BDBM50331134 2-methyl-2-(4-(2-(piperidin-1-yl)-7-(3-(trifluoromethyl)pyridin-2-yl)-6,7,8,9-tetrahydro-5H-pyrimido[5,4-d]azepin-4-ylamino)phenyl)propanoic acid::CHEMBL1289501::US9422293, 186::US9738649, Example 186

SMILES CC(C)(C(O)=O)c1ccc(Nc2nc(nc3CCN(CCc23)c2ncccc2C(F)(F)F)N2CCCCC2)cc1

InChI Key InChIKey=MTRRARFCGONWPC-UHFFFAOYSA-N

Data  5 IC50

  Tab Delimited (TSV)   2D SDfile   Computed 3D by Vconf -m prep SDfile
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Similarity at least:  must be >=0.5
Exact match

Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB

Found 5 hits for monomerid = 50331134   

TargetTransient receptor potential cation channel subfamily V member 1(Human)
Janssen Pharmaceutica

US Patent
LigandPNGBDBM50331134(2-methyl-2-(4-(2-(piperidin-1-yl)-7-(3-(trifluorom...)
Affinity DataIC50: 50nMT: 2°CAssay Description:HEK293 cells were transfected with human TRPV1 cloned in pcDNA3.1zeo(+) using the Effectene non-liposomal lipid based transfection kit (Qiagen) (hTRP...More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/21/2017
Entry Details
Go to US Patent

LigandPNGBDBM50331134(2-methyl-2-(4-(2-(piperidin-1-yl)-7-(3-(trifluorom...)
Affinity DataIC50: 140nMT: 2°CAssay Description:The assay was performed as described below, using HEK293 cells transfected with rat TRPV1 (rTRPV1/HEK293). These cells had a geneticin selection mark...More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/21/2017
Entry Details
Go to US Patent

TargetTransient receptor potential cation channel subfamily V member 1(Human)
Janssen Pharmaceutica

US Patent
LigandPNGBDBM50331134(2-methyl-2-(4-(2-(piperidin-1-yl)-7-(3-(trifluorom...)
Affinity DataIC50: 58nMAssay Description:Antagonist activity at human recombinant TRPV1 assessed as inhibition of capsaicin-induced in intracellular calcium levels by cell-based FLIPR assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
6/14/2011
Entry Details Article
PubMed
TargetTransient receptor potential cation channel subfamily V member 1(Human)
Janssen Pharmaceutica

US Patent
LigandPNGBDBM50331134(2-methyl-2-(4-(2-(piperidin-1-yl)-7-(3-(trifluorom...)
Affinity DataIC50: 50nMAssay Description:HEK293 cells were transfected with human TRPV1 cloned in pcDNA3.1zeo(+) using the Effectene non-liposomal lipid based transfection kit (Qiagen) (hTRP...More data for this Ligand-Target Pair
In Depth
Date in BDB:
7/1/2019
Entry Details
Go to US Patent

LigandPNGBDBM50331134(2-methyl-2-(4-(2-(piperidin-1-yl)-7-(3-(trifluorom...)
Affinity DataIC50: 140nMAssay Description:The assay was performed as described above, using HEK293 cells transfected with rat TRPV1 (rTRPV1/HEK293). These cells had a geneticin selection mark...More data for this Ligand-Target Pair
In Depth
Date in BDB:
7/1/2019
Entry Details
Go to US Patent