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 (2015)
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 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]