tripitramine [Ligand Id: 361] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL265256 (Tripitramine) |
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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 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]
