Click here for a description of the charts and data table
Please tell us if you are using this feature and what you think!
ChEMBL ligand: CHEMBL7634 |
---|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
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 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]