pilocarpine [Ligand Id: 305] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL550 (Pilocarpine, Ocusert pilo, Ocusert pilo-20, Ocusert pilo-40)
  • Muscarinic acetylcholine receptor DM1 in Drosophila melanogaster [ChEMBL: CHEMBL2366467] [UniProtKB: P16395]
  • 5.54
1 CHEMBL550_lig_chart_1 Muscarinic acetylcholine receptor DM1 Drosophila melanogaster
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  • M1 receptor/Muscarinic acetylcholine receptor M1 in Human [ChEMBL: CHEMBL216] [GtoPdb: 13] [UniProtKB: P11229]
  • M1 receptor/Muscarinic acetylcholine receptor M1 in Mouse [ChEMBL: CHEMBL3733] [GtoPdb: 13] [UniProtKB: P12657]
  • M1 receptor/Muscarinic acetylcholine receptor M1 in Rat [ChEMBL: CHEMBL276] [GtoPdb: 13] [UniProtKB: P08482]
  • 5.2
2 CHEMBL550_lig_chart_2 Muscarinic acetylcholine receptor M1 HumanMouseRat
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  • M2 receptor/Muscarinic acetylcholine receptor M2 in Human [ChEMBL: CHEMBL211] [GtoPdb: 14] [UniProtKB: P08172]
  • M2 receptor/Muscarinic acetylcholine receptor M2 in Rat [ChEMBL: CHEMBL309] [GtoPdb: 14] [UniProtKB: P10980]
  • 5.01
3 CHEMBL550_lig_chart_3 Muscarinic acetylcholine receptor M2 HumanRat
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  • M5 receptor/Muscarinic acetylcholine receptor M5 in Human [ChEMBL: CHEMBL2035] [GtoPdb: 17] [UniProtKB: P08912]
  • 4.99
4 CHEMBL550_lig_chart_4 Muscarinic acetylcholine receptor M5 Human
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  • M3 receptor in Human [GtoPdb: 15] [UniProtKB: P20309]
  • This target only has 1 pki data point
  • 5.1
5 CHEMBL550_lig_chart_5 M3 receptor Human
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  • M4 receptor in Human [GtoPdb: 16] [UniProtKB: P08173]
  • This target only has 1 pki data point
  • 5.2
6 CHEMBL550_lig_chart_6 M4 receptor Human
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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 B 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 28:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]