clobenpropit [Ligand Id: 1223] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL14690 (Clobenpropit)
  • H3 receptor/Histamine H3 receptor in Human [ChEMBL: CHEMBL264] [GtoPdb: 264] [UniProtKB: Q9Y5N1]
  • H3 receptor/Histamine H3 receptor in Mouse [ChEMBL: CHEMBL3263] [GtoPdb: 264] [UniProtKB: P58406]
  • H3 receptor/Histamine H3 receptor in Rat [ChEMBL: CHEMBL4124] [GtoPdb: 264] [UniProtKB: Q9QYN8]
  • Histamine H3 receptor in Guinea pig [ChEMBL: CHEMBL5076] [UniProtKB: Q9JI35]
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  • H4 receptor/Histamine H4 receptor in Human [ChEMBL: CHEMBL3759] [GtoPdb: 265] [UniProtKB: Q9H3N8]
  • H4 receptor/Histamine H4 receptor in Mouse [ChEMBL: CHEMBL5657] [GtoPdb: 265] [UniProtKB: Q91ZY2]
  • H4 receptor in Rat [GtoPdb: 265] [UniProtKB: Q91ZY1]
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  • H1 receptor in Human [GtoPdb: 262] [UniProtKB: P35367]
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  • H2 receptor in Human [GtoPdb: 263] [UniProtKB: P25021]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
H3 receptor/Histamine H3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL264] [GtoPdb: 264] [UniProtKB: Q9Y5N1]
ChEMBL Antagonist activity at human histamine H3 receptor expressed in CHO cells assessed as inhibition of forskolin/R-alpha-methylhistamine-induced cAMP accumulation after 1.5 hrs by TR-FRET immunoassay F 10 pKd 0.1 nM Kd Bioorg. Med. Chem. Lett. (2013) 23: 6415-6420 [PMID:24140447]
ChEMBL Displacement of [3H]N-alpha-methylhistamine from human histamine H3 receptor expressed in human SK-N-MC cells by liquid scintillation counting B 8.5 pKi 3.16 nM Ki Bioorg. Med. Chem. (2009) 17: 3987-3994 [PMID:19414267]
ChEMBL Displacement of [3H]histamine from human H3 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting B 8.55 pKi 2.82 nM Ki J. Med. Chem. (2011) 54: 8136-8147 [PMID:22003888]
ChEMBL Inhibition of [125I]iodoproxyfan binding to human histamine H3 receptor of CHO-K1 cells B 8.62 pKi 2.4 nM Ki Bioorg. Med. Chem. Lett. (2001) 11: 951-954 [PMID:11294398]
ChEMBL Displacement of [125I]iodoproxyfan from human histamine H3 receptor expressing CHO cells B 8.62 pKi 2.4 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 8.62 pKi 2.4 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 8.62 pKi 2.4 nM Ki Bioorg. Med. Chem. (2011) 19: 2850-2858 [PMID:21498080]
ChEMBL Antagonist potency against human H3 receptor in GTPgamma-S-Assay F 9.22 pKi 0.6 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 9.24 pKi 0.58 nM Ki J. Med. Chem. (2004) 47: 2833-2838 [PMID:15139761]
GtoPdb - - 9.41 pKi 0.39 nM Ki J Pharmacol Exp Ther (2003) 305: 887-96 [PMID:12606603];
J Pharmacol Exp Ther (2000) 293: 771-8 [PMID:10869375];
Biochem J (2001) 355: 279-88 [PMID:11284713];
J Pharmacol Exp Ther (2001) 299: 908-14 [PMID:11714875];
Br J Pharmacol (2000) 131: 1247-50 [PMID:11090094];
Eur J Pharmacol (2002) 453: 33-41 [PMID:12393057];
Mol Pharmacol (2001) 59: 420-6 [PMID:11179434]
ChEMBL Displacement of [3H]N-alpha-methylhistamine from human histamine H3 receptor expressed in CHO cells B 9.47 pKi 0.34 nM Ki J. Med. Chem. (2008) 51: 2944-2953 [PMID:18433114]
ChEMBL Antagonist activity against human histamine H3 receptor expressed in human HT1080 cells assessed as inhibition of (R)-alpha-methylhistamine-induced increase in intracellular calcium level by FLIPR assay F 9 pIC50 1 nM IC50 Bioorg. Med. Chem. Lett. (2010) 20: 6246-6249 [PMID:20833043]
ChEMBL Antagonist activity at human histamine H3 receptor expressed in CHO cells assessed as inhibition of forskolin/R-alpha-methylhistamine-induced cAMP accumulation after 1.5 hrs by TR-FRET immunoassay F 9.1 pIC50 0.79 nM IC50 Bioorg. Med. Chem. Lett. (2013) 23: 6415-6420 [PMID:24140447]
H3 receptor/Histamine H3 receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3263] [GtoPdb: 264] [UniProtKB: P58406]
ChEMBL Displacement of 3-([1,1,1-3H]methyl)-2-(4-{[3-(1-pyrrolidinyl)propyl]oxy}phenyl)-4(3H)-quinazolinone from mouse histamine H3 receptor expressed in HEK293 cells B 9.22 pKi 0.6 nM Ki Bioorg. Med. Chem. Lett. (2009) 19: 4075-4078 [PMID:19553110]
GtoPdb - - 9.5 pKi - - - Eur J Pharmacol (2003) 467: 57-65 [PMID:12706455]
ChEMBL Antagonist activity against mouse histamine H3 receptor expressed in human HT1080 cells assessed as inhibition of (R)-alpha-methylhistamine-induced increase in intracellular calcium level by FLIPR assay F 9 pIC50 1 nM IC50 Bioorg. Med. Chem. Lett. (2010) 20: 6246-6249 [PMID:20833043]
ChEMBL Inverse agonist activity at mouse histamine H3 receptor overexpressed in HEK293 cells by [35S]GTPgammaS binding assay F 8.77 pEC50 1.7 nM EC50 Bioorg. Med. Chem. Lett. (2009) 19: 4075-4078 [PMID:19553110]
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 8.85 pKi 1.4 nM Ki Bioorg. Med. Chem. Lett. (2001) 11: 951-954 [PMID:11294398]
ChEMBL In vitro antagonistic activity against histamine H3-receptor in an assay with K+-evoked depolarisation-induced release of [3H]histamine of synaptosomes of rat cerebral cortex F 9.2 pKi 0.63 nM Ki Bioorg. Med. Chem. Lett. (1996) 6: 2013-2018
ChEMBL Effect on histamine H3 receptors in vitro, on synaptosomes of rat cerebral cortex for the release of [3H]histamine B 9.22 pKi 0.6 nM Ki J. Med. Chem. (2000) 43: 3987-3994 [PMID:11052804]
ChEMBL In vitro antagonistic activity against Histamine H3 receptor on Synaptosomes of rat cerebral cortex. F 9.22 pKi 0.6 nM Ki J. Med. Chem. (1996) 39: 1157-1163 [PMID:8676353]
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 9.22 pKi 0.6 nM Ki Bioorg. Med. Chem. Lett. (2000) 10: 2379-2382 [PMID:11055360]
ChEMBL In vitro Histamine H3 receptor antagonist activity in an assay with K+-evoked depolarization-induced release of [3H]histamine from synaptosomes of rat cerebral cortex F 9.22 pKi 0.6 nM Ki Bioorg. Med. Chem. Lett. (1998) 8: 2011-2016 [PMID:9873477]
ChEMBL In vitro antagonist potency at Histamine H3 receptor measured as K+-evoked [3H]histamine release from synaptosomes of rat cerebral cortex. F 9.22 pKi 0.6 nM Ki J. Med. Chem. (1998) 41: 4171-4176 [PMID:9767653]
ChEMBL Effect at histamine H3 receptors (in vitro) on synaptosomes of rat cerebral cortex assayed by functional H3-receptor assay. B 9.22 pKi 0.6 nM Ki J. Med. Chem. (1999) 42: 593-600 [PMID:10052966]
ChEMBL Compound was tested for its ability to displace [3H]Nalpha-methylhistamine from histamine H3 receptors in homogenates of rat cerebral cortex B 9.6 pKi 0.25 nM Ki J. Med. Chem. (2001) 44: 1666-1674 [PMID:11356102]
ChEMBL Histamine H3 receptor affinity of compound was determined in rat cortical membranes using the H3 selective agonist ligand, [3H]N-alpha-methylhistamine F 9.74 pKi 0.18 nM Ki Bioorg. Med. Chem. Lett. (1997) 7: 3017-3022
ChEMBL Inhibition of [3H]- N-alpha-methylhistamine from histamine H3 receptor B 9.74 pKi 0.18 nM Ki Bioorg. Med. Chem. Lett. (1998) 8: 1133-1138 [PMID:9871722]
ChEMBL Binding affinity against H3 receptor in rat cerebral cortex membranes was evaluated using [3H]N-methyl-histamine as radioligand B 9.8 pKi 0.16 nM Ki Bioorg. Med. Chem. Lett. (1996) 6: 833-838
GtoPdb - - 9.8 pKi - - - J Pharmacol Exp Ther (2003) 305: 887-96 [PMID:12606603];
J Pharmacol Exp Ther (2000) 293: 771-8 [PMID:10869375];
J Pharmacol Exp Ther (2001) 299: 908-14 [PMID:11714875];
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]
Histamine H3 receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5076] [UniProtKB: Q9JI35]
ChEMBL Displacement of [3H]Nalpha-methylhistamine from histamine H3 receptors in homogenates of rat cerebral cortex B 9.8 pKd 0.16 nM Kd J. Med. Chem. (2001) 44: 1666-1674 [PMID:11356102]
H4 receptor/Histamine H4 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3759] [GtoPdb: 265] [UniProtKB: Q9H3N8]
ChEMBL Displacement of [3H]JNJ7777120 from human H4 receptor E5.46Q mutant expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting B 7.3 pKi 50.12 nM Ki J. Med. Chem. (2011) 54: 8136-8147 [PMID:22003888]
ChEMBL Displacement of [3H]histamine from human H4 receptor N4.57Y mutant expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting B 7.8 pKi 15.85 nM Ki J. Med. Chem. (2011) 54: 8136-8147 [PMID:22003888]
ChEMBL Displacement of [3H]histamine from human H4 receptor V3.40A mutant expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting B 8 pKi 10 nM Ki J. Med. Chem. (2011) 54: 8136-8147 [PMID:22003888]
ChEMBL Displacement of [3H]histamine from human histamine H4 receptor expressed in human SK-N-MC cells by liquid scintillation counting B 8 pKi 10 nM Ki Bioorg. Med. Chem. (2009) 17: 3987-3994 [PMID:19414267]
ChEMBL Displacement of [3H]histamine from human H4 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting B 8 pKi 10 nM Ki J. Med. Chem. (2011) 54: 8136-8147 [PMID:22003888]
GtoPdb - - 8.3 pKi 5.01 nM Ki J Pharmacol Exp Ther (2003) 305: 887-96 [PMID:12606603];
Mol Pharmacol (2001) 59: 420-6 [PMID:11179434];
J Pharmacol Exp Ther (2001) 299: 121-30 [PMID:11561071];
J Pharmacol Exp Ther (2001) 296: 1058-66 [PMID:11181941];
J Pharmacol Exp Ther (2005) 314: 1310-21 [PMID:15947036]
ChEMBL Displacement of [3H]histamine from human histamine H4 receptor expressed in SK-NM-C cells B 8.3 pKi 5 nM Ki J. Med. Chem. (2008) 51: 3145-3153 [PMID:18459760]
ChEMBL Displacement of [3H]histamine from human full-length histamine H4 receptor expressed in HEK293 cells after 60 mins B 8.37 pKi 4.3 nM Ki Bioorg. Med. Chem. (2011) 19: 2850-2858 [PMID:21498080]
ChEMBL Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells B 8.37 pKi 4.3 nM Ki Bioorg. Med. Chem. Lett. (2009) 19: 6682-6685 [PMID:19846299]
ChEMBL Displacement of [3H]histamine from human H4 receptor T5.42A mutant expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting B 8.6 pKi 2.51 nM Ki J. Med. Chem. (2011) 54: 8136-8147 [PMID:22003888]
ChEMBL Displacement of [3H]histamine from human H4 receptor T6.55M mutant expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting B 8.8 pKi 1.58 nM Ki J. Med. Chem. (2011) 54: 8136-8147 [PMID:22003888]
ChEMBL Displacement of [3H]histamine from human H4 receptor Q7.42L mutant expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting B 9 pKi 1 nM Ki J. Med. Chem. (2011) 54: 8136-8147 [PMID:22003888]
ChEMBL Agonist activity at human H4R by [35S]-GTPgammaS-binding assay B 7.65 pEC50 22.39 nM EC50 J Med Chem (2019) 62: 8338-8356 [PMID:31469288]
H4 receptor/Histamine H4 receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5657] [GtoPdb: 265] [UniProtKB: Q91ZY2]
GtoPdb - - 7.8 pKi - - - J Pharmacol Exp Ther (2001) 299: 121-30 [PMID:11561071]
ChEMBL Agonist activity at mouse H4R by [35S]-GTPgammaS-binding assay B 6.07 pEC50 851.14 nM EC50 J Med Chem (2019) 62: 8338-8356 [PMID:31469288]
H4 receptor in Rat [GtoPdb: 265] [UniProtKB: Q91ZY1]
GtoPdb - - 7.2 pKi - - - J Pharmacol Exp Ther (2001) 299: 121-30 [PMID:11561071]
H1 receptor in Human [GtoPdb: 262] [UniProtKB: P35367]
GtoPdb - - 5.6 pKi - - - J Pharmacol Exp Ther (2003) 305: 887-96 [PMID:12606603]
H2 receptor in Human [GtoPdb: 263] [UniProtKB: P25021]
GtoPdb - - 5.2 pKi - - - J Pharmacol Exp Ther (2003) 305: 887-96 [PMID:12606603]

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]