oxotremorine [Ligand Id: 302] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL7634
  • acetylcholinesterase (Cartwright blood group)/Acetylcholinesterase in Mouse [ChEMBL: CHEMBL3198] [GtoPdb: 2465] [UniProtKB: P21836]
  • 7.3
1 CHEMBL7634_lig_chart_1 Acetylcholinesterase Mouse
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  • Muscarinic acetylcholine receptor DM1 in Drosophila melanogaster [ChEMBL: CHEMBL2366467] [UniProtKB: P16395]
  • 4.69
2 CHEMBL7634_lig_chart_2 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]
  • 6.71
3 CHEMBL7634_lig_chart_3 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 Mouse [ChEMBL: CHEMBL3197] [GtoPdb: 14] [UniProtKB: Q9ERZ4]
  • M2 receptor/Muscarinic acetylcholine receptor M2 in Rat [ChEMBL: CHEMBL309] [GtoPdb: 14] [UniProtKB: P10980]
  • 7.15
4 CHEMBL7634_lig_chart_4 Muscarinic acetylcholine receptor M2 HumanMouseRat
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  • M3 receptor/Muscarinic acetylcholine receptor M3 in Human [ChEMBL: CHEMBL245] [GtoPdb: 15] [UniProtKB: P20309]
  • Muscarinic acetylcholine receptor M3 in Guinea pig [ChEMBL: CHEMBL5498] [UniProtKB: Q8VH26]
  • This target only has 1 pki data point
  • 0
5 CHEMBL7634_lig_chart_5 Muscarinic acetylcholine receptor M3 HumanGuinea pig
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  • M4 receptor/Muscarinic acetylcholine receptor M4 in Human [ChEMBL: CHEMBL1821] [GtoPdb: 16] [UniProtKB: P08173]
  • 6.8
6 CHEMBL7634_lig_chart_6 Muscarinic acetylcholine receptor M4 Human
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  • M5 receptor/Muscarinic acetylcholine receptor M5 in Human [ChEMBL: CHEMBL2035] [GtoPdb: 17] [UniProtKB: P08912]
  • This target only has 0 pki data point
  • 0
7 CHEMBL7634_lig_chart_7 Muscarinic acetylcholine receptor M5 Human
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
acetylcholinesterase (Cartwright blood group)/Acetylcholinesterase in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3198] [GtoPdb: 2465] [UniProtKB: P21836]
ChEMBL Compound was evaluated for the binding affinity by displacing [3H]methylscopolamine [3H]NMS from mouse cerebral cortex tissue. B 5.82 pKi 1500 nM Ki J. Med. Chem. (1992) 35: 1102-1108 [PMID:1552502]
ChEMBL Compound was evaluated for the binding affinity by displacing [3H]oxotremorine from mouse cerebral cortex tissue. B 8.77 pKi 1.7 nM Ki J. Med. Chem. (1992) 35: 1102-1108 [PMID:1552502]
Muscarinic acetylcholine receptor DM1 in Drosophila melanogaster (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2366467] [UniProtKB: P16395]
ChEMBL Displacement of [3H]AF-DX 384 from Drosophila melanogaster mAChR by scintillation counting B 4.67 pKi 21500 nM Ki J Agric Food Chem (2007) 55: 2276-2281 [PMID:17319687]
ChEMBL Displacement of [3H]QNB from Drosophila melanogaster mAChR by scintillation counting B 4.71 pKi 19400 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]
GtoPdb - - 5.5 pKi - - - Br J Pharmacol (1995) 114: 1241-9 [PMID:7620715];
Mol Pharmacol (1997) 52: 172-9 [PMID:9224827]
ChEMBL Inhibition of [3H]- oxotremorine-M binding to human Muscarinic acetylcholine receptor M1 expressed in CHO cell membranes B 7.77 pKi 17 nM Ki J. Med. Chem. (2000) 43: 2514-2522 [PMID:10891110]
ChEMBL Binding affinity to human cloned muscarinic M1 receptor expressed in CHO cells B 8.95 pKi 1.12 nM Ki Bioorg. Med. Chem. (2008) 16: 3049-3058 [PMID:18182302]
ChEMBL Ability to displace [3H]N-methylscopolamine from Muscarinic acetylcholine receptor M1 expressed in CHO cells. B 4.57 pIC50 27100 nM IC50 Bioorg. Med. Chem. Lett. (2001) 11: 2855-2857 [PMID:11597415]
ChEMBL Compound was evaluated for its ability to displace [3H]N-methylscopolamine ([3H]NMS) binding to cloned CHO cell lines expressing Muscarinic acetylcholine receptor M1 B 5.05 pIC50 9000 nM IC50 J. Med. Chem. (1998) 41: 109-116 [PMID:9438027]
ChEMBL Displacement of [3H]QNB in genetically transformed mouse cell line (m1C2) transfected with Muscarinic acetylcholine receptor M1 B 6.44 pIC50 364 nM IC50 Bioorg. Med. Chem. Lett. (1992) 2: 803-808
ChEMBL Ability to displace [3H]oxotremorine from Muscarinic acetylcholine receptor M1 expressed in CHO cells. B 8.64 pIC50 2.3 nM IC50 Bioorg. Med. Chem. Lett. (2001) 11: 2855-2857 [PMID:11597415]
ChEMBL In Vitro evaluation activity at the cloned Human Muscarinic acetylcholine receptor M1 determined by receptor selection and amplification technology (R-SAT) B 6.41 pEC50 390 nM EC50 J. Med. Chem. (1995) 38: 2188-2195 [PMID:7783150]
ChEMBL Agonist activity at human m1 muscarinic acetylcholine receptor expressed in HEK293 cells assessed as calcium mobilization by FLIPR assay F 8.8 pEC50 1.6 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 6.57 pEC50 270 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 - - 6 pKi - - - J Pharmacol Exp Ther (1989) 248: 661-70 [PMID:2537406]
ChEMBL Compound was evaluated for its binding affinity towards muscarinic acetylcholine receptor in rat cortex B 6.71 pKi 196 nM Ki J. Med. Chem. (1992) 35: 1550-1557 [PMID:1578480]
ChEMBL Binding affinity at [3H]PZ radiolabeled muscarinic M1 receptor in rat cortex. B 6.92 pKi 120 nM Ki J. Med. Chem. (1993) 36: 3533-3541 [PMID:8246221]
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 6.44 pIC50 360 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 6.95 pIC50 113 nM IC50 J. Med. Chem. (1992) 35: 15-27 [PMID:1732522]
ChEMBL Binding affinity against Muscarinic receptor M1 in rat brain using [3H]-PZ (pirenzepine) radioligand at a concentration of 1 nM B 7 pIC50 100 nM IC50 Bioorg. Med. Chem. Lett. (1997) 7: 1033-1036
M2 receptor/Muscarinic acetylcholine receptor M2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL211] [GtoPdb: 14] [UniProtKB: P08172]
ChEMBL Displacement of [3H]NMS from human muscarinic acetylcholine receptor M2 B 5 pKi 10000 nM Ki J Med Chem (2017) 60: 3314-3334 [PMID:28388054]
ChEMBL Displacement of [3H]UR-AP060 from human muscarinic acetylcholine receptor M2 expressed in CHOK9 cell homogenate after 3 hrs by liquid scintillation counting assay B 5 pKi 10000 nM Ki J Med Chem (2017) 60: 3314-3334 [PMID:28388054]
ChEMBL Inhibition of [3H]- quinuclidinyl benzilate binding to human Muscarinic acetylcholine receptor M2 expressed in CHO cell membrane B 6.18 pKi 660 nM Ki J. Med. Chem. (2000) 43: 2514-2522 [PMID:10891110]
ChEMBL Binding affinity to human cloned muscarinic M2 receptor expressed in CHO cells B 6.49 pKi 323.59 nM Ki Bioorg. Med. Chem. (2008) 16: 3049-3058 [PMID:18182302]
GtoPdb - - 6.6 pKi - - - Br J Pharmacol (1995) 114: 1241-9 [PMID:7620715];
Mol Pharmacol (1997) 52: 172-9 [PMID:9224827]
ChEMBL Displacement of [3H]UNSW-MK259 from human muscarinic acetylcholine receptor M2 expressed in CHOK9 cells after 3 hrs by liquid scintillation counting assay B 6.83 pKi 147.91 nM Ki J Med Chem (2017) 60: 3314-3334 [PMID:28388054]
ChEMBL Inhibition of [3H]- oxotremorine-M binding to human Muscarinic acetylcholine receptor M2 expressed in CHO cell membranes B 7.77 pKi 17 nM Ki J. Med. Chem. (2000) 43: 2514-2522 [PMID:10891110]
ChEMBL Compound was evaluated for its ability to displace [3H]- N-methyl-scopolamine ([3H]NMS) binding to cloned CHO cell lines expressing Muscarinic acetylcholine receptor M2 B 6.4 pIC50 400 nM IC50 J. Med. Chem. (1998) 41: 109-116 [PMID:9438027]
ChEMBL In Vitro activity at the cloned Human Muscarinic acetylcholine receptor M2 determined by receptor selection and amplification technology (R-SAT). B 7.72 pEC50 19 nM EC50 J. Med. Chem. (1995) 38: 2188-2195 [PMID:7783150]
M2 receptor/Muscarinic acetylcholine receptor M2 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3197] [GtoPdb: 14] [UniProtKB: Q9ERZ4]
ChEMBL Ability to displace [3H]methylscopolamine ([3H]NMS) from mouse cerebral cortex B 5.82 pKi 1500 nM Ki J. Med. Chem. (1992) 35: 3141-3147 [PMID:1507203]
ChEMBL Ability to displace [3H]oxotremorine ([3H]-OXO-M) from mouse cerebral cortex B 8.77 pKi 1.7 nM Ki J. Med. Chem. (1992) 35: 3141-3147 [PMID:1507203]
M2 receptor/Muscarinic acetylcholine receptor M2 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL309] [GtoPdb: 14] [UniProtKB: P10980]
GtoPdb - - 6.5 pKi - - - J Pharmacol Exp Ther (1998) 284: 500-7 [PMID:9454790]
ChEMBL Binding affinity at [3H]QNB and GppNHp radiolabeled muscarinic M2 receptor in rat heart. B 6.8 pKi 160 nM Ki J. Med. Chem. (1993) 36: 3533-3541 [PMID:8246221]
ChEMBL Compound was evaluated for its binding affinity towards muscarinic acetylcholine receptor M2 in rat brainstem B 7.08 pKi 84 nM Ki J. Med. Chem. (1992) 35: 1550-1557 [PMID:1578480]
ChEMBL Binding affinity at [3H]QNB radiolabeled muscarinic M2 receptor in rat cortex. B 7.22 pKi 60 nM Ki J. Med. Chem. (1993) 36: 3533-3541 [PMID:8246221]
ChEMBL Binding affinity at [3H]CD radiolabeled muscarinic M2 receptor in rat cortex. B 9.3 pKi 0.5 nM Ki J. Med. Chem. (1993) 36: 3533-3541 [PMID:8246221]
ChEMBL Binding affinity at [3H]QNB radiolabeled muscarinic M2 receptor in rat heart. B 9.3 pKi 0.5 nM Ki J. Med. Chem. (1993) 36: 3533-3541 [PMID:8246221]
ChEMBL Binding affinity against Muscarinic receptor M2 in rat brain using [3H]QNB (quinuclidinyl benzylate) radioligand at a concentration of 0.12 nM B 5.7 pIC50 2000 nM IC50 Bioorg. Med. Chem. Lett. (1997) 7: 1033-1036
ChEMBL Compound was evaluated for the displacement of the muscarinic QNB in rat heart homogenate containing the pharmacologic M2 receptor (M2-QNB heart) B 6.07 pIC50 860 nM IC50 Bioorg. Med. Chem. Lett. (1991) 1: 147-150
ChEMBL Displacement of [3H]QNB from Muscarinic acetylcholine receptor M2 from rat heart homogenates B 6.07 pIC50 858 nM IC50 Bioorg. Med. Chem. Lett. (1992) 2: 803-808
ChEMBL Muscarinic receptor M2 in rat heart using [3H]QNB (quinuclidinyl benzylate) radioligand as a M2 non-selective muscarinic receptor antagonist at a concentration of 0.12 nM F 7.08 pIC50 84 nM IC50 Bioorg. Med. Chem. Lett. (1997) 7: 1033-1036
M3 receptor/Muscarinic acetylcholine receptor M3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL245] [GtoPdb: 15] [UniProtKB: P20309]
GtoPdb - - 5.3 pKi - - - Br J Pharmacol (1995) 114: 1241-9 [PMID:7620715];
Mol Pharmacol (1997) 52: 172-9 [PMID:9224827]
ChEMBL Compound was evaluated for its ability to displace [3H]N-methylscopolamine ([3H]NMS) binding to cloned CHO cell lines expressing Muscarinic acetylcholine receptor M3 B 4.77 pIC50 17000 nM IC50 J. Med. Chem. (1998) 41: 109-116 [PMID:9438027]
ChEMBL In Vitro activity at the cloned Human Muscarinic acetylcholine receptor M3 determined by receptor selection and amplification technology (R-SAT) B 6.68 pEC50 210 nM EC50 J. Med. Chem. (1995) 38: 2188-2195 [PMID:7783150]
Muscarinic acetylcholine receptor M3 in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5498] [UniProtKB: Q8VH26]
ChEMBL Dissociation constant for complex with muscarinic acetylcholine receptor M3 of guinea pig ileum B 5.92 pKd 1200 nM Kd J. Med. Chem. (1992) 35: 3270-3279 [PMID:1507212]
ChEMBL Muscarinic acetylcholine receptor M3 agonistic/antagonistic activity in guinea pig ileum F 7.3 pEC50 50 nM EC50 J. Med. Chem. (1992) 35: 3270-3279 [PMID:1507212]
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 Inhibition of [3H]- quinuclidinyl benzilate binding to Muscarinic acetylcholine receptor M4 expressed in CHO cell membranes B 6.8 pKi 160 nM Ki J. Med. Chem. (2000) 43: 2514-2522 [PMID:10891110]
ChEMBL Inhibition of [3H]- oxotremorine-M binding to human Muscarinic acetylcholine receptor M4 in CHO cell membranes B 8.82 pKi 1.5 nM Ki J. Med. Chem. (2000) 43: 2514-2522 [PMID:10891110]
ChEMBL Compound was evaluated for its ability to displace [3H]- N-methyl-scopolamine ([3H]-NMS) binding to cloned CHO cell lines expressing Muscarinic acetylcholine receptor M4 B 5.3 pIC50 5000 nM IC50 J. Med. Chem. (1998) 41: 109-116 [PMID:9438027]
ChEMBL In Vitro activity at the cloned Human Muscarinic acetylcholine receptor M4 determined by receptor selection and amplification technology (R-SAT) B 7.48 pEC50 33 nM EC50 J. Med. Chem. (1995) 38: 2188-2195 [PMID:7783150]
ChEMBL Agonist activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as decrease in isoproterenol-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol by Glosensor cAMP reagent/plate reader based luminescence assay B 7.85 pEC50 14 nM EC50 ACS Med Chem Lett (2019) 10: 941-948 [PMID:31223452]
ChEMBL Positive allosteric modulatory activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as as increase in acteylcholine-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol/acetylcholine by Glosensor cAMP reagent/plate reader based luminescence assay B 8.05 pEC50 9 nM EC50 ACS Med Chem Lett (2019) 10: 941-948 [PMID:31223452]
M5 receptor/Muscarinic acetylcholine receptor M5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2035] [GtoPdb: 17] [UniProtKB: P08912]
ChEMBL Compound was evaluated for its ability to displace [3H]- N-methyl-scopolamine ([3H]NMS) binding to cloned CHO cell lines expressing Muscarinic acetylcholine receptor M5 B 5.1 pIC50 8000 nM IC50 J. Med. Chem. (1998) 41: 109-116 [PMID:9438027]
ChEMBL In Vitro activity at the cloned Human Muscarinic acetylcholine receptor M5 determined by receptor selection and amplification technology (R-SAT) B 7.26 pEC50 55 nM EC50 J. Med. Chem. (1995) 38: 2188-2195 [PMID:7783150]

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]