pilocarpine [Ligand Id: 305] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL550 (Ocucarpine, 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 | Partial agonist activity at N-terminal FLAG tagged/C-terminal NanoLuc tagged human muscarinic M1 receptor expressed in HEK293T cells using furimazine as substrate assessed as receptor activation preincubated with substrate for 1 min followed by compound addition and measured for 6 mins 27 sec by NanoBRET assay | B | 6.09 | pEC50 | 812.83 | nM | EC50 | J Nat Prod (2023) 86: 869-881 [PMID:37042802] |
| 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] |
| ChEMBL | Partial agonist activity at C-terminal NanoLuc tagged human muscarinic M2 receptor expressed in HEK293T cells using furimazine as substrate assessed as receptor activation preincubated with substrate for 1 min followed by compound addition and measured for 6 mins 27 sec by NanoBRET assay | B | 6 | pEC50 | 1000 | nM | EC50 | J Nat Prod (2023) 86: 869-881 [PMID:37042802] |
| 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 |
| M3 receptor/Muscarinic acetylcholine receptor M3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL245] [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] |
| ChEMBL | Partial agonist activity at C-terminal NanoLuc tagged human muscarinic M3 receptor expressed in HEK293T cells using furimazine as substrate assessed as receptor activation preincubated with substrate for 1 min followed by compound addition and measured for 6 mins 27 sec by NanoBRET assay | B | 5.84 | pEC50 | 1445.44 | nM | EC50 | J Nat Prod (2023) 86: 869-881 [PMID:37042802] |
| M4 receptor/Muscarinic acetylcholine receptor M4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1821] [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 | Partial agonist activity at N-terminal FLAG tagged/C-terminal NanoLuc tagged human muscarinic M4 receptor expressed in HEK293T cells using furimazine as substrate assessed as receptor activation preincubated with substrate for 1 min followed by compound addition and measured for 6 mins 27 sec by NanoBRET assay | B | 5.48 | pEC50 | 3311.31 | nM | EC50 | J Nat Prod (2023) 86: 869-881 [PMID:37042802] |
| 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] |
| ChEMBL | Partial agonist activity at N-terminal FLAG tagged/C-terminal NanoLuc tagged human muscarinic M5 receptor expressed in HEK293T cells using furimazine as substrate assessed as receptor activation preincubated with substrate for 1 min followed by compound addition and measured for 6 mins 27 sec by NanoBRET assay | B | 6.2 | pEC50 | 630.96 | nM | EC50 | J Nat Prod (2023) 86: 869-881 [PMID:37042802] |
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]
