tripitramine [Ligand Id: 361] activity data from GtoPdb and ChEMBL
Click here for a description of the charts and data table
Please tell us if you are using this feature and what you think!
| ChEMBL ligand: CHEMBL265256 (Tripitramine) |
|---|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
| 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 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]
