brucine [Ligand Id: 342] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL501756 (10,11-dimethoxystrychnine, 2,3-dimethoxystrychnine, Brucinum, NSC-757797)
  • M1 receptor/Muscarinic acetylcholine receptor M1 in Human [ChEMBL: CHEMBL216] [GtoPdb: 13] [UniProtKB: P11229]
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  • M2 receptor in Human [GtoPdb: 14] [UniProtKB: P08172]
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  • M3 receptor in Human [GtoPdb: 15] [UniProtKB: P20309]
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  • M4 receptor in Human [GtoPdb: 16] [UniProtKB: P08173]
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  • M5 receptor in Human [GtoPdb: 17] [UniProtKB: P08912]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
M1 receptor/Muscarinic acetylcholine receptor M1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL216] [GtoPdb: 13] [UniProtKB: P11229]
GtoPdb - - 4.5 pKd - - - Mol Pharmacol (1998) 53: 573-89 [PMID:9495826]
GtoPdb - - 5.8 pKd 1780 nM Kd Mol Pharmacol (1999) 55: 778-86 [PMID:10101037];
Mol Pharmacol (1997) 52: 172-9 [PMID:9224827];
Mol Pharmacol (1998) 53: 573-89 [PMID:9495826]
ChEMBL Competitive inhibition of EGFP-fused human M1 receptor N-terminal truncated at 17 residues expressed in HEK293 cells after 4 hrs by FRET assay in presence of para-LRB-AC42 B 4.35 pKi 44668.36 nM Ki J. Med. Chem. (2012) 55: 2125-2143 [PMID:22329602]
TAS2R10/Taste receptor type 2 member 10 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3559704] [GtoPdb: 666] [UniProtKB: Q9NYW0]
ChEMBL Activity at human TAS2R10 expressed in HEK-293T-Galpha16-gustducin44 cells assessed as effect on calcium response by FLIPR assay F 4.22 pEC50 60000 nM EC50 EP-2267129-B1. Bitter taste receptors (null)
M2 receptor in Human [GtoPdb: 14] [UniProtKB: P08172]
GtoPdb - - 4.3 pKd - - - Mol Pharmacol (1998) 53: 573-89 [PMID:9495826]
GtoPdb - - 4.6 pKd - - - Mol Pharmacol (1997) 52: 172-9 [PMID:9224827];
Mol Pharmacol (1998) 53: 573-89 [PMID:9495826]
M3 receptor in Human [GtoPdb: 15] [UniProtKB: P20309]
GtoPdb - - 4 pKd - - - Mol Pharmacol (1997) 52: 172-9 [PMID:9224827];
Mol Pharmacol (1998) 53: 573-89 [PMID:9495826]
M4 receptor in Human [GtoPdb: 16] [UniProtKB: P08173]
GtoPdb - - 6 pKd - - - Mol Pharmacol (1997) 52: 172-9 [PMID:9224827];
Mol Pharmacol (1998) 53: 573-89 [PMID:9495826]
M5 receptor in Human [GtoPdb: 17] [UniProtKB: P08912]
GtoPdb - - 2.9 pKd - - - Mol Pharmacol (1998) 53: 573-89 [PMID:9495826]

ChEMBL data shown on this page come from version 31:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, Cibrián-Uhalte E, Davies M, Dedman N, Karlsson A, Magariños 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]