 1.6 CN1CCN(CC1)C(=O)c1nc2c([nH]1)cc(cc2)Cl 15454206
1223 940 32 None -338 11 Rat 7.2 pKi = 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 308 6 2 3 3.2 Clc1ccc(cc1)CN=C(SCCCc1cnc[nH]1)N 11561071
2790 940 32 None -338 11 Rat 7.2 pKi = 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 308 6 2 3 3.2 Clc1ccc(cc1)CN=C(SCCCc1cnc[nH]1)N 11561071
CHEMBL14690 940 32 None -338 11 Rat 7.2 pKi = 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 308 6 2 3 3.2 Clc1ccc(cc1)CN=C(SCCCc1cnc[nH]1)N 11561071
1274 4001 12 None 19 2 Human 7.5 pKi = 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 161 3 4 3 -1.1 NC(=N)SCCN=C(N)N 17154494
3063228 4001 12 None 19 2 Human 7.5 pKi = 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 161 3 4 3 -1.1 NC(=N)SCCN=C(N)N 17154494
CHEMBL1196470 4001 12 None 19 2 Human 7.5 pKi = 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 161 3 4 3 -1.1 NC(=N)SCCN=C(N)N 17154494
1269 121 33 None 213 3 Human 7.8 pKi = 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 125 2 2 2 0.2 Cc1c(CCN)nc[nH]1 15947036
1269 121 33 None 213 3 Human 7.8 pKi = 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 125 2 2 2 0.2 Cc1c(CCN)nc[nH]1 16432504
37463 121 33 None 213 3 Human 7.8 pKi = 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 125 2 2 2 0.2 Cc1c(CCN)nc[nH]1 15947036
37463 121 33 None 213 3 Human 7.8 pKi = 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 125 2 2 2 0.2 Cc1c(CCN)nc[nH]1 16432504
CHEMBL275443 121 33 None 213 3 Human 7.8 pKi = 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 125 2 2 2 0.2 Cc1c(CCN)nc[nH]1 15947036
CHEMBL275443 121 33 None 213 3 Human 7.8 pKi = 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 125 2 2 2 0.2 Cc1c(CCN)nc[nH]1 16432504
1223 940 32 None -363 11 Mouse 7.8 pKi = 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 308 6 2 3 3.2 Clc1ccc(cc1)CN=C(SCCCc1cnc[nH]1)N 11561071
2790 940 32 None -363 11 Mouse 7.8 pKi = 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 308 6 2 3 3.2 Clc1ccc(cc1)CN=C(SCCCc1cnc[nH]1)N 11561071
CHEMBL14690 940 32 None -363 11 Mouse 7.8 pKi = 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 308 6 2 3 3.2 Clc1ccc(cc1)CN=C(SCCCc1cnc[nH]1)N 11561071
1223 940 32 None -60 11 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 308 6 2 3 3.2 Clc1ccc(cc1)CN=C(SCCCc1cnc[nH]1)N 11179434
1223 940 32 None -60 11 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 308 6 2 3 3.2 Clc1ccc(cc1)CN=C(SCCCc1cnc[nH]1)N 11181941
1223 940 32 None -60 11 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 308 6 2 3 3.2 Clc1ccc(cc1)CN=C(SCCCc1cnc[nH]1)N 11561071
1223 940 32 None -60 11 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 308 6 2 3 3.2 Clc1ccc(cc1)CN=C(SCCCc1cnc[nH]1)N 12606603
1223 940 32 None -60 11 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 308 6 2 3 3.2 Clc1ccc(cc1)CN=C(SCCCc1cnc[nH]1)N 15947036
2790 940 32 None -60 11 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 308 6 2 3 3.2 Clc1ccc(cc1)CN=C(SCCCc1cnc[nH]1)N 11179434
2790 940 32 None -60 11 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 308 6 2 3 3.2 Clc1ccc(cc1)CN=C(SCCCc1cnc[nH]1)N 11181941
2790 940 32 None -60 11 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 308 6 2 3 3.2 Clc1ccc(cc1)CN=C(SCCCc1cnc[nH]1)N 11561071
2790 940 32 None -60 11 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 308 6 2 3 3.2 Clc1ccc(cc1)CN=C(SCCCc1cnc[nH]1)N 12606603
2790 940 32 None -60 11 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 308 6 2 3 3.2 Clc1ccc(cc1)CN=C(SCCCc1cnc[nH]1)N 15947036
CHEMBL14690 940 32 None -60 11 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 308 6 2 3 3.2 Clc1ccc(cc1)CN=C(SCCCc1cnc[nH]1)N 11179434
CHEMBL14690 940 32 None -60 11 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 308 6 2 3 3.2 Clc1ccc(cc1)CN=C(SCCCc1cnc[nH]1)N 11181941
CHEMBL14690 940 32 None -60 11 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 308 6 2 3 3.2 Clc1ccc(cc1)CN=C(SCCCc1cnc[nH]1)N 11561071
CHEMBL14690 940 32 None -60 11 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 308 6 2 3 3.2 Clc1ccc(cc1)CN=C(SCCCc1cnc[nH]1)N 12606603
CHEMBL14690 940 32 None -60 11 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 308 6 2 3 3.2 Clc1ccc(cc1)CN=C(SCCCc1cnc[nH]1)N 15947036
24994634 2111 26 None -2 7 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 221 2 2 5 0.7 N[C@@H]1CCN(C1)c1cc(nc(n1)N)C(C)C 24495018
24994634 2111 26 None -2 7 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 221 2 2 5 0.7 N[C@@H]1CCN(C1)c1cc(nc(n1)N)C(C)C 26084539
8984 2111 26 None -2 7 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 221 2 2 5 0.7 N[C@@H]1CCN(C1)c1cc(nc(n1)N)C(C)C 24495018
8984 2111 26 None -2 7 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 221 2 2 5 0.7 N[C@@H]1CCN(C1)c1cc(nc(n1)N)C(C)C 26084539
CHEMBL3236549 2111 26 None -2 7 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 221 2 2 5 0.7 N[C@@H]1CCN(C1)c1cc(nc(n1)N)C(C)C 24495018
CHEMBL3236549 2111 26 None -2 7 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 221 2 2 5 0.7 N[C@@H]1CCN(C1)c1cc(nc(n1)N)C(C)C 26084539
45257132 3626 3 None 42 4 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 366 4 2 6 2.7 CN1CCN(CC1)c1cc(NCc2c(Cl)cccc2Cl)nc(n1)N 26084539
8983 3626 3 None 42 4 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 366 4 2 6 2.7 CN1CCN(CC1)c1cc(NCc2c(Cl)cccc2Cl)nc(n1)N 26084539
CHEMBL595180 3626 3 None 42 4 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 366 4 2 6 2.7 CN1CCN(CC1)c1cc(NCc2c(Cl)cccc2Cl)nc(n1)N 26084539
1278 2119 79 None -3 8 Human 8.1 pKi = 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 14722321
1278 2119 79 None -3 8 Human 8.1 pKi = 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 15947036
1278 2119 79 None -3 8 Human 8.1 pKi = 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 16854056
1279 2119 79 None -3 8 Human 8.1 pKi = 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 14722321
1279 2119 79 None -3 8 Human 8.1 pKi = 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 15947036
1279 2119 79 None -3 8 Human 8.1 pKi = 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 16854056
4908365 2119 79 None -3 8 Human 8.1 pKi = 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 14722321
4908365 2119 79 None -3 8 Human 8.1 pKi = 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 15947036
4908365 2119 79 None -3 8 Human 8.1 pKi = 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 16854056
CHEMBL129198 2119 79 None -3 8 Human 8.1 pKi = 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 14722321
CHEMBL129198 2119 79 None -3 8 Human 8.1 pKi = 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 15947036
CHEMBL129198 2119 79 None -3 8 Human 8.1 pKi = 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 16854056
117072554 1992 0 None 81 4 Human 8.3 pKi = 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 450 5 2 6 2.3 CN1CCN(CC1)C1=CC(=NC(N1)N)c1ccc2c(c1)CN(CC2)C(=O)CCC1CCCC1 26084539
8982 1992 0 None 81 4 Human 8.3 pKi = 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 450 5 2 6 2.3 CN1CCN(CC1)C1=CC(=NC(N1)N)c1ccc2c(c1)CN(CC2)C(=O)CCC1CCCC1 26084539
24745335 292 7 None 4 5 Human 8.3 pKi = 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 262 5 3 6 0.7 CN[C@@H]1CCN(C1)c1cc(NCC2CC2)nc(n1)N 26084539
8985 292 7 None 4 5 Human 8.3 pKi = 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 262 5 3 6 0.7 CN[C@@H]1CCN(C1)c1cc(NCC2CC2)nc(n1)N 26084539
CHEMBL1915540 292 7 None 4 5 Human 8.3 pKi = 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 262 5 3 6 0.7 CN[C@@H]1CCN(C1)c1cc(NCC2CC2)nc(n1)N 26084539
DB15027 292 7 None 4 5 Human 8.3 pKi = 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 262 5 3 6 0.7 CN[C@@H]1CCN(C1)c1cc(NCC2CC2)nc(n1)N 26084539
5048 3084 57 None -48977 7 Human 4.0 pKi > 4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 295 8 0 2 4.2 Clc1ccc(cc1)CCCOCCCN1CCCCC1 26084539
8924 3084 57 None -48977 7 Human 4.0 pKi > 4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 295 8 0 2 4.2 Clc1ccc(cc1)CCCOCCCN1CCCCC1 26084539
9948102 3084 57 None -48977 7 Human 4.0 pKi > 4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 295 8 0 2 4.2 Clc1ccc(cc1)CCCOCCCN1CCCCC1 26084539
CHEMBL462605 3084 57 None -48977 7 Human 4.0 pKi > 4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 295 8 0 2 4.2 Clc1ccc(cc1)CCCOCCCN1CCCCC1 26084539
DB11642 3084 57 None -48977 7 Human 4.0 pKi > 4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 295 8 0 2 4.2 Clc1ccc(cc1)CCCOCCCN1CCCCC1 26084539
441082 1140 40 None -2137 8 Human 5.0 pKi > 5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 356 1 0 2 4.8 CN([C@H]1CC[C@]2(C(=CC[C@@H]3[C@@H]2CC[C@]24[C@H]3CC[C@@H]4[C@@H](N(C2)C)C)C1)C)C 26084539
8981 1140 40 None -2137 8 Human 5.0 pKi > 5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 356 1 0 2 4.8 CN([C@H]1CC[C@]2(C(=CC[C@@H]3[C@@H]2CC[C@]24[C@H]3CC[C@@H]4[C@@H](N(C2)C)C)C1)C)C 26084539
CHEMBL191703 1140 40 None -2137 8 Human 5.0 pKi > 5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 356 1 0 2 4.8 CN([C@H]1CC[C@]2(C(=CC[C@@H]3[C@@H]2CC[C@]24[C@H]3CC[C@@H]4[C@@H](N(C2)C)C)C1)C)C 26084539
11697697 2510 19 None -6309 6 Human 5.0 pKi > 5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 431 6 0 5 4.6 Cc1nc2cccc(c2c(=O)n1c1ccc(cc1)OCCCN1CCCC1)C(F)(F)F 26084539
7346 2510 19 None -6309 6 Human 5.0 pKi > 5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 431 6 0 5 4.6 Cc1nc2cccc(c2c(=O)n1c1ccc(cc1)OCCCN1CCCC1)C(F)(F)F 26084539
CHEMBL476323 2510 19 None -6309 6 Human 5.0 pKi > 5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 431 6 0 5 4.6 Cc1nc2cccc(c2c(=O)n1c1ccc(cc1)OCCCN1CCCC1)C(F)(F)F 26084539
DB11910 2510 19 None -6309 6 Human 5.0 pKi > 5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 431 6 0 5 4.6 Cc1nc2cccc(c2c(=O)n1c1ccc(cc1)OCCCN1CCCC1)C(F)(F)F 26084539
1547484 927 70 None -5 20 Human 8.2 pKi None 8.2 Binding
NoneNone
Drug Central 368 6 0 2 5.1 c1ccc(cc1)/C=C/CN1CCN(CC1)C(c1ccccc1)c1ccccc1 None
654 927 70 None -5 20 Human 8.2 pKi None 8.2 Binding
NoneNone
Drug Central 368 6 0 2 5.1 c1ccc(cc1)/C=C/CN1CCN(CC1)C(c1ccccc1)c1ccccc1 None
9072 927 70 None -5 20 Human 8.2 pKi None 8.2 Binding
NoneNone
Drug Central 368 6 0 2 5.1 c1ccc(cc1)/C=C/CN1CCN(CC1)C(c1ccccc1)c1ccccc1 None
CHEMBL43064 927 70 None -5 20 Human 8.2 pKi None 8.2 Binding
NoneNone
Drug Central 368 6 0 2 5.1 c1ccc(cc1)/C=C/CN1CCN(CC1)C(c1ccccc1)c1ccccc1 None
DB00568 927 70 None -5 20 Human 8.2 pKi None 8.2 Binding
NoneNone
Drug Central 368 6 0 2 5.1 c1ccc(cc1)/C=C/CN1CCN(CC1)C(c1ccccc1)c1ccccc1 None
10058807 1987 2 None -1 2 Human 5.2 pKi None 5.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 206 4 3 3 -0.0 CN=C(NC#N)NCCCc1cnc[nH]1 11179436
1276 1987 2 None -1 2 Human 5.2 pKi None 5.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 206 4 3 3 -0.0 CN=C(NC#N)NCCCc1cnc[nH]1 11179436
CHEMBL2261340 1987 2 None -1 2 Human 5.2 pKi None 5.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 206 4 3 3 -0.0 CN=C(NC#N)NCCCc1cnc[nH]1 11179436
135398737 944 89 None -54 91 Mouse 5.5 pKi None 5.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 11561071
38 944 89 None -54 91 Mouse 5.5 pKi None 5.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 11561071
722 944 89 None -54 91 Mouse 5.5 pKi None 5.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 11561071
CHEMBL42 944 89 None -54 91 Mouse 5.5 pKi None 5.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 11561071
DB00363 944 89 None -54 91 Mouse 5.5 pKi None 5.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 11561071
1238 2051 11 None -19 3 Human 5.5 pKi None 5.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 125 2 2 2 0.3 C[C@@H](Cc1cnc[nH]1)N 11181941
6603865 2051 11 None -19 3 Human 5.5 pKi None 5.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 125 2 2 2 0.3 C[C@@H](Cc1cnc[nH]1)N 11181941
CHEMBL11919 2051 11 None -19 3 Human 5.5 pKi None 5.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 125 2 2 2 0.3 C[C@@H](Cc1cnc[nH]1)N 11181941
1248 1396 27 None -15 6 Human 5.7 pKi None 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 161 4 2 3 0.6 CN(CCCSC(=N)N)C 11179434
1248 1396 27 None -15 6 Human 5.7 pKi None 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 161 4 2 3 0.6 CN(CCCSC(=N)N)C 11179436
1248 1396 27 None -15 6 Human 5.7 pKi None 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 161 4 2 3 0.6 CN(CCCSC(=N)N)C 11181941
1248 1396 27 None -15 6 Human 5.7 pKi None 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 161 4 2 3 0.6 CN(CCCSC(=N)N)C 15947036
3077 1396 27 None -15 6 Human 5.7 pKi None 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 161 4 2 3 0.6 CN(CCCSC(=N)N)C 11179434
3077 1396 27 None -15 6 Human 5.7 pKi None 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 161 4 2 3 0.6 CN(CCCSC(=N)N)C 11179436
3077 1396 27 None -15 6 Human 5.7 pKi None 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 161 4 2 3 0.6 CN(CCCSC(=N)N)C 11181941
3077 1396 27 None -15 6 Human 5.7 pKi None 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 161 4 2 3 0.6 CN(CCCSC(=N)N)C 15947036
90045 1396 27 None -15 6 Human 5.7 pKi None 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 161 4 2 3 0.6 CN(CCCSC(=N)N)C 11179434
90045 1396 27 None -15 6 Human 5.7 pKi None 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 161 4 2 3 0.6 CN(CCCSC(=N)N)C 11179436
90045 1396 27 None -15 6 Human 5.7 pKi None 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 161 4 2 3 0.6 CN(CCCSC(=N)N)C 11181941
90045 1396 27 None -15 6 Human 5.7 pKi None 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 161 4 2 3 0.6 CN(CCCSC(=N)N)C 15947036
CHEMBL12344 1396 27 None -15 6 Human 5.7 pKi None 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 161 4 2 3 0.6 CN(CCCSC(=N)N)C 11179434
CHEMBL12344 1396 27 None -15 6 Human 5.7 pKi None 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 161 4 2 3 0.6 CN(CCCSC(=N)N)C 11179436
CHEMBL12344 1396 27 None -15 6 Human 5.7 pKi None 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 161 4 2 3 0.6 CN(CCCSC(=N)N)C 11181941
CHEMBL12344 1396 27 None -15 6 Human 5.7 pKi None 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 161 4 2 3 0.6 CN(CCCSC(=N)N)C 15947036
135398737 944 89 None -44 91 Rat 5.7 pKi None 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 11561071
38 944 89 None -44 91 Rat 5.7 pKi None 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 11561071
722 944 89 None -44 91 Rat 5.7 pKi None 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 11561071
CHEMBL42 944 89 None -44 91 Rat 5.7 pKi None 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 11561071
DB00363 944 89 None -44 91 Rat 5.7 pKi None 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 11561071
11313837 2464 7 None -1995 2 Human 5.7 pKi None 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 179 2 1 2 1.3 CN1CCC(CC1)Cc1[nH]cnc1 15771452
1254 2464 7 None -1995 2 Human 5.7 pKi None 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 179 2 1 2 1.3 CN1CCC(CC1)Cc1[nH]cnc1 15771452
CHEMBL175782 2464 7 None -1995 2 Human 5.7 pKi None 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 179 2 1 2 1.3 CN1CCC(CC1)Cc1[nH]cnc1 15771452
124846 1915 0 None - 1 Human 5.9 pKi None 5.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 382 10 3 3 4.1 CC(NCCc1cnc[nH]1)CCCCC(=O)Nc1ccc(cc1)C(F)(F)F 11179436
1273 1915 0 None - 1 Human 5.9 pKi None 5.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 382 10 3 3 4.1 CC(NCCc1cnc[nH]1)CCCCC(=O)Nc1ccc(cc1)C(F)(F)F 11179436
CHEMBL67601 1915 0 None - 1 Human 5.9 pKi None 5.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 382 10 3 3 4.1 CC(NCCc1cnc[nH]1)CCCCC(=O)Nc1ccc(cc1)C(F)(F)F 11179436
12656 2009 0 None - 1 Human 5.9 pKi None 5.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 139 3 1 2 0.5 CN(CCc1[nH]cnc1)C 16432504
1270 2009 0 None - 1 Human 5.9 pKi None 5.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 139 3 1 2 0.5 CN(CCc1[nH]cnc1)C 16432504
CHEMBL12704 2009 0 None - 1 Human 5.9 pKi None 5.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 139 3 1 2 0.5 CN(CCc1[nH]cnc1)C 16432504
1194 46 3 None -1318 4 Human 6.0 pKi None 6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 265 3 2 2 2.3 NCCc1cnc([nH]1)c1cccc(c1)Br 15947036
23786499 46 3 None -1318 4 Human 6.0 pKi None 6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 265 3 2 2 2.3 NCCc1cnc([nH]1)c1cccc(c1)Br 15947036
CHEMBL26116 46 3 None -1318 4 Human 6.0 pKi None 6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 265 3 2 2 2.3 NCCc1cnc([nH]1)c1cccc(c1)Br 15947036
1229 732 0 None -19 6 Rat 6.0 pKi None 6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 262 5 3 2 2.0 CNC(=S)NCCCCc1cccc2c1cn[nH]2 11561071
5311293 732 0 None -19 6 Rat 6.0 pKi None 6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 262 5 3 2 2.0 CNC(=S)NCCCCc1cccc2c1cn[nH]2 11561071
1229 732 0 None -15 6 Mouse 6.1 pKi None 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 262 5 3 2 2.0 CNC(=S)NCCCCc1cccc2c1cn[nH]2 11561071
5311293 732 0 None -15 6 Mouse 6.1 pKi None 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 262 5 3 2 2.0 CNC(=S)NCCCCc1cccc2c1cn[nH]2 11561071
1236 2036 23 None -851 7 Rat 6.2 pKi None 6.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 125 2 2 2 0.3 C[C@H](Cc1cnc[nH]1)N 11561071
1237 2036 23 None -851 7 Rat 6.2 pKi None 6.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 125 2 2 2 0.3 C[C@H](Cc1cnc[nH]1)N 11561071
156615 2036 23 None -851 7 Rat 6.2 pKi None 6.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 125 2 2 2 0.3 C[C@H](Cc1cnc[nH]1)N 11561071
CHEMBL268229 2036 23 None -851 7 Rat 6.2 pKi None 6.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 125 2 2 2 0.3 C[C@H](Cc1cnc[nH]1)N 11561071
1241 2006 46 None -407 5 Rat 6.3 pKi None 6.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 125 2 1 3 -0.1 Cn1cc(nc1)CCN 11561071
1242 2006 46 None -407 5 Rat 6.3 pKi None 6.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 125 2 1 3 -0.1 Cn1cc(nc1)CCN 11561071
3614 2006 46 None -407 5 Rat 6.3 pKi None 6.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 125 2 1 3 -0.1 Cn1cc(nc1)CCN 11561071
CHEMBL507 2006 46 None -407 5 Rat 6.3 pKi None 6.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 125 2 1 3 -0.1 Cn1cc(nc1)CCN 11561071
1268 82 0 None - 1 Human 6.4 pKi None 6.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 221 4 3 5 -2.0 OCCN1CN(CO)C(=S)N(C1)CO 15947036
1268 82 0 None - 1 Human 6.4 pKi None 6.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 221 4 3 5 -2.0 OCCN1CN(CO)C(=S)N(C1)CO 16432504
92613 82 0 None - 1 Human 6.4 pKi None 6.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 221 4 3 5 -2.0 OCCN1CN(CO)C(=S)N(C1)CO 15947036
92613 82 0 None - 1 Human 6.4 pKi None 6.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 221 4 3 5 -2.0 OCCN1CN(CO)C(=S)N(C1)CO 16432504
1236 2036 23 None -537 7 Mouse 6.4 pKi None 6.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 125 2 2 2 0.3 C[C@H](Cc1cnc[nH]1)N 11561071
1237 2036 23 None -537 7 Mouse 6.4 pKi None 6.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 125 2 2 2 0.3 C[C@H](Cc1cnc[nH]1)N 11561071
156615 2036 23 None -537 7 Mouse 6.4 pKi None 6.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 125 2 2 2 0.3 C[C@H](Cc1cnc[nH]1)N 11561071
CHEMBL268229 2036 23 None -537 7 Mouse 6.4 pKi None 6.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 125 2 2 2 0.3 C[C@H](Cc1cnc[nH]1)N 11561071
135398737 944 89 None -57 91 Human 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 11179434
135398737 944 89 None -57 91 Human 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 11179436
135398737 944 89 None -57 91 Human 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 11561071
135398737 944 89 None -57 91 Human 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 15947036
38 944 89 None -57 91 Human 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 11179434
38 944 89 None -57 91 Human 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 11179436
38 944 89 None -57 91 Human 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 11561071
38 944 89 None -57 91 Human 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 15947036
722 944 89 None -57 91 Human 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 11179434
722 944 89 None -57 91 Human 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 11179436
722 944 89 None -57 91 Human 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 11561071
722 944 89 None -57 91 Human 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 15947036
CHEMBL42 944 89 None -57 91 Human 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 11179434
CHEMBL42 944 89 None -57 91 Human 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 11179436
CHEMBL42 944 89 None -57 91 Human 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 11561071
CHEMBL42 944 89 None -57 91 Human 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 15947036
DB00363 944 89 None -57 91 Human 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 11179434
DB00363 944 89 None -57 91 Human 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 11179436
DB00363 944 89 None -57 91 Human 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 11561071
DB00363 944 89 None -57 91 Human 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 15947036
1241 2006 46 None -257 5 Mouse 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 125 2 1 3 -0.1 Cn1cc(nc1)CCN 11561071
1242 2006 46 None -257 5 Mouse 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 125 2 1 3 -0.1 Cn1cc(nc1)CCN 11561071
3614 2006 46 None -257 5 Mouse 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 125 2 1 3 -0.1 Cn1cc(nc1)CCN 11561071
CHEMBL507 2006 46 None -257 5 Mouse 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 125 2 1 3 -0.1 Cn1cc(nc1)CCN 11561071
1236 2036 23 None -204 7 Human 6.7 pKi None 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 125 2 2 2 0.3 C[C@H](Cc1cnc[nH]1)N 11179434
1236 2036 23 None -204 7 Human 6.7 pKi None 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 125 2 2 2 0.3 C[C@H](Cc1cnc[nH]1)N 11179436
1236 2036 23 None -204 7 Human 6.7 pKi None 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 125 2 2 2 0.3 C[C@H](Cc1cnc[nH]1)N 11181941
1236 2036 23 None -204 7 Human 6.7 pKi None 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 125 2 2 2 0.3 C[C@H](Cc1cnc[nH]1)N 11561071
1237 2036 23 None -204 7 Human 6.7 pKi None 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 125 2 2 2 0.3 C[C@H](Cc1cnc[nH]1)N 11179434
1237 2036 23 None -204 7 Human 6.7 pKi None 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 125 2 2 2 0.3 C[C@H](Cc1cnc[nH]1)N 11179436
1237 2036 23 None -204 7 Human 6.7 pKi None 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 125 2 2 2 0.3 C[C@H](Cc1cnc[nH]1)N 11181941
1237 2036 23 None -204 7 Human 6.7 pKi None 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 125 2 2 2 0.3 C[C@H](Cc1cnc[nH]1)N 11561071
156615 2036 23 None -204 7 Human 6.7 pKi None 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 125 2 2 2 0.3 C[C@H](Cc1cnc[nH]1)N 11179434
156615 2036 23 None -204 7 Human 6.7 pKi None 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 125 2 2 2 0.3 C[C@H](Cc1cnc[nH]1)N 11179436
156615 2036 23 None -204 7 Human 6.7 pKi None 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 125 2 2 2 0.3 C[C@H](Cc1cnc[nH]1)N 11181941
156615 2036 23 None -204 7 Human 6.7 pKi None 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 125 2 2 2 0.3 C[C@H](Cc1cnc[nH]1)N 11561071
CHEMBL268229 2036 23 None -204 7 Human 6.7 pKi None 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 125 2 2 2 0.3 C[C@H](Cc1cnc[nH]1)N 11179434
CHEMBL268229 2036 23 None -204 7 Human 6.7 pKi None 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 125 2 2 2 0.3 C[C@H](Cc1cnc[nH]1)N 11179436
CHEMBL268229 2036 23 None -204 7 Human 6.7 pKi None 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 125 2 2 2 0.3 C[C@H](Cc1cnc[nH]1)N 11181941
CHEMBL268229 2036 23 None -204 7 Human 6.7 pKi None 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 125 2 2 2 0.3 C[C@H](Cc1cnc[nH]1)N 11561071
1271 2005 0 None - 1 Human 6.7 pKi None 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 139 3 1 3 0.4 NCCc1ncn(c1)CC 16432504
44292270 2005 0 None - 1 Human 6.7 pKi None 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 139 3 1 3 0.4 NCCc1ncn(c1)CC 16432504
CHEMBL46296 2005 0 None - 1 Human 6.7 pKi None 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 139 3 1 3 0.4 NCCc1ncn(c1)CC 16432504
1239 2002 23 None -154 5 Human 7.0 pKi None 7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 125 3 2 2 0.2 CNCCc1cnc[nH]1 11179436
1239 2002 23 None -154 5 Human 7.0 pKi None 7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 125 3 2 2 0.2 CNCCc1cnc[nH]1 11181941
1240 2002 23 None -154 5 Human 7.0 pKi None 7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 125 3 2 2 0.2 CNCCc1cnc[nH]1 11179436
1240 2002 23 None -154 5 Human 7.0 pKi None 7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 125 3 2 2 0.2 CNCCc1cnc[nH]1 11181941
912 2002 23 None -154 5 Human 7.0 pKi None 7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 125 3 2 2 0.2 CNCCc1cnc[nH]1 11179436
912 2002 23 None -154 5 Human 7.0 pKi None 7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 125 3 2 2 0.2 CNCCc1cnc[nH]1 11181941
CHEMBL268490 2002 23 None -154 5 Human 7.0 pKi None 7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 125 3 2 2 0.2 CNCCc1cnc[nH]1 11179436
CHEMBL268490 2002 23 None -154 5 Human 7.0 pKi None 7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 125 3 2 2 0.2 CNCCc1cnc[nH]1 11181941
1229 732 0 None -1 6 Human 7.1 pKi None 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 262 5 3 2 2.0 CNC(=S)NCCCCc1cccc2c1cn[nH]2 11179434
1229 732 0 None -1 6 Human 7.1 pKi None 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 262 5 3 2 2.0 CNC(=S)NCCCCc1cccc2c1cn[nH]2 11179436
1229 732 0 None -1 6 Human 7.1 pKi None 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 262 5 3 2 2.0 CNC(=S)NCCCCc1cccc2c1cn[nH]2 11181941
1229 732 0 None -1 6 Human 7.1 pKi None 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 262 5 3 2 2.0 CNC(=S)NCCCCc1cccc2c1cn[nH]2 11561071
1229 732 0 None -1 6 Human 7.1 pKi None 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 262 5 3 2 2.0 CNC(=S)NCCCCc1cccc2c1cn[nH]2 15947036
5311293 732 0 None -1 6 Human 7.1 pKi None 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 262 5 3 2 2.0 CNC(=S)NCCCCc1cccc2c1cn[nH]2 11179434
5311293 732 0 None -1 6 Human 7.1 pKi None 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 262 5 3 2 2.0 CNC(=S)NCCCCc1cccc2c1cn[nH]2 11179436
5311293 732 0 None -1 6 Human 7.1 pKi None 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 262 5 3 2 2.0 CNC(=S)NCCCCc1cccc2c1cn[nH]2 11181941
5311293 732 0 None -1 6 Human 7.1 pKi None 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 262 5 3 2 2.0 CNC(=S)NCCCCc1cccc2c1cn[nH]2 11561071
5311293 732 0 None -1 6 Human 7.1 pKi None 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 262 5 3 2 2.0 CNC(=S)NCCCCc1cccc2c1cn[nH]2 15947036
1204 1901 114 None -12 23 Rat 7.2 pKi None 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 11561071
1247 1901 114 None -12 23 Rat 7.2 pKi None 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 11561071
1375 1901 114 None -12 23 Rat 7.2 pKi None 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 11561071
774 1901 114 None -12 23 Rat 7.2 pKi None 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 11561071
CHEMBL90 1901 114 None -12 23 Rat 7.2 pKi None 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 11561071
DB05381 1901 114 None -12 23 Rat 7.2 pKi None 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 11561071
1204 1901 114 None -15 23 Mouse 7.4 pKi None 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 11561071
1247 1901 114 None -15 23 Mouse 7.4 pKi None 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 11561071
1375 1901 114 None -15 23 Mouse 7.4 pKi None 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 11561071
774 1901 114 None -15 23 Mouse 7.4 pKi None 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 11561071
CHEMBL90 1901 114 None -15 23 Mouse 7.4 pKi None 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 11561071
DB05381 1901 114 None -15 23 Mouse 7.4 pKi None 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 11561071
1241 2006 46 None -89 5 Human 7.5 pKi None 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 125 2 1 3 -0.1 Cn1cc(nc1)CCN 11179434
1241 2006 46 None -89 5 Human 7.5 pKi None 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 125 2 1 3 -0.1 Cn1cc(nc1)CCN 11561071
1241 2006 46 None -89 5 Human 7.5 pKi None 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 125 2 1 3 -0.1 Cn1cc(nc1)CCN 16432504
1242 2006 46 None -89 5 Human 7.5 pKi None 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 125 2 1 3 -0.1 Cn1cc(nc1)CCN 11179434
1242 2006 46 None -89 5 Human 7.5 pKi None 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 125 2 1 3 -0.1 Cn1cc(nc1)CCN 11561071
1242 2006 46 None -89 5 Human 7.5 pKi None 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 125 2 1 3 -0.1 Cn1cc(nc1)CCN 16432504
3614 2006 46 None -89 5 Human 7.5 pKi None 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 125 2 1 3 -0.1 Cn1cc(nc1)CCN 11179434
3614 2006 46 None -89 5 Human 7.5 pKi None 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 125 2 1 3 -0.1 Cn1cc(nc1)CCN 11561071
3614 2006 46 None -89 5 Human 7.5 pKi None 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 125 2 1 3 -0.1 Cn1cc(nc1)CCN 16432504
CHEMBL507 2006 46 None -89 5 Human 7.5 pKi None 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 125 2 1 3 -0.1 Cn1cc(nc1)CCN 11179434
CHEMBL507 2006 46 None -89 5 Human 7.5 pKi None 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 125 2 1 3 -0.1 Cn1cc(nc1)CCN 11561071
CHEMBL507 2006 46 None -89 5 Human 7.5 pKi None 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 125 2 1 3 -0.1 Cn1cc(nc1)CCN 16432504
1267 3744 43 None -21 25 Mouse 7.6 pKi None 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 11561071
1267 3744 43 None -14 25 Rat 7.6 pKi None 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 11561071
3035905 3744 43 None -21 25 Mouse 7.6 pKi None 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 11561071
3035905 3744 43 None -14 25 Rat 7.6 pKi None 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 11561071
CHEMBL260374 3744 43 None -21 25 Mouse 7.6 pKi None 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 11561071
CHEMBL260374 3744 43 None -14 25 Rat 7.6 pKi None 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 11561071
1266 2026 0 None -23 3 Human 7.7 pKi None 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 416 9 3 4 2.8 N[C@H](SCCCc1cnc[nH]1)NCCc1ccc(cc1)I 11179436
3960 2026 0 None -23 3 Human 7.7 pKi None 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 416 9 3 4 2.8 N[C@H](SCCCc1cnc[nH]1)NCCc1ccc(cc1)I 11179436
5311186 2026 0 None -23 3 Human 7.7 pKi None 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 416 9 3 4 2.8 N[C@H](SCCCc1cnc[nH]1)NCCc1ccc(cc1)I 11179436
1226 1988 16 None 2 6 Human 7.8 pKi None 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 321 9 4 4 1.2 NC(=NCCCc1cnc[nH]1)NCCSCc1nc[nH]c1C 11179434
1226 1988 16 None 2 6 Human 7.8 pKi None 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 321 9 4 4 1.2 NC(=NCCCc1cnc[nH]1)NCCSCc1nc[nH]c1C 15947036
41376 1988 16 None 2 6 Human 7.8 pKi None 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 321 9 4 4 1.2 NC(=NCCCc1cnc[nH]1)NCCSCc1nc[nH]c1C 11179434
41376 1988 16 None 2 6 Human 7.8 pKi None 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 321 9 4 4 1.2 NC(=NCCCc1cnc[nH]1)NCCSCc1nc[nH]c1C 15947036
CHEMBL12608 1988 16 None 2 6 Human 7.8 pKi None 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 321 9 4 4 1.2 NC(=NCCCc1cnc[nH]1)NCCSCc1nc[nH]c1C 11179434
CHEMBL12608 1988 16 None 2 6 Human 7.8 pKi None 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 321 9 4 4 1.2 NC(=NCCCc1cnc[nH]1)NCCSCc1nc[nH]c1C 15947036
1251 1983 34 None -100 5 Human 7.8 pKi None 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 165 2 2 2 1.0 N1CCC(CC1)Cc1[nH]cnc1 11179434
1251 1983 34 None -100 5 Human 7.8 pKi None 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 165 2 2 2 1.0 N1CCC(CC1)Cc1[nH]cnc1 11179436
1251 1983 34 None -100 5 Human 7.8 pKi None 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 165 2 2 2 1.0 N1CCC(CC1)Cc1[nH]cnc1 14640553
3035842 1983 34 None -100 5 Human 7.8 pKi None 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 165 2 2 2 1.0 N1CCC(CC1)Cc1[nH]cnc1 11179434
3035842 1983 34 None -100 5 Human 7.8 pKi None 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 165 2 2 2 1.0 N1CCC(CC1)Cc1[nH]cnc1 11179436
3035842 1983 34 None -100 5 Human 7.8 pKi None 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 165 2 2 2 1.0 N1CCC(CC1)Cc1[nH]cnc1 14640553
CHEMBL18661 1983 34 None -100 5 Human 7.8 pKi None 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 165 2 2 2 1.0 N1CCC(CC1)Cc1[nH]cnc1 11179434
CHEMBL18661 1983 34 None -100 5 Human 7.8 pKi None 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 165 2 2 2 1.0 N1CCC(CC1)Cc1[nH]cnc1 11179436
CHEMBL18661 1983 34 None -100 5 Human 7.8 pKi None 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 165 2 2 2 1.0 N1CCC(CC1)Cc1[nH]cnc1 14640553
1204 1901 114 None -3 23 Human 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 11179434
1204 1901 114 None -3 23 Human 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 11179436
1204 1901 114 None -3 23 Human 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 11181941
1204 1901 114 None -3 23 Human 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 11561071
1204 1901 114 None -3 23 Human 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 15454206
1204 1901 114 None -3 23 Human 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 15947036
1204 1901 114 None -3 23 Human 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 16432504
1247 1901 114 None -3 23 Human 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 11179434
1247 1901 114 None -3 23 Human 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 11179436
1247 1901 114 None -3 23 Human 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 11181941
1247 1901 114 None -3 23 Human 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 11561071
1247 1901 114 None -3 23 Human 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 15454206
1247 1901 114 None -3 23 Human 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 15947036
1247 1901 114 None -3 23 Human 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 16432504
1375 1901 114 None -3 23 Human 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 11179434
1375 1901 114 None -3 23 Human 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 11179436
1375 1901 114 None -3 23 Human 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 11181941
1375 1901 114 None -3 23 Human 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 11561071
1375 1901 114 None -3 23 Human 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 15454206
1375 1901 114 None -3 23 Human 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 15947036
1375 1901 114 None -3 23 Human 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 16432504
774 1901 114 None -3 23 Human 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 11179434
774 1901 114 None -3 23 Human 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 11179436
774 1901 114 None -3 23 Human 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 11181941
774 1901 114 None -3 23 Human 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 11561071
774 1901 114 None -3 23 Human 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 15454206
774 1901 114 None -3 23 Human 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 15947036
774 1901 114 None -3 23 Human 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 16432504
CHEMBL90 1901 114 None -3 23 Human 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 11179434
CHEMBL90 1901 114 None -3 23 Human 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 11179436
CHEMBL90 1901 114 None -3 23 Human 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 11181941
CHEMBL90 1901 114 None -3 23 Human 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 11561071
CHEMBL90 1901 114 None -3 23 Human 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 15454206
CHEMBL90 1901 114 None -3 23 Human 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 15947036
CHEMBL90 1901 114 None -3 23 Human 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 16432504
DB05381 1901 114 None -3 23 Human 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 11179434
DB05381 1901 114 None -3 23 Human 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 11179436
DB05381 1901 114 None -3 23 Human 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 11181941
DB05381 1901 114 None -3 23 Human 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 11561071
DB05381 1901 114 None -3 23 Human 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 15454206
DB05381 1901 114 None -3 23 Human 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 15947036
DB05381 1901 114 None -3 23 Human 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 16432504
11957573 1979 29 None -27 6 Mouse 8.2 pKi None 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 170 3 3 3 0.6 NC(=N)SCCc1cnc[nH]1 11561071
11957573 1979 29 None -27 6 Rat 8.2 pKi None 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 170 3 3 3 0.6 NC(=N)SCCc1cnc[nH]1 11561071
1250 1979 29 None -27 6 Mouse 8.2 pKi None 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 170 3 3 3 0.6 NC(=N)SCCc1cnc[nH]1 11561071
1250 1979 29 None -27 6 Rat 8.2 pKi None 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 170 3 3 3 0.6 NC(=N)SCCc1cnc[nH]1 11561071
3692 1979 29 None -27 6 Mouse 8.2 pKi None 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 170 3 3 3 0.6 NC(=N)SCCc1cnc[nH]1 11561071
3692 1979 29 None -27 6 Rat 8.2 pKi None 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 170 3 3 3 0.6 NC(=N)SCCc1cnc[nH]1 11561071
CHEMBL19439 1979 29 None -27 6 Mouse 8.2 pKi None 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 170 3 3 3 0.6 NC(=N)SCCc1cnc[nH]1 11561071
CHEMBL19439 1979 29 None -27 6 Rat 8.2 pKi None 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 170 3 3 3 0.6 NC(=N)SCCc1cnc[nH]1 11561071
11957573 1979 29 None -40 6 Human 8.6 pKi None 8.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 170 3 3 3 0.6 NC(=N)SCCc1cnc[nH]1 11179434
11957573 1979 29 None -40 6 Human 8.6 pKi None 8.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 170 3 3 3 0.6 NC(=N)SCCc1cnc[nH]1 11179436
11957573 1979 29 None -40 6 Human 8.6 pKi None 8.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 170 3 3 3 0.6 NC(=N)SCCc1cnc[nH]1 11181941
11957573 1979 29 None -40 6 Human 8.6 pKi None 8.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 170 3 3 3 0.6 NC(=N)SCCc1cnc[nH]1 11561071
1250 1979 29 None -40 6 Human 8.6 pKi None 8.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 170 3 3 3 0.6 NC(=N)SCCc1cnc[nH]1 11179434
1250 1979 29 None -40 6 Human 8.6 pKi None 8.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 170 3 3 3 0.6 NC(=N)SCCc1cnc[nH]1 11179436
1250 1979 29 None -40 6 Human 8.6 pKi None 8.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 170 3 3 3 0.6 NC(=N)SCCc1cnc[nH]1 11181941
1250 1979 29 None -40 6 Human 8.6 pKi None 8.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 170 3 3 3 0.6 NC(=N)SCCc1cnc[nH]1 11561071
3692 1979 29 None -40 6 Human 8.6 pKi None 8.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 170 3 3 3 0.6 NC(=N)SCCc1cnc[nH]1 11179434
3692 1979 29 None -40 6 Human 8.6 pKi None 8.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 170 3 3 3 0.6 NC(=N)SCCc1cnc[nH]1 11179436
3692 1979 29 None -40 6 Human 8.6 pKi None 8.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 170 3 3 3 0.6 NC(=N)SCCc1cnc[nH]1 11181941
3692 1979 29 None -40 6 Human 8.6 pKi None 8.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 170 3 3 3 0.6 NC(=N)SCCc1cnc[nH]1 11561071
CHEMBL19439 1979 29 None -40 6 Human 8.6 pKi None 8.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 170 3 3 3 0.6 NC(=N)SCCc1cnc[nH]1 11179434
CHEMBL19439 1979 29 None -40 6 Human 8.6 pKi None 8.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 170 3 3 3 0.6 NC(=N)SCCc1cnc[nH]1 11179436
CHEMBL19439 1979 29 None -40 6 Human 8.6 pKi None 8.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 170 3 3 3 0.6 NC(=N)SCCc1cnc[nH]1 11181941
CHEMBL19439 1979 29 None -40 6 Human 8.6 pKi None 8.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 170 3 3 3 0.6 NC(=N)SCCc1cnc[nH]1 11561071