ciproxifan [Ligand Id: 1265] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL14638 (Ciproxifan)
  • acetylcholinesterase (Cartwright blood group)/Acetylcholinesterase in Human [ChEMBL: CHEMBL220] [GtoPdb: 2465] [UniProtKB: P22303]
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  • α2A-adrenoceptor/Alpha-2a adrenergic receptor in Human [ChEMBL: CHEMBL1867] [GtoPdb: 25] [UniProtKB: P08913]
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  • α2C-adrenoceptor/Alpha-2c adrenergic receptor in Human [ChEMBL: CHEMBL1916] [GtoPdb: 27] [UniProtKB: P18825]
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  • butyrylcholinesterase/Butyrylcholinesterase in Human [ChEMBL: CHEMBL1914] [GtoPdb: 2471] [UniProtKB: P06276]
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  • H1 receptor/Histamine H1 receptor in Human [ChEMBL: CHEMBL231] [GtoPdb: 262] [UniProtKB: P35367]
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  • H2 receptor/Histamine H2 receptor in Human [ChEMBL: CHEMBL1941] [GtoPdb: 263] [UniProtKB: P25021]
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  • H3 receptor/Histamine H3 receptor in Human [ChEMBL: CHEMBL264] [GtoPdb: 264] [UniProtKB: Q9Y5N1]
  • H3 receptor in Mouse [GtoPdb: 264] [UniProtKB: P58406]
  • H3 receptor/Histamine H3 receptor in Rat [ChEMBL: CHEMBL4124] [GtoPdb: 264] [UniProtKB: Q9QYN8]
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  • H4 receptor/Histamine H4 receptor in Human [ChEMBL: CHEMBL3759] [GtoPdb: 265] [UniProtKB: Q9H3N8]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
acetylcholinesterase (Cartwright blood group)/Acetylcholinesterase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL220] [GtoPdb: 2465] [UniProtKB: P22303]
ChEMBL Inhibition of human AChE B 4.06 pIC50 86100 nM IC50 Eur J Med Chem (2019) 180: 690-706 [PMID:31401465]
ChEMBL Inhibition of human acetylcholinesterase expressed in HEK 293 cells using acetylthiocholine iodide as substrate by Ellman's method B 4.06 pIC50 86100 nM IC50 Bioorg Med Chem (2019) 27: 895-930 [PMID:30744931]
α2A-adrenoceptor/Alpha-2a adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1867] [GtoPdb: 25] [UniProtKB: P08913]
ChEMBL Displacement of [3H]rauwolscine from human adrenergic alpha 2C10 receptor expressed in mouse LTK- cells B 7.37 pKi 42.66 nM Ki J. Med. Chem. (2008) 51: 5423-5430 [PMID:18683917]
α2C-adrenoceptor/Alpha-2c adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1916] [GtoPdb: 27] [UniProtKB: P18825]
ChEMBL Displacement of [3H]rauwolscine from human adrenergic alpha 2C4 receptor expressed in mouse LTK- cells B 7.2 pKi 63.1 nM Ki J. Med. Chem. (2008) 51: 5423-5430 [PMID:18683917]
butyrylcholinesterase/Butyrylcholinesterase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1914] [GtoPdb: 2471] [UniProtKB: P06276]
ChEMBL Inhibition of human BChE B 4.11 pIC50 77300 nM IC50 Eur J Med Chem (2019) 180: 690-706 [PMID:31401465]
ChEMBL Inhibition of human plasma butyrylcholinesterase by Ellman's method B 4.11 pIC50 77300 nM IC50 Bioorg Med Chem (2019) 27: 895-930 [PMID:30744931]
H1 receptor/Histamine H1 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL231] [GtoPdb: 262] [UniProtKB: P35367]
GtoPdb - - 5 pKi >10000 nM Ki Pharmacol Rev (2015) 67: 601-55 [PMID:26084539]
ChEMBL Displacement of [3H]mepyramine from human histamine H1 receptor B 5 pKi >10000 nM Ki J. Med. Chem. (2008) 51: 5423-5430 [PMID:18683917]
ChEMBL Antagonist activity at human recombinant histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced effect by FLIPR assay B 5.6 pKi >2511.89 nM Ki Bioorg. Med. Chem. Lett. (2013) 23: 6897-6901 [PMID:24161834]
H2 receptor/Histamine H2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1941] [GtoPdb: 263] [UniProtKB: P25021]
GtoPdb - - 5 pKi >10000 nM Ki Pharmacol Rev (2015) 67: 601-55 [PMID:26084539]
ChEMBL Displacement of [3H]tiotidine from human histamine H2 receptor B 5 pKi >10000 nM Ki J. Med. Chem. (2008) 51: 5423-5430 [PMID:18683917]
H3 receptor/Histamine H3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL264] [GtoPdb: 264] [UniProtKB: Q9Y5N1]
ChEMBL Antagonist potency against human histamine H3 receptor expressed in CHO cells was determined by GTPgamma-S-assay F 7.03 pKi 94 nM Ki J. Med. Chem. (2004) 47: 2833-2838 [PMID:15139761]
ChEMBL Antagonist potency against human H3 receptor in GTPgamma-S-Assay F 7.03 pKi 94 nM Ki J. Med. Chem. (2005) 48: 306-311 [PMID:15634025]
ChEMBL Displacement of [3H]NAMH from histamine H3 receptor in human cortex B 7.05 pKi 89.13 nM Ki J. Med. Chem. (2008) 51: 5423-5430 [PMID:18683917]
ChEMBL Antagonist activity at human histamine H3 receptor expressed in CHOK1 cells assessed as inhibition of GTPgammaS binding by scintillation proximity assay F 7.2 pKi 63.1 nM Ki Bioorg. Med. Chem. Lett. (2013) 23: 6897-6901 [PMID:24161834]
ChEMBL In vitro binding affinity was determined as displacement of [3H]N-R-methylhistamine from C6 cell membranes expressing human histamine H3 receptor B 7.2 pKi 63.1 nM Ki J. Med. Chem. (2005) 48: 38-55 [PMID:15634000]
ChEMBL Displacement of [3H]NAMH from human full length histamine H3 receptor expressed in rat C6 cells B 7.2 pKi 63.1 nM Ki J. Med. Chem. (2008) 51: 5423-5430 [PMID:18683917]
ChEMBL In vitro binding affinity was determined as displacement of [3H]N-R-methylhistamine from C6 cell membranes expressing human histamine H3 receptor B 7.2 pKi 63 nM Ki J. Med. Chem. (2005) 48: 38-55 [PMID:15634000]
ChEMBL Binding affinity to human H3 receptor B 7.2 pKi 63 nM Ki J. Med. Chem. (2012) 55: 2406-2415 [PMID:22313227]
GtoPdb - - 7.3 pKi - - - J Pharmacol Exp Ther (2003) 305: 887-96 [PMID:12606603];
Biochem Pharmacol (2004) 68: 933-45 [PMID:15294456];
Biochem J (2001) 355: 279-88 [PMID:11284713];
Br J Pharmacol (2000) 131: 1247-50 [PMID:11090094];
Eur J Pharmacol (2002) 453: 33-41 [PMID:12393057];
Pharmacol Rev (2015) 67: 601-55 [PMID:26084539]
ChEMBL Displacement of [3H]-N-alpha-methylhistamine from human H3R expressed in HEK293 cell membranes incubated for 90 mins by liquid scintillation counting method B 7.34 pKi 46 nM Ki Bioorg Med Chem (2019) 27: 895-930 [PMID:30744931]
ChEMBL Displacement of [125I]iodoproxyfan from human histamine H3 receptor expressing CHO cells B 7.34 pKi 46 nM Ki J. Med. Chem. (2003) 46: 1523-1530 [PMID:12672253]
ChEMBL Displacement of [3H]iodoproxyfan from human histamine H3 receptor expressed in CHO-K1 cells B 7.34 pKi 46 nM Ki Bioorg. Med. Chem. Lett. (2009) 19: 6682-6685 [PMID:19846299]
ChEMBL Displacement of [125I]iodoproxyfan from human full-length histamine H3 receptor expressed in HEK293 cells after 60 mins B 7.34 pKi 46 nM Ki Bioorg. Med. Chem. (2011) 19: 2850-2858 [PMID:21498080]
ChEMBL Displacement of [3H]Nalpha-methylhistamine from human recombinant histamine H3 receptor expressed in HEK-293 cells B 7.34 pKi 46 nM Ki ACS Med. Chem. Lett. (2013) 4: 269-273 [PMID:24900647]
ChEMBL Binding affinity to human H3R B 7.34 pKi 46 nM Ki Eur J Med Chem (2018) 148: 487-497 [PMID:29477889]
ChEMBL Inhibition of human histamine H3 receptor B 7.34 pKi 46 nM Ki Eur J Med Chem (2019) 180: 690-706 [PMID:31401465]
ChEMBL Inhibition of [125I]iodoproxyfan binding to human histamine H3 receptor of CHO-K1 cells B 7.34 pKi 46 nM Ki Bioorg. Med. Chem. Lett. (2001) 11: 951-954 [PMID:11294398]
H3 receptor in Mouse [GtoPdb: 264] [UniProtKB: P58406]
GtoPdb - - 9.4 pKi - - - J Neurochem (2004) 90: 1331-8 [PMID:15341517]
H3 receptor/Histamine H3 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4124] [GtoPdb: 264] [UniProtKB: Q9QYN8]
ChEMBL Inhibition of [125I]iodoproxyfan from rat histamine H3 receptor expressed in CHO-K1 cells B 8.41 pKi 3.9 nM Ki Bioorg. Med. Chem. Lett. (2001) 11: 951-954 [PMID:11294398]
ChEMBL Displacement of [3H]NAMH from histamine H3 receptor in rat cortex B 9.2 pKi 0.63 nM Ki J. Med. Chem. (2008) 51: 5423-5430 [PMID:18683917]
ChEMBL In vitro binding affinity was determined as displacement of [3H]N-R-methylhistamine from C6 cell membranes expressing rat histamine H3 receptor B 9.29 pKi 0.51 nM Ki J. Med. Chem. (2005) 48: 38-55 [PMID:15634000]
ChEMBL Displacement of [3H]NAMH from rat full length histamine H3 receptor expressed in rat C6 cells B 9.29 pKi 0.51 nM Ki J. Med. Chem. (2008) 51: 5423-5430 [PMID:18683917]
ChEMBL In vitro binding affinity was determined as displacement of [3H]N-R-methylhistamine from C6 cell membranes expressing rat histamine H3 receptor B 9.29 pKi 0.51 nM Ki J. Med. Chem. (2005) 48: 38-55 [PMID:15634000]
GtoPdb - - 9.3 pKi - - - J Pharmacol Exp Ther (2003) 305: 887-96 [PMID:12606603];
Biochem Pharmacol (2004) 68: 933-45 [PMID:15294456];
Biochem Biophys Res Commun (2001) 280: 75-80 [PMID:11162480];
Br J Pharmacol (2000) 131: 1247-50 [PMID:11090094];
Eur J Pharmacol (2002) 453: 33-41 [PMID:12393057]
ChEMBL In vitro binding affinity against rat histamine H3 receptor B 9.31 pKi 0.49 nM Ki J. Med. Chem. (2004) 47: 2678-2687 [PMID:15115409]
ChEMBL In vitro inhibitory activity against Histamine H3 receptor for K+ evoked depolarization-induced release of [3H]histamine from synaptosomes of rat cerebral cortex B 9.31 pKi 0.49 nM Ki Bioorg. Med. Chem. Lett. (2000) 10: 2379-2382 [PMID:11055360]
ChEMBL Histamine H3 receptor antagonist activity in an assay with K+ evoked depolarization-induced release of [3H]-histamine from rat synaptosomes. F 9.31 pKi 0.49 nM Ki J. Med. Chem. (2000) 43: 3335-3343 [PMID:10966752]
H4 receptor/Histamine H4 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3759] [GtoPdb: 265] [UniProtKB: Q9H3N8]
ChEMBL Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells B 5.73 pKi 1862.09 nM Ki J. Med. Chem. (2008) 51: 5423-5430 [PMID:18683917]
GtoPdb - - 5.73 pKi - - - J Pharmacol Exp Ther (2003) 305: 887-96 [PMID:12606603];
Biochem Pharmacol (2004) 68: 933-45 [PMID:15294456];
Pharmacol Rev (2015) 67: 601-55 [PMID:26084539]
ChEMBL Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells B 6.21 pKi 612 nM Ki Bioorg. Med. Chem. Lett. (2009) 19: 6682-6685 [PMID:19846299]
ChEMBL Displacement of [3H]histamine from human full-length histamine H4 receptor expressed in HEK293 cells after 60 mins B 6.21 pKi 612 nM Ki Bioorg. Med. Chem. (2011) 19: 2850-2858 [PMID:21498080]
Monoamine oxidase A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1951] [GtoPdb: 2489] [UniProtKB: P21397]
ChEMBL Inhibition of human MAOA B 4.94 pIC50 11400 nM IC50 Eur J Med Chem (2019) 180: 690-706 [PMID:31401465]
ChEMBL Inhibition of recombinant human MAOA expressed in baculovirus infected BTI insect cells using p-tyramine as substrate by Amplex red reagent/horseradish peroxidase coupled fluorescence assay B 4.94 pIC50 11400 nM IC50 Bioorg Med Chem (2019) 27: 895-930 [PMID:30744931]
ChEMBL Inhibition of human MAO-A expressed in baculovirus infected insect cell membranes using kynuramine as substrate up to 30 mins by spectrophotometric method B 4.96 pIC50 11000 nM IC50 Eur J Med Chem (2018) 148: 487-497 [PMID:29477889]
Monoamine oxidase B in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2039] [GtoPdb: 2490] [UniProtKB: P27338]
ChEMBL Inhibition of human MAO-B expressed in baculovirus infected insect cell membranes using kynuramine as substrate up to 30 mins by spectrophotometric method B 5.68 pIC50 2100 nM IC50 Eur J Med Chem (2018) 148: 487-497 [PMID:29477889]
ChEMBL Inhibition of recombinant human MAOB expressed in baculovirus infected BTI insect cells using p-tyramine as substrate by Amplex red reagent/horseradish peroxidase coupled fluorescence assay B 5.68 pIC50 2100 nM IC50 Bioorg Med Chem (2019) 27: 895-930 [PMID:30744931]
ChEMBL Inhibition of human MAOB B 5.72 pIC50 1900 nM IC50 Eur J Med Chem (2019) 180: 690-706 [PMID:31401465]

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]