BDBM8963 CHEMBL32823::Homodimeric Tacrine Analog 3b::N-[7-(1,2,3,4-tetrahydroacridin-9-ylamino)heptyl]-1,2,3,4-tetrahydroacridin-9-amine::Tacrine Dimer 3b::Tacrine-Based Inhibitor 2f::tacrine homobivalent compound 3a

SMILES C(CCCNc1c2CCCCc2nc2ccccc12)CCCNc1c2CCCCc2nc2ccccc12

InChI Key InChIKey=ITZOKHKOFJOBFS-UHFFFAOYSA-N

Data  9 KI  46 IC50

PDB links: 2 PDB IDs match this monomer.

  Tab Delimited (TSV)   2D SDfile   Computed 3D by Vconf -m prep SDfile
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Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB

Found 27 hits for monomerid = 8963   

TargetAcetylcholinesterase(Homo sapiens (Human))
Universita Di Siena

LigandPNGBDBM8963(CHEMBL32823 | Homodimeric Tacrine Analog 3b | N-[7...)
Affinity DataKi:  1.30nM ΔG°:  -12.1kcal/molepH: 8.0 T: 2°CAssay Description:Inhibition of enzyme activity was measured over a substrate concentration range of 0.01-30 mM and at least six inhibitor concentrations to determine ...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetAcetylcholinesterase(Bos taurus (bovine))
Universit£

Curated by ChEMBL
LigandPNGBDBM8963(CHEMBL32823 | Homodimeric Tacrine Analog 3b | N-[7...)
Affinity DataKi:  1.30nMAssay Description:Inhibition of fetal bovine serum AChEMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetAcetylcholinesterase(Bos taurus (bovine))
Universit£

Curated by ChEMBL
LigandPNGBDBM8963(CHEMBL32823 | Homodimeric Tacrine Analog 3b | N-[7...)
Affinity DataKi:  1.30nMAssay Description:Inhibition of fetal Bovine serum AChEMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetAcetylcholinesterase(Homo sapiens (Human))
Universita Di Siena

LigandPNGBDBM8963(CHEMBL32823 | Homodimeric Tacrine Analog 3b | N-[7...)
Affinity DataKi:  1.30nM ΔG°:  -12.1kcal/molepH: 8.0 T: 2°CAssay Description:Inhibition of enzyme activity was measured over a substrate concentration range of 0.01-30 mM and at least six inhibitor concentrations to determine ...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetAcetylcholinesterase(Rattus norvegicus (rat))
Institute Of Science

Curated by ChEMBL
LigandPNGBDBM8963(CHEMBL32823 | Homodimeric Tacrine Analog 3b | N-[7...)
Affinity DataIC50:  1.5nMAssay Description:Inhibition of rat brain AChEMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetAcetylcholinesterase(Homo sapiens (Human))
Universita Di Siena

LigandPNGBDBM8963(CHEMBL32823 | Homodimeric Tacrine Analog 3b | N-[7...)
Affinity DataIC50:  0.810nMAssay Description:Inhibition of human serum recombinant AChE by Ellman's methodMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetAcetylcholinesterase(Homo sapiens (Human))
Universita Di Siena

LigandPNGBDBM8963(CHEMBL32823 | Homodimeric Tacrine Analog 3b | N-[7...)
Affinity DataIC50:  0.810nMAssay Description:Inhibition of recombinant human AChE using acetylthiocholine iodide as substrate preincubated for 20 mins followed by substrate addition by Ellman's ...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetAcetylcholinesterase(Homo sapiens (Human))
Universita Di Siena

LigandPNGBDBM8963(CHEMBL32823 | Homodimeric Tacrine Analog 3b | N-[7...)
Affinity DataIC50:  0.200nMAssay Description:Inhibition of AChEMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetAcetylcholinesterase(Electrophorus electricus (Electric eel))
University Of Waterloo

Curated by ChEMBL
LigandPNGBDBM8963(CHEMBL32823 | Homodimeric Tacrine Analog 3b | N-[7...)
Affinity DataIC50:  1.80nMAssay Description:Inhibition of electric eel AChEMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetAcetylcholinesterase(Homo sapiens (Human))
Universita Di Siena

LigandPNGBDBM8963(CHEMBL32823 | Homodimeric Tacrine Analog 3b | N-[7...)
Affinity DataIC50:  4nMAssay Description:Inhibition of human AChE incubated with compounf for 5 mins before addition of substrate acetylthiocholine iodide by Ellman's methodMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetAcetylcholinesterase(Homo sapiens (Human))
Universita Di Siena

LigandPNGBDBM8963(CHEMBL32823 | Homodimeric Tacrine Analog 3b | N-[7...)
Affinity DataIC50:  0.810nMAssay Description:Mixed-type inhibition of human AChE assessed as hydrolysis of acetylthiocholine by Lineweaver-Burk plot analysisMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetAcetylcholinesterase(Rattus norvegicus (rat))
Institute Of Science

Curated by ChEMBL
LigandPNGBDBM8963(CHEMBL32823 | Homodimeric Tacrine Analog 3b | N-[7...)
Affinity DataIC50:  1.5nMAssay Description:Inhibitory potency against acetylcholinesterase (AChE) of rat cortex homogenate with ethopropazine as BChE inhibitorMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetAcetylcholinesterase(Rattus norvegicus (rat))
Institute Of Science

Curated by ChEMBL
LigandPNGBDBM8963(CHEMBL32823 | Homodimeric Tacrine Analog 3b | N-[7...)
Affinity DataIC50:  0.400nMAssay Description:Inhibition of AChE in rat brain cortex using acetylthiocholine iodide as substrate incubated for 8 mins by Ellman's methodMore data for this Ligand-Target Pair
In DepthDetails PubMed
TargetAcetylcholinesterase(Homo sapiens (Human))
Universita Di Siena

LigandPNGBDBM8963(CHEMBL32823 | Homodimeric Tacrine Analog 3b | N-[7...)
Affinity DataIC50:  0.590nMAssay Description:Inhibitory concentration against human acetylcholinesteraseMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetAcetylcholinesterase(Electrophorus electricus (Electric eel))
University Of Waterloo

Curated by ChEMBL
LigandPNGBDBM8963(CHEMBL32823 | Homodimeric Tacrine Analog 3b | N-[7...)
Affinity DataIC50:  0.170nMAssay Description:Inhibition of electric eel AChE using acetylthiocholine chloride as substrate preincubated for 15 mins by Ellman's methodMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetAcetylcholinesterase(Rattus norvegicus (rat))
Institute Of Science

Curated by ChEMBL
LigandPNGBDBM8963(CHEMBL32823 | Homodimeric Tacrine Analog 3b | N-[7...)
Affinity DataIC50:  5.30nMAssay Description:Inhibition of Wistar rat brain AChE using acetylthiochloline iodide as substrate after 30 mins by Ellman's methodMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetAcetylcholinesterase(Rattus norvegicus (rat))
Institute Of Science

Curated by ChEMBL
LigandPNGBDBM8963(CHEMBL32823 | Homodimeric Tacrine Analog 3b | N-[7...)
Affinity DataIC50:  4.10nMAssay Description:Inhibition of AChE in Wistar rat brain cortex using acetylthiocholine iodide as substrate by Ellman's colorimetric methodMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetAcetylcholinesterase(Rattus norvegicus (rat))
Institute Of Science

Curated by ChEMBL
LigandPNGBDBM8963(CHEMBL32823 | Homodimeric Tacrine Analog 3b | N-[7...)
Affinity DataIC50:  0.200nMpH: 7.4 T: 2°CAssay Description:The cholinesterase assays were performed using colorimetric method reported by Ellman. Enzyme activity was determined by measuring the absorbance at...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetAcetylcholinesterase(Rattus norvegicus (rat))
Institute Of Science

Curated by ChEMBL
LigandPNGBDBM8963(CHEMBL32823 | Homodimeric Tacrine Analog 3b | N-[7...)
Affinity DataIC50:  1.5nMAssay Description:Inhibition of rat AChEMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetAcetylcholinesterase(Rattus norvegicus (rat))
Institute Of Science

Curated by ChEMBL
LigandPNGBDBM8963(CHEMBL32823 | Homodimeric Tacrine Analog 3b | N-[7...)
Affinity DataIC50:  0.400nMAssay Description:Inhibition of rat cortex AChE using acetylthiocholine iodide as substrate measured after 8 mins in presence of BuChE inhibitor ethopropazine by Ellma...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetAcetylcholinesterase(Mus musculus (mouse))TBA
LigandPNGBDBM8963(CHEMBL32823 | Homodimeric Tacrine Analog 3b | N-[7...)
Affinity DataIC50:  1.90nMAssay Description:Inhibition of mouse brain AChEMore data for this Ligand-Target Pair
In DepthDetails PubMed
TargetAcetylcholinesterase(Homo sapiens (Human))
Universita Di Siena

LigandPNGBDBM8963(CHEMBL32823 | Homodimeric Tacrine Analog 3b | N-[7...)
Affinity DataIC50:  0.810nMAssay Description:Inhibition of human AChEMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetAcetylcholinesterase(Mus musculus (mouse))TBA
LigandPNGBDBM8963(CHEMBL32823 | Homodimeric Tacrine Analog 3b | N-[7...)
Affinity DataIC50:  1.90nMAssay Description:Inhibition of AChE in Swiss Webster mouse cerebral homogenate using acetylthiocholine iodide as substrate preincubated for 10 mins followed substrate...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetAcetylcholinesterase(Homo sapiens (Human))
Universita Di Siena

LigandPNGBDBM8963(CHEMBL32823 | Homodimeric Tacrine Analog 3b | N-[7...)
Affinity DataIC50:  0.400nMAssay Description:Inhibition of AChE (unknown origin)More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetAcetylcholinesterase(Rattus norvegicus (rat))
Institute Of Science

Curated by ChEMBL
LigandPNGBDBM8963(CHEMBL32823 | Homodimeric Tacrine Analog 3b | N-[7...)
Affinity DataIC50:  0.400nMAssay Description:Inhibition of rat brain Acetylcholinesterase using acetylthiocholine as substrate in presence of BChE inhibitor ethopropazine by spectrophotometric m...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetAcetylcholinesterase(Homo sapiens (Human))
Universita Di Siena

LigandPNGBDBM8963(CHEMBL32823 | Homodimeric Tacrine Analog 3b | N-[7...)
Affinity DataIC50:  0.810nMAssay Description:Inhibition of human recombinant AChE using acetylthiocholine iodide as substrate preincubated with enzyme for 20 mins followed by susbtrate addition ...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetAcetylcholinesterase(Rattus norvegicus (rat))
Institute Of Science

Curated by ChEMBL
LigandPNGBDBM8963(CHEMBL32823 | Homodimeric Tacrine Analog 3b | N-[7...)
Affinity DataIC50:  1.5nMAssay Description:The cholinesterase assays were performed using colorimetric method reported by Ellman. Enzyme activity was determined by measuring the absorbance at...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed