mecamylamine [Ligand Id: 3990] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL267936 (Mecamilamina, 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 34:
Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
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]
