Ligand source activities (1 row/activity)





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DOI

155524115 176547 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 176547 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 176547 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 176547 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 176547 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 176547 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 176547 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 176547 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 176547 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 6604 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 6604 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 176451 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 176451 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 176451 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 176451 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 176451 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 176451 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 176320 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 176320 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 176320 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 176320 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 58889 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 58889 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 176495 4 None -10 4 Mouse 9.0 pEC50 = 9 Functional
Agonist activity at mouse H4R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by luciferase reporter gene assayAgonist activity at mouse H4R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by luciferase reporter gene assay
ChEMBL 207 4 2 5 0.2 CCCNC1CN(c2ccnc(N)n2)C1 10.1021/acs.jmedchem.9b01462
CHEMBL4441731 176495 4 None -10 4 Mouse 9.0 pEC50 = 9 Functional
Agonist activity at mouse H4R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by luciferase reporter gene assayAgonist activity at mouse H4R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by luciferase reporter gene assay
ChEMBL 207 4 2 5 0.2 CCCNC1CN(c2ccnc(N)n2)C1 10.1021/acs.jmedchem.9b01462
CHEMBL4596734 176495 4 None -10 4 Mouse 9.0 pEC50 = 9 Functional
Agonist activity at mouse H4R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by luciferase reporter gene assayAgonist activity at mouse H4R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by luciferase reporter gene assay
ChEMBL 207 4 2 5 0.2 CCCNC1CN(c2ccnc(N)n2)C1 10.1021/acs.jmedchem.9b01462
155513612 176320 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 176320 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 176320 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 176320 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 176451 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 176451 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 176451 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 3682 10 None - 1 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 366 4 2 6 2.7 CN1CCN(CC1)c1cc(NCc2c(Cl)cccc2Cl)nc(n1)N 10.1016/j.bmc.2009.08.059
8983 3682 10 None - 1 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 366 4 2 6 2.7 CN1CCN(CC1)c1cc(NCc2c(Cl)cccc2Cl)nc(n1)N 10.1016/j.bmc.2009.08.059
CHEMBL595180 3682 10 None - 1 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 366 4 2 6 2.7 CN1CCN(CC1)c1cc(NCc2c(Cl)cccc2Cl)nc(n1)N 10.1016/j.bmc.2009.08.059
155552061 176478 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 176478 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 176478 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 176667 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 176667 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 176667 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 3682 10 None - 1 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of GTPase by [gamma-32P]GTP spontaneous degradation assayAgonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of GTPase by [gamma-32P]GTP spontaneous degradation assay
ChEMBL 366 4 2 6 2.7 CN1CCN(CC1)c1cc(NCc2c(Cl)cccc2Cl)nc(n1)N 10.1016/j.bmc.2009.08.059
8983 3682 10 None - 1 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of GTPase by [gamma-32P]GTP spontaneous degradation assayAgonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of GTPase by [gamma-32P]GTP spontaneous degradation assay
ChEMBL 366 4 2 6 2.7 CN1CCN(CC1)c1cc(NCc2c(Cl)cccc2Cl)nc(n1)N 10.1016/j.bmc.2009.08.059
CHEMBL595180 3682 10 None - 1 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of GTPase by [gamma-32P]GTP spontaneous degradation assayAgonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of GTPase by [gamma-32P]GTP spontaneous degradation assay
ChEMBL 366 4 2 6 2.7 CN1CCN(CC1)c1cc(NCc2c(Cl)cccc2Cl)nc(n1)N 10.1016/j.bmc.2009.08.059
58227373 176508 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 176508 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 176508 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 176320 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 176320 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 176320 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 176320 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 56482 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 56482 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 56482 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 56482 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 188438 19 None -1 2 Rat 8.0 pEC50 = 8 Functional
Antagonist activity at rat histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assayAntagonist activity at rat histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assay
ChEMBL 295 1 2 5 1.8 Nc1nc2c(c(N3CC[C@@H](N)C3)n1)CCCc1ccccc1-2 10.1021/jm800670r
CHEMBL502347 188438 19 None -1 2 Rat 8.0 pEC50 = 8 Functional
Antagonist activity at rat histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assayAntagonist activity at rat histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assay
ChEMBL 295 1 2 5 1.8 Nc1nc2c(c(N3CC[C@@H](N)C3)n1)CCCc1ccccc1-2 10.1021/jm800670r
10105117 104195 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 104195 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 140200 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 140200 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 56481 3 None 1 3 Human 7.0 pEC50 = 7 Functional
Agonist activity at human recombinant histamine H4 receptor expressed in human SK-N-MC cells co-expressing SRE-Luc by luciferase reporter gene assayAgonist activity at human recombinant histamine H4 receptor expressed in human SK-N-MC cells co-expressing SRE-Luc by luciferase reporter gene assay
ChEMBL 271 2 2 3 3.0 Cc1ccc2[nH]c(/C(=N\O)C3CCN(C)CC3)cc2c1 10.1016/j.bmcl.2010.10.041
CHEMBL1632412 56481 3 None 1 3 Human 7.0 pEC50 = 7 Functional
Agonist activity at human recombinant histamine H4 receptor expressed in human SK-N-MC cells co-expressing SRE-Luc by luciferase reporter gene assayAgonist activity at human recombinant histamine H4 receptor expressed in human SK-N-MC cells co-expressing SRE-Luc by luciferase reporter gene assay
ChEMBL 271 2 2 3 3.0 Cc1ccc2[nH]c(/C(=N\O)C3CCN(C)CC3)cc2c1 10.1016/j.bmcl.2010.10.041
4024 2015 20 None -3388 2 Human 6.0 pEC50 = 6 Functional
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 159 2 1 2 1.4 n1ccc(cc1)Cc1c[nH]cn1 10.1016/j.bmcl.2010.10.041
9989505 2015 20 None -3388 2 Human 6.0 pEC50 = 6 Functional
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 159 2 1 2 1.4 n1ccc(cc1)Cc1c[nH]cn1 10.1016/j.bmcl.2010.10.041
CHEMBL82298 2015 20 None -3388 2 Human 6.0 pEC50 = 6 Functional
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 159 2 1 2 1.4 n1ccc(cc1)Cc1c[nH]cn1 10.1016/j.bmcl.2010.10.041
58227259 117142 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 117142 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 45 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 45 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 45 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 61562 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 61562 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 139220 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 139220 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 200176 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 200176 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 187626 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 187626 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 187563 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 187563 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 187595 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 187595 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 187626 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 187626 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 78680 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 78680 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 202145 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 202145 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 187629 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 187629 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 3804 49 None -17 5 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19 protein by steady-state GTPase assayAgonist activity at human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19 protein by steady-state GTPase assay
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1021/jm900526h
3035905 3804 49 None -17 5 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19 protein by steady-state GTPase assayAgonist activity at human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19 protein by steady-state GTPase assay
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1021/jm900526h
CHEMBL260374 3804 49 None -17 5 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19 protein by steady-state GTPase assayAgonist activity at human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19 protein by steady-state GTPase assay
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1021/jm900526h
44480708 5775 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 5775 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 61526 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 61526 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 1932 119 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 1932 119 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 1932 119 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 1932 119 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 1932 119 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 1932 119 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 140238 3 None 10 2 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human histamine H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assayAgonist activity at human histamine H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 368 7 3 4 3.1 N#C/N=C(/NCCSc1ccccc1)NC[C@H]1CC[C@H](c2c[nH]cn2)C1 10.1021/acs.jmedchem.6b00120
CHEMBL3805361 140238 3 None 10 2 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human histamine H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assayAgonist activity at human histamine H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 368 7 3 4 3.1 N#C/N=C(/NCCSc1ccccc1)NC[C@H]1CC[C@H](c2c[nH]cn2)C1 10.1021/acs.jmedchem.6b00120
1204 1932 119 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 1932 119 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 1932 119 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 1932 119 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 1932 119 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 1932 119 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 199908 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 199908 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 140242 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 140242 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 140247 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 140247 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 140315 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 140315 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 117122 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 117122 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 187333 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 187333 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 187583 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 187583 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 188402 38 None -2 2 Rat 6.9 pEC50 = 6.9 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 193 1 1 5 -0.2 CN1CCN(c2ccnc(N)n2)CC1 10.1021/jm8005959
CHEMBL501882 188402 38 None -2 2 Rat 6.9 pEC50 = 6.9 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 193 1 1 5 -0.2 CN1CCN(c2ccnc(N)n2)CC1 10.1021/jm8005959
25128831 172613 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 172613 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 56479 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 56479 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 188418 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 188418 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 140315 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 140315 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 61558 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 61558 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 1932 119 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 1932 119 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 1932 119 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 1932 119 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 1932 119 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 1932 119 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 187254 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 187254 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 2010 34 None -54 5 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human histamine H4 receptorAgonist activity at human histamine H4 receptor
ChEMBL 170 3 3 3 0.6 NC(=N)SCCc1cnc[nH]1 10.1021/jm100064d
1250 2010 34 None -54 5 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human histamine H4 receptorAgonist activity at human histamine H4 receptor
ChEMBL 170 3 3 3 0.6 NC(=N)SCCc1cnc[nH]1 10.1021/jm100064d
3692 2010 34 None -54 5 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human histamine H4 receptorAgonist activity at human histamine H4 receptor
ChEMBL 170 3 3 3 0.6 NC(=N)SCCc1cnc[nH]1 10.1021/jm100064d
CHEMBL19439 2010 34 None -54 5 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human histamine H4 receptorAgonist activity at human histamine H4 receptor
ChEMBL 170 3 3 3 0.6 NC(=N)SCCc1cnc[nH]1 10.1021/jm100064d
11957573 2010 34 None -54 5 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 170 3 3 3 0.6 NC(=N)SCCc1cnc[nH]1 10.1016/j.bmcl.2010.10.041
1250 2010 34 None -54 5 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 170 3 3 3 0.6 NC(=N)SCCc1cnc[nH]1 10.1016/j.bmcl.2010.10.041
3692 2010 34 None -54 5 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 170 3 3 3 0.6 NC(=N)SCCc1cnc[nH]1 10.1016/j.bmcl.2010.10.041
CHEMBL19439 2010 34 None -54 5 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 170 3 3 3 0.6 NC(=N)SCCc1cnc[nH]1 10.1016/j.bmcl.2010.10.041
1253 2058 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 2058 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 2058 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 4063 16 None -25 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 184 4 3 3 1.0 NC(=N)SCCCc1cnc[nH]1 10.1016/j.bmcl.2010.10.041
1246 4063 16 None -25 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 184 4 3 3 1.0 NC(=N)SCCCc1cnc[nH]1 10.1016/j.bmcl.2010.10.041
CHEMBL281576 4063 16 None -25 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 184 4 3 3 1.0 NC(=N)SCCCc1cnc[nH]1 10.1016/j.bmcl.2010.10.041
1204 1932 119 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 1932 119 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 1932 119 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 1932 119 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 1932 119 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 1932 119 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 3804 49 None -17 5 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1021/acs.jmedchem.0c00160
3035905 3804 49 None -17 5 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1021/acs.jmedchem.0c00160
CHEMBL260374 3804 49 None -17 5 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1021/acs.jmedchem.0c00160
44482032 5732 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 5732 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 187225 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 187225 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 5636 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 5636 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 187662 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 187662 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 187587 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 187587 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 187587 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 187587 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 187403 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 187403 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 140304 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 140304 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 58892 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 58892 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 108577 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 108577 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 103786 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 103786 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 2082 13 None -1258 2 Human 4.9 pEC50 = 4.9 Functional
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 125 2 2 2 0.3 C[C@@H](Cc1cnc[nH]1)N 10.1016/j.bmcl.2010.10.041
6603865 2082 13 None -1258 2 Human 4.9 pEC50 = 4.9 Functional
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 125 2 2 2 0.3 C[C@@H](Cc1cnc[nH]1)N 10.1016/j.bmcl.2010.10.041
CHEMBL11919 2082 13 None -1258 2 Human 4.9 pEC50 = 4.9 Functional
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 125 2 2 2 0.3 C[C@@H](Cc1cnc[nH]1)N 10.1016/j.bmcl.2010.10.041
11043445 56479 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 56479 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 109629 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 109629 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 5763 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 5763 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 109629 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 109629 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 140302 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 140302 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 1932 119 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 1932 119 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 1932 119 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 1932 119 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 1932 119 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 1932 119 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 108577 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 108577 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 187283 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 187283 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 140238 3 None 10 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human histamine H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assayAgonist activity at human histamine H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 368 7 3 4 3.1 N#C/N=C(/NCCSc1ccccc1)NC[C@H]1CC[C@H](c2c[nH]cn2)C1 10.1021/acs.jmedchem.6b00120
CHEMBL3805361 140238 3 None 10 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human histamine H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assayAgonist activity at human histamine H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 368 7 3 4 3.1 N#C/N=C(/NCCSc1ccccc1)NC[C@H]1CC[C@H](c2c[nH]cn2)C1 10.1021/acs.jmedchem.6b00120
11846634 78009 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 78009 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 78460 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 78460 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 189062 14 None 1 2 Rat 7.8 pEC50 = 7.8 Functional
Antagonist activity at rat histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assayAntagonist activity at rat histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assay
ChEMBL 295 1 2 5 1.6 Nc1nc2c(c(N3CCNCC3)n1)CCCc1ccccc1-2 10.1021/jm800670r
CHEMBL509540 189062 14 None 1 2 Rat 7.8 pEC50 = 7.8 Functional
Antagonist activity at rat histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assayAntagonist activity at rat histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assay
ChEMBL 295 1 2 5 1.6 Nc1nc2c(c(N3CCNCC3)n1)CCCc1ccccc1-2 10.1021/jm800670r
44482030 5675 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 5675 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 187404 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 187404 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 187628 13 None - 1 Rat 5.8 pEC50 = 5.8 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 209 1 2 6 -0.5 CN1CCN(c2cc(O)nc(N)n2)CC1 10.1021/jm8005959
CHEMBL494909 187628 13 None - 1 Rat 5.8 pEC50 = 5.8 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 209 1 2 6 -0.5 CN1CCN(c2cc(O)nc(N)n2)CC1 10.1021/jm8005959
127048828 140320 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 140320 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 117125 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 117125 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 187183 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 187183 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 187481 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 187481 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 2014 39 None -204 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human histamine H4 receptorAgonist activity at human histamine H4 receptor
ChEMBL 165 2 2 2 1.0 N1CCC(CC1)Cc1[nH]cnc1 10.1021/jm100064d
3035842 2014 39 None -204 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human histamine H4 receptorAgonist activity at human histamine H4 receptor
ChEMBL 165 2 2 2 1.0 N1CCC(CC1)Cc1[nH]cnc1 10.1021/jm100064d
CHEMBL18661 2014 39 None -204 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human histamine H4 receptorAgonist activity at human histamine H4 receptor
ChEMBL 165 2 2 2 1.0 N1CCC(CC1)Cc1[nH]cnc1 10.1021/jm100064d
1251 2014 39 None -204 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 165 2 2 2 1.0 N1CCC(CC1)Cc1[nH]cnc1 10.1016/j.bmcl.2010.10.041
3035842 2014 39 None -204 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 165 2 2 2 1.0 N1CCC(CC1)Cc1[nH]cnc1 10.1016/j.bmcl.2010.10.041
CHEMBL18661 2014 39 None -204 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 165 2 2 2 1.0 N1CCC(CC1)Cc1[nH]cnc1 10.1016/j.bmcl.2010.10.041
25149712 178986 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 178986 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 184225 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 184225 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 2150 84 None 1 4 Human 7.8 pEC50 = 7.8 Functional
Inverse agonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of [35S]GTPgammaS bindingInverse agonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1016/j.bmc.2009.08.059
1279 2150 84 None 1 4 Human 7.8 pEC50 = 7.8 Functional
Inverse agonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of [35S]GTPgammaS bindingInverse agonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1016/j.bmc.2009.08.059
4908365 2150 84 None 1 4 Human 7.8 pEC50 = 7.8 Functional
Inverse agonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of [35S]GTPgammaS bindingInverse agonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1016/j.bmc.2009.08.059
CHEMBL129198 2150 84 None 1 4 Human 7.8 pEC50 = 7.8 Functional
Inverse agonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of [35S]GTPgammaS bindingInverse agonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1016/j.bmc.2009.08.059
127048890 140295 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 140295 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 6584 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 6584 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 5774 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 5774 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 58892 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 58892 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 176320 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 176320 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 176320 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 176320 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 1932 119 None -102 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 1932 119 None -102 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 1932 119 None -102 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 1932 119 None -102 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 1932 119 None -102 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 1932 119 None -102 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 1424 28 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 161 4 2 3 0.6 CN(CCCSC(=N)N)C 10.1016/j.bmcl.2010.10.041
3077 1424 28 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 161 4 2 3 0.6 CN(CCCSC(=N)N)C 10.1016/j.bmcl.2010.10.041
90045 1424 28 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 161 4 2 3 0.6 CN(CCCSC(=N)N)C 10.1016/j.bmcl.2010.10.041
CHEMBL12344 1424 28 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 161 4 2 3 0.6 CN(CCCSC(=N)N)C 10.1016/j.bmcl.2010.10.041
5310982 93612 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 93612 4 None -3 2 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human recombinant histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2 by steady-state GTPase activity assayAgonist activity at human recombinant histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2 by steady-state GTPase activity assay
ChEMBL 255 3 2 2 2.6 NCCc1c[nH]c(-c2cccc(C(F)(F)F)c2)n1 10.1016/j.bmcl.2010.10.041
1269 121 41 None -35 6 Mouse 5.8 pEC50 = 5.8 Functional
Agonist activity at mouse histamine H4 receptorAgonist activity at mouse histamine H4 receptor
ChEMBL 125 2 2 2 0.2 Cc1c(CCN)nc[nH]1 10.1016/j.bmcl.2010.10.041
37463 121 41 None -35 6 Mouse 5.8 pEC50 = 5.8 Functional
Agonist activity at mouse histamine H4 receptorAgonist activity at mouse histamine H4 receptor
ChEMBL 125 2 2 2 0.2 Cc1c(CCN)nc[nH]1 10.1016/j.bmcl.2010.10.041
CHEMBL275443 121 41 None -35 6 Mouse 5.8 pEC50 = 5.8 Functional
Agonist activity at mouse histamine H4 receptorAgonist activity at mouse histamine H4 receptor
ChEMBL 125 2 2 2 0.2 Cc1c(CCN)nc[nH]1 10.1016/j.bmcl.2010.10.041
53233802 61547 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 61547 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 187585 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 187585 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 1932 119 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 1932 119 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 1932 119 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 1932 119 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 1932 119 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 1932 119 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 1932 119 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 1932 119 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 1932 119 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 1932 119 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 1932 119 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 1932 119 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 5676 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 5676 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 173896 60 None - 1 Rat 4.8 pEC50 = 4.8 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 227 1 1 5 0.5 CN1CCN(c2cc(Cl)nc(N)n2)CC1 10.1021/jm8005959
CHEMBL454007 173896 60 None - 1 Rat 4.8 pEC50 = 4.8 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 227 1 1 5 0.5 CN1CCN(c2cc(Cl)nc(N)n2)CC1 10.1021/jm8005959
21638785 188658 5 None 1 2 Mouse 7.8 pEC50 = 7.8 Functional
Antagonist activity at mouse histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assayAntagonist activity at mouse histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assay
ChEMBL 263 1 2 2 1.9 O=C(c1cc2cc(Cl)ccc2[nH]1)N1CCNCC1 10.1021/jm800670r
CHEMBL503605 188658 5 None 1 2 Mouse 7.8 pEC50 = 7.8 Functional
Antagonist activity at mouse histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assayAntagonist activity at mouse histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assay
ChEMBL 263 1 2 2 1.9 O=C(c1cc2cc(Cl)ccc2[nH]1)N1CCNCC1 10.1021/jm800670r
127051958 140278 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 140278 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 193130 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 193130 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 187704 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 187704 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 187594 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 187594 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 188252 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 188252 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 176463 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 176463 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 176463 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 189062 14 None -1 2 Mouse 7.7 pEC50 = 7.7 Functional
Antagonist activity at mouse histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assayAntagonist activity at mouse histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assay
ChEMBL 295 1 2 5 1.6 Nc1nc2c(c(N3CCNCC3)n1)CCCc1ccccc1-2 10.1021/jm800670r
CHEMBL509540 189062 14 None -1 2 Mouse 7.7 pEC50 = 7.7 Functional
Antagonist activity at mouse histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assayAntagonist activity at mouse histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assay
ChEMBL 295 1 2 5 1.6 Nc1nc2c(c(N3CCNCC3)n1)CCCc1ccccc1-2 10.1021/jm800670r
1204 1932 119 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 1932 119 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 1932 119 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 1932 119 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 1932 119 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 1932 119 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 170613 7 None - 1 Rat 5.7 pEC50 = 5.7 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 259 2 2 6 0.2 CN1CCN(c2cc(-c3cn[nH]c3)nc(N)n2)CC1 10.1021/jm8005959
CHEMBL445091 170613 7 None - 1 Rat 5.7 pEC50 = 5.7 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 259 2 2 6 0.2 CN1CCN(c2cc(-c3cn[nH]c3)nc(N)n2)CC1 10.1021/jm8005959
25128831 172613 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 172613 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 187376 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 187376 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 171414 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 171414 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 176478 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 176478 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 176478 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 199904 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 199904 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 80266 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 80266 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 1932 119 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 1932 119 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 1932 119 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 1932 119 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 1932 119 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 1932 119 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 15495 24 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 212 5 3 2 1.2 C/N=C(\S)NCCCCc1c[nH]cn1 10.1016/j.bmcl.2010.10.041
CHEMBL12160 15495 24 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 212 5 3 2 1.2 C/N=C(\S)NCCCCc1c[nH]cn1 10.1016/j.bmcl.2010.10.041
53321919 56478 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 56478 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 102911 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 102911 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 192717 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 192717 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 193109 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 193109 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 5209 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 5209 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 206981 35 None -4 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 125 3 2 2 0.3 NCCCc1c[nH]cn1 10.1016/j.bmcl.2010.10.041
CHEMBL4634086 206981 35 None -4 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 125 3 2 2 0.3 NCCCc1c[nH]cn1 10.1016/j.bmcl.2010.10.041
CHEMBL91353 206981 35 None -4 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 125 3 2 2 0.3 NCCCc1c[nH]cn1 10.1016/j.bmcl.2010.10.041
155513612 176320 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 176320 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 176320 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 176320 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 56481 3 None -1 3 Mouse 6.7 pEC50 = 6.7 Functional
Agonist activity at mouse histamine H4 receptor by luciferase reporter gene assayAgonist activity at mouse histamine H4 receptor by luciferase reporter gene assay
ChEMBL 271 2 2 3 3.0 Cc1ccc2[nH]c(/C(=N\O)C3CCN(C)CC3)cc2c1 10.1016/j.bmcl.2010.10.041
CHEMBL1632412 56481 3 None -1 3 Mouse 6.7 pEC50 = 6.7 Functional
Agonist activity at mouse histamine H4 receptor by luciferase reporter gene assayAgonist activity at mouse histamine H4 receptor by luciferase reporter gene assay
ChEMBL 271 2 2 3 3.0 Cc1ccc2[nH]c(/C(=N\O)C3CCN(C)CC3)cc2c1 10.1016/j.bmcl.2010.10.041
136192874 56483 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 56483 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 200054 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 200054 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 5301 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 5301 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 5301 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 5301 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 5290 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 5290 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 2150 84 None -1 4 Mouse 8.6 pEC50 = 8.6 Functional
Antagonist activity at mouse histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assayAntagonist activity at mouse histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assay
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/jm800670r
1279 2150 84 None -1 4 Mouse 8.6 pEC50 = 8.6 Functional
Antagonist activity at mouse histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assayAntagonist activity at mouse histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assay
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/jm800670r
4908365 2150 84 None -1 4 Mouse 8.6 pEC50 = 8.6 Functional
Antagonist activity at mouse histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assayAntagonist activity at mouse histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assay
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/jm800670r
CHEMBL129198 2150 84 None -1 4 Mouse 8.6 pEC50 = 8.6 Functional
Antagonist activity at mouse histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assayAntagonist activity at mouse histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assay
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/jm800670r
1278 2150 84 None -1 4 Rat 8.6 pEC50 = 8.6 Functional
Antagonist activity at rat histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assayAntagonist activity at rat histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assay
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/jm800670r
1279 2150 84 None -1 4 Rat 8.6 pEC50 = 8.6 Functional
Antagonist activity at rat histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assayAntagonist activity at rat histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assay
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/jm800670r
4908365 2150 84 None -1 4 Rat 8.6 pEC50 = 8.6 Functional
Antagonist activity at rat histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assayAntagonist activity at rat histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assay
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/jm800670r
CHEMBL129198 2150 84 None -1 4 Rat 8.6 pEC50 = 8.6 Functional
Antagonist activity at rat histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assayAntagonist activity at rat histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assay
ChEMBL 277 1 1 2 2.2 CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl 10.1021/jm800670r
58227260 117132 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 117132 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 77952 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 77952 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 1932 119 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 1932 119 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 1932 119 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 1932 119 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 1932 119 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 1932 119 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 199679 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 199679 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 1932 119 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 1932 119 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 1932 119 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 1932 119 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 1932 119 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 1932 119 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 140207 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 140207 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 187282 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 187282 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 140200 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 140200 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 187179 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 187179 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 187254 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 187254 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 5290 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 5290 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 2348 53 None -26 34 Human 6.7 pEC50 = 6.7 Functional
Activity at human histamine H4 receptor transfected in SK-N-MC cells by cAMP assayActivity at human histamine H4 receptor transfected in SK-N-MC cells by cAMP assay
ChEMBL 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 10.1021/jm051008s
205 2348 53 None -26 34 Human 6.7 pEC50 = 6.7 Functional
Activity at human histamine H4 receptor transfected in SK-N-MC cells by cAMP assayActivity at human histamine H4 receptor transfected in SK-N-MC cells by cAMP assay
ChEMBL 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 10.1021/jm051008s
3964 2348 53 None -26 34 Human 6.7 pEC50 = 6.7 Functional
Activity at human histamine H4 receptor transfected in SK-N-MC cells by cAMP assayActivity at human histamine H4 receptor transfected in SK-N-MC cells by cAMP assay
ChEMBL 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 10.1021/jm051008s
CHEMBL831 2348 53 None -26 34 Human 6.7 pEC50 = 6.7 Functional
Activity at human histamine H4 receptor transfected in SK-N-MC cells by cAMP assayActivity at human histamine H4 receptor transfected in SK-N-MC cells by cAMP assay
ChEMBL 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 10.1021/jm051008s
DB00408 2348 53 None -26 34 Human 6.7 pEC50 = 6.7 Functional
Activity at human histamine H4 receptor transfected in SK-N-MC cells by cAMP assayActivity at human histamine H4 receptor transfected in SK-N-MC cells by cAMP assay
ChEMBL 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 10.1021/jm051008s
753256 179350 12 None - 1 Rat 6.7 pEC50 = 6.7 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 208 1 2 6 -0.6 CN1CCN(c2cc(N)nc(N)n2)CC1 10.1021/jm8005959
CHEMBL473662 179350 12 None - 1 Rat 6.7 pEC50 = 6.7 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 208 1 2 6 -0.6 CN1CCN(c2cc(N)nc(N)n2)CC1 10.1021/jm8005959
25131560 187346 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 187346 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 953 41 None -21 4 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human H4R by [35S]-GTPgammaS-binding assayAgonist activity at human H4R by [35S]-GTPgammaS-binding assay
ChEMBL 308 6 2 3 3.2 Clc1ccc(cc1)CN=C(SCCCc1cnc[nH]1)N 10.1021/acs.jmedchem.9b01342
2790 953 41 None -21 4 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human H4R by [35S]-GTPgammaS-binding assayAgonist activity at human H4R by [35S]-GTPgammaS-binding assay
ChEMBL 308 6 2 3 3.2 Clc1ccc(cc1)CN=C(SCCCc1cnc[nH]1)N 10.1021/acs.jmedchem.9b01342
CHEMBL14690 953 41 None -21 4 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human H4R by [35S]-GTPgammaS-binding assayAgonist activity at human H4R by [35S]-GTPgammaS-binding assay
ChEMBL 308 6 2 3 3.2 Clc1ccc(cc1)CN=C(SCCCc1cnc[nH]1)N 10.1021/acs.jmedchem.9b01342
155512725 176241 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 176241 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 176241 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 5209 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 5209 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 187182 5 None - 1 Rat 6.6 pEC50 = 6.6 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 270 2 1 6 0.9 CN1CCN(c2cc(-c3ccncc3)nc(N)n2)CC1 10.1021/jm8005959
CHEMBL492241 187182 5 None - 1 Rat 6.6 pEC50 = 6.6 Functional
Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 270 2 1 6 0.9 CN1CCN(c2cc(-c3ccncc3)nc(N)n2)CC1 10.1021/jm8005959
44568855 193194 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 193194 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 172012 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 172012 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 187354 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 187354 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 140194 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 140194 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 187661 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 187661 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 192723 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 192723 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 187350 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 187350 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 187589 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 187589 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 172598 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 172598 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 8091 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 8091 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 140309 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 140309 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 109479 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 109479 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 187626 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 187626 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 188816 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 188816 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 187626 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 187626 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 115917 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 115917 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 1932 119 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 1932 119 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 1932 119 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 1932 119 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 1932 119 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 1932 119 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 2019 20 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 321 9 4 4 1.2 NC(=NCCCc1cnc[nH]1)NCCSCc1nc[nH]c1C 10.1016/j.bmcl.2010.10.041
41376 2019 20 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 321 9 4 4 1.2 NC(=NCCCc1cnc[nH]1)NCCSCc1nc[nH]c1C 10.1016/j.bmcl.2010.10.041
CHEMBL12608 2019 20 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 321 9 4 4 1.2 NC(=NCCCc1cnc[nH]1)NCCSCc1nc[nH]c1C 10.1016/j.bmcl.2010.10.041
25133970 187588 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 187588 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 172456 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 172456 2 None 3 2 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assayAgonist activity at human histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
ChEMBL 259 2 1 7 -0.0 CN1CCN(c2cc(-n3ccnc3)nc(N)n2)CC1 10.1021/jm8005959
1269 121 41 None -56 6 Rat 5.6 pEC50 = 5.6 Functional
Agonist activity at rat histamine H4 receptorAgonist activity at rat histamine H4 receptor
ChEMBL 125 2 2 2 0.2 Cc1c(CCN)nc[nH]1 10.1016/j.bmcl.2010.10.041
37463 121 41 None -56 6 Rat 5.6 pEC50 = 5.6 Functional
Agonist activity at rat histamine H4 receptorAgonist activity at rat histamine H4 receptor
ChEMBL 125 2 2 2 0.2 Cc1c(CCN)nc[nH]1 10.1016/j.bmcl.2010.10.041
CHEMBL275443 121 41 None -56 6 Rat 5.6 pEC50 = 5.6 Functional
Agonist activity at rat histamine H4 receptorAgonist activity at rat histamine H4 receptor
ChEMBL 125 2 2 2 0.2 Cc1c(CCN)nc[nH]1 10.1016/j.bmcl.2010.10.041
44480958 5673 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 5673 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 188871 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 188871 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 140311 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 140311 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 199943 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 199943 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 187187 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 187187 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 205174 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 205174 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 176241 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 176241 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 176241 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 140302 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 140302 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 1932 119 None -102 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 1932 119 None -102 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 1932 119 None -102 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 1932 119 None -102 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 1932 119 None -102 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 1932 119 None -102 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 187481 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 187481 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 176495 4 None -31 4 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human H4R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by CRE-luciferase reporter gene assayAgonist activity at human H4R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by CRE-luciferase reporter gene assay
ChEMBL 207 4 2 5 0.2 CCCNC1CN(c2ccnc(N)n2)C1 10.1021/acs.jmedchem.9b01462
CHEMBL4441731 176495 4 None -31 4 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human H4R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by CRE-luciferase reporter gene assayAgonist activity at human H4R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by CRE-luciferase reporter gene assay
ChEMBL 207 4 2 5 0.2 CCCNC1CN(c2ccnc(N)n2)C1 10.1021/acs.jmedchem.9b01462
CHEMBL4596734 176495 4 None -31 4 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human H4R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by CRE-luciferase reporter gene assayAgonist activity at human H4R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by CRE-luciferase reporter gene assay
ChEMBL 207 4 2 5 0.2 CCCNC1CN(c2ccnc(N)n2)C1 10.1021/acs.jmedchem.9b01462
46890072 6910 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 6910 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 7316 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 7316 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 176508 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 176508 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 176508 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 188658 5 None -1 2 Rat 7.5 pEC50 = 7.5 Functional
Antagonist activity at rat histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assayAntagonist activity at rat histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assay
ChEMBL 263 1 2 2 1.9 O=C(c1cc2cc(Cl)ccc2[nH]1)N1CCNCC1 10.1021/jm800670r
CHEMBL503605 188658 5 None -1 2 Rat 7.5 pEC50 = 7.5 Functional
Antagonist activity at rat histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assayAntagonist activity at rat histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assay
ChEMBL 263 1 2 2 1.9 O=C(c1cc2cc(Cl)ccc2[nH]1)N1CCNCC1 10.1021/jm800670r
25130911 185230 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 185230 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 117185 13 None - 1 Human 6.5 pEC50 = 6.5 Functional
Activity at human histamine H4 receptor transfected in SK-N-MC cells by cAMP assayActivity at human histamine H4 receptor transfected in SK-N-MC cells by cAMP assay
ChEMBL 293 0 0 4 3.1 CN1CCN(C2=Nc3ccccc3Oc3ccccc32)CC1 10.1021/jm051008s
CHEMBL339414 117185 13 None - 1 Human 6.5 pEC50 = 6.5 Functional
Activity at human histamine H4 receptor transfected in SK-N-MC cells by cAMP assayActivity at human histamine H4 receptor transfected in SK-N-MC cells by cAMP assay
ChEMBL 293 0 0 4 3.1 CN1CCN(C2=Nc3ccccc3Oc3ccccc32)CC1 10.1021/jm051008s
1267 3804 49 None -8 5 Mouse 6.5 pEC50 = 6.5 Functional
Agonist activity at mouse H4R expressed in HEK293-SF-mH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at mouse H4R expressed in HEK293-SF-mH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1021/acs.jmedchem.0c00160
3035905 3804 49 None -8 5 Mouse 6.5 pEC50 = 6.5 Functional
Agonist activity at mouse H4R expressed in HEK293-SF-mH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at mouse H4R expressed in HEK293-SF-mH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1021/acs.jmedchem.0c00160
CHEMBL260374 3804 49 None -8 5 Mouse 6.5 pEC50 = 6.5 Functional
Agonist activity at mouse H4R expressed in HEK293-SF-mH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at mouse H4R expressed in HEK293-SF-mH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 10.1021/acs.jmedchem.0c00160
25130579 187712 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 187712 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 5362 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 5362 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 199798 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 199798 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 2009 16 None -18 2 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 139 4 2 2 0.7 NCCCCc1cnc[nH]1 10.1016/j.bmcl.2010.10.041
13499360 2009 16 None -18 2 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 139 4 2 2 0.7 NCCCCc1cnc[nH]1 10.1016/j.bmcl.2010.10.041
CHEMBL90019 2009 16 None -18 2 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
ChEMBL 139 4 2 2 0.7 NCCCCc1cnc[nH]1 10.1016/j.bmcl.2010.10.041
1269 121 41 None 35 6 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human recombinant histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2 by steady-state GTPase activity assayAgonist activity at human recombinant histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2 by steady-state GTPase activity assay
ChEMBL 125 2 2 2 0.2 Cc1c(CCN)nc[nH]1 10.1016/j.bmcl.2010.10.041
37463 121 41 None 35 6 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human recombinant histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2 by steady-state GTPase activity assayAgonist activity at human recombinant histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2 by steady-state GTPase activity assay
ChEMBL 125 2 2 2 0.2 Cc1c(CCN)nc[nH]1 10.1016/j.bmcl.2010.10.041
CHEMBL275443 121 41 None 35 6 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human recombinant histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2 by steady-state GTPase activity assayAgonist activity at human recombinant histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2 by steady-state GTPase activity assay
ChEMBL 125 2 2 2 0.2 Cc1c(CCN)nc[nH]1 10.1016/j.bmcl.2010.10.041
25129528 187186 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 187186 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 193103 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 193103 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 117136 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 117136 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 115918 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 115918 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 117133 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 117133 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 5362 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 5362 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 193259 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 193259 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 187380 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 187380 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 5776 6 None 20 2 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19 protein by steady-state GTPase assayAgonist activity at human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19 protein by steady-state GTPase assay
ChEMBL 342 9 3 4 2.5 N#C/N=C(/NCCCCc1c[nH]cn1)NCCSc1ccccc1 10.1021/jm900526h
CHEMBL1078642 5776 6 None 20 2 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19 protein by steady-state GTPase assayAgonist activity at human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19 protein by steady-state GTPase assay
ChEMBL 342 9 3 4 2.5 N#C/N=C(/NCCCCc1c[nH]cn1)NCCSc1ccccc1 10.1021/jm900526h
46890549 6585 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 6585 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 5630 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 5630 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 180766 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 180766 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 82081 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 82081 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 170187 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 170187 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 4064 16 None -776 4 Rat 4.5 pEC50 = 4.5 Functional
Agonist activity at rat H4R by [35S]-GTPgammaS-binding assayAgonist activity at rat H4R by [35S]-GTPgammaS-binding assay
ChEMBL 161 3 4 3 -1.1 NC(=N)SCCN=C(N)N 10.1021/acs.jmedchem.9b01342
3063228 4064 16 None -776 4 Rat 4.5 pEC50 = 4.5 Functional
Agonist activity at rat H4R by [35S]-GTPgammaS-binding assayAgonist activity at rat H4R by [35S]-GTPgammaS-binding assay
ChEMBL 161 3 4 3 -1.1 NC(=N)SCCN=C(N)N 10.1021/acs.jmedchem.9b01342
CHEMBL1196470 4064 16 None -776 4 Rat 4.5 pEC50 = 4.5 Functional
Agonist activity at rat H4R by [35S]-GTPgammaS-binding assayAgonist activity at rat H4R by [35S]-GTPgammaS-binding assay
ChEMBL 161 3 4 3 -1.1 NC(=N)SCCN=C(N)N 10.1021/acs.jmedchem.9b01342
155517880 176667 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 176667 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 176667 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 176478 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 176478 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 176478 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 187251 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 187251 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 187381 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 187381 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 109478 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 109478 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 187252 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 187252 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 187564 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 187564 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 5776 6 None 20 2 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human histamine H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assayAgonist activity at human histamine H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 342 9 3 4 2.5 N#C/N=C(/NCCCCc1c[nH]cn1)NCCSc1ccccc1 10.1021/acs.jmedchem.6b00120
CHEMBL1078642 5776 6 None 20 2 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human histamine H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assayAgonist activity at human histamine H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assay
ChEMBL 342 9 3 4 2.5 N#C/N=C(/NCCCCc1c[nH]cn1)NCCSc1ccccc1 10.1021/acs.jmedchem.6b00120
44478385 5776 6 None 20 2 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human recombinant histamine H4 receptor-RGS19 fusion protein expressed in Sf9 cells coexpressing Galphai2,Gbeta1gamma2 assessed as [35S]GTPgammaS binding after 90 mins by liquid scintillation countingAgonist activity at human recombinant histamine H4 receptor-RGS19 fusion protein expressed in Sf9 cells coexpressing Galphai2,Gbeta1gamma2 assessed as [35S]GTPgammaS binding after 90 mins by liquid scintillation counting
ChEMBL 342 9 3 4 2.5 N#C/N=C(/NCCCCc1c[nH]cn1)NCCSc1ccccc1 10.1039/C3MD00245D
CHEMBL1078642 5776 6 None 20 2 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human recombinant histamine H4 receptor-RGS19 fusion protein expressed in Sf9 cells coexpressing Galphai2,Gbeta1gamma2 assessed as [35S]GTPgammaS binding after 90 mins by liquid scintillation countingAgonist activity at human recombinant histamine H4 receptor-RGS19 fusion protein expressed in Sf9 cells coexpressing Galphai2,Gbeta1gamma2 assessed as [35S]GTPgammaS binding after 90 mins by liquid scintillation counting
ChEMBL 342 9 3 4 2.5 N#C/N=C(/NCCCCc1c[nH]cn1)NCCSc1ccccc1 10.1039/C3MD00245D
25129527 187414 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 187414 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 199867 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 199867 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 140266 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 140266 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 4064 16 None 7 4 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human H4R by [35S]-GTPgammaS-binding assayAgonist activity at human H4R by [35S]-GTPgammaS-binding assay
ChEMBL 161 3 4 3 -1.1 NC(=N)SCCN=C(N)N 10.1021/acs.jmedchem.9b01342
3063228 4064 16 None 7 4 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human H4R by [35S]-GTPgammaS-binding assayAgonist activity at human H4R by [35S]-GTPgammaS-binding assay
ChEMBL 161 3 4 3 -1.1 NC(=N)SCCN=C(N)N 10.1021/acs.jmedchem.9b01342
CHEMBL1196470 4064 16 None 7 4 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human H4R by [35S]-GTPgammaS-binding assayAgonist activity at human H4R by [35S]-GTPgammaS-binding assay
ChEMBL 161 3 4 3 -1.1 NC(=N)SCCN=C(N)N 10.1021/acs.jmedchem.9b01342
11846465 141932 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 141932 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 187585 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 187585 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 187404 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 187404 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 6604 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 6604 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 41 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 41 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 41 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 56482 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 56482 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 187287 45 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 187287 45 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 187287 45 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 187287 45 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 75691 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 75691 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 17987 34 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 17987 34 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 117128 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 117128 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 176508 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 176508 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 176508 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 192718 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 192718 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 180766 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 180766 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 193178 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 193178 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 108568 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 108568 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 82079 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 82079 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 3804 49 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 3804 49 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 3804 49 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 187184 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 187184 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 187380 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 187380 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 2150 84 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 2150 84 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 2150 84 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 2150 84 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 188402 38 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 188402 38 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 187413 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 187413 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 199866 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 199866 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 140250 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 140250 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 187181 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 187181 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 170376 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 170376 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 109477 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 109477 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 186885 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 186885 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 187225 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 187225 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 187587 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 187587 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 6515 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 6515 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 200083 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 200083 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 117115 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 117115 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 187254 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 187254 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 187668 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 187668 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 187701 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 187701 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 188438 19 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 188438 19 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 61524 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 61524 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 7385 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 7385 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 4064 16 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 4064 16 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 4064 16 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 4064 16 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 4064 16 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 4064 16 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 56481 3 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 56481 3 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 2500 8 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 2500 8 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 2500 8 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 109360 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 109360 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 1932 119 None -53 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 1932 119 None -53 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 1932 119 None -53 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 1932 119 None -53 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 1932 119 None -53 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 1932 119 None -53 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 176320 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 176320 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 176320 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 176320 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 176241 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 176241 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 176241 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 176463 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 176463 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 176463 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 174302 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 174302 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 187335 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 187335 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 140197 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 140197 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 1932 119 None -102 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 1932 119 None -102 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 1932 119 None -102 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 1932 119 None -102 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 1932 119 None -102 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 1932 119 None -102 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 61522 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 61522 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 187181 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 187181 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 140245 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 140245 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 109476 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 109476 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 109743 11 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 109743 11 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 109360 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 109360 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 187288 1 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 187288 1 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 199988 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 199988 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 5624 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 5624 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 187290 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 187290 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 187587 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 187587 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 187587 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 187587 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 199904 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 199904 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 193178 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 193178 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 176667 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 176667 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 176667 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 195349 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 195349 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 195349 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 192718 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 192718 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 7046 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 7046 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 202158 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 202158 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 6516 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 6516 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 3195 19 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 3195 19 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 3195 19 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 204474 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 204474 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 204534 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 204534 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 56483 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 56483 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 2067 25 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 2067 25 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 2067 25 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 2067 25 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 187379 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 187379 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 187254 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 187254 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 171851 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 171851 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 187245 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 187245 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 1932 119 None -53 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 1932 119 None -53 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 1932 119 None -53 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 1932 119 None -53 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 1932 119 None -53 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 1932 119 None -53 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 188739 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 188739 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 1932 119 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 1932 119 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 1932 119 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 1932 119 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 1932 119 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 1932 119 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 179052 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 179052 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 1932 119 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 1932 119 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 1932 119 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 1932 119 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 1932 119 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 1932 119 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 3804 49 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 3804 49 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 3804 49 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 41 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 41 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 41 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 3804 49 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 3804 49 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 3804 49 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 5642 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 5642 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 7312 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 7312 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 178272 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 178272 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 178272 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 2150 84 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 2150 84 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 2150 84 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 2150 84 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 5150 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 5150 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 117129 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 117129 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 5713 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 5713 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 5358 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 5358 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 7394 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 7394 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 5799 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 5799 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 109271 10 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 109271 10 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 109271 10 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 109271 10 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 82078 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 82078 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 109271 10 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 109271 10 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 204485 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 204485 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 1932 119 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 1932 119 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 1932 119 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 1932 119 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 1932 119 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 1932 119 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 56483 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 56483 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 3804 49 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 3804 49 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 3804 49 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 2033 24 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 2033 24 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 2033 24 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 2033 24 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 5150 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 5150 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 2150 84 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 2150 84 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 2150 84 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 2150 84 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 180766 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 180766 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 5358 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 5358 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 7394 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 7394 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 176320 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 176320 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 176320 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 176320 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 172456 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 172456 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 187349 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 187349 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 188755 7 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 188755 7 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 82065 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 82065 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 82080 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 82080 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 199908 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 199908 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 139281 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 139281 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 172761 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 172761 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 117124 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 117124 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 953 41 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 953 41 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 953 41 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 108207 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 108207 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 61545 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 61545 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 117130 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 117130 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 1932 119 None -53 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 1932 119 None -53 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 1932 119 None -53 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 1932 119 None -53 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 1932 119 None -53 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 1932 119 None -53 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 1932 119 None -53 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 1932 119 None -53 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 1932 119 None -53 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 1932 119 None -53 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 1932 119 None -53 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 1932 119 None -53 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 4064 16 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 4064 16 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 4064 16 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 187701 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 187701 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 3804 49 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 3804 49 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 3804 49 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 169460 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 169460 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 187249 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 187249 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 193106 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 193106 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 193106 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 193106 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 117127 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 117127 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 199679 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 199679 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 137266 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 137266 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 176463 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 176463 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 176463 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 188871 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 188871 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 187713 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 187713 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 137285 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 137285 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 5677 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 5677 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 187334 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 187334 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 295 12 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 295 12 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 295 12 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 295 12 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 295 12 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 295 12 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 295 12 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 295 12 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 178240 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 178240 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 178240 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 199508 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 199508 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 69740 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 69740 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 80260 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 80260 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 89725 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 89725 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 89726 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 89726 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 2150 84 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 2150 84 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 2150 84 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 2150 84 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 2132 34 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 2132 34 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 2132 34 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 175303 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 175303 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 174238 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 174238 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 80347 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 80347 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 112178 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 112178 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 3804 49 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 3804 49 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 3804 49 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 2150 84 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 2150 84 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 2150 84 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 2150 84 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 2150 84 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 2150 84 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 2150 84 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 2150 84 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 15769 4 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 15769 4 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 2150 84 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 2150 84 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 2150 84 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 2150 84 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 174251 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 174251 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 1909 20 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 1909 20 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 1909 20 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 7976 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 7976 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 8162 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 8162 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 2150 84 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 2150 84 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 2150 84 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 2150 84 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 172541 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 172541 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 199556 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 199556 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 8274 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 8274 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 8163 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 8163 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 295 12 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 295 12 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 295 12 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 295 12 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 2150 84 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 2150 84 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 2150 84 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 2150 84 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 7912 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 7912 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 123914 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 123914 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 69738 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 69738 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 69737 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 69737 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 2150 84 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 2150 84 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 2150 84 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 2150 84 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 112176 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 112176 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 295 12 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 295 12 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 295 12 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 295 12 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 2132 34 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 2132 34 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 2132 34 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 124021 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 124021 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 3804 49 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 3804 49 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 3804 49 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 3804 49 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 3804 49 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 3804 49 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 173409 9 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 173409 9 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 1909 20 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 1909 20 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 1909 20 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 8246 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 8246 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 89729 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 89729 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 8106 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 8106 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 69739 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 69739 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 178240 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 178240 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 178240 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 2150 84 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 2150 84 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 2150 84 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 2150 84 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 80346 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 80346 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 89728 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 89728 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 3804 49 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 3804 49 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 3804 49 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 117133 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 117133 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 110133 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 110133 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 110124 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 110124 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 110126 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 110126 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 110125 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 110125 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 110147 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 110147 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 61540 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 61540 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 61539 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 61539 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 110128 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 110128 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 117112 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 117112 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 117118 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 117118 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 117121 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 117121 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 61561 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 61561 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 61529 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 61529 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 61531 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 61531 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 61552 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 61552 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 188739 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 188739 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 68048 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 68048 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 110137 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 110137 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 110140 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 110140 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 110144 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 110144 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 61537 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 61537 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 117139 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 117139 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 117142 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 117142 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 110125 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 110125 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 68101 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 68101 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 117017 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 117017 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 2142 31 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 2142 31 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 2142 31 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 110141 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 110141 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 110142 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 110142 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 61519 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 61519 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 61550 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 61550 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 125051 4 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 125051 4 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 6589 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 6589 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 109798 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 109798 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 14965 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 14965 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 18875 5 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 18875 5 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 61532 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 61532 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 117136 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 117136 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 14690 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 14690 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 18940 6 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 18940 6 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 18918 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 18918 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 7291 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 7291 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 7316 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 7316 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 110134 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 110134 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 195591 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 195591 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 195591 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 61525 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 61525 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 2132 34 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 2132 34 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 2132 34 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 18842 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 18842 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 19424 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 19424 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 72519 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 72519 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 97220 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 97220 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 168662 11 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 168662 11 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 110136 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 110136 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 110149 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 110149 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 110130 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 110130 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 110155 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 110155 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 141313 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 141313 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 6392 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 6392 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 115918 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 115918 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 110143 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 110143 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 19258 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 19258 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 72571 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 72571 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 117119 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 117119 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 19379 56 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 19379 56 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 110150 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 110150 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 2142 31 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 2142 31 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 2142 31 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 68183 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 68183 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 110140 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 110140 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 7024 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 7024 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 67080 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 67080 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 114427 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 114427 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 132817 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 132817 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 6515 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 6515 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 7024 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 7024 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 8378 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 8378 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 19423 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 19423 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 2142 31 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 2142 31 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 2142 31 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 140934 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 140934 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 7312 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 7312 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 2150 84 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 2150 84 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 2150 84 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 2150 84 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 19442 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 19442 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 110146 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 110146 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 61555 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 61555 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 117134 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 117134 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 117143 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 117143 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 2150 84 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 2150 84 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 2150 84 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 2150 84 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 19442 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 19442 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 118108 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 118108 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 19165 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 19165 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 116844 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 116844 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 117023 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 117023 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 68218 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 68218 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 68219 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 68219 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 295 12 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 295 12 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 295 12 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 295 12 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 195499 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 195499 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 195499 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 68212 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 68212 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 69915 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 69915 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 68220 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 68220 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 69869 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 69869 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 68210 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 68210 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 68212 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 68212 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 69902 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 69902 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 69914 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 69914 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 69867 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 69867 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 68211 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 68211 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 69912 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 69912 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 68209 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 68209 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 68209 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 68209 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 69738 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 69738 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 69903 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 69903 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 68217 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 68217 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 68210 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 68210 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 2132 34 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 2132 34 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 2132 34 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 2132 34 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 2132 34 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 2132 34 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 69737 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 69737 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 69904 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 69904 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 2150 84 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 2150 84 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 2150 84 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 2150 84 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 69739 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 69739 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 68211 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 68211 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 69910 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 69910 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 68216 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 68216 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 68216 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 68216 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 2150 84 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 2150 84 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 2150 84 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 2150 84 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 2150 84 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 2150 84 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 2150 84 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 2150 84 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 2150 84 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 2150 84 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 2150 84 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 2150 84 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 3804 49 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 3804 49 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 3804 49 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 69740 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 69740 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 69906 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 69906 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 69913 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 69913 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 69911 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 69911 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 68217 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 68217 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 69868 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 69868 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 2532 43 None -2 33 Human 8.2 pEC50 = 8.2 Functional
NoneNone
Drug Central 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
1796 2532 43 None -2 33 Human 8.2 pEC50 = 8.2 Functional
NoneNone
Drug Central 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
4184 2532 43 None -2 33 Human 8.2 pEC50 = 8.2 Functional
NoneNone
Drug Central 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
CHEMBL6437 2532 43 None -2 33 Human 8.2 pEC50 = 8.2 Functional
NoneNone
Drug Central 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
DB06148 2532 43 None -2 33 Human 8.2 pEC50 = 8.2 Functional
NoneNone
Drug Central 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
1225 1471 26 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 1471 26 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 1471 26 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 1471 26 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 1471 26 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 173473 101 None 60 6 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 173473 101 None 60 6 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 831 0 None - 1 Human 8.1 pIC50 None 8.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 15265943




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DOI

51354301 58892 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 58892 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 75691 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 75691 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 109489 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 109489 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 45741 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 45741 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 205613 2 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 205613 2 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 176241 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 176241 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 176241 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 3804 49 None -33 26 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 3804 49 None -33 26 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 3804 49 None -33 26 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 46018 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 46018 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 176547 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 176547 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 176547 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 1932 119 None -3 24 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 1932 119 None -3 24 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 1932 119 None -3 24 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 1932 119 None -3 24 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 1932 119 None -3 24 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 1932 119 None -3 24 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 2067 25 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 2067 25 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 2067 25 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 2067 25 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 6392 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 6392 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 7316 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 7316 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 1932 119 None -3 24 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 1932 119 None -3 24 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 1932 119 None -3 24 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 1932 119 None -3 24 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 1932 119 None -3 24 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 1932 119 None -3 24 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 1932 119 None -3 24 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 1932 119 None -3 24 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 1932 119 None -3 24 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 1932 119 None -3 24 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 1932 119 None -3 24 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 1932 119 None -3 24 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 2150 84 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 2150 84 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 2150 84 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 2150 84 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 176547 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 176547 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 176547 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 205198 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 205198 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 1932 119 None -3 24 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 1932 119 None -3 24 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 1932 119 None -3 24 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 1932 119 None -3 24 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 1932 119 None -3 24 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 1932 119 None -3 24 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 110130 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 110130 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 176508 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 176508 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 176508 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 176478 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 176478 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 176478 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 8511 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 8511 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 176508 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 176508 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 176508 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 176667 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 176667 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 176667 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 184225 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 184225 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 184225 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 184225 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 184225 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 184225 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 196482 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 196482 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 196482 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 179925 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 179925 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 105213 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 105213 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 205244 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 205244 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 104168 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 104168 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 176547 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 176547 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 176547 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 140238 3 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 140238 3 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 176320 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 176320 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 176320 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 176320 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 179768 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 179768 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 176241 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 176241 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 176241 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 178353 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 178353 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 8761 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 8761 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 45928 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 45928 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 206981 35 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 206981 35 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 206981 35 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 8760 1 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 8760 1 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 176667 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 176667 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 176667 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 1932 119 None -15 24 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 1932 119 None -15 24 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 1932 119 None -15 24 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 1932 119 None -15 24 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 1932 119 None -15 24 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 1932 119 None -15 24 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 1932 119 None -15 24 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 1932 119 None -15 24 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 1932 119 None -15 24 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 1932 119 None -15 24 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 1932 119 None -15 24 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 1932 119 None -15 24 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 140238 3 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 140238 3 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 96154 10 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 96154 10 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 2150 84 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 2150 84 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 2150 84 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 2150 84 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 176451 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 176451 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 176451 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 176320 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 176320 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 176320 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 176320 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 179770 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 179770 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 3804 49 None -21 26 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 3804 49 None -21 26 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 3804 49 None -21 26 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 109469 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 109469 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 176451 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 176451 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 176451 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 180766 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 180766 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 179100 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 179100 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 205284 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 205284 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 205687 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 205687 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 189694 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 189694 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 1932 119 None -3 24 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 1932 119 None -3 24 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 1932 119 None -3 24 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 1932 119 None -3 24 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 1932 119 None -3 24 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 1932 119 None -3 24 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 1932 119 None -3 24 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 1932 119 None -3 24 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 1932 119 None -3 24 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 1932 119 None -3 24 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 1932 119 None -3 24 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 1932 119 None -3 24 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 176508 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 176508 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 176508 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 176478 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 176478 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 176478 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 176463 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 176463 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 176463 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 140247 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 140247 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 1932 119 None -12 24 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 1932 119 None -12 24 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 1932 119 None -12 24 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 1932 119 None -12 24 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 1932 119 None -12 24 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 1932 119 None -12 24 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 195349 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 195349 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 195349 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 176241 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 176241 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 176241 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 44073 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 44073 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 176547 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 176547 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 176547 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 8763 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 8763 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 169773 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 169773 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 169201 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 169201 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 176463 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 176463 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 176463 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 176320 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 176320 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 176320 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 176320 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 178240 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 178240 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 178240 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 140228 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 140228 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 2010 34 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 2010 34 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 2010 34 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 2010 34 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 176320 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 176320 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 176320 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 176320 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 140200 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 140200 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 1932 119 None -3 24 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 1932 119 None -3 24 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 1932 119 None -3 24 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 1932 119 None -3 24 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 1932 119 None -3 24 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 1932 119 None -3 24 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 6604 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 6604 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 2014 39 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 2014 39 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 2014 39 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 2014 39 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 2014 39 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 2014 39 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 104415 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 104415 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 140228 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 140228 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 188436 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 188436 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 176451 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 176451 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 176451 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 8509 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 8509 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 140200 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 140200 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 187254 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 187254 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 178272 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 178272 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 178272 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 176463 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 176463 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 176463 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 179200 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 179200 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 157365 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 157365 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 189588 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 189588 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 110125 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 110125 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 28895 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 28895 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 45760 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 45760 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 1932 119 None -3 24 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 1932 119 None -3 24 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 1932 119 None -3 24 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 1932 119 None -3 24 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 1932 119 None -3 24 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 1932 119 None -3 24 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 109470 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 109470 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 95484 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 95484 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 110568 8 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 110568 8 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 8762 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 8762 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 179052 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 179052 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 176478 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 176478 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 176478 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 176667 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 176667 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 176667 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 2009 16 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 2009 16 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 2009 16 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 2009 16 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 2009 16 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 2009 16 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 1932 119 None -3 24 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 1932 119 None -3 24 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 1932 119 None -3 24 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 1932 119 None -3 24 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 1932 119 None -3 24 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 1932 119 None -3 24 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 2015 20 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 2015 20 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 2015 20 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 1932 119 None -15 24 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 1932 119 None -15 24 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 1932 119 None -15 24 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 1932 119 None -15 24 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 1932 119 None -15 24 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 1932 119 None -15 24 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 8162 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 8162 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 8415 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 8415 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 61329 12 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 61329 12 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 8245 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 8245 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 183111 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 183111 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 160965 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 160965 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 1432 83 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 1432 83 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 1432 83 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 1432 83 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 1432 83 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 1432 83 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 8246 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 8246 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 182159 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 182159 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 7977 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 7977 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 8163 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 8163 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 182945 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 182945 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 7970 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 7970 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 7971 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 7971 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 8275 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 8275 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 178240 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 178240 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 178240 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 8104 1 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 8104 1 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 1389 114 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 1389 114 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 1389 114 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 1389 114 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 1389 114 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 8346 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 8346 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 182767 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 182767 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 183434 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 183434 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 8194 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 8194 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 182719 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 182719 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 8378 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 8378 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 8244 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 8244 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 14076 22 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 14076 22 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 7720 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 7720 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 2182 50 None -21379 21 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 2182 50 None -21379 21 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 2182 50 None -21379 21 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 2182 50 None -21379 21 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 2182 50 None -21379 21 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 181872 6 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 181872 6 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 102941 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 102941 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 147359 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 147359 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 7997 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 7997 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 181860 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 181860 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 182990 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 182990 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 1909 20 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 1909 20 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 1909 20 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 182353 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 182353 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 182240 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 182240 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 182908 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 182908 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 7976 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 7976 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 2150 84 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 2150 84 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 2150 84 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 2150 84 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 1909 20 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 1909 20 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 1909 20 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 183238 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 183238 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 7713 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 7713 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 182528 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 182528 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 182068 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 182068 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 182827 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 182827 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 8371 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 8371 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 7912 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 7912 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 181850 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 181850 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 8103 29 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 8103 29 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 183073 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 183073 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 2150 84 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 2150 84 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 2150 84 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 2150 84 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 183574 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 183574 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 183448 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 183448 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 8347 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 8347 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 183287 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 183287 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 3804 49 None -33 26 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 3804 49 None -33 26 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 3804 49 None -33 26 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 182694 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 182694 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 183131 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 183131 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 183037 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 183037 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 182488 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 182488 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 182202 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 182202 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 182076 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 182076 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 181652 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 181652 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 182579 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 182579 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 182804 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 182804 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 8337 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 8337 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 182710 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 182710 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 182144 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 182144 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 181804 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 181804 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
CHEMBL5087167 215074 0 None - 2 Mouse 5.2 pIC50 = 5.2 Binding
mBMMC chemotaxismBMMC chemotaxis
ChEMBL None None None Cn1cc2c(-c3c(-c4ccc(F)cn4)nn4c3COC(C)(C)C4)ccnc2n1 10.6019/CHEMBL5058645
89477445 182050 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 182050 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 183340 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 183340 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 2142 31 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 2142 31 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 2142 31 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 8274 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 8274 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 8129 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 8129 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 2150 84 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 2150 84 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 2150 84 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 2150 84 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 8106 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 8106 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 8416 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 8416 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 7721 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 7721 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 2150 84 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 2150 84 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 2150 84 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 2150 84 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 89728 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 89728 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 80266 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 80266 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 178240 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 178240 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 178240 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 958 93 None -57 89 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
38 958 93 None -57 89 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
722 958 93 None -57 89 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 958 93 None -57 89 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 958 93 None -57 89 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 2142 31 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 2142 31 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 2142 31 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 80266 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 80266 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 89729 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 89729 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 1932 119 None -12 24 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 1932 119 None -12 24 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 1932 119 None -12 24 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 1932 119 None -12 24 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 1932 119 None -12 24 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 1932 119 None -12 24 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 958 93 None -57 89 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
38 958 93 None -57 89 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
722 958 93 None -57 89 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 958 93 None -57 89 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 958 93 None -57 89 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 176320 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 176320 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 176320 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 176320 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 178272 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 178272 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 178272 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 1932 119 None -3 24 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 1932 119 None -3 24 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 1932 119 None -3 24 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 1932 119 None -3 24 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 1932 119 None -3 24 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 1932 119 None -3 24 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 3159 96 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 3159 96 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 3159 96 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 3159 96 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 3159 96 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 192762 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 192762 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 192762 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 192766 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 192766 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 192766 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 192779 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 192779 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 192779 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 192785 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 192785 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 192785 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 192801 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 192801 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 192801 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 192803 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 192803 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 192803 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 192805 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 192805 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 192805 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 192808 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 192808 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 192808 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 192809 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 192809 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 192809 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 192826 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 192826 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 192826 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 192835 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 192835 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 192835 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 192846 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 192846 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 192846 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 192848 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 192848 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 192848 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 192851 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 192851 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 192851 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 192865 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 192865 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 192865 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 192881 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 192881 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 192881 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 192882 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 192882 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 192882 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 192893 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 192893 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 192893 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 192895 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 192895 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 192895 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 192900 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 192900 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 192900 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 192906 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 192906 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 192906 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 192910 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 192910 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 192910 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 192924 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 192924 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 192924 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 192926 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 192926 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 192926 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 192968 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 192968 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 192968 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 192973 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 192973 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 192973 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 192979 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 192979 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 192979 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 192997 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 192997 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 192997 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 193006 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 193006 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 193006 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 193010 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 193010 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 193010 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 193014 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 193014 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 193014 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 193018 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 193018 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 193018 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 193019 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 193019 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 193019 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 193020 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 193020 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 193020 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 193026 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 193026 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 193026 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 193031 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 193031 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 193031 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 193035 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 193035 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 193035 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 193040 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 193040 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 193040 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 193041 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 193041 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 193041 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 193045 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 193045 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 193045 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 193048 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 193048 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 193048 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 178240 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 178240 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 178240 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 178272 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 178272 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 178272 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 176320 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 176320 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 176320 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 176320 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 178240 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 178240 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 178240 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 958 93 None -57 89 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
38 958 93 None -57 89 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
722 958 93 None -57 89 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 958 93 None -57 89 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 958 93 None -57 89 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 89726 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 89726 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 176320 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 176320 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 176320 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 176320 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 176320 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 176320 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 176320 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 176320 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 80266 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 80266 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 295 12 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 295 12 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 295 12 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 295 12 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 2150 84 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 2150 84 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 2150 84 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 2150 84 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 953 41 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 953 41 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 953 41 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 953 41 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 953 41 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 953 41 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 178240 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 178240 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 178240 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 176320 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 176320 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 176320 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 176320 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 176320 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 176320 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 176320 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 176320 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 176320 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 176320 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 176320 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 176320 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 176320 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 176320 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 176320 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 176320 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 176320 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 176320 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 176320 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 176320 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 178240 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 178240 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 178240 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 69740 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 69740 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 176320 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 176320 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 176320 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 176320 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 178240 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 178240 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 178240 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 1932 119 None -15 24 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 1932 119 None -15 24 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 1932 119 None -15 24 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 1932 119 None -15 24 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 1932 119 None -15 24 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 1932 119 None -15 24 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 178240 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 178240 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 178240 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 1932 119 None -3 24 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 1932 119 None -3 24 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 1932 119 None -3 24 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 1932 119 None -3 24 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 1932 119 None -3 24 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 1932 119 None -3 24 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 178240 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 178240 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 178240 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 176320 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 176320 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 176320 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 176320 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 176320 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 176320 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 176320 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 176320 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 178240 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 178240 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 178240 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 178240 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 178240 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 178240 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 178240 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 178240 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 178240 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 958 93 None -57 89 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
38 958 93 None -57 89 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
722 958 93 None -57 89 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 958 93 None -57 89 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 958 93 None -57 89 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 80266 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 80266 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 178272 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 178272 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 178272 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 178272 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 178272 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 178272 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 89725 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 89725 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 178240 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 178240 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 178240 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 61535 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 61535 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 68048 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 68048 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 61531 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 61531 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 6604 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 6604 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 61528 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 61528 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 68040 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 68040 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 8162 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 8162 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 68131 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 68131 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 117133 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 117133 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 68106 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 68106 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 61533 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 61533 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 68101 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 68101 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 110128 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 110128 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 1932 119 None -3 24 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 1932 119 None -3 24 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 1932 119 None -3 24 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 1932 119 None -3 24 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 1932 119 None -3 24 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 1932 119 None -3 24 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 953 41 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 953 41 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 953 41 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 61552 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 61552 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 61562 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 61562 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 136457 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 136457 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 110125 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 110125 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 117120 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 117120 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 136457 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 136457 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 68111 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 68111 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 68133 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 68133 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 140835 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 140835 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 8984 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 8984 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 110126 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 110126 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 68047 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 68047 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 68049 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 68049 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 8984 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 8984 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 176547 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 176547 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 176547 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 110125 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 110125 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 176547 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 176547 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 176547 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 110124 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 110124 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 5890 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 5890 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 193178 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 193178 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 110143 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 110143 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 5890 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 5890 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 199556 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 199556 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 953 41 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 953 41 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 953 41 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 195499 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 195499 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 195499 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 1932 119 None -3 24 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 1932 119 None -3 24 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 1932 119 None -3 24 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 1932 119 None -3 24 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 1932 119 None -3 24 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 1932 119 None -3 24 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 2010 34 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 2010 34 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 2010 34 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 2010 34 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 68218 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 68218 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 110151 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 110151 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 110132 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 110132 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 7785 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 7785 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 187414 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 187414 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 68212 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 68212 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 112170 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 112170 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 2009 16 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 2009 16 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 2009 16 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 4063 16 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 4063 16 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 4063 16 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 204534 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 204534 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 89646 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 89646 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 89671 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 89671 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 953 41 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 953 41 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 953 41 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 953 41 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 953 41 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 953 41 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 2009 16 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 2009 16 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 2009 16 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 61547 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 61547 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 75683 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 75683 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 199429 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 199429 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 953 41 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 953 41 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 953 41 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 196014 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 196014 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 196014 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 196015 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 196015 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 196015 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 196482 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 196482 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 196482 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 68129 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 68129 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 68136 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 68136 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 68139 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 68139 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 295 12 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 295 12 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 295 12 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 295 12 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 89731 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 89731 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 89725 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 89725 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 193106 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 193106 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 56480 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 56480 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 199508 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 199508 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 75799 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 75799 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 141297 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 141297 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 205244 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 205244 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 61525 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 61525 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 75680 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 75680 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 75688 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 75688 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 58887 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 58887 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 196202 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 196202 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 196202 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 110145 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 110145 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 75644 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 75644 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 67062 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 67062 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 5150 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 5150 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 89658 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 89658 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 89669 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 89669 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 18945 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 18945 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 75639 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 75639 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 75659 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 75659 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 104168 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 104168 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 7025 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 7025 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 98970 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 98970 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 117432 12 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 117432 12 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 89653 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 89653 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 117135 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 117135 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 69902 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 69902 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 80266 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 80266 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 96122 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 96122 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 138611 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 138611 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 68100 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 68100 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 173831 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 173831 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 179309 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 179309 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 186786 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 186786 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 173831 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 173831 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 186786 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 186786 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 86487 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 86487 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 5150 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 5150 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 67884 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 67884 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 68119 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 68119 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 140228 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 140228 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 63120 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 63120 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 63120 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 112190 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 112190 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 16421 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 16421 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 166487 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 166487 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 174239 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 174239 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 174239 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 174239 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 172908 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 172908 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 2150 84 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 2150 84 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 2150 84 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 2150 84 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 12398 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 12398 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 12398 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 12398 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 138716 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 138716 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 61548 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 61548 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 187588 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 187588 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 69728 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 69728 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 117116 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 117116 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 158650 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 158650 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 137417 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 137417 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 112171 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 112171 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 156111 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 156111 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 117017 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 117017 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 117017 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 117017 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 3846 26 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 3846 26 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 3846 26 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 3846 26 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 150329 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 150329 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 193106 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 193106 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 115913 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 115913 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 68134 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 68134 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 117017 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 117017 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 110136 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 110136 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 89721 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 89721 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 199199 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 199199 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 89718 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 89718 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 3682 10 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 3682 10 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 3682 10 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 176320 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 176320 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 176320 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 176320 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 96534 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 96534 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 2150 84 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 2150 84 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 2150 84 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 2150 84 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 160963 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 160963 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 1432 83 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 1432 83 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 1432 83 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 1432 83 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 1432 83 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 1432 83 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 2037 52 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 2037 52 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 2037 52 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 2037 52 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 69722 15 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 69722 15 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 58905 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 58905 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 185932 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 185932 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 186019 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 186019 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 176385 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 176385 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 176385 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 123918 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 123918 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 58882 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 58882 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 58902 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 58902 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 77948 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 77948 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 61549 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 61549 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 117122 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 117122 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 96341 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 96341 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 8091 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 8091 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 75016 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 75016 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 80118 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 80118 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 5496 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 5496 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 5496 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 117123 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 117123 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 2150 84 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 2150 84 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 2150 84 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 2150 84 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 112188 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 112188 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 2150 84 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 2150 84 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 2150 84 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 2150 84 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 3682 10 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 3682 10 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 3682 10 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 2142 31 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 2142 31 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 2142 31 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 2142 31 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 2142 31 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 2142 31 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 110142 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 110142 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 68107 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 68107 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 2150 84 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 2150 84 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 2150 84 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 2150 84 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 2150 84 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 2150 84 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 2150 84 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 2150 84 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 1932 119 None -3 24 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 1932 119 None -3 24 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 1932 119 None -3 24 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 1932 119 None -3 24 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 1932 119 None -3 24 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 1932 119 None -3 24 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 2150 84 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 2150 84 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 2150 84 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 2150 84 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 1932 119 None -3 24 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 1932 119 None -3 24 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 1932 119 None -3 24 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 1932 119 None -3 24 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 1932 119 None -3 24 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 1932 119 None -3 24 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 1932 119 None -3 24 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 1932 119 None -3 24 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 1932 119 None -3 24 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 1932 119 None -3 24 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 1932 119 None -3 24 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 1932 119 None -3 24 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 176320 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 176320 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 176320 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 176320 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 2019 20 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 2019 20 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 2019 20 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 295 12 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 295 12 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 295 12 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 295 12 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 89714 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 89714 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 89732 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 89732 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 295 12 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 295 12 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 295 12 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 295 12 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 2142 31 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 2142 31 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 2142 31 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 2142 31 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 2142 31 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 2142 31 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 188180 9 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 188180 9 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 188180 9 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 1932 119 None -3 24 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 1932 119 None -3 24 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 1932 119 None -3 24 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 1932 119 None -3 24 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 1932 119 None -3 24 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 1932 119 None -3 24 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 176320 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 176320 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 176320 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 176320 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 1932 119 None -3 24 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 1932 119 None -3 24 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 1932 119 None -3 24 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 1932 119 None -3 24 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 1932 119 None -3 24 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 1932 119 None -3 24 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 2009 16 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 2009 16 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 2009 16 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 2058 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 2058 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 2058 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 169016 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 169016 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 169016 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 169016 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 169016 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 169016 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 2058 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 2058 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 2058 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 1932 119 None -3 24 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 1932 119 None -3 24 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 1932 119 None -3 24 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 1932 119 None -3 24 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 1932 119 None -3 24 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 1932 119 None -3 24 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 19434 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 19434 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 75668 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 75668 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 188658 5 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 188658 5 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 199534 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 199534 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 4063 16 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 4063 16 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 4063 16 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 194907 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 194907 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 194907 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 2150 84 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 2150 84 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 2150 84 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 2150 84 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 2009 16 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 2009 16 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 2009 16 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 192717 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 192717 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 140315 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 140315 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 68045 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 68045 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 202612 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 202612 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 174724 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 174724 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 193041 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 193041 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 193041 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 184838 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 184838 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 5799 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 5799 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 68121 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 68121 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 6280 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 6280 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 6280 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 295 12 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 295 12 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 295 12 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 295 12 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 295 12 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 295 12 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 295 12 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 295 12 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 953 41 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 953 41 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 953 41 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 6280 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 6280 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 6280 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 104415 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 104415 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 3804 49 None -33 26 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 3804 49 None -33 26 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 3804 49 None -33 26 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 10381 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 10381 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 16036 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 16036 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 3804 49 None -33 26 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 3804 49 None -33 26 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 3804 49 None -33 26 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 109271 10 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 109271 10 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 68143 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 68143 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 3804 49 None -33 26 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 3804 49 None -33 26 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 3804 49 None -33 26 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 2150 84 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 2150 84 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 2150 84 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 2150 84 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 109271 10 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 109271 10 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 204474 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 204474 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 71612 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 71612 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 71612 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 76211 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 76211 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 76673 3 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 76673 3 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 3804 49 None -33 26 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 3804 49 None -33 26 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 3804 49 None -33 26 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 109271 10 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 109271 10 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 93612 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 93612 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 89650 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 89650 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 89665 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 89665 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 205284 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 205284 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 5362 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 5362 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 56479 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 56479 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 193018 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 193018 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 193018 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 75645 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 75645 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 115912 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 115912 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 112172 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 112172 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 80347 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 80347 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 61553 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 61553 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 68211 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 68211 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 68211 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 68211 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 172591 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 172591 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 172591 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 172591 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 68117 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 68117 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 96111 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 96111 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 185662 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 185662 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 5362 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 5362 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 69867 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 69867 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 2150 84 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 2150 84 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 2150 84 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 2150 84 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 68123 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 68123 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 176463 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 176463 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 176463 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 1932 119 None -3 24 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 1932 119 None -3 24 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 1932 119 None -3 24 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 1932 119 None -3 24 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 1932 119 None -3 24 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 1932 119 None -3 24 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 81113 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 81113 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 16758 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 16758 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 159003 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 159003 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 117185 13 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 117185 13 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 105213 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 105213 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 96075 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 96075 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 63159 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 63159 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 63159 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 186378 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 186378 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 61546 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 61546 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 63159 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 63159 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 63159 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 7373 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 7373 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 176038 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 176038 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 117126 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 117126 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 71613 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 71613 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 71613 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 173413 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 173413 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 173413 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 173413 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 185098 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 185098 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 185942 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 185942 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 186335 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 186335 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 56479 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 56479 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 1932 119 None -12 24 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 1932 119 None -12 24 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 1932 119 None -12 24 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 1932 119 None -12 24 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 1932 119 None -12 24 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 1932 119 None -12 24 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 14530 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 14530 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 68095 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 68095 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 200016 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 200016 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 68124 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 68124 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 89726 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 89726 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 19379 56 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 19379 56 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 96137 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 96137 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 80019 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 80019 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 137358 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 137358 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 184584 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 184584 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 68187 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 68187 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 19424 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 19424 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 19424 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 19424 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 2150 84 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 2150 84 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 2150 84 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 2150 84 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 6392 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 6392 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 19424 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 19424 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 178240 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 178240 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 178240 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 187287 45 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 187287 45 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 2009 16 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 2009 16 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 2009 16 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 1932 119 None -3 24 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 1932 119 None -3 24 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 1932 119 None -3 24 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 1932 119 None -3 24 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 1932 119 None -3 24 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 1932 119 None -3 24 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 158888 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 158888 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 89720 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 89720 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 61551 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 61551 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 189346 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 189346 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 58896 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 58896 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 86469 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 86469 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 86495 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 86495 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 178277 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 178277 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 178277 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 97020 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 97020 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 67883 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 67883 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 117109 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 117109 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 79980 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 79980 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 199859 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 199859 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 87008 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 87008 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 137346 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 137346 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 68120 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 68120 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 2067 25 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 2067 25 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 2067 25 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 2067 25 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 199866 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 199866 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 5500 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 5500 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 5500 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 166692 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 166692 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 116835 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 116835 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 116835 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 116835 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 136617 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 136617 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 71625 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 71625 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 71625 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 112184 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 112184 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 193227 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 193227 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 156131 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 156131 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 193227 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 193227 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 185616 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 185616 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 61527 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 61527 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 200434 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 200434 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 200434 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 10380 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 10380 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 68147 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 68147 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 118108 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 118108 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 168662 11 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 168662 11 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 118108 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 118108 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 168662 11 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 168662 11 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 69736 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 69736 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 61545 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 61545 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 118108 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 118108 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 168662 11 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 168662 11 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 89729 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 89729 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 69740 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 69740 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 89717 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 89717 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 187481 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 187481 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 199201 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 199201 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 56483 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 56483 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 173409 9 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 173409 9 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 56483 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 56483 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 1932 119 None -3 24 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 1932 119 None -3 24 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 1932 119 None -3 24 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 1932 119 None -3 24 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 1932 119 None -3 24 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 1932 119 None -3 24 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 953 41 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 953 41 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 953 41 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 1932 119 None -3 24 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 1932 119 None -3 24 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 1932 119 None -3 24 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 1932 119 None -3 24 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 1932 119 None -3 24 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 1932 119 None -3 24 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 2150 84 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 2150 84 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 2150 84 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 2150 84 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 19442 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 19442 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 75687 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 75687 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 168662 11 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 168662 11 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 2150 84 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 2150 84 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 2150 84 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 2150 84 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 188180 9 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 188180 9 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 188180 9 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 195349 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 195349 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 195349 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 2150 84 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 2150 84 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 2150 84 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 2150 84 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 176495 4 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 176495 4 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 176495 4 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 187583 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 187583 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 199988 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 199988 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 7368 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 7368 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 199386 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 199386 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 137450 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 137450 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 179097 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 179097 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 58886 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 58886 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 6603 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 6603 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 63165 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 63165 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 63165 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 176874 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 176874 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 179309 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 179309 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 3804 49 None -33 26 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 3804 49 None -33 26 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 3804 49 None -33 26 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 115919 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 115919 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 167427 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 167427 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 63165 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 63165 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 63165 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 63172 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 63172 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 63172 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 140315 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 140315 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 63172 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 63172 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 63172 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 68144 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 68144 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 68109 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 68109 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 68126 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 68126 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 199900 14 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 199900 14 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 953 41 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 953 41 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 953 41 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 169016 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 169016 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 75020 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 75020 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 140544 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 140544 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 75640 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 75640 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 75646 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 75646 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 196183 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 196183 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 196183 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 196230 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 196230 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 1932 119 None -3 24 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 1932 119 None -3 24 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 1932 119 None -3 24 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 1932 119 None -3 24 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 1932 119 None -3 24 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 1932 119 None -3 24 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 140765 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 140765 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 45 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 45 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 45 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 137285 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 137285 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 75678 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 75678 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 96295 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 96295 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 67877 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 67877 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 35336 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 35336 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 75676 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 75676 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 110154 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 110154 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 68209 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 68209 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 69740 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 69740 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 188180 9 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 188180 9 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 188180 9 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 115914 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 115914 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 117117 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 117117 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 68209 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 68209 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 68184 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 68184 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 71641 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 71641 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 71641 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 89722 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 89722 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 199904 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 199904 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 172541 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 172541 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 68317 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 68317 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 1389 114 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 1389 114 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 1389 114 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 1389 114 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 1389 114 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 61543 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 61543 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 6249 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 6249 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 6249 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 91870 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 91870 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 65629 6 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 10.6019/CHEMBL5212743
CHEMBL1834199 65629 6 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 10.6019/CHEMBL5212743
137634349 156015 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 156015 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 186473 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 186473 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 176152 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 176152 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 95978 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 95978 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 2150 84 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 2150 84 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 2150 84 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 2150 84 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 16754 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 16754 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 19379 56 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 19379 56 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 69731 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 69731 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 2150 84 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 2150 84 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 2150 84 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 2150 84 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 19379 56 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 19379 56 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 199428 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 199428 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 184562 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 184562 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 86484 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 86484 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 137276 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 137276 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 180509 9 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 180509 9 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 184716 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 184716 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 157820 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 157820 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 69740 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 69740 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 112174 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 112174 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 7369 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 7369 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 117114 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 117114 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 80092 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 80092 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 199389 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 199389 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 958 93 None -57 89 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
38 958 93 None -57 89 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
722 958 93 None -57 89 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 958 93 None -57 89 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 958 93 None -57 89 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 67881 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 67881 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 185862 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 185862 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 3804 49 None -33 26 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 3804 49 None -33 26 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 3804 49 None -33 26 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 123917 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 123917 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 112189 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 112189 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 68220 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 68220 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 199904 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 199904 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 68114 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 68114 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 2150 84 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 2150 84 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 2150 84 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 2150 84 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 15495 24 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 15495 24 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 140302 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 140302 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 68116 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 68116 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 58883 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 58883 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 177122 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 177122 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 58885 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 58885 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 2067 25 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 2067 25 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 2067 25 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 2067 25 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 199817 33 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 199817 33 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 174251 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 174251 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 176616 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 176616 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 176616 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 187481 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 187481 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 174233 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 174233 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 193273 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 193273 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 174233 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 174233 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 193273 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 193273 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 942 60 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 942 60 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 942 60 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 2142 31 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 2142 31 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 2142 31 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 2142 31 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 2142 31 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 2142 31 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 213975 10 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 10.6019/CHEMBL5212743
54581937 61523 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 61523 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 157738 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 157738 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 116844 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 116844 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 116844 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 116844 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 69732 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 69732 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 115918 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 115918 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 115918 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 115918 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 68053 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 68053 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 68112 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 68112 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 114427 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 114427 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 116844 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 116844 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 8378 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 8378 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 199383 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 199383 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 89728 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 89728 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 56481 3 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 56481 3 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 56482 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 56482 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 2150 84 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 2150 84 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 2150 84 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 2150 84 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 2014 39 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 2014 39 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 2014 39 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 2014 39 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 2014 39 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 2014 39 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 2014 39 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 2014 39 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 2014 39 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 139262 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 139262 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 187287 45 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 187287 45 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 75650 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 75650 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 75690 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 75690 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 116844 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 116844 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 1932 119 None -3 24 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 1932 119 None -3 24 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 1932 119 None -3 24 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 1932 119 None -3 24 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 1932 119 None -3 24 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 1932 119 None -3 24 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 2150 84 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 2150 84 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 2150 84 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 2150 84 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 139281 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 139281 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 176329 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 176329 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 176329 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 184454 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 184454 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 185088 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 185088 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 176320 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 176320 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 176320 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 176320 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 178246 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 178246 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 178246 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 137467 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 137467 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 68170 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 68170 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 69903 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 69903 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 56481 3 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 56481 3 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 66899 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 66899 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 5209 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 5209 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 958 93 None -57 89 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
38 958 93 None -57 89 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
722 958 93 None -57 89 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 958 93 None -57 89 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 958 93 None -57 89 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 75030 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 75030 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 76049 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 76049 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 65123 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 65123 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 19379 56 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 19379 56 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 187414 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 187414 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 75670 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 75670 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 96017 5 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 96017 5 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 176629 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 176629 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 176629 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 2500 8 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 2500 8 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 2500 8 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 2500 8 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 2500 8 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 2500 8 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 89661 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 89661 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 69866 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 69866 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 75636 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 75636 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 75648 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 75648 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 66940 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 66940 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 5290 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 5290 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 109629 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 109629 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 137518 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 137518 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 184544 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 184544 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 61524 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 61524 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 61561 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 61561 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 115921 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 115921 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 117112 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 117112 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 117125 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 117125 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 117130 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 117130 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 8163 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 8163 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 68132 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 68132 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 68138 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 68138 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 110148 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 110148 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 2150 84 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 2150 84 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 2150 84 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 2150 84 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 295 12 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 295 12 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 295 12 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 295 12 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 295 12 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 295 12 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 295 12 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 295 12 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 110147 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 110147 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 68050 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 68050 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 953 41 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 953 41 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 953 41 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 7785 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 7785 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 5599 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 5599 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 2150 84 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 2150 84 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 2150 84 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 2150 84 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 2150 84 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 2150 84 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 2150 84 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 2150 84 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 159587 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 159587 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 110133 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 110133 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 187254 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 187254 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 6516 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 6516 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 2132 34 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 2132 34 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 2132 34 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 110122 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 110122 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 110125 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 110125 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 68130 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 68130 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 295 12 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 295 12 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 295 12 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 295 12 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 295 12 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 295 12 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 295 12 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 295 12 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 3125 71 None -562 30 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 3125 71 None -562 30 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 3125 71 None -562 30 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 3125 71 None -562 30 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 3125 71 None -562 30 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 14076 22 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 14076 22 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 7022 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 7022 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 68319 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 68319 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 68320 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 68320 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 68325 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 68325 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 69864 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 69864 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 118441 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 118441 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 112176 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 112176 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 176636 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 176636 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 176636 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 176472 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 176472 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 176472 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 96311 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 96311 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 203649 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 203649 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 110309 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 110309 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 96311 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 96311 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 5290 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 5290 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 202145 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 202145 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 200178 18 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 200178 18 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 58904 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 58904 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 69909 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 69909 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 149129 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 149129 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 110140 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 110140 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 117107 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 117107 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 110140 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 110140 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 110141 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 110141 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 68098 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 68098 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 68103 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 68103 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 68118 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 68118 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 72571 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 72571 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 58898 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 58898 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 89723 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 89723 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 2014 39 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 2014 39 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 2014 39 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 2182 50 None -21379 21 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 2182 50 None -21379 21 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 2182 50 None -21379 21 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 2182 50 None -21379 21 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 2182 50 None -21379 21 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 68214 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 68214 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 68214 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 68214 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 68214 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 68214 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 68215 14 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 68215 14 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 68215 14 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 68215 14 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 192766 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 192766 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 192766 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 180509 9 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 180509 9 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 1932 119 None -15 24 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 1932 119 None -15 24 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 1932 119 None -15 24 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 1932 119 None -15 24 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 1932 119 None -15 24 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 1932 119 None -15 24 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 185110 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 185110 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 109629 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 109629 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 159526 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 159526 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 10902 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 10902 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 117108 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 117108 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 1932 119 None -3 24 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 1932 119 None -3 24 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 1932 119 None -3 24 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 1932 119 None -3 24 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 1932 119 None -3 24 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 1932 119 None -3 24 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 176417 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 176417 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 176417 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 155723 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 155723 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 58903 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 58903 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 108568 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 108568 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 10384 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 10384 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 140238 3 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 140238 3 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 2014 39 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 2014 39 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 2014 39 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 84229 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 84229 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 202379 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 202379 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 69724 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 69724 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 174231 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 174231 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 174231 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 174231 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 199509 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 199509 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 5209 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 5209 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 124020 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 124020 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 67878 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 67878 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 185260 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 185260 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 6537 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 6537 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 71629 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 71629 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 71629 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 96031 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 96031 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 96251 61 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 96251 61 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 96134 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 96134 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 19165 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 19165 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 19165 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 19165 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 69740 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 69740 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 14965 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 14965 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 19165 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 19165 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 199908 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 199908 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 68322 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 68322 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 144097 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 144097 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 144774 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 144774 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 7242 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 7242 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 69725 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 69725 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 192835 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 192835 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 192835 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 96223 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 96223 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 96298 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 96298 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 185133 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 185133 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 68326 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 68326 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 112182 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 112182 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 112182 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 112182 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 200176 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 200176 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 186938 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 186938 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 112179 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 112179 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 69730 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 69730 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 61559 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 61559 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 174238 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 174238 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 207031 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 207031 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 140200 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 140200 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 117140 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 117140 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 69031 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 69031 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 150652 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 150652 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 79057 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 79057 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 2015 20 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 2015 20 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 2015 20 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 123920 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 123920 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 173655 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 173655 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 199867 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 199867 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 11265 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 11265 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 11265 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 61536 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 61536 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 199908 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 199908 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 110127 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 110127 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 110134 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 110134 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 68141 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 68141 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 125051 4 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 125051 4 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 2019 20 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 2019 20 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 2019 20 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 104195 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 104195 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 204481 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 204481 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 1932 119 None -3 24 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 1932 119 None -3 24 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 1932 119 None -3 24 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 1932 119 None -3 24 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 1932 119 None -3 24 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 1932 119 None -3 24 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 89656 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 89656 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 19379 56 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 19379 56 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 19165 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 19165 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 19379 56 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 19379 56 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 75647 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 75647 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 89730 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 89730 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 80266 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 80266 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 195050 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 195050 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 195050 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 195472 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 195472 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 195503 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 195503 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 195503 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 195591 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 195591 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 195591 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 196040 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 196040 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 196040 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 1932 119 None -3 24 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 1932 119 None -3 24 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 1932 119 None -3 24 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 1932 119 None -3 24 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 1932 119 None -3 24 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 1932 119 None -3 24 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 4064 16 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 4064 16 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 4064 16 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 118108 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 118108 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 188658 5 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 188658 5 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 140302 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 140302 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 137881 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 137881 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 137881 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 137881 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 68167 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 68167 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 199948 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 199948 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 2015 20 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 2015 20 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 2015 20 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 2017 21 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 2017 21 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 2017 21 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 2067 25 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 2067 25 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 2067 25 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 2067 25 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 2017 21 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 2017 21 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 2017 21 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 12770 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 12770 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 12770 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 75633 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 75633 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 75669 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 75669 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 75675 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 75675 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 75689 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 75689 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 58910 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 58910 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 56477 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 56477 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 56477 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 109360 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 109360 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 89663 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 89663 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 75632 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 75632 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 75657 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 75657 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 156317 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 156317 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 109360 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 109360 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 66703 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 66703 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 66790 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 66790 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 125517 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 125517 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 140121 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 140121 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 86490 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 86490 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 123924 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 123924 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 123914 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 123914 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 61521 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 61521 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 110131 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 110131 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 186937 1 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 186937 1 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 186937 1 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 186937 1 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 123922 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 123922 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 2132 34 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 2132 34 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 2132 34 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 2132 34 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 2132 34 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 2132 34 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 6589 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 6589 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 84263 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 84263 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 69910 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 69910 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 84263 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 84263 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 141977 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 141977 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 68099 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 68099 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 2132 34 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 2132 34 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 2132 34 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 96132 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 96132 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 174238 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 174238 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 200975 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 200975 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 18852 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 18852 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 176324 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 176324 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 176324 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 186083 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 186083 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 137489 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 137489 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 86497 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 86497 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 123921 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 123921 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 175376 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 175376 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 86494 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 86494 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 69904 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 69904 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 136861 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 136861 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 189085 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 189085 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 202598 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 202598 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 160171 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 160171 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 176386 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 176386 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 176386 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 96222 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 96222 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 184950 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 184950 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 159353 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 159353 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 3804 49 None -33 26 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 3804 49 None -33 26 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 3804 49 None -33 26 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 148563 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 148563 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 97220 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 97220 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 3804 49 None -33 26 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 3804 49 None -33 26 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 3804 49 None -33 26 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 89728 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 89728 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 78009 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 78009 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 68173 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 68173 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 58894 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 58894 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 187587 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 187587 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 187587 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 187587 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 67882 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 67882 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 173264 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 173264 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 61522 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 61522 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 84843 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 84843 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 110146 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 110146 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 80266 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 80266 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 80266 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 80266 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 179281 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 179281 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 179281 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 179281 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 178320 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 178320 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 178320 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 199943 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 199943 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 172843 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 172843 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 140934 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 140934 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 79852 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 79852 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 79852 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 69734 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 69734 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 61530 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 61530 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 68110 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 68110 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 89729 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 89729 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 71627 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 71627 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 71627 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 140245 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 140245 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 5981 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 5981 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 5981 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 179350 12 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 179350 12 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 200054 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 200054 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 69021 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 69021 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 86483 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 86483 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 173469 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 173469 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 178244 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 178244 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 178244 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 155195 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 155195 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 96057 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 96057 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 156157 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 156157 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 123888 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 123888 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 156272 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 156272 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 61526 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 61526 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 61529 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 61529 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 61537 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 61537 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 61558 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 61558 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 117128 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 117128 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 72519 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 72519 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 61529 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 61529 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 61561 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 61561 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 89673 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 89673 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 187414 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 187414 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 7746 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 7746 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 19442 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 19442 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 7316 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 7316 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 2150 84 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 2150 84 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 2150 84 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 2150 84 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 89715 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 89715 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 191386 10 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 191386 10 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 140849 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 140849 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 68054 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 68054 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 68127 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 68127 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 192718 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 192718 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 192718 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 192718 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 2010 34 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 2010 34 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 2010 34 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 2010 34 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 68096 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 68096 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 193106 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 193106 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 176451 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 176451 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 176451 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 188438 19 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 188438 19 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 2150 84 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 2150 84 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 2150 84 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 2150 84 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 3804 49 None -33 26 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 3804 49 None -33 26 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 3804 49 None -33 26 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 188658 5 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 188658 5 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 110137 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 110137 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 68105 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 68105 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 141313 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 141313 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 89713 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 89713 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 77952 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 77952 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 176320 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 176320 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 176320 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 176320 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 18945 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 18945 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 18945 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 18945 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 157967 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 157967 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 155976 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 155976 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 185452 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 185452 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 186069 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 186069 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 186565 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 186565 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 2142 31 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 2142 31 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 2142 31 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 2142 31 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 2142 31 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 2142 31 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 176384 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 176384 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 176384 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 201027 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 201027 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 139220 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 139220 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 19258 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 19258 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 19258 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 19258 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 188402 38 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 188402 38 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 68140 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 68140 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 19258 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 19258 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 139057 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 139057 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 56482 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 56482 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 18940 6 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 18940 6 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 206981 35 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 206981 35 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 206981 35 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 4064 16 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 4064 16 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 4064 16 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 206981 35 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 206981 35 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 206981 35 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 89648 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 89648 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 4064 16 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 4064 16 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 4064 16 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 71630 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 71630 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 71630 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 4064 16 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 4064 16 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 4064 16 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 2150 84 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 2150 84 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 2150 84 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 2150 84 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 75637 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 75637 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 75638 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 75638 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 75671 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 75671 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 75686 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 75686 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 118108 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 118108 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 196010 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 196010 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 196010 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 16759 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 16759 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 157442 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 157442 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 10904 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 10904 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 69866 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 69866 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 56480 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 56480 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 1424 28 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 1424 28 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 1424 28 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 1424 28 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 2033 24 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 2033 24 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 2033 24 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 2033 24 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 89651 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 89651 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 169016 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 169016 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 75019 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 75019 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 75541 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 75541 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 75572 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 75572 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 1424 28 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 1424 28 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 1424 28 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 1424 28 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 19379 56 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 19379 56 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 75642 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 75642 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 1424 28 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 1424 28 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 1424 28 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 1424 28 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 66758 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 66758 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 89652 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 89652 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 89660 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 89660 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 12772 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 12772 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 12772 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 137474 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 137474 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 186467 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 186467 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 69865 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 69865 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 167240 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 167240 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 18918 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 18918 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 18918 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 18918 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 69723 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 69723 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 99221 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 99221 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 7385 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 7385 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 18918 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 18918 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 68330 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 68330 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 115915 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 115915 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 68177 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 68177 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 96319 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 96319 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 139266 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 139266 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 139266 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 173866 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 173866 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 185722 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 185722 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 184383 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 184383 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 68316 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 68316 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 188866 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 188866 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 3804 49 None -33 26 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 3804 49 None -33 26 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 3804 49 None -33 26 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 110135 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 110135 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 86498 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 86498 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 117119 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 117119 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 68166 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 68166 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 68179 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 68179 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 67080 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 67080 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 199485 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 199485 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 178272 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 178272 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 178272 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 189079 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 189079 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 189079 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 189079 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 86499 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 86499 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 155692 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 155692 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 187626 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 187626 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 187626 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 187626 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 123811 26 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 123811 26 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 193010 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 193010 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 193010 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 187587 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 187587 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 187587 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 187587 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 202100 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 202100 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 202158 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 202158 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 68175 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 68175 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 186148 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 186148 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 68315 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 68315 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 187587 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 187587 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 68180 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 68180 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 140934 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 140934 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 2150 84 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 2150 84 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 2150 84 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 2150 84 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 89716 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 89716 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 189024 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 189024 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 189024 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 189024 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 140311 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 140311 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 199906 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 199906 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 199725 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 199725 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 123919 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 123919 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 176320 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 176320 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 176320 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 176320 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 140768 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 140768 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 110153 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 110153 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 61555 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 61555 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 110129 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 110129 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 110144 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 110144 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 176241 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 176241 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 176241 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 16753 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 16753 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 86464 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 86464 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 68169 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 68169 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 186850 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 186850 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 96123 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 96123 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 186850 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 186850 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 184903 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 184903 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 137359 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 137359 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 86488 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 86488 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 117141 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 117141 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 68182 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 68182 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 80346 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 80346 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 173427 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 173427 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 173427 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 173427 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 185198 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 185198 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 86500 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 86500 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 124022 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 124022 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 68186 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 68186 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 112177 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 112177 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 63124 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 63124 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 63124 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 123923 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 123923 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 19455 51 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 19455 51 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 19455 51 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 19455 51 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 19379 56 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 19379 56 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 173426 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 173426 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 173426 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 173426 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 141932 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 141932 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 71600 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 71600 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 71600 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 58909 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 58909 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 159310 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 159310 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 63124 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 63124 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 63124 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 117137 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 117137 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 60199 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 60199 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 60199 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 110123 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 110123 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 68137 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 68137 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 187181 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 187181 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 187181 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 187181 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 15495 24 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 15495 24 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 89645 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 89645 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 89662 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 89662 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 4060 6 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 4060 6 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 4060 6 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 74447 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 74447 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 139492 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 139492 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 75660 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 75660 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 75672 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 75672 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 75679 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 75679 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 75692 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 75692 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 96349 20 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 96349 20 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 187181 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 187181 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 96349 20 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 96349 20 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 196160 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 196160 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 953 41 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 953 41 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 953 41 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 86465 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 86465 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 108577 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 108577 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 89659 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 89659 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 76022 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 76022 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 13008 28 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 13008 28 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 13008 28 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 2150 84 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 2150 84 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 2150 84 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 2150 84 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 75662 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 75662 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 75673 25 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 75673 25 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 75677 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 75677 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 75682 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 75682 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 75691 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 75691 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 2082 13 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 2082 13 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 2082 13 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 12802 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 12802 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 12802 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 75634 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 75634 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 156156 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 156156 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 167082 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 167082 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 159196 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 159196 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 2150 84 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 2150 84 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 2150 84 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 2150 84 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 2150 84 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 2150 84 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 2150 84 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 2150 84 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 2150 84 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 2150 84 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 2150 84 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 2150 84 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 145930 1 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 145930 1 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 2150 84 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 2150 84 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 2150 84 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 2150 84 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 69738 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 69738 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 199556 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 199556 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 2150 84 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 2150 84 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 2150 84 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 2150 84 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 61539 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 61539 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 117118 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 117118 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 2150 84 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 2150 84 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 2150 84 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 2150 84 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 2150 84 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 2150 84 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 2150 84 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 2150 84 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 2150 84 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 2150 84 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 2150 84 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 2150 84 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 2150 84 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 2150 84 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 2150 84 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 2150 84 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 199385 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 199385 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 953 41 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 953 41 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 953 41 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 953 41 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 953 41 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 953 41 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 187181 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 187181 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 199508 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 199508 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 187181 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 187181 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 2150 84 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 2150 84 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 2150 84 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 2150 84 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 68219 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 68219 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 69911 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 69911 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 69913 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 69913 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 188438 19 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 188438 19 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 2150 84 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 2150 84 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 2150 84 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 2150 84 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 188438 19 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 188438 19 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 8378 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 8378 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 68097 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 68097 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 192717 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 192717 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 1932 119 None -3 24 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 1932 119 None -3 24 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 1932 119 None -3 24 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 1932 119 None -3 24 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 1932 119 None -3 24 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 1932 119 None -3 24 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 2150 84 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 2150 84 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 2150 84 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 2150 84 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 199556 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 199556 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 61557 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 61557 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 68128 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 68128 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 132817 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 132817 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 156967 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 156967 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 86466 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 86466 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 192906 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 192906 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 192906 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 179282 3 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 179282 3 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 179282 3 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 179282 3 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 112173 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 112173 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 187626 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 187626 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 187626 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 187626 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 72012 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 72012 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 68174 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 68174 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 63147 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 63147 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 63147 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 200178 18 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 200178 18 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 1932 119 None -15 24 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 1932 119 None -15 24 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 1932 119 None -15 24 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 1932 119 None -15 24 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 1932 119 None -15 24 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 1932 119 None -15 24 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 7024 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 7024 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 68168 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 68168 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 71599 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 71599 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 71599 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 173409 9 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 173409 9 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 199679 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 199679 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 205174 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 205174 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 157981 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 157981 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 63147 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 63147 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 63147 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 123915 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 123915 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 112181 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 112181 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 5895 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 5895 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 5895 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 3804 49 None -33 26 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 3804 49 None -33 26 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 3804 49 None -33 26 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 137281 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 137281 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 185377 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 185377 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 1432 83 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 1432 83 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 1432 83 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 1432 83 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 1432 83 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 1432 83 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 113386 1 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 113386 1 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 3804 49 None -33 26 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 3804 49 None -33 26 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 3804 49 None -33 26 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 3804 49 None -33 26 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 3804 49 None -33 26 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 3804 49 None -33 26 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 110155 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 110155 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 68113 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 68113 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 112180 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 112180 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 186886 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 186886 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 108577 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 108577 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 96058 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 96058 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 61542 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 61542 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 99221 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 99221 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 68115 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 68115 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 86491 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 86491 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 68171 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 68171 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 176483 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 176483 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 176483 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 58906 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 58906 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 58907 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 58907 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 192997 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 192997 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 192997 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 63166 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 63166 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 63166 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 184718 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 184718 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 63166 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 63166 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 63166 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 117131 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 117131 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 3804 49 None -33 26 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 3804 49 None -33 26 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 3804 49 None -33 26 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 78460 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 78460 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 115910 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 115910 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 58897 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 58897 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 205613 2 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 205613 2 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 2348 53 None -134 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 2348 53 None -134 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 2348 53 None -134 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 2348 53 None -134 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 2348 53 None -134 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 184436 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 184436 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 86493 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 86493 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 18842 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 18842 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 18842 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 18842 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 199679 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 199679 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 83453 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 83453 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 68052 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 68052 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 18842 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 18842 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 115916 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 115916 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 96059 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 96059 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 141820 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 141820 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 68122 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 68122 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 2132 34 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 2132 34 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 2132 34 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 2132 34 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 2132 34 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 2132 34 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 169016 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 169016 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 3804 49 None -33 26 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 3804 49 None -33 26 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 3804 49 None -33 26 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 174554 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 174554 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 96135 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 96135 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 205198 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 205198 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 60171 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 60171 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 60171 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 118146 34 None -20 12 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 118146 34 None -20 12 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 7746 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 7746 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 86467 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 86467 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 123913 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 123913 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 176320 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 176320 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 176320 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 176320 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 201219 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 201219 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 192926 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 192926 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 192926 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 185788 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 185788 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 69912 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 69912 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 117023 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 117023 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 19423 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 19423 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 19423 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 19423 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 69739 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 69739 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 188438 19 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 188438 19 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 953 41 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 953 41 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 953 41 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 2150 84 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 2150 84 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 2150 84 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 2150 84 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 2150 84 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 2150 84 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 2150 84 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 2150 84 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 117143 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 117143 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 2150 84 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 2150 84 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 2150 84 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 2150 84 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 8378 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 8378 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 110121 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 110121 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 19423 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 19423 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 176547 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 176547 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 176547 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 75667 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 75667 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 187287 45 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 187287 45 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 106051 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 106051 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 187287 45 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 187287 45 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 193178 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 193178 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 176547 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 176547 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 176547 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 193178 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 193178 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 192718 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 192718 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 16052 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 16052 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 68142 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 68142 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 89729 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 89729 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 6910 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 6910 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 2142 31 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 2142 31 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 2142 31 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 2142 31 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 2142 31 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 2142 31 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 199600 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 199600 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 187481 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 187481 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 16053 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 16053 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 110130 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 110130 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 186855 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 186855 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 187317 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 187317 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 96154 10 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 96154 10 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 96154 10 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 96154 10 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 68055 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 68055 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 191386 10 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 191386 10 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 199563 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 199563 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 61534 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 61534 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 115920 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 115920 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 68104 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 68104 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 2150 84 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 2150 84 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 2150 84 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 2150 84 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 56480 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 56480 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 56481 3 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 56481 3 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 89725 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 89725 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 3804 49 None -14 26 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 3804 49 None -14 26 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 3804 49 None -14 26 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 953 41 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 953 41 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 953 41 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 953 41 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 953 41 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 953 41 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 41 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 41 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 41 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 3195 19 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 3195 19 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 3195 19 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 204485 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 204485 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 953 41 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 953 41 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 953 41 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 953 41 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 953 41 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 953 41 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 953 41 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 953 41 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 953 41 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 953 41 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 953 41 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 953 41 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 89667 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 89667 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 89672 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 89672 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 74442 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 74442 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 76048 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 76048 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 138707 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 138707 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 18842 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 18842 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 199203 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 199203 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 195217 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 195217 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 195217 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 63123 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 63123 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 63123 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 7160 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 7160 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 3804 49 None -33 26 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 3804 49 None -33 26 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 3804 49 None -33 26 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 1932 119 None -15 24 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 1932 119 None -15 24 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 1932 119 None -15 24 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 1932 119 None -15 24 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 1932 119 None -15 24 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 1932 119 None -15 24 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 3804 49 None -33 26 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 3804 49 None -33 26 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 3804 49 None -33 26 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 3804 49 None -33 26 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 3804 49 None -33 26 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 3804 49 None -33 26 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 3804 49 None -33 26 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 3804 49 None -33 26 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 3804 49 None -33 26 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 3804 49 None -33 26 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 3804 49 None -33 26 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 3804 49 None -33 26 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 3804 49 None -33 26 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 3804 49 None -33 26 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 3804 49 None -33 26 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 3804 49 None -33 26 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 3804 49 None -33 26 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 3804 49 None -33 26 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 89616 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 89616 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 4061 11 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 4061 11 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 4061 11 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 75531 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 75531 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 76311 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 76311 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 75681 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 75681 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 958 93 None -57 89 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
38 958 93 None -57 89 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
722 958 93 None -57 89 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 958 93 None -57 89 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 958 93 None -57 89 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 123686 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 123686 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 404 33 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 404 33 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 404 33 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 75643 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 75643 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 75674 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 75674 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 63123 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 63123 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 63123 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 18945 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 18945 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 68216 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 68216 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 68216 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 68216 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 112187 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 112187 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 69906 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 69906 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 16051 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 16051 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 61538 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 61538 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 117111 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 117111 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 205687 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 205687 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 112175 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 112175 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 69868 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 69868 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 187354 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 187354 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 112178 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 112178 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 110138 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 110138 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 124019 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 124019 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 112178 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 112178 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 15507 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 15507 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 167111 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 167111 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 68046 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 68046 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 89727 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 89727 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 179350 12 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 179350 12 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 200083 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 200083 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 295 12 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 295 12 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 295 12 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 295 12 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 295 12 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 295 12 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 295 12 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 295 12 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 58899 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 58899 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 86496 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 86496 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 202073 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 202073 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 184984 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 184984 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 69735 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 69735 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 117127 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 117127 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 117136 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 117136 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 6909 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 6909 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 109798 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 109798 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 87008 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 87008 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 157210 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 157210 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 186809 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 186809 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 186809 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 186809 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 189085 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 189085 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 96297 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 96297 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 5776 6 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 5776 6 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 186886 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 186886 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 96296 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 96296 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 155952 11 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 155952 11 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 61541 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 61541 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 68323 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 68323 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 178341 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 178341 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 178341 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 186783 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 186783 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 58901 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 58901 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 60200 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 60200 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 60200 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 96160 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 96160 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 186783 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 186783 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 136732 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 136732 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 199085 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 199085 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 192851 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 192851 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 192851 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 193045 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 193045 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 193045 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 67876 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 67876 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 185132 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 185132 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 68321 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 68321 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 86486 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 86486 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 1932 119 None 1 24 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 1932 119 None 1 24 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 1932 119 None 1 24 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 1932 119 None 1 24 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 1932 119 None 1 24 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 1932 119 None 1 24 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 2150 84 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 2150 84 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 2150 84 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 2150 84 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 2150 84 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 2150 84 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 2150 84 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 2150 84 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 69719 26 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 69719 26 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 69737 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 69737 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 80266 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 80266 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 96154 10 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 96154 10 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 61519 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 61519 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 61550 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 61550 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 188739 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 188739 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 61550 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 61550 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 115917 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 115917 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 117121 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 117121 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 117139 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 117139 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 295 12 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 295 12 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 295 12 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 295 12 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 295 12 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 295 12 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 295 12 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 295 12 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 2010 34 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 2010 34 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 2010 34 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 2010 34 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 89657 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 89657 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 2150 84 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 2150 84 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 2150 84 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 2150 84 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 2010 34 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 2010 34 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 2010 34 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 2010 34 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 187287 45 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 187287 45 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 2150 84 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 2150 84 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 2150 84 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 2150 84 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 19423 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 19423 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 75664 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 75664 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 75665 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 75665 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 75666 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 75666 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 2010 34 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 2010 34 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 2010 34 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 2010 34 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 89728 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 89728 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 69915 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 69915 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 1932 119 None -3 24 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 1932 119 None -3 24 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 1932 119 None -3 24 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 1932 119 None -3 24 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 1932 119 None -3 24 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 1932 119 None -3 24 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 173411 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 173411 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 173411 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 173411 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 112185 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 112185 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 68327 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 68327 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 174355 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 174355 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 174355 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 174355 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 192924 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 192924 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 192924 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 7258 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 7258 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 18875 5 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 18875 5 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 18875 5 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 18875 5 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 18875 5 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 18875 5 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 161795 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 161795 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 942 60 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 942 60 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 942 60 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 942 60 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 942 60 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 942 60 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 68185 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 68185 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 176563 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 176563 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 176563 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 186782 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 186782 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 186782 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 186782 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 157906 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 157906 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 110140 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 110140 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 117129 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 117129 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 1932 119 None -12 24 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 1932 119 None -12 24 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 1932 119 None -12 24 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 1932 119 None -12 24 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 1932 119 None -12 24 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 1932 119 None -12 24 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 66828 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 66828 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 176478 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 176478 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 176478 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 1932 119 None -3 24 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 1932 119 None -3 24 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 1932 119 None -3 24 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 1932 119 None -3 24 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 1932 119 None -3 24 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 1932 119 None -3 24 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 2150 84 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 2150 84 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 2150 84 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 2150 84 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 1932 119 None -3 24 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 1932 119 None -3 24 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 1932 119 None -3 24 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 1932 119 None -3 24 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 1932 119 None -3 24 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 1932 119 None -3 24 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 2150 84 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 2150 84 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 2150 84 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 2150 84 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 1932 119 None -3 24 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 1932 119 None -3 24 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 1932 119 None -3 24 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 1932 119 None -3 24 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 1932 119 None -3 24 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 1932 119 None -3 24 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 2150 84 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 2150 84 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 2150 84 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 2150 84 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 2150 84 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 2150 84 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 2150 84 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 2150 84 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 103786 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 103786 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 1932 119 None -3 24 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 1932 119 None -3 24 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 1932 119 None -3 24 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 1932 119 None -3 24 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 1932 119 None -3 24 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 1932 119 None -3 24 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 2150 84 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 2150 84 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 2150 84 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 2150 84 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 1932 119 None -3 24 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 1932 119 None -3 24 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 1932 119 None -3 24 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 1932 119 None -3 24 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 1932 119 None -3 24 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 1932 119 None -3 24 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 2150 84 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 2150 84 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 2150 84 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 2150 84 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 1932 119 None -3 24 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 1932 119 None -3 24 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 1932 119 None -3 24 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 1932 119 None -3 24 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 1932 119 None -3 24 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 1932 119 None -3 24 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 2150 84 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 2150 84 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 2150 84 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 2150 84 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 169016 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 169016 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 74420 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 74420 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 74998 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 74998 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 76577 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 76577 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 3804 49 None -33 26 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 3804 49 None -33 26 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 3804 49 None -33 26 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 161795 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 161795 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 187287 45 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 187287 45 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 187414 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 187414 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 75684 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 75684 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 75685 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 75685 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 3804 49 None -33 26 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 3804 49 None -33 26 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 3804 49 None -33 26 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 3804 49 None -33 26 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 3804 49 None -33 26 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 3804 49 None -33 26 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 3804 49 None -33 26 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 3804 49 None -33 26 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 3804 49 None -33 26 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 96342 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 96342 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 195194 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 195194 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 195194 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 195250 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 195250 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 3804 49 None -33 26 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 3804 49 None -33 26 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 3804 49 None -33 26 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 2017 21 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 2017 21 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 2017 21 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 89664 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 89664 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 76006 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 76006 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 61885 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 61885 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 96160 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 96160 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 65128 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 65128 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 75661 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 75661 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 186759 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 186759 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 136573 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 136573 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 5358 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 5358 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 192803 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 192803 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 192803 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 75635 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 75635 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 186408 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 186408 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 5961 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 5961 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 5961 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 61554 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 61554 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 112183 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 112183 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 136734 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 136734 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 79996 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 79996 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 139529 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 139529 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 5358 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 5358 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 185575 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 185575 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 69729 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 69729 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 84264 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 84264 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 84264 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 84264 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 68145 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 68145 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 3804 49 None -21 26 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 3804 49 None -21 26 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 3804 49 None -21 26 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 199907 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 199907 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 58888 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 58888 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 157365 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 157365 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 69727 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 69727 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 67880 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 67880 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 137492 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 137492 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 91867 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 91867 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 184590 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 184590 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 86492 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 86492 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 61520 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 61520 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 2150 84 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 2150 84 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 2150 84 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 2150 84 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 117124 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 117124 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 176667 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 176667 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 176667 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 176667 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 176667 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 176667 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 6588 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 6588 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 186759 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 186759 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 205244 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 205244 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 29077 13 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 29077 13 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 136638 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 136638 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 192762 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 192762 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 192762 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 192785 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 192785 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 192785 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 100237 32 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 100237 32 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 5894 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 5894 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 5894 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 19434 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 19434 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 19434 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 19434 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 117115 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 117115 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 14690 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 14690 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 19434 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 19434 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 5599 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 5599 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 89719 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 89719 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 173409 9 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 173409 9 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 173409 9 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 173409 9 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 199454 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 199454 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 189062 14 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 189062 14 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 80260 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 80260 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 68108 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 68108 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 68125 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 68125 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 188180 9 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 188180 9 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 188180 9 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 56482 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 56482 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 56483 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 56483 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 1932 119 None -3 24 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 1932 119 None -3 24 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 1932 119 None -3 24 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 1932 119 None -3 24 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 1932 119 None -3 24 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 1932 119 None -3 24 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 1932 119 None -3 24 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 1932 119 None -3 24 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 1932 119 None -3 24 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 1932 119 None -3 24 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 1932 119 None -3 24 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 1932 119 None -3 24 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 56478 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 56478 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 102911 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 102911 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 176495 4 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 176495 4 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 176495 4 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 89674 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 89674 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 187287 45 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 187287 45 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 58900 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 58900 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 106052 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 106052 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 69914 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 69914 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 89725 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 89725 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 186784 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 186784 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 189062 14 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 189062 14 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 202029 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 202029 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 18910 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 18910 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 124021 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 124021 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 63163 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 63163 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 63163 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 166887 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 166887 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
CHEMBL4748908 214035 1 None -8 12 Human 6.2 pKi = 6.2 Binding
GPCRScan assay: inhibition of H4GPCRScan assay: inhibition of H4
ChEMBL None None None CN1CCN(c2ccnc(NCCc3ccccc3)n2)CC1 10.6019/CHEMBL4800732
156013005 177499 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 177499 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 192779 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 192779 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 192779 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 63163 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 63163 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 63163 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 189062 14 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 189062 14 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 199798 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 199798 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
CHEMBL4748908 214035 1 None -8 12 Human 6.2 pKi = 6.2 Binding
GPCRScan assay: inhibition of H4GPCRScan assay: inhibition of H4
ChEMBL None None None CN1CCN(c2ccnc(NCCc3ccccc3)n2)CC1 10.6019/CHEMBL4800732
46228083 199741 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 199741 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 6585 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 6585 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 137494 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 137494 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 175329 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 175329 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 86462 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 86462 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 69869 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 69869 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 68102 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 68102 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 193006 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 193006 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 193006 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 193020 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 193020 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 193020 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 96121 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 96121 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 86972 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 86972 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 159126 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 159126 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 68051 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 68051 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 71628 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 71628 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 71628 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 159126 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 159126 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 186939 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 186939 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 186939 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 186939 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 192895 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 192895 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 192895 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 169679 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 169679 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 169679 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 169679 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 169679 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 169679 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 185730 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 185730 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 68146 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 68146 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 61532 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 61532 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 7312 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 7312 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 110139 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 110139 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 953 41 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 953 41 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 953 41 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 58892 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 58892 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 184425 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 184425 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 193014 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 193014 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 193014 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 193035 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 193035 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 193035 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 137460 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 137460 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 95484 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 95484 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 5930 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 5930 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 3804 49 None -33 26 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 3804 49 None -33 26 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 3804 49 None -33 26 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 189062 14 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 189062 14 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 191386 10 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 191386 10 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 1932 119 None -15 24 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 1932 119 None -15 24 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 1932 119 None -15 24 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 1932 119 None -15 24 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 1932 119 None -15 24 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 1932 119 None -15 24 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 2132 34 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 2132 34 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 2132 34 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 3804 49 None -21 26 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 3804 49 None -21 26 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 3804 49 None -21 26 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 175101 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 175101 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 89649 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 89649 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 89655 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 89655 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 89666 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 89666 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 89668 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 89668 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 76017 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 76017 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 75644 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 75644 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 75649 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 75649 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 75663 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 75663 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 75693 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 75693 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 58908 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 58908 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 186784 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 186784 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 78680 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 78680 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 19379 56 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 19379 56 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 112186 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 112186 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 182947 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 182947 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 5301 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 5301 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 17987 34 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 17987 34 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 89654 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 89654 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 74954 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 74954 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 76519 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 76519 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 138503 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 138503 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 65124 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 65124 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 75641 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 75641 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 75658 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 75658 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 126645 6 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 126645 6 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 7394 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 7394 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 505 81 None -117 42 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
249 505 81 None -117 42 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 505 81 None -117 42 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 505 81 None -117 42 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 505 81 None -117 42 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 12771 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 12771 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 12771 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 185274 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 185274 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 18940 6 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 18940 6 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 19442 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 19442 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 1932 119 None -3 24 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 1932 119 None -3 24 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 1932 119 None -3 24 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 1932 119 None -3 24 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 1932 119 None -3 24 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 1932 119 None -3 24 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 18940 6 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 18940 6 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 19442 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 19442 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 2150 84 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 2150 84 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 2150 84 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 2150 84 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 61391 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 61391 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 2150 84 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 2150 84 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 2150 84 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 2150 84 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 115917 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 115917 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 117134 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 117134 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 117142 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 117142 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 2150 84 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 2150 84 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 2150 84 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 2150 84 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 110149 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 110149 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 68135 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 68135 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 18940 6 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 18940 6 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 19442 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 19442 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 199453 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 199453 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 187643 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 187643 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 58889 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 58889 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 176508 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 176508 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 176508 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 193048 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 193048 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 193048 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 6515 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 6515 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 200150 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 200150 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 176056 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 176056 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 184943 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 184943 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 185580 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 185580 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 186429 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 186429 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 7394 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 7394 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 86489 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 86489 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 68217 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 68217 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 68217 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 68217 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 117138 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 117138 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 167111 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 167111 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 68210 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 68210 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 61556 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 61556 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 68210 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 68210 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 69908 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 69908 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 112191 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 112191 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 68176 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 68176 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 6584 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 6584 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 16744 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 16744 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 10383 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 10383 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 89726 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 89726 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 189745 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 319 3 1 5 3.1 CN1CCN(c2nc(Nc3ccccc3)c3ccccc3n2)CC1 10.1021/jm800876b
CHEMBL515870 189745 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 319 3 1 5 3.1 CN1CCN(c2nc(Nc3ccccc3)c3ccccc3n2)CC1 10.1021/jm800876b
25178130 189745 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 319 3 1 5 3.1 CN1CCN(c2nc(Nc3ccccc3)c3ccccc3n2)CC1 10.1021/jm901379s
CHEMBL515870 189745 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 319 3 1 5 3.1 CN1CCN(c2nc(Nc3ccccc3)c3ccccc3n2)CC1 10.1021/jm901379s
164622153 185568 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 185568 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 61544 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 61544 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 123914 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 123914 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 117132 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 117132 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 68328 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 68328 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 140247 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 140247 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 186321 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 186321 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 86468 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 86468 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 68178 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 68178 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 68172 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 68172 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 68181 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 68181 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 7291 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 7291 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 71601 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 71601 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 71601 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 71603 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 71603 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 71603 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 173446 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 173446 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 58895 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 58895 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 174238 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 174238 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 16421 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 16421 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 189100 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 189100 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 5301 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 5301 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 192801 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 192801 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 192801 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 67879 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 67879 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 10382 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 10382 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 86463 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 86463 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 1932 119 None -3 24 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 1932 119 None -3 24 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 1932 119 None -3 24 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 1932 119 None -3 24 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 1932 119 None -3 24 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 1932 119 None -3 24 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 61540 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 61540 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 68183 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 68183 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 83460 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 83460 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 68183 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 68183 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 68056 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 68056 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 89726 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 89726 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 187354 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 187354 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 89724 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 89724 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 199430 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 199430 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 110150 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 110150 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 68183 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 68183 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 68212 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 68212 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 69733 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 69733 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 1424 28 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 1424 28 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 1424 28 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 1424 28 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 72938 7 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 72938 7 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 123838 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 123838 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 80313 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 80313 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 123916 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 123916 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 68221 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 68221 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 69721 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 69721 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 204049 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 204049 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 204049 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 58884 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 58884 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 137488 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 137488 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 115911 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 115911 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 84230 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 84230 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 68329 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 68329 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 178309 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 178309 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 178309 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 110312 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 110312 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 68318 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 68318 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 69726 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 69726 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 137266 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 137266 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 186785 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 186785 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 189100 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 189100 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 186785 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 186785 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 186156 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 186156 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 117113 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 117113 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 117110 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 117110 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 7243 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 7243 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 69907 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 69907 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 156118 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 156118 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 137295 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 137295 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 140200 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 140200 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 187254 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 187254 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 86485 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 86485 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 140238 3 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 140238 3 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 2182 50 None -21379 21 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 2182 50 None -21379 21 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 2182 50 None -21379 21 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 2182 50 None -21379 21 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 2182 50 None -21379 21 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 1389 114 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 1389 114 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 1389 114 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 1389 114 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 1389 114 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 1909 20 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 1909 20 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 1909 20 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 1909 20 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 1909 20 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 1909 20 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 2150 84 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 2150 84 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 2150 84 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 2150 84 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 1932 119 None -12 24 Rat 6.9 pKd None 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 11561071
1247 1932 119 None -12 24 Rat 6.9 pKd None 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 11561071
1375 1932 119 None -12 24 Rat 6.9 pKd None 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 11561071
774 1932 119 None -12 24 Rat 6.9 pKd None 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 11561071
CHEMBL90 1932 119 None -12 24 Rat 6.9 pKd None 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 11561071
DB05381 1932 119 None -12 24 Rat 6.9 pKd None 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 11561071
1236 2067 25 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 2067 25 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 2067 25 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 2067 25 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 1932 119 None -15 24 Mouse 7.4 pKd None 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 11561071
1247 1932 119 None -15 24 Mouse 7.4 pKd None 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 11561071
1375 1932 119 None -15 24 Mouse 7.4 pKd None 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 11561071
774 1932 119 None -15 24 Mouse 7.4 pKd None 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 11561071
CHEMBL90 1932 119 None -15 24 Mouse 7.4 pKd None 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 11561071
DB05381 1932 119 None -15 24 Mouse 7.4 pKd None 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 11561071
1241 2037 52 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 2037 52 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 2037 52 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 2037 52 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 1932 119 None -3 24 Human 7.9 pKd None 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 10973974
1204 1932 119 None -3 24 Human 7.9 pKd None 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 11179434
1204 1932 119 None -3 24 Human 7.9 pKd None 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 11179435
1204 1932 119 None -3 24 Human 7.9 pKd None 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 11181941
1204 1932 119 None -3 24 Human 7.9 pKd None 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 11561071
1204 1932 119 None -3 24 Human 7.9 pKd None 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 16432504
1247 1932 119 None -3 24 Human 7.9 pKd None 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 10973974
1247 1932 119 None -3 24 Human 7.9 pKd None 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 11179434
1247 1932 119 None -3 24 Human 7.9 pKd None 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 11179435
1247 1932 119 None -3 24 Human 7.9 pKd None 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 11181941
1247 1932 119 None -3 24 Human 7.9 pKd None 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 11561071
1247 1932 119 None -3 24 Human 7.9 pKd None 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 16432504
1375 1932 119 None -3 24 Human 7.9 pKd None 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 10973974
1375 1932 119 None -3 24 Human 7.9 pKd None 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 11179434
1375 1932 119 None -3 24 Human 7.9 pKd None 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 11179435
1375 1932 119 None -3 24 Human 7.9 pKd None 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 11181941
1375 1932 119 None -3 24 Human 7.9 pKd None 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 11561071
1375 1932 119 None -3 24 Human 7.9 pKd None 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 16432504
774 1932 119 None -3 24 Human 7.9 pKd None 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 10973974
774 1932 119 None -3 24 Human 7.9 pKd None 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 11179434
774 1932 119 None -3 24 Human 7.9 pKd None 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 11179435
774 1932 119 None -3 24 Human 7.9 pKd None 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 11181941
774 1932 119 None -3 24 Human 7.9 pKd None 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 11561071
774 1932 119 None -3 24 Human 7.9 pKd None 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 16432504
CHEMBL90 1932 119 None -3 24 Human 7.9 pKd None 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 10973974
CHEMBL90 1932 119 None -3 24 Human 7.9 pKd None 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 11179434
CHEMBL90 1932 119 None -3 24 Human 7.9 pKd None 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 11179435
CHEMBL90 1932 119 None -3 24 Human 7.9 pKd None 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 11181941
CHEMBL90 1932 119 None -3 24 Human 7.9 pKd None 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 11561071
CHEMBL90 1932 119 None -3 24 Human 7.9 pKd None 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 16432504
DB05381 1932 119 None -3 24 Human 7.9 pKd None 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 10973974
DB05381 1932 119 None -3 24 Human 7.9 pKd None 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 11179434
DB05381 1932 119 None -3 24 Human 7.9 pKd None 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 11179435
DB05381 1932 119 None -3 24 Human 7.9 pKd None 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 11181941
DB05381 1932 119 None -3 24 Human 7.9 pKd None 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 11561071
DB05381 1932 119 None -3 24 Human 7.9 pKd None 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 16432504
None 216141 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 1932 119 3H-Histamine 1 24 Guinea pig 9.9 pKi = 9.9 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
1247 1932 119 3H-Histamine 1 24 Guinea pig 9.9 pKi = 9.9 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
1375 1932 119 3H-Histamine 1 24 Guinea pig 9.9 pKi = 9.9 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
774 1932 119 3H-Histamine 1 24 Guinea pig 9.9 pKi = 9.9 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
CHEMBL90 1932 119 3H-Histamine 1 24 Guinea pig 9.9 pKi = 9.9 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
DB05381 1932 119 3H-Histamine 1 24 Guinea pig 9.9 pKi = 9.9 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
None 216141 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
179 400 115 3H-Histamine -4365 49 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 400 115 3H-Histamine -4365 49 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
963 400 115 3H-Histamine -4365 49 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 400 115 3H-Histamine -4365 49 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 400 115 3H-Histamine -4365 49 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
242 470 124 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
34 470 124 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 470 124 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 470 124 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 470 124 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 937 116 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 937 116 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 937 116 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 937 116 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
645 937 116 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
645 937 116 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 937 116 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 937 116 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 937 116 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 937 116 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 1301 62 3H-Histamine -301 50 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
2913 1301 62 3H-Histamine -301 50 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
765 1301 62 3H-Histamine -301 50 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
CHEMBL516 1301 62 3H-Histamine -301 50 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
DB00434 1301 62 3H-Histamine -301 50 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
1248 1424 28 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 1424 28 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 1424 28 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 1424 28 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 1432 83 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 1432 83 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 1432 83 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 1432 83 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 1432 83 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 1432 83 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 1662 50 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 1662 50 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 1662 50 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 1662 50 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 1662 50 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 1911 93 3H-Histamine -6918 83 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 1911 93 3H-Histamine -6918 83 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 1911 93 3H-Histamine -6918 83 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 1911 93 3H-Histamine -6918 83 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 1911 93 3H-Histamine -6918 83 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 2914 112 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 2914 112 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 2914 112 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 2914 112 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 3159 96 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 3159 96 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 3159 96 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 3159 96 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 3159 96 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 3256 77 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 3256 77 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 3256 77 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 3256 77 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 3256 77 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 3291 68 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 3291 68 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 3291 68 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 3291 68 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 3331 118 3H-Histamine -26915 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 3331 118 3H-Histamine -26915 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 3331 118 3H-Histamine -26915 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 3331 118 3H-Histamine -26915 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 3331 118 3H-Histamine -26915 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 3691 61 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 3691 61 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 3691 61 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 3853 55 3H-Histamine -912 44 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 3853 55 3H-Histamine -912 44 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 3853 55 3H-Histamine -912 44 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 3853 55 3H-Histamine -912 44 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 3853 55 3H-Histamine -912 44 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 4006 60 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 4006 60 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 4006 60 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 4006 60 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 4143 73 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 4143 73 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 4143 73 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 4143 73 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 4143 73 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 27112 30 3H-Histamine -38 42 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 27112 30 3H-Histamine -38 42 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 46800 99 3H-Histamine -1 29 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 46800 99 3H-Histamine -1 29 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 46800 99 3H-Histamine -1 29 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 70300 19 3H-Histamine -776 33 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 70300 19 3H-Histamine -776 33 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 70300 19 3H-Histamine -776 33 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 91835 10 3H-8-OH-DPAT -66069 45 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 91835 10 3H-8-OH-DPAT -66069 45 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 107531 20 3H-Histamine -58884 53 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
9903970 107531 20 3H-Histamine -58884 53 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
CHEMBL3187365 107531 20 3H-Histamine -58884 53 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
CHEMBL3544974 107531 20 3H-Histamine -58884 53 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
446220 133521 14 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 133521 14 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 196535 92 3H-Histamine -1 29 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 196535 92 3H-Histamine -1 29 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 200551 115 3H-Histamine -1 29 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 200551 115 3H-Histamine -1 29 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 200551 115 3H-Histamine -1 29 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 202274 22 3H-Histamine -239 43 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 151 2 2 2 1.1 CC(N)C(O)c1ccccc1 None
4786 202274 22 3H-Histamine -239 43 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 151 2 2 2 1.1 CC(N)C(O)c1ccccc1 None
CHEMBL61006 202274 22 3H-Histamine -239 43 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 151 2 2 2 1.1 CC(N)C(O)c1ccccc1 None
4054 205501 72 3H-Histamine -1 36 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 179 0 1 1 2.7 CC12CC3CC(C)(C1)CC(N)(C3)C2 None
CHEMBL1699 205501 72 3H-Histamine -1 36 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 179 0 1 1 2.7 CC12CC3CC(C)(C1)CC(N)(C3)C2 None
CHEMBL807 205501 72 3H-Histamine -1 36 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 179 0 1 1 2.7 CC12CC3CC(C)(C1)CC(N)(C3)C2 None
11954259 215979 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 215993 0 3H-Histamine -1 28 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 216019 0 3H-Histamine -41686 37 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 216141 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 216179 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 216179 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 216311 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 216312 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 216313 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 216314 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 216315 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 216316 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 216317 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 216325 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 216326 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 216389 0 3H-Histamine -1 29 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 216390 0 3H-Histamine -1 28 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 216393 0 3H-Histamine -1412 26 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 216394 0 3H-Histamine -1 29 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 216395 0 3H-Histamine -7 28 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 216489 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 2035 69 3H-Histamine -363 39 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 2035 69 3H-Histamine -363 39 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 2035 69 3H-Histamine -363 39 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 1932 119 3H-Histamine 1 24 Guinea pig 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
1247 1932 119 3H-Histamine 1 24 Guinea pig 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
1375 1932 119 3H-Histamine 1 24 Guinea pig 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
774 1932 119 3H-Histamine 1 24 Guinea pig 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
CHEMBL90 1932 119 3H-Histamine 1 24 Guinea pig 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
DB05381 1932 119 3H-Histamine 1 24 Guinea pig 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
1225 1471 26 3H-PYRILAMINE -371 22 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 1471 26 3H-PYRILAMINE -371 22 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 1471 26 3H-PYRILAMINE -371 22 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 1471 26 3H-PYRILAMINE -371 22 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 1471 26 3H-PYRILAMINE -371 22 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 2019 20 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 2019 20 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 2019 20 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 953 41 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 953 41 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 953 41 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 2014 39 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 2014 39 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 2014 39 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 2058 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 2058 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 2058 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 216254 0 3H-Histamine -13 19 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 216254 0 3H-N-alpha-methylhistamine -13 19 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 953 41 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 953 41 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 953 41 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 3804 49 3H-Histamine -33 26 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 3804 49 3H-N-alpha-methylhistamine -33 26 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 3804 49 3H-Histamine -33 26 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 3804 49 3H-N-alpha-methylhistamine -33 26 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 3804 49 3H-Histamine -33 26 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 3804 49 3H-N-alpha-methylhistamine -33 26 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 940 74 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
654 940 74 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 940 74 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 940 74 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 940 74 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 216156 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 953 41 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 953 41 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 953 41 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 1932 119 3H-Histamine -3 24 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
1204 1932 119 3H-N-alpha-methylhistamine -3 24 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
1247 1932 119 3H-Histamine -3 24 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
1247 1932 119 3H-N-alpha-methylhistamine -3 24 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
1375 1932 119 3H-Histamine -3 24 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
1375 1932 119 3H-N-alpha-methylhistamine -3 24 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
774 1932 119 3H-Histamine -3 24 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
774 1932 119 3H-N-alpha-methylhistamine -3 24 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
CHEMBL90 1932 119 3H-Histamine -3 24 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
CHEMBL90 1932 119 3H-N-alpha-methylhistamine -3 24 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
DB05381 1932 119 3H-Histamine -3 24 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
DB05381 1932 119 3H-N-alpha-methylhistamine -3 24 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
2286 3183 51 3H-PYRILAMINE -10 30 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C None
4927 3183 51 3H-PYRILAMINE -10 30 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C None
7282 3183 51 3H-PYRILAMINE -10 30 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C None
CHEMBL643 3183 51 3H-PYRILAMINE -10 30 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C None
DB01069 3183 51 3H-PYRILAMINE -10 30 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C None
1204 1932 119 3H-Histamine -3 24 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
1247 1932 119 3H-Histamine -3 24 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
1375 1932 119 3H-Histamine -3 24 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
774 1932 119 3H-Histamine -3 24 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
CHEMBL90 1932 119 3H-Histamine -3 24 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
DB05381 1932 119 3H-Histamine -3 24 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
3032915 15495 24 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 15495 24 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 1932 119 3H-JNJ 7777120 -3 24 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
1247 1932 119 3H-JNJ 7777120 -3 24 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
1375 1932 119 3H-JNJ 7777120 -3 24 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
774 1932 119 3H-JNJ 7777120 -3 24 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
CHEMBL90 1932 119 3H-JNJ 7777120 -3 24 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
DB05381 1932 119 3H-JNJ 7777120 -3 24 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
1251 2014 39 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 2014 39 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 2014 39 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 2014 39 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 2014 39 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 2014 39 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 2014 39 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 2014 39 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 2014 39 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 216254 0 125I-iodophenpropit -13 19 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 216254 0 3H-JNJ 7777120 -13 19 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 4153 61 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 4153 61 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 4153 61 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 4153 61 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 4153 61 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 958 93 3H-Histamine -57 89 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 958 93 3H-Histamine -57 89 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 958 93 3H-Histamine -57 89 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 958 93 3H-Histamine -57 89 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 958 93 3H-Histamine -57 89 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
1204 1932 119 3H-Histamine -3 24 Human 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
1247 1932 119 3H-Histamine -3 24 Human 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
1375 1932 119 3H-Histamine -3 24 Human 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
774 1932 119 3H-Histamine -3 24 Human 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
CHEMBL90 1932 119 3H-Histamine -3 24 Human 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
DB05381 1932 119 3H-Histamine -3 24 Human 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
11957573 2010 34 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 2010 34 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 2010 34 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 2010 34 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 1301 62 3H-PYRILAMINE -301 50 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
2913 1301 62 3H-PYRILAMINE -301 50 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
765 1301 62 3H-PYRILAMINE -301 50 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
CHEMBL516 1301 62 3H-PYRILAMINE -301 50 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
DB00434 1301 62 3H-PYRILAMINE -301 50 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
1241 2037 52 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 2037 52 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 2037 52 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 2037 52 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 216141 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 3805 58 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 3805 58 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 3805 58 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 3805 58 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 3805 58 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 1932 119 125I-iodophenpropit -3 24 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
1247 1932 119 125I-iodophenpropit -3 24 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
1375 1932 119 125I-iodophenpropit -3 24 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
774 1932 119 125I-iodophenpropit -3 24 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
CHEMBL90 1932 119 125I-iodophenpropit -3 24 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
DB05381 1932 119 125I-iodophenpropit -3 24 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
1226 2019 20 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 2019 20 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 2019 20 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 216156 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 3804 49 3H-Histamine -33 26 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 3804 49 3H-Histamine -33 26 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 3804 49 3H-Histamine -33 26 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 918 51 3H-PYRILAMINE -295 21 Human 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C None
1213 918 51 3H-PYRILAMINE -295 21 Human 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C None
2725 918 51 3H-PYRILAMINE -295 21 Human 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C None
33036 918 51 3H-PYRILAMINE -295 21 Human 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C None
4411 918 51 3H-PYRILAMINE -295 21 Human 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C None
616 918 51 3H-PYRILAMINE -295 21 Human 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C None
6976 918 51 3H-PYRILAMINE -295 21 Human 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C None
716121 918 51 3H-PYRILAMINE -295 21 Human 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C None
CHEMBL1201353 918 51 3H-PYRILAMINE -295 21 Human 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C None
CHEMBL1554789 918 51 3H-PYRILAMINE -295 21 Human 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C None
CHEMBL505 918 51 3H-PYRILAMINE -295 21 Human 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C None
DB01114 918 51 3H-PYRILAMINE -295 21 Human 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C None
DB13679 918 51 3H-PYRILAMINE -295 21 Human 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C None
135398737 958 93 125I-iodophenpropit -57 89 Human 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 958 93 125I-iodophenpropit -57 89 Human 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 958 93 125I-iodophenpropit -57 89 Human 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 958 93 125I-iodophenpropit -57 89 Human 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 958 93 125I-iodophenpropit -57 89 Human 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
1239 2033 24 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 2033 24 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 2033 24 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 2033 24 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
180 401 56 3H-PYRILAMINE -32 40 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
200 401 56 3H-PYRILAMINE -32 40 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
2160 401 56 3H-PYRILAMINE -32 40 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
CHEMBL629 401 56 3H-PYRILAMINE -32 40 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
DB00321 401 56 3H-PYRILAMINE -32 40 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
1204 1932 119 3H-PYRILAMINE -3 24 Human 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
1247 1932 119 3H-PYRILAMINE -3 24 Human 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
1375 1932 119 3H-PYRILAMINE -3 24 Human 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
774 1932 119 3H-PYRILAMINE -3 24 Human 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
CHEMBL90 1932 119 3H-PYRILAMINE -3 24 Human 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
DB05381 1932 119 3H-PYRILAMINE -3 24 Human 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
None 216141 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 1424 28 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 1424 28 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 1424 28 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 1424 28 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 2010 34 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 2010 34 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 2010 34 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 2010 34 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 19455 51 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 19455 51 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 1932 119 3H-Histamine -3 24 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
1247 1932 119 3H-Histamine -3 24 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
1375 1932 119 3H-Histamine -3 24 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
774 1932 119 3H-Histamine -3 24 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
CHEMBL90 1932 119 3H-Histamine -3 24 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
DB05381 1932 119 3H-Histamine -3 24 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
1267 3804 49 125I-iodophenpropit -33 26 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 3804 49 125I-iodophenpropit -33 26 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 3804 49 125I-iodophenpropit -33 26 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 15495 24 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 15495 24 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 15495 24 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 15495 24 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 958 93 3H-JNJ 7777120 -57 89 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 958 93 3H-JNJ 7777120 -57 89 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 958 93 3H-JNJ 7777120 -57 89 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 958 93 3H-JNJ 7777120 -57 89 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 958 93 3H-JNJ 7777120 -57 89 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
45073439 216157 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 1432 83 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 1432 83 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 1432 83 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 1432 83 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 1432 83 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 1432 83 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 32000 67 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 32000 67 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 32000 67 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 953 41 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 953 41 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 953 41 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 13441 42 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 13441 42 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 13441 42 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 3804 49 3H-Histamine -33 26 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 3804 49 3H-Histamine -33 26 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 3804 49 3H-Histamine -33 26 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 3804 49 3H-Histamine -33 26 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 3804 49 3H-Histamine -33 26 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 3804 49 3H-Histamine -33 26 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 55585 119 None -891 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 55585 119 None -891 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 505 81 None -117 42 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
249 505 81 None -117 42 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 505 81 None -117 42 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 505 81 None -117 42 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 505 81 None -117 42 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 199668 72 None - 1 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 456 6 3 6 2.7 CC(C)Nc1cccnc1N1CCN(C(=O)c2cc3cc(NS(C)(=O)=O)ccc3[nH]2)CC1 None
CHEMBL593 199668 72 None - 1 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 456 6 3 6 2.7 CC(C)Nc1cccnc1N1CCN(C(=O)c2cc3cc(NS(C)(=O)=O)ccc3[nH]2)CC1 None
1613 2348 53 None -134 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 2348 53 None -134 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 2348 53 None -134 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 2348 53 None -134 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 2348 53 None -134 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 118146 34 None -20 12 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 291 0 0 3 2.9 CN1CCN(C2=Nc3ccccc3Cc3ccccc32)CC1 None
CHEMBL340801 118146 34 None -20 12 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 291 0 0 3 2.9 CN1CCN(C2=Nc3ccccc3Cc3ccccc32)CC1 None
4761 13441 42 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 13441 42 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 13441 42 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 958 93 None -54 89 Mouse 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 958 93 None -54 89 Mouse 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 958 93 None -54 89 Mouse 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 958 93 None -54 89 Mouse 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 958 93 None -54 89 Mouse 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
100 3805 58 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 3805 58 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 3805 58 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 3805 58 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 3805 58 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 3125 71 None -562 30 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 3125 71 None -562 30 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 3125 71 None -562 30 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 3125 71 None -562 30 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 3125 71 None -562 30 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 958 93 None -44 89 Rat 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 958 93 None -44 89 Rat 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 958 93 None -44 89 Rat 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 958 93 None -44 89 Rat 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 958 93 None -44 89 Rat 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
103 4153 61 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 4153 61 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 4153 61 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 4153 61 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 4153 61 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 919 68 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
621 919 68 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
83 919 68 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 919 68 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 919 68 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 919 68 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
621 919 68 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
83 919 68 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 919 68 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 919 68 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 2348 53 3H-Histamine -134 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 2348 53 3H-Histamine -134 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 2348 53 3H-Histamine -134 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 2348 53 3H-Histamine -134 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 2348 53 3H-Histamine -134 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 958 93 3H-Histamine -57 89 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 958 93 3H-Histamine -57 89 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 958 93 3H-Histamine -57 89 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 958 93 3H-Histamine -57 89 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 958 93 3H-Histamine -57 89 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
11957573 2010 34 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 2010 34 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 2010 34 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 2010 34 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 32000 67 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 32000 67 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 32000 67 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 918 51 None -295 21 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C None
1213 918 51 None -295 21 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C None
2725 918 51 None -295 21 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C None
33036 918 51 None -295 21 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C None
4411 918 51 None -295 21 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C None
616 918 51 None -295 21 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C None
6976 918 51 None -295 21 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C None
716121 918 51 None -295 21 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C None
CHEMBL1201353 918 51 None -295 21 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C None
CHEMBL1554789 918 51 None -295 21 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C None
CHEMBL505 918 51 None -295 21 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C None
DB01114 918 51 None -295 21 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C None
DB13679 918 51 None -295 21 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C None
2286 3183 51 None -10 30 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C None
4927 3183 51 None -10 30 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C None
7282 3183 51 None -10 30 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C None
CHEMBL643 3183 51 None -10 30 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C None
DB01069 3183 51 None -10 30 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C None
2726 919 68 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
621 919 68 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
83 919 68 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 919 68 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 919 68 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 1932 119 None -15 24 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 1932 119 None -15 24 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 1932 119 None -15 24 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 1932 119 None -15 24 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 1932 119 None -15 24 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 1932 119 None -15 24 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 1932 119 None -12 24 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 1932 119 None -12 24 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 1932 119 None -12 24 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 1932 119 None -12 24 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 1932 119 None -12 24 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 1932 119 None -12 24 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 953 41 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 953 41 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 953 41 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 953 41 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 953 41 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 953 41 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 2532 43 3H-PYRILAMINE -389 58 Human 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
1796 2532 43 3H-PYRILAMINE -389 58 Human 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
4184 2532 43 3H-PYRILAMINE -389 58 Human 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
CHEMBL6437 2532 43 3H-PYRILAMINE -389 58 Human 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
DB06148 2532 43 3H-PYRILAMINE -389 58 Human 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
1267 3804 49 3H-JNJ 7777120 -33 26 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 3804 49 3H-JNJ-5207852 -33 26 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 3804 49 3H-JNJ 7777120 -33 26 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 3804 49 3H-JNJ-5207852 -33 26 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 3804 49 3H-JNJ 7777120 -33 26 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 3804 49 3H-JNJ-5207852 -33 26 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 1932 119 None -3 24 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 1932 119 None -3 24 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 1932 119 None -3 24 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 1932 119 None -3 24 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 1932 119 None -3 24 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 1932 119 None -3 24 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 1932 119 3H-Histamine -3 24 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
1247 1932 119 3H-Histamine -3 24 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
1375 1932 119 3H-Histamine -3 24 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
774 1932 119 3H-Histamine -3 24 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
CHEMBL90 1932 119 3H-Histamine -3 24 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
DB05381 1932 119 3H-Histamine -3 24 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
180 401 56 None -32 40 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
200 401 56 None -32 40 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
2160 401 56 None -32 40 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
CHEMBL629 401 56 None -32 40 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
DB00321 401 56 None -32 40 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
277 1301 62 None -301 50 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
2913 1301 62 None -301 50 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
765 1301 62 None -301 50 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
CHEMBL516 1301 62 None -301 50 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
DB00434 1301 62 None -301 50 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
1204 1932 119 None 1 24 Guinea pig 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
1247 1932 119 None 1 24 Guinea pig 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
1375 1932 119 None 1 24 Guinea pig 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
774 1932 119 None 1 24 Guinea pig 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
CHEMBL90 1932 119 None 1 24 Guinea pig 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
DB05381 1932 119 None 1 24 Guinea pig 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
135398737 958 93 None -57 89 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 958 93 None -57 89 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 958 93 None -57 89 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 958 93 None -57 89 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 958 93 None -57 89 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
135398737 958 93 3H-Histamine -57 89 Human 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 958 93 3H-Histamine -57 89 Human 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 958 93 3H-Histamine -57 89 Human 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 958 93 3H-Histamine -57 89 Human 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 958 93 3H-Histamine -57 89 Human 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
135398737 958 93 3H-PYRILAMINE -57 89 Human 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 958 93 3H-PYRILAMINE -57 89 Human 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 958 93 3H-PYRILAMINE -57 89 Human 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 958 93 3H-PYRILAMINE -57 89 Human 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 958 93 3H-PYRILAMINE -57 89 Human 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
115237 55585 119 3H-Histamine -891 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 55585 119 3H-Histamine -891 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 2014 39 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 2014 39 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 2014 39 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 3846 26 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 3846 26 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 3846 26 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 3846 26 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 942 60 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 942 60 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 942 60 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 942 60 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 942 60 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 942 60 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 942 60 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 942 60 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 942 60 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 3804 49 None -33 26 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 3804 49 None -33 26 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 3804 49 None -33 26 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 3804 49 None -33 26 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 3804 49 None -33 26 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 3804 49 None -33 26 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 3804 49 None -33 26 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 3804 49 None -33 26 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 3804 49 None -33 26 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 3804 49 None -33 26 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 3804 49 None -33 26 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 3804 49 None -33 26 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 3804 49 None -33 26 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 3804 49 None -33 26 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 3804 49 None -33 26 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 3804 49 None -33 26 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 3804 49 None -33 26 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 3804 49 None -33 26 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 2132 34 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 2132 34 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 2132 34 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 953 41 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 953 41 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 953 41 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 4064 16 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 4064 16 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 4064 16 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 41 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 41 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 41 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 41 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 41 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 41 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 953 41 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 953 41 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 953 41 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 953 41 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 953 41 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 953 41 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 953 41 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 953 41 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 953 41 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 953 41 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 953 41 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 953 41 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 953 41 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 953 41 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 953 41 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 953 41 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 953 41 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 953 41 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 2142 31 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 2142 31 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 2142 31 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 2142 31 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 2142 31 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 2142 31 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 3682 10 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 3682 10 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 3682 10 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 2150 84 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 2150 84 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 2150 84 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 2150 84 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 2150 84 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 2150 84 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 2150 84 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 2150 84 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 2150 84 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 2150 84 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 2150 84 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 2150 84 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 2023 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 2023 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 295 12 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 295 12 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 295 12 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 295 12 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 3133 64 None -48977 7 Human 4.0 pKi > 4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 295 8 0 2 4.2 Clc1ccc(cc1)CCCOCCCN1CCCCC1 26084539
8924 3133 64 None -48977 7 Human 4.0 pKi > 4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 295 8 0 2 4.2 Clc1ccc(cc1)CCCOCCCN1CCCCC1 26084539
9948102 3133 64 None -48977 7 Human 4.0 pKi > 4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 295 8 0 2 4.2 Clc1ccc(cc1)CCCOCCCN1CCCCC1 26084539
CHEMBL462605 3133 64 None -48977 7 Human 4.0 pKi > 4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 295 8 0 2 4.2 Clc1ccc(cc1)CCCOCCCN1CCCCC1 26084539
DB11642 3133 64 None -48977 7 Human 4.0 pKi > 4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 295 8 0 2 4.2 Clc1ccc(cc1)CCCOCCCN1CCCCC1 26084539
441082 1163 48 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 1163 48 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 1163 48 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 2547 24 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 2547 24 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 2547 24 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 2547 24 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 940 74 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
654 940 74 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 940 74 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 940 74 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 940 74 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 2018 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 2018 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 2018 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 958 93 None -54 89 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
38 958 93 None -54 89 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
722 958 93 None -54 89 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 958 93 None -54 89 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 958 93 None -54 89 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 2082 13 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 2082 13 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 2082 13 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 1424 28 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 1424 28 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 1424 28 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 1424 28 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 1424 28 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 1424 28 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 1424 28 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 1424 28 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 1424 28 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 1424 28 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 1424 28 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 1424 28 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 1424 28 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 1424 28 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 1424 28 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 1424 28 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 958 93 None -44 89 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
38 958 93 None -44 89 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
722 958 93 None -44 89 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 958 93 None -44 89 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 958 93 None -44 89 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 2500 8 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 2500 8 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 2500 8 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 1946 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 1946 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 1946 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 2040 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 2040 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 2040 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 45 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 45 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 45 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 743 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 743 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 743 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 743 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 2067 25 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 2067 25 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 2067 25 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 2067 25 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 2037 52 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 2037 52 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 2037 52 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 2037 52 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 2067 25 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 2067 25 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 2067 25 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 2067 25 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 958 93 None -57 89 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 958 93 None -57 89 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 958 93 None -57 89 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 958 93 None -57 89 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
38 958 93 None -57 89 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
38 958 93 None -57 89 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
38 958 93 None -57 89 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
38 958 93 None -57 89 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
722 958 93 None -57 89 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
722 958 93 None -57 89 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
722 958 93 None -57 89 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
722 958 93 None -57 89 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 958 93 None -57 89 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 958 93 None -57 89 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 958 93 None -57 89 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 958 93 None -57 89 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 958 93 None -57 89 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 958 93 None -57 89 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 958 93 None -57 89 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 958 93 None -57 89 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 2037 52 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 2037 52 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 2037 52 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 2037 52 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 2067 25 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 2067 25 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 2067 25 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 2067 25 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 2067 25 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 2067 25 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 2067 25 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 2067 25 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 2067 25 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 2067 25 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 2067 25 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 2067 25 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 2067 25 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 2067 25 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 2067 25 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 2067 25 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 2036 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 2036 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 2036 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 2033 24 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 2033 24 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 2033 24 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 2033 24 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 2033 24 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 2033 24 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 2033 24 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 2033 24 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 743 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 743 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 743 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 743 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 743 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 743 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 743 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 743 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 743 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 743 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 1932 119 None -12 24 Rat 7.2 pKi None 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 11561071
1247 1932 119 None -12 24 Rat 7.2 pKi None 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 11561071
1375 1932 119 None -12 24 Rat 7.2 pKi None 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 11561071
774 1932 119 None -12 24 Rat 7.2 pKi None 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 11561071
CHEMBL90 1932 119 None -12 24 Rat 7.2 pKi None 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 11561071
DB05381 1932 119 None -12 24 Rat 7.2 pKi None 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 11561071
1204 1932 119 None -15 24 Mouse 7.4 pKi None 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 11561071
1247 1932 119 None -15 24 Mouse 7.4 pKi None 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 11561071
1375 1932 119 None -15 24 Mouse 7.4 pKi None 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 11561071
774 1932 119 None -15 24 Mouse 7.4 pKi None 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 11561071
CHEMBL90 1932 119 None -15 24 Mouse 7.4 pKi None 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 11561071
DB05381 1932 119 None -15 24 Mouse 7.4 pKi None 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 11561071
1241 2037 52 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 2037 52 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 2037 52 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 2037 52 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 2037 52 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 2037 52 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 2037 52 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 2037 52 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 2037 52 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 2037 52 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 2037 52 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 2037 52 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 3804 49 None -21 26 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 3804 49 None -14 26 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 3804 49 None -21 26 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 3804 49 None -14 26 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 3804 49 None -21 26 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 3804 49 None -14 26 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 2057 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 2057 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 2057 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 2019 20 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 2019 20 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 2019 20 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 2019 20 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 2019 20 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 2019 20 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 2014 39 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 2014 39 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 2014 39 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 2014 39 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 2014 39 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 2014 39 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 2014 39 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 2014 39 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 2014 39 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 1932 119 None -3 24 Human 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 11179434
1204 1932 119 None -3 24 Human 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 11179436
1204 1932 119 None -3 24 Human 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 11181941
1204 1932 119 None -3 24 Human 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 11561071
1204 1932 119 None -3 24 Human 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 15454206
1204 1932 119 None -3 24 Human 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 15947036
1204 1932 119 None -3 24 Human 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 16432504
1247 1932 119 None -3 24 Human 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 11179434
1247 1932 119 None -3 24 Human 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 11179436
1247 1932 119 None -3 24 Human 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 11181941
1247 1932 119 None -3 24 Human 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 11561071
1247 1932 119 None -3 24 Human 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 15454206
1247 1932 119 None -3 24 Human 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 15947036
1247 1932 119 None -3 24 Human 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 16432504
1375 1932 119 None -3 24 Human 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 11179434
1375 1932 119 None -3 24 Human 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 11179436
1375 1932 119 None -3 24 Human 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 11181941
1375 1932 119 None -3 24 Human 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 11561071
1375 1932 119 None -3 24 Human 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 15454206
1375 1932 119 None -3 24 Human 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 15947036
1375 1932 119 None -3 24 Human 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 16432504
774 1932 119 None -3 24 Human 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 11179434
774 1932 119 None -3 24 Human 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 11179436
774 1932 119 None -3 24 Human 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 11181941
774 1932 119 None -3 24 Human 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 11561071
774 1932 119 None -3 24 Human 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 15454206
774 1932 119 None -3 24 Human 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 15947036
774 1932 119 None -3 24 Human 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 16432504
CHEMBL90 1932 119 None -3 24 Human 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 11179434
CHEMBL90 1932 119 None -3 24 Human 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 11179436
CHEMBL90 1932 119 None -3 24 Human 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 11181941
CHEMBL90 1932 119 None -3 24 Human 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 11561071
CHEMBL90 1932 119 None -3 24 Human 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 15454206
CHEMBL90 1932 119 None -3 24 Human 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 15947036
CHEMBL90 1932 119 None -3 24 Human 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 16432504
DB05381 1932 119 None -3 24 Human 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 11179434
DB05381 1932 119 None -3 24 Human 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 11179436
DB05381 1932 119 None -3 24 Human 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 11181941
DB05381 1932 119 None -3 24 Human 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 11561071
DB05381 1932 119 None -3 24 Human 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 15454206
DB05381 1932 119 None -3 24 Human 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 15947036
DB05381 1932 119 None -3 24 Human 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 111 2 2 2 -0.1 NCCc1cnc[nH]1 16432504
11957573 2010 34 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 2010 34 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 2010 34 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 2010 34 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 2010 34 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 2010 34 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 2010 34 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 2010 34 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 2010 34 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 2010 34 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 2010 34 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 2010 34 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 2010 34 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 2010 34 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 2010 34 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 2010 34 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 2010 34 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 2010 34 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 2010 34 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 2010 34 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 2010 34 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 2010 34 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 2010 34 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 2010 34 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