mecamylamine [Ligand Id: 3990] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL267936 (Mecamylamine) |
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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 Pestic 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 Pestic 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: 462, 475, 471, 477, 476] [UniProtKB: P02708, P07510, P11230, Q04844, Q07001] | ||||||||
| 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: 464, 465, 463, 472, 473, 474, 466, 467, 469, 468, 470] [UniProtKB: P32297, P43681, Q15822, P17787, Q05901, P30926, P30532, Q15825, Q9UGM1, P36544, Q9GZZ6] | ||||||||
| 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: 464, 465, 463, 472, 473, 474, 466, 467, 469, 468, 470] [UniProtKB: P04757, P09483, P12389, P12390, P12391, P12392, P20420, P43143, P43144, Q05941, Q9JLB5] | ||||||||
| 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: 474, 463] [UniProtKB: P30926, Q15822] | ||||||||
| 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: 472, 464] [UniProtKB: P17787, P32297] | ||||||||
| 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: 474, 464] [UniProtKB: P30926, P32297] | ||||||||
| 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: 472, 465] [UniProtKB: P17787, P43681] | ||||||||
| 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 33:
Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
Davies M, Nowotka M, Papadatos G, Dedman N, Gaulton A, Atkinson F, Bellis L, Overington JP. (2015) 'ChEMBL web services: streamlining access to drug discovery data and utilities.' Nucleic Acids Res., 43(W1). DOI: 10.1093/nar/gkv352. [EPMCID:25883136]
