BDBM435146 US10584127, Compound E1-8.2::US11136328, Compound E1-8.2::US11752155, Compound E1-8.2B'

SMILES Cc1ccc(COC(=O)N2CC[C@H](CNc3ncc4cn[nH]c4n3)C(F)(F)C2)cc1

InChI Key

Data  1 KI  16 IC50

  Tab Delimited (TSV)   2D SDfile   Computed 3D by Vconf -m prep SDfile
Find this compound or compounds like it in BindingDB:
   Substructure
Similarity at least:  must be >=0.5
Exact match

Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB

Found 17 hits for monomerid = 435146   

TargetGlutamate receptor ionotropic, NMDA 2B(Rattus norvegicus (Rat))
Rugen Holdings (Cayman)

US Patent
LigandPNGBDBM435146(US10584127, Compound E1-8.2 | US11136328, Compound...)
Affinity DataKi:  1.40nMAssay Description:HEK293 cell lines stably expressing cloned human NR1/NR2B and NR1/NR2A, respectively, were established according to standard previously described met...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetPotassium voltage-gated channel subfamily H member 2(Homo sapiens (Human))
Rugen Holdings (Cayman)

US Patent
LigandPNGBDBM435146(US10584127, Compound E1-8.2 | US11136328, Compound...)
Affinity DataIC50:  6.80E+3nMAssay Description:The assay was performed on hERG channel stably expressed in HEK293 cells. The cells were cultured at 37° C. in a humidified CO2 incubator in the grow...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetPotassium voltage-gated channel subfamily H member 2(Homo sapiens (Human))
Rugen Holdings (Cayman)

US Patent
LigandPNGBDBM435146(US10584127, Compound E1-8.2 | US11136328, Compound...)
Affinity DataIC50:  6.80E+3nMAssay Description:The assay was performed on hERG channel stably expressed in HEK293 cells. The cells were cultured at 37° C. in a humidified CO2 incubator in the grow...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetCytochrome P450 2D6(Homo sapiens (Human))
Rugen Holdings (Cayman)

US Patent
LigandPNGBDBM435146(US10584127, Compound E1-8.2 | US11136328, Compound...)
Affinity DataIC50:  5.90E+3nMAssay Description:Inhibitory activities of test compounds on 5 major isoforms of CYP P450 were evaluated by using pooled human liver microsome (HLM, purchased from BD ...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetGlutamate receptor ionotropic, NMDA 2B(Homo sapiens (Human))
Rugen Holdings (Cayman)

US Patent
LigandPNGBDBM435146(US10584127, Compound E1-8.2 | US11136328, Compound...)
Affinity DataIC50:  17nMAssay Description:HEK293 cell lines stably expressing cloned human NR1/NR2B and NR1/NR2A, respectively, were established according to standard previously described met...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetGlutamate receptor ionotropic, NMDA 2A(Homo sapiens (Human))
Rugen Holdings (Cayman)

US Patent
LigandPNGBDBM435146(US10584127, Compound E1-8.2 | US11136328, Compound...)
Affinity DataIC50: >1.00E+4nMAssay Description:HEK293 cell lines stably expressing cloned human NR1/NR2B and NR1/NR2A, respectively, were established according to standard previously described met...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetGlutamate receptor ionotropic, NMDA 2B(Homo sapiens (Human))
Rugen Holdings (Cayman)

US Patent
LigandPNGBDBM435146(US10584127, Compound E1-8.2 | US11136328, Compound...)
Affinity DataIC50:  17nMAssay Description:HEK293 cell lines stably expressing cloned human NR1/NR2B and NR1/NR2A, respectively, were established according to standard previously described met...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetPotassium voltage-gated channel subfamily H member 2(Homo sapiens (Human))
Rugen Holdings (Cayman)

US Patent
LigandPNGBDBM435146(US10584127, Compound E1-8.2 | US11136328, Compound...)
Affinity DataIC50:  6.80E+3nMAssay Description:The assay was performed on hERG channel stably expressed in HEK293 cells. The cells were cultured at 37° C. in a humidified CO2 incubator in the grow...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetGlutamate receptor ionotropic, NMDA 2B(Homo sapiens (Human))
Rugen Holdings (Cayman)

US Patent
LigandPNGBDBM435146(US10584127, Compound E1-8.2 | US11136328, Compound...)
Affinity DataIC50:  17nMAssay Description:HEK293 cell lines stably expressing cloned human NR1/NR2B and NR1/NR2A, respectively, were established according to standard previously described met...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetCytochrome P450 2D6(Homo sapiens (Human))
Rugen Holdings (Cayman)

US Patent
LigandPNGBDBM435146(US10584127, Compound E1-8.2 | US11136328, Compound...)
Affinity DataIC50:  5.90E+3nMAssay Description:Inhibitory activities of test compounds on 5 major isoforms of CYP P450 were evaluated by using pooled human liver microsome (HLM, purchased from BD ...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetGlutamate receptor ionotropic, NMDA 2B(Homo sapiens (Human))
Rugen Holdings (Cayman)

US Patent
LigandPNGBDBM435146(US10584127, Compound E1-8.2 | US11136328, Compound...)
Affinity DataIC50:  17nMAssay Description:HEK293 cell lines stably expressing cloned human NR1/NR2B and NR1/NR2A, respectively, were established according to standard previously described met...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetCytochrome P450 2D6(Homo sapiens (Human))
Rugen Holdings (Cayman)

US Patent
LigandPNGBDBM435146(US10584127, Compound E1-8.2 | US11136328, Compound...)
Affinity DataIC50:  5.90E+3nMAssay Description:Inhibitory activities of test compounds on 5 major isoforms of CYP P450 were evaluated by using pooled human liver microsome (HLM, purchased from BD ...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetGlutamate receptor ionotropic, NMDA 2B(Homo sapiens (Human))
Rugen Holdings (Cayman)

US Patent
LigandPNGBDBM435146(US10584127, Compound E1-8.2 | US11136328, Compound...)
Affinity DataIC50:  17nMAssay Description:HEK293 cell lines stably expressing cloned human NR1/NR2B and NR1/NR2A, respectively, were established according to standard previously described met...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetGlutamate receptor ionotropic, NMDA 2A(Homo sapiens (Human))
Rugen Holdings (Cayman)

US Patent
LigandPNGBDBM435146(US10584127, Compound E1-8.2 | US11136328, Compound...)
Affinity DataIC50: >1.00E+7nMAssay Description:This example describes an NR2B receptor binding assay in rat brain using [3H] (E)-N1-(2-methoxybenzyl)-cinnamidine (see below). The binding assay met...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetGlutamate receptor ionotropic, NMDA 2B(Homo sapiens (Human))
Rugen Holdings (Cayman)

US Patent
LigandPNGBDBM435146(US10584127, Compound E1-8.2 | US11136328, Compound...)
Affinity DataIC50:  17nMAssay Description:HEK293 cell lines stably expressing cloned human NR1/NR2B and NR1/NR2A, respectively, were established according to standard previously described met...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetGlutamate receptor ionotropic, NMDA 2B(Homo sapiens (Human))
Rugen Holdings (Cayman)

US Patent
LigandPNGBDBM435146(US10584127, Compound E1-8.2 | US11136328, Compound...)
Affinity DataIC50:  17nMAssay Description:HEK293 cell lines stably expressing cloned human NR1/NR2B and NR1/NR2A, respectively, were established according to standard previously described met...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetGlutamate receptor ionotropic, NMDA 2A(Homo sapiens (Human))
Rugen Holdings (Cayman)

US Patent
LigandPNGBDBM435146(US10584127, Compound E1-8.2 | US11136328, Compound...)
Affinity DataIC50: >1.00E+7nMAssay Description:HEK293 cell lines stably expressing cloned human NR1/NR2B and NR1/NR2A, respectively, were established according to standard previously described met...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent