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Compile Data Set for Download or QSAR

Found 94 hits of ic50 data for polymerid = 2289   
Target/Host
(Institution)
LigandTarget/Host
Links
Ligand
Links
Trg + Lig
Links
Ki
nM
ΔG°
kcal/mole
IC50
nM
Kd
nM
EC50/IC50
nM
koff
s-1
kon
M-1s-1
pHTemp
°C
Histamine receptor (H4)


(Homo sapiens (human))
BDBM50356884
PNG
(CHEMBL1915540)
Show SMILES CN[C@@H]1CCN(C1)c1cc(NCC2CC2)nc(N)n1
Show InChI InChI=1S/C13H22N6/c1-15-10-4-5-19(8-10)12-6-11(17-13(14)18-12)16-7-9-2-3-9/h6,9-10,15H,2-5,7-8H2,1H3,(H3,14,16,17,18)/t10-/m1/s1
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n/an/a 0.650n/an/an/an/an/an/a



Pfizer Inc.

Curated by ChEMBL


Assay Description
Antagonist activity at H4R in human eosinophils assessed as inhibition of histamine-induced shape change by GAFS assay


Bioorg Med Chem Lett 21: 6596-602 (2011)

More data for this
Ligand-Target Pair
Histamine receptor (H4)


(Homo sapiens (human))
BDBM50315348
PNG
((R)-8-chloro-4-(3-(methylamino)pyrrolidin-1-yl)ben...)
Show SMILES CN[C@@H]1CCN(C1)c1nc(N)nc2c3cc(Cl)ccc3oc12
Show InChI InChI=1S/C15H16ClN5O/c1-18-9-4-5-21(7-9)14-13-12(19-15(17)20-14)10-6-8(16)2-3-11(10)22-13/h2-3,6,9,18H,4-5,7H2,1H3,(H2,17,19,20)/t9-/m1/s1
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n/an/a 1n/an/an/an/an/an/a



Argenta Discovery Ltd.

Curated by ChEMBL


Assay Description
Displacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assay


Bioorg Med Chem Lett 20: 2516-9 (2010)

More data for this
Ligand-Target Pair
Histamine receptor (H4)


(Homo sapiens (human))
BDBM50356884
PNG
(CHEMBL1915540)
Show SMILES CN[C@@H]1CCN(C1)c1cc(NCC2CC2)nc(N)n1
Show InChI InChI=1S/C13H22N6/c1-15-10-4-5-19(8-10)12-6-11(17-13(14)18-12)16-7-9-2-3-9/h6,9-10,15H,2-5,7-8H2,1H3,(H3,14,16,17,18)/t10-/m1/s1
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n/an/a 1.30n/an/an/an/an/an/a



Pfizer Inc.

Curated by ChEMBL


Assay Description
Antagonist activity at H4R in human eosinophils assessed as inhibition of histamine-induced actin polymerisation


Bioorg Med Chem Lett 21: 6596-602 (2011)

More data for this
Ligand-Target Pair
Histamine receptor (H4)


(Homo sapiens (human))
BDBM50315348
PNG
((R)-8-chloro-4-(3-(methylamino)pyrrolidin-1-yl)ben...)
Show SMILES CN[C@@H]1CCN(C1)c1nc(N)nc2c3cc(Cl)ccc3oc12
Show InChI InChI=1S/C15H16ClN5O/c1-18-9-4-5-21(7-9)14-13-12(19-15(17)20-14)10-6-8(16)2-3-11(10)22-13/h2-3,6,9,18H,4-5,7H2,1H3,(H2,17,19,20)/t9-/m1/s1
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n/an/a 3n/an/an/an/an/an/a



Argenta Discovery Ltd.

Curated by ChEMBL


Assay Description
Inverse agonist activity at human histamine H4 receptor assessed as inhibition of [35S]GTPgammaS binding after 15 mins by scintillation proximity ass...


Bioorg Med Chem Lett 20: 2516-9 (2010)

More data for this
Ligand-Target Pair
Histamine receptor (H4)


(Homo sapiens (human))
BDBM50315349
PNG
((S)-8-chloro-4-(3-(methylamino)pyrrolidin-1-yl)ben...)
Show SMILES CN[C@H]1CCN(C1)c1nc(N)nc2c3cc(Cl)ccc3oc12
Show InChI InChI=1S/C15H16ClN5O/c1-18-9-4-5-21(7-9)14-13-12(19-15(17)20-14)10-6-8(16)2-3-11(10)22-13/h2-3,6,9,18H,4-5,7H2,1H3,(H2,17,19,20)/t9-/m0/s1
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n/an/a 4n/an/an/an/an/an/a



Argenta Discovery Ltd.

Curated by ChEMBL


Assay Description
Inverse agonist activity at human histamine H4 receptor assessed as inhibition of [35S]GTPgammaS binding after 15 mins by scintillation proximity ass...


Bioorg Med Chem Lett 20: 2516-9 (2010)

More data for this
Ligand-Target Pair
Histamine receptor (H4)


(Homo sapiens (human))
BDBM50356884
PNG
(CHEMBL1915540)
Show SMILES CN[C@@H]1CCN(C1)c1cc(NCC2CC2)nc(N)n1
Show InChI InChI=1S/C13H22N6/c1-15-10-4-5-19(8-10)12-6-11(17-13(14)18-12)16-7-9-2-3-9/h6,9-10,15H,2-5,7-8H2,1H3,(H3,14,16,17,18)/t10-/m1/s1
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n/an/a 4.90n/an/an/an/an/an/a



Pfizer Inc.

Curated by ChEMBL


Assay Description
Antagonist activity at H4R in human eosinophils assessed as inhibition of histamine-induced CD11b upregulation


Bioorg Med Chem Lett 21: 6596-602 (2011)

More data for this
Ligand-Target Pair
Histamine receptor (H4)


(Homo sapiens (human))
BDBM22566
PNG
(5-chloro-2-[(4-methylpiperazin-1-yl)carbonyl]-1H-i...)
Show SMILES CN1CCN(CC1)C(=O)c1cc2cc(Cl)ccc2[nH]1
Show InChI InChI=1S/C14H16ClN3O/c1-17-4-6-18(7-5-17)14(19)13-9-10-8-11(15)2-3-12(10)16-13/h2-3,8-9,16H,4-7H2,1H3
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n/an/a 5.30n/an/an/an/an/an/a



Pfizer Inc.

Curated by ChEMBL


Assay Description
Antagonist activity at H4R in human eosinophils assessed as inhibition of histamine-induced actin polymerisation


Bioorg Med Chem Lett 21: 6596-602 (2011)

More data for this
Ligand-Target Pair
Histamine receptor (H4)


(Homo sapiens (human))
BDBM50415489
PNG
(CHEMBL591969)
Show SMILES CN1CCN(CC1)c1nc(NCCS(N)(=O)=O)c2cc(Cl)ccc2n1
Show InChI InChI=1S/C15H21ClN6O2S/c1-21-5-7-22(8-6-21)15-19-13-3-2-11(16)10-12(13)14(20-15)18-4-9-25(17,23)24/h2-3,10H,4-9H2,1H3,(H2,17,23,24)(H,18,19,20)
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n/an/a 10n/an/an/an/an/an/a



Griffin Discoveries BV

Curated by ChEMBL


Assay Description
Inverse agonist activity at human histamine H4 receptor expressed in HEK293T cells by CRE-beta-galactosidase assay


J Med Chem 53: 2390-400 (2010)

More data for this
Ligand-Target Pair
Histamine receptor (H4)


(Homo sapiens (human))
BDBM50315349
PNG
((S)-8-chloro-4-(3-(methylamino)pyrrolidin-1-yl)ben...)
Show SMILES CN[C@H]1CCN(C1)c1nc(N)nc2c3cc(Cl)ccc3oc12
Show InChI InChI=1S/C15H16ClN5O/c1-18-9-4-5-21(7-9)14-13-12(19-15(17)20-14)10-6-8(16)2-3-11(10)22-13/h2-3,6,9,18H,4-5,7H2,1H3,(H2,17,19,20)/t9-/m0/s1
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n/an/a 13n/an/an/an/an/an/a



Argenta Discovery Ltd.

Curated by ChEMBL


Assay Description
Displacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assay


Bioorg Med Chem Lett 20: 2516-9 (2010)

More data for this
Ligand-Target Pair
Histamine receptor (H4)


(Homo sapiens (human))
BDBM50315314
PNG
(8-chloro-4-(4-methylpiperazin-1-yl)benzofuro[3,2-d...)
Show SMILES CN1CCN(CC1)c1ncnc2c3cc(Cl)ccc3oc12
Show InChI InChI=1S/C15H15ClN4O/c1-19-4-6-20(7-5-19)15-14-13(17-9-18-15)11-8-10(16)2-3-12(11)21-14/h2-3,8-9H,4-7H2,1H3
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n/an/a 19n/an/an/an/an/an/a



Argenta Discovery Ltd.

Curated by ChEMBL


Assay Description
Displacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assay


Bioorg Med Chem Lett 20: 2516-9 (2010)

More data for this
Ligand-Target Pair
Histamine receptor (H4)


(Homo sapiens (human))
BDBM50315333
PNG
((R)-N-methyl-1-(8-(trifluoromethyl)benzofuro[3,2-d...)
Show SMILES CN[C@@H]1CCN(C1)c1ncnc2c3cc(ccc3oc12)C(F)(F)F
Show InChI InChI=1S/C16H15F3N4O/c1-20-10-4-5-23(7-10)15-14-13(21-8-22-15)11-6-9(16(17,18)19)2-3-12(11)24-14/h2-3,6,8,10,20H,4-5,7H2,1H3/t10-/m1/s1
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n/an/a 30n/an/an/an/an/an/a



Argenta Discovery Ltd.

Curated by ChEMBL


Assay Description
Displacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assay


Bioorg Med Chem Lett 20: 2516-9 (2010)

More data for this
Ligand-Target Pair
Histamine receptor (H4)


(Homo sapiens (human))
BDBM22566
PNG
(5-chloro-2-[(4-methylpiperazin-1-yl)carbonyl]-1H-i...)
Show SMILES CN1CCN(CC1)C(=O)c1cc2cc(Cl)ccc2[nH]1
Show InChI InChI=1S/C14H16ClN3O/c1-17-4-6-18(7-5-17)14(19)13-9-10-8-11(15)2-3-12(10)16-13/h2-3,8-9,16H,4-7H2,1H3
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n/an/a 30n/an/an/an/an/an/a



Pfizer Inc.

Curated by ChEMBL


Assay Description
Antagonist activity at H4R in human eosinophils assessed as inhibition of imetit-induced shape change by GAFS assay


Bioorg Med Chem Lett 21: 6596-602 (2011)

More data for this
Ligand-Target Pair
Histamine receptor (H4)


(Homo sapiens (human))
BDBM50315323
PNG
((R)-1-(8-chlorobenzofuro[3,2-d]pyrimidin-4-yl)-N-m...)
Show SMILES CN[C@@H]1CCN(C1)c1ncnc2c3cc(Cl)ccc3oc12
Show InChI InChI=1S/C15H15ClN4O/c1-17-10-4-5-20(7-10)15-14-13(18-8-19-15)11-6-9(16)2-3-12(11)21-14/h2-3,6,8,10,17H,4-5,7H2,1H3/t10-/m1/s1
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n/an/a 33n/an/an/an/an/an/a



Argenta Discovery Ltd.

Curated by ChEMBL


Assay Description
Displacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assay


Bioorg Med Chem Lett 20: 2516-9 (2010)

More data for this
Ligand-Target Pair
Histamine receptor (H4)


(Homo sapiens (human))
BDBM50361015
PNG
(CHEMBL592379)
Show SMILES CN1CCN(CC1)c1nc(NCCS(=O)(=O)Nc2ccccc2)c2cc(Cl)ccc2n1
Show InChI InChI=1S/C21H25ClN6O2S/c1-27-10-12-28(13-11-27)21-24-19-8-7-16(22)15-18(19)20(25-21)23-9-14-31(29,30)26-17-5-3-2-4-6-17/h2-8,15,26H,9-14H2,1H3,(H,23,24,25)
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n/an/a 33.1n/an/an/an/an/an/a



Griffin Discoveries BV

Curated by ChEMBL


Assay Description
Inverse agonist activity at human histamine H4 receptor expressed in HEK293T cells by CRE-beta-galactosidase assay


J Med Chem 53: 2390-400 (2010)

More data for this
Ligand-Target Pair
Histamine receptor (H4)


(Homo sapiens (human))
BDBM50315339
PNG
(8-chloro-2-methyl-4-(4-methylpiperazin-1-yl)benzof...)
Show SMILES CN1CCN(CC1)c1nc(C)nc2c3cc(Cl)ccc3oc12
Show InChI InChI=1S/C16H17ClN4O/c1-10-18-14-12-9-11(17)3-4-13(12)22-15(14)16(19-10)21-7-5-20(2)6-8-21/h3-4,9H,5-8H2,1-2H3
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n/an/a 37n/an/an/an/an/an/a



Argenta Discovery Ltd.

Curated by ChEMBL


Assay Description
Displacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assay


Bioorg Med Chem Lett 20: 2516-9 (2010)

More data for this
Ligand-Target Pair
Histamine receptor (H4)


(Homo sapiens (human))
BDBM50315342
PNG
(8-chloro-4-(4-methylpiperazin-1-yl)-2-(trifluorome...)
Show SMILES CN1CCN(CC1)c1nc(nc2c3cc(Cl)ccc3oc12)C(F)(F)F
Show InChI InChI=1S/C16H14ClF3N4O/c1-23-4-6-24(7-5-23)14-13-12(21-15(22-14)16(18,19)20)10-8-9(17)2-3-11(10)25-13/h2-3,8H,4-7H2,1H3
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n/an/a 39n/an/an/an/an/an/a



Argenta Discovery Ltd.

Curated by ChEMBL


Assay Description
Inverse agonist activity at human histamine H4 receptor assessed as inhibition of [35S]GTPgammaS binding after 15 mins by scintillation proximity ass...


Bioorg Med Chem Lett 20: 2516-9 (2010)

More data for this
Ligand-Target Pair
Histamine receptor (H4)


(Homo sapiens (human))
BDBM50315323
PNG
((R)-1-(8-chlorobenzofuro[3,2-d]pyrimidin-4-yl)-N-m...)
Show SMILES CN[C@@H]1CCN(C1)c1ncnc2c3cc(Cl)ccc3oc12
Show InChI InChI=1S/C15H15ClN4O/c1-17-10-4-5-20(7-10)15-14-13(18-8-19-15)11-6-9(16)2-3-12(11)21-14/h2-3,6,8,10,17H,4-5,7H2,1H3/t10-/m1/s1
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n/an/a 41n/an/an/an/an/an/a



Argenta Discovery Ltd.

Curated by ChEMBL


Assay Description
Inverse agonist activity at human histamine H4 receptor assessed as inhibition of [35S]GTPgammaS binding after 15 mins by scintillation proximity ass...


Bioorg Med Chem Lett 20: 2516-9 (2010)

More data for this
Ligand-Target Pair
Histamine receptor (H4)


(Homo sapiens (human))
BDBM50361010
PNG
(CHEMBL1935572)
Show SMILES CN1CCN(CC1)c1nc(N)nc2cc(ccc12)-c1ccsc1
Show InChI InChI=1S/C17H19N5S/c1-21-5-7-22(8-6-21)16-14-3-2-12(13-4-9-23-11-13)10-15(14)19-17(18)20-16/h2-4,9-11H,5-8H2,1H3,(H2,18,19,20)
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n/an/a 46n/an/an/an/an/an/a



Griffin Discoveries BV

Curated by ChEMBL


Assay Description
Antagonist activity at human H4 receptor expressed in HEK293T cells assessed as inhibition of histamine-induced [35S]GTPgammaS binding


Bioorg Med Chem Lett 22: 461-7 (2011)

More data for this
Ligand-Target Pair
Histamine receptor (H4)


(Homo sapiens (human))
BDBM50361035
PNG
(CHEMBL1935571)
Show SMILES CN1CCN(CC1)c1nc(N)nc2cc(ccc12)-c1ccoc1
Show InChI InChI=1S/C17H19N5O/c1-21-5-7-22(8-6-21)16-14-3-2-12(13-4-9-23-11-13)10-15(14)19-17(18)20-16/h2-4,9-11H,5-8H2,1H3,(H2,18,19,20)
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n/an/a 47n/an/an/an/an/an/a



Griffin Discoveries BV

Curated by ChEMBL


Assay Description
Antagonist activity at human H4 receptor expressed in HEK293T cells assessed as inhibition of histamine-induced [35S]GTPgammaS binding


Bioorg Med Chem Lett 22: 461-7 (2011)

More data for this
Ligand-Target Pair
Histamine receptor (H4)


(Homo sapiens (human))
BDBM50412494
PNG
(CHEMBL452847 | VUF-10497)
Show SMILES CN1CCN(CC1)c1nc(NCc2cccs2)c2cc(Cl)ccc2n1
Show InChI InChI=1S/C18H20ClN5S/c1-23-6-8-24(9-7-23)18-21-16-5-4-13(19)11-15(16)17(22-18)20-12-14-3-2-10-25-14/h2-5,10-11H,6-9,12H2,1H3,(H,20,21,22)
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n/an/a 69.2n/an/an/an/an/an/a



Vrije Universiteit Amsterdam

Curated by ChEMBL


Assay Description
Inverse agonist activity at human histamine H4 receptor expressed in HEK293T cells by CRE-beta-galactosidase assay


J Med Chem 51: 7855-65 (2008)

More data for this
Ligand-Target Pair
Histamine receptor (H4)


(Homo sapiens (human))
BDBM50315317
PNG
(8-chloro-4-((1S,4S)-5-methyl-2,5-diazabicyclo[2.2....)
Show SMILES CN1C[C@@H]2C[C@H]1CN2c1ncnc2c1oc1ccc(Cl)cc21
Show InChI InChI=1S/C16H15ClN4O/c1-20-6-11-5-10(20)7-21(11)16-15-14(18-8-19-16)12-4-9(17)2-3-13(12)22-15/h2-4,8,10-11H,5-7H2,1H3/t10-,11-/m0/s1
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n/an/a 70n/an/an/an/an/an/a



Argenta Discovery Ltd.

Curated by ChEMBL


Assay Description
Inverse agonist activity at human histamine H4 receptor assessed as inhibition of [35S]GTPgammaS binding after 15 mins by scintillation proximity ass...


Bioorg Med Chem Lett 20: 2516-9 (2010)

More data for this
Ligand-Target Pair
Histamine receptor (H4)


(Homo sapiens (human))
BDBM50315331
PNG
(1-(8-chlorobenzofuro[3,2-d]pyrimidin-4-yl)-N-methy...)
Show SMILES CNC1CN(C1)c1ncnc2c3cc(Cl)ccc3oc12
Show InChI InChI=1S/C14H13ClN4O/c1-16-9-5-19(6-9)14-13-12(17-7-18-14)10-4-8(15)2-3-11(10)20-13/h2-4,7,9,16H,5-6H2,1H3
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n/an/a 76n/an/an/an/an/an/a



Argenta Discovery Ltd.

Curated by ChEMBL


Assay Description
Inverse agonist activity at human histamine H4 receptor assessed as inhibition of [35S]GTPgammaS binding after 15 mins by scintillation proximity ass...


Bioorg Med Chem Lett 20: 2516-9 (2010)

More data for this
Ligand-Target Pair
Histamine receptor (H4)


(Homo sapiens (human))
BDBM50315342
PNG
(8-chloro-4-(4-methylpiperazin-1-yl)-2-(trifluorome...)
Show SMILES CN1CCN(CC1)c1nc(nc2c3cc(Cl)ccc3oc12)C(F)(F)F
Show InChI InChI=1S/C16H14ClF3N4O/c1-23-4-6-24(7-5-23)14-13-12(21-15(22-14)16(18,19)20)10-8-9(17)2-3-11(10)25-13/h2-3,8H,4-7H2,1H3
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n/an/a 83n/an/an/an/an/an/a



Argenta Discovery Ltd.

Curated by ChEMBL


Assay Description
Displacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assay


Bioorg Med Chem Lett 20: 2516-9 (2010)

More data for this
Ligand-Target Pair
Histamine receptor (H4)


(Homo sapiens (human))
BDBM50361011
PNG
(CHEMBL1935573)
Show SMILES CN1CCN(CC1)c1nc(N)nc2cc(ccc12)-c1ccco1
Show InChI InChI=1S/C17H19N5O/c1-21-6-8-22(9-7-21)16-13-5-4-12(15-3-2-10-23-15)11-14(13)19-17(18)20-16/h2-5,10-11H,6-9H2,1H3,(H2,18,19,20)
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n/an/a 83n/an/an/an/an/an/a



Griffin Discoveries BV

Curated by ChEMBL


Assay Description
Antagonist activity at human H4 receptor expressed in HEK293T cells assessed as inhibition of histamine-induced [35S]GTPgammaS binding


Bioorg Med Chem Lett 22: 461-7 (2011)

More data for this
Ligand-Target Pair
Histamine receptor (H4)


(Homo sapiens (human))
BDBM50315332
PNG
((R)-N-methyl-1-(8-methylbenzofuro[3,2-d]pyrimidin-...)
Show SMILES CN[C@@H]1CCN(C1)c1ncnc2c1oc1ccc(C)cc21
Show InChI InChI=1S/C16H18N4O/c1-10-3-4-13-12(7-10)14-15(21-13)16(19-9-18-14)20-6-5-11(8-20)17-2/h3-4,7,9,11,17H,5-6,8H2,1-2H3/t11-/m1/s1
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n/an/a 86n/an/an/an/an/an/a



Argenta Discovery Ltd.

Curated by ChEMBL


Assay Description
Displacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assay


Bioorg Med Chem Lett 20: 2516-9 (2010)

More data for this
Ligand-Target Pair
Histamine receptor (H4)


(Homo sapiens (human))
BDBM22566
PNG
(5-chloro-2-[(4-methylpiperazin-1-yl)carbonyl]-1H-i...)
Show SMILES CN1CCN(CC1)C(=O)c1cc2cc(Cl)ccc2[nH]1
Show InChI InChI=1S/C14H16ClN3O/c1-17-4-6-18(7-5-17)14(19)13-9-10-8-11(15)2-3-12(10)16-13/h2-3,8-9,16H,4-7H2,1H3
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n/an/a 86n/an/an/an/an/an/a



Boehringer Ingelheim RCV GmbH& Co KG

Curated by ChEMBL


Assay Description
Inhibition of histamine H4 receptor-mediated chemotaxis in human eosinophils


Eur J Med Chem 54: 660-8 (2012)

More data for this
Ligand-Target Pair
Histamine receptor (H4)


(Homo sapiens (human))
BDBM50315331
PNG
(1-(8-chlorobenzofuro[3,2-d]pyrimidin-4-yl)-N-methy...)
Show SMILES CNC1CN(C1)c1ncnc2c3cc(Cl)ccc3oc12
Show InChI InChI=1S/C14H13ClN4O/c1-16-9-5-19(6-9)14-13-12(17-7-18-14)10-4-8(15)2-3-11(10)20-13/h2-4,7,9,16H,5-6H2,1H3
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n/an/a 87n/an/an/an/an/an/a



Argenta Discovery Ltd.

Curated by ChEMBL


Assay Description
Displacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assay


Bioorg Med Chem Lett 20: 2516-9 (2010)

More data for this
Ligand-Target Pair
Histamine receptor (H4)


(Homo sapiens (human))
BDBM50315347
PNG
(8-chloro-2-methoxy-4-(4-methylpiperazin-1-yl)benzo...)
Show SMILES COc1nc(N2CCN(C)CC2)c2oc3ccc(Cl)cc3c2n1
Show InChI InChI=1S/C16H17ClN4O2/c1-20-5-7-21(8-6-20)15-14-13(18-16(19-15)22-2)11-9-10(17)3-4-12(11)23-14/h3-4,9H,5-8H2,1-2H3
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n/an/a 90n/an/an/an/an/an/a



Argenta Discovery Ltd.

Curated by ChEMBL


Assay Description
Displacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assay


Bioorg Med Chem Lett 20: 2516-9 (2010)

More data for this
Ligand-Target Pair
Histamine receptor (H4)


(Homo sapiens (human))
BDBM50315322
PNG
(1-(8-chlorobenzofuro[3,2-d]pyrimidin-4-yl)-N-methy...)
Show SMILES CNC1CCN(C1)c1ncnc2c3cc(Cl)ccc3oc12
Show InChI InChI=1S/C15H15ClN4O/c1-17-10-4-5-20(7-10)15-14-13(18-8-19-15)11-6-9(16)2-3-12(11)21-14/h2-3,6,8,10,17H,4-5,7H2,1H3
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n/an/a 95n/an/an/an/an/an/a



Argenta Discovery Ltd.

Curated by ChEMBL


Assay Description
Displacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assay


Bioorg Med Chem Lett 20: 2516-9 (2010)

More data for this
Ligand-Target Pair
Histamine receptor (H4)


(Homo sapiens (human))
BDBM50361012
PNG
(CHEMBL1935574)
Show SMILES Nc1nc(N2CCNCC2)c2ccc(cc2n1)-c1ccco1
Show InChI InChI=1S/C16H17N5O/c17-16-19-13-10-11(14-2-1-9-22-14)3-4-12(13)15(20-16)21-7-5-18-6-8-21/h1-4,9-10,18H,5-8H2,(H2,17,19,20)
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n/an/a 106n/an/an/an/an/an/a



Griffin Discoveries BV

Curated by ChEMBL


Assay Description
Antagonist activity at human H4 receptor expressed in HEK293T cells assessed as inhibition of histamine-induced [35S]GTPgammaS binding


Bioorg Med Chem Lett 22: 461-7 (2011)

More data for this
Ligand-Target Pair
Histamine receptor (H4)


(Homo sapiens (human))
BDBM50194205
PNG
((1R,2S)-trans-2-[2-(4-chlorobenzylamino)ethyl]-1-(...)
Show SMILES Clc1ccc(CNCC[C@@H]2C[C@H]2c2cnc[nH]2)cc1
Show InChI InChI=1S/C15H18ClN3/c16-13-3-1-11(2-4-13)8-17-6-5-12-7-14(12)15-9-18-10-19-15/h1-4,9-10,12,14,17H,5-8H2,(H,18,19)/t12-,14-/m1/s1
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n/an/a 110n/an/an/an/an/an/a



Hokkaido University

Curated by ChEMBL


Assay Description
Antagonist activity at human H4 receptor expressed in 293-EBNA cells assessed as inhibition of histamine agonist activity by luciferase reporter gene...


J Med Chem 49: 5587-96 (2006)

More data for this
Ligand-Target Pair
Histamine receptor (H4)


(Homo sapiens (human))
BDBM50315317
PNG
(8-chloro-4-((1S,4S)-5-methyl-2,5-diazabicyclo[2.2....)
Show SMILES CN1C[C@@H]2C[C@H]1CN2c1ncnc2c1oc1ccc(Cl)cc21
Show InChI InChI=1S/C16H15ClN4O/c1-20-6-11-5-10(20)7-21(11)16-15-14(18-8-19-16)12-4-9(17)2-3-13(12)22-15/h2-4,8,10-11H,5-7H2,1H3/t10-,11-/m0/s1
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n/an/a 111n/an/an/an/an/an/a



Argenta Discovery Ltd.

Curated by ChEMBL


Assay Description
Displacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assay


Bioorg Med Chem Lett 20: 2516-9 (2010)

More data for this
Ligand-Target Pair
Histamine receptor (H4)


(Homo sapiens (human))
BDBM50315325
PNG
(1-(8-chlorobenzofuro[3,2-d]pyrimidin-4-yl)pyrrolid...)
Show SMILES NC1CCN(C1)c1ncnc2c1oc1ccc(Cl)cc21
Show InChI InChI=1S/C14H13ClN4O/c15-8-1-2-11-10(5-8)12-13(20-11)14(18-7-17-12)19-4-3-9(16)6-19/h1-2,5,7,9H,3-4,6,16H2
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n/an/a 126n/an/an/an/an/an/a



Argenta Discovery Ltd.

Curated by ChEMBL


Assay Description
Displacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assay


Bioorg Med Chem Lett 20: 2516-9 (2010)

More data for this
Ligand-Target Pair
Histamine receptor (H4)


(Homo sapiens (human))
BDBM50397292
PNG
(CHEMBL454890 | VUF-10499)
Show SMILES CN1CCN(CC1)c1nc(NCc2ccoc2)c2cc(Cl)ccc2n1
Show InChI InChI=1S/C18H20ClN5O/c1-23-5-7-24(8-6-23)18-21-16-3-2-14(19)10-15(16)17(22-18)20-11-13-4-9-25-12-13/h2-4,9-10,12H,5-8,11H2,1H3,(H,20,21,22)
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n/an/a 145n/an/an/an/an/an/a



Vrije Universiteit Amsterdam

Curated by ChEMBL


Assay Description
Inverse agonist activity at human histamine H4 receptor expressed in HEK293T cells by CRE-beta-galactosidase assay


J Med Chem 51: 7855-65 (2008)

More data for this
Ligand-Target Pair
Histamine receptor (H4)


(Homo sapiens (human))
BDBM50315318
PNG
(8-chloro-4-(5-methyl-2,5-diazabicyclo[2.2.2]octan-...)
Show SMILES CN1CC2CCC1CN2c1ncnc2c1oc1ccc(Cl)cc21
Show InChI InChI=1S/C17H17ClN4O/c1-21-7-12-4-3-11(21)8-22(12)17-16-15(19-9-20-17)13-6-10(18)2-5-14(13)23-16/h2,5-6,9,11-12H,3-4,7-8H2,1H3
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n/an/a 169n/an/an/an/an/an/a



Argenta Discovery Ltd.

Curated by ChEMBL


Assay Description
Displacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assay


Bioorg Med Chem Lett 20: 2516-9 (2010)

More data for this
Ligand-Target Pair
Histamine receptor (H4)


(Homo sapiens (human))
BDBM50315338
PNG
((R)-1-(7-chlorobenzofuro[3,2-d]pyrimidin-4-yl)-N-m...)
Show SMILES CN[C@@H]1CCN(C1)c1ncnc2c3ccc(Cl)cc3oc12
Show InChI InChI=1S/C15H15ClN4O/c1-17-10-4-5-20(7-10)15-14-13(18-8-19-15)11-3-2-9(16)6-12(11)21-14/h2-3,6,8,10,17H,4-5,7H2,1H3/t10-/m1/s1
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n/an/a 171n/an/an/an/an/an/a



Argenta Discovery Ltd.

Curated by ChEMBL


Assay Description
Displacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assay


Bioorg Med Chem Lett 20: 2516-9 (2010)

More data for this
Ligand-Target Pair
Histamine receptor (H4)


(Homo sapiens (human))
BDBM22566
PNG
(5-chloro-2-[(4-methylpiperazin-1-yl)carbonyl]-1H-i...)
Show SMILES CN1CCN(CC1)C(=O)c1cc2cc(Cl)ccc2[nH]1
Show InChI InChI=1S/C14H16ClN3O/c1-17-4-6-18(7-5-17)14(19)13-9-10-8-11(15)2-3-12(10)16-13/h2-3,8-9,16H,4-7H2,1H3
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n/an/a 199n/an/an/an/an/an/a



Pfizer Inc.

Curated by ChEMBL


Assay Description
Antagonist activity at H4R in human eosinophils assessed as inhibition of histamine-induced shape change by GAFS assay


Bioorg Med Chem Lett 21: 6596-602 (2011)

More data for this
Ligand-Target Pair
Histamine receptor (H4)


(Homo sapiens (human))
BDBM22566
PNG
(5-chloro-2-[(4-methylpiperazin-1-yl)carbonyl]-1H-i...)
Show SMILES CN1CCN(CC1)C(=O)c1cc2cc(Cl)ccc2[nH]1
Show InChI InChI=1S/C14H16ClN3O/c1-17-4-6-18(7-5-17)14(19)13-9-10-8-11(15)2-3-12(10)16-13/h2-3,8-9,16H,4-7H2,1H3
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n/an/a 200n/an/an/an/an/an/a



Merck Research Laboratories

Curated by ChEMBL


Assay Description
Antagonist actiivty at human H4R expressed in human U2OS cells assessed as inhibition of [35S]GTPgammaS binding after 30 mins by scintillation proxim...


J Med Chem 57: 6887-96 (2014)

More data for this
Ligand-Target Pair
Histamine receptor (H4)


(Homo sapiens (human))
BDBM22566
PNG
(5-chloro-2-[(4-methylpiperazin-1-yl)carbonyl]-1H-i...)
Show SMILES CN1CCN(CC1)C(=O)c1cc2cc(Cl)ccc2[nH]1
Show InChI InChI=1S/C14H16ClN3O/c1-17-4-6-18(7-5-17)14(19)13-9-10-8-11(15)2-3-12(10)16-13/h2-3,8-9,16H,4-7H2,1H3
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n/an/a 221n/an/an/an/an/an/a



Pfizer Inc.

Curated by ChEMBL


Assay Description
Antagonist activity at H4R in human eosinophils assessed as inhibition of histamine-induced CD11b upregulation


Bioorg Med Chem Lett 21: 6596-602 (2011)

More data for this
Ligand-Target Pair
Histamine receptor (H4)


(Homo sapiens (human))
BDBM50315320
PNG
(8-chloro-4-(hexahydropyrrolo[1,2-a]pyrazin-2(1H)-y...)
Show SMILES Clc1ccc2oc3c(ncnc3c2c1)N1CCN2CCCC2C1
Show InChI InChI=1S/C17H17ClN4O/c18-11-3-4-14-13(8-11)15-16(23-14)17(20-10-19-15)22-7-6-21-5-1-2-12(21)9-22/h3-4,8,10,12H,1-2,5-7,9H2
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n/an/a 236n/an/an/an/an/an/a



Argenta Discovery Ltd.

Curated by ChEMBL


Assay Description
Displacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assay


Bioorg Med Chem Lett 20: 2516-9 (2010)

More data for this
Ligand-Target Pair
Histamine receptor (H4)


(Homo sapiens (human))
BDBM50315324
PNG
((S)-1-(8-chlorobenzofuro[3,2-d]pyrimidin-4-yl)-N-m...)
Show SMILES CN[C@H]1CCN(C1)c1ncnc2c3cc(Cl)ccc3oc12
Show InChI InChI=1S/C15H15ClN4O/c1-17-10-4-5-20(7-10)15-14-13(18-8-19-15)11-6-9(16)2-3-12(11)21-14/h2-3,6,8,10,17H,4-5,7H2,1H3/t10-/m0/s1
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n/an/a 285n/an/an/an/an/an/a



Argenta Discovery Ltd.

Curated by ChEMBL


Assay Description
Displacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assay


Bioorg Med Chem Lett 20: 2516-9 (2010)

More data for this
Ligand-Target Pair
Histamine receptor (H4)


(Homo sapiens (human))
BDBM50315324
PNG
((S)-1-(8-chlorobenzofuro[3,2-d]pyrimidin-4-yl)-N-m...)
Show SMILES CN[C@H]1CCN(C1)c1ncnc2c3cc(Cl)ccc3oc12
Show InChI InChI=1S/C15H15ClN4O/c1-17-10-4-5-20(7-10)15-14-13(18-8-19-15)11-6-9(16)2-3-12(11)21-14/h2-3,6,8,10,17H,4-5,7H2,1H3/t10-/m0/s1
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n/an/a 292n/an/an/an/an/an/a



Argenta Discovery Ltd.

Curated by ChEMBL


Assay Description
Inverse agonist activity at human histamine H4 receptor assessed as inhibition of [35S]GTPgammaS binding after 15 mins by scintillation proximity ass...


Bioorg Med Chem Lett 20: 2516-9 (2010)

More data for this
Ligand-Target Pair
Histamine receptor (H4)


(Homo sapiens (human))
BDBM50315344
PNG
(8-chloro-2-cyclopropyl-4-(4-methylpiperazin-1-yl)b...)
Show SMILES CN1CCN(CC1)c1nc(nc2c3cc(Cl)ccc3oc12)C1CC1
Show InChI InChI=1S/C18H19ClN4O/c1-22-6-8-23(9-7-22)18-16-15(20-17(21-18)11-2-3-11)13-10-12(19)4-5-14(13)24-16/h4-5,10-11H,2-3,6-9H2,1H3
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n/an/a 310n/an/an/an/an/an/a



Argenta Discovery Ltd.

Curated by ChEMBL


Assay Description
Displacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assay


Bioorg Med Chem Lett 20: 2516-9 (2010)

More data for this
Ligand-Target Pair
Histamine receptor (H4)


(Homo sapiens (human))
BDBM50127245
PNG
(CHEMBL3628042)
Show SMILES CN1CCN(CC1)c1nc(N)nc(\C=C\c2cccc(Cl)c2)n1
Show InChI InChI=1S/C16H19ClN6/c1-22-7-9-23(10-8-22)16-20-14(19-15(18)21-16)6-5-12-3-2-4-13(17)11-12/h2-6,11H,7-10H2,1H3,(H2,18,19,20,21)/b6-5+
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n/an/a 439n/an/an/an/an/an/a



Jagiellonian University Medical College

Curated by ChEMBL


Assay Description
Antagonist activity at human H4R expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by TR-FRET immuno...


Citation and Details
More data for this
Ligand-Target Pair
Histamine receptor (H4)


(Homo sapiens (human))
BDBM50315319
PNG
(8-chloro-4-(8-methyl-3,8-diazabicyclo[3.2.1]octan-...)
Show SMILES CN1C2CCC1CN(C2)c1ncnc2c3cc(Cl)ccc3oc12
Show InChI InChI=1S/C17H17ClN4O/c1-21-11-3-4-12(21)8-22(7-11)17-16-15(19-9-20-17)13-6-10(18)2-5-14(13)23-16/h2,5-6,9,11-12H,3-4,7-8H2,1H3
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n/an/a 440n/an/an/an/an/an/a



Argenta Discovery Ltd.

Curated by ChEMBL


Assay Description
Displacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assay


Bioorg Med Chem Lett 20: 2516-9 (2010)

More data for this
Ligand-Target Pair
Histamine receptor (H4)


(Homo sapiens (human))
BDBM50021536
PNG
(CHEMBL3290576)
Show SMILES CN1CCN(CC1)c1nc(N)nc(n1)-c1ccc(Cl)cc1
Show InChI InChI=1S/C14H17ClN6/c1-20-6-8-21(9-7-20)14-18-12(17-13(16)19-14)10-2-4-11(15)5-3-10/h2-5H,6-9H2,1H3,(H2,16,17,18,19)
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n/an/a 512n/an/an/an/an/an/a



Jagiellonian University Medical College

Curated by ChEMBL


Assay Description
Antagonist activity at human histamine H4 receptor expressed in gamma-irradiated recombinant CHO cells assessed as inhibition of forskolin/histamine-...


Eur J Med Chem 83: 534-46 (2014)

More data for this
Ligand-Target Pair
Histamine receptor (H4)


(Homo sapiens (human))
BDBM50127253
PNG
(CHEMBL3629828)
Show SMILES CN1CCN(CC1)c1nc(N)nc(\C=C\c2cccc(C)c2)n1
Show InChI InChI=1S/C17H22N6/c1-13-4-3-5-14(12-13)6-7-15-19-16(18)21-17(20-15)23-10-8-22(2)9-11-23/h3-7,12H,8-11H2,1-2H3,(H2,18,19,20,21)/b7-6+
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n/an/a 606n/an/an/an/an/an/a



Jagiellonian University Medical College

Curated by ChEMBL


Assay Description
Antagonist activity at human H4R expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by TR-FRET immuno...


Citation and Details
More data for this
Ligand-Target Pair
Histamine receptor (H4)


(Homo sapiens (human))
BDBM22914
PNG
(CHEMBL260374 | N-cyclohexyl-4-(1H-imidazol-5-yl)pi...)
Show SMILES S=C(NC1CCCCC1)N1CCC(CC1)c1cnc[nH]1
Show InChI InChI=1S/C15H24N4S/c20-15(18-13-4-2-1-3-5-13)19-8-6-12(7-9-19)14-10-16-11-17-14/h10-13H,1-9H2,(H,16,17)(H,18,20)
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n/an/a 667n/an/an/an/an/an/a



Zhejiang University

Curated by ChEMBL


Assay Description
Antagonist activity at histamine H4 receptor expressed in HEK293 cells co-transfected with pCRE-Luc gene assessed as inhibition of forskolin/histamin...


Bioorg Med Chem 19: 7158-67 (2011)

More data for this
Ligand-Target Pair
Histamine receptor (H4)


(Homo sapiens (human))
BDBM22914
PNG
(CHEMBL260374 | N-cyclohexyl-4-(1H-imidazol-5-yl)pi...)
Show SMILES S=C(NC1CCCCC1)N1CCC(CC1)c1cnc[nH]1
Show InChI InChI=1S/C15H24N4S/c20-15(18-13-4-2-1-3-5-13)19-8-6-12(7-9-19)14-10-16-11-17-14/h10-13H,1-9H2,(H,16,17)(H,18,20)
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n/an/a 680n/an/an/an/an/an/a



Hokkaido University

Curated by ChEMBL


Assay Description
Antagonist activity at human H4 receptor expressed in 293-EBNA cells assessed as inhibition of histamine agonist activity by luciferase reporter gene...


J Med Chem 49: 5587-96 (2006)

More data for this
Ligand-Target Pair
Histamine receptor (H4)


(Homo sapiens (human))
BDBM50194208
PNG
((1S,2R)-trans-2-[2-(4-chlorobenzylamino)ethyl]-1-(...)
Show SMILES Clc1ccc(CNCC[C@H]2C[C@@H]2c2cnc[nH]2)cc1
Show InChI InChI=1S/C15H18ClN3/c16-13-3-1-11(2-4-13)8-17-6-5-12-7-14(12)15-9-18-10-19-15/h1-4,9-10,12,14,17H,5-8H2,(H,18,19)/t12-,14-/m0/s1
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n/an/a 860n/an/an/an/an/an/a



Hokkaido University

Curated by ChEMBL


Assay Description
Antagonist activity at human H4 receptor expressed in 293-EBNA cells assessed as inhibition of histamine agonist activity by luciferase reporter gene...


J Med Chem 49: 5587-96 (2006)

More data for this
Ligand-Target Pair
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