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
Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB
Found 47 hits for monomerid = 20284
TargetTransient receptor potential cation channel subfamily V member 1(Homo sapiens (Human))
Johnson & Johnson Pharmaceutical Research And Development
Curated by ChEMBL
Johnson & Johnson Pharmaceutical Research And Development
Curated by ChEMBL
Affinity DataKi: 120nMAssay Description:Binding affinity towards human vanilloid receptor subtype 1 expressed in HEK293 cell membrane using [3H]-RTX as radioligand.More data for this Ligand-Target Pair
3D Structure (crystal)TargetTransient receptor potential cation channel subfamily V member 1(Homo sapiens (Human))
Johnson & Johnson Pharmaceutical Research And Development
Curated by ChEMBL
Johnson & Johnson Pharmaceutical Research And Development
Curated by ChEMBL
Affinity DataKi: 120nMAssay Description:Binding affinity towards cloned human vanilloid receptor subtype 1 in HEK293 cell membranes using [3H]-RTX as radioligandMore data for this Ligand-Target Pair
TargetTransient receptor potential cation channel subfamily V member 1(Rattus norvegicus (rat))
Seoul National University
Curated by ChEMBL
Seoul National University
Curated by ChEMBL
Affinity DataKi: 520nMAssay Description:Antagonist activity at rat TRPV1 expressed in CHO cells assessed as inhibition of calcium uptakeMore data for this Ligand-Target Pair
TargetTransient receptor potential cation channel subfamily V member 1(Rattus norvegicus (rat))
Seoul National University
Curated by ChEMBL
Seoul National University
Curated by ChEMBL
Affinity DataKi: 520nMAssay Description:Antagonist activity towards rat TRPV1 expressed in CHO cellsMore data for this Ligand-Target Pair
TargetTransient receptor potential cation channel subfamily V member 1(Rattus norvegicus (rat))
Seoul National University
Curated by ChEMBL
Seoul National University
Curated by ChEMBL
Affinity DataKi: 520nMAssay Description:Antagonist activity for rat TRPV1 expressed in CHO cellsMore data for this Ligand-Target Pair
TargetTransient receptor potential cation channel subfamily V member 1(Rattus norvegicus (rat))
Seoul National University
Curated by ChEMBL
Seoul National University
Curated by ChEMBL
Affinity DataKi: 520nMAssay Description:Inhibition of capsaicin-induced [Ca2+] uptake by Rat Vanilloid receptor 1 (VR1) expressing CHO cellsMore data for this Ligand-Target Pair
TargetTransient receptor potential cation channel subfamily V member 1(Rattus norvegicus (rat))
Seoul National University
Curated by ChEMBL
Seoul National University
Curated by ChEMBL
Affinity DataKi: 1.20E+3nMAssay Description:Displacement of [3H]RTX from Vanilloid receptor in Rat spinal cord membranesMore data for this Ligand-Target Pair
TargetTransient receptor potential cation channel subfamily V member 1(Homo sapiens (Human))
Johnson & Johnson Pharmaceutical Research And Development
Curated by ChEMBL
Johnson & Johnson Pharmaceutical Research And Development
Curated by ChEMBL
Affinity DataKi: 1.29E+3nM ΔG°: -8.03kcal/mole EC50: 282nMpH: 7.4 T: 2°CAssay Description:The hTRPV1-expressing CHO cell membranes were incubated with [3H]A-778317 and test compounds to establish equilibrium. After incubation was terminate...More data for this Ligand-Target Pair
TargetTransient receptor potential cation channel subfamily V member 1(Rattus norvegicus (rat))
Seoul National University
Curated by ChEMBL
Seoul National University
Curated by ChEMBL
Affinity DataKi: 1.30E+3nM ΔG°: -8.35kcal/mole EC50: 520nMpH: 7.4 T: 2°CAssay Description:Binding assay mixtures were set up and contained [3H] RTX, various concentrations of competing ligands, and rVR1-transfected CHO cells. Nonspecific b...More data for this Ligand-Target Pair
TargetTransient receptor potential cation channel subfamily V member 1(Rattus norvegicus (rat))
Seoul National University
Curated by ChEMBL
Seoul National University
Curated by ChEMBL
Affinity DataKi: 1.30E+3nMAssay Description:In vitro binding affinity towards Rat Vanilloid receptor 1 (VR1) by [3H]-RTX displacement.More data for this Ligand-Target Pair
TargetTransient receptor potential cation channel subfamily V member 1(Rattus norvegicus (rat))
Seoul National University
Curated by ChEMBL
Seoul National University
Curated by ChEMBL
Affinity DataKi: 1.30E+3nM ΔG°: -8.35kcal/mole EC50: 520nMpH: 7.4 T: 2°CAssay Description:Binding assay mixtures were set up and contained [3H] RTX, various concentrations of competing ligands, and rVR1-transfected CHO cells. Nonspecific b...More data for this Ligand-Target Pair
TargetTransient receptor potential cation channel subfamily V member 1(Rattus norvegicus (rat))
Seoul National University
Curated by ChEMBL
Seoul National University
Curated by ChEMBL
Affinity DataKi: 1.30E+3nMAssay Description:Displacement of [3H]RTX from rat TRPV1 expressed in CHO cellsMore data for this Ligand-Target Pair
TargetTransient receptor potential cation channel subfamily V member 1(Rattus norvegicus (rat))
Seoul National University
Curated by ChEMBL
Seoul National University
Curated by ChEMBL
Affinity DataKi: 1.30E+3nMAssay Description:In vitro binding affinity for rat TRPV1 expressed in CHO cells using [3H]-RTXMore data for this Ligand-Target Pair
TargetTransient receptor potential cation channel subfamily V member 1(Rattus norvegicus (rat))
Seoul National University
Curated by ChEMBL
Seoul National University
Curated by ChEMBL
Affinity DataKi: 1.30E+3nMAssay Description:In vitro inhibition of [3H]-RTX binding to rat TRPV1 expressed in CHO cellsMore data for this Ligand-Target Pair
TargetTransient receptor potential cation channel subfamily V member 1(Rattus norvegicus (rat))
Seoul National University
Curated by ChEMBL
Seoul National University
Curated by ChEMBL
TargetTransient receptor potential cation channel subfamily V member 1(Rattus norvegicus (rat))
Seoul National University
Curated by ChEMBL
Seoul National University
Curated by ChEMBL
Affinity DataIC50: 887nMAssay Description:Antagonist activity at rat TRPV1 expressed in CHO cells assessed as blockade of capsaicin-induced receptor activation by [45Ca2+] uptake assayMore data for this Ligand-Target Pair
TargetTransient receptor potential cation channel subfamily V member 1(Homo sapiens (Human))
Johnson & Johnson Pharmaceutical Research And Development
Curated by ChEMBL
Johnson & Johnson Pharmaceutical Research And Development
Curated by ChEMBL
Affinity DataIC50: 4nMAssay Description:In vitro inhibition of anandamide activated human TRPV1 receptor in [Ca2+] influx assayMore data for this Ligand-Target Pair
TargetTransient receptor potential cation channel subfamily V member 1(Homo sapiens (Human))
Johnson & Johnson Pharmaceutical Research And Development
Curated by ChEMBL
Johnson & Johnson Pharmaceutical Research And Development
Curated by ChEMBL
Affinity DataIC50: 4nMAssay Description:In vitro inhibition of anandamide activated human TRPV1 receptor in [Ca2+] influx assayMore data for this Ligand-Target Pair
TargetTransient receptor potential cation channel subfamily V member 1/2/4(Rattus norvegicus)
Seoul National University
Curated by ChEMBL
Seoul National University
Curated by ChEMBL
Affinity DataIC50: 650nMAssay Description:In vitro inhibitory concentration was determined against [45Ca2+]- influx in rat DRG neuronsMore data for this Ligand-Target Pair
TargetTransient receptor potential cation channel subfamily V member 1(Rattus norvegicus (rat))
Seoul National University
Curated by ChEMBL
Seoul National University
Curated by ChEMBL
Affinity DataIC50: 365nMAssay Description:Inhibition of rat transient receptor potential vanilloid 1 receptor (n=2)More data for this Ligand-Target Pair
TargetTransient receptor potential cation channel subfamily V member 1(Rattus norvegicus (rat))
Seoul National University
Curated by ChEMBL
Seoul National University
Curated by ChEMBL
Affinity DataIC50: 4nMAssay Description:In vitro inhibition of acid activated rat TRPV1 receptor in [Ca2+] influx assayMore data for this Ligand-Target Pair
TargetTransient receptor potential cation channel subfamily V member 1(Rattus norvegicus (rat))
Seoul National University
Curated by ChEMBL
Seoul National University
Curated by ChEMBL
Affinity DataIC50: 58nMAssay 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 ...More data for this Ligand-Target Pair
TargetTransient receptor potential cation channel subfamily V member 1(Homo sapiens (Human))
Johnson & Johnson Pharmaceutical Research And Development
Curated by ChEMBL
Johnson & Johnson Pharmaceutical Research And Development
Curated by ChEMBL
Affinity DataIC50: 68nMAssay Description:Antagonist activity against human TRPV1 expressed in T-REx HEK cells assessed as inhibition of capsaicin-induced increase in intracellular Ca2+ accum...More data for this Ligand-Target Pair
TargetTransient receptor potential cation channel subfamily V member 1(Rattus norvegicus (rat))
Seoul National University
Curated by ChEMBL
Seoul National University
Curated by ChEMBL
Affinity DataIC50: 220nMAssay Description:Antagonist activity at rat TRPV1 expressed in CHO cells assessed as blockade of capsaicin-induced receptor activation by aequorin based assayMore data for this Ligand-Target Pair
TargetTransient receptor potential cation channel subfamily V member 1(Homo sapiens (Human))
Johnson & Johnson Pharmaceutical Research And Development
Curated by ChEMBL
Johnson & Johnson Pharmaceutical Research And Development
Curated by ChEMBL
Affinity DataIC50: 100nMAssay Description:Antagonistic activity towards human vanilloid receptor subtype 1 expressed in HEK293 cell membrane, as inhibition of agonist-induced intracellular [C...More data for this Ligand-Target Pair
TargetTransient receptor potential cation channel subfamily V member 1(Homo sapiens (Human))
Johnson & Johnson Pharmaceutical Research And Development
Curated by ChEMBL
Johnson & Johnson Pharmaceutical Research And Development
Curated by ChEMBL
Affinity DataIC50: 2.60E+3nMAssay Description:Inhibition of TRPV1 (unknown origin)More data for this Ligand-Target Pair
TargetTransient receptor potential cation channel subfamily V member 1(Homo sapiens (Human))
Johnson & Johnson Pharmaceutical Research And Development
Curated by ChEMBL
Johnson & Johnson Pharmaceutical Research And Development
Curated by ChEMBL
Affinity DataIC50: 150nMAssay Description:Antagonist activity at human brain TRPV1 expressed in HEK293T cells assessed as inhibition of CAP-induced intracellular Ca2+ influx by fluorescence-b...More data for this Ligand-Target Pair
TargetTransient receptor potential cation channel subfamily V member 1/2/4(Rattus norvegicus)
Seoul National University
Curated by ChEMBL
Seoul National University
Curated by ChEMBL
Affinity DataIC50: 6.50E+5nMAssay Description:Antagonistic activity against vanilloid receptor as concentration to reduce the response to 0.5 mM capsaicin by 50% from neonatal rat culture spinal ...More data for this Ligand-Target Pair
TargetTransient receptor potential cation channel subfamily V member 1/2/4(Rattus norvegicus)
Seoul National University
Curated by ChEMBL
Seoul National University
Curated by ChEMBL
Affinity DataIC50: 590nMAssay Description:Inhibition of [Ca2+] uptake in dorsal root ganglion (DRG) neurons from neonatal Sprague-Dawley ratMore data for this Ligand-Target Pair
TargetTransient receptor potential cation channel subfamily V member 1(Homo sapiens (Human))
Johnson & Johnson Pharmaceutical Research And Development
Curated by ChEMBL
Johnson & Johnson Pharmaceutical Research And Development
Curated by ChEMBL
Affinity DataEC50: 2.51E+3nMAssay Description:Antagonist activity at human TRPV1 expressed in tetracycline-stimulated HEK293 cells assessed as inhibition of capsaicin-induced intracellular calciu...More data for this Ligand-Target Pair
TargetTransient receptor potential cation channel subfamily V member 1/2/4(Rattus norvegicus)
Seoul National University
Curated by ChEMBL
Seoul National University
Curated by ChEMBL
Affinity DataIC50: 650nMAssay Description:In vitro antagonist activity at the vanilloid receptor in rat DRG neurons.More data for this Ligand-Target Pair
TargetTransient receptor potential cation channel subfamily V member 1(Homo sapiens (Human))
Johnson & Johnson Pharmaceutical Research And Development
Curated by ChEMBL
Johnson & Johnson Pharmaceutical Research And Development
Curated by ChEMBL
Affinity DataIC50: 69nMAssay Description:Antagonist activity at human TRPV1 expressed in CHO cells assessed as blockade of acid-induced receptor activation by [45Ca2+] uptake assayMore data for this Ligand-Target Pair
TargetTransient receptor potential cation channel subfamily V member 1(Homo sapiens (Human))
Johnson & Johnson Pharmaceutical Research And Development
Curated by ChEMBL
Johnson & Johnson Pharmaceutical Research And Development
Curated by ChEMBL
Affinity DataIC50: 53nMAssay Description:Antagonist activity at human TRPV1 expressed in CHO cells assessed as blockade of capsaicin-induced receptor activation by [45Ca2+] uptake assayMore data for this Ligand-Target Pair
TargetTransient receptor potential cation channel subfamily V member 1(Rattus norvegicus (rat))
Seoul National University
Curated by ChEMBL
Seoul National University
Curated by ChEMBL
Affinity DataIC50: >4.00E+4nMAssay Description:Antagonist activity at rat TRPV1 expressed in CHO cells assessed as blockade of acid-induced receptor activation by [45Ca2+] uptake assayMore data for this Ligand-Target Pair
TargetTransient receptor potential cation channel subfamily V member 1(Rattus norvegicus (rat))
Seoul National University
Curated by ChEMBL
Seoul National University
Curated by ChEMBL
Affinity DataIC50: >3.00E+4nMAssay Description:Antagonist activity at rat TRPV1 expressed in CHO cells assessed as blockade of acid-induced receptor activation by aequorin based assayMore data for this Ligand-Target Pair
TargetTransient receptor potential cation channel subfamily V member 1(Homo sapiens (Human))
Johnson & Johnson Pharmaceutical Research And Development
Curated by ChEMBL
Johnson & Johnson Pharmaceutical Research And Development
Curated by ChEMBL
Affinity DataIC50: 39nMAssay Description:Antagonist activity at human TRPV1 expressed in CHO cells assessed as blockade of capsaicin-induced receptor activation by aequorin based assayMore data for this Ligand-Target Pair
TargetTransient receptor potential cation channel subfamily V member 1(Homo sapiens (Human))
Johnson & Johnson Pharmaceutical Research And Development
Curated by ChEMBL
Johnson & Johnson Pharmaceutical Research And Development
Curated by ChEMBL
Affinity DataIC50: 320nMAssay Description:Antagonist activity at human TRPV1 expressed in CHO cells assessed as blockade of acid-induced receptor activation by aequorin based assayMore data for this Ligand-Target Pair
TargetTransient receptor potential cation channel subfamily V member 1(Homo sapiens (Human))
Johnson & Johnson Pharmaceutical Research And Development
Curated by ChEMBL
Johnson & Johnson Pharmaceutical Research And Development
Curated by ChEMBL
Affinity DataIC50: 56nMAssay Description:Inhibition of 100 nM capsaicin effect on intracellular [Ca2+] concentration in HEK293 cells expressing human TRPV1More data for this Ligand-Target Pair
TargetTransient receptor potential cation channel subfamily V member 1(Homo sapiens (Human))
Johnson & Johnson Pharmaceutical Research And Development
Curated by ChEMBL
Johnson & Johnson Pharmaceutical Research And Development
Curated by ChEMBL
Affinity DataIC50: 334nMAssay Description:Inhibition of calcium influx evoked by capsaicin in human TRPV1 expressing cells by fluorescence assayMore data for this Ligand-Target Pair
TargetTransient receptor potential cation channel subfamily V member 1(Homo sapiens (Human))
Johnson & Johnson Pharmaceutical Research And Development
Curated by ChEMBL
Johnson & Johnson Pharmaceutical Research And Development
Curated by ChEMBL
Affinity DataIC50: 5nMAssay Description:In vitro inhibition of PMA-activated human TRPV1 receptor in [Ca2+] influx assayMore data for this Ligand-Target Pair
TargetTransient receptor potential cation channel subfamily V member 1(Homo sapiens (Human))
Johnson & Johnson Pharmaceutical Research And Development
Curated by ChEMBL
Johnson & Johnson Pharmaceutical Research And Development
Curated by ChEMBL
Affinity DataIC50: 5nMAssay Description:In vitro inhibition of PMA-activated human TRPV1 receptor in [Ca2+] influx assayMore data for this Ligand-Target Pair
TargetTransient receptor potential cation channel subfamily V member 1(Homo sapiens (Human))
Johnson & Johnson Pharmaceutical Research And Development
Curated by ChEMBL
Johnson & Johnson Pharmaceutical Research And Development
Curated by ChEMBL
Affinity DataIC50: 420nMAssay Description:Inhibition of capsaicin-induced calcium uptake by transient receptor potential vanilloid type 1 expressed in CHO cellsMore data for this Ligand-Target Pair
TargetTransient receptor potential cation channel subfamily V member 1/2/4(Rattus norvegicus)
Seoul National University
Curated by ChEMBL
Seoul National University
Curated by ChEMBL
Affinity DataIC50: 600nMAssay Description:Ability to inhibit [Ca2+] influx neonatal rat cultured spinal sensory neurons.More data for this Ligand-Target Pair
TargetTransient receptor potential cation channel subfamily V member 1/2/4(Rattus norvegicus)
Seoul National University
Curated by ChEMBL
Seoul National University
Curated by ChEMBL
Affinity DataEC50: >1.00E+5nMAssay Description:Ability to cause [Ca2+] influx in neonatal rat cultured spinal sensory neurons.More data for this Ligand-Target Pair
TargetTransient receptor potential cation channel subfamily V member 1(Homo sapiens (Human))
Johnson & Johnson Pharmaceutical Research And Development
Curated by ChEMBL
Johnson & Johnson Pharmaceutical Research And Development
Curated by ChEMBL
Affinity DataIC50: 100nMAssay Description:Binding affinity towards cloned human vanilloid receptor subtype 1 in HEK293 cell membranes using [3H]-RTX as radioligandMore data for this Ligand-Target Pair
TargetTransient receptor potential cation channel subfamily V member 1(Homo sapiens (Human))
Johnson & Johnson Pharmaceutical Research And Development
Curated by ChEMBL
Johnson & Johnson Pharmaceutical Research And Development
Curated by ChEMBL
Affinity DataEC50: 32nMpH: 7.2 T: 2°CAssay 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...More data for this Ligand-Target Pair
TargetTransient receptor potential cation channel subfamily V member 1(Homo sapiens (Human))
Johnson & Johnson Pharmaceutical Research And Development
Curated by ChEMBL
Johnson & Johnson Pharmaceutical Research And Development
Curated by ChEMBL
Affinity DataIC50: 74nMAssay Description:Inhibition of human transient receptor potential vanilloid 1 receptor (n=5)More data for this Ligand-Target Pair