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Compile Data Set for Download or QSAR

Found 157 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 H4 receptor


(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 H4 receptor


(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 H4 receptor


(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 H4 receptor


(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 H4 receptor


(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 H4 receptor


(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 H4 receptor


(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 H4 receptor


(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 H4 receptor


(Homo sapiens (Human))
BDBM294419
PNG
(US9586959, Compound 98)
Show SMILES CN1CCN(CC1)c1nc2ncc(Cl)cc2n2nc(C)nc12
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n/an/a 11n/an/an/an/a7.525



Lilly Research Laboratories





Bioorg Med Chem Lett 14: 3925-8 (2004)

More data for this
Ligand-Target Pair
Histamine H4 receptor


(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 H4 receptor


(Homo sapiens (Human))
BDBM294378
PNG
(US9586959, Compound 31)
Show SMILES CN1CCN(CC1)c1nc2ncc(Cl)cc2c2nc(C)nn12
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n/an/a 16n/an/an/an/a7.525



Lilly Research Laboratories





Bioorg Med Chem Lett 14: 3925-8 (2004)

More data for this
Ligand-Target Pair
Histamine H4 receptor


(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 H4 receptor


(Homo sapiens (Human))
BDBM294427
PNG
(US9586959, Compound disclosed in WO 2010030785, Ex...)
Show SMILES CN1CCN(CC1)c1nc2ccc(Cl)cc2n2cnnc12
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n/an/a 22n/an/an/an/a7.525



Lilly Research Laboratories





Bioorg Med Chem Lett 14: 3925-8 (2004)

More data for this
Ligand-Target Pair
Histamine H4 receptor


(Homo sapiens (Human))
BDBM294418
PNG
(US9586959, Compound 96)
Show SMILES CN1CCN(CC1)c1nc2ncc(Br)cc2n2nnnc12
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n/an/a 28n/an/an/an/a7.525



Lilly Research Laboratories





Bioorg Med Chem Lett 14: 3925-8 (2004)

More data for this
Ligand-Target Pair
Histamine H4 receptor


(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 H4 receptor


(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 H4 receptor


(Homo sapiens (Human))
BDBM294373
PNG
(US9586959, Compound 104 | US9586959, Compound 24 |...)
Show SMILES CNC1CN(C1)c1nc2ncc(Br)cc2n2cnnc12
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n/an/a 30n/an/an/an/a7.525



Lilly Research Laboratories





Bioorg Med Chem Lett 14: 3925-8 (2004)

More data for this
Ligand-Target Pair
Histamine H4 receptor


(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 H4 receptor


(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 H4 receptor


(Homo sapiens (Human))
BDBM294386
PNG
(US9586959, Compound 49)
Show SMILES CN1CCN(CC1)c1nc2ncc(I)cc2n2cnnc12
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n/an/a 34n/an/an/an/a7.525



Lilly Research Laboratories





Bioorg Med Chem Lett 14: 3925-8 (2004)

More data for this
Ligand-Target Pair
Histamine H4 receptor


(Homo sapiens (Human))
BDBM294407
PNG
(US9586959, Compound 69 | US9586959, Compound 95)
Show SMILES CNC1CN(C1)c1nc2ncc(Br)cc2n2nnnc12
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n/an/a 35n/an/an/an/a7.525



Lilly Research Laboratories





Bioorg Med Chem Lett 14: 3925-8 (2004)

More data for this
Ligand-Target Pair
Histamine H4 receptor


(Homo sapiens (Human))
BDBM294373
PNG
(US9586959, Compound 104 | US9586959, Compound 24 |...)
Show SMILES CNC1CN(C1)c1nc2ncc(Br)cc2n2cnnc12
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n/an/a 36n/an/an/an/a7.525



Lilly Research Laboratories





Bioorg Med Chem Lett 14: 3925-8 (2004)

More data for this
Ligand-Target Pair
Histamine H4 receptor


(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 H4 receptor


(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 H4 receptor


(Homo sapiens (Human))
BDBM294361
PNG
(US9586959, Compound 4)
Show SMILES CN1CCN(CC1)c1nc2ncc(Cl)cc2n2cnnc12
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n/an/a 40n/an/an/an/a7.525



Lilly Research Laboratories





Bioorg Med Chem Lett 14: 3925-8 (2004)

More data for this
Ligand-Target Pair
Histamine H4 receptor


(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 H4 receptor


(Homo sapiens (Human))
BDBM294414
PNG
(US9586959, Compound 92)
Show SMILES CN1CCN(CC1)C1=Nc2ncc(Cl)cc2C2OC(C)=NC12 |c:21,t:8|
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n/an/a 42n/an/an/an/a7.525



Lilly Research Laboratories





Bioorg Med Chem Lett 14: 3925-8 (2004)

More data for this
Ligand-Target Pair
Histamine H4 receptor


(Homo sapiens (Human))
BDBM294407
PNG
(US9586959, Compound 69 | US9586959, Compound 95)
Show SMILES CNC1CN(C1)c1nc2ncc(Br)cc2n2nnnc12
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n/an/a 44n/an/an/an/a7.525



Lilly Research Laboratories





Bioorg Med Chem Lett 14: 3925-8 (2004)

More data for this
Ligand-Target Pair
Histamine H4 receptor


(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 H4 receptor


(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 H4 receptor


(Homo sapiens (Human))
BDBM294377
PNG
(US9586959, Compound 29)
Show SMILES Clc1cnc2nc(N3CCN4CCCC4C3)c3nncn3c2c1
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n/an/a 49n/an/an/an/a7.525



Lilly Research Laboratories





Bioorg Med Chem Lett 14: 3925-8 (2004)

More data for this
Ligand-Target Pair
Histamine H4 receptor


(Homo sapiens (Human))
BDBM294368
PNG
(US9586959, Compound 18)
Show SMILES CNC1CN(C1)c1nc2ncc(Cl)cc2n2cnnc12
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n/an/a 55n/an/an/an/a7.525



Lilly Research Laboratories





Bioorg Med Chem Lett 14: 3925-8 (2004)

More data for this
Ligand-Target Pair
Histamine H4 receptor


(Homo sapiens (Human))
BDBM294408
PNG
(US9586959, Compound 74)
Show SMILES Brc1cnc2nc(N3CCN4CCCC4C3)c3nncn3c2c1
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n/an/a 60n/an/an/an/a7.525



Lilly Research Laboratories





Bioorg Med Chem Lett 14: 3925-8 (2004)

More data for this
Ligand-Target Pair
Histamine H4 receptor


(Homo sapiens (Human))
BDBM294416
PNG
(US9586959, Compound 94)
Show SMILES CN1CCN(CC1)c1nc2ncc(Cl)cc2n2nnnc12
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n/an/a 62n/an/an/an/a7.525



Lilly Research Laboratories





Bioorg Med Chem Lett 14: 3925-8 (2004)

More data for this
Ligand-Target Pair
Histamine H4 receptor


(Homo sapiens (Human))
BDBM294409
PNG
(US9586959, Compound 75)
Show SMILES Ic1cnc2nc(N3CCN4CCCC4C3)c3nncn3c2c1
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n/an/a 64n/an/an/an/a7.525



Lilly Research Laboratories





Bioorg Med Chem Lett 14: 3925-8 (2004)

More data for this
Ligand-Target Pair
Histamine H4 receptor


(Homo sapiens (Human))
BDBM294415
PNG
(US9586959, Compound 93)
Show SMILES CNC1CN(C1)c1nc2ncc(Cl)cc2n2nnnc12
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n/an/a 65n/an/an/an/a7.525



Lilly Research Laboratories





Bioorg Med Chem Lett 14: 3925-8 (2004)

More data for this
Ligand-Target Pair
Histamine H4 receptor


(Homo sapiens (Human))
BDBM294385
PNG
(US9586959, Compound 48)
Show SMILES CNC1CN(C1)c1nc2ncc(I)cc2n2cnnc12
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n/an/a 65n/an/an/an/a7.525



Lilly Research Laboratories





Bioorg Med Chem Lett 14: 3925-8 (2004)

More data for this
Ligand-Target Pair
Histamine H4 receptor


(Homo sapiens (Human))
BDBM294366
PNG
(US9586959, Compound 16)
Show SMILES Brc1cnc2nc(N3CCNCC3)c3nncn3c2c1
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n/an/a 65n/an/an/an/a7.525



Lilly Research Laboratories





Bioorg Med Chem Lett 14: 3925-8 (2004)

More data for this
Ligand-Target Pair
Histamine H4 receptor


(Homo sapiens (Human))
BDBM294364
PNG
(US9586959, Compound 12)
Show SMILES CN1CCN(CC1)c1nc2ncc(Br)cc2n2cnnc12
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n/an/a 67n/an/an/an/a7.525



Lilly Research Laboratories





Bioorg Med Chem Lett 14: 3925-8 (2004)

More data for this
Ligand-Target Pair
Histamine H4 receptor


(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 H4 receptor


(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 H4 receptor


(Homo sapiens (Human))
BDBM294382
PNG
(US9586959, Compound 43)
Show SMILES CN1CCN(CC1)c1nc2ncc(Cl)cc2c2cn(C)nc12
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n/an/a 70n/an/an/an/a7.525



Lilly Research Laboratories





Bioorg Med Chem Lett 14: 3925-8 (2004)

More data for this
Ligand-Target Pair
Histamine H4 receptor


(Homo sapiens (Human))
BDBM294379
PNG
(US9586959, Compound 32)
Show SMILES Cc1nc2c3cc(Cl)cnc3nc(N3CCNCC3)n2n1
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n/an/a 73n/an/an/an/a7.525



Lilly Research Laboratories





Bioorg Med Chem Lett 14: 3925-8 (2004)

More data for this
Ligand-Target Pair
Histamine H4 receptor


(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 H4 receptor


(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 H4 receptor


(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 H4 receptor


(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 H4 receptor


(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 H4 receptor


(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 H4 receptor


(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
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