oxotremorine [Ligand Id: 302] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL7634 |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| acetylcholinesterase (Yt 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 | Displacement of 4-(2-((1E,3E)-5-((E)-1-(6-((3,5-Bis((2-(3-(1-(4-(1-(2-oxo-2-(11-oxo-10,11-dihydro-5H-dibenzo[b,e][1,4]diazepin-5-yl)ethyl)piperidin-4-yl)butyl)-1H-imidazol-4-yl)propanamido)ethyl)carbamoyl)benzyl)amino)-6-oxohexyl)-3,3-dimethyl-5-sulfoindolin-2-ylidene)penta-1,3-dien-1-yl)-3,3-dimethyl-3H-indol-1-ium-1-yl)butane-1-sulfonate Tris(hydrotrifluoroacetate) fluorescent tracer from human muscarinic M2 receptor expressed in CHO-K9 cells measured after 60 mins by Hoechst H33342 dye based confocal plate reader assay | B | 5.75 | pKi | 1778.28 | nM | Ki | J Med Chem (2020) 63: 4133-4154 [PMID:32233403] |
| ChEMBL | Displacement of 4-(2-((1E,3E)-5-((E)-3,3-Dimethyl-1-(6-oxo-6-((2-(3-(1-(4-(1-(2-oxo-2-(11-oxo-10,11-dihydro-5H-dibenzo[b,e][1,4]diazepin-5-yl)ethyl)piperidin-4-yl)butyl)-1H-imidazol-4-yl)propanamido)ethyl)-amino)hexyl)-5-sulfoindolin-2-ylidene)penta-1,3-dien-1-yl)-3,3-dimethyl-3H-indol-1-ium-1-yl)butane-1-sulfonateHydrotrifluoroacetate fluorescent tracer from human muscarinic M2 receptor expressed in CHO-K9 cells measured after 60 mins by Hoechst H33342 dye based confocal plate reader assay | B | 5.99 | pKi | 1023.29 | nM | Ki | J Med Chem (2020) 63: 4133-4154 [PMID:32233403] |
| ChEMBL | Displacement of 4-(2-((1E,3E)-5-((E)-3,3-Dimethyl-1-(6-oxo-6-((2-(4-(4-(1-(2-oxo-2-(11-oxo-10,11-dihydro-5H-dibenzo[b,e][1,4]diazepin-5-yl)ethyl)piperidin-4-yl)butyl)piperazin-1-yl)ethyl)amino)hexyl)-5-sulfoindolin-2-ylidene)penta-1,3-dien-1-yl)-3,3-dimethyl-3H-indol-1-ium-1-yl)butane-1-sulfonate Bis(hydrotrifluoroacetate) fluorescent tracer from human muscarinic M2 receptor expressed in CHO-K9 cells measured after 60 mins by Hoechst H33342 dye based confocal plate reader assay | B | 6.07 | pKi | 851.14 | nM | Ki | J Med Chem (2020) 63: 4133-4154 [PMID:32233403] |
| 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 | F | 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 | F | 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 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]
