tripitramine [Ligand Id: 361] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL265256 (Tripitramine)
  • M1 receptor/Muscarinic acetylcholine receptor M1 in Human [ChEMBL: CHEMBL216] [GtoPdb: 13] [UniProtKB: P11229]
  • M1 receptor/Muscarinic acetylcholine receptor M1 in Rat [ChEMBL: CHEMBL276] [GtoPdb: 13] [UniProtKB: P08482]
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  • M2 receptor/Muscarinic acetylcholine receptor M2 in Human [ChEMBL: CHEMBL211] [GtoPdb: 14] [UniProtKB: P08172]
  • M2 receptor/Muscarinic acetylcholine receptor M2 in Rat [ChEMBL: CHEMBL309] [GtoPdb: 14] [UniProtKB: P10980]
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  • M3 receptor/Muscarinic acetylcholine receptor M3 in Human [ChEMBL: CHEMBL245] [GtoPdb: 15] [UniProtKB: P20309]
  • M3 receptor/Muscarinic acetylcholine receptor M3 in Rat [ChEMBL: CHEMBL320] [GtoPdb: 15] [UniProtKB: P08483]
  • Muscarinic acetylcholine receptor M3 in Guinea pig [ChEMBL: CHEMBL5498] [UniProtKB: Q8VH26]
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  • M4 receptor/Muscarinic acetylcholine receptor M4 in Human [ChEMBL: CHEMBL1821] [GtoPdb: 16] [UniProtKB: P08173]
  • M4 receptor/Muscarinic acetylcholine receptor M4 in Rat [ChEMBL: CHEMBL317] [GtoPdb: 16] [UniProtKB: P08485]
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  • M5 receptor/Muscarinic acetylcholine receptor M5 in Human [ChEMBL: CHEMBL2035] [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]
ChEMBL Displacement of [3H]N-methylscopolamine chloride from human cloned muscarinic M1 receptor expressed in CHOK1 cells B 8.45 pKi 3.55 nM Ki Bioorg. Med. Chem. (2008) 16: 7311-7320 [PMID:18595721]
ChEMBL Affinity for Muscarinic acetylcholine receptor M1 expressed in CHO cells by [3H]NMS displacement. B 8.8 pKi 1.58 nM Ki Bioorg. Med. Chem. Lett. (2001) 11: 1241-1243 [PMID:11354386]
GtoPdb - - 8.8 pKi - - - Eur J Pharmacol (1994) 268: 459-462 [PMID:7805774]
M1 receptor/Muscarinic acetylcholine receptor M1 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL276] [GtoPdb: 13] [UniProtKB: P08482]
ChEMBL Affinity constant measured against M1 muscarinic receptor in rat cortex B 7.63 pKi 23.44 nM Ki J. Med. Chem. (1993) 36: 3734-3737 [PMID:8246244]
ChEMBL Tested for affinity constant against M1 muscarinic receptor in rat cortex using [3H]pirenzepine B 7.63 pKi 23.44 nM Ki J. Med. Chem. (1994) 37: 3363-3372 [PMID:7932564]
ChEMBL Binding affinity for rat cortex Muscarinic acetylcholine receptor M1 B 8.45 pKi 3.55 nM Ki J. Med. Chem. (1998) 41: 4150-4160 [PMID:9767650]
M2 receptor/Muscarinic acetylcholine receptor M2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL211] [GtoPdb: 14] [UniProtKB: P08172]
ChEMBL Antagonist affinity evaluated against Muscarinic acetylcholine receptor M2 in isolated guinea pig left atrium F 9.65 pKd 0.22 nM Kd J. Med. Chem. (1998) 41: 4150-4160 [PMID:9767650]
ChEMBL Antagonistic activity measured in isolated guinea pig left atrium (M2 receptor) F 9.75 pKd 0.18 nM Kd J. Med. Chem. (1993) 36: 3734-3737 [PMID:8246244]
ChEMBL Antagonistic activity against M2 muscarinic receptor in guinea pig left atrium derived by plotting log(DR - 1) vs log[antagonist] F 9.75 pKd 0.18 nM Kd J. Med. Chem. (1994) 37: 3363-3372 [PMID:7932564]
ChEMBL Displacement of [3H]N-methylscopolamine chloride from human cloned muscarinic M2 receptor expressed in CHOK1 cells B 9.52 pKi 0.3 nM Ki Bioorg. Med. Chem. (2008) 16: 7311-7320 [PMID:18595721]
ChEMBL Affinity for Muscarinic acetylcholine receptor M2 expressed in CHO cells by [3H]NMS displacement. B 9.57 pKi 0.27 nM Ki Bioorg. Med. Chem. Lett. (2001) 11: 1241-1243 [PMID:11354386]
GtoPdb - - 9.6 pKi - - - Eur J Pharmacol (1994) 268: 459-462 [PMID:7805774]
M2 receptor/Muscarinic acetylcholine receptor M2 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL309] [GtoPdb: 14] [UniProtKB: P10980]
ChEMBL Inhibition of [3H]NMS binding to rat heart Muscarinic acetylcholine receptor M2 B 9.52 pKi 0.3 nM Ki J. Med. Chem. (1998) 41: 4150-4160 [PMID:9767650]
ChEMBL Affinity constant measured against M2 muscarinic receptor in rat heart r B 9.54 pKi 0.29 nM Ki J. Med. Chem. (1993) 36: 3734-3737 [PMID:8246244]
ChEMBL Tested for affinity constant against M2 muscarinic receptor rat heart using [3H]-NMS B 9.54 pKi 0.29 nM Ki J. Med. Chem. (1994) 37: 3363-3372 [PMID:7932564]
M3 receptor/Muscarinic acetylcholine receptor M3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL245] [GtoPdb: 15] [UniProtKB: P20309]
GtoPdb - - 6.83 pKi - - - Bioorg Med Chem (2008) 16: 7311-20 [PMID:18595721]
ChEMBL Displacement of [3H]N-methylscopolamine chloride from human cloned muscarinic M3 receptor expressed in CHOK1 cells B 6.83 pKi 147.91 nM Ki Bioorg. Med. Chem. (2008) 16: 7311-7320 [PMID:18595721]
ChEMBL Affinity for Muscarinic acetylcholine receptor M3 expressed in CHO cells by [3H]-NMS displacement. B 7.42 pKi 38.02 nM Ki Bioorg. Med. Chem. Lett. (2001) 11: 1241-1243 [PMID:11354386]
M3 receptor/Muscarinic acetylcholine receptor M3 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL320] [GtoPdb: 15] [UniProtKB: P08483]
ChEMBL Affinity constant measured against M3 muscarinic receptor in rat submaxillary gland B 6.19 pKi 645.65 nM Ki J. Med. Chem. (1993) 36: 3734-3737 [PMID:8246244]
ChEMBL Tested for affinity constant against M3 muscarinic receptor in rat submaxillary gland using [3H]NMS B 6.19 pKi 645.65 nM Ki J. Med. Chem. (1994) 37: 3363-3372 [PMID:7932564]
ChEMBL Inhibition of [3H]NMS binding to rat submaxillary gland Muscarinic acetylcholine receptor M3 B 6.83 pKi 147.91 nM Ki J. Med. Chem. (1998) 41: 4150-4160 [PMID:9767650]
Muscarinic acetylcholine receptor M3 in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5498] [UniProtKB: Q8VH26]
ChEMBL Antagonistic activity measured in isolated guinea pig left ileum (M3 receptor) F 6.55 pKd 281.84 nM Kd J. Med. Chem. (1993) 36: 3734-3737 [PMID:8246244]
ChEMBL Antagonist affinity evaluated against Muscarinic acetylcholine receptor M3 in isolated guinea pig longitudinal Ileum. F 6.55 pKd 281.84 nM Kd J. Med. Chem. (1998) 41: 4150-4160 [PMID:9767650]
ChEMBL Antagonistic activity against M3 muscarinic receptor in guinea pig left ileum derived by plotting log(DR - 1) vs log[antagonist] F 6.55 pKd 281.84 nM Kd J. Med. Chem. (1994) 37: 3363-3372 [PMID:7932564]
M4 receptor/Muscarinic acetylcholine receptor M4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1821] [GtoPdb: 16] [UniProtKB: P08173]
GtoPdb - - 7.94 pKi - - - Bioorg Med Chem (2008) 16: 7311-20 [PMID:18595721]
ChEMBL Displacement of [3H]N-methylscopolamine chloride from human cloned muscarinic M4 receptor expressed in CHOK1 cells B 7.94 pKi 11.48 nM Ki Bioorg. Med. Chem. (2008) 16: 7311-7320 [PMID:18595721]
ChEMBL Affinity for Muscarinic acetylcholine receptor M4 expressed in CHO cells by [3H]NMS displacement. B 8.19 pKi 6.46 nM Ki Bioorg. Med. Chem. Lett. (2001) 11: 1241-1243 [PMID:11354386]
M4 receptor/Muscarinic acetylcholine receptor M4 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL317] [GtoPdb: 16] [UniProtKB: P08485]
ChEMBL Affinity constant measured against M4 muscarinic receptor rat NG108-15 cells B 7.93 pKi 11.75 nM Ki J. Med. Chem. (1993) 36: 3734-3737 [PMID:8246244]
ChEMBL Inhibition of NG 108-15 binding to Muscarinic acetylcholine receptor M4 B 7.94 pKi 11.48 nM Ki J. Med. Chem. (1998) 41: 4150-4160 [PMID:9767650]
M5 receptor/Muscarinic acetylcholine receptor M5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2035] [GtoPdb: 17] [UniProtKB: P08912]
ChEMBL Affinity for Muscarinic acetylcholine receptor M5 expressed in CHO cells by [3H]NMS displacement. B 7.47 pKi 33.88 nM Ki Bioorg. Med. Chem. Lett. (2001) 11: 1241-1243 [PMID:11354386]
GtoPdb - - 7.5 pKi - - - Eur J Pharmacol (1994) 268: 459-462 [PMID:7805774]

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]