Compile Data Set for Download or QSAR
Report error Found 33 Enz. Inhib. hit(s) with Target = 'Isoform Alpha-4-2 of Neuronal acetylcholine receptor subunit alpha-4 (Alpha-4-2)'
LigandPNGBDBM184561(US9150581, RTI-7527-(-)-102 | US9150581, RTI-7527-...)
Affinity DataKi:  0.00900nMAssay Description:The Ki values for the inhibition of [3H]epibatidine binding at the α4β2 nAChR in male rat cerebral cortex for compounds are listed in Table...More data for this Ligand-Target Pair
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Date in BDB:
6/20/2016
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LigandPNGBDBM50143320(2-(6-Chloro-pyridin-3-yl)-7-aza-bicyclo[2.2.1]hept...)
Affinity DataKi:  0.0180nM ΔG°:  -61.3kJ/molepH: 7.4 T: 2°CAssay Description:Adult male rat cerebral cortices (Pelfreeze Biological, Rogers, Ark.) were homogenized in 39 volumes of ice-cold 50 mM Tris buffer (pH 7.4 at 4° C.) ...More data for this Ligand-Target Pair
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Date in BDB:
4/4/2017
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LigandPNGBDBM184561(US9150581, RTI-7527-(-)-102 | US9150581, RTI-7527-...)
Affinity DataKi:  0.0210nMAssay Description:The Ki values for the inhibition of [3H]epibatidine binding at the α4β2 nAChR in male rat cerebral cortex for compounds are listed in Table...More data for this Ligand-Target Pair
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Date in BDB:
6/20/2016
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LigandPNGBDBM184561(US9150581, RTI-7527-(-)-102 | US9150581, RTI-7527-...)
Affinity DataKi:  0.0220nMAssay Description:The Ki values for the inhibition of [3H]epibatidine binding at the α4β2 nAChR in male rat cerebral cortex for compounds are listed in Table...More data for this Ligand-Target Pair
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Date in BDB:
6/20/2016
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LigandPNGBDBM50395218(CHEMBL2164666 | US9150581, RTI-7527-192)
Affinity DataKi:  0.0300nMAssay Description:The Ki values for the inhibition of [3H]epibatidine binding at the α4β2 nAChR in male rat cerebral cortex for compounds are listed in Table...More data for this Ligand-Target Pair
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Date in BDB:
6/20/2016
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LigandPNGBDBM221044(US9284322, Table 6, Compound 10)
Affinity DataKi:  0.0400nM ΔG°:  -59.3kJ/molepH: 7.4 T: 2°CAssay Description:Adult male rat cerebral cortices (Pelfreeze Biological, Rogers, Ark.) were homogenized in 39 volumes of ice-cold 50 mM Tris buffer (pH 7.4 at 4° C.) ...More data for this Ligand-Target Pair
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Date in BDB:
4/4/2017
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LigandPNGBDBM221036(US9284322, Table 6, Compound 2)
Affinity DataKi:  0.0490nM ΔG°:  -58.8kJ/molepH: 7.4 T: 2°CAssay Description:Adult male rat cerebral cortices (Pelfreeze Biological, Rogers, Ark.) were homogenized in 39 volumes of ice-cold 50 mM Tris buffer (pH 7.4 at 4° C.) ...More data for this Ligand-Target Pair
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Date in BDB:
4/4/2017
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LigandPNGBDBM221037(US9284322, Table 6, Compound 3)
Affinity DataKi:  0.0630nM ΔG°:  -58.2kJ/molepH: 7.4 T: 2°CAssay Description:Adult male rat cerebral cortices (Pelfreeze Biological, Rogers, Ark.) were homogenized in 39 volumes of ice-cold 50 mM Tris buffer (pH 7.4 at 4° C.) ...More data for this Ligand-Target Pair
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Date in BDB:
4/4/2017
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LigandPNGBDBM221041(US9284322, Table 6, Compound 7)
Affinity DataKi:  0.0670nM ΔG°:  -58.1kJ/molepH: 7.4 T: 2°CAssay Description:Adult male rat cerebral cortices (Pelfreeze Biological, Rogers, Ark.) were homogenized in 39 volumes of ice-cold 50 mM Tris buffer (pH 7.4 at 4° C.) ...More data for this Ligand-Target Pair
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Date in BDB:
4/4/2017
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LigandPNGBDBM86805(CAS_45263788 | NSC_45263788 | rac-2-(5-(3-chloroph...)
Affinity DataKi:  0.0730nMAssay Description:The Ki values for the inhibition of [3H]epibatidine binding at the α4β2 nAChR in male rat cerebral cortex for compounds are listed in Table...More data for this Ligand-Target Pair
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Date in BDB:
6/20/2016
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LigandPNGBDBM50395220(CHEMBL2164664 | US9150581, RTI-7527-(+/-)-154)
Affinity DataKi:  0.0800nMAssay Description:The Ki values for the inhibition of [3H]epibatidine binding at the α4β2 nAChR in male rat cerebral cortex for compounds are listed in Table...More data for this Ligand-Target Pair
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Date in BDB:
6/20/2016
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LigandPNGBDBM50395220(CHEMBL2164664 | US9150581, RTI-7527-(+/-)-154)
Affinity DataKi:  0.0820nMAssay Description:The Ki values for the inhibition of [3H]epibatidine binding at the α4β2 nAChR in male rat cerebral cortex for compounds are listed in Table...More data for this Ligand-Target Pair
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Date in BDB:
6/20/2016
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LigandPNGBDBM221040(US9284322, Table 6, Compound 6)
Affinity DataKi:  0.120nM ΔG°:  -56.6kJ/molepH: 7.4 T: 2°CAssay Description:Adult male rat cerebral cortices (Pelfreeze Biological, Rogers, Ark.) were homogenized in 39 volumes of ice-cold 50 mM Tris buffer (pH 7.4 at 4° C.) ...More data for this Ligand-Target Pair
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Date in BDB:
4/4/2017
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LigandPNGBDBM221048(US9303017, Varenicline | US9284322, varenicline)
Affinity DataKi:  0.120nM ΔG°:  -56.6kJ/molepH: 7.4 T: 2°CAssay Description:Adult male rat cerebral cortices (Pelfreeze Biological, Rogers, Ark.) were homogenized in 39 volumes of ice-cold 50 mM Tris buffer (pH 7.4 at 4° C.) ...More data for this Ligand-Target Pair
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Date in BDB:
4/4/2017
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PDB3D3D Structure (crystal)
LigandPNGBDBM50395217(CHEMBL2164667 | US9150581, RTI-7527-168)
Affinity DataKi:  0.120nMAssay Description:The Ki values for the inhibition of [3H]epibatidine binding at the α4β2 nAChR in male rat cerebral cortex for compounds are listed in Table...More data for this Ligand-Target Pair
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Date in BDB:
6/20/2016
Entry Details
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LigandPNGBDBM221045(US9284322, Table 7, Compound 1)
Affinity DataKi:  0.120nM ΔG°:  -56.6kJ/molepH: 7.4 T: 2°CAssay Description:Adult male rat cerebral cortices (Pelfreeze Biological, Rogers, Ark.) were homogenized in 39 volumes of ice-cold 50 mM Tris buffer (pH 7.4 at 4° C.) ...More data for this Ligand-Target Pair
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Date in BDB:
4/4/2017
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LigandPNGBDBM221039(US9284322, Table 6, Compound 5)
Affinity DataKi:  0.130nM ΔG°:  -56.4kJ/molepH: 7.4 T: 2°CAssay Description:Adult male rat cerebral cortices (Pelfreeze Biological, Rogers, Ark.) were homogenized in 39 volumes of ice-cold 50 mM Tris buffer (pH 7.4 at 4° C.) ...More data for this Ligand-Target Pair
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Date in BDB:
4/4/2017
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LigandPNGBDBM221043(US9284322, Table 6, Compound 9)
Affinity DataKi:  0.130nM ΔG°:  -56.4kJ/molepH: 7.4 T: 2°CAssay Description:Adult male rat cerebral cortices (Pelfreeze Biological, Rogers, Ark.) were homogenized in 39 volumes of ice-cold 50 mM Tris buffer (pH 7.4 at 4° C.) ...More data for this Ligand-Target Pair
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Date in BDB:
4/4/2017
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LigandPNGBDBM50395220(CHEMBL2164664 | US9150581, RTI-7527-(+/-)-154)
Affinity DataKi:  0.170nMAssay Description:The Ki values for the inhibition of [3H]epibatidine binding at the α4β2 nAChR in male rat cerebral cortex for compounds are listed in Table...More data for this Ligand-Target Pair
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Date in BDB:
6/20/2016
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LigandPNGBDBM50171007(4-[5-(7-Aza-bicyclo[2.2.1]hept-2-yl)-2-fluoro-pyri...)
Affinity DataKi:  0.190nMAssay Description:The Ki values for the inhibition of [3H]epibatidine binding at the α4β2 nAChR in male rat cerebral cortex for compounds are listed in Table...More data for this Ligand-Target Pair
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Date in BDB:
6/20/2016
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LigandPNGBDBM86806(NSC_45263762 | CAS_45263762 | rac-2-(6-fluoro-5-ph...)
Affinity DataKi:  0.240nMAssay Description:The Ki values for the inhibition of [3H]epibatidine binding at the α4β2 nAChR in male rat cerebral cortex for compounds are listed in Table...More data for this Ligand-Target Pair
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Date in BDB:
6/20/2016
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LigandPNGBDBM86806(NSC_45263762 | CAS_45263762 | rac-2-(6-fluoro-5-ph...)
Affinity DataKi:  0.240nMAssay Description:The Ki values for the inhibition of [3H]epibatidine binding at the α4β2 nAChR in male rat cerebral cortex for compounds are listed in Table...More data for this Ligand-Target Pair
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Date in BDB:
6/20/2016
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LigandPNGBDBM221038(US9284322, Table 6, Compound 4)
Affinity DataKi:  0.25nM ΔG°:  -54.8kJ/molepH: 7.4 T: 2°CAssay Description:Adult male rat cerebral cortices (Pelfreeze Biological, Rogers, Ark.) were homogenized in 39 volumes of ice-cold 50 mM Tris buffer (pH 7.4 at 4° C.) ...More data for this Ligand-Target Pair
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Date in BDB:
4/4/2017
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LigandPNGBDBM86806(NSC_45263762 | CAS_45263762 | rac-2-(6-fluoro-5-ph...)
Affinity DataKi:  0.260nMAssay Description:The Ki values for the inhibition of [3H]epibatidine binding at the α4β2 nAChR in male rat cerebral cortex for compounds are listed in Table...More data for this Ligand-Target Pair
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Date in BDB:
6/20/2016
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LigandPNGBDBM221049(US9284322, Table 7, Compound 3)
Affinity DataKi:  0.320nM ΔG°:  -54.2kJ/molepH: 7.4 T: 2°CAssay Description:Adult male rat cerebral cortices (Pelfreeze Biological, Rogers, Ark.) were homogenized in 39 volumes of ice-cold 50 mM Tris buffer (pH 7.4 at 4° C.) ...More data for this Ligand-Target Pair
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Date in BDB:
4/4/2017
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LigandPNGBDBM221035(US9284322, Table 6, Compound 1)
Affinity DataKi:  0.350nM ΔG°:  -54.0kJ/molepH: 7.4 T: 2°CAssay Description:Adult male rat cerebral cortices (Pelfreeze Biological, Rogers, Ark.) were homogenized in 39 volumes of ice-cold 50 mM Tris buffer (pH 7.4 at 4° C.) ...More data for this Ligand-Target Pair
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Date in BDB:
4/4/2017
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LigandPNGBDBM184563(US9150581, RTI-7527-169)
Affinity DataKi:  0.360nMAssay Description:The Ki values for the inhibition of [3H]epibatidine binding at the α4β2 nAChR in male rat cerebral cortex for compounds are listed in Table...More data for this Ligand-Target Pair
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Date in BDB:
6/20/2016
Entry Details
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LigandPNGBDBM50395221(CHEMBL2164663 | US9150581, RTI-7527-153)
Affinity DataKi:  0.440nMAssay Description:The Ki values for the inhibition of [3H]epibatidine binding at the α4β2 nAChR in male rat cerebral cortex for compounds are listed in Table...More data for this Ligand-Target Pair
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Date in BDB:
6/20/2016
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LigandPNGBDBM184560(US9150581, RTI-7527-107)
Affinity DataKi:  0.530nMAssay Description:The Ki values for the inhibition of [3H]epibatidine binding at the α4β2 nAChR in male rat cerebral cortex for compounds are listed in Table...More data for this Ligand-Target Pair
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Date in BDB:
6/20/2016
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LigandPNGBDBM221046(US9284322, Table 7, Compound 2)
Affinity DataKi:  0.840nM ΔG°:  -51.8kJ/molepH: 7.4 T: 2°CAssay Description:Adult male rat cerebral cortices (Pelfreeze Biological, Rogers, Ark.) were homogenized in 39 volumes of ice-cold 50 mM Tris buffer (pH 7.4 at 4° C.) ...More data for this Ligand-Target Pair
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Date in BDB:
4/4/2017
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LigandPNGBDBM50395219(CHEMBL2164665 | US9150581, RTI-7527-193)
Affinity DataKi:  0.940nMAssay Description:The Ki values for the inhibition of [3H]epibatidine binding at the α4β2 nAChR in male rat cerebral cortex for compounds are listed in Table...More data for this Ligand-Target Pair
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Date in BDB:
6/20/2016
Entry Details
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LigandPNGBDBM221042(US9284322, Table 6, Compound 8)
Affinity DataKi:  1.18nM ΔG°:  -51.0kJ/molepH: 7.4 T: 2°CAssay Description:Adult male rat cerebral cortices (Pelfreeze Biological, Rogers, Ark.) were homogenized in 39 volumes of ice-cold 50 mM Tris buffer (pH 7.4 at 4° C.) ...More data for this Ligand-Target Pair
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Date in BDB:
4/4/2017
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LigandPNGBDBM50004108((R,S)-nicotine | (RS)-nicotine | nicotine | (+-)-n...)
Affinity DataKi:  1.5nM ΔG°:  -50.4kJ/molepH: 7.4 T: 2°CAssay Description:Adult male rat cerebral cortices (Pelfreeze Biological, Rogers, Ark.) were homogenized in 39 volumes of ice-cold 50 mM Tris buffer (pH 7.4 at 4° C.) ...More data for this Ligand-Target Pair
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Date in BDB:
4/4/2017
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