pilocarpine [Ligand Id: 305] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL550 (Ocucarpine, Ocusert pilo, Ocusert pilo-20, Ocusert pilo-40, Pilocarpine, Pilocarpinum, Pilocarpol, Pilokarpin, Spersacarpine, Syncarpine) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| Muscarinic acetylcholine receptor DM1 in Drosophila melanogaster (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2366467] [UniProtKB: P16395] | ||||||||
| ChEMBL | Displacement of [3H]QNB from Drosophila melanogaster mAChR by scintillation counting | B | 5.53 | pKi | 2980 | nM | Ki | J Agric Food Chem (2007) 55: 2276-2281 [PMID:17319687] |
| ChEMBL | Displacement of [3H]AF-DX 384 from Drosophila melanogaster mAChR by scintillation counting | B | 5.55 | pKi | 2800 | nM | Ki | J Agric Food Chem (2007) 55: 2276-2281 [PMID:17319687] |
| M1 receptor/Muscarinic acetylcholine receptor M1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL216] [GtoPdb: 13] [UniProtKB: P11229] | ||||||||
| ChEMBL | Binding affinity to muscarinic M1 acetylcholine receptor (unknown origin) | B | 5.57 | pKd | 2691.53 | nM | Kd | J Med Chem (2015) 58: 560-576 [PMID:25478907] |
| ChEMBL | Displacement of [3H]NMS from human muscarinic M1 acetylcholine receptor expressed in CHO cell membranes by radioligand binding assay | B | 5.57 | pKd | 2691.53 | nM | Kd | J Med Chem (2015) 58: 560-576 [PMID:25478907] |
| GtoPdb | - | - | 5.1 | pKi | - | - | - |
Br J Pharmacol (1995) 114: 1241-9 [PMID:7620715]; Mol Pharmacol (1997) 52: 172-9 [PMID:9224827] |
| ChEMBL | Binding affinity to muscarinic M1 acetylcholine receptor (unknown origin) | B | 5.1 | pKi | 7943.28 | nM | Ki | J Med Chem (2015) 58: 560-576 [PMID:25478907] |
| ChEMBL | Binding affinity to human cloned muscarinic M1 receptor expressed in CHO cells | B | 5.18 | pKi | 6606.93 | nM | Ki | Bioorg Med Chem (2008) 16: 3049-3058 [PMID:18182302] |
| ChEMBL | Stimulation of phosphoinositide hydrolysis in A9L cells expressing human m1 receptor | F | 5.06 | pEC50 | 8792 | nM | EC50 | Bioorg Med Chem Lett (1998) 8: 2897-2902 [PMID:9873644] |
| ChEMBL | Partial agonist activity at human muscarinic M1 acetylcholine receptor expressed in CHO cells assessed as increase in IP1 accumulation incubated for 30 mins by FRET based HTRF assay | F | 6.08 | pEC50 | 831.76 | nM | EC50 | J Med Chem (2015) 58: 560-576 [PMID:25478907] |
| ChEMBL | Agonist activity at human m1 muscarinic acetylcholine receptor expressed in HEK293 cells assessed as calcium mobilization by FLIPR assay | F | 7.76 | pEC50 | 17.5 | nM | EC50 | Bioorg Med Chem Lett (2015) 25: 1546-1551 [PMID:25765911] |
| M1 receptor/Muscarinic acetylcholine receptor M1 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3733] [GtoPdb: 13] [UniProtKB: P12657] | ||||||||
| ChEMBL | Tested against Muscarinic acetylcholine receptor M1 expressed in A9 L cell line | B | 5.16 | pEC50 | 6900 | nM | EC50 | J Med Chem (1997) 40: 1230-1246 [PMID:9111297] |
| M1 receptor/Muscarinic acetylcholine receptor M1 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL276] [GtoPdb: 13] [UniProtKB: P08482] | ||||||||
| GtoPdb | - | - | 4.9 | pKi | - | - | - | J Pharmacol Exp Ther (1989) 248: 661-70 [PMID:2537406] |
| ChEMBL | Compound was evaluated for its affinity towards Muscarinic acetylcholine receptor M1, using [3H]- pirenzepine, a radioligand displacement assay in rat hippocampal membranes | B | 5.51 | pKi | 3100 | nM | Ki | Bioorg Med Chem Lett (1995) 5: 1813-1818 |
| ChEMBL | Compound was evaluated for the displacement of the muscarinic QNB in a genetically transformed rat cell line (m1c2) transfected with cloned m1 receptors (m1-QNBm1c2) | B | 5.35 | pIC50 | 4430 | nM | IC50 | Bioorg Med Chem Lett (1991) 1: 147-150 |
| ChEMBL | Ability to displace [3H]pirenzepine (pir) from muscarinic acetylcholine receptor M1 in rat cortical tissue. | B | 6.02 | pIC50 | 960 | nM | IC50 | J Med Chem (1992) 35: 15-27 [PMID:1732522] |
| M2 receptor/Muscarinic acetylcholine receptor M2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL211] [GtoPdb: 14] [UniProtKB: P08172] | ||||||||
| GtoPdb | - | - | 4.9 | pKi | - | - | - |
Br J Pharmacol (1995) 114: 1241-9 [PMID:7620715]; Mol Pharmacol (1997) 52: 172-9 [PMID:9224827] |
| ChEMBL | Binding affinity to human cloned muscarinic M2 receptor expressed in CHO cells | B | 4.92 | pKi | 12022.64 | nM | Ki | Bioorg Med Chem (2008) 16: 3049-3058 [PMID:18182302] |
| ChEMBL | Stimulation of cAMP in CHO cells expressing human m2 receptor | F | 4.2 | pEC50 | 63000 | nM | EC50 | Bioorg Med Chem Lett (1998) 8: 2897-2902 [PMID:9873644] |
| M2 receptor/Muscarinic acetylcholine receptor M2 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL309] [GtoPdb: 14] [UniProtKB: P10980] | ||||||||
| ChEMBL | Central presynaptic activity as effect on electrically evoked acetylcholine release from rat hippocampal slices (M2 model) | F | 5 | pKd | 10000 | nM | Kd | J Med Chem (1992) 35: 15-27 [PMID:1732522] |
| ChEMBL | Compound was evaluated for its affinity towards Muscarinic acetylcholine receptor M2, using [3H]- N-methyl-scopolamine, a radioligand displacement assay in rat heart membranes | B | 5.01 | pKi | 9800 | nM | Ki | Bioorg Med Chem Lett (1995) 5: 1813-1818 |
| ChEMBL | Compound was evaluated for the displacement of the muscarinic QNB in rat heart homogenate containing the pharmacologic M2 receptor (M2-QNB heart) | B | 5.06 | pIC50 | 8800 | nM | IC50 | Bioorg Med Chem Lett (1991) 1: 147-150 |
| M5 receptor/Muscarinic acetylcholine receptor M5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2035] [GtoPdb: 17] [UniProtKB: P08912] | ||||||||
| ChEMBL | Binding affinity to human cloned muscarinic M5 receptor expressed in CHO cells | B | 4.99 | pKi | 10232.93 | nM | Ki | Bioorg Med Chem (2008) 16: 3049-3058 [PMID:18182302] |
| GtoPdb | - | - | 5 | pKi | - | - | - |
J Pharmacol Exp Ther (2005) 315: 313-9 [PMID:16002459]; Mol Pharmacol (2016) 90: 427-36 [PMID:27461343]; J Pharmacol Exp Ther (1995) 274: 378-84 [PMID:7616422] |
| M3 receptor in Human [GtoPdb: 15] [UniProtKB: P20309] | ||||||||
| GtoPdb | - | - | 5.1 | pKi | - | - | - |
Br J Pharmacol (1995) 114: 1241-9 [PMID:7620715]; Mol Pharmacol (1997) 52: 172-9 [PMID:9224827] |
| M4 receptor in Human [GtoPdb: 16] [UniProtKB: P08173] | ||||||||
| GtoPdb | - | - | 5.2 | pKi | - | - | - |
Br J Pharmacol (1995) 114: 1241-9 [PMID:7620715]; Mol Pharmacol (1997) 52: 172-9 [PMID:9224827] |
ChEMBL data shown on this page come from version 32:
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]
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