himbacine [Ligand Id: 324] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL277642 (Himbacine)
  • Acetylcholinesterase in Electrophorus electricus [ChEMBL: CHEMBL4078] [UniProtKB: O42275]
  • This target only has 0 pki data point
  • 0
1 CHEMBL277642_lig_chart_1 Acetylcholinesterase Electrophorus electricus
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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 Rat [ChEMBL: CHEMBL276] [GtoPdb: 13] [UniProtKB: P08482]
  • 7.15
2 CHEMBL277642_lig_chart_2 Muscarinic acetylcholine receptor M1 HumanRat
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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 Rat [ChEMBL: CHEMBL309] [GtoPdb: 14] [UniProtKB: P10980]
  • 7.9
3 CHEMBL277642_lig_chart_3 Muscarinic acetylcholine receptor M2 HumanRat
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  • M3 receptor/Muscarinic acetylcholine receptor M3 in Human [ChEMBL: CHEMBL245] [GtoPdb: 15] [UniProtKB: P20309]
  • 7.03
4 CHEMBL277642_lig_chart_4 Muscarinic acetylcholine receptor M3 Human
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  • M4 receptor/Muscarinic acetylcholine receptor M4 in Human [ChEMBL: CHEMBL1821] [GtoPdb: 16] [UniProtKB: P08173]
  • M4 receptor/Muscarinic acetylcholine receptor M4 in Mouse [ChEMBL: CHEMBL4572] [GtoPdb: 16] [UniProtKB: P32211]
  • M4 receptor/Muscarinic acetylcholine receptor M4 in Rat [ChEMBL: CHEMBL317] [GtoPdb: 16] [UniProtKB: P08485]
  • 0
5 CHEMBL277642_lig_chart_5 Muscarinic acetylcholine receptor M4 HumanMouseRat
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  • M5 receptor/Muscarinic acetylcholine receptor M5 in Human [ChEMBL: CHEMBL2035] [GtoPdb: 17] [UniProtKB: P08912]
  • 6.4
6 CHEMBL277642_lig_chart_6 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 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 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]