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BDBM20284 CHEMBL391997::CPZ::Capsazepine::N-[2-(4-chlorophenyl)ethyl]-7,8-dihydroxy-1,3,4,5-tetrahydro-2-benzazepine-2-carbothioamide::N-[2-(4-chlorophenyl)ethyl]-7,8-dihydroxy-2,3,4,5-tetrahydro-1H-2-benzazepine-2-carbothioamide

SMILES: Oc1cc2CCCN(Cc2cc1O)C(=S)NCCc1ccc(Cl)cc1

InChI Key: InChIKey=DRCMAZOSEIMCHM-UHFFFAOYSA-N

Data: 15 KI  34 IC50  6 EC50

PDB links: 1 PDB ID matches this monomer.

Find this compound or compounds like it in BindingDB or PDB:
   Substructure
Similarity at least:  must be >=0.5
Exact match

Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB

Found 52 hits for monomerid = 20284   
Target/Host
(Institution)
LigandTarget/Host
Links
Ligand
Links
Trg + Lig
Links
Ki
nM
ΔG°
kcal/mole
IC50
nM
Kd
nM
EC50/IC50
nM
koff
s-1
kon
M-1s-1
pHTemp
°C
Transient receptor potential cation channel subfamily V member 1


(Homo sapiens (Human))
BDBM20284
PNG
(CHEMBL391997 | CPZ | Capsazepine | N-[2-(4-chlorop...)
Show SMILES Oc1cc2CCCN(Cc2cc1O)C(=S)NCCc1ccc(Cl)cc1
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)
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120n/an/an/an/an/an/an/an/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/s0960-894x(04)00533-5
BindingDB Entry DOI: 10.7270/Q2FB52D6
More data for this
Ligand-Target Pair
3D
3D Structure (crystal)
Transient receptor potential cation channel subfamily V member 1


(Homo sapiens (Human))
BDBM20284
PNG
(CHEMBL391997 | CPZ | Capsazepine | N-[2-(4-chlorop...)
Show SMILES Oc1cc2CCCN(Cc2cc1O)C(=S)NCCc1ccc(Cl)cc1
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)
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120n/an/an/an/an/an/an/an/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)


Article DOI: 10.1016/j.bmcl.2003.09.090
BindingDB Entry DOI: 10.7270/Q2VQ323X
More data for this
Ligand-Target Pair
3D
3D Structure (crystal)
Vanilloid receptor


(Rattus norvegicus (rat))
BDBM20284
PNG
(CHEMBL391997 | CPZ | Capsazepine | N-[2-(4-chlorop...)
Show SMILES Oc1cc2CCCN(Cc2cc1O)C(=S)NCCc1ccc(Cl)cc1
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)
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520n/an/an/an/an/an/an/an/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
3D Structure (crystal)
Vanilloid receptor


(Rattus norvegicus (rat))
BDBM20284
PNG
(CHEMBL391997 | CPZ | Capsazepine | N-[2-(4-chlorop...)
Show SMILES Oc1cc2CCCN(Cc2cc1O)C(=S)NCCc1ccc(Cl)cc1
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)
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520n/an/an/an/an/an/an/an/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
3D Structure (crystal)
Vanilloid receptor


(Rattus norvegicus (rat))
BDBM20284
PNG
(CHEMBL391997 | CPZ | Capsazepine | N-[2-(4-chlorop...)
Show SMILES Oc1cc2CCCN(Cc2cc1O)C(=S)NCCc1ccc(Cl)cc1
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)
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520n/an/an/an/an/an/an/an/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
3D Structure (crystal)
Vanilloid receptor


(Rattus norvegicus (rat))
BDBM20284
PNG
(CHEMBL391997 | CPZ | Capsazepine | N-[2-(4-chlorop...)
Show SMILES Oc1cc2CCCN(Cc2cc1O)C(=S)NCCc1ccc(Cl)cc1
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)
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520n/an/an/an/an/an/an/an/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
3D Structure (crystal)
Vanilloid receptor


(Rattus norvegicus (rat))
BDBM20284
PNG
(CHEMBL391997 | CPZ | Capsazepine | N-[2-(4-chlorop...)
Show SMILES Oc1cc2CCCN(Cc2cc1O)C(=S)NCCc1ccc(Cl)cc1
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)
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1.20E+3n/an/an/an/an/an/an/an/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
3D Structure (crystal)
Transient receptor potential cation channel subfamily V member 1


(Homo sapiens (Human))
BDBM20284
PNG
(CHEMBL391997 | CPZ | Capsazepine | N-[2-(4-chlorop...)
Show SMILES Oc1cc2CCCN(Cc2cc1O)C(=S)NCCc1ccc(Cl)cc1
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)
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1.29E+3 -8.03n/an/a 282n/an/a7.425



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
3D Structure (crystal)
Vanilloid receptor


(Rattus norvegicus (rat))
BDBM20284
PNG
(CHEMBL391997 | CPZ | Capsazepine | N-[2-(4-chlorop...)
Show SMILES Oc1cc2CCCN(Cc2cc1O)C(=S)NCCc1ccc(Cl)cc1
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)
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1.30E+3 -8.35n/an/a 520n/an/a7.437



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
3D Structure (crystal)
Vanilloid receptor


(Rattus norvegicus (rat))
BDBM20284
PNG
(CHEMBL391997 | CPZ | Capsazepine | N-[2-(4-chlorop...)
Show SMILES Oc1cc2CCCN(Cc2cc1O)C(=S)NCCc1ccc(Cl)cc1
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)
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1.30E+3n/an/an/an/an/an/an/an/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
3D Structure (crystal)
Vanilloid receptor


(Rattus norvegicus (rat))
BDBM20284
PNG
(CHEMBL391997 | CPZ | Capsazepine | N-[2-(4-chlorop...)
Show SMILES Oc1cc2CCCN(Cc2cc1O)C(=S)NCCc1ccc(Cl)cc1
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)
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1.30E+3 -8.35n/an/a 520n/an/a7.437



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
3D Structure (crystal)
Vanilloid receptor


(Rattus norvegicus (rat))
BDBM20284
PNG
(CHEMBL391997 | CPZ | Capsazepine | N-[2-(4-chlorop...)
Show SMILES Oc1cc2CCCN(Cc2cc1O)C(=S)NCCc1ccc(Cl)cc1
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)
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1.30E+3n/an/an/an/an/an/an/an/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
3D Structure (crystal)
Vanilloid receptor


(Rattus norvegicus (rat))
BDBM20284
PNG
(CHEMBL391997 | CPZ | Capsazepine | N-[2-(4-chlorop...)
Show SMILES Oc1cc2CCCN(Cc2cc1O)C(=S)NCCc1ccc(Cl)cc1
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)
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1.30E+3n/an/an/an/an/an/an/an/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
3D Structure (crystal)
Vanilloid receptor


(Rattus norvegicus (rat))
BDBM20284
PNG
(CHEMBL391997 | CPZ | Capsazepine | N-[2-(4-chlorop...)
Show SMILES Oc1cc2CCCN(Cc2cc1O)C(=S)NCCc1ccc(Cl)cc1
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)
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1.30E+3n/an/an/an/an/an/an/an/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
3D Structure (crystal)
Vanilloid receptor


(Rattus norvegicus (rat))
BDBM20284
PNG
(CHEMBL391997 | CPZ | Capsazepine | N-[2-(4-chlorop...)
Show SMILES Oc1cc2CCCN(Cc2cc1O)C(=S)NCCc1ccc(Cl)cc1
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)
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4.30E+3n/an/an/an/an/an/an/an/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
3D Structure (crystal)
Vanilloid receptor


(Rattus norvegicus (rat))
BDBM20284
PNG
(CHEMBL391997 | CPZ | Capsazepine | N-[2-(4-chlorop...)
Show SMILES Oc1cc2CCCN(Cc2cc1O)C(=S)NCCc1ccc(Cl)cc1
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)
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n/an/a 887n/an/an/an/an/an/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
3D Structure (crystal)
Transient receptor potential cation channel subfamily V member 1


(Homo sapiens (Human))
BDBM20284
PNG
(CHEMBL391997 | CPZ | Capsazepine | N-[2-(4-chlorop...)
Show SMILES Oc1cc2CCCN(Cc2cc1O)C(=S)NCCc1ccc(Cl)cc1
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)
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n/an/a 3n/an/an/an/an/an/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
3D Structure (crystal)
Transient receptor potential cation channel subfamily V member 1


(Homo sapiens (Human))
BDBM20284
PNG
(CHEMBL391997 | CPZ | Capsazepine | N-[2-(4-chlorop...)
Show SMILES Oc1cc2CCCN(Cc2cc1O)C(=S)NCCc1ccc(Cl)cc1
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)
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n/an/a 4n/an/an/an/an/an/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
3D Structure (crystal)
Vanilloid receptor


(Rattus norvegicus-Rattus norvegicus (rat))
BDBM20284
PNG
(CHEMBL391997 | CPZ | Capsazepine | N-[2-(4-chlorop...)
Show SMILES Oc1cc2CCCN(Cc2cc1O)C(=S)NCCc1ccc(Cl)cc1
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)
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n/an/a 650n/an/an/an/an/an/a



Seoul National University

Curated by ChEMBL


Assay Description
In vitro inhibitory concentration was determined against [45Ca2+]- influx in rat DRG neurons


Bioorg Med Chem Lett 14: 1693-6 (2004)


Article DOI: 10.1016/j.bmcl.2004.01.041
More data for this
Ligand-Target Pair
3D
3D Structure (crystal)
Vanilloid receptor


(Rattus norvegicus (rat))
BDBM20284
PNG
(CHEMBL391997 | CPZ | Capsazepine | N-[2-(4-chlorop...)
Show SMILES Oc1cc2CCCN(Cc2cc1O)C(=S)NCCc1ccc(Cl)cc1
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)
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n/an/a 365n/an/an/an/an/an/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
3D Structure (crystal)
Vanilloid receptor


(Rattus norvegicus (rat))
BDBM20284
PNG
(CHEMBL391997 | CPZ | Capsazepine | N-[2-(4-chlorop...)
Show SMILES Oc1cc2CCCN(Cc2cc1O)C(=S)NCCc1ccc(Cl)cc1
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)
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n/an/a 4n/an/an/an/an/an/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
3D Structure (crystal)
Vanilloid receptor


(Rattus norvegicus (rat))
BDBM20284
PNG
(CHEMBL391997 | CPZ | Capsazepine | N-[2-(4-chlorop...)
Show SMILES Oc1cc2CCCN(Cc2cc1O)C(=S)NCCc1ccc(Cl)cc1
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)
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n/an/a 58n/an/an/an/an/an/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)


Article DOI: 10.1016/s0960-894x(03)00759-5
BindingDB Entry DOI: 10.7270/Q28P5ZW4
More data for this
Ligand-Target Pair
3D
3D Structure (crystal)
Transient receptor potential cation channel subfamily V member 1


(Homo sapiens (Human))
BDBM20284
PNG
(CHEMBL391997 | CPZ | Capsazepine | N-[2-(4-chlorop...)
Show SMILES Oc1cc2CCCN(Cc2cc1O)C(=S)NCCc1ccc(Cl)cc1
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)
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n/an/a 68n/an/an/an/an/an/a


TBA

Assay Description
Antagonist activity against human TRPV1 expressed in T-REx HEK cells assessed as inhibition of capsaicin-induced increase in intracellular Ca2+ accum...


Citation and Details

Article DOI: 10.1021/np500235b
BindingDB Entry DOI: 10.7270/Q27S7QDF
More data for this
Ligand-Target Pair
3D
3D Structure (crystal)
Transient receptor potential cation channel subfamily M member 8


(Mus musculus)
BDBM20284
PNG
(CHEMBL391997 | CPZ | Capsazepine | N-[2-(4-chlorop...)
Show SMILES Oc1cc2CCCN(Cc2cc1O)C(=S)NCCc1ccc(Cl)cc1
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)
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n/an/a>5.00E+4n/an/an/an/an/an/a


TBA

Assay Description
Antagonist activity against mouse TRPM8 expressed in T-REx HEK cells assessed as inhibition of icilin-induced increase in intracellular Ca2+ accumula...


Citation and Details

Article DOI: 10.1021/np500235b
BindingDB Entry DOI: 10.7270/Q27S7QDF
More data for this
Ligand-Target Pair
Transient receptor potential cation channel subfamily M member 8


(Mus musculus)
BDBM20284
PNG
(CHEMBL391997 | CPZ | Capsazepine | N-[2-(4-chlorop...)
Show SMILES Oc1cc2CCCN(Cc2cc1O)C(=S)NCCc1ccc(Cl)cc1
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)
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n/an/a 5.00E+4n/an/an/an/an/an/a


TBA

Assay Description
Antagonist activity against mouse TRPM8 expressed in T-REx HEK cells assessed as inhibition of menthol-induced increase in intracellular Ca2+ accumul...


Citation and Details

Article DOI: 10.1021/np500235b
BindingDB Entry DOI: 10.7270/Q27S7QDF
More data for this
Ligand-Target Pair
Vanilloid receptor


(Rattus norvegicus (rat))
BDBM20284
PNG
(CHEMBL391997 | CPZ | Capsazepine | N-[2-(4-chlorop...)
Show SMILES Oc1cc2CCCN(Cc2cc1O)C(=S)NCCc1ccc(Cl)cc1
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)
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n/an/a 220n/an/an/an/an/an/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
3D Structure (crystal)
Transient receptor potential cation channel subfamily V member 1


(Homo sapiens (Human))
BDBM20284
PNG
(CHEMBL391997 | CPZ | Capsazepine | N-[2-(4-chlorop...)
Show SMILES Oc1cc2CCCN(Cc2cc1O)C(=S)NCCc1ccc(Cl)cc1
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)
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n/an/a 100n/an/an/an/an/an/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/s0960-894x(04)00533-5
BindingDB Entry DOI: 10.7270/Q2FB52D6
More data for this
Ligand-Target Pair
3D
3D Structure (crystal)
Transient receptor potential cation channel subfamily V member 1


(Homo sapiens (Human))
BDBM20284
PNG
(CHEMBL391997 | CPZ | Capsazepine | N-[2-(4-chlorop...)
Show SMILES Oc1cc2CCCN(Cc2cc1O)C(=S)NCCc1ccc(Cl)cc1
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)
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n/an/a 2.60E+3n/an/an/an/an/an/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
3D Structure (crystal)
Transient receptor potential cation channel subfamily M member 8 (TRPM8)


(Homo sapiens (Human))
BDBM20284
PNG
(CHEMBL391997 | CPZ | Capsazepine | N-[2-(4-chlorop...)
Show SMILES Oc1cc2CCCN(Cc2cc1O)C(=S)NCCc1ccc(Cl)cc1
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)
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n/an/a 1.80E+4n/an/an/an/an/an/a



Glenmark Pharmaceuticals Ltd.

Curated by ChEMBL


Assay Description
Inhibition of TRPM8 (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
Transient receptor potential cation channel subfamily M member 8


(Mus musculus)
BDBM20284
PNG
(CHEMBL391997 | CPZ | Capsazepine | N-[2-(4-chlorop...)
Show SMILES Oc1cc2CCCN(Cc2cc1O)C(=S)NCCc1ccc(Cl)cc1
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)
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n/an/a>5.00E+4n/an/an/an/an/an/a



University of Shizuoka

Curated by ChEMBL


Assay Description
Antagonist at TRPM8 isolated from mouse dorsal root ganglion cells expressed in HEK T-REx cells assessed as inhibition of icilin-induced intracellula...


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
Transient receptor potential cation channel subfamily M member 8


(Mus musculus)
BDBM20284
PNG
(CHEMBL391997 | CPZ | Capsazepine | N-[2-(4-chlorop...)
Show SMILES Oc1cc2CCCN(Cc2cc1O)C(=S)NCCc1ccc(Cl)cc1
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)
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n/an/a 5.00E+4n/an/an/an/an/an/a



University of Shizuoka

Curated by ChEMBL


Assay Description
Antagonist at TRPM8 isolated from mouse dorsal root ganglion cells expressed in HEK T-REx cells assessed as inhibition of menthol-induced intracellul...


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
Transient receptor potential cation channel subfamily V member 1


(Homo sapiens (Human))
BDBM20284
PNG
(CHEMBL391997 | CPZ | Capsazepine | N-[2-(4-chlorop...)
Show SMILES Oc1cc2CCCN(Cc2cc1O)C(=S)NCCc1ccc(Cl)cc1
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)
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n/an/a 150n/an/an/an/an/an/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
3D Structure (crystal)
Vanilloid receptor


(Rattus norvegicus-Rattus norvegicus (rat))
BDBM20284
PNG
(CHEMBL391997 | CPZ | Capsazepine | N-[2-(4-chlorop...)
Show SMILES Oc1cc2CCCN(Cc2cc1O)C(=S)NCCc1ccc(Cl)cc1
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)
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n/an/a 6.50E+5n/an/an/an/an/an/a



Seoul National University

Curated by ChEMBL


Assay Description
Antagonistic activity against vanilloid receptor as concentration to reduce the response to 0.5 mM capsaicin by 50% from neonatal rat culture spinal ...


Bioorg Med Chem Lett 13: 601-4 (2003)


Article DOI: 10.1016/s0960-894x(02)01040-5
More data for this
Ligand-Target Pair
3D
3D Structure (crystal)
Vanilloid receptor


(Rattus norvegicus-Rattus norvegicus (rat))
BDBM20284
PNG
(CHEMBL391997 | CPZ | Capsazepine | N-[2-(4-chlorop...)
Show SMILES Oc1cc2CCCN(Cc2cc1O)C(=S)NCCc1ccc(Cl)cc1
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)
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n/an/a 590n/an/an/an/an/an/a



Seoul National University

Curated by ChEMBL


Assay Description
Inhibition of [Ca2+] uptake in dorsal root ganglion (DRG) neurons from neonatal Sprague-Dawley rat


Bioorg Med Chem Lett 13: 4389-93 (2003)


Article DOI: 10.1016/j.bmcl.2003.09.024
More data for this
Ligand-Target Pair
3D
3D Structure (crystal)
Transient receptor potential cation channel subfamily V member 1


(Homo sapiens (Human))
BDBM20284
PNG
(CHEMBL391997 | CPZ | Capsazepine | N-[2-(4-chlorop...)
Show SMILES Oc1cc2CCCN(Cc2cc1O)C(=S)NCCc1ccc(Cl)cc1
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)
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n/an/an/an/a 2.51E+3n/an/an/an/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
3D Structure (crystal)
Vanilloid receptor


(Rattus norvegicus-Rattus norvegicus (rat))
BDBM20284
PNG
(CHEMBL391997 | CPZ | Capsazepine | N-[2-(4-chlorop...)
Show SMILES Oc1cc2CCCN(Cc2cc1O)C(=S)NCCc1ccc(Cl)cc1
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)
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n/an/a 650n/an/an/an/an/an/a



Seoul National University

Curated by ChEMBL


Assay Description
In vitro antagonist activity at the vanilloid receptor in rat DRG neurons.


Bioorg Med Chem Lett 14: 787-91 (2004)


Article DOI: 10.1016/j.bmcl.2003.11.019
More data for this
Ligand-Target Pair
3D
3D Structure (crystal)
Transient receptor potential cation channel subfamily V member 1


(Homo sapiens (Human))
BDBM20284
PNG
(CHEMBL391997 | CPZ | Capsazepine | N-[2-(4-chlorop...)
Show SMILES Oc1cc2CCCN(Cc2cc1O)C(=S)NCCc1ccc(Cl)cc1
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)
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n/an/a 69n/an/an/an/an/an/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
3D Structure (crystal)
Transient receptor potential cation channel subfamily V member 1


(Homo sapiens (Human))
BDBM20284
PNG
(CHEMBL391997 | CPZ | Capsazepine | N-[2-(4-chlorop...)
Show SMILES Oc1cc2CCCN(Cc2cc1O)C(=S)NCCc1ccc(Cl)cc1
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)
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n/an/a 53n/an/an/an/an/an/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
3D Structure (crystal)
Vanilloid receptor


(Rattus norvegicus (rat))
BDBM20284
PNG
(CHEMBL391997 | CPZ | Capsazepine | N-[2-(4-chlorop...)
Show SMILES Oc1cc2CCCN(Cc2cc1O)C(=S)NCCc1ccc(Cl)cc1
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)
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n/an/a>4.00E+4n/an/an/an/an/an/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
3D Structure (crystal)
Vanilloid receptor


(Rattus norvegicus (rat))
BDBM20284
PNG
(CHEMBL391997 | CPZ | Capsazepine | N-[2-(4-chlorop...)
Show SMILES Oc1cc2CCCN(Cc2cc1O)C(=S)NCCc1ccc(Cl)cc1
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)
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n/an/a>3.00E+4n/an/an/an/an/an/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
3D Structure (crystal)
Transient receptor potential cation channel subfamily V member 1


(Homo sapiens (Human))
BDBM20284
PNG
(CHEMBL391997 | CPZ | Capsazepine | N-[2-(4-chlorop...)
Show SMILES Oc1cc2CCCN(Cc2cc1O)C(=S)NCCc1ccc(Cl)cc1
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)
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n/an/a 39n/an/an/an/an/an/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
3D Structure (crystal)
Transient receptor potential cation channel subfamily V member 1


(Homo sapiens (Human))
BDBM20284
PNG
(CHEMBL391997 | CPZ | Capsazepine | N-[2-(4-chlorop...)
Show SMILES Oc1cc2CCCN(Cc2cc1O)C(=S)NCCc1ccc(Cl)cc1
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)
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n/an/a 320n/an/an/an/an/an/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
3D Structure (crystal)
Transient receptor potential cation channel subfamily V member 1


(Homo sapiens (Human))
BDBM20284
PNG
(CHEMBL391997 | CPZ | Capsazepine | N-[2-(4-chlorop...)
Show SMILES Oc1cc2CCCN(Cc2cc1O)C(=S)NCCc1ccc(Cl)cc1
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)
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n/an/a 56n/an/an/an/an/an/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
3D Structure (crystal)
Transient receptor potential cation channel subfamily V member 1


(Homo sapiens (Human))
BDBM20284
PNG
(CHEMBL391997 | CPZ | Capsazepine | N-[2-(4-chlorop...)
Show SMILES Oc1cc2CCCN(Cc2cc1O)C(=S)NCCc1ccc(Cl)cc1
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)
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n/an/a 334n/an/an/an/an/an/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
3D Structure (crystal)
Transient receptor potential cation channel subfamily V member 1


(Homo sapiens (Human))
BDBM20284
PNG
(CHEMBL391997 | CPZ | Capsazepine | N-[2-(4-chlorop...)
Show SMILES Oc1cc2CCCN(Cc2cc1O)C(=S)NCCc1ccc(Cl)cc1
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)
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n/an/a 5n/an/an/an/an/an/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
3D Structure (crystal)
Transient receptor potential cation channel subfamily V member 1


(Homo sapiens (Human))
BDBM20284
PNG
(CHEMBL391997 | CPZ | Capsazepine | N-[2-(4-chlorop...)
Show SMILES Oc1cc2CCCN(Cc2cc1O)C(=S)NCCc1ccc(Cl)cc1
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)
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n/an/a 3n/an/an/an/an/an/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
3D Structure (crystal)
Transient receptor potential cation channel subfamily V member 1


(Homo sapiens (Human))
BDBM20284
PNG
(CHEMBL391997 | CPZ | Capsazepine | N-[2-(4-chlorop...)
Show SMILES Oc1cc2CCCN(Cc2cc1O)C(=S)NCCc1ccc(Cl)cc1
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)
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n/an/a 420n/an/an/an/an/an/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
3D Structure (crystal)
Vanilloid receptor


(Rattus norvegicus-Rattus norvegicus (rat))
BDBM20284
PNG
(CHEMBL391997 | CPZ | Capsazepine | N-[2-(4-chlorop...)
Show SMILES Oc1cc2CCCN(Cc2cc1O)C(=S)NCCc1ccc(Cl)cc1
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)
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n/an/a 600n/an/an/an/an/an/a



Sookmyung Women's University

Curated by ChEMBL


Assay Description
Ability to inhibit [Ca2+] influx neonatal rat cultured spinal sensory neurons.


Bioorg Med Chem Lett 13: 1549-52 (2003)


Article DOI: 10.1016/s0960-894x(03)00178-1
More data for this
Ligand-Target Pair
3D
3D Structure (crystal)
Vanilloid receptor


(Rattus norvegicus-Rattus norvegicus (rat))
BDBM20284
PNG
(CHEMBL391997 | CPZ | Capsazepine | N-[2-(4-chlorop...)
Show SMILES Oc1cc2CCCN(Cc2cc1O)C(=S)NCCc1ccc(Cl)cc1
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)
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n/an/an/an/a>1.00E+5n/an/an/an/a



Sookmyung Women's University

Curated by ChEMBL


Assay Description
Ability to cause [Ca2+] influx in neonatal rat cultured spinal sensory neurons.


Bioorg Med Chem Lett 13: 1549-52 (2003)


Article DOI: 10.1016/s0960-894x(03)00178-1
More data for this
Ligand-Target Pair
3D
3D Structure (crystal)
Transient receptor potential cation channel subfamily V member 1


(Homo sapiens (Human))
BDBM20284
PNG
(CHEMBL391997 | CPZ | Capsazepine | N-[2-(4-chlorop...)
Show SMILES Oc1cc2CCCN(Cc2cc1O)C(=S)NCCc1ccc(Cl)cc1
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)
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n/an/a 100n/an/an/an/an/an/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)


Article DOI: 10.1016/j.bmcl.2003.09.090
BindingDB Entry DOI: 10.7270/Q2VQ323X
More data for this
Ligand-Target Pair
3D
3D Structure (crystal)
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