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ChEMBL ligand: CHEMBL43383 |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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M1 receptor/Muscarinic acetylcholine receptor M1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL216] [GtoPdb: 13] [UniProtKB: P11229] | ||||||||
ChEMBL | Binding affinity to muscarinic M1 receptor (unknown origin) expressed in CHO cells | B | 7.3 | pKi | 50.12 | nM | Ki | J Med Chem (2019) 62: 5358-5369 [PMID:31074983] |
GtoPdb | - | - | 7.5 | pKi | - | - | - |
J Pharmacol Exp Ther (1991) 256: 727-33 [PMID:1994002]; Eur J Pharmacol (1998) 349: 285-92 [PMID:9671109] |
ChEMBL | Displacement of [3H]-NMS from human muscarinic M1 receptor expressed in stable CHO-K1 cells by radioligand binding assay | B | 7.54 | pKi | 28.84 | nM | Ki | J Med Chem (2019) 62: 5358-5369 [PMID:31074983] |
M1 receptor/Muscarinic acetylcholine receptor M1 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL276] [GtoPdb: 13] [UniProtKB: P08482] | ||||||||
ChEMBL | Tested for affinity constant against M1 muscarinic receptor in rat cortex using [3H]pirenzepine | B | 6.98 | pKi | 104.71 | nM | Ki | J Med Chem (1994) 37: 3363-3372 [PMID:7932564] |
ChEMBL | Affinity constant measured against M1 muscarinic receptor in rat cortex | B | 7.6 | pKi | 25.12 | nM | Ki | J Med Chem (1993) 36: 3734-3737 [PMID:8246244] |
M2 receptor/Muscarinic acetylcholine receptor M2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL211] [GtoPdb: 14] [UniProtKB: P08172] | ||||||||
ChEMBL | Antagonistic activity against M2 muscarinic receptor in guinea pig left atrium derived by plotting log(DR - 1) vs log[antagonist] | F | 8.03 | pKd | 9.33 | nM | Kd | J Med Chem (1994) 37: 3363-3372 [PMID:7932564] |
ChEMBL | Antagonistic activity measured in isolated guinea pig left atrium (M2 receptor) | F | 8.5 | pKd | 3.16 | nM | Kd | J Med Chem (1993) 36: 3734-3737 [PMID:8246244] |
ChEMBL | Binding affinity to muscarinic M2 receptor (unknown origin) expressed in CHO cells | B | 8.3 | pKi | 5.01 | nM | Ki | J Med Chem (2019) 62: 5358-5369 [PMID:31074983] |
ChEMBL | Displacement of [3H]-NMS from human muscarinic M2 receptor expressed in stable CHO-K1 cells by radioligand binding assay | B | 8.37 | pKi | 4.27 | nM | Ki | J Med Chem (2019) 62: 5358-5369 [PMID:31074983] |
GtoPdb | - | - | 8.4 | pKi | - | - | - |
J Pharmacol Exp Ther (1991) 256: 727-33 [PMID:1994002]; Eur J Pharmacol (1998) 349: 285-92 [PMID:9671109] |
M2 receptor/Muscarinic acetylcholine receptor M2 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL309] [GtoPdb: 14] [UniProtKB: P10980] | ||||||||
ChEMBL | Affinity constant measured against M2 muscarinic receptor in rat heart | B | 8.3 | pKi | 5.01 | 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 | 8.49 | pKi | 3.24 | 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] | ||||||||
ChEMBL | Binding affinity to muscarinic M3 receptor (unknown origin) expressed in CHO cells | B | 7 | pKi | 100 | nM | Ki | J Med Chem (2019) 62: 5358-5369 [PMID:31074983] |
ChEMBL | Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in stable CHO-K1 cells by radioligand binding assay | B | 7.2 | pKi | 63.1 | nM | Ki | J Med Chem (2019) 62: 5358-5369 [PMID:31074983] |
GtoPdb | - | - | 7.3 | pKi | - | - | - |
J Pharmacol Exp Ther (1991) 256: 727-33 [PMID:1994002]; Eur J Pharmacol (1998) 349: 285-92 [PMID:9671109] |
M3 receptor/Muscarinic acetylcholine receptor M3 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL320] [GtoPdb: 15] [UniProtKB: P08483] | ||||||||
ChEMBL | Tested for affinity constant against M3 muscarinic receptor in rat submaxillary gland using [3H]NMS | B | 6.6 | pKi | 251.19 | nM | Ki | J Med Chem (1994) 37: 3363-3372 [PMID:7932564] |
ChEMBL | Affinity constant measured against M3 muscarinic receptor in rat submaxillary gland | B | 6.8 | pKi | 158.49 | nM | Ki | J Med Chem (1993) 36: 3734-3737 [PMID:8246244] |
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 | 6.6 | pKd | 251.19 | nM | Kd | J Med Chem (1993) 36: 3734-3737 [PMID:8246244] |
ChEMBL | Antagonistic activity against M3 muscarinic receptor in guinea pig left ileum derived by plotting log(DR - 1) vs log[antagonist] | F | 7 | pKd | 100 | 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] | ||||||||
ChEMBL | Binding affinity to muscarinic M4 receptor (unknown origin) expressed in CHO cells | B | 8.1 | pKi | 7.94 | nM | Ki | J Med Chem (2019) 62: 5358-5369 [PMID:31074983] |
ChEMBL | Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in stable CHO-K1 cells by radioligand binding assay | B | 8.19 | pKi | 6.46 | nM | Ki | J Med Chem (2019) 62: 5358-5369 [PMID:31074983] |
GtoPdb | - | - | 8.2 | pKi | - | - | - |
J Pharmacol Exp Ther (1991) 256: 727-33 [PMID:1994002]; Eur J Pharmacol (1998) 349: 285-92 [PMID:9671109] |
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 | 8 | pKi | 10 | nM | Ki | J Med Chem (1993) 36: 3734-3737 [PMID:8246244] |
M5 receptor/Muscarinic acetylcholine receptor M5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2035] [GtoPdb: 17] [UniProtKB: P08912] | ||||||||
ChEMBL | Binding affinity to muscarinic M5 receptor (unknown origin) expressed in CHO cells | B | 5.9 | pKi | 1258.93 | nM | Ki | J Med Chem (2019) 62: 5358-5369 [PMID:31074983] |
ChEMBL | Displacement of [3H]-NMS from human muscarinic M5 receptor expressed in stable CHO-K1 cells by radioligand binding assay | B | 6.08 | pKi | 831.76 | nM | Ki | J Med Chem (2019) 62: 5358-5369 [PMID:31074983] |
GtoPdb | - | - | 7.8 | pKi | - | - | - |
J Pharmacol Exp Ther (1991) 256: 727-33 [PMID:1994002]; Eur J Pharmacol (1998) 349: 285-92 [PMID:9671109] |
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]