himbacine [Ligand Id: 324] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL277642 (Himbacine) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| Acetylcholinesterase in Electrophorus electricus (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4078] [UniProtKB: O42275] | ||||||||
| ChEMBL | Inhibition of electric eel AChE by Ellman's method | B | 4.64 | pIC50 | 22720 | nM | IC50 | Bioorg Med Chem (2012) 20: 6669-6679 [PMID:23062825] |
| M1 receptor/Muscarinic acetylcholine receptor M1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL216] [GtoPdb: 13] [UniProtKB: P11229] | ||||||||
| ChEMBL | Displacement of [3H]QNB from muscarinic receptor 1 expressed in CHO-K1 cells | B | 6.77 | pKd | 168 | nM | Kd | Bioorg Med Chem Lett (1993) 3: 1247-1252 |
| ChEMBL | Binding affinity against M1 receptor expressed in CHO-K1 cells transfected with human muscarinic receptor sequence using radioligand [3H]quinuclidinyl benzilate ([3H]QNB) | B | 6.83 | pKd | 148 | nM | Kd | Bioorg Med Chem Lett (1995) 5: 61-66 |
| ChEMBL | Binding affinity against human muscarine receptor (hM1) cloned in CHO cells | B | 6.8 | pKi | 158.49 | nM | Ki | Bioorg Med Chem Lett (2002) 12: 1909-1912 [PMID:12113806] |
| ChEMBL | Affinity for Muscarinic acetylcholine receptor M1 expressed in CHO cells by [3H]NMS displacement. | B | 6.97 | pKi | 107.15 | nM | Ki | Bioorg Med Chem Lett (2001) 11: 1241-1243 [PMID:11354386] |
| ChEMBL | Binding affinity against human muscarine receptor (hM1) cloned in CHO cells | B | 6.97 | pKi | 107.15 | nM | Ki | Bioorg Med Chem Lett (2002) 12: 1909-1912 [PMID:12113806] |
| GtoPdb | - | - | 7.1 | pKi | - | - | - |
FEBS Lett (1994) 352: 91-4 [PMID:7925952]; J Pharmacol Exp Ther (1992) 263: 663-7 [PMID:1331410]; J Pharmacol Exp Ther (1991) 256: 727-33 [PMID:1994002] |
| ChEMBL | In vitro inhibitory activity against cloned human M1 muscarinic receptor | B | 7.32 | pKi | 48 | nM | Ki | Bioorg Med Chem Lett (2004) 14: 3967-3970 [PMID:15225708] |
| ChEMBL | Binding affinity towards human muscarinic M1 receptor in CHO-KI cells using [3H]- QNB as radioligand | B | 8.35 | pKi | 4.5 | nM | Ki | Bioorg Med Chem Lett (1999) 9: 901-906 [PMID:10206558] |
| ChEMBL | Evaluated for its binding affinity at human muscarinic receptor m1 by displacement of [3H]NMS binding using membranes in transfected chinese hamster ovarian cell | B | 6.26 | pIC50 | 548.2 | nM | IC50 | Bioorg Med Chem Lett (1998) 8: 1991-1996 [PMID:9873472] |
| M1 receptor/Muscarinic acetylcholine receptor M1 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL276] [GtoPdb: 13] [UniProtKB: P08482] | ||||||||
| ChEMBL | The compound was tested in vitro for binding activity against M1 muscarinic receptor in homogenates of the cerebral cortex of rat using [3H]pirenzepine as radioligand | B | 7.1 | pKi | 79.43 | nM | Ki | Bioorg Med Chem Lett (2002) 12: 3271-3273 [PMID:12392730] |
| ChEMBL | Binding affinity against the muscarinic M1 (cortex) subtype was evaluated using [3H]pirenzepine | B | 7.2 | pKi | 63.1 | nM | Ki | Bioorg Med Chem Lett (2002) 12: 2871-2873 [PMID:12270166] |
| M2 receptor/Muscarinic acetylcholine receptor M2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL211] [GtoPdb: 14] [UniProtKB: P08172] | ||||||||
| ChEMBL | Binding affinity towards human muscarinic M2 receptor in CHO-KI cells using [3H]- QNB as radioligand | B | 7.32 | pKi | 48.4 | nM | Ki | Bioorg Med Chem Lett (1999) 9: 901-906 [PMID:10206558] |
| ChEMBL | Affinity for Muscarinic acetylcholine receptor M2 expressed in CHO cells by [3H]NMS displacement. | B | 8 | pKi | 10 | nM | Ki | Bioorg Med Chem Lett (2001) 11: 1241-1243 [PMID:11354386] |
| ChEMBL | Binding affinity against human muscarine receptor (hM2) cloned in CHO cells | B | 8 | pKi | 10 | nM | Ki | Bioorg Med Chem Lett (2002) 12: 1909-1912 [PMID:12113806] |
| ChEMBL | Binding affinity against human muscarine receptor (hM2) cloned in CHO cells | B | 8.33 | pKi | 4.68 | nM | Ki | Bioorg Med Chem Lett (2002) 12: 1909-1912 [PMID:12113806] |
| ChEMBL | In vitro inhibitory activity against cloned human M2 muscarinic receptor | B | 8.35 | pKi | 4.5 | nM | Ki | Bioorg Med Chem Lett (2004) 14: 3967-3970 [PMID:15225708] |
| GtoPdb | - | - | 8.4 | pKi | - | - | - |
FEBS Lett (1994) 352: 91-4 [PMID:7925952]; J Pharmacol Exp Ther (1992) 263: 663-7 [PMID:1331410]; J Pharmacol Exp Ther (1998) 284: 500-7 [PMID:9454790]; J Pharmacol Exp Ther (1991) 256: 727-33 [PMID:1994002] |
| ChEMBL | Evaluated for its binding affinity at human muscarinic receptor m2 by displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cell | B | 7.76 | pIC50 | 17.5 | nM | IC50 | Bioorg Med Chem Lett (1998) 8: 1991-1996 [PMID:9873472] |
| M2 receptor/Muscarinic acetylcholine receptor M2 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL309] [GtoPdb: 14] [UniProtKB: P10980] | ||||||||
| ChEMBL | Binding affinity against M2 receptor in rat brainstem cells using radioligand [3H]quinuclidinyl benzilate ([3H]QNB) | B | 8 | pKd | 10 | nM | Kd | Bioorg Med Chem Lett (1995) 5: 61-66 |
| ChEMBL | Displacement of [3H]QNB from rat brain stem muscarinic receptor 2 (M2) | B | 8.04 | pKd | 9.05 | nM | Kd | Bioorg Med Chem Lett (1993) 3: 1247-1252 |
| ChEMBL | Dissociation constant for the blocking of heart muscarinic M2 receptor was reported. | B | 8.16 | pKd | 6.9 | nM | Kd | Bioorg Med Chem Lett (1992) 2: 797-802 |
| ChEMBL | Dissociation constant for the blocking of brainstem muscarinic M2 receptor was reported. | B | 8.34 | pKd | 4.6 | nM | Kd | Bioorg Med Chem Lett (1992) 2: 797-802 |
| ChEMBL | Dissociation constant for the blocking of cardiac muscarinic M2 receptor was reported. | B | 8.52 | pKd | 3 | nM | Kd | Bioorg Med Chem Lett (1992) 2: 797-802 |
| ChEMBL | The compound was tested in vitro for binding activity against M2 muscarinic receptor in homogenates of the brainstem of rat using [3H]quinuclidinyl benzilate (QNB) as radioligand | B | 7.9 | pKi | 12.59 | nM | Ki | Bioorg Med Chem Lett (2002) 12: 3271-3273 [PMID:12392730] |
| GtoPdb | - | - | 7.9 | pKi | - | - | - | J Pharmacol Exp Ther (1998) 284: 500-7 [PMID:9454790] |
| ChEMBL | Binding affinity against the muscarinic M2 (brainstem) subtype was evaluated using [3H]quinuclidinyl benzilate | B | 8 | pKi | 10 | nM | Ki | Bioorg Med Chem Lett (2002) 12: 2871-2873 [PMID:12270166] |
| M3 receptor/Muscarinic acetylcholine receptor M3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL245] [GtoPdb: 15] [UniProtKB: P20309] | ||||||||
| ChEMBL | Binding affinity against human muscarine receptor (hM3) cloned in CHO cells | B | 6.98 | pKi | 104.71 | nM | Ki | Bioorg Med Chem Lett (2002) 12: 1909-1912 [PMID:12113806] |
| ChEMBL | Affinity for Muscarinic acetylcholine receptor M3 expressed in CHO cells by [3H]-NMS displacement. | B | 7.03 | pKi | 93.33 | nM | Ki | Bioorg Med Chem Lett (2001) 11: 1241-1243 [PMID:11354386] |
| ChEMBL | Binding affinity against human muscarine receptor (hM3) cloned in CHO cells | B | 7.03 | pKi | 93.33 | nM | Ki | Bioorg Med Chem Lett (2002) 12: 1909-1912 [PMID:12113806] |
| GtoPdb | - | - | 7.2 | pKi | - | - | - |
FEBS Lett (1994) 352: 91-4 [PMID:7925952]; J Pharmacol Exp Ther (1992) 263: 663-7 [PMID:1331410]; J Pharmacol Exp Ther (1991) 256: 727-33 [PMID:1994002] |
| ChEMBL | Evaluated for its binding affinity at human muscarinic receptor m3 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cell | B | 6.48 | pIC50 | 333.6 | nM | IC50 | Bioorg Med Chem Lett (1998) 8: 1991-1996 [PMID:9873472] |
| M4 receptor/Muscarinic acetylcholine receptor M4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1821] [GtoPdb: 16] [UniProtKB: P08173] | ||||||||
| ChEMBL | Affinity for Muscarinic acetylcholine receptor M4 expressed in CHO cells by [3H]NMS displacement. | B | 7.96 | pKi | 10.96 | nM | Ki | Bioorg Med Chem Lett (2001) 11: 1241-1243 [PMID:11354386] |
| ChEMBL | Binding affinity against human muscarine receptor (hM4) cloned in CHO cells | B | 7.96 | pKi | 10.96 | nM | Ki | Bioorg Med Chem Lett (2002) 12: 1909-1912 [PMID:12113806] |
| ChEMBL | Binding affinity against human muscarine receptor (hM4) cloned in CHO cells | B | 8.06 | pKi | 8.71 | nM | Ki | Bioorg Med Chem Lett (2002) 12: 1909-1912 [PMID:12113806] |
| GtoPdb | - | - | 8.2 | pKi | - | - | Ki |
FEBS Lett (1994) 352: 91-4 [PMID:7925952]; J Pharmacol Exp Ther (1992) 263: 663-7 [PMID:1331410]; J Pharmacol Exp Ther (1991) 256: 727-33 [PMID:1994002] |
| GtoPdb | - | - | 8.4 | pKi | 4 | nM | Ki | Invest Ophthalmol Vis Sci (2018) 59: 2778-2791 [PMID:29860464] |
| ChEMBL | Evaluated for its binding affinity at human muscarinic receptor m4 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cell | B | 6.94 | pIC50 | 114.4 | nM | IC50 | Bioorg Med Chem Lett (1998) 8: 1991-1996 [PMID:9873472] |
| M4 receptor/Muscarinic acetylcholine receptor M4 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4572] [GtoPdb: 16] [UniProtKB: P32211] | ||||||||
| ChEMBL | Potency assessed to inhibit cAMP levels in N1E-115 neuroblastoma cells, for blocking oxotremorine-M in functional assay for Muscarinic acetylcholine receptor M4 | F | 7.95 | pKd | 11.3 | nM | Kd | Bioorg Med Chem Lett (1992) 2: 797-802 |
| M4 receptor/Muscarinic acetylcholine receptor M4 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL317] [GtoPdb: 16] [UniProtKB: P08485] | ||||||||
| ChEMBL | Potency assessed to inhibit cAMP levels in rat striatum, for blocking oxotremorine-M, in functional assay for Muscarinic acetylcholine receptor M4 | F | 8.27 | pKd | 5.4 | nM | Kd | Bioorg Med Chem Lett (1992) 2: 797-802 |
| M5 receptor/Muscarinic acetylcholine receptor M5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2035] [GtoPdb: 17] [UniProtKB: P08912] | ||||||||
| ChEMBL | Affinity for Muscarinic acetylcholine receptor M5 expressed in CHO cells by [3H]NMS displacement. | B | 6.31 | pKi | 489.78 | nM | Ki | Bioorg Med Chem Lett (2001) 11: 1241-1243 [PMID:11354386] |
| GtoPdb | - | - | 6.5 | pKi | - | - | - |
FEBS Lett (1994) 352: 91-4 [PMID:7925952]; J Pharmacol Exp Ther (1992) 263: 663-7 [PMID:1331410]; J Pharmacol Exp Ther (1991) 256: 727-33 [PMID:1994002] |
| ChEMBL | Evaluated for its binding affinity at human muscarinic receptor m5 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cell | B | 5.99 | pIC50 | 1016 | nM | IC50 | Bioorg Med Chem Lett (1998) 8: 1991-1996 [PMID:9873472] |
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]
