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

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ChEMBL ligand: CHEMBL14638 (Ciproxifan)
  • acetylcholinesterase (Yt blood group)/Acetylcholinesterase in Human [ChEMBL: CHEMBL220] [GtoPdb: 2465] [UniProtKB: P22303]
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  • A1 receptor/Adenosine A1 receptor in Human [ChEMBL: CHEMBL226] [GtoPdb: 18] [UniProtKB: P30542]
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  • A2A receptor/Adenosine A2a receptor in Human [ChEMBL: CHEMBL251] [GtoPdb: 19] [UniProtKB: P29274]
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  • A2B receptor/Adenosine A2b receptor in Human [ChEMBL: CHEMBL255] [GtoPdb: 20] [UniProtKB: P29275]
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  • A3 receptor/Adenosine A3 receptor in Human [ChEMBL: CHEMBL256] [GtoPdb: 21] [UniProtKB: P0DMS8]
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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 (Yt 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]
A1 receptor/Adenosine A1 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL226] [GtoPdb: 18] [UniProtKB: P30542]
ChEMBL Displacement of [3H]CCPA from human recombinant adenosine A1 receptor expressed in CHO cells by liquid scintillation counting analysis B 6 pKi >1000 nM Ki J Med Chem (2021) 64: 8246-8262 [PMID:34107215]
A2A receptor/Adenosine A2a receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL251] [GtoPdb: 19] [UniProtKB: P29274]
ChEMBL Displacement of [3H]MSX-2 from human recombinant adenosine A2A receptor expressed in CHO cells by liquid scintillation counting analysis B 6 pKi >1000 nM Ki J Med Chem (2021) 64: 8246-8262 [PMID:34107215]
A2B receptor/Adenosine A2b receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL255] [GtoPdb: 20] [UniProtKB: P29275]
ChEMBL Displacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cells by liquid scintillation counting analysis B 6 pKi >1000 nM Ki J Med Chem (2021) 64: 8246-8262 [PMID:34107215]
A3 receptor/Adenosine A3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL256] [GtoPdb: 21] [UniProtKB: P0DMS8]
ChEMBL Displacement of [3H]PSB-11 from human recombinant adenosine A3 receptor expressed in CHO cells by liquid scintillation counting analysis B 6 pKi >1000 nM Ki J Med Chem (2021) 64: 8246-8262 [PMID:34107215]
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 Displacement of [3H] N-alpha methylhistamine from human recombinant histamine H3 receptor expressed in HEK293 cells measured after 90 mins B 6.65 pKi 224 nM Ki J Med Chem (2021) 64: 8246-8262 [PMID:34107215]
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 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 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 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 63.1 nM Ki J Med Chem (2005) 48: 38-55 [PMID:15634000]
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 nM Ki J Med Chem (2005) 48: 38-55 [PMID:15634000]
ChEMBL Binding affinity to human H3R B 7.2 pKi 63 nM Ki Eur J Med Chem (2021) 213: 113041-113041 [PMID:33261900]
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]UR-PI294 from human SP-FLAG-tagged H3R expressed in HEK293T cells measured after 60 to 120 mins by liquid scintillation counting analysis B 7.31 pKi 48.9 nM Ki Eur J Med Chem (2021) 213: 113041-113041 [PMID:33261900]
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 [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 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]
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 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]
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 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]