Found 41 hits Enz. Inhib. hit(s) with Target = 'Transient receptor potential cation channel subfamily V member 1' and Ligand = 'BDBM20284' 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 V member 1
(Homo sapiens (Human)) | BDBM20284
(CHEMBL391997 | CPZ | Capsazepine | N-[2-(4-chlorop...)Show InChI InChI=1S/C19H21ClN2O2S/c20-16-5-3-13(4-6-16)7-8-21-19(25)22-9-1-2-14-10-17(23)18(24)11-15(14)12-22/h3-6,10-11,23-24H,1-2,7-9,12H2,(H,21,25) | PDB MMDB
Reactome pathway KEGG
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| 120 | n/a | n/a | n/a | n/a | n/a | n/a | n/a | n/a |
Johnson & Johnson Pharmaceutical Research and Development
Curated by ChEMBL
| Assay Description Binding affinity towards human vanilloid receptor subtype 1 expressed in HEK293 cell membrane using [3H]-RTX as radioligand. |
Bioorg Med Chem Lett 14: 3053-6 (2004)
Article DOI: 10.1016/j.bmcl.2004.04.038 BindingDB Entry DOI: 10.7270/Q2FB52D6 |
More data for this Ligand-Target Pair | 3D Structure (crystal) |
Transient receptor potential cation channel subfamily V member 1
(Homo sapiens (Human)) | BDBM20284
(CHEMBL391997 | CPZ | Capsazepine | N-[2-(4-chlorop...)Show InChI InChI=1S/C19H21ClN2O2S/c20-16-5-3-13(4-6-16)7-8-21-19(25)22-9-1-2-14-10-17(23)18(24)11-15(14)12-22/h3-6,10-11,23-24H,1-2,7-9,12H2,(H,21,25) | PDB MMDB
Reactome pathway KEGG
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| 120 | n/a | n/a | n/a | n/a | n/a | n/a | n/a | n/a |
Johnson & Johnson Pharmaceutical Research and Development
Curated by ChEMBL
| Assay Description Binding affinity towards cloned human vanilloid receptor subtype 1 in HEK293 cell membranes using [3H]-RTX as radioligand |
Bioorg Med Chem Lett 14: 531-4 (2003)
BindingDB Entry DOI: 10.7270/Q2VQ323X |
More data for this Ligand-Target Pair | 3D Structure (crystal) |
Transient receptor potential cation channel subfamily V member 1
(Rattus norvegicus (rat)) | BDBM20284
(CHEMBL391997 | CPZ | Capsazepine | N-[2-(4-chlorop...)Show InChI InChI=1S/C19H21ClN2O2S/c20-16-5-3-13(4-6-16)7-8-21-19(25)22-9-1-2-14-10-17(23)18(24)11-15(14)12-22/h3-6,10-11,23-24H,1-2,7-9,12H2,(H,21,25) | PDB MMDB
Reactome pathway KEGG
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| 520 | n/a | n/a | n/a | n/a | n/a | n/a | n/a | n/a |
Seoul National University
Curated by ChEMBL
| Assay Description Antagonist activity at rat TRPV1 expressed in CHO cells assessed as inhibition of calcium uptake |
Bioorg Med Chem Lett 17: 214-9 (2006)
Article DOI: 10.1016/j.bmcl.2006.09.059 BindingDB Entry DOI: 10.7270/Q27D2TSX |
More data for this Ligand-Target Pair | 3D Structure (crystal) |
Transient receptor potential cation channel subfamily V member 1
(Rattus norvegicus (rat)) | BDBM20284
(CHEMBL391997 | CPZ | Capsazepine | N-[2-(4-chlorop...)Show InChI InChI=1S/C19H21ClN2O2S/c20-16-5-3-13(4-6-16)7-8-21-19(25)22-9-1-2-14-10-17(23)18(24)11-15(14)12-22/h3-6,10-11,23-24H,1-2,7-9,12H2,(H,21,25) | PDB MMDB
Reactome pathway KEGG
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| 520 | n/a | n/a | n/a | n/a | n/a | n/a | n/a | n/a |
Seoul National University
Curated by ChEMBL
| Assay Description Inhibition of capsaicin-induced [Ca2+] uptake by Rat Vanilloid receptor 1 (VR1) expressing CHO cells |
J Med Chem 46: 3116-26 (2003)
Article DOI: 10.1021/jm030089u BindingDB Entry DOI: 10.7270/Q2SB4551 |
More data for this Ligand-Target Pair | 3D Structure (crystal) |
Transient receptor potential cation channel subfamily V member 1
(Rattus norvegicus (rat)) | BDBM20284
(CHEMBL391997 | CPZ | Capsazepine | N-[2-(4-chlorop...)Show InChI InChI=1S/C19H21ClN2O2S/c20-16-5-3-13(4-6-16)7-8-21-19(25)22-9-1-2-14-10-17(23)18(24)11-15(14)12-22/h3-6,10-11,23-24H,1-2,7-9,12H2,(H,21,25) | PDB MMDB
Reactome pathway KEGG
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| 520 | n/a | n/a | n/a | n/a | n/a | n/a | n/a | n/a |
Seoul National University
Curated by ChEMBL
| Assay Description Antagonist activity for rat TRPV1 expressed in CHO cells |
Bioorg Med Chem Lett 15: 4136-42 (2005)
Article DOI: 10.1016/j.bmcl.2005.06.009 BindingDB Entry DOI: 10.7270/Q23B5ZN0 |
More data for this Ligand-Target Pair | 3D Structure (crystal) |
Transient receptor potential cation channel subfamily V member 1
(Rattus norvegicus (rat)) | BDBM20284
(CHEMBL391997 | CPZ | Capsazepine | N-[2-(4-chlorop...)Show InChI InChI=1S/C19H21ClN2O2S/c20-16-5-3-13(4-6-16)7-8-21-19(25)22-9-1-2-14-10-17(23)18(24)11-15(14)12-22/h3-6,10-11,23-24H,1-2,7-9,12H2,(H,21,25) | PDB MMDB
Reactome pathway KEGG
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| 520 | n/a | n/a | n/a | n/a | n/a | n/a | n/a | n/a |
Seoul National University
Curated by ChEMBL
| Assay Description Antagonist activity towards rat TRPV1 expressed in CHO cells |
Bioorg Med Chem Lett 15: 4143-50 (2005)
Article DOI: 10.1016/j.bmcl.2005.06.006 BindingDB Entry DOI: 10.7270/Q2JH3KQB |
More data for this Ligand-Target Pair | 3D Structure (crystal) |
Transient receptor potential cation channel subfamily V member 1
(Rattus norvegicus (rat)) | BDBM20284
(CHEMBL391997 | CPZ | Capsazepine | N-[2-(4-chlorop...)Show InChI InChI=1S/C19H21ClN2O2S/c20-16-5-3-13(4-6-16)7-8-21-19(25)22-9-1-2-14-10-17(23)18(24)11-15(14)12-22/h3-6,10-11,23-24H,1-2,7-9,12H2,(H,21,25) | PDB MMDB
Reactome pathway KEGG
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| 1.20E+3 | n/a | n/a | n/a | n/a | n/a | n/a | n/a | n/a |
Institute
Curated by ChEMBL
| Assay Description Displacement of [3H]RTX from Vanilloid receptor in Rat spinal cord membranes |
J Med Chem 39: 3123-31 (1996)
Article DOI: 10.1021/jm960063l BindingDB Entry DOI: 10.7270/Q2VT1SRD |
More data for this Ligand-Target Pair | 3D Structure (crystal) |
Transient receptor potential cation channel subfamily V member 1
(Homo sapiens (Human)) | BDBM20284
(CHEMBL391997 | CPZ | Capsazepine | N-[2-(4-chlorop...)Show InChI InChI=1S/C19H21ClN2O2S/c20-16-5-3-13(4-6-16)7-8-21-19(25)22-9-1-2-14-10-17(23)18(24)11-15(14)12-22/h3-6,10-11,23-24H,1-2,7-9,12H2,(H,21,25) | PDB MMDB
Reactome pathway KEGG
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| 1.29E+3 | -33.6 | n/a | n/a | 282 | n/a | n/a | 7.4 | 25 |
Abbott Laboratories
| Assay Description The hTRPV1-expressing CHO cell membranes were incubated with [3H]A-778317 and test compounds to establish equilibrium. After incubation was terminate... |
J Pharmacol Exp Ther 323: 285-93 (2007)
Article DOI: 10.1124/jpet.107.124305 BindingDB Entry DOI: 10.7270/Q28K77B0 |
More data for this Ligand-Target Pair | 3D Structure (crystal) |
Transient receptor potential cation channel subfamily V member 1
(Rattus norvegicus (rat)) | BDBM20284
(CHEMBL391997 | CPZ | Capsazepine | N-[2-(4-chlorop...)Show InChI InChI=1S/C19H21ClN2O2S/c20-16-5-3-13(4-6-16)7-8-21-19(25)22-9-1-2-14-10-17(23)18(24)11-15(14)12-22/h3-6,10-11,23-24H,1-2,7-9,12H2,(H,21,25) | PDB MMDB
Reactome pathway KEGG
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| 1.30E+3 | n/a | n/a | n/a | n/a | n/a | n/a | n/a | n/a |
Seoul National University
Curated by ChEMBL
| Assay Description Displacement of [3H]RTX from rat TRPV1 expressed in CHO cells |
Bioorg Med Chem Lett 17: 214-9 (2006)
Article DOI: 10.1016/j.bmcl.2006.09.059 BindingDB Entry DOI: 10.7270/Q27D2TSX |
More data for this Ligand-Target Pair | 3D Structure (crystal) |
Transient receptor potential cation channel subfamily V member 1
(Rattus norvegicus (rat)) | BDBM20284
(CHEMBL391997 | CPZ | Capsazepine | N-[2-(4-chlorop...)Show InChI InChI=1S/C19H21ClN2O2S/c20-16-5-3-13(4-6-16)7-8-21-19(25)22-9-1-2-14-10-17(23)18(24)11-15(14)12-22/h3-6,10-11,23-24H,1-2,7-9,12H2,(H,21,25) | PDB MMDB
Reactome pathway KEGG
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| 1.30E+3 | -34.9 | n/a | n/a | 520 | n/a | n/a | 7.4 | 37 |
Seoul National University
| Assay Description Binding assay mixtures were set up and contained [3H] RTX, various concentrations of competing ligands, and rVR1-transfected CHO cells. Nonspecific b... |
J Med Chem 51: 57-67 (2008)
Article DOI: 10.1021/jm701049p BindingDB Entry DOI: 10.7270/Q2222S1N |
More data for this Ligand-Target Pair | 3D Structure (crystal) |
Transient receptor potential cation channel subfamily V member 1
(Rattus norvegicus (rat)) | BDBM20284
(CHEMBL391997 | CPZ | Capsazepine | N-[2-(4-chlorop...)Show InChI InChI=1S/C19H21ClN2O2S/c20-16-5-3-13(4-6-16)7-8-21-19(25)22-9-1-2-14-10-17(23)18(24)11-15(14)12-22/h3-6,10-11,23-24H,1-2,7-9,12H2,(H,21,25) | PDB MMDB
Reactome pathway KEGG
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| 1.30E+3 | -34.9 | n/a | n/a | 520 | n/a | n/a | 7.4 | 37 |
Seoul National University
| Assay Description Binding assay mixtures were set up and contained [3H] RTX, various concentrations of competing ligands, and rVR1-transfected CHO cells. Nonspecific b... |
Bioorg Med Chem 15: 6043-53 (2007)
Article DOI: 10.1016/j.bmc.2007.06.041 BindingDB Entry DOI: 10.7270/Q2X928KS |
More data for this Ligand-Target Pair | 3D Structure (crystal) |
Transient receptor potential cation channel subfamily V member 1
(Rattus norvegicus (rat)) | BDBM20284
(CHEMBL391997 | CPZ | Capsazepine | N-[2-(4-chlorop...)Show InChI InChI=1S/C19H21ClN2O2S/c20-16-5-3-13(4-6-16)7-8-21-19(25)22-9-1-2-14-10-17(23)18(24)11-15(14)12-22/h3-6,10-11,23-24H,1-2,7-9,12H2,(H,21,25) | PDB MMDB
Reactome pathway KEGG
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| 1.30E+3 | n/a | n/a | n/a | n/a | n/a | n/a | n/a | n/a |
Seoul National University
Curated by ChEMBL
| Assay Description In vitro binding affinity towards Rat Vanilloid receptor 1 (VR1) by [3H]-RTX displacement. |
J Med Chem 46: 3116-26 (2003)
Article DOI: 10.1021/jm030089u BindingDB Entry DOI: 10.7270/Q2SB4551 |
More data for this Ligand-Target Pair | 3D Structure (crystal) |
Transient receptor potential cation channel subfamily V member 1
(Rattus norvegicus (rat)) | BDBM20284
(CHEMBL391997 | CPZ | Capsazepine | N-[2-(4-chlorop...)Show InChI InChI=1S/C19H21ClN2O2S/c20-16-5-3-13(4-6-16)7-8-21-19(25)22-9-1-2-14-10-17(23)18(24)11-15(14)12-22/h3-6,10-11,23-24H,1-2,7-9,12H2,(H,21,25) | PDB MMDB
Reactome pathway KEGG
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| 1.30E+3 | n/a | n/a | n/a | n/a | n/a | n/a | n/a | n/a |
Seoul National University
Curated by ChEMBL
| Assay Description In vitro binding affinity for rat TRPV1 expressed in CHO cells using [3H]-RTX |
Bioorg Med Chem Lett 15: 4136-42 (2005)
Article DOI: 10.1016/j.bmcl.2005.06.009 BindingDB Entry DOI: 10.7270/Q23B5ZN0 |
More data for this Ligand-Target Pair | 3D Structure (crystal) |
Transient receptor potential cation channel subfamily V member 1
(Rattus norvegicus (rat)) | BDBM20284
(CHEMBL391997 | CPZ | Capsazepine | N-[2-(4-chlorop...)Show InChI InChI=1S/C19H21ClN2O2S/c20-16-5-3-13(4-6-16)7-8-21-19(25)22-9-1-2-14-10-17(23)18(24)11-15(14)12-22/h3-6,10-11,23-24H,1-2,7-9,12H2,(H,21,25) | PDB MMDB
Reactome pathway KEGG
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| 1.30E+3 | n/a | n/a | n/a | n/a | n/a | n/a | n/a | n/a |
Seoul National University
Curated by ChEMBL
| Assay Description In vitro inhibition of [3H]-RTX binding to rat TRPV1 expressed in CHO cells |
Bioorg Med Chem Lett 15: 4143-50 (2005)
Article DOI: 10.1016/j.bmcl.2005.06.006 BindingDB Entry DOI: 10.7270/Q2JH3KQB |
More data for this Ligand-Target Pair | 3D Structure (crystal) |
Transient receptor potential cation channel subfamily V member 1
(Rattus norvegicus (rat)) | BDBM20284
(CHEMBL391997 | CPZ | Capsazepine | N-[2-(4-chlorop...)Show InChI InChI=1S/C19H21ClN2O2S/c20-16-5-3-13(4-6-16)7-8-21-19(25)22-9-1-2-14-10-17(23)18(24)11-15(14)12-22/h3-6,10-11,23-24H,1-2,7-9,12H2,(H,21,25) | PDB MMDB
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| 4.30E+3 | n/a | n/a | n/a | n/a | n/a | n/a | n/a | n/a |
Merck Sharp and Dohme
Curated by PDSP Ki Database
| |
J Pharmacol Exp Ther 303: 1052-60 (2002)
Article DOI: 10.1124/jpet.102.040394 BindingDB Entry DOI: 10.7270/Q279437S |
More data for this Ligand-Target Pair | 3D Structure (crystal) |
Transient receptor potential cation channel subfamily V member 1
(Rattus norvegicus (rat)) | BDBM20284
(CHEMBL391997 | CPZ | Capsazepine | N-[2-(4-chlorop...)Show InChI InChI=1S/C19H21ClN2O2S/c20-16-5-3-13(4-6-16)7-8-21-19(25)22-9-1-2-14-10-17(23)18(24)11-15(14)12-22/h3-6,10-11,23-24H,1-2,7-9,12H2,(H,21,25) | PDB MMDB
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| n/a | n/a | 4 | n/a | n/a | n/a | n/a | n/a | n/a |
Johnson & Johnson Pharmaceutical Research and Development L.L.C.
Curated by ChEMBL
| Assay Description In vitro inhibition of acid activated rat TRPV1 receptor in [Ca2+] influx assay |
J Med Chem 48: 1857-72 (2005)
Article DOI: 10.1021/jm0495071 BindingDB Entry DOI: 10.7270/Q2KH0MT8 |
More data for this Ligand-Target Pair | 3D Structure (crystal) |
Transient receptor potential cation channel subfamily V member 1
(Homo sapiens (Human)) | BDBM20284
(CHEMBL391997 | CPZ | Capsazepine | N-[2-(4-chlorop...)Show InChI InChI=1S/C19H21ClN2O2S/c20-16-5-3-13(4-6-16)7-8-21-19(25)22-9-1-2-14-10-17(23)18(24)11-15(14)12-22/h3-6,10-11,23-24H,1-2,7-9,12H2,(H,21,25) | PDB MMDB
Reactome pathway KEGG
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| n/a | n/a | 4 | n/a | n/a | n/a | n/a | n/a | n/a |
Johnson & Johnson Pharmaceutical Research and Development L.L.C.
Curated by ChEMBL
| Assay Description In vitro inhibition of anandamide activated human TRPV1 receptor in [Ca2+] influx assay |
J Med Chem 48: 1857-72 (2005)
Article DOI: 10.1021/jm0495071 BindingDB Entry DOI: 10.7270/Q2KH0MT8 |
More data for this Ligand-Target Pair | 3D Structure (crystal) |
Transient receptor potential cation channel subfamily V member 1
(Homo sapiens (Human)) | BDBM20284
(CHEMBL391997 | CPZ | Capsazepine | N-[2-(4-chlorop...)Show InChI InChI=1S/C19H21ClN2O2S/c20-16-5-3-13(4-6-16)7-8-21-19(25)22-9-1-2-14-10-17(23)18(24)11-15(14)12-22/h3-6,10-11,23-24H,1-2,7-9,12H2,(H,21,25) | PDB MMDB
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| n/a | n/a | 4 | n/a | n/a | n/a | n/a | n/a | n/a |
Johnson & Johnson Pharmaceutical Research and Development L.L.C.
Curated by ChEMBL
| Assay Description In vitro inhibition of anandamide activated human TRPV1 receptor in [Ca2+] influx assay |
J Med Chem 48: 1857-72 (2005)
Article DOI: 10.1021/jm0495071 BindingDB Entry DOI: 10.7270/Q2KH0MT8 |
More data for this Ligand-Target Pair | 3D Structure (crystal) |
Transient receptor potential cation channel subfamily V member 1
(Homo sapiens (Human)) | BDBM20284
(CHEMBL391997 | CPZ | Capsazepine | N-[2-(4-chlorop...)Show InChI InChI=1S/C19H21ClN2O2S/c20-16-5-3-13(4-6-16)7-8-21-19(25)22-9-1-2-14-10-17(23)18(24)11-15(14)12-22/h3-6,10-11,23-24H,1-2,7-9,12H2,(H,21,25) | PDB MMDB
Reactome pathway KEGG
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| n/a | n/a | 5 | n/a | n/a | n/a | n/a | n/a | n/a |
Johnson & Johnson Pharmaceutical Research and Development L.L.C.
Curated by ChEMBL
| Assay Description In vitro inhibition of PMA-activated human TRPV1 receptor in [Ca2+] influx assay |
J Med Chem 48: 1857-72 (2005)
Article DOI: 10.1021/jm0495071 BindingDB Entry DOI: 10.7270/Q2KH0MT8 |
More data for this Ligand-Target Pair | 3D Structure (crystal) |
Transient receptor potential cation channel subfamily V member 1
(Homo sapiens (Human)) | BDBM20284
(CHEMBL391997 | CPZ | Capsazepine | N-[2-(4-chlorop...)Show InChI InChI=1S/C19H21ClN2O2S/c20-16-5-3-13(4-6-16)7-8-21-19(25)22-9-1-2-14-10-17(23)18(24)11-15(14)12-22/h3-6,10-11,23-24H,1-2,7-9,12H2,(H,21,25) | PDB MMDB
Reactome pathway KEGG
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| n/a | n/a | 5 | n/a | n/a | n/a | n/a | n/a | n/a |
Johnson & Johnson Pharmaceutical Research and Development L.L.C.
Curated by ChEMBL
| Assay Description In vitro inhibition of PMA-activated human TRPV1 receptor in [Ca2+] influx assay |
J Med Chem 48: 1857-72 (2005)
Article DOI: 10.1021/jm0495071 BindingDB Entry DOI: 10.7270/Q2KH0MT8 |
More data for this Ligand-Target Pair | 3D Structure (crystal) |
Transient receptor potential cation channel subfamily V member 1
(Homo sapiens (Human)) | BDBM20284
(CHEMBL391997 | CPZ | Capsazepine | N-[2-(4-chlorop...)Show InChI InChI=1S/C19H21ClN2O2S/c20-16-5-3-13(4-6-16)7-8-21-19(25)22-9-1-2-14-10-17(23)18(24)11-15(14)12-22/h3-6,10-11,23-24H,1-2,7-9,12H2,(H,21,25) | PDB MMDB
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| n/a | n/a | 39 | n/a | n/a | n/a | n/a | n/a | n/a |
GlaxoSmithKline
Curated by ChEMBL
| Assay Description Antagonist activity at human TRPV1 expressed in CHO cells assessed as blockade of capsaicin-induced receptor activation by aequorin based assay |
J Med Chem 50: 2589-96 (2007)
Article DOI: 10.1021/jm060637e BindingDB Entry DOI: 10.7270/Q269737M |
More data for this Ligand-Target Pair | 3D Structure (crystal) |
Transient receptor potential cation channel subfamily V member 1
(Homo sapiens (Human)) | BDBM20284
(CHEMBL391997 | CPZ | Capsazepine | N-[2-(4-chlorop...)Show InChI InChI=1S/C19H21ClN2O2S/c20-16-5-3-13(4-6-16)7-8-21-19(25)22-9-1-2-14-10-17(23)18(24)11-15(14)12-22/h3-6,10-11,23-24H,1-2,7-9,12H2,(H,21,25) | PDB MMDB
Reactome pathway KEGG
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| PDB Article PubMed
| n/a | n/a | 53 | n/a | n/a | n/a | n/a | n/a | n/a |
GlaxoSmithKline
Curated by ChEMBL
| Assay Description Antagonist activity at human TRPV1 expressed in CHO cells assessed as blockade of capsaicin-induced receptor activation by [45Ca2+] uptake assay |
J Med Chem 50: 2589-96 (2007)
Article DOI: 10.1021/jm060637e BindingDB Entry DOI: 10.7270/Q269737M |
More data for this Ligand-Target Pair | 3D Structure (crystal) |
Transient receptor potential cation channel subfamily V member 1
(Homo sapiens (Human)) | BDBM20284
(CHEMBL391997 | CPZ | Capsazepine | N-[2-(4-chlorop...)Show InChI InChI=1S/C19H21ClN2O2S/c20-16-5-3-13(4-6-16)7-8-21-19(25)22-9-1-2-14-10-17(23)18(24)11-15(14)12-22/h3-6,10-11,23-24H,1-2,7-9,12H2,(H,21,25) | PDB MMDB
Reactome pathway KEGG
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| PDB Article PubMed
| n/a | n/a | 56 | n/a | n/a | n/a | n/a | n/a | n/a |
Farmaceutiche
Curated by ChEMBL
| Assay Description Inhibition of 100 nM capsaicin effect on intracellular [Ca2+] concentration in HEK293 cells expressing human TRPV1 |
J Med Chem 48: 4663-9 (2005)
Article DOI: 10.1021/jm050139q BindingDB Entry DOI: 10.7270/Q2R49Q8H |
More data for this Ligand-Target Pair | 3D Structure (crystal) |
Transient receptor potential cation channel subfamily V member 1
(Rattus norvegicus (rat)) | BDBM20284
(CHEMBL391997 | CPZ | Capsazepine | N-[2-(4-chlorop...)Show InChI InChI=1S/C19H21ClN2O2S/c20-16-5-3-13(4-6-16)7-8-21-19(25)22-9-1-2-14-10-17(23)18(24)11-15(14)12-22/h3-6,10-11,23-24H,1-2,7-9,12H2,(H,21,25) | PDB MMDB
Reactome pathway KEGG
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| n/a | n/a | 58 | n/a | n/a | n/a | n/a | n/a | n/a |
Purdue Pharma L.P.
Curated by ChEMBL
| Assay Description Vanilloid receptor subtype 1 antagonist activity based on its ability to block capsaicin-induced (CAP) activation of the rat VR1 channel in a HEK293 ... |
Bioorg Med Chem Lett 13: 3611-6 (2003)
BindingDB Entry DOI: 10.7270/Q28P5ZW4 |
More data for this Ligand-Target Pair | 3D Structure (crystal) |
Transient receptor potential cation channel subfamily V member 1
(Homo sapiens (Human)) | BDBM20284
(CHEMBL391997 | CPZ | Capsazepine | N-[2-(4-chlorop...)Show InChI InChI=1S/C19H21ClN2O2S/c20-16-5-3-13(4-6-16)7-8-21-19(25)22-9-1-2-14-10-17(23)18(24)11-15(14)12-22/h3-6,10-11,23-24H,1-2,7-9,12H2,(H,21,25) | PDB MMDB
Reactome pathway KEGG
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| n/a | n/a | 68 | n/a | n/a | n/a | n/a | n/a | n/a |
University of Shizuoka
Curated by ChEMBL
| Assay Description Antagonist activity against human TRPV1 expressed in T-REx HEK cells assessed as inhibition of capsaicin-induced increase in intracellular Ca2+ accum... |
J. Nat. Prod. 77: 1831-8 (2014)
Article DOI: 10.1021/np500235b BindingDB Entry DOI: 10.7270/Q27S7QDF |
More data for this Ligand-Target Pair | 3D Structure (crystal) |
Transient receptor potential cation channel subfamily V member 1
(Homo sapiens (Human)) | BDBM20284
(CHEMBL391997 | CPZ | Capsazepine | N-[2-(4-chlorop...)Show InChI InChI=1S/C19H21ClN2O2S/c20-16-5-3-13(4-6-16)7-8-21-19(25)22-9-1-2-14-10-17(23)18(24)11-15(14)12-22/h3-6,10-11,23-24H,1-2,7-9,12H2,(H,21,25) | PDB MMDB
Reactome pathway KEGG
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| n/a | n/a | 69 | n/a | n/a | n/a | n/a | n/a | n/a |
GlaxoSmithKline
Curated by ChEMBL
| Assay Description Antagonist activity at human TRPV1 expressed in CHO cells assessed as blockade of acid-induced receptor activation by [45Ca2+] uptake assay |
J Med Chem 50: 2589-96 (2007)
Article DOI: 10.1021/jm060637e BindingDB Entry DOI: 10.7270/Q269737M |
More data for this Ligand-Target Pair | 3D Structure (crystal) |
Transient receptor potential cation channel subfamily V member 1
(Homo sapiens (Human)) | BDBM20284
(CHEMBL391997 | CPZ | Capsazepine | N-[2-(4-chlorop...)Show InChI InChI=1S/C19H21ClN2O2S/c20-16-5-3-13(4-6-16)7-8-21-19(25)22-9-1-2-14-10-17(23)18(24)11-15(14)12-22/h3-6,10-11,23-24H,1-2,7-9,12H2,(H,21,25) | PDB MMDB
Reactome pathway KEGG
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| n/a | n/a | 74 | n/a | n/a | n/a | n/a | n/a | n/a |
Johnson & Johnson Pharmaceutical Research and Development L.L.C.
Curated by ChEMBL
| Assay Description Inhibition of human transient receptor potential vanilloid 1 receptor (n=5) |
J Med Chem 48: 1857-72 (2005)
Article DOI: 10.1021/jm0495071 BindingDB Entry DOI: 10.7270/Q2KH0MT8 |
More data for this Ligand-Target Pair | 3D Structure (crystal) |
Transient receptor potential cation channel subfamily V member 1
(Homo sapiens (Human)) | BDBM20284
(CHEMBL391997 | CPZ | Capsazepine | N-[2-(4-chlorop...)Show InChI InChI=1S/C19H21ClN2O2S/c20-16-5-3-13(4-6-16)7-8-21-19(25)22-9-1-2-14-10-17(23)18(24)11-15(14)12-22/h3-6,10-11,23-24H,1-2,7-9,12H2,(H,21,25) | PDB MMDB
Reactome pathway KEGG
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| n/a | n/a | 100 | n/a | n/a | n/a | n/a | n/a | n/a |
Johnson & Johnson Pharmaceutical Research and Development
Curated by ChEMBL
| Assay Description Binding affinity towards cloned human vanilloid receptor subtype 1 in HEK293 cell membranes using [3H]-RTX as radioligand |
Bioorg Med Chem Lett 14: 531-4 (2003)
BindingDB Entry DOI: 10.7270/Q2VQ323X |
More data for this Ligand-Target Pair | 3D Structure (crystal) |
Transient receptor potential cation channel subfamily V member 1
(Homo sapiens (Human)) | BDBM20284
(CHEMBL391997 | CPZ | Capsazepine | N-[2-(4-chlorop...)Show InChI InChI=1S/C19H21ClN2O2S/c20-16-5-3-13(4-6-16)7-8-21-19(25)22-9-1-2-14-10-17(23)18(24)11-15(14)12-22/h3-6,10-11,23-24H,1-2,7-9,12H2,(H,21,25) | PDB MMDB
Reactome pathway KEGG
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B.MOAD DrugBank antibodypedia GoogleScholar AffyNet
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| n/a | n/a | 100 | n/a | n/a | n/a | n/a | n/a | n/a |
Johnson & Johnson Pharmaceutical Research and Development
Curated by ChEMBL
| Assay Description Antagonistic activity towards human vanilloid receptor subtype 1 expressed in HEK293 cell membrane, as inhibition of agonist-induced intracellular [C... |
Bioorg Med Chem Lett 14: 3053-6 (2004)
Article DOI: 10.1016/j.bmcl.2004.04.038 BindingDB Entry DOI: 10.7270/Q2FB52D6 |
More data for this Ligand-Target Pair | 3D Structure (crystal) |
Transient receptor potential cation channel subfamily V member 1
(Homo sapiens (Human)) | BDBM20284
(CHEMBL391997 | CPZ | Capsazepine | N-[2-(4-chlorop...)Show InChI InChI=1S/C19H21ClN2O2S/c20-16-5-3-13(4-6-16)7-8-21-19(25)22-9-1-2-14-10-17(23)18(24)11-15(14)12-22/h3-6,10-11,23-24H,1-2,7-9,12H2,(H,21,25) | PDB MMDB
Reactome pathway KEGG
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| n/a | n/a | 150 | n/a | n/a | n/a | n/a | n/a | n/a |
University of Shizuoka
Curated by ChEMBL
| Assay Description Antagonist activity at human brain TRPV1 expressed in HEK293T cells assessed as inhibition of CAP-induced intracellular Ca2+ influx by fluorescence-b... |
J Nat Prod 77: 285-97 (2014)
Article DOI: 10.1021/np400885u BindingDB Entry DOI: 10.7270/Q20P11H1 |
More data for this Ligand-Target Pair | 3D Structure (crystal) |
Transient receptor potential cation channel subfamily V member 1
(Rattus norvegicus (rat)) | BDBM20284
(CHEMBL391997 | CPZ | Capsazepine | N-[2-(4-chlorop...)Show InChI InChI=1S/C19H21ClN2O2S/c20-16-5-3-13(4-6-16)7-8-21-19(25)22-9-1-2-14-10-17(23)18(24)11-15(14)12-22/h3-6,10-11,23-24H,1-2,7-9,12H2,(H,21,25) | PDB MMDB
Reactome pathway KEGG
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| n/a | n/a | 220 | n/a | n/a | n/a | n/a | n/a | n/a |
GlaxoSmithKline
Curated by ChEMBL
| Assay Description Antagonist activity at rat TRPV1 expressed in CHO cells assessed as blockade of capsaicin-induced receptor activation by aequorin based assay |
J Med Chem 50: 2589-96 (2007)
Article DOI: 10.1021/jm060637e BindingDB Entry DOI: 10.7270/Q269737M |
More data for this Ligand-Target Pair | 3D Structure (crystal) |
Transient receptor potential cation channel subfamily V member 1
(Homo sapiens (Human)) | BDBM20284
(CHEMBL391997 | CPZ | Capsazepine | N-[2-(4-chlorop...)Show InChI InChI=1S/C19H21ClN2O2S/c20-16-5-3-13(4-6-16)7-8-21-19(25)22-9-1-2-14-10-17(23)18(24)11-15(14)12-22/h3-6,10-11,23-24H,1-2,7-9,12H2,(H,21,25) | PDB MMDB
Reactome pathway KEGG
UniProtKB/SwissProt
B.MOAD DrugBank antibodypedia GoogleScholar AffyNet
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CHEMBL MCE PC cid PC sid PDB UniChem
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| PDB Article PubMed
| n/a | n/a | 320 | n/a | n/a | n/a | n/a | n/a | n/a |
GlaxoSmithKline
Curated by ChEMBL
| Assay Description Antagonist activity at human TRPV1 expressed in CHO cells assessed as blockade of acid-induced receptor activation by aequorin based assay |
J Med Chem 50: 2589-96 (2007)
Article DOI: 10.1021/jm060637e BindingDB Entry DOI: 10.7270/Q269737M |
More data for this Ligand-Target Pair | 3D Structure (crystal) |
Transient receptor potential cation channel subfamily V member 1
(Homo sapiens (Human)) | BDBM20284
(CHEMBL391997 | CPZ | Capsazepine | N-[2-(4-chlorop...)Show InChI InChI=1S/C19H21ClN2O2S/c20-16-5-3-13(4-6-16)7-8-21-19(25)22-9-1-2-14-10-17(23)18(24)11-15(14)12-22/h3-6,10-11,23-24H,1-2,7-9,12H2,(H,21,25) | PDB MMDB
Reactome pathway KEGG
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| n/a | n/a | 334 | n/a | n/a | n/a | n/a | n/a | n/a |
Novartis Institutes for Biomedical Research
Curated by ChEMBL
| Assay Description Inhibition of calcium influx evoked by capsaicin in human TRPV1 expressing cells by fluorescence assay |
J Med Chem 49: 471-4 (2006)
Article DOI: 10.1021/jm051058x BindingDB Entry DOI: 10.7270/Q2RX9BNT |
More data for this Ligand-Target Pair | 3D Structure (crystal) |
Transient receptor potential cation channel subfamily V member 1
(Rattus norvegicus (rat)) | BDBM20284
(CHEMBL391997 | CPZ | Capsazepine | N-[2-(4-chlorop...)Show InChI InChI=1S/C19H21ClN2O2S/c20-16-5-3-13(4-6-16)7-8-21-19(25)22-9-1-2-14-10-17(23)18(24)11-15(14)12-22/h3-6,10-11,23-24H,1-2,7-9,12H2,(H,21,25) | PDB MMDB
Reactome pathway KEGG
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| n/a | n/a | 365 | n/a | n/a | n/a | n/a | n/a | n/a |
Johnson & Johnson Pharmaceutical Research and Development L.L.C.
Curated by ChEMBL
| Assay Description Inhibition of rat transient receptor potential vanilloid 1 receptor (n=2) |
J Med Chem 48: 1857-72 (2005)
Article DOI: 10.1021/jm0495071 BindingDB Entry DOI: 10.7270/Q2KH0MT8 |
More data for this Ligand-Target Pair | 3D Structure (crystal) |
Transient receptor potential cation channel subfamily V member 1
(Homo sapiens (Human)) | BDBM20284
(CHEMBL391997 | CPZ | Capsazepine | N-[2-(4-chlorop...)Show InChI InChI=1S/C19H21ClN2O2S/c20-16-5-3-13(4-6-16)7-8-21-19(25)22-9-1-2-14-10-17(23)18(24)11-15(14)12-22/h3-6,10-11,23-24H,1-2,7-9,12H2,(H,21,25) | PDB MMDB
Reactome pathway KEGG
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| n/a | n/a | 420 | n/a | n/a | n/a | n/a | n/a | n/a |
Amgen Inc.
Curated by ChEMBL
| Assay Description Inhibition of capsaicin-induced calcium uptake by transient receptor potential vanilloid type 1 expressed in CHO cells |
J Med Chem 48: 71-90 (2005)
Article DOI: 10.1021/jm049485i BindingDB Entry DOI: 10.7270/Q2J67GDG |
More data for this Ligand-Target Pair | 3D Structure (crystal) |
Transient receptor potential cation channel subfamily V member 1
(Rattus norvegicus (rat)) | BDBM20284
(CHEMBL391997 | CPZ | Capsazepine | N-[2-(4-chlorop...)Show InChI InChI=1S/C19H21ClN2O2S/c20-16-5-3-13(4-6-16)7-8-21-19(25)22-9-1-2-14-10-17(23)18(24)11-15(14)12-22/h3-6,10-11,23-24H,1-2,7-9,12H2,(H,21,25) | PDB MMDB
Reactome pathway KEGG
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| n/a | n/a | 887 | n/a | n/a | n/a | n/a | n/a | n/a |
GlaxoSmithKline
Curated by ChEMBL
| Assay Description Antagonist activity at rat TRPV1 expressed in CHO cells assessed as blockade of capsaicin-induced receptor activation by [45Ca2+] uptake assay |
J Med Chem 50: 2589-96 (2007)
Article DOI: 10.1021/jm060637e BindingDB Entry DOI: 10.7270/Q269737M |
More data for this Ligand-Target Pair | 3D Structure (crystal) |
Transient receptor potential cation channel subfamily V member 1
(Homo sapiens (Human)) | BDBM20284
(CHEMBL391997 | CPZ | Capsazepine | N-[2-(4-chlorop...)Show InChI InChI=1S/C19H21ClN2O2S/c20-16-5-3-13(4-6-16)7-8-21-19(25)22-9-1-2-14-10-17(23)18(24)11-15(14)12-22/h3-6,10-11,23-24H,1-2,7-9,12H2,(H,21,25) | PDB MMDB
Reactome pathway KEGG
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| PDB Article PubMed
| n/a | n/a | 2.60E+3 | n/a | n/a | n/a | n/a | n/a | n/a |
Glenmark Pharmaceuticals Ltd.
Curated by ChEMBL
| Assay Description Inhibition of TRPV1 (unknown origin) |
Bioorg Med Chem 21: 6542-53 (2013)
Article DOI: 10.1016/j.bmc.2013.08.031 BindingDB Entry DOI: 10.7270/Q2TH8P5S |
More data for this Ligand-Target Pair | 3D Structure (crystal) |
Transient receptor potential cation channel subfamily V member 1
(Rattus norvegicus (rat)) | BDBM20284
(CHEMBL391997 | CPZ | Capsazepine | N-[2-(4-chlorop...)Show InChI InChI=1S/C19H21ClN2O2S/c20-16-5-3-13(4-6-16)7-8-21-19(25)22-9-1-2-14-10-17(23)18(24)11-15(14)12-22/h3-6,10-11,23-24H,1-2,7-9,12H2,(H,21,25) | PDB MMDB
Reactome pathway KEGG
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| n/a | n/a | >3.00E+4 | n/a | n/a | n/a | n/a | n/a | n/a |
GlaxoSmithKline
Curated by ChEMBL
| Assay Description Antagonist activity at rat TRPV1 expressed in CHO cells assessed as blockade of acid-induced receptor activation by aequorin based assay |
J Med Chem 50: 2589-96 (2007)
Article DOI: 10.1021/jm060637e BindingDB Entry DOI: 10.7270/Q269737M |
More data for this Ligand-Target Pair | 3D Structure (crystal) |
Transient receptor potential cation channel subfamily V member 1
(Rattus norvegicus (rat)) | BDBM20284
(CHEMBL391997 | CPZ | Capsazepine | N-[2-(4-chlorop...)Show InChI InChI=1S/C19H21ClN2O2S/c20-16-5-3-13(4-6-16)7-8-21-19(25)22-9-1-2-14-10-17(23)18(24)11-15(14)12-22/h3-6,10-11,23-24H,1-2,7-9,12H2,(H,21,25) | PDB MMDB
Reactome pathway KEGG
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| n/a | n/a | >4.00E+4 | n/a | n/a | n/a | n/a | n/a | n/a |
GlaxoSmithKline
Curated by ChEMBL
| Assay Description Antagonist activity at rat TRPV1 expressed in CHO cells assessed as blockade of acid-induced receptor activation by [45Ca2+] uptake assay |
J Med Chem 50: 2589-96 (2007)
Article DOI: 10.1021/jm060637e BindingDB Entry DOI: 10.7270/Q269737M |
More data for this Ligand-Target Pair | 3D Structure (crystal) |
Transient receptor potential cation channel subfamily V member 1
(Homo sapiens (Human)) | BDBM20284
(CHEMBL391997 | CPZ | Capsazepine | N-[2-(4-chlorop...)Show InChI InChI=1S/C19H21ClN2O2S/c20-16-5-3-13(4-6-16)7-8-21-19(25)22-9-1-2-14-10-17(23)18(24)11-15(14)12-22/h3-6,10-11,23-24H,1-2,7-9,12H2,(H,21,25) | PDB MMDB
Reactome pathway KEGG
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| n/a | n/a | n/a | n/a | 32 | n/a | n/a | 7.2 | 25 |
GSK
| Assay Description One day before the assay was performed, human TRPV1 expressed in 1321N1 astrocytoma cells were plated onto 96-well assay plates and grown until 2.5 h... |
Bioorg Med Chem Lett 14: 3631-4 (2004)
Article DOI: 10.1016/j.bmcl.2004.05.028 BindingDB Entry DOI: 10.7270/Q24T6GM8 |
More data for this Ligand-Target Pair | 3D Structure (crystal) |
Transient receptor potential cation channel subfamily V member 1
(Homo sapiens (Human)) | BDBM20284
(CHEMBL391997 | CPZ | Capsazepine | N-[2-(4-chlorop...)Show InChI InChI=1S/C19H21ClN2O2S/c20-16-5-3-13(4-6-16)7-8-21-19(25)22-9-1-2-14-10-17(23)18(24)11-15(14)12-22/h3-6,10-11,23-24H,1-2,7-9,12H2,(H,21,25) | PDB MMDB
Reactome pathway KEGG
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| PDB Article PubMed
| n/a | n/a | n/a | n/a | 2.51E+3 | n/a | n/a | n/a | n/a |
Universidad de Antioquia
Curated by ChEMBL
| Assay Description Antagonist activity at human TRPV1 expressed in tetracycline-stimulated HEK293 cells assessed as inhibition of capsaicin-induced intracellular calciu... |
Bioorg Med Chem 18: 3299-306 (2010)
Article DOI: 10.1016/j.bmc.2010.03.013 BindingDB Entry DOI: 10.7270/Q24M95RD |
More data for this Ligand-Target Pair | 3D Structure (crystal) |