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 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]
