Found 22 hits Enz. Inhib. hit(s) with Target = 'Potassium channel subfamily K member 10' Target/Host (Institution) | Ligand | Target/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 | pH | Temp °C |
Potassium channel subfamily K member 10
(Homo sapiens (Human)) | BDBM25759
(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 | PDB
UniProtKB/SwissProt
GoogleScholar AffyNet
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CHEMBL DrugBank MCE KEGG PC cid PC sid PDB UniChem
Patents
Similars
| Article PubMed
| n/a | n/a | 7.60E+3 | n/a | n/a | n/a | n/a | n/a | n/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
(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 | PDB
UniProtKB/SwissProt
GoogleScholar AffyNet
| Purchase
CHEMBL DrugBank MCE KEGG PC cid PC sid PDB UniChem
Patents
Similars
| Article PubMed
| n/a | n/a | 2.40E+4 | n/a | n/a | n/a | n/a | n/a | n/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
(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+ | PDB
UniProtKB/SwissProt
GoogleScholar AffyNet
| CHEMBL PC cid PC sid UniChem
Patents
Similars
| Article PubMed
| n/a | n/a | 6.20E+4 | n/a | n/a | n/a | n/a | n/a | n/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
(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+ | PDB
UniProtKB/SwissProt
GoogleScholar AffyNet
| PC cid PC sid UniChem
| Article PubMed
| n/a | n/a | 1.00E+5 | n/a | n/a | n/a | n/a | n/a | n/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
(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+ | PDB
UniProtKB/SwissProt
GoogleScholar AffyNet
| PC cid PC sid UniChem
| Article PubMed
| n/a | n/a | >1.00E+5 | n/a | n/a | n/a | n/a | n/a | n/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
(CHEMBL4741659)Show SMILES OC(=O)c1cc(sc1NC(=O)c1ccc(SC(F)(F)F)cc1)-c1ccccc1 | PDB
UniProtKB/SwissProt
GoogleScholar AffyNet
| PC cid PC sid UniChem
| Article PubMed
| n/a | n/a | n/a | n/a | >3.00E+4 | n/a | n/a | n/a | n/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
(CHEMBL4776102)Show SMILES OC(=O)c1cc(Cl)ccc1NC(=O)c1ccc(SC(F)(F)F)cc1 | PDB
UniProtKB/SwissProt
GoogleScholar AffyNet
| PC cid PC sid UniChem
| Article PubMed
| n/a | n/a | n/a | n/a | 6.80E+3 | n/a | n/a | n/a | n/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
(CHEMBL4747631)Show SMILES OC(=O)c1ccc(Br)cc1NC(=O)c1ccc(SC(F)(F)F)cc1 | PDB
UniProtKB/SwissProt
GoogleScholar AffyNet
| PC cid PC sid UniChem
| Article PubMed
| n/a | n/a | n/a | n/a | 5.90E+3 | n/a | n/a | n/a | n/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
(CHEMBL4759642)Show SMILES OC(=O)c1cc(Br)ccc1NC(=O)c1ccc(SC(F)(F)F)cc1 | PDB
UniProtKB/SwissProt
GoogleScholar AffyNet
| PC cid PC sid UniChem
| Article PubMed
| n/a | n/a | n/a | n/a | 7.70E+3 | n/a | n/a | n/a | n/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
(CHEMBL4759521)Show SMILES OC(=O)c1cc(Br)c(F)cc1NC(=O)c1ccc(SC(F)(F)F)cc1 | PDB
UniProtKB/SwissProt
GoogleScholar AffyNet
| PC cid PC sid UniChem
| Article PubMed
| n/a | n/a | n/a | n/a | 5.50E+3 | n/a | n/a | n/a | n/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
(CHEMBL4758530)Show SMILES COc1ccc(C(O)=O)c(NC(=O)c2ccc(SC(F)(F)F)cc2)c1 | PDB
UniProtKB/SwissProt
GoogleScholar AffyNet
| PC cid PC sid UniChem
| Article PubMed
| n/a | n/a | n/a | n/a | 2.85E+4 | n/a | n/a | n/a | n/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
(CHEMBL4747514)Show SMILES COc1ccc(NC(=O)c2ccc(SC(F)(F)F)cc2)c(c1)C(O)=O | PDB
UniProtKB/SwissProt
GoogleScholar AffyNet
| PC cid PC sid UniChem
| Article PubMed
| n/a | n/a | n/a | n/a | >3.00E+4 | n/a | n/a | n/a | n/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
(CHEMBL4795261)Show SMILES OC(=O)c1cc(OC(F)(F)F)ccc1NC(=O)c1ccc(SC(F)(F)F)cc1 | PDB
UniProtKB/SwissProt
GoogleScholar AffyNet
| PC cid PC sid UniChem
| Article PubMed
| n/a | n/a | n/a | n/a | 5.60E+3 | n/a | n/a | n/a | n/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
(CHEMBL4784090)Show SMILES OC(=O)c1cc(ccc1NC(=O)c1ccc(SC(F)(F)F)cc1)[N+]([O-])=O | PDB
UniProtKB/SwissProt
GoogleScholar AffyNet
| PC cid PC sid UniChem
| Article PubMed
| n/a | n/a | n/a | n/a | 2.65E+4 | n/a | n/a | n/a | n/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
(CHEMBL4750436) | PDB
UniProtKB/SwissProt
GoogleScholar AffyNet
| PC cid PC sid UniChem
| Article PubMed
| n/a | n/a | n/a | n/a | >3.00E+4 | n/a | n/a | n/a | n/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
(CHEMBL4750599)Show SMILES Cc1sc(NC(=O)c2ccc(SC(F)(F)F)cc2)c(C(O)=O)c1C | PDB
UniProtKB/SwissProt
GoogleScholar AffyNet
| PC cid PC sid UniChem
| Article PubMed
| n/a | n/a | n/a | n/a | <3.60E+3 | n/a | n/a | n/a | n/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
(CHEMBL4778307) | PDB
UniProtKB/SwissProt
GoogleScholar AffyNet
| PC cid PC sid UniChem
| Article PubMed
| n/a | n/a | n/a | n/a | >3.00E+4 | n/a | n/a | n/a | n/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
(CHEMBL4745050) | PDB
UniProtKB/SwissProt
GoogleScholar AffyNet
| PC cid PC sid UniChem
| Article PubMed
| n/a | n/a | n/a | n/a | 5.00E+3 | n/a | n/a | n/a | n/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
(CHEMBL1417584)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) | PDB
UniProtKB/SwissProt
GoogleScholar AffyNet
| Purchase
CHEMBL MCE PC cid PC sid UniChem
Patents
| Article PubMed
| n/a | n/a | n/a | n/a | 7.70E+3 | n/a | n/a | n/a | n/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
(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+ | PDB
UniProtKB/SwissProt
GoogleScholar AffyNet
| PC cid PC sid UniChem
| Article PubMed
| n/a | n/a | n/a | n/a | 1.67E+5 | n/a | n/a | n/a | n/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
(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) | PDB
UniProtKB/SwissProt
GoogleScholar AffyNet
| Purchase
CHEMBL MCE PC cid PC sid UniChem
Similars
| Article PubMed
| n/a | n/a | n/a | n/a | 3.00E+4 | n/a | n/a | n/a | n/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
(CHEMBL4780579)Show SMILES OC(=O)c1ccc(Cl)cc1NC(=O)c1ccc(SC(F)(F)F)cc1 | PDB
UniProtKB/SwissProt
GoogleScholar AffyNet
| PC cid PC sid UniChem
| Article PubMed
| n/a | n/a | n/a | n/a | 7.50E+3 | n/a | n/a | n/a | n/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 | |