Found 6 hits Enz. Inhib. hit(s) with Target = 'Transient receptor potential cation channel subfamily M member 8' and Ligand = 'BDBM50241426' 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 |
Transient receptor potential cation channel subfamily M member 8
(Rattus norvegicus (Rat)) | BDBM50241426
![PNG](/data/jpeg/tenK5024/BindingDB_50241426.png) (3-(2-hydroxyphenyl)-6-(3-nitrophenyl)-3,4-dihydrop...)Show SMILES Oc1ccccc1N1CC=C(NC1=O)c1cccc(c1)[N+]([O-])=O |c:10| Show InChI InChI=1S/C16H13N3O4/c20-15-7-2-1-6-14(15)18-9-8-13(17-16(18)21)11-4-3-5-12(10-11)19(22)23/h1-8,10,20H,9H2,(H,17,21) | PDB
UniProtKB/SwissProt
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| PDB Article PubMed
| n/a | n/a | 58 | n/a | n/a | n/a | n/a | n/a | n/a |
National Research Council
Curated by ChEMBL
| Assay Description Antagonist activity against rat TRPM8 expressed in HEK293 cells assessed as inhibition of icilin-induced intracellular Ca2+ level pre-treated 5 mins ... |
Bioorg Med Chem Lett 25: 2285-90 (2015)
Article DOI: 10.1016/j.bmcl.2015.04.032 BindingDB Entry DOI: 10.7270/Q2QZ2CP2 |
More data for this Ligand-Target Pair | ![3D 3D](/images/Docked_3d.png) 3D Structure (crystal) |
Transient receptor potential cation channel subfamily M member 8
(Homo sapiens (Human)) | BDBM50241426
![PNG](/data/jpeg/tenK5024/BindingDB_50241426.png) (3-(2-hydroxyphenyl)-6-(3-nitrophenyl)-3,4-dihydrop...)Show SMILES Oc1ccccc1N1CC=C(NC1=O)c1cccc(c1)[N+]([O-])=O |c:10| Show InChI InChI=1S/C16H13N3O4/c20-15-7-2-1-6-14(15)18-9-8-13(17-16(18)21)11-4-3-5-12(10-11)19(22)23/h1-8,10,20H,9H2,(H,17,21) | PDB
KEGG
UniProtKB/SwissProt
DrugBank antibodypedia GoogleScholar AffyNet ![](/images/AffyNet_logo.png)
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| n/a | n/a | n/a | n/a | 300 | n/a | n/a | n/a | n/a |
TBA
| |
Citation and Details
|
More data for this Ligand-Target Pair | ![3D 3D](/images/Docked_3d.png) 3D Structure (crystal) |
Transient receptor potential cation channel subfamily M member 8
(Homo sapiens (Human)) | BDBM50241426
![PNG](/data/jpeg/tenK5024/BindingDB_50241426.png) (3-(2-hydroxyphenyl)-6-(3-nitrophenyl)-3,4-dihydrop...)Show SMILES Oc1ccccc1N1CC=C(NC1=O)c1cccc(c1)[N+]([O-])=O |c:10| Show InChI InChI=1S/C16H13N3O4/c20-15-7-2-1-6-14(15)18-9-8-13(17-16(18)21)11-4-3-5-12(10-11)19(22)23/h1-8,10,20H,9H2,(H,17,21) | PDB
KEGG
UniProtKB/SwissProt
DrugBank antibodypedia GoogleScholar AffyNet ![](/images/AffyNet_logo.png)
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CHEMBL MCE PC cid PC sid PDB UniChem
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Pfizer Inc.
Curated by ChEMBL
| Assay Description Inhibition of human TRPM8 (unknown origin) expressed in HEK293 cells assessed as inhibition of WS12-induced Ca2+ elevation by FLIPR assay |
Bioorg Med Chem Lett 23: 6118-22 (2013)
Article DOI: 10.1016/j.bmcl.2013.09.016 BindingDB Entry DOI: 10.7270/Q2125V4N |
More data for this Ligand-Target Pair | ![3D 3D](/images/Docked_3d.png) 3D Structure (crystal) |
Transient receptor potential cation channel subfamily M member 8
(Homo sapiens (Human)) | BDBM50241426
![PNG](/data/jpeg/tenK5024/BindingDB_50241426.png) (3-(2-hydroxyphenyl)-6-(3-nitrophenyl)-3,4-dihydrop...)Show SMILES Oc1ccccc1N1CC=C(NC1=O)c1cccc(c1)[N+]([O-])=O |c:10| Show InChI InChI=1S/C16H13N3O4/c20-15-7-2-1-6-14(15)18-9-8-13(17-16(18)21)11-4-3-5-12(10-11)19(22)23/h1-8,10,20H,9H2,(H,17,21) | PDB
KEGG
UniProtKB/SwissProt
DrugBank antibodypedia GoogleScholar AffyNet ![](/images/AffyNet_logo.png)
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| n/a | n/a | n/a | n/a | 60 | n/a | n/a | n/a | n/a |
Ferrara University
Curated by ChEMBL
| Assay Description Activation of TRPM8 channel |
J Med Chem 53: 5085-107 (2010)
Article DOI: 10.1021/jm100062h BindingDB Entry DOI: 10.7270/Q2416Z02 |
More data for this Ligand-Target Pair | ![3D 3D](/images/Docked_3d.png) 3D Structure (crystal) |
Transient receptor potential cation channel subfamily M member 8
(Rattus norvegicus (Rat)) | BDBM50241426
![PNG](/data/jpeg/tenK5024/BindingDB_50241426.png) (3-(2-hydroxyphenyl)-6-(3-nitrophenyl)-3,4-dihydrop...)Show SMILES Oc1ccccc1N1CC=C(NC1=O)c1cccc(c1)[N+]([O-])=O |c:10| Show InChI InChI=1S/C16H13N3O4/c20-15-7-2-1-6-14(15)18-9-8-13(17-16(18)21)11-4-3-5-12(10-11)19(22)23/h1-8,10,20H,9H2,(H,17,21) | PDB
UniProtKB/SwissProt
GoogleScholar AffyNet ![](/images/AffyNet_logo.png)
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CHEMBL MCE PC cid PC sid PDB UniChem
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| n/a | n/a | n/a | n/a | 110 | n/a | n/a | n/a | n/a |
National Research Council
Curated by ChEMBL
| Assay Description Agonist activity at rat TRPM8 expressed in HEK293 cells assessed as induction of intracellular Ca2+ level by Fluo-4-AM dye based spectrofluorimetry |
Bioorg Med Chem Lett 25: 2285-90 (2015)
Article DOI: 10.1016/j.bmcl.2015.04.032 BindingDB Entry DOI: 10.7270/Q2QZ2CP2 |
More data for this Ligand-Target Pair | ![3D 3D](/images/Docked_3d.png) 3D Structure (crystal) |
Transient receptor potential cation channel subfamily M member 8
(Rattus norvegicus (Rat)) | BDBM50241426
![PNG](/data/jpeg/tenK5024/BindingDB_50241426.png) (3-(2-hydroxyphenyl)-6-(3-nitrophenyl)-3,4-dihydrop...)Show SMILES Oc1ccccc1N1CC=C(NC1=O)c1cccc(c1)[N+]([O-])=O |c:10| Show InChI InChI=1S/C16H13N3O4/c20-15-7-2-1-6-14(15)18-9-8-13(17-16(18)21)11-4-3-5-12(10-11)19(22)23/h1-8,10,20H,9H2,(H,17,21) | PDB
UniProtKB/SwissProt
GoogleScholar AffyNet ![](/images/AffyNet_logo.png)
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CHEMBL MCE PC cid PC sid PDB UniChem
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| PDB Article PubMed
| n/a | n/a | n/a | n/a | 190 | n/a | n/a | n/a | n/a |
Università di Milano
Curated by ChEMBL
| Assay Description Agonist activity at rat recombinant TRPM8 receptor expressed in HEK293 cells assessed as increase in intracellular calcium concentration by fluorimet... |
Bioorg Med Chem 17: 1636-9 (2009)
Article DOI: 10.1016/j.bmc.2008.12.057 BindingDB Entry DOI: 10.7270/Q28915RH |
More data for this Ligand-Target Pair | ![3D 3D](/images/Docked_3d.png) 3D Structure (crystal) |