mecamylamine [Ligand Id: 3990] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL267936 (Mecamylamine)
  • Acetylcholine receptor protein alpha chain in Torpedo californica [ChEMBL: CHEMBL3097] [UniProtKB: P02710]
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  • nicotinic acetylcholine receptor α1 subunit/nicotinic acetylcholine receptor γ subunit/nicotinic acetylcholine receptor β1 subunit/nicotinic acetylcholine receptor ε subunit/nicotinic acetylcholine receptor δ subunit/Muscle-type nicotinic acetylcholine receptor in Human [ChEMBL: CHEMBL2362997] [GtoPdb: 462475471477476] [UniProtKB: P02708P07510P11230Q04844Q07001]
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  • nicotinic acetylcholine receptor α3 subunit/nicotinic acetylcholine receptor α4 subunit/nicotinic acetylcholine receptor α2 subunit/nicotinic acetylcholine receptor β2 subunit/nicotinic acetylcholine receptor β3 subunit/nicotinic acetylcholine receptor β4 subunit/nicotinic acetylcholine receptor α5 subunit/nicotinic acetylcholine receptor α6 subunit/nicotinic acetylcholine receptor α9 subunit/nicotinic acetylcholine receptor α7 subunit/nicotinic acetylcholine receptor α10 subunit in Human [GtoPdb: 464465463472473474466467469468470] [UniProtKB: P32297P43681Q15822P17787Q05901P30926P30532Q15825Q9UGM1P36544Q9GZZ6]
  • nicotinic acetylcholine receptor α3 subunit/nicotinic acetylcholine receptor α4 subunit/nicotinic acetylcholine receptor α2 subunit/nicotinic acetylcholine receptor β2 subunit/nicotinic acetylcholine receptor β3 subunit/nicotinic acetylcholine receptor β4 subunit/nicotinic acetylcholine receptor α5 subunit/nicotinic acetylcholine receptor α6 subunit/nicotinic acetylcholine receptor α9 subunit/nicotinic acetylcholine receptor α7 subunit/nicotinic acetylcholine receptor α10 subunit/Neuronal acetylcholine receptor in Rat [ChEMBL: CHEMBL2094110] [GtoPdb: 464465463472473474466467469468470] [UniProtKB: P04757P09483P12389P12390P12391P12392P20420P43143P43144Q05941Q9JLB5]
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  • nicotinic acetylcholine receptor β4 subunit/nicotinic acetylcholine receptor α2 subunit/Neuronal acetylcholine receptor; alpha2/beta4 in Human [ChEMBL: CHEMBL2109230] [GtoPdb: 474463] [UniProtKB: P30926Q15822]
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  • nicotinic acetylcholine receptor β2 subunit/nicotinic acetylcholine receptor α3 subunit/Neuronal acetylcholine receptor; alpha3/beta2 in Human [ChEMBL: CHEMBL2109234] [GtoPdb: 472464] [UniProtKB: P17787P32297]
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  • nicotinic acetylcholine receptor β4 subunit/nicotinic acetylcholine receptor α3 subunit/Neuronal acetylcholine receptor; alpha3/beta4 in Human [ChEMBL: CHEMBL1907594] [GtoPdb: 474464] [UniProtKB: P30926P32297]
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  • nicotinic acetylcholine receptor β2 subunit/nicotinic acetylcholine receptor α4 subunit/Neuronal acetylcholine receptor; alpha4/beta2 in Human [ChEMBL: CHEMBL1907589] [GtoPdb: 472465] [UniProtKB: P17787P43681]
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  • nicotinic acetylcholine receptor α7 subunit/Neuronal acetylcholine receptor protein alpha-7 subunit in Human [ChEMBL: CHEMBL2492] [GtoPdb: 468] [UniProtKB: P36544]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
Acetylcholine receptor protein alpha chain in Torpedo californica (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3097] [UniProtKB: P02710]
ChEMBL Displacement of [3H]PCP from nAChR in Torpedo nobiliana electric organs membranes by scintillation counting method B 4.61 pIC50 24700 nM IC50 J Pesticide Sci (1995) 20: 49-56
ChEMBL Displacement of [3H]PCP from nAChR in Torpedo nobiliana electric organs membranes in presence of 100 uM carbachol by scintillation counting method B 6.22 pIC50 596 nM IC50 J Pesticide Sci (1995) 20: 49-56
nicotinic acetylcholine receptor α1 subunit/nicotinic acetylcholine receptor γ subunit/nicotinic acetylcholine receptor β1 subunit/nicotinic acetylcholine receptor ε subunit/nicotinic acetylcholine receptor δ subunit/Muscle-type nicotinic acetylcholine receptor in Human (target type: PROTEIN COMPLEX GROUP) [ChEMBL: CHEMBL2362997] [GtoPdb: 462475471477476] [UniProtKB: P02708P07510P11230Q04844Q07001]
GtoPdb - - 5.82 pIC50 ~1500 nM IC50
ChEMBL Compound was evaluated for functional potencies and efficacies at human muscle type Nicotinic acetylcholine receptor in TE671 cells B 4.52 pEC50 30000 nM EC50 J. Med. Chem. (1997) 40: 4169-4194 [PMID:9435889]
nicotinic acetylcholine receptor α3 subunit/nicotinic acetylcholine receptor α4 subunit/nicotinic acetylcholine receptor α2 subunit/nicotinic acetylcholine receptor β2 subunit/nicotinic acetylcholine receptor β3 subunit/nicotinic acetylcholine receptor β4 subunit/nicotinic acetylcholine receptor α5 subunit/nicotinic acetylcholine receptor α6 subunit/nicotinic acetylcholine receptor α9 subunit/nicotinic acetylcholine receptor α7 subunit/nicotinic acetylcholine receptor α10 subunit in Human [GtoPdb: 464465463472473474466467469468470] [UniProtKB: P32297P43681Q15822P17787Q05901P30926P30532Q15825Q9UGM1P36544Q9GZZ6]
GtoPdb - - 4.81 pIC50 15600 nM IC50
GtoPdb - - 4.96 pIC50 11000 nM IC50
GtoPdb - - 5.12 pIC50 7600 nM IC50
GtoPdb - - 5.44 pIC50 3600 nM IC50
GtoPdb - - 6.41 pIC50 390 nM IC50
GtoPdb - - 6.48 pIC50 330 nM IC50
nicotinic acetylcholine receptor α3 subunit/nicotinic acetylcholine receptor α4 subunit/nicotinic acetylcholine receptor α2 subunit/nicotinic acetylcholine receptor β2 subunit/nicotinic acetylcholine receptor β3 subunit/nicotinic acetylcholine receptor β4 subunit/nicotinic acetylcholine receptor α5 subunit/nicotinic acetylcholine receptor α6 subunit/nicotinic acetylcholine receptor α9 subunit/nicotinic acetylcholine receptor α7 subunit/nicotinic acetylcholine receptor α10 subunit/Neuronal acetylcholine receptor in Rat (target type: PROTEIN COMPLEX GROUP) [ChEMBL: CHEMBL2094110] [GtoPdb: 464465463472473474466467469468470] [UniProtKB: P04757P09483P12389P12390P12391P12392P20420P43143P43144Q05941Q9JLB5]
ChEMBL Compound was evaluated for functional potency and efficacy at rat Nicotinic acetylcholine receptor in PC12 cells (ganglionic) B 6.7 pEC50 200 nM EC50 J. Med. Chem. (1997) 40: 4169-4194 [PMID:9435889]
nicotinic acetylcholine receptor β4 subunit/nicotinic acetylcholine receptor α2 subunit/Neuronal acetylcholine receptor; alpha2/beta4 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2109230] [GtoPdb: 474463] [UniProtKB: P30926Q15822]
ChEMBL Inhibitory concentration against Nicotinic acetylcholine receptor alpha2-beta4 B 4.8 pIC50 16000 nM IC50 J. Med. Chem. (2005) 48: 4705-4745 [PMID:16033252]
ChEMBL Inhibitory concentration against Nicotinic acetylcholine receptor alpha2-beta4 B 5.51 pIC50 3100 nM IC50 J. Med. Chem. (2005) 48: 4705-4745 [PMID:16033252]
nicotinic acetylcholine receptor β2 subunit/nicotinic acetylcholine receptor α3 subunit/Neuronal acetylcholine receptor; alpha3/beta2 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2109234] [GtoPdb: 472464] [UniProtKB: P17787P32297]
GtoPdb - - 5.12 pIC50 7600 nM IC50
GtoPdb - - 6.41 pIC50 390 nM IC50
ChEMBL Inhibitory concentration against Nicotinic acetylcholine receptor alpha3-beta2 B 6.55 pIC50 280 nM IC50 J. Med. Chem. (2005) 48: 4705-4745 [PMID:16033252]
nicotinic acetylcholine receptor β4 subunit/nicotinic acetylcholine receptor α3 subunit/Neuronal acetylcholine receptor; alpha3/beta4 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL1907594] [GtoPdb: 474464] [UniProtKB: P30926P32297]
GtoPdb - - 5.12 pIC50 7600 nM IC50
ChEMBL Inhibitory concentration against Nicotinic acetylcholine receptor alpha3-beta4 B 5.42 pIC50 3800 nM IC50 J. Med. Chem. (2005) 48: 4705-4745 [PMID:16033252]
ChEMBL Inhibitory concentration against Nicotinic acetylcholine receptor alpha3-beta4 B 5.47 pIC50 3400 nM IC50 J. Med. Chem. (2005) 48: 4705-4745 [PMID:16033252]
ChEMBL Inhibitory concentration against Nicotinic acetylcholine receptor alpha3-beta4 B 5.85 pIC50 1400 nM IC50 J. Med. Chem. (2005) 48: 4705-4745 [PMID:16033252]
ChEMBL Antagonist activity at human alpha3beta4 nAChR expressed in HEK-tsA201 cells assessed as inhibition of epibatidine-induced intracellular calcium level by fluorescence plate reader analysis B 6.15 pIC50 700 nM IC50 Bioorg. Med. Chem. (2013) 21: 4730-4743 [PMID:23757208]
GtoPdb - - 6.41 pIC50 390 nM IC50
ChEMBL Inhibitory activity against nicotinic acetylcholine receptor alpha3-beta4 B 7 pIC50 100 nM IC50 Bioorg. Med. Chem. Lett. (2004) 14: 3739-3742 [PMID:15203153]
nicotinic acetylcholine receptor β2 subunit/nicotinic acetylcholine receptor α4 subunit/Neuronal acetylcholine receptor; alpha4/beta2 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL1907589] [GtoPdb: 472465] [UniProtKB: P17787P43681]
GtoPdb - - 5.44 pIC50 3600 nM IC50
ChEMBL Antagonist activity at human alpha4beta2 nAChR expressed in HEK-tsA201 cells assessed as inhibition of epibatidine-induced intracellular calcium level by fluorescence plate reader analysis B 6.22 pIC50 600 nM IC50 Bioorg. Med. Chem. (2013) 21: 4730-4743 [PMID:23757208]
GtoPdb - - 6.48 pIC50 330 nM IC50
nicotinic acetylcholine receptor α7 subunit/Neuronal acetylcholine receptor protein alpha-7 subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2492] [GtoPdb: 468] [UniProtKB: P36544]
GtoPdb - - 4.81 pIC50 15600 nM IC50
ChEMBL Inhibitory concentration against Nicotinic acetylcholine receptor alpha 7 B 4.91 pIC50 12300 nM IC50 J. Med. Chem. (2005) 48: 4705-4745 [PMID:16033252]
ChEMBL Ability to block activation of acetylcholine-stimulated currents in human alpha-7 homomers expressed in oocytes F 5.74 pIC50 1800 nM IC50 J. Med. Chem. (1997) 40: 4169-4194 [PMID:9435889]
Plasmodium falciparum (target type: ORGANISM) [ChEMBL: CHEMBL364]
ChEMBL In vitro inhibitory activity against multidrug-resistant Plasmodium falciparum W2 Indochina F 4.04 pIC50 91400 nM IC50 J. Med. Chem. (2002) 45: 3195-3209 [PMID:12109904]
ChEMBL Concentration required to reduce chloroquine IC50 by 50% F 5.22 pIC50 6000 nM IC50 J. Med. Chem. (2002) 45: 3195-3209 [PMID:12109904]

ChEMBL data shown on this page come from version 27:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]