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PubMed code 22189138

Compile data set for download or QSAR
Found 62 hits of Enzyme Inhibition Constant Data   
Target/Host
(Institution)
LigandTarget/Host
Links
Ligand
Links
Trg + Lig
Links
Ki
nM
ΔG°
kJ/mole
IC50
nM
Kd
nM
EC50/IC50
nM
koff
s-1
kon
M-1s-1
pHTemp
°C
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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PubMed
4n/an/an/an/an/an/an/an/a



Pfizer Inc.

Curated by ChEMBL


Assay Description
Binding affinity to human histamine H4 receptor


Bioorg Med Chem Lett 22: 1156-9 (2012)


Article DOI: 10.1016/j.bmcl.2011.11.098
BindingDB Entry DOI: 10.7270/Q2Q81DJD
More data for this
Ligand-Target Pair
Histamine H4 receptor


(Homo sapiens (Human))
BDBM50362216
PNG
(CHEMBL1938977)
Show SMILES CN1C[C@H]2CN(C[C@H]2C1)C(=N)c1nc2ccc(F)cc2[nH]1 |r|
Show InChI InChI=1S/C15H18FN5/c1-20-5-9-7-21(8-10(9)6-20)14(17)15-18-12-3-2-11(16)4-13(12)19-15/h2-4,9-10,17H,5-8H2,1H3,(H,18,19)/t9-,10+
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PubMed
4.60n/an/an/an/an/an/an/an/a



Pfizer Inc.

Curated by ChEMBL


Assay Description
Displacement of [3H]histamine from human recombinant histamine H4 receptor expressed in CHO cells coexpressing Ga15 by radioligand filtration binding...


Bioorg Med Chem Lett 22: 1156-9 (2012)


Article DOI: 10.1016/j.bmcl.2011.11.098
BindingDB Entry DOI: 10.7270/Q2Q81DJD
More data for this
Ligand-Target Pair
Histamine H4 receptor


(Homo sapiens (Human))
BDBM50362214
PNG
(CHEMBL1938975)
Show SMILES CN1C[C@H]2CN(C[C@H]2C1)C(=N)c1nc2ccc(F)c(C)c2[nH]1 |r|
Show InChI InChI=1S/C16H20FN5/c1-9-12(17)3-4-13-14(9)20-16(19-13)15(18)22-7-10-5-21(2)6-11(10)8-22/h3-4,10-11,18H,5-8H2,1-2H3,(H,19,20)/t10-,11+
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4.60n/an/an/an/an/an/an/an/a



Pfizer Inc.

Curated by ChEMBL


Assay Description
Displacement of [3H]histamine from human recombinant histamine H4 receptor expressed in CHO cells coexpressing Ga15 by radioligand filtration binding...


Bioorg Med Chem Lett 22: 1156-9 (2012)


Article DOI: 10.1016/j.bmcl.2011.11.098
BindingDB Entry DOI: 10.7270/Q2Q81DJD
More data for this
Ligand-Target Pair
Histamine H4 receptor


(Homo sapiens (Human))
BDBM50362218
PNG
(CHEMBL1938979)
Show SMILES CN1C[C@H]2CN(C[C@H]2C1)C(=N)c1nc2ccccc2[nH]1 |r|
Show InChI InChI=1S/C15H19N5/c1-19-6-10-8-20(9-11(10)7-19)14(16)15-17-12-4-2-3-5-13(12)18-15/h2-5,10-11,16H,6-9H2,1H3,(H,17,18)/t10-,11+
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6.5n/an/an/an/an/an/an/an/a



Pfizer Inc.

Curated by ChEMBL


Assay Description
Displacement of [3H]histamine from human recombinant histamine H4 receptor expressed in CHO cells coexpressing Ga15 by radioligand filtration binding...


Bioorg Med Chem Lett 22: 1156-9 (2012)


Article DOI: 10.1016/j.bmcl.2011.11.098
BindingDB Entry DOI: 10.7270/Q2Q81DJD
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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6.80n/an/an/an/an/an/an/an/a



Pfizer Inc.

Curated by ChEMBL


Assay Description
Antagonist activity at human histamine H4 receptor expressed in HEK293 cells assessed as rev inhibition of forskolin-stimulated cAMP accumulation by ...


Bioorg Med Chem Lett 22: 1156-9 (2012)


Article DOI: 10.1016/j.bmcl.2011.11.098
BindingDB Entry DOI: 10.7270/Q2Q81DJD
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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PubMed
6.80n/an/an/an/an/an/an/an/a



Pfizer Inc.

Curated by ChEMBL


Assay Description
Antagonist activity at human histamine H4 receptor expressed in HEK293 cells assessed as rev inhibition of forskolin-stimulated cAMP accumulation by ...


Bioorg Med Chem Lett 22: 1156-9 (2012)


Article DOI: 10.1016/j.bmcl.2011.11.098
BindingDB Entry DOI: 10.7270/Q2Q81DJD
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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8n/an/an/an/an/an/an/an/a



Pfizer Inc.

Curated by ChEMBL


Assay Description
Displacement of [3H]histamine from human recombinant histamine H4 receptor expressed in CHO cells coexpressing Ga15 by radioligand filtration binding...


Bioorg Med Chem Lett 22: 1156-9 (2012)


Article DOI: 10.1016/j.bmcl.2011.11.098
BindingDB Entry DOI: 10.7270/Q2Q81DJD
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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8n/an/an/an/an/an/an/an/a



Pfizer Inc.

Curated by ChEMBL


Assay Description
Displacement of [3H]histamine from human recombinant histamine H4 receptor expressed in CHO cells coexpressing Ga15 by radioligand filtration binding...


Bioorg Med Chem Lett 22: 1156-9 (2012)


Article DOI: 10.1016/j.bmcl.2011.11.098
BindingDB Entry DOI: 10.7270/Q2Q81DJD
More data for this
Ligand-Target Pair
Histamine H4 receptor


(Homo sapiens (Human))
BDBM50362216
PNG
(CHEMBL1938977)
Show SMILES CN1C[C@H]2CN(C[C@H]2C1)C(=N)c1nc2ccc(F)cc2[nH]1 |r|
Show InChI InChI=1S/C15H18FN5/c1-20-5-9-7-21(8-10(9)6-20)14(17)15-18-12-3-2-11(16)4-13(12)19-15/h2-4,9-10,17H,5-8H2,1H3,(H,18,19)/t9-,10+
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9.10n/an/an/an/an/an/an/an/a



Pfizer Inc.

Curated by ChEMBL


Assay Description
Antagonist activity at human histamine H4 receptor expressed in HEK293 cells assessed as rev inhibition of forskolin-stimulated cAMP accumulation by ...


Bioorg Med Chem Lett 22: 1156-9 (2012)


Article DOI: 10.1016/j.bmcl.2011.11.098
BindingDB Entry DOI: 10.7270/Q2Q81DJD
More data for this
Ligand-Target Pair
Histamine H4 receptor


(Homo sapiens (Human))
BDBM50362214
PNG
(CHEMBL1938975)
Show SMILES CN1C[C@H]2CN(C[C@H]2C1)C(=N)c1nc2ccc(F)c(C)c2[nH]1 |r|
Show InChI InChI=1S/C16H20FN5/c1-9-12(17)3-4-13-14(9)20-16(19-13)15(18)22-7-10-5-21(2)6-11(10)8-22/h3-4,10-11,18H,5-8H2,1-2H3,(H,19,20)/t10-,11+
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9.30n/an/an/an/an/an/an/an/a



Pfizer Inc.

Curated by ChEMBL


Assay Description
Antagonist activity at human histamine H4 receptor expressed in HEK293 cells assessed as rev inhibition of forskolin-stimulated cAMP accumulation by ...


Bioorg Med Chem Lett 22: 1156-9 (2012)


Article DOI: 10.1016/j.bmcl.2011.11.098
BindingDB Entry DOI: 10.7270/Q2Q81DJD
More data for this
Ligand-Target Pair
Histamine H4 receptor


(Homo sapiens (Human))
BDBM50356888
PNG
(CHEMBL1915348)
Show SMILES CN1C[C@H]2CN(C[C@H]2C1)C(=N)c1nc2cc(F)c(F)cc2[nH]1 |r|
Show InChI InChI=1S/C15H17F2N5/c1-21-4-8-6-22(7-9(8)5-21)14(18)15-19-12-2-10(16)11(17)3-13(12)20-15/h2-3,8-9,18H,4-7H2,1H3,(H,19,20)/t8-,9+
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9.5n/an/an/an/an/an/an/an/a



Pfizer Inc.

Curated by ChEMBL


Assay Description
Displacement of [3H]histamine from human recombinant histamine H4 receptor expressed in CHO cells coexpressing Ga15 by radioligand filtration binding...


Bioorg Med Chem Lett 22: 1156-9 (2012)


Article DOI: 10.1016/j.bmcl.2011.11.098
BindingDB Entry DOI: 10.7270/Q2Q81DJD
More data for this
Ligand-Target Pair
Histamine H4 receptor


(Homo sapiens (Human))
BDBM50362218
PNG
(CHEMBL1938979)
Show SMILES CN1C[C@H]2CN(C[C@H]2C1)C(=N)c1nc2ccccc2[nH]1 |r|
Show InChI InChI=1S/C15H19N5/c1-19-6-10-8-20(9-11(10)7-19)14(16)15-17-12-4-2-3-5-13(12)18-15/h2-5,10-11,16H,6-9H2,1H3,(H,17,18)/t10-,11+
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12.4n/an/an/an/an/an/an/an/a



Pfizer Inc.

Curated by ChEMBL


Assay Description
Antagonist activity at human histamine H4 receptor expressed in HEK293 cells assessed as rev inhibition of forskolin-stimulated cAMP accumulation by ...


Bioorg Med Chem Lett 22: 1156-9 (2012)


Article DOI: 10.1016/j.bmcl.2011.11.098
BindingDB Entry DOI: 10.7270/Q2Q81DJD
More data for this
Ligand-Target Pair
Histamine H4 receptor


(Homo sapiens (Human))
BDBM50356885
PNG
(CHEMBL1915345)
Show SMILES CN1C[C@H]2CN(C[C@H]2C1)C(=O)c1cc2cc(Cl)ccc2[nH]1 |r|
Show InChI InChI=1S/C16H18ClN3O/c1-19-6-11-8-20(9-12(11)7-19)16(21)15-5-10-4-13(17)2-3-14(10)18-15/h2-5,11-12,18H,6-9H2,1H3/t11-,12+
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16n/an/an/an/an/an/an/an/a



Pfizer Inc.

Curated by ChEMBL


Assay Description
Displacement of [3H]histamine from human recombinant histamine H4 receptor expressed in CHO cells coexpressing Ga15 by radioligand filtration binding...


Bioorg Med Chem Lett 22: 1156-9 (2012)


Article DOI: 10.1016/j.bmcl.2011.11.098
BindingDB Entry DOI: 10.7270/Q2Q81DJD
More data for this
Ligand-Target Pair
Histamine H4 receptor


(Homo sapiens (Human))
BDBM50356888
PNG
(CHEMBL1915348)
Show SMILES CN1C[C@H]2CN(C[C@H]2C1)C(=N)c1nc2cc(F)c(F)cc2[nH]1 |r|
Show InChI InChI=1S/C15H17F2N5/c1-21-4-8-6-22(7-9(8)5-21)14(18)15-19-12-2-10(16)11(17)3-13(12)20-15/h2-3,8-9,18H,4-7H2,1H3,(H,19,20)/t8-,9+
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17.2n/an/an/an/an/an/an/an/a



Pfizer Inc.

Curated by ChEMBL


Assay Description
Antagonist activity at human histamine H4 receptor expressed in HEK293 cells assessed as rev inhibition of forskolin-stimulated cAMP accumulation by ...


Bioorg Med Chem Lett 22: 1156-9 (2012)


Article DOI: 10.1016/j.bmcl.2011.11.098
BindingDB Entry DOI: 10.7270/Q2Q81DJD
More data for this
Ligand-Target Pair
Histamine H4 receptor


(Homo sapiens (Human))
BDBM50362217
PNG
(CHEMBL1938978)
Show SMILES CN1C[C@H]2CN(C[C@H]2C1)C(=N)c1nc2c(F)c(F)c(F)cc2[nH]1 |r|
Show InChI InChI=1S/C15H16F3N5/c1-22-3-7-5-23(6-8(7)4-22)14(19)15-20-10-2-9(16)11(17)12(18)13(10)21-15/h2,7-8,19H,3-6H2,1H3,(H,20,21)/t7-,8+
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20n/an/an/an/an/an/an/an/a



Pfizer Inc.

Curated by ChEMBL


Assay Description
Antagonist activity at human histamine H4 receptor expressed in HEK293 cells assessed as rev inhibition of forskolin-stimulated cAMP accumulation by ...


Bioorg Med Chem Lett 22: 1156-9 (2012)


Article DOI: 10.1016/j.bmcl.2011.11.098
BindingDB Entry DOI: 10.7270/Q2Q81DJD
More data for this
Ligand-Target Pair
Histamine H4 receptor


(Homo sapiens (Human))
BDBM50362215
PNG
(CHEMBL1938976)
Show SMILES CN1C[C@H]2CN(C[C@H]2C1)C(=N)c1nc2ccc(F)c(F)c2[nH]1 |r|
Show InChI InChI=1S/C15H17F2N5/c1-21-4-8-6-22(7-9(8)5-21)14(18)15-19-11-3-2-10(16)12(17)13(11)20-15/h2-3,8-9,18H,4-7H2,1H3,(H,19,20)/t8-,9+
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24n/an/an/an/an/an/an/an/a



Pfizer Inc.

Curated by ChEMBL


Assay Description
Antagonist activity at human histamine H4 receptor expressed in HEK293 cells assessed as rev inhibition of forskolin-stimulated cAMP accumulation by ...


Bioorg Med Chem Lett 22: 1156-9 (2012)


Article DOI: 10.1016/j.bmcl.2011.11.098
BindingDB Entry DOI: 10.7270/Q2Q81DJD
More data for this
Ligand-Target Pair
Histamine H4 receptor


(Homo sapiens (Human))
BDBM50362213
PNG
(CHEMBL1938974)
Show SMILES CN1C[C@H]2CN(C[C@H]2C1)C(=N)c1nc2ccc(Cl)cc2[nH]1 |r|
Show InChI InChI=1S/C15H18ClN5/c1-20-5-9-7-21(8-10(9)6-20)14(17)15-18-12-3-2-11(16)4-13(12)19-15/h2-4,9-10,17H,5-8H2,1H3,(H,18,19)/t9-,10+
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26n/an/an/an/an/an/an/an/a



Pfizer Inc.

Curated by ChEMBL


Assay Description
Displacement of [3H]histamine from human recombinant histamine H4 receptor expressed in CHO cells coexpressing Ga15 by radioligand filtration binding...


Bioorg Med Chem Lett 22: 1156-9 (2012)


Article DOI: 10.1016/j.bmcl.2011.11.098
BindingDB Entry DOI: 10.7270/Q2Q81DJD
More data for this
Ligand-Target Pair
Histamine H4 receptor


(Homo sapiens (Human))
BDBM50356885
PNG
(CHEMBL1915345)
Show SMILES CN1C[C@H]2CN(C[C@H]2C1)C(=O)c1cc2cc(Cl)ccc2[nH]1 |r|
Show InChI InChI=1S/C16H18ClN3O/c1-19-6-11-8-20(9-12(11)7-19)16(21)15-5-10-4-13(17)2-3-14(10)18-15/h2-5,11-12,18H,6-9H2,1H3/t11-,12+
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27n/an/an/an/an/an/an/an/a



Pfizer Inc.

Curated by ChEMBL


Assay Description
Antagonist activity at human histamine H4 receptor expressed in HEK293 cells assessed as rev inhibition of forskolin-stimulated cAMP accumulation by ...


Bioorg Med Chem Lett 22: 1156-9 (2012)


Article DOI: 10.1016/j.bmcl.2011.11.098
BindingDB Entry DOI: 10.7270/Q2Q81DJD
More data for this
Ligand-Target Pair
Histamine H4 receptor


(Homo sapiens (Human))
BDBM50179335
PNG
((5-Chloro-1H-benzoimidazol-2-yl)-(4-methyl-piperaz...)
Show SMILES CN1CCN(CC1)C(=O)c1nc2ccc(Cl)cc2[nH]1
Show InChI InChI=1S/C13H15ClN4O/c1-17-4-6-18(7-5-17)13(19)12-15-10-3-2-9(14)8-11(10)16-12/h2-3,8H,4-7H2,1H3,(H,15,16)
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39.6n/an/an/an/an/an/an/an/a



Pfizer Inc.

Curated by ChEMBL


Assay Description
Antagonist activity at human histamine H4 receptor expressed in HEK293 cells assessed as rev inhibition of forskolin-stimulated cAMP accumulation by ...


Bioorg Med Chem Lett 22: 1156-9 (2012)


Article DOI: 10.1016/j.bmcl.2011.11.098
BindingDB Entry DOI: 10.7270/Q2Q81DJD
More data for this
Ligand-Target Pair
Histamine H4 receptor


(Homo sapiens (Human))
BDBM50179335
PNG
((5-Chloro-1H-benzoimidazol-2-yl)-(4-methyl-piperaz...)
Show SMILES CN1CCN(CC1)C(=O)c1nc2ccc(Cl)cc2[nH]1
Show InChI InChI=1S/C13H15ClN4O/c1-17-4-6-18(7-5-17)13(19)12-15-10-3-2-9(14)8-11(10)16-12/h2-3,8H,4-7H2,1H3,(H,15,16)
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47.7n/an/an/an/an/an/an/an/a



Pfizer Inc.

Curated by ChEMBL


Assay Description
Displacement of [3H]histamine from human recombinant histamine H4 receptor expressed in CHO cells coexpressing Ga15 by radioligand filtration binding...


Bioorg Med Chem Lett 22: 1156-9 (2012)


Article DOI: 10.1016/j.bmcl.2011.11.098
BindingDB Entry DOI: 10.7270/Q2Q81DJD
More data for this
Ligand-Target Pair
Histamine H4 receptor


(Homo sapiens (Human))
BDBM50362215
PNG
(CHEMBL1938976)
Show SMILES CN1C[C@H]2CN(C[C@H]2C1)C(=N)c1nc2ccc(F)c(F)c2[nH]1 |r|
Show InChI InChI=1S/C15H17F2N5/c1-21-4-8-6-22(7-9(8)5-21)14(18)15-19-11-3-2-10(16)12(17)13(11)20-15/h2-3,8-9,18H,4-7H2,1H3,(H,19,20)/t8-,9+
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49n/an/an/an/an/an/an/an/a



Pfizer Inc.

Curated by ChEMBL


Assay Description
Displacement of [3H]histamine from human recombinant histamine H4 receptor expressed in CHO cells coexpressing Ga15 by radioligand filtration binding...


Bioorg Med Chem Lett 22: 1156-9 (2012)


Article DOI: 10.1016/j.bmcl.2011.11.098
BindingDB Entry DOI: 10.7270/Q2Q81DJD
More data for this
Ligand-Target Pair
Histamine H4 receptor


(Homo sapiens (Human))
BDBM50362204
PNG
(CHEMBL1938845)
Show SMILES CN1C[C@H]2CN(C[C@H]2C1)C(=O)c1nc2ccc(F)c(C)c2[nH]1 |r|
Show InChI InChI=1S/C16H19FN4O/c1-9-12(17)3-4-13-14(9)19-15(18-13)16(22)21-7-10-5-20(2)6-11(10)8-21/h3-4,10-11H,5-8H2,1-2H3,(H,18,19)/t10-,11+
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52n/an/an/an/an/an/an/an/a



Pfizer Inc.

Curated by ChEMBL


Assay Description
Displacement of [3H]histamine from human recombinant histamine H4 receptor expressed in CHO cells coexpressing Ga15 by radioligand filtration binding...


Bioorg Med Chem Lett 22: 1156-9 (2012)


Article DOI: 10.1016/j.bmcl.2011.11.098
BindingDB Entry DOI: 10.7270/Q2Q81DJD
More data for this
Ligand-Target Pair
Histamine H4 receptor


(Homo sapiens (Human))
BDBM50362213
PNG
(CHEMBL1938974)
Show SMILES CN1C[C@H]2CN(C[C@H]2C1)C(=N)c1nc2ccc(Cl)cc2[nH]1 |r|
Show InChI InChI=1S/C15H18ClN5/c1-20-5-9-7-21(8-10(9)6-20)14(17)15-18-12-3-2-11(16)4-13(12)19-15/h2-4,9-10,17H,5-8H2,1H3,(H,18,19)/t9-,10+
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56n/an/an/an/an/an/an/an/a



Pfizer Inc.

Curated by ChEMBL


Assay Description
Antagonist activity at human histamine H4 receptor expressed in HEK293 cells assessed as rev inhibition of forskolin-stimulated cAMP accumulation by ...


Bioorg Med Chem Lett 22: 1156-9 (2012)


Article DOI: 10.1016/j.bmcl.2011.11.098
BindingDB Entry DOI: 10.7270/Q2Q81DJD
More data for this
Ligand-Target Pair
Histamine H4 receptor


(Homo sapiens (Human))
BDBM50362217
PNG
(CHEMBL1938978)
Show SMILES CN1C[C@H]2CN(C[C@H]2C1)C(=N)c1nc2c(F)c(F)c(F)cc2[nH]1 |r|
Show InChI InChI=1S/C15H16F3N5/c1-22-3-7-5-23(6-8(7)4-22)14(19)15-20-10-2-9(16)11(17)12(18)13(10)21-15/h2,7-8,19H,3-6H2,1H3,(H,20,21)/t7-,8+
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70n/an/an/an/an/an/an/an/a



Pfizer Inc.

Curated by ChEMBL


Assay Description
Displacement of [3H]histamine from human recombinant histamine H4 receptor expressed in CHO cells coexpressing Ga15 by radioligand filtration binding...


Bioorg Med Chem Lett 22: 1156-9 (2012)


Article DOI: 10.1016/j.bmcl.2011.11.098
BindingDB Entry DOI: 10.7270/Q2Q81DJD
More data for this
Ligand-Target Pair
Histamine H4 receptor


(Homo sapiens (Human))
BDBM50362205
PNG
(CHEMBL1938846)
Show SMILES CN1C[C@H]2CN(C[C@H]2C1)C(=O)c1nc2ccc(F)c(F)c2[nH]1 |r|
Show InChI InChI=1S/C15H16F2N4O/c1-20-4-8-6-21(7-9(8)5-20)15(22)14-18-11-3-2-10(16)12(17)13(11)19-14/h2-3,8-9H,4-7H2,1H3,(H,18,19)/t8-,9+
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74n/an/an/an/an/an/an/an/a



Pfizer Inc.

Curated by ChEMBL


Assay Description
Displacement of [3H]histamine from human recombinant histamine H4 receptor expressed in CHO cells coexpressing Ga15 by radioligand filtration binding...


Bioorg Med Chem Lett 22: 1156-9 (2012)


Article DOI: 10.1016/j.bmcl.2011.11.098
BindingDB Entry DOI: 10.7270/Q2Q81DJD
More data for this
Ligand-Target Pair
Histamine H4 receptor


(Homo sapiens (Human))
BDBM50356886
PNG
(CHEMBL1915346)
Show SMILES CN1C[C@H]2CN(C[C@H]2C1)C(=O)c1nc2ccc(F)cc2[nH]1 |r|
Show InChI InChI=1S/C15H17FN4O/c1-19-5-9-7-20(8-10(9)6-19)15(21)14-17-12-3-2-11(16)4-13(12)18-14/h2-4,9-10H,5-8H2,1H3,(H,17,18)/t9-,10+
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83n/an/an/an/an/an/an/an/a



Pfizer Inc.

Curated by ChEMBL


Assay Description
Displacement of [3H]histamine from human recombinant histamine H4 receptor expressed in CHO cells coexpressing Ga15 by radioligand filtration binding...


Bioorg Med Chem Lett 22: 1156-9 (2012)


Article DOI: 10.1016/j.bmcl.2011.11.098
BindingDB Entry DOI: 10.7270/Q2Q81DJD
More data for this
Ligand-Target Pair
Histamine H4 receptor


(Homo sapiens (Human))
BDBM50362211
PNG
(CHEMBL1938972)
Show SMILES CN1C[C@H]2CN(C[C@H]2C1)C(=O)c1cc2cc(Cl)cnc2[nH]1 |r|
Show InChI InChI=1S/C15H17ClN4O/c1-19-5-10-7-20(8-11(10)6-19)15(21)13-3-9-2-12(16)4-17-14(9)18-13/h2-4,10-11H,5-8H2,1H3,(H,17,18)/t10-,11+
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83n/an/an/an/an/an/an/an/a



Pfizer Inc.

Curated by ChEMBL


Assay Description
Displacement of [3H]histamine from human recombinant histamine H4 receptor expressed in CHO cells coexpressing Ga15 by radioligand filtration binding...


Bioorg Med Chem Lett 22: 1156-9 (2012)


Article DOI: 10.1016/j.bmcl.2011.11.098
BindingDB Entry DOI: 10.7270/Q2Q81DJD
More data for this
Ligand-Target Pair
Histamine H4 receptor


(Homo sapiens (Human))
BDBM50362204
PNG
(CHEMBL1938845)
Show SMILES CN1C[C@H]2CN(C[C@H]2C1)C(=O)c1nc2ccc(F)c(C)c2[nH]1 |r|
Show InChI InChI=1S/C16H19FN4O/c1-9-12(17)3-4-13-14(9)19-15(18-13)16(22)21-7-10-5-20(2)6-11(10)8-21/h3-4,10-11H,5-8H2,1-2H3,(H,18,19)/t10-,11+
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97n/an/an/an/an/an/an/an/a



Pfizer Inc.

Curated by ChEMBL


Assay Description
Antagonist activity at human histamine H4 receptor expressed in HEK293 cells assessed as rev inhibition of forskolin-stimulated cAMP accumulation by ...


Bioorg Med Chem Lett 22: 1156-9 (2012)


Article DOI: 10.1016/j.bmcl.2011.11.098
BindingDB Entry DOI: 10.7270/Q2Q81DJD
More data for this
Ligand-Target Pair
Histamine H4 receptor


(Homo sapiens (Human))
BDBM50362206
PNG
(CHEMBL1938967)
Show SMILES CN1C[C@H]2CN(C[C@H]2C1)C(=O)c1nc2ccccc2[nH]1 |r|
Show InChI InChI=1S/C15H18N4O/c1-18-6-10-8-19(9-11(10)7-18)15(20)14-16-12-4-2-3-5-13(12)17-14/h2-5,10-11H,6-9H2,1H3,(H,16,17)/t10-,11+
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102n/an/an/an/an/an/an/an/a



Pfizer Inc.

Curated by ChEMBL


Assay Description
Displacement of [3H]histamine from human recombinant histamine H4 receptor expressed in CHO cells coexpressing Ga15 by radioligand filtration binding...


Bioorg Med Chem Lett 22: 1156-9 (2012)


Article DOI: 10.1016/j.bmcl.2011.11.098
BindingDB Entry DOI: 10.7270/Q2Q81DJD
More data for this
Ligand-Target Pair
Histamine H4 receptor


(Homo sapiens (Human))
BDBM50356887
PNG
(CHEMBL1915347)
Show SMILES CN1C[C@H]2CN(C[C@H]2C1)C(=O)c1nc2cc(F)c(F)cc2[nH]1 |r|
Show InChI InChI=1S/C15H16F2N4O/c1-20-4-8-6-21(7-9(8)5-20)15(22)14-18-12-2-10(16)11(17)3-13(12)19-14/h2-3,8-9H,4-7H2,1H3,(H,18,19)/t8-,9+
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128n/an/an/an/an/an/an/an/a



Pfizer Inc.

Curated by ChEMBL


Assay Description
Displacement of [3H]histamine from human recombinant histamine H4 receptor expressed in CHO cells coexpressing Ga15 by radioligand filtration binding...


Bioorg Med Chem Lett 22: 1156-9 (2012)


Article DOI: 10.1016/j.bmcl.2011.11.098
BindingDB Entry DOI: 10.7270/Q2Q81DJD
More data for this
Ligand-Target Pair
Histamine H4 receptor


(Homo sapiens (Human))
BDBM50362203
PNG
(CHEMBL1938844)
Show SMILES CN1C[C@H]2CN(C[C@H]2C1)C(=O)c1nc2ccc(Cl)cc2[nH]1 |r|
Show InChI InChI=1S/C15H17ClN4O/c1-19-5-9-7-20(8-10(9)6-19)15(21)14-17-12-3-2-11(16)4-13(12)18-14/h2-4,9-10H,5-8H2,1H3,(H,17,18)/t9-,10+
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129n/an/an/an/an/an/an/an/a



Pfizer Inc.

Curated by ChEMBL


Assay Description
Displacement of [3H]histamine from human recombinant histamine H4 receptor expressed in CHO cells coexpressing Ga15 by radioligand filtration binding...


Bioorg Med Chem Lett 22: 1156-9 (2012)


Article DOI: 10.1016/j.bmcl.2011.11.098
BindingDB Entry DOI: 10.7270/Q2Q81DJD
More data for this
Ligand-Target Pair
Histamine H4 receptor


(Homo sapiens (Human))
BDBM50362205
PNG
(CHEMBL1938846)
Show SMILES CN1C[C@H]2CN(C[C@H]2C1)C(=O)c1nc2ccc(F)c(F)c2[nH]1 |r|
Show InChI InChI=1S/C15H16F2N4O/c1-20-4-8-6-21(7-9(8)5-20)15(22)14-18-11-3-2-10(16)12(17)13(11)19-14/h2-3,8-9H,4-7H2,1H3,(H,18,19)/t8-,9+
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134n/an/an/an/an/an/an/an/a



Pfizer Inc.

Curated by ChEMBL


Assay Description
Antagonist activity at human histamine H4 receptor expressed in HEK293 cells assessed as rev inhibition of forskolin-stimulated cAMP accumulation by ...


Bioorg Med Chem Lett 22: 1156-9 (2012)


Article DOI: 10.1016/j.bmcl.2011.11.098
BindingDB Entry DOI: 10.7270/Q2Q81DJD
More data for this
Ligand-Target Pair
Histamine H4 receptor


(Homo sapiens (Human))
BDBM50356886
PNG
(CHEMBL1915346)
Show SMILES CN1C[C@H]2CN(C[C@H]2C1)C(=O)c1nc2ccc(F)cc2[nH]1 |r|
Show InChI InChI=1S/C15H17FN4O/c1-19-5-9-7-20(8-10(9)6-19)15(21)14-17-12-3-2-11(16)4-13(12)18-14/h2-4,9-10H,5-8H2,1H3,(H,17,18)/t9-,10+
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145n/an/an/an/an/an/an/an/a



Pfizer Inc.

Curated by ChEMBL


Assay Description
Antagonist activity at human histamine H4 receptor expressed in HEK293 cells assessed as rev inhibition of forskolin-stimulated cAMP accumulation by ...


Bioorg Med Chem Lett 22: 1156-9 (2012)


Article DOI: 10.1016/j.bmcl.2011.11.098
BindingDB Entry DOI: 10.7270/Q2Q81DJD
More data for this
Ligand-Target Pair
Histamine H4 receptor


(Homo sapiens (Human))
BDBM50362206
PNG
(CHEMBL1938967)
Show SMILES CN1C[C@H]2CN(C[C@H]2C1)C(=O)c1nc2ccccc2[nH]1 |r|
Show InChI InChI=1S/C15H18N4O/c1-18-6-10-8-19(9-11(10)7-18)15(20)14-16-12-4-2-3-5-13(12)17-14/h2-5,10-11H,6-9H2,1H3,(H,16,17)/t10-,11+
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189n/an/an/an/an/an/an/an/a



Pfizer Inc.

Curated by ChEMBL


Assay Description
Antagonist activity at human histamine H4 receptor expressed in HEK293 cells assessed as rev inhibition of forskolin-stimulated cAMP accumulation by ...


Bioorg Med Chem Lett 22: 1156-9 (2012)


Article DOI: 10.1016/j.bmcl.2011.11.098
BindingDB Entry DOI: 10.7270/Q2Q81DJD
More data for this
Ligand-Target Pair
Histamine H4 receptor


(Homo sapiens (Human))
BDBM50362203
PNG
(CHEMBL1938844)
Show SMILES CN1C[C@H]2CN(C[C@H]2C1)C(=O)c1nc2ccc(Cl)cc2[nH]1 |r|
Show InChI InChI=1S/C15H17ClN4O/c1-19-5-9-7-20(8-10(9)6-19)15(21)14-17-12-3-2-11(16)4-13(12)18-14/h2-4,9-10H,5-8H2,1H3,(H,17,18)/t9-,10+
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218n/an/an/an/an/an/an/an/a



Pfizer Inc.

Curated by ChEMBL


Assay Description
Antagonist activity at human histamine H4 receptor expressed in HEK293 cells assessed as rev inhibition of forskolin-stimulated cAMP accumulation by ...


Bioorg Med Chem Lett 22: 1156-9 (2012)


Article DOI: 10.1016/j.bmcl.2011.11.098
BindingDB Entry DOI: 10.7270/Q2Q81DJD
More data for this
Ligand-Target Pair
Histamine H4 receptor


(Homo sapiens (Human))
BDBM50356887
PNG
(CHEMBL1915347)
Show SMILES CN1C[C@H]2CN(C[C@H]2C1)C(=O)c1nc2cc(F)c(F)cc2[nH]1 |r|
Show InChI InChI=1S/C15H16F2N4O/c1-20-4-8-6-21(7-9(8)5-20)15(22)14-18-12-2-10(16)11(17)3-13(12)19-14/h2-3,8-9H,4-7H2,1H3,(H,18,19)/t8-,9+
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236n/an/an/an/an/an/an/an/a



Pfizer Inc.

Curated by ChEMBL


Assay Description
Antagonist activity at human histamine H4 receptor expressed in HEK293 cells assessed as rev inhibition of forskolin-stimulated cAMP accumulation by ...


Bioorg Med Chem Lett 22: 1156-9 (2012)


Article DOI: 10.1016/j.bmcl.2011.11.098
BindingDB Entry DOI: 10.7270/Q2Q81DJD
More data for this
Ligand-Target Pair
Histamine H4 receptor


(Homo sapiens (Human))
BDBM50362210
PNG
(CHEMBL1938971)
Show SMILES CN1C[C@H]2CN(C[C@H]2C1)C(=O)c1cc2cccnc2[nH]1 |r|
Show InChI InChI=1S/C15H18N4O/c1-18-6-11-8-19(9-12(11)7-18)15(20)13-5-10-3-2-4-16-14(10)17-13/h2-5,11-12H,6-9H2,1H3,(H,16,17)/t11-,12+
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973n/an/an/an/an/an/an/an/a



Pfizer Inc.

Curated by ChEMBL


Assay Description
Displacement of [3H]histamine from human recombinant histamine H4 receptor expressed in CHO cells coexpressing Ga15 by radioligand filtration binding...


Bioorg Med Chem Lett 22: 1156-9 (2012)


Article DOI: 10.1016/j.bmcl.2011.11.098
BindingDB Entry DOI: 10.7270/Q2Q81DJD
More data for this
Ligand-Target Pair
Histamine H3 receptor


(Homo sapiens (Human))
BDBM50362216
PNG
(CHEMBL1938977)
Show SMILES CN1C[C@H]2CN(C[C@H]2C1)C(=N)c1nc2ccc(F)cc2[nH]1 |r|
Show InChI InChI=1S/C15H18FN5/c1-20-5-9-7-21(8-10(9)6-20)14(17)15-18-12-3-2-11(16)4-13(12)19-15/h2-4,9-10,17H,5-8H2,1H3,(H,18,19)/t9-,10+
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1.19E+3n/an/an/an/an/an/an/an/a



Pfizer Inc.

Curated by ChEMBL


Assay Description
Binding affinity to human histamine H3 receptor


Bioorg Med Chem Lett 22: 1156-9 (2012)


Article DOI: 10.1016/j.bmcl.2011.11.098
BindingDB Entry DOI: 10.7270/Q2Q81DJD
More data for this
Ligand-Target Pair
Histamine H4 receptor


(Homo sapiens (Human))
BDBM50362207
PNG
(CHEMBL1938968)
Show SMILES CCN1C[C@H]2CN(C[C@H]2C1)C(=O)c1nc2ccc(Cl)cc2[nH]1 |r|
Show InChI InChI=1S/C16H19ClN4O/c1-2-20-6-10-8-21(9-11(10)7-20)16(22)15-18-13-4-3-12(17)5-14(13)19-15/h3-5,10-11H,2,6-9H2,1H3,(H,18,19)/t10-,11+
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1.96E+3n/an/an/an/an/an/an/an/a



Pfizer Inc.

Curated by ChEMBL


Assay Description
Displacement of [3H]histamine from human recombinant histamine H4 receptor expressed in CHO cells coexpressing Ga15 by radioligand filtration binding...


Bioorg Med Chem Lett 22: 1156-9 (2012)


Article DOI: 10.1016/j.bmcl.2011.11.098
BindingDB Entry DOI: 10.7270/Q2Q81DJD
More data for this
Ligand-Target Pair
Histamine H4 receptor


(Homo sapiens (Human))
BDBM50362212
PNG
(CHEMBL1938973)
Show SMILES CN1C[C@H]2CN(C[C@H]2C1)C(=O)c1cc2ccc(Cl)nc2[nH]1 |r|
Show InChI InChI=1S/C15H17ClN4O/c1-19-5-10-7-20(8-11(10)6-19)15(21)12-4-9-2-3-13(16)18-14(9)17-12/h2-4,10-11H,5-8H2,1H3,(H,17,18)/t10-,11+
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2.09E+3n/an/an/an/an/an/an/an/a



Pfizer Inc.

Curated by ChEMBL


Assay Description
Displacement of [3H]histamine from human recombinant histamine H4 receptor expressed in CHO cells coexpressing Ga15 by radioligand filtration binding...


Bioorg Med Chem Lett 22: 1156-9 (2012)


Article DOI: 10.1016/j.bmcl.2011.11.098
BindingDB Entry DOI: 10.7270/Q2Q81DJD
More data for this
Ligand-Target Pair
Histamine H4 receptor


(Homo sapiens (Human))
BDBM50362208
PNG
(CHEMBL1938969)
Show SMILES CC(C)N1C[C@H]2CN(C[C@H]2C1)C(=O)c1nc2ccc(Cl)cc2[nH]1 |r|
Show InChI InChI=1S/C17H21ClN4O/c1-10(2)21-6-11-8-22(9-12(11)7-21)17(23)16-19-14-4-3-13(18)5-15(14)20-16/h3-5,10-12H,6-9H2,1-2H3,(H,19,20)/t11-,12+
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2.67E+3n/an/an/an/an/an/an/an/a



Pfizer Inc.

Curated by ChEMBL


Assay Description
Displacement of [3H]histamine from human recombinant histamine H4 receptor expressed in CHO cells coexpressing Ga15 by radioligand filtration binding...


Bioorg Med Chem Lett 22: 1156-9 (2012)


Article DOI: 10.1016/j.bmcl.2011.11.098
BindingDB Entry DOI: 10.7270/Q2Q81DJD
More data for this
Ligand-Target Pair
Histamine H3 receptor


(Homo sapiens (Human))
BDBM50356888
PNG
(CHEMBL1915348)
Show SMILES CN1C[C@H]2CN(C[C@H]2C1)C(=N)c1nc2cc(F)c(F)cc2[nH]1 |r|
Show InChI InChI=1S/C15H17F2N5/c1-21-4-8-6-22(7-9(8)5-21)14(18)15-19-12-2-10(16)11(17)3-13(12)20-15/h2-3,8-9,18H,4-7H2,1H3,(H,19,20)/t8-,9+
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3.09E+3n/an/an/an/an/an/an/an/a



Pfizer Inc.

Curated by ChEMBL


Assay Description
Binding affinity to human histamine H3 receptor


Bioorg Med Chem Lett 22: 1156-9 (2012)


Article DOI: 10.1016/j.bmcl.2011.11.098
BindingDB Entry DOI: 10.7270/Q2Q81DJD
More data for this
Ligand-Target Pair
Histamine H4 receptor


(Homo sapiens (Human))
BDBM50362202
PNG
(CHEMBL1938843)
Show SMILES CN1CCN(CC1)C(=O)c1cc2cccnc2[nH]1
Show InChI InChI=1S/C13H16N4O/c1-16-5-7-17(8-6-16)13(18)11-9-10-3-2-4-14-12(10)15-11/h2-4,9H,5-8H2,1H3,(H,14,15)
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3.10E+3n/an/an/an/an/an/an/an/a



Pfizer Inc.

Curated by ChEMBL


Assay Description
Displacement of [3H]histamine from human recombinant histamine H4 receptor expressed in CHO cells coexpressing Ga15 by radioligand filtration binding...


Bioorg Med Chem Lett 22: 1156-9 (2012)


Article DOI: 10.1016/j.bmcl.2011.11.098
BindingDB Entry DOI: 10.7270/Q2Q81DJD
More data for this
Ligand-Target Pair
Histamine H4 receptor


(Homo sapiens (Human))
BDBM50362201
PNG
(CHEMBL1938842)
Show SMILES CN1CCN(CC1)C(=O)c1cn2cc(Cl)ccc2n1
Show InChI InChI=1S/C13H15ClN4O/c1-16-4-6-17(7-5-16)13(19)11-9-18-8-10(14)2-3-12(18)15-11/h2-3,8-9H,4-7H2,1H3
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3.17E+3n/an/an/an/an/an/an/an/a



Pfizer Inc.

Curated by ChEMBL


Assay Description
Displacement of [3H]histamine from human recombinant histamine H4 receptor expressed in CHO cells coexpressing Ga15 by radioligand filtration binding...


Bioorg Med Chem Lett 22: 1156-9 (2012)


Article DOI: 10.1016/j.bmcl.2011.11.098
BindingDB Entry DOI: 10.7270/Q2Q81DJD
More data for this
Ligand-Target Pair
Histamine H4 receptor


(Homo sapiens (Human))
BDBM50362207
PNG
(CHEMBL1938968)
Show SMILES CCN1C[C@H]2CN(C[C@H]2C1)C(=O)c1nc2ccc(Cl)cc2[nH]1 |r|
Show InChI InChI=1S/C16H19ClN4O/c1-2-20-6-10-8-21(9-11(10)7-20)16(22)15-18-13-4-3-12(17)5-14(13)19-15/h3-5,10-11H,2,6-9H2,1H3,(H,18,19)/t10-,11+
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3.30E+3n/an/an/an/an/an/an/an/a



Pfizer Inc.

Curated by ChEMBL


Assay Description
Antagonist activity at human histamine H4 receptor expressed in HEK293 cells assessed as rev inhibition of forskolin-stimulated cAMP accumulation by ...


Bioorg Med Chem Lett 22: 1156-9 (2012)


Article DOI: 10.1016/j.bmcl.2011.11.098
BindingDB Entry DOI: 10.7270/Q2Q81DJD
More data for this
Ligand-Target Pair
Histamine H3 receptor


(Homo sapiens (Human))
BDBM50362218
PNG
(CHEMBL1938979)
Show SMILES CN1C[C@H]2CN(C[C@H]2C1)C(=N)c1nc2ccccc2[nH]1 |r|
Show InChI InChI=1S/C15H19N5/c1-19-6-10-8-20(9-11(10)7-19)14(16)15-17-12-4-2-3-5-13(12)18-15/h2-5,10-11,16H,6-9H2,1H3,(H,17,18)/t10-,11+
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3.81E+3n/an/an/an/an/an/an/an/a



Pfizer Inc.

Curated by ChEMBL


Assay Description
Binding affinity to human histamine H3 receptor


Bioorg Med Chem Lett 22: 1156-9 (2012)


Article DOI: 10.1016/j.bmcl.2011.11.098
BindingDB Entry DOI: 10.7270/Q2Q81DJD
More data for this
Ligand-Target Pair
Histamine H4 receptor


(Homo sapiens (Human))
BDBM50362208
PNG
(CHEMBL1938969)
Show SMILES CC(C)N1C[C@H]2CN(C[C@H]2C1)C(=O)c1nc2ccc(Cl)cc2[nH]1 |r|
Show InChI InChI=1S/C17H21ClN4O/c1-10(2)21-6-11-8-22(9-12(11)7-21)17(23)16-19-14-4-3-13(18)5-15(14)20-16/h3-5,10-12H,6-9H2,1-2H3,(H,19,20)/t11-,12+
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4.49E+3n/an/an/an/an/an/an/an/a



Pfizer Inc.

Curated by ChEMBL


Assay Description
Antagonist activity at human histamine H4 receptor expressed in HEK293 cells assessed as rev inhibition of forskolin-stimulated cAMP accumulation by ...


Bioorg Med Chem Lett 22: 1156-9 (2012)


Article DOI: 10.1016/j.bmcl.2011.11.098
BindingDB Entry DOI: 10.7270/Q2Q81DJD
More data for this
Ligand-Target Pair
Histamine H4 receptor


(Homo sapiens (Human))
BDBM50362209
PNG
(CHEMBL1938970)
Show SMILES Clc1ccc2nc([nH]c2c1)C(=O)N1C[C@@H]2CNC[C@@H]2C1 |r|
Show InChI InChI=1S/C14H15ClN4O/c15-10-1-2-11-12(3-10)18-13(17-11)14(20)19-6-8-4-16-5-9(8)7-19/h1-3,8-9,16H,4-7H2,(H,17,18)/t8-,9+
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5.08E+3n/an/an/an/an/an/an/an/a



Pfizer Inc.

Curated by ChEMBL


Assay Description
Displacement of [3H]histamine from human recombinant histamine H4 receptor expressed in CHO cells coexpressing Ga15 by radioligand filtration binding...


Bioorg Med Chem Lett 22: 1156-9 (2012)


Article DOI: 10.1016/j.bmcl.2011.11.098
BindingDB Entry DOI: 10.7270/Q2Q81DJD
More data for this
Ligand-Target Pair
Histamine H4 receptor


(Homo sapiens (Human))
BDBM50362209
PNG
(CHEMBL1938970)
Show SMILES Clc1ccc2nc([nH]c2c1)C(=O)N1C[C@@H]2CNC[C@@H]2C1 |r|
Show InChI InChI=1S/C14H15ClN4O/c15-10-1-2-11-12(3-10)18-13(17-11)14(20)19-6-8-4-16-5-9(8)7-19/h1-3,8-9,16H,4-7H2,(H,17,18)/t8-,9+
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8.18E+3n/an/an/an/an/an/an/an/a



Pfizer Inc.

Curated by ChEMBL


Assay Description
Antagonist activity at human histamine H4 receptor expressed in HEK293 cells assessed as rev inhibition of forskolin-stimulated cAMP accumulation by ...


Bioorg Med Chem Lett 22: 1156-9 (2012)


Article DOI: 10.1016/j.bmcl.2011.11.098
BindingDB Entry DOI: 10.7270/Q2Q81DJD
More data for this
Ligand-Target Pair
Histamine H3 receptor


(Homo sapiens (Human))
BDBM50356885
PNG
(CHEMBL1915345)
Show SMILES CN1C[C@H]2CN(C[C@H]2C1)C(=O)c1cc2cc(Cl)ccc2[nH]1 |r|
Show InChI InChI=1S/C16H18ClN3O/c1-19-6-11-8-20(9-12(11)7-19)16(21)15-5-10-4-13(17)2-3-14(10)18-15/h2-5,11-12,18H,6-9H2,1H3/t11-,12+
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8.75E+3n/an/an/an/an/an/an/an/a



Pfizer Inc.

Curated by ChEMBL


Assay Description
Binding affinity to human histamine H3 receptor


Bioorg Med Chem Lett 22: 1156-9 (2012)


Article DOI: 10.1016/j.bmcl.2011.11.098
BindingDB Entry DOI: 10.7270/Q2Q81DJD
More data for this
Ligand-Target Pair
Histamine H4 receptor


(Homo sapiens (Human))
BDBM50362201
PNG
(CHEMBL1938842)
Show SMILES CN1CCN(CC1)C(=O)c1cn2cc(Cl)ccc2n1
Show InChI InChI=1S/C13H15ClN4O/c1-16-4-6-17(7-5-16)13(19)11-9-18-8-10(14)2-3-12(18)15-11/h2-3,8-9H,4-7H2,1H3
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>1.14E+4n/an/an/an/an/an/an/an/a



Pfizer Inc.

Curated by ChEMBL


Assay Description
Antagonist activity at human histamine H4 receptor expressed in HEK293 cells assessed as rev inhibition of forskolin-stimulated cAMP accumulation by ...


Bioorg Med Chem Lett 22: 1156-9 (2012)


Article DOI: 10.1016/j.bmcl.2011.11.098
BindingDB Entry DOI: 10.7270/Q2Q81DJD
More data for this
Ligand-Target Pair
Histamine H3 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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1.53E+4n/an/an/an/an/an/an/an/a



Pfizer Inc.

Curated by ChEMBL


Assay Description
Binding affinity to human histamine H3 receptor


Bioorg Med Chem Lett 22: 1156-9 (2012)


Article DOI: 10.1016/j.bmcl.2011.11.098
BindingDB Entry DOI: 10.7270/Q2Q81DJD
More data for this
Ligand-Target Pair
Histamine H3 receptor


(Homo sapiens (Human))
BDBM50356886
PNG
(CHEMBL1915346)
Show SMILES CN1C[C@H]2CN(C[C@H]2C1)C(=O)c1nc2ccc(F)cc2[nH]1 |r|
Show InChI InChI=1S/C15H17FN4O/c1-19-5-9-7-20(8-10(9)6-19)15(21)14-17-12-3-2-11(16)4-13(12)18-14/h2-4,9-10H,5-8H2,1H3,(H,17,18)/t9-,10+
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1.55E+4n/an/an/an/an/an/an/an/a



Pfizer Inc.

Curated by ChEMBL


Assay Description
Binding affinity to human histamine H3 receptor


Bioorg Med Chem Lett 22: 1156-9 (2012)


Article DOI: 10.1016/j.bmcl.2011.11.098
BindingDB Entry DOI: 10.7270/Q2Q81DJD
More data for this
Ligand-Target Pair
Histamine H3 receptor


(Homo sapiens (Human))
BDBM50356887
PNG
(CHEMBL1915347)
Show SMILES CN1C[C@H]2CN(C[C@H]2C1)C(=O)c1nc2cc(F)c(F)cc2[nH]1 |r|
Show InChI InChI=1S/C15H16F2N4O/c1-20-4-8-6-21(7-9(8)5-20)15(22)14-18-12-2-10(16)11(17)3-13(12)19-14/h2-3,8-9H,4-7H2,1H3,(H,18,19)/t8-,9+
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1.79E+4n/an/an/an/an/an/an/an/a



Pfizer Inc.

Curated by ChEMBL


Assay Description
Binding affinity to human histamine H3 receptor


Bioorg Med Chem Lett 22: 1156-9 (2012)


Article DOI: 10.1016/j.bmcl.2011.11.098
BindingDB Entry DOI: 10.7270/Q2Q81DJD
More data for this
Ligand-Target Pair
Histamine H3 receptor


(Homo sapiens (Human))
BDBM50179335
PNG
((5-Chloro-1H-benzoimidazol-2-yl)-(4-methyl-piperaz...)
Show SMILES CN1CCN(CC1)C(=O)c1nc2ccc(Cl)cc2[nH]1
Show InChI InChI=1S/C13H15ClN4O/c1-17-4-6-18(7-5-17)13(19)12-15-10-3-2-9(14)8-11(10)16-12/h2-3,8H,4-7H2,1H3,(H,15,16)
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2.00E+4n/an/an/an/an/an/an/an/a



Pfizer Inc.

Curated by ChEMBL


Assay Description
Binding affinity to human histamine H3 receptor


Bioorg Med Chem Lett 22: 1156-9 (2012)


Article DOI: 10.1016/j.bmcl.2011.11.098
BindingDB Entry DOI: 10.7270/Q2Q81DJD
More data for this
Ligand-Target Pair
Histamine H4 receptor


(Homo sapiens (Human))
BDBM50362200
PNG
(CHEMBL1938841)
Show SMILES CN1CCN(CC1)C(=O)c1cn2ccncc2n1
Show InChI InChI=1S/C12H15N5O/c1-15-4-6-16(7-5-15)12(18)10-9-17-3-2-13-8-11(17)14-10/h2-3,8-9H,4-7H2,1H3
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>2.00E+4n/an/an/an/an/an/an/an/a



Pfizer Inc.

Curated by ChEMBL


Assay Description
Antagonist activity at human histamine H4 receptor expressed in HEK293 cells assessed as rev inhibition of forskolin-stimulated cAMP accumulation by ...


Bioorg Med Chem Lett 22: 1156-9 (2012)


Article DOI: 10.1016/j.bmcl.2011.11.098
BindingDB Entry DOI: 10.7270/Q2Q81DJD
More data for this
Ligand-Target Pair
Histamine H3 receptor


(Homo sapiens (Human))
BDBM50362217
PNG
(CHEMBL1938978)
Show SMILES CN1C[C@H]2CN(C[C@H]2C1)C(=N)c1nc2c(F)c(F)c(F)cc2[nH]1 |r|
Show InChI InChI=1S/C15H16F3N5/c1-22-3-7-5-23(6-8(7)4-22)14(19)15-20-10-2-9(16)11(17)12(18)13(10)21-15/h2,7-8,19H,3-6H2,1H3,(H,20,21)/t7-,8+
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>2.00E+4n/an/an/an/an/an/an/an/a



Pfizer Inc.

Curated by ChEMBL


Assay Description
Binding affinity to human histamine H3 receptor


Bioorg Med Chem Lett 22: 1156-9 (2012)


Article DOI: 10.1016/j.bmcl.2011.11.098
BindingDB Entry DOI: 10.7270/Q2Q81DJD
More data for this
Ligand-Target Pair
Histamine H3 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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>2.00E+4n/an/an/an/an/an/an/an/a



Pfizer Inc.

Curated by ChEMBL


Assay Description
Binding affinity to human histamine H3 receptor


Bioorg Med Chem Lett 22: 1156-9 (2012)


Article DOI: 10.1016/j.bmcl.2011.11.098
BindingDB Entry DOI: 10.7270/Q2Q81DJD
More data for this
Ligand-Target Pair
Histamine H4 receptor


(Homo sapiens (Human))
BDBM50362200
PNG
(CHEMBL1938841)
Show SMILES CN1CCN(CC1)C(=O)c1cn2ccncc2n1
Show InChI InChI=1S/C12H15N5O/c1-15-4-6-16(7-5-15)12(18)10-9-17-3-2-13-8-11(17)14-10/h2-3,8-9H,4-7H2,1H3
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2.01E+4n/an/an/an/an/an/an/an/a



Pfizer Inc.

Curated by ChEMBL


Assay Description
Displacement of [3H]histamine from human recombinant histamine H4 receptor expressed in CHO cells coexpressing Ga15 by radioligand filtration binding...


Bioorg Med Chem Lett 22: 1156-9 (2012)


Article DOI: 10.1016/j.bmcl.2011.11.098
BindingDB Entry DOI: 10.7270/Q2Q81DJD
More data for this
Ligand-Target Pair
Histamine H3 receptor


(Homo sapiens (Human))
BDBM50362201
PNG
(CHEMBL1938842)
Show SMILES CN1CCN(CC1)C(=O)c1cn2cc(Cl)ccc2n1
Show InChI InChI=1S/C13H15ClN4O/c1-16-4-6-17(7-5-16)13(19)11-9-18-8-10(14)2-3-12(18)15-11/h2-3,8-9H,4-7H2,1H3
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2.86E+4n/an/an/an/an/an/an/an/a



Pfizer Inc.

Curated by ChEMBL


Assay Description
Binding affinity to human histamine H3 receptor


Bioorg Med Chem Lett 22: 1156-9 (2012)


Article DOI: 10.1016/j.bmcl.2011.11.098
BindingDB Entry DOI: 10.7270/Q2Q81DJD
More data for this
Ligand-Target Pair
Histamine H4 receptor


(Homo sapiens (Human))
BDBM50362202
PNG
(CHEMBL1938843)
Show SMILES CN1CCN(CC1)C(=O)c1cc2cccnc2[nH]1
Show InChI InChI=1S/C13H16N4O/c1-16-5-7-17(8-6-16)13(18)11-9-10-3-2-4-14-12(10)15-11/h2-4,9H,5-8H2,1H3,(H,14,15)
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>2.99E+4n/an/an/an/an/an/an/an/a



Pfizer Inc.

Curated by ChEMBL


Assay Description
Antagonist activity at human histamine H4 receptor expressed in HEK293 cells assessed as rev inhibition of forskolin-stimulated cAMP accumulation by ...


Bioorg Med Chem Lett 22: 1156-9 (2012)


Article DOI: 10.1016/j.bmcl.2011.11.098
BindingDB Entry DOI: 10.7270/Q2Q81DJD
More data for this
Ligand-Target Pair
Histamine H3 receptor


(Homo sapiens (Human))
BDBM50362202
PNG
(CHEMBL1938843)
Show SMILES CN1CCN(CC1)C(=O)c1cc2cccnc2[nH]1
Show InChI InChI=1S/C13H16N4O/c1-16-5-7-17(8-6-16)13(18)11-9-10-3-2-4-14-12(10)15-11/h2-4,9H,5-8H2,1H3,(H,14,15)
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3.66E+4n/an/an/an/an/an/an/an/a



Pfizer Inc.

Curated by ChEMBL


Assay Description
Binding affinity to human histamine H3 receptor


Bioorg Med Chem Lett 22: 1156-9 (2012)


Article DOI: 10.1016/j.bmcl.2011.11.098
BindingDB Entry DOI: 10.7270/Q2Q81DJD
More data for this
Ligand-Target Pair
* indicates data uncertainty>20%