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Found 33 Enz. Inhib. hit(s) with Target = 'Isoform Alpha-4-2 of Neuronal acetylcholine receptor subunit alpha-4 (Alpha-4-2)'
TargetIsoform Alpha-4-2 of Neuronal acetylcholine receptor subunit alpha-4 (Alpha-4-2)(Rattus norvegicus (Rat))
Research Triangle Institute

US Patent
LigandPNGBDBM184561(US9150581, RTI-7527-(+/-)-102 | US9150581, RTI-752...)
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
In DepthDetails US Patent
LigandPNGBDBM50143320((+)-epibatidine | (-)-1-epidatidine | (1S,2S,4R)-2...)
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
In DepthDetails US Patent
TargetIsoform Alpha-4-2 of Neuronal acetylcholine receptor subunit alpha-4 (Alpha-4-2)(Rattus norvegicus (Rat))
Research Triangle Institute

US Patent
LigandPNGBDBM184561(US9150581, RTI-7527-(+/-)-102 | US9150581, RTI-752...)
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
In DepthDetails US Patent
TargetIsoform Alpha-4-2 of Neuronal acetylcholine receptor subunit alpha-4 (Alpha-4-2)(Rattus norvegicus (Rat))
Research Triangle Institute

US Patent
LigandPNGBDBM184561(US9150581, RTI-7527-(+/-)-102 | US9150581, RTI-752...)
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
In DepthDetails US Patent
TargetIsoform Alpha-4-2 of Neuronal acetylcholine receptor subunit alpha-4 (Alpha-4-2)(Rattus norvegicus (Rat))
Research Triangle Institute

US Patent
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
In DepthDetails US Patent
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
Ligand InfoPC cidPC sid
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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
Ligand InfoPC cidPC sid
In DepthDetails US Patent
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
Ligand InfoPC cidPC sid
In DepthDetails US Patent
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
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetIsoform Alpha-4-2 of Neuronal acetylcholine receptor subunit alpha-4 (Alpha-4-2)(Rattus norvegicus (Rat))
Research Triangle Institute

US Patent
LigandPNGBDBM86805(CAS_45263788 | NSC_45263788 | US9150581, RTI-7527-...)
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
In DepthDetails US Patent
TargetIsoform Alpha-4-2 of Neuronal acetylcholine receptor subunit alpha-4 (Alpha-4-2)(Rattus norvegicus (Rat))
Research Triangle Institute

US Patent
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
In DepthDetails US Patent
TargetIsoform Alpha-4-2 of Neuronal acetylcholine receptor subunit alpha-4 (Alpha-4-2)(Rattus norvegicus (Rat))
Research Triangle Institute

US Patent
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
In DepthDetails US Patent
TargetIsoform Alpha-4-2 of Neuronal acetylcholine receptor subunit alpha-4 (Alpha-4-2)(Rattus norvegicus (Rat))
Research Triangle Institute

US Patent
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
In DepthDetails US Patent
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
Ligand InfoPC cidPC sid
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LigandPNGBDBM221048(US9284322, varenicline | US9303017, 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
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
Ligand InfoPC cidPC sid
In DepthDetails US Patent
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
Ligand InfoPC cidPC sid
In DepthDetails US Patent
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
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetIsoform Alpha-4-2 of Neuronal acetylcholine receptor subunit alpha-4 (Alpha-4-2)(Rattus norvegicus (Rat))
Research Triangle Institute

US Patent
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
In DepthDetails US Patent
TargetIsoform Alpha-4-2 of Neuronal acetylcholine receptor subunit alpha-4 (Alpha-4-2)(Rattus norvegicus (Rat))
Research Triangle Institute

US Patent
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
In DepthDetails US Patent
TargetIsoform Alpha-4-2 of Neuronal acetylcholine receptor subunit alpha-4 (Alpha-4-2)(Rattus norvegicus (Rat))
Research Triangle Institute

US Patent
LigandPNGBDBM86806(CAS_45263762 | NSC_45263762 | US9150581, RTI-7527-...)
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
In DepthDetails US Patent
TargetIsoform Alpha-4-2 of Neuronal acetylcholine receptor subunit alpha-4 (Alpha-4-2)(Rattus norvegicus (Rat))
Research Triangle Institute

US Patent
LigandPNGBDBM86806(CAS_45263762 | NSC_45263762 | US9150581, RTI-7527-...)
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
In DepthDetails US Patent
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
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetIsoform Alpha-4-2 of Neuronal acetylcholine receptor subunit alpha-4 (Alpha-4-2)(Rattus norvegicus (Rat))
Research Triangle Institute

US Patent
LigandPNGBDBM86806(CAS_45263762 | NSC_45263762 | US9150581, RTI-7527-...)
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
In DepthDetails US Patent
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
Ligand InfoPC cidPC sid
In DepthDetails US Patent
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
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetIsoform Alpha-4-2 of Neuronal acetylcholine receptor subunit alpha-4 (Alpha-4-2)(Rattus norvegicus (Rat))
Research Triangle Institute

US Patent
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
In DepthDetails US Patent
TargetIsoform Alpha-4-2 of Neuronal acetylcholine receptor subunit alpha-4 (Alpha-4-2)(Rattus norvegicus (Rat))
Research Triangle Institute

US Patent
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
In DepthDetails US Patent
TargetIsoform Alpha-4-2 of Neuronal acetylcholine receptor subunit alpha-4 (Alpha-4-2)(Rattus norvegicus (Rat))
Research Triangle Institute

US Patent
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
In DepthDetails US Patent
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
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetIsoform Alpha-4-2 of Neuronal acetylcholine receptor subunit alpha-4 (Alpha-4-2)(Rattus norvegicus (Rat))
Research Triangle Institute

US Patent
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
In DepthDetails US Patent
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
Ligand InfoPC cidPC sid
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LigandPNGBDBM50004108((+-)-nicotine | (R,S)-nicotine | (RS)-nicotine | 3...)
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