histamine [Ligand Id: 1204] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL90 (.beta.-aminoethylglyoxaline, Ergamine, Ergotidine, Histamine, NSC-33792)
  • H1 receptor/Histamine H1 receptor in Human [ChEMBL: CHEMBL231] [GtoPdb: 262] [UniProtKB: P35367]
  • H1 receptor/Histamine H1 receptor in Rat [ChEMBL: CHEMBL4701] [GtoPdb: 262] [UniProtKB: P31390]
  • Histamine H1 receptor in Guinea pig [ChEMBL: CHEMBL3943] [UniProtKB: P31389]
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  • H2 receptor/Histamine H2 receptor in Human [ChEMBL: CHEMBL1941] [GtoPdb: 263] [UniProtKB: P25021]
  • H2 receptor in Rat [GtoPdb: 263] [UniProtKB: P25102]
  • Histamine H2 receptor in Guinea pig [ChEMBL: CHEMBL2882] [UniProtKB: P47747]
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  • 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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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
H1 receptor/Histamine H1 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL231] [GtoPdb: 262] [UniProtKB: P35367]
ChEMBL Displacement of [3H]mepyramine from human wild-type histamine H1 receptor expressed in COS-7 cells by liquid scintillation counting B 4.1 pKi 79432.82 nM Ki Nat Chem Biol (2005) 1: 98-103 [PMID:16408006]
ChEMBL Displacement of [3H]mepyramine from human histamine H1 receptor S3.36T mutant expressed in COS-7 cells by liquid scintillation counting B 4.1 pKi 79432.82 nM Ki Nat Chem Biol (2005) 1: 98-103 [PMID:16408006]
ChEMBL Displacement of [3H]mepyramine from human histamine H1 receptor S3.36C mutant expressed in COS-7 cells by liquid scintillation counting B 4.4 pKi 39810.72 nM Ki Nat Chem Biol (2005) 1: 98-103 [PMID:16408006]
ChEMBL Displacement of [3H]mepyramine from human histamine H1 receptor N7.45Q mutant expressed in COS-7 cells by liquid scintillation counting B 4.5 pKi 31622.78 nM Ki Nat Chem Biol (2005) 1: 98-103 [PMID:16408006]
ChEMBL Displacement of [3H]mepyramine from human histamine H1 receptor N7.45C mutant expressed in COS-7 cells by liquid scintillation counting B 4.7 pKi 19952.62 nM Ki Nat Chem Biol (2005) 1: 98-103 [PMID:16408006]
ChEMBL Displacement of [3H]mepyramine from human histamine H1 receptor N7.45S mutant expressed in COS-7 cells by liquid scintillation counting B 4.9 pKi 12589.25 nM Ki Nat Chem Biol (2005) 1: 98-103 [PMID:16408006]
ChEMBL Binding affinity to histamine H1 receptor (unknown origin) B 5.22 pKi 6000 nM Ki J Med Chem (2015) 58: 7119-7127 [PMID:25993395]
ChEMBL Displacement of [3H]mepyramine from human histamine H1 receptor expressed in sf9 insect cell membranes co-expressing RGS4 incubated for 60 mins by microbeta scintillation counting method B 5.62 pKi 2398.83 nM Ki Eur J Med Chem (2021) 214: 113190-113190 [PMID:33548637]
GtoPdb - - 5.9 pKi - - - Eur J Biochem (1994) 224: 489-95 [PMID:7925364];
J Pharmacol Exp Ther (2002) 302: 328-36 [PMID:12065734];
J Pharmacol Exp Ther (2006) 317: 139-46 [PMID:16394198];
J Pharmacol Exp Ther (2003) 305: 1104-15 [PMID:12626648];
Eur J Biochem (2004) 271: 2636-46 [PMID:15206929]
ChEMBL Antagonism of the human histamine H1 receptor F 6 pIC50 ~1000 nM IC50 Bioorg Med Chem Lett (1997) 7: 2819-2824
ChEMBL Inhibitory activity against human Histamine H1 receptor B 6.8 pIC50 158.49 nM IC50 J Med Chem (2003) 46: 5812-5824 [PMID:14667234]
ChEMBL Agonist activity at human recombinant histamine H1 receptor expressed in Sf9 cells coexpressing RGS4 by steady-state GTPase activity assay F 6.7 pEC50 199.53 nM EC50 Bioorg Med Chem Lett (2010) 20: 7191-7199 [PMID:21044842]
ChEMBL Activity at human recombinant histamine H1 receptor expressed in Sf9 cells coexpressing RGS4 by steady-state GTPase activity assay B 6.72 pEC50 190.55 nM EC50 Bioorg Med Chem Lett (2010) 20: 3173-3176 [PMID:20409707]
ChEMBL Agonist activity at human recombinant histamine H1 receptor expressed in Sf9 cells coexpressing RGS4 preincubated for 2 mins before [gamma32P]GTP addition measured after 20 mins by steady-state GTPase activity assay B 6.72 pEC50 190.55 nM EC50 Medchemcomm (2014) 5: 72-81
ChEMBL Agonist activity at human H1 receptor expressed in insect Sf9 cells co-expressing RGS4 assessed as gamma[32P]GTP binding by liquid scintillation counting B 6.72 pEC50 190.55 nM EC50 J Med Chem (2009) 52: 2623-2627 [PMID:19317445]
ChEMBL Agonist activity at human histamine H1 receptor expressed in Sf9 cells coexpressing RGS4 by steady-state GTPase assay F 6.72 pEC50 190.55 nM EC50 J Med Chem (2009) 52: 6297-6313 [PMID:19791743]
ChEMBL Agonist activity at human histamine H1 receptor expressed in sf9 cell membrane co-expressing RGS4 or RGS9 assessed as increase in 32Pi level incubated for 20 mins by liquid scintillation counting in presence of [gamma32P]GTP B 6.72 pEC50 190 nM EC50 J Med Chem (2016) 59: 3452-3470 [PMID:27007611]
ChEMBL Activity at human recombinant histamine H1 receptor expressed in Sf9 cells coexpressing RGS4 by steady-state GTPase activity assay B 6.72 pEC50 190 nM EC50 J Med Chem (2008) 51: 7193-7204 [PMID:18950149]
ChEMBL Agonist activity at human H1 receptor expressed in 293-EBNA cells by luciferase reporter gene assay F 7.35 pEC50 45 nM EC50 J Med Chem (2006) 49: 5587-5596 [PMID:16942032]
ChEMBL Inhibition of human Histamine H1 receptor using [3H]pyrilamine B 7.89 pEC50 13 nM EC50 J Med Chem (2003) 46: 1980-1988 [PMID:12723960]
H1 receptor/Histamine H1 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4701] [GtoPdb: 262] [UniProtKB: P31390]
ChEMBL Relative potency against Histamine H1 receptor in rat aorta F 8 pKd 10 nM Kd J Med Chem (2003) 46: 5458-5470 [PMID:14640554]
ChEMBL Effective concentration against histamine H1 receptor in rat aorta B 5.35 pEC50 4466.84 nM EC50 J Med Chem (2003) 46: 5458-5470 [PMID:14640554]
Histamine H1 receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3943] [UniProtKB: P31389]
ChEMBL Compound was evaluated for mepyramine antagonism effects in guinea pig aorta (relaxation) at a mepyramine concentration of 100 nM F 8 pKd 10 nM Kd J Med Chem (2000) 43: 1071-1084 [PMID:10737740]
ChEMBL Relative potency against Histamine H1 receptor in endothelium-Denuded rings of guinea pig Aorta F 9 pKd 1 nM Kd J Med Chem (2003) 46: 5458-5470 [PMID:14640554]
ChEMBL Compound was evaluated for mepyramine antagonism effects in guinea pig aorta (contraction) at a mepyramine concentration of 100 nM F 9 pKd 1 nM Kd J Med Chem (2000) 43: 1071-1084 [PMID:10737740]
ChEMBL Compound was evaluated for mepyramine antagonism effects in guinea pig ileum (contraction) at a mepyramine concentration of 100 nM F 9.07 pKd 0.85 nM Kd J Med Chem (2000) 43: 1071-1084 [PMID:10737740]
ChEMBL Contractile effects antagonized by mepyramine (0.3-100 nM) against Histamine H1 receptor in guinea pig ileum F 9.07 pKd 0.85 nM Kd Bioorg Med Chem Lett (1998) 8: 2583-2588 [PMID:9873585]
ChEMBL Compound was evaluated for mepyramine antagonism effects in guinea pig ileum (contraction) at a mepyramine concentration of 100 nM F 9.11 pKd 0.78 nM Kd J Med Chem (2000) 43: 1071-1084 [PMID:10737740]
ChEMBL Compound was tested for the contractile effects antagonized by mepyramine (1-1000 nM) against Histamine H1 receptor of guinea pig aorta. F 9.11 pKd 0.78 nM Kd Bioorg Med Chem Lett (1998) 8: 2583-2588 [PMID:9873585]
ChEMBL Binding affinity against H1 receptor of guinea pig by the displacement of [3H]mepyramine, bound to membranes of CHO cells B 4.9 pKi 12589.25 nM Ki J Med Chem (1995) 38: 266-271 [PMID:7830269]
ChEMBL Effective concentration against histamine H1 receptor in guinea pig ileum B 6.7 pEC50 199.53 nM EC50 J Med Chem (2003) 46: 5458-5470 [PMID:14640554]
ChEMBL Agonist activity at histamine H1 receptor in guinea pig ileum F 6.7 pEC50 199.53 nM EC50 Bioorg Med Chem Lett (2006) 16: 672-676 [PMID:16266803]
ChEMBL Effective concentration against histamine H1 receptor in endothelium-Denuded rings of guinea pig Aorta B 6.79 pEC50 162.18 nM EC50 J Med Chem (2003) 46: 5458-5470 [PMID:14640554]
H2 receptor/Histamine H2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1941] [GtoPdb: 263] [UniProtKB: P25021]
ChEMBL Displacement of [125I]iodoaminopotentidine from human histamine H2 receptor expressed in CHO cells B 4.3 pKi 50118.72 nM Ki Bioorg Med Chem Lett (2010) 20: 7191-7199 [PMID:21044842]
ChEMBL Binding affinity against human H2 receptor by the displacement of [125I]iodoaminopotentidine, bound to membranes of CHO cells. B 4.4 pKi 39810.72 nM Ki J Med Chem (1995) 38: 266-271 [PMID:7830269]
ChEMBL Binding affinity to histamine H2 receptor (unknown origin) B 5.3 pKi 5000 nM Ki J Med Chem (2015) 58: 7119-7127 [PMID:25993395]
ChEMBL Displacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins by scintillation counting method B 6.53 pKi 295.12 nM Ki ACS Med Chem Lett (2020) 11: 1521-1528 [PMID:32832018]
ChEMBL Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method B 6.58 pKi 263.03 nM Ki Eur J Med Chem (2021) 214: 113190-113190 [PMID:33548637]
ChEMBL Displacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in Sf9 cell membranes by competitive binding assay B 6.58 pKi 263.03 nM Ki Bioorg Med Chem Lett (2021) 52: 128388-128388 [PMID:34600035]
ChEMBL Agonist activity at human H2 receptor expressed in HEK293T-ARRB1 cells assessed as stimulation of beta-arrestin 1 recruitment F 5.26 pEC50 5495.41 nM EC50 Bioorg Med Chem Lett (2021) 52: 128388-128388 [PMID:34600035]
ChEMBL Agonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assay F 5.42 pEC50 3801.89 nM EC50 Eur J Med Chem (2021) 214: 113190-113190 [PMID:33548637]
ChEMBL Agonist activity at NlucN/mini-Gi protein-fused human H2R stably expressed in HEK293T cells assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assay F 5.42 pEC50 3801.89 nM EC50 Bioorg Med Chem Lett (2021) 52: 128388-128388 [PMID:34600035]
ChEMBL Antagonist activity at Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins in presence of histamine by GTPgammaS binding assay F 5.8 pEC50 1584.89 nM EC50 ACS Med Chem Lett (2020) 11: 1521-1528 [PMID:32832018]
ChEMBL Agonist activity at human H2 receptor expressed in Sf9 cell membranes co-exprssing GsalphaS assessed as stimulation of [35S]GTPgammaS binding incubated for 90 mins by scintillation counting analysis F 5.85 pEC50 1412.54 nM EC50 Bioorg Med Chem Lett (2021) 52: 128388-128388 [PMID:34600035]
ChEMBL Agonist activity at GsalphaS-fused human histamine H2 receptor expressed in Sf9 cells by [35S]GTPgammaS binding assay F 5.9 pEC50 1258.93 nM EC50 Bioorg Med Chem Lett (2010) 20: 3173-3176 [PMID:20409707]
ChEMBL Agonist activity at human recombinant histamine H2 receptor-Gsalphas fusion protein expressed in Sf9 cells assessed as [35S]GTPgammaS binding after 90 mins by liquid scintillation counting F 5.92 pEC50 1202.26 nM EC50 Medchemcomm (2014) 5: 72-81
ChEMBL Agonist activity at human H2 receptor expressed in insect Sf9 cells co-expressing GsalphaS fusion protein assessed as gamma[32P]GTP binding by liquid scintillation counting B 5.92 pEC50 1202.26 nM EC50 J Med Chem (2009) 52: 2623-2627 [PMID:19317445]
ChEMBL Agonist activity at human histamine H2 receptor expressed in Sf9 cells coexpressing GsalphaS protein by steady-state GTPase assay F 5.92 pEC50 1202.26 nM EC50 J Med Chem (2009) 52: 6297-6313 [PMID:19791743]
ChEMBL Agonist activity at human recombinant histamine H2 receptor-Gsalphas fusion protein expressed in Sf9 cells preincubated for 2 mins before [gamma32P]GTP addition measured after 20 mins by steady-state GTPase activity assay B 5.92 pEC50 1202.26 nM EC50 Medchemcomm (2014) 5: 72-81
ChEMBL Activity at human recombinant histamine H2 receptor-Gsalpha fusion protein expressed in Sf9 cells by steady-state GTPase activity assay B 5.92 pEC50 1200 nM EC50 J Med Chem (2008) 51: 7193-7204 [PMID:18950149]
ChEMBL Agonist activity at human histamine receptor expressed in sf9 insect cell membranes co-exprssing GsalphaS incubated for 90 mins [35S]GTPgammaS binding based microbeta scintillation counting analysis F 6.01 pEC50 977.24 nM EC50 Eur J Med Chem (2021) 214: 113190-113190 [PMID:33548637]
ChEMBL Agonist activity at human H2 receptor expressed in 293-EBNA cells by luciferase reporter gene assay F 6.19 pEC50 650 nM EC50 J Med Chem (2006) 49: 5587-5596 [PMID:16942032]
ChEMBL Inhibition of human Histamine H2 receptor using [3H]tiotidine B 6.33 pEC50 463 nM EC50 J Med Chem (2003) 46: 1980-1988 [PMID:12723960]
ChEMBL Agonist activity at human H2 receptor expressed in HEK293T-ARRB2 cells assessed as stimulation of beta-arrestin 2 recruitment F 6.94 pEC50 114.82 nM EC50 Bioorg Med Chem Lett (2021) 52: 128388-128388 [PMID:34600035]
H2 receptor in Rat [GtoPdb: 263] [UniProtKB: P25102]
GtoPdb - - 3.8 pKi - - - Br J Pharmacol (1997) 122: 867-74 [PMID:9384502]
Histamine H2 receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2882] [UniProtKB: P47747]
ChEMBL Compound is evaluated for histamine H2 receptor agonistic activity in guinea pig cerebral cortex using [3H]tiotidine as radioligand F 4.16 pKd 69183.1 nM Kd J Med Chem (1992) 35: 3239-3246 [PMID:1507209]
ChEMBL Agonist activity at GsalphaS-fused guinea pig histamine H2 receptor expressed in Sf9 cells by [35S]GTPgammaS binding assay F 5.92 pEC50 1202.26 nM EC50 Bioorg Med Chem Lett (2010) 20: 3173-3176 [PMID:20409707]
ChEMBL Activity at guinea pig recombinant histamine H2 receptor-Gsalpha fusion protein expressed in Sf9 cells by steady-state GTPase activity assay B 5.92 pEC50 1200 nM EC50 J Med Chem (2008) 51: 7193-7204 [PMID:18950149]
ChEMBL Agonist activity at histamine H2 receptor in guinea pig spontaneously beating right atrium assessed as positive chronotropic activity F 6 pEC50 1000 nM EC50 J Med Chem (2008) 51: 7193-7204 [PMID:18950149]
ChEMBL Agonist activity at guinea pig atrium histamine H2 receptor assessed as potentiation of histamine-induced response after 30 mins B 6 pEC50 1000 nM EC50 Medchemcomm (2014) 5: 72-81
ChEMBL Agonist activity at histamine H2 receptor in spontaneously beating guinea pig atrium F 6 pEC50 1000 nM EC50 Bioorg Med Chem Lett (2010) 20: 3173-3176 [PMID:20409707]
ChEMBL Agonist activity at histamine H2 receptor in guinea pig atrium assessed as increase in heart rate F 6 pEC50 1000 nM EC50 J Med Chem (2009) 52: 2623-2627 [PMID:19317445]
ChEMBL Agonist activity at guinea pig right atrium histamine H2 receptor assessed as increase in heart rate incubated for 30 mins in presence of cimetidine F 6.16 pEC50 691.83 nM EC50 Eur J Med Chem (2021) 214: 113190-113190 [PMID:33548637]
H3 receptor/Histamine H3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL264] [GtoPdb: 264] [UniProtKB: Q9Y5N1]
ChEMBL Binding affinity in Nluc-hH3R assessed in HEK293 cells by NanoBRET binding assay B 6.23 pKi 588.84 nM Ki J Med Chem (2021) 64: 11695-11708 [PMID:34309390]
ChEMBL Binding affinity in Nluc-hH3R assessed in HEK293T cells by NanoBRET binding assay B 6.3 pKi 501.19 nM Ki J Med Chem (2021) 64: 11695-11708 [PMID:34309390]
ChEMBL Histamine H3 receptor competition binding using [3H]Na-methylhistamine B 7.47 pKi 33.88 nM Ki J Med Chem (2003) 46: 3162-3165 [PMID:12825954]
ChEMBL Displacement of [3H]UR-P129 from human histamine H3 receptor expressed in sf9 insect cell membranes co-expressing Galphai2/Gbeta1gamma2 incubated for 60 mins by microbeta scintillation counting method B 7.59 pKi 25.7 nM Ki Eur J Med Chem (2021) 214: 113190-113190 [PMID:33548637]
ChEMBL Binding affinity to histamine H3 receptor (unknown origin) B 7.8 pKi 16 nM Ki J Med Chem (2015) 58: 7119-7127 [PMID:25993395]
ChEMBL Binding affinity to histamine H3 receptor (unknown origin) B 7.89 pKi 12.8 nM Ki Bioorg Med Chem Lett (2016) 26: 5263-5266 [PMID:27692832]
ChEMBL Displacement of [3H]NAMH from human H3R expressed in HEK293T cells incubated for 2 hrs by microbeta scintillation counting analysis B 7.9 pKi 12.59 nM Ki J Med Chem (2019) 62: 10848-10866 [PMID:31675226]
ChEMBL Displacement of [3H]N-alpha-methylhistamine from human histamine H3 receptor expressed in HEK293 cells after 60 mins by liquid scintillation counting B 7.93 pKi 11.75 nM Ki J Med Chem (2011) 54: 1693-1703 [PMID:21348462]
ChEMBL Displacement of [3H]Nalpha-methylhistamine from human histamine H3 receptor expressed in human SK-N-MC cells B 8 pKi 10 nM Ki Bioorg Med Chem Lett (2010) 20: 7191-7199 [PMID:21044842]
ChEMBL Displacement of [3H]-N-alpha-methylhistamine from human histamine H3 receptor expressed in SK-N-MC cells incubated for 40 min by liquid scintillation counting analysis B 8 pKi 10 nM Ki J Med Chem (2019) 62: 10848-10866 [PMID:31675226]
ChEMBL Inhibitory activity measured by [3H]- N alpha- methyl-histamine binding to membranes of SK-N-MC cells expressing the human Histamine H3 receptor B 8.03 pKi 9.33 nM Ki J Med Chem (2003) 46: 5445-5457 [PMID:14640553]
ChEMBL Displacement of [3H]histamine from human H3 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting B 8.2 pKi 6.31 nM Ki J Med Chem (2011) 54: 8136-8147 [PMID:22003888]
ChEMBL Displacement of [3H[N-alpha-methylhistamine form human recombinant histamine H3 receptor expressed in CHO cells after 1 hr by liquid scintillation counting B 8.28 pKi 5.2 nM Ki J Med Chem (2010) 53: 3840-3844 [PMID:20384344]
GtoPdb - - 8.3 pKi - - - J Pharmacol Exp Ther (2000) 293: 771-8 [PMID:10869375];
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];
Mol Pharmacol (2001) 59: 420-6 [PMID:11179434];
J Med Chem (2003) 46: 5445-57 [PMID:14640553]
ChEMBL Displacement of [3H]-Histamine from human histamine 3 receptor transfected in HEK293T cells incubated for 16 hrs by liquid scintillation counter analysis B 8.6 pKi 2.51 nM Ki Bioorg Med Chem (2021) 30: 115924-115924 [PMID:33333448]
ChEMBL Agonist activity at human recombinant histamine H3 receptor expressed in CHO cells assessed as [35S]GTPgammaS binding after 1 hr by liquid scintillation counting F 6.19 pEC50 640 nM EC50 J Med Chem (2010) 53: 3840-3844 [PMID:20384344]
ChEMBL Agonist activity at human H3 receptor expressed in 293-EBNA cells by luciferase reporter gene assay F 7.06 pEC50 88 nM EC50 J Med Chem (2006) 49: 5587-5596 [PMID:16942032]
ChEMBL Inhibition of human Histamine H3 receptor using [3H]N-alpha-methyl histamine B 7.11 pEC50 77 nM EC50 J Med Chem (2003) 46: 1980-1988 [PMID:12723960]
ChEMBL Agonist activity at human H3R expressed on HEK293T cells by [35S]GTPgammaS binding assay F 7.2 pEC50 63.1 nM EC50 J Med Chem (2019) 62: 10848-10866 [PMID:31675226]
ChEMBL Agonist activity at human H3 receptor stably transfected in CHO-DUKX cells assessed as increase in cAMP accumulation by measuring reduction in forskolin level by HitHunter-cAMP assay F 7.52 pEC50 30 nM EC50 Eur J Med Chem (2020) 191: 112150-112150 [PMID:32105981]
ChEMBL Agonist activity at human H3 receptor expressed in insect Sf9 cells co-expressing Gialpha2, Gbeta1gamma2 and RGS4 assessed as gamma[32P]GTP binding by liquid scintillation counting B 7.6 pEC50 25.12 nM EC50 J Med Chem (2009) 52: 2623-2627 [PMID:19317445]
ChEMBL Agonist activity at human histamine H3 receptor expressed in Sf9 cells coexpressing Gialpha-2-Gbeta-1-gamma-2 and RGS4 proteins protein by steady-state GTPase assay F 7.6 pEC50 25.12 nM EC50 J Med Chem (2009) 52: 6297-6313 [PMID:19791743]
ChEMBL Agonist activity at human recombinant histamine H3 receptor expressed in Sf9 cells coexpressing Galphai2,Gbeta1gamma2 and RGS4 preincubated for 2 mins before [gamma32P]GTP addition measured after 20 mins by steady-state GTPase activity assay B 7.6 pEC50 25.12 nM EC50 Medchemcomm (2014) 5: 72-81
ChEMBL Activity at human recombinant histamine H3 receptor expressed in Sf9 cells coexpressing Galphai, G-beta-1-gamma-2 and RGS4 by steady-state GTPase activity assay B 7.6 pEC50 25.1 nM EC50 J Med Chem (2008) 51: 7193-7204 [PMID:18950149]
ChEMBL Agonist activity at human histamine H3 receptor expressed in HEK293 cells assessed by forskolin induced cAMP response element activation by luciferase reporter gene assay F 7.8 pEC50 15.85 nM EC50 J Med Chem (2011) 54: 1693-1703 [PMID:21348462]
ChEMBL Agonist activity at human histamine H3 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assay F 7.89 pEC50 13 nM EC50 J Med Chem (2016) 59: 3452-3470 [PMID:27007611]
ChEMBL Agonist activity at human recombinant histamine H3 receptor expressed in Sf9 cells coexpressing Galphai2,Gbeta1gamma2 and RGS4 assessed as [35S]GTPgammaS binding after 90 mins by liquid scintillation counting F 7.89 pEC50 12.88 nM EC50 Medchemcomm (2014) 5: 72-81
ChEMBL Activity at human recombinant histamine H3 receptor expressed in Sf9 cells coexpressing Galphai, Gbeta1gamma2 and RGS4 by steady-state GTPase activity assay B 7.89 pEC50 12.88 nM EC50 Bioorg Med Chem Lett (2010) 20: 3173-3176 [PMID:20409707]
ChEMBL Inhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H3 receptor B 8.01 pEC50 9.77 nM EC50 J Med Chem (2003) 46: 5445-5457 [PMID:14640553]
ChEMBL Agonist activity at human histamine H3 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay F 8.3 pEC50 5.01 nM EC50 Bioorg Med Chem Lett (2010) 20: 7191-7199 [PMID:21044842]
ChEMBL Agonist activity at human H3R expressed on SK-N-MC cells assessed as inhibition of forskolin-induced beta galactosidase activity preincubated with forskolin for 6 hrs followed compound addition by CRE-luciferase reporter gene assay F 8.3 pEC50 5.01 nM EC50 J Med Chem (2019) 62: 10848-10866 [PMID:31675226]
ChEMBL Inhibition of the forskolin-stimulated cAMP production in SK-N-MC cells expressing human Histamine H3 receptor F 8.39 pEC50 4.07 nM EC50 J Med Chem (2003) 46: 3162-3165 [PMID:12825954]
ChEMBL Agonist activity at human H3 receptor expressed in CHO cells assessed as increase in cAMP accumulation by measuring reduction in forskolin level incubated for 4 hrs by CRE/MRE-luciferase reporter gene assay F 8.4 pEC50 4 nM EC50 Eur J Med Chem (2020) 191: 112150-112150 [PMID:32105981]
ChEMBL Agonist activity at human H3R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by CRE-luciferase reporter gene assay F 8.6 pEC50 2.51 nM EC50 J Med Chem (2019) 62: 10848-10866 [PMID:31675226]
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 7.17 pKi 68 nM Ki Bioorg Med Chem Lett (2009) 19: 4075-4078 [PMID:19553110]
GtoPdb - - 7.8 pKi - - - Eur J Pharmacol (2003) 467: 57-65 [PMID:12706455];
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]
GtoPdb - - 7.9 pKi - - - J Pharmacol Exp Ther (2000) 293: 771-8 [PMID:10869375];
Biochem Biophys Res Commun (2001) 280: 75-80 [PMID:11162480];
Br J Pharmacol (2000) 131: 1247-50 [PMID:11090094]
ChEMBL In vitro binding affinity was measured against Histamine H3 receptor on rat cerebral cortex. B 8.2 pKi 6.31 nM Ki J Med Chem (1999) 42: 1115-1122 [PMID:10197956]
Histamine H3 receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5076] [UniProtKB: Q9JI35]
ChEMBL Binding affinity towards histamine H3 receptor using [3H](R)-alpha-methylhistamine as radioligand in guinea pig ileum LMMP homogenates B 7.98 pKi 10.47 nM Ki Bioorg Med Chem Lett (1999) 9: 1825-1830 [PMID:10406649]
ChEMBL Binding affinity towards histamine H3 receptor using [3H](R)-alpha-methylhistamine as radioligand in guinea pig cortical homogenates B 9.84 pKi 0.14 nM Ki Bioorg Med Chem Lett (1999) 9: 1825-1830 [PMID:10406649]
H4 receptor/Histamine H4 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3759] [GtoPdb: 265] [UniProtKB: Q9H3N8]
ChEMBL Binding affinity to human H4R B 8.3 pKd 5 nM Kd J Med Chem (2019) 62: 8338-8356 [PMID:31469288]
ChEMBL Displacement of [3H]histamine from human recombinant histamine H4 receptor B 7.22 pKi 60 nM Ki Bioorg Med Chem Lett (2010) 20: 3367-3371 [PMID:20452213]
ChEMBL Displacement of [3H]histamine from human histamine H4 receptor expressed in sf9 insect cell membranes co-expressing Galphai2/Gbeta1gamma2 incubated for 60 mins by microbeta scintillation counting method B 7.6 pKi 25.12 nM Ki Eur J Med Chem (2021) 214: 113190-113190 [PMID:33548637]
ChEMBL Displacement of [3H]histamine from wild type human histamine H4 receptor transfected in HEK293T cells after 1 hr by liquid scintillation counting analysis B 7.7 pKi 19.95 nM Ki Medchemcomm (2013) 4: 193-204
ChEMBL Displacement of [3H]histamine from human H4 receptor 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 histamine H4 receptor expressed in human SK-N-MC cells after 1 hr B 7.8 pKi 15.85 nM Ki Medchemcomm (2015) 6: 1003-1017
ChEMBL Inhibition of [3H]-histamine binding to membranes of SK-N-MC cells expressing the human Histamine H4 receptor B 7.84 pKi 14.45 nM Ki J Med Chem (2003) 46: 5445-5457 [PMID:14640553]
ChEMBL Displacement of [3H]histamine from human histamine H4 receptor expressed in SK-NM-C cells B 7.87 pKi 13.4 nM Ki J Med Chem (2008) 51: 3145-3153 [PMID:18459760]
ChEMBL Binding affinity to human recombinant histamine H4 receptor expressed in human SK-N-MC cells by radioligand displacement assay B 7.9 pKi 12.59 nM Ki Bioorg Med Chem Lett (2010) 20: 7191-7199 [PMID:21044842]
ChEMBL Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells B 7.92 pKi 12.02 nM Ki J Med Chem (2010) 53: 2390-2400 [PMID:20192225]
ChEMBL Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells after 60 mins by liquid scintillation counting B 7.92 pKi 12.02 nM Ki J Med Chem (2011) 54: 1693-1703 [PMID:21348462]
ChEMBL Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells B 7.92 pKi 12.02 nM Ki J Med Chem (2008) 51: 2457-2467 [PMID:18357976]
ChEMBL Displacement of [3H]histamine from human H4 receptor expressed in HEK cell membranes B 8.05 pKi 9 nM Ki Bioorg Med Chem Lett (2012) 22: 461-467 [PMID:22153663]
ChEMBL Binding affinity to histamine H4 receptor (unknown origin) B 8.1 pKi 8 nM Ki J Med Chem (2015) 58: 7119-7127 [PMID:25993395]
ChEMBL Binding affinity towards human histamine H4 receptor was determined by [3H]Na-methylhistamine binding to SK-N-MC cell membranes B 8.1 pKi 7.94 nM Ki Bioorg Med Chem Lett (2004) 14: 5251-5256 [PMID:15454206]
ChEMBL Displacement of [3H]-histamine from human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2 B 8.1 pKi 7.94 nM Ki Bioorg Med Chem Lett (2010) 20: 7191-7199 [PMID:21044842]
GtoPdb - - 8.3 pKi - - - 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];
Mol Pharmacol (2001) 59: 434-41 [PMID:11179436];
J Pharmacol Exp Ther (2005) 314: 1310-21 [PMID:15947036];
Br J Pharmacol (2006) 147: 744-54 [PMID:16432504];
Bioorg Med Chem Lett (2004) 14: 5251-6 [PMID:15454206]
ChEMBL Binding affinity to human histamine H4 receptor B 8.32 pKi 4.8 nM Ki J Med Chem (2015) 58: 7119-7127 [PMID:25993395]
ChEMBL Binding affinity to histamine H4 receptor (unknown origin) B 8.8 pKi 1.6 nM Ki Bioorg Med Chem Lett (2016) 26: 5263-5266 [PMID:27692832]
ChEMBL Displacement of [3H]-Histamine from human histamine 4 receptor transfected in HEK293T cells incubated for 16 hrs by liquid scintillation counter analysis B 9 pKi 1 nM Ki Bioorg Med Chem (2021) 30: 115924-115924 [PMID:33333448]
ChEMBL Agonist activity at human H4 receptor expressed in 293-EBNA cells by luciferase reporter gene assay F 5.74 pEC50 1800 nM EC50 J Med Chem (2006) 49: 5587-5596 [PMID:16942032]
ChEMBL Agonist activity at human recombinant histamine H4 receptor expressed in human SK-N-MC cells co-expressing SRE-Luc by luciferase reporter gene assay F 7.1 pEC50 79.43 nM EC50 Bioorg Med Chem Lett (2010) 20: 7191-7199 [PMID:21044842]
ChEMBL Inhibition of human Histamine H4 receptor B 7.12 pEC50