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Compile Data Set for Download or QSAR

Found 22 hits Enz. Inhib. hit(s) with Target = 'Potassium channel subfamily K member 10'   
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
Potassium channel subfamily K member 10


(Homo sapiens (Human))
BDBM25759
PNG
(CHEMBL723 | Carvedilol | Coreg | Dilatrend | Eucar...)
Show SMILES COc1ccccc1OCCNCC(O)COc1cccc2[nH]c3ccccc3c12
Show InChI InChI=1S/C24H26N2O4/c1-28-21-10-4-5-11-22(21)29-14-13-25-15-17(27)16-30-23-12-6-9-20-24(23)18-7-2-3-8-19(18)26-20/h2-12,17,25-27H,13-16H2,1H3
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n/an/a 7.60E+3n/an/an/an/an/an/a



Universit£ Clermont Auvergne

Curated by ChEMBL


Assay Description
Inhibition of of TREK2 (unknown origin) expressed in HEK293 cells assessed as reduction in channel currents


J Med Chem 59: 5149-57 (2016)


Article DOI: 10.1021/acs.jmedchem.5b00671
BindingDB Entry DOI: 10.7270/Q2319XSS
More data for this
Ligand-Target Pair
Potassium channel subfamily K member 10


(Homo sapiens (Human))
BDBM25759
PNG
(CHEMBL723 | Carvedilol | Coreg | Dilatrend | Eucar...)
Show SMILES COc1ccccc1OCCNCC(O)COc1cccc2[nH]c3ccccc3c12
Show InChI InChI=1S/C24H26N2O4/c1-28-21-10-4-5-11-22(21)29-14-13-25-15-17(27)16-30-23-12-6-9-20-24(23)18-7-2-3-8-19(18)26-20/h2-12,17,25-27H,13-16H2,1H3
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n/an/a 2.40E+4n/an/an/an/an/an/a



Universit£ Clermont Auvergne

Curated by ChEMBL


Assay Description
Inhibition of of TREK2 (unknown origin) expressed in oocytes assessed as reduction in channel currents


J Med Chem 59: 5149-57 (2016)


Article DOI: 10.1021/acs.jmedchem.5b00671
BindingDB Entry DOI: 10.7270/Q2319XSS
More data for this
Ligand-Target Pair
Potassium channel subfamily K member 10


(Rattus norvegicus)
BDBM50174835
PNG
(4'-(4-toluenesulfonamido)-4-hydroxychalcone | 4'-(...)
Show SMILES Cc1ccc(cc1)S(=O)(=O)Nc1ccc(cc1)C(=O)\C=C\c1ccc(O)cc1
Show InChI InChI=1S/C22H19NO4S/c1-16-2-13-21(14-3-16)28(26,27)23-19-9-7-18(8-10-19)22(25)15-6-17-4-11-20(24)12-5-17/h2-15,23-24H,1H3/b15-6+
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n/an/a 6.20E+4n/an/an/an/an/an/a



Gyeongsang National University

Curated by ChEMBL


Assay Description
Inhibition of rat TREK2 channel -mediated current expressed in HEK293 at 60 mV holding potential by patch clamp method


Bioorg Med Chem Lett 20: 4237-9 (2010)


Article DOI: 10.1016/j.bmcl.2010.05.033
BindingDB Entry DOI: 10.7270/Q25Q4ZXM
More data for this
Ligand-Target Pair
Potassium channel subfamily K member 10


(Rattus norvegicus)
BDBM50482294
PNG
(CHEMBL1170811)
Show SMILES COc1ccc(\C=C\C(=O)c2ccc(NS(=O)(=O)c3ccc(C)cc3)cc2)cc1
Show InChI InChI=1S/C23H21NO4S/c1-17-3-14-22(15-4-17)29(26,27)24-20-10-8-19(9-11-20)23(25)16-7-18-5-12-21(28-2)13-6-18/h3-16,24H,1-2H3/b16-7+
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n/an/a 1.00E+5n/an/an/an/an/an/a



Gyeongsang National University

Curated by ChEMBL


Assay Description
Inhibition of rat TREK2 channel -mediated current expressed in HEK293 at 60 mV holding potential by patch clamp method


Bioorg Med Chem Lett 20: 4237-9 (2010)


Article DOI: 10.1016/j.bmcl.2010.05.033
BindingDB Entry DOI: 10.7270/Q25Q4ZXM
More data for this
Ligand-Target Pair
Potassium channel subfamily K member 10


(Rattus norvegicus)
BDBM50482296
PNG
(CHEMBL1169729)
Show SMILES Cc1ccc(cc1)S(=O)(=O)Nc1ccc(cc1)C(=O)\C=C\c1ccccc1
Show InChI InChI=1S/C22H19NO3S/c1-17-7-14-21(15-8-17)27(25,26)23-20-12-10-19(11-13-20)22(24)16-9-18-5-3-2-4-6-18/h2-16,23H,1H3/b16-9+
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n/an/a>1.00E+5n/an/an/an/an/an/a



Gyeongsang National University

Curated by ChEMBL


Assay Description
Inhibition of rat TREK2 channel -mediated current expressed in HEK293 at 60 mV holding potential by patch clamp method


Bioorg Med Chem Lett 20: 4237-9 (2010)


Article DOI: 10.1016/j.bmcl.2010.05.033
BindingDB Entry DOI: 10.7270/Q25Q4ZXM
More data for this
Ligand-Target Pair
Potassium channel subfamily K member 10


(Homo sapiens (Human))
BDBM50546011
PNG
(CHEMBL4741659)
Show SMILES OC(=O)c1cc(sc1NC(=O)c1ccc(SC(F)(F)F)cc1)-c1ccccc1
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n/an/an/an/a>3.00E+4n/an/an/an/a


TBA

Assay Description
Activation of human TREK2 by thallium flux mobilization assay


Citation and Details

Article DOI: 10.1016/j.bmcl.2019.04.048
BindingDB Entry DOI: 10.7270/Q2XS6006
More data for this
Ligand-Target Pair
Potassium channel subfamily K member 10


(Homo sapiens (Human))
BDBM50546001
PNG
(CHEMBL4776102)
Show SMILES OC(=O)c1cc(Cl)ccc1NC(=O)c1ccc(SC(F)(F)F)cc1
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n/an/an/an/a 6.80E+3n/an/an/an/a


TBA

Assay Description
Activation of human TREK2 by thallium flux mobilization assay


Citation and Details

Article DOI: 10.1016/j.bmcl.2019.04.048
BindingDB Entry DOI: 10.7270/Q2XS6006
More data for this
Ligand-Target Pair
Potassium channel subfamily K member 10


(Homo sapiens (Human))
BDBM50546002
PNG
(CHEMBL4747631)
Show SMILES OC(=O)c1ccc(Br)cc1NC(=O)c1ccc(SC(F)(F)F)cc1
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n/an/an/an/a 5.90E+3n/an/an/an/a


TBA

Assay Description
Activation of human TREK2 by thallium flux mobilization assay


Citation and Details

Article DOI: 10.1016/j.bmcl.2019.04.048
BindingDB Entry DOI: 10.7270/Q2XS6006
More data for this
Ligand-Target Pair
Potassium channel subfamily K member 10


(Homo sapiens (Human))
BDBM50546003
PNG
(CHEMBL4759642)
Show SMILES OC(=O)c1cc(Br)ccc1NC(=O)c1ccc(SC(F)(F)F)cc1
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n/an/an/an/a 7.70E+3n/an/an/an/a


TBA

Assay Description
Activation of human TREK2 by thallium flux mobilization assay


Citation and Details

Article DOI: 10.1016/j.bmcl.2019.04.048
BindingDB Entry DOI: 10.7270/Q2XS6006
More data for this
Ligand-Target Pair
Potassium channel subfamily K member 10


(Homo sapiens (Human))
BDBM50546004
PNG
(CHEMBL4759521)
Show SMILES OC(=O)c1cc(Br)c(F)cc1NC(=O)c1ccc(SC(F)(F)F)cc1
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n/an/an/an/a 5.50E+3n/an/an/an/a


TBA

Assay Description
Activation of human TREK2 by thallium flux mobilization assay


Citation and Details

Article DOI: 10.1016/j.bmcl.2019.04.048
BindingDB Entry DOI: 10.7270/Q2XS6006
More data for this
Ligand-Target Pair
Potassium channel subfamily K member 10


(Homo sapiens (Human))
BDBM50546005
PNG
(CHEMBL4758530)
Show SMILES COc1ccc(C(O)=O)c(NC(=O)c2ccc(SC(F)(F)F)cc2)c1
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n/an/an/an/a 2.85E+4n/an/an/an/a


TBA

Assay Description
Activation of human TREK2 by thallium flux mobilization assay


Citation and Details

Article DOI: 10.1016/j.bmcl.2019.04.048
BindingDB Entry DOI: 10.7270/Q2XS6006
More data for this
Ligand-Target Pair
Potassium channel subfamily K member 10


(Homo sapiens (Human))
BDBM50546006
PNG
(CHEMBL4747514)
Show SMILES COc1ccc(NC(=O)c2ccc(SC(F)(F)F)cc2)c(c1)C(O)=O
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n/an/an/an/a>3.00E+4n/an/an/an/a


TBA

Assay Description
Activation of human TREK2 by thallium flux mobilization assay


Citation and Details

Article DOI: 10.1016/j.bmcl.2019.04.048
BindingDB Entry DOI: 10.7270/Q2XS6006
More data for this
Ligand-Target Pair
Potassium channel subfamily K member 10


(Homo sapiens (Human))
BDBM50546007
PNG
(CHEMBL4795261)
Show SMILES OC(=O)c1cc(OC(F)(F)F)ccc1NC(=O)c1ccc(SC(F)(F)F)cc1
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n/an/an/an/a 5.60E+3n/an/an/an/a


TBA

Assay Description
Activation of human TREK2 by thallium flux mobilization assay


Citation and Details

Article DOI: 10.1016/j.bmcl.2019.04.048
BindingDB Entry DOI: 10.7270/Q2XS6006
More data for this
Ligand-Target Pair
Potassium channel subfamily K member 10


(Homo sapiens (Human))
BDBM50546008
PNG
(CHEMBL4784090)
Show SMILES OC(=O)c1cc(ccc1NC(=O)c1ccc(SC(F)(F)F)cc1)[N+]([O-])=O
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n/an/an/an/a 2.65E+4n/an/an/an/a


TBA

Assay Description
Activation of human TREK2 by thallium flux mobilization assay


Citation and Details

Article DOI: 10.1016/j.bmcl.2019.04.048
BindingDB Entry DOI: 10.7270/Q2XS6006
More data for this
Ligand-Target Pair
Potassium channel subfamily K member 10


(Homo sapiens (Human))
BDBM50546009
PNG
(CHEMBL4750436)
Show SMILES OC(=O)c1ccsc1NC(=O)c1ccc(SC(F)(F)F)cc1
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n/an/an/an/a>3.00E+4n/an/an/an/a


TBA

Assay Description
Activation of human TREK2 by thallium flux mobilization assay


Citation and Details

Article DOI: 10.1016/j.bmcl.2019.04.048
BindingDB Entry DOI: 10.7270/Q2XS6006
More data for this
Ligand-Target Pair
Potassium channel subfamily K member 10


(Homo sapiens (Human))
BDBM50546010
PNG
(CHEMBL4750599)
Show SMILES Cc1sc(NC(=O)c2ccc(SC(F)(F)F)cc2)c(C(O)=O)c1C
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n/an/an/an/a<3.60E+3n/an/an/an/a


TBA

Assay Description
Activation of human TREK2 by thallium flux mobilization assay


Citation and Details

Article DOI: 10.1016/j.bmcl.2019.04.048
BindingDB Entry DOI: 10.7270/Q2XS6006
More data for this
Ligand-Target Pair
Potassium channel subfamily K member 10


(Homo sapiens (Human))
BDBM50545999
PNG
(CHEMBL4778307)
Show SMILES OC(=O)c1cc(F)ccc1NC(=O)c1ccc(SC(F)(F)F)cc1
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n/an/an/an/a>3.00E+4n/an/an/an/a


TBA

Assay Description
Activation of human TREK2 by thallium flux mobilization assay


Citation and Details

Article DOI: 10.1016/j.bmcl.2019.04.048
BindingDB Entry DOI: 10.7270/Q2XS6006
More data for this
Ligand-Target Pair
Potassium channel subfamily K member 10


(Homo sapiens (Human))
BDBM50545998
PNG
(CHEMBL4745050)
Show SMILES OC(=O)c1ccccc1NC(=O)c1ccc(SC(F)(F)F)cc1
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n/an/an/an/a 5.00E+3n/an/an/an/a


TBA

Assay Description
Activation of human TREK2 by thallium flux mobilization assay


Citation and Details

Article DOI: 10.1016/j.bmcl.2019.04.048
BindingDB Entry DOI: 10.7270/Q2XS6006
More data for this
Ligand-Target Pair
Potassium channel subfamily K member 10


(Homo sapiens (Human))
BDBM50197060
PNG
(CHEMBL1417584)
Show SMILES C1CCc2c(C1)cccc2Nc1ccccc1-c1nnn[nH]1
Show InChI InChI=1S/C17H17N5/c1-2-8-13-12(6-1)7-5-11-15(13)18-16-10-4-3-9-14(16)17-19-21-22-20-17/h3-5,7,9-11,18H,1-2,6,8H2,(H,19,20,21,22)
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n/an/an/an/a 7.70E+3n/an/an/an/a


TBA

Assay Description
Activation of human TREK2 by thallium flux mobilization assay


Citation and Details

Article DOI: 10.1016/j.bmcl.2019.04.048
BindingDB Entry DOI: 10.7270/Q2XS6006
More data for this
Ligand-Target Pair
Potassium channel subfamily K member 10


(Rattus norvegicus)
BDBM50482295
PNG
(CHEMBL401762)
Show SMILES Cc1ccc(cc1)S(=O)(=O)Oc1ccc(cc1)C(=O)\C=C\c1ccc(O)cc1
Show InChI InChI=1S/C22H18O5S/c1-16-2-13-21(14-3-16)28(25,26)27-20-11-7-18(8-12-20)22(24)15-6-17-4-9-19(23)10-5-17/h2-15,23H,1H3/b15-6+
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n/an/an/an/a 1.67E+5n/an/an/an/a



Gyeongsang National University

Curated by ChEMBL


Assay Description
Activation of rat TREK2 channel -mediated current expressed in HEK293 at 60 mV holding potential by patch clamp method


Bioorg Med Chem Lett 20: 4237-9 (2010)


Article DOI: 10.1016/j.bmcl.2010.05.033
BindingDB Entry DOI: 10.7270/Q25Q4ZXM
More data for this
Ligand-Target Pair
Potassium channel subfamily K member 10


(Homo sapiens (Human))
BDBM50180656
PNG
(CHEMBL3818503)
Show SMILES CC1(C)c2cc(Cl)ccc2N(CCc2nnn[nH]2)c2ccc(Cl)cc12
Show InChI InChI=1S/C18H17Cl2N5/c1-18(2)13-9-11(19)3-5-15(13)25(8-7-17-21-23-24-22-17)16-6-4-12(20)10-14(16)18/h3-6,9-10H,7-8H2,1-2H3,(H,21,22,23,24)
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n/an/an/an/a 3.00E+4n/an/an/an/a



Universit£ Clermont Auvergne

Curated by ChEMBL


Assay Description
Activation of TREK2 (unknown origin) expressed in Xenopus oocytes assessed as increase in channel currents


J Med Chem 59: 5149-57 (2016)


Article DOI: 10.1021/acs.jmedchem.5b00671
BindingDB Entry DOI: 10.7270/Q2319XSS
More data for this
Ligand-Target Pair
Potassium channel subfamily K member 10


(Homo sapiens (Human))
BDBM50546000
PNG
(CHEMBL4780579)
Show SMILES OC(=O)c1ccc(Cl)cc1NC(=O)c1ccc(SC(F)(F)F)cc1
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n/an/an/an/a 7.50E+3n/an/an/an/a


TBA

Assay Description
Activation of human TREK2 by thallium flux mobilization assay


Citation and Details

Article DOI: 10.1016/j.bmcl.2019.04.048
BindingDB Entry DOI: 10.7270/Q2XS6006
More data for this
Ligand-Target Pair