[3H]histamine [Ligand Id: 1247] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL90 (.beta.-aminoethylglyoxaline, Ergamine, Ergotidine, Histamine, NSC-33792) |
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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 histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysis | B | 8.35 | pKd | 4.5 | nM | Kd | J Med Chem (2021) 64: 8684-8709 [PMID:34110814] |
| 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] |
| ChEMBL | Displacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysis | B | 5.62 | pKi | 2398.83 | nM | Ki | J Med Chem (2021) 64: 8684-8709 [PMID:34110814] |
| 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 [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis | B | 7.91 | pKd | 12.2 | nM | Kd | J Med Chem (2021) 64: 8684-8709 [PMID:34110814] |
| 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 | Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis | B | 6.58 | pKi | 263.03 | nM | Ki | J Med Chem (2021) 64: 8684-8709 [PMID:34110814] |
| 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 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 | 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 human histamine H2 receptor stably expressed in HEK293T cells co-expressing ARRB2 incubated for 60 mins by beta-arrestin2 recruitment assay | F | 5.42 | pEC50 | 3801.89 | nM | EC50 | J Med Chem (2021) 64: 8684-8709 [PMID:34110814] |
| 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 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 | 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 | 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] |
| ChEMBL | Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assay | F | 6.94 | pEC50 | 114.82 | nM | EC50 | J Med Chem (2021) 64: 8684-8709 [PMID:34110814] |
| 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 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 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 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 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] |
| ChEMBL | Agonist activity at histamine H2 receptor in spontaneous beating guinea pig right atrium assessed as increase in heart beat | F | 6.16 | pEC50 | 691.83 | nM | EC50 | J Med Chem (2021) 64: 8684-8709 [PMID:34110814] |
| ChEMBL | Agonist activity at guinea pig histamine H2 receptor stably transfected in HEK293T cells co-expressing NlucN-mGs/gpH2R-NlucC by mini-G protein recruitment assay | F | 6.6 | pEC50 | 251.19 | nM | EC50 | J Med Chem (2021) 64: 8684-8709 [PMID:34110814] |
| H3 receptor/Histamine H3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL264] [GtoPdb: 264] [UniProtKB: Q9Y5N1] | ||||||||
| GtoPdb | - | - | 8 | pKd | - | - | - |
Mol Pharmacol (2001) 59: 420-6 [PMID:11179434]; Mol Pharmacol (2001) 59: 427-33 [PMID:11179435] |
| ChEMBL | Displacement of [3H]Nalpha-methylhistamine from human histamine H3 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis | B | 8.52 | pKd | 3 | nM | Kd | J Med Chem (2021) 64: 8684-8709 [PMID:34110814] |
| ChEMBL | Binding affinity to SP-FLAG tagged human histamine H3 receptor expressed in HEK293T cells using sodium containing Leibovitz's L-15 medium incubated for 60 min by scintillation counter analysis | B | 5.93 | pKi | 1174.9 | nM | Ki | ACS Med Chem Lett (2023) 14: 1589-1595 [PMID:37974943] |
| 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 | Displacement of Clobenpropit-BODIPY-630/650 from Nluc-tagged human histamine H3 receptor expressed in HEK293T cells incubated for 2 hrs by NanoBRET assay | B | 6.3 | pKi | 501.19 | nM | Ki | ACS Med Chem Lett (2023) 14: 1589-1595 [PMID:37974943] |
| 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 | Displacement of [3H]UR-MN259 from SP-FLAG tagged human histamine H3 receptor expressed in HEK293T cells assessed as inhibition constant incubated for 60 min by scintillation counter analysis | B | 6.41 | pKi | 389.05 | nM | Ki | ACS Med Chem Lett (2023) 14: 1589-1595 [PMID:37974943] |
| 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 | Displacement of [3H]Nalpha-methylhistamine from human histamine H3 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis | B | 7.59 | pKi | 25.7 | nM | Ki | J Med Chem (2021) 64: 8684-8709 [PMID:34110814] |
| ChEMBL | Displacement of [3H]Nalpha-methylhistamine from human histamine H3 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis | B | 7.6 | pKi | 25.12 | nM | Ki | ACS Med Chem Lett (2023) 14: 1589-1595 [PMID:37974943] |
| 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 | Displacement of [3H]N-methylhistamine from SP-FLAG tagged human histamine H3 receptor expressed in SK-N-MC cells incubated for 40 mins | B | 8 | pKi | 10 | nM | Ki | ACS Med Chem Lett (2023) 14: 1589-1595 [PMID:37974943] |
| 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] |
| 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] |
| H3 receptor/Histamine H3 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4124] [GtoPdb: 264] [UniProtKB: Q9QYN8] | ||||||||
| 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 | Displacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis | B | 7.8 | pKd | 16 | nM | Kd | J Med Chem (2021) 64: 8684-8709 [PMID:34110814] |
| ChEMBL | Binding affinity to human H4R | B | 8.3 | pKd | 5 | nM | Kd | J Med Chem (2019) 62: 8338-8356 [PMID:31469288] |
| GtoPdb | - | - | 8.4 | pKd | - | - | - |
Mol Pharmacol (2001) 59: 420-6 [PMID:11179434]; Mol Pharmacol (2001) 59: 427-33 [PMID:11179435]; J Pharmacol Exp Ther (2001) 299: 121-30 [PMID:11561071]; J Pharmacol Exp Ther (2001) 296: 1058-66 [PMID:11181941]; J Biol Chem (2000) 275: 36781-6 [PMID:10973974]; Br J Pharmacol (2006) 147: 744-54 [PMID:16432504] |
| 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 stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis | B | 7.6 | pKi | 25.12 | nM | Ki | J Med Chem (2021) 64: 8684-8709 [PMID:34110814] |
| 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 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 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 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 | 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] |
| 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 | 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 | 75 | nM | EC50 | J Med Chem (2003) 46: 1980-1988 [PMID:12723960] |
| ChEMBL | Inhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H4 receptor | B | 7.26 | pEC50 | 54.95 | nM | EC50 | J Med Chem (2003) 46: 5445-5457 [PMID:14640553] |
| ChEMBL | Agonist activity at human H4R expressed in HEK293T-beta-arr2-hH4R cells by beta-arrestin2 recruitment assay | B | 7.47 | pEC50 | 33.88 | nM | EC50 | J Med Chem (2019) 62: 8338-8356 [PMID:31469288] |
| ChEMBL | Agonist activity at human histamine H4 receptor expressed in HEK293 cells assessed by forskolin induced cAMP response element activation by luciferase reporter gene assay | F | 7.6 | pEC50 | 25.12 | nM | EC50 | J Med Chem (2011) 54: 1693-1703 [PMID:21348462] |
| ChEMBL | Inhibition of the forskolin-stimulated cAMP production in SK-N-MC cells expressing human Histamine H4 receptor | F | 7.68 | pEC50 | 20.89 | nM | EC50 | J Med Chem (2003) 46: 3162-3165 [PMID:12825954] |
| ChEMBL | Agonist activity at human recombinant histamine H4 receptor-RGS19 fusion protein expressed in Sf9 cells coexpressing Galphai2,Gbeta1gamma2 assessed as [35S]GTPgammaS binding after 90 mins by liquid scintillation counting | F | 7.69 | pEC50 | 20.42 | nM | EC50 | Medchemcomm (2014) 5: 72-81 |
| ChEMBL | Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay | F | 7.7 | pEC50 | 19.95 | nM | EC50 | Bioorg Med Chem Lett (2010) 20: 7191-7199 [PMID:21044842] |
| ChEMBL | Agonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay | F | 7.77 | pEC50 | 16.98 | nM | EC50 | J Med Chem (2019) 62: 8338-8356 [PMID:31469288] |
| ChEMBL | Agonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of [35S]GTPgammaS binding | F | 7.86 | pEC50 | 13.8 | nM | EC50 | Bioorg Med Chem (2009) 17: 7186-7196 [PMID:19773175] |
| ChEMBL | Agonist activity at human SF-His6-tagged histamine H4 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated response incubated for 5 hrs by luciferase reporter gene assay | B | 7.89 | pEC50 | 13 | nM | EC50 | J Med Chem (2016) 59: 3452-3470 [PMID:27007611] |
| ChEMBL | Agonist activity at human recombinant histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2 by steady-state GTPase activity assay | F | 7.9 | pEC50 | 12.59 | nM | EC50 | Bioorg Med Chem Lett (2010) 20: 7191-7199 [PMID:21044842] |
| ChEMBL | Agonist activity at human H4 receptor expressed in insect Sf9 cells co-expressing RGS19 fusion protein and Gialpha2, Gbeta1gamma2 assessed as gamma[32P]GTP binding by liquid scintillation counting | B | 7.92 | pEC50 | 12.02 | nM | EC50 | J Med Chem (2009) 52: 2623-2627 [PMID:19317445] |
| ChEMBL | Agonist activity at human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19 protein by steady-state GTPase assay | F | 7.92 | pEC50 | 12.02 | nM | EC50 | J Med Chem (2009) 52: 6297-6313 [PMID:19791743] |
| ChEMBL | Agonist activity at human recombinant histamine H4 receptor-RGS19 fusion protein expressed in Sf9 cells coexpressing Galphai2,Gbeta1gamma2 preincubated for 2 mins before [gamma32P]GTP addition measured after 20 mins by steady-state GTPase activity assay | B | 7.92 | pEC50 | 12.02 | nM | EC50 | Medchemcomm (2014) 5: 72-81 |
| ChEMBL | Agonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of GTPase by [gamma-32P]GTP spontaneous degradation assay | F | 7.93 | pEC50 | 11.75 | nM | EC50 | Bioorg Med Chem (2009) 17: 7186-7196 [PMID:19773175] |
| ChEMBL | Activity at human recombinant histamine H4 receptor-RGS4 fusion protein expressed in Sf9 cells coexpressing Galphai2 and G-beta-1-gamma-2 by steady-state GTPase activity assay | B | 7.94 | pEC50 | 11.6 | nM | EC50 | J Med Chem (2008) 51: 7193-7204 [PMID:18950149] |
| ChEMBL | Agonist activity at human histamine H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assay | F | 7.96 | pEC50 | 11 | nM | EC50 | J Med Chem (2016) 59: 3452-3470 [PMID:27007611] |
| ChEMBL | Activity at human recombinant GAIP-fused histamine H4 receptor expressed in Sf9 cells coexpressing Galphai, Gbeta1gamma2 by steady-state GTPase activity assay | B | 8.04 | pEC50 | 9.12 | nM | EC50 | Bioorg Med Chem Lett (2010) 20: 3173-3176 [PMID:20409707] |
| ChEMBL | Antagonist activity at human histamine 4 receptor expressed in Sf9 cell membranes co-expressing Galphai2 and Gbeta1gamma2 assessed as [35S]GTPgammaS binding by scintillation counting | F | 8.1 | pEC50 | 7.94 | nM | EC50 | Bioorg Med Chem Lett (2016) 26: 292-300 [PMID:26718844] |
| ChEMBL | Agonist activity at human H4R by [35S]-GTPgammaS-binding assay | F | 8.13 | pEC50 | 7.41 | 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] | ||||||||
| ChEMBL | Binding affinity to mouse H4R | B | 7.38 | pKd | 42 | nM | Kd | J Med Chem (2019) 62: 8338-8356 [PMID:31469288] |
| GtoPdb | - | - | 7.4 | pKd | - | - | - | J Pharmacol Exp Ther (2001) 299: 121-30 [PMID:11561071] |
| ChEMBL | Binding affinity to mouse histamine H4 receptor expressed in human SK-N-MC cells by radioligand displacement assay | B | 7.1 | pKi | 79.43 | nM | Ki | Bioorg Med Chem Lett (2010) 20: 7191-7199 [PMID:21044842] |
| ChEMBL | Binding affinity to mouse histamine H4 receptor | B | 7.38 | pKi | 42 | nM | Ki | J Med Chem (2015) 58: 7119-7127 [PMID:25993395] |
| ChEMBL | Agonist activity at mouse H4R by [35S]-GTPgammaS-binding assay | F | 5.17 | pEC50 | 6760.83 | nM | EC50 | J Med Chem (2019) 62: 8338-8356 [PMID:31469288] |
| ChEMBL | Agonist activity at mouse histamine H4 receptor by luciferase reporter gene assay | F | 5.3 | pEC50 | 5011.87 | nM | EC50 | Bioorg Med Chem Lett (2010) 20: 7191-7199 [PMID:21044842] |
| ChEMBL | Agonist activity at mouse H4R expressed in HEK293T-beta-arr2-mH4R cells by beta-arrestin2 recruitment assay | B | 5.63 | pEC50 | 2344.23 | nM | EC50 | J Med Chem (2019) 62: 8338-8356 [PMID:31469288] |
| ChEMBL | Agonist activity at mouse SF-His6-tagged histamine H4 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated response incubated for 5 hrs by luciferase reporter gene assay | B | 7.03 | pEC50 | 94 | nM | EC50 | J Med Chem (2016) 59: 3452-3470 [PMID:27007611] |
| ChEMBL | Agonist activity at mouse H4R expressed in HEK293-SF-mH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay | F | 7.06 | pEC50 | 87.1 | nM | EC50 | J Med Chem (2019) 62: 8338-8356 [PMID:31469288] |
| H4 receptor/Histamine H4 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4468] [GtoPdb: 265] [UniProtKB: Q91ZY1] | ||||||||
| ChEMBL | Binding affinity to rat H4R | B | 6.87 | pKd | 134 | nM | Kd | J Med Chem (2019) 62: 8338-8356 [PMID:31469288] |
| GtoPdb | - | - | 6.9 | pKd | - | - | - | J Pharmacol Exp Ther (2001) 299: 121-30 [PMID:11561071] |
| ChEMBL | Binding affinity to rat histamine H4 receptor | B | 6.87 | pKi | 136 | nM | Ki | J Med Chem (2015) 58: 7119-7127 [PMID:25993395] |
| ChEMBL | Binding affinity to rat histamine H4 receptor expressed in human SK-N-MC cells by radioligand displacement assay | B | 7.2 | pKi | 63.1 | nM | Ki | Bioorg Med Chem Lett (2010) 20: 7191-7199 [PMID:21044842] |
| ChEMBL | Agonist activity at rat H4R by [35S]-GTPgammaS-binding assay | F | 4.28 | pEC50 | 52480.75 | nM | EC50 | J Med Chem (2019) 62: 8338-8356 [PMID:31469288] |
| ChEMBL | Agonist activity at rat H4R expressed in HEK293T-beta-arr2-rH4R cells by beta-arrestin2 recruitment assay | B | 5.43 | pEC50 | 3715.35 | nM | EC50 | J Med Chem (2019) 62: 8338-8356 [PMID:31469288] |
| ChEMBL | Agonist activity at rat H4R expressed in HEK293-SF-rH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay | F | 6.53 | pEC50 | 295.12 | nM | EC50 | J Med Chem (2019) 62: 8338-8356 [PMID:31469288] |
| ChEMBL | Agonist activity at rat histamine H4 receptor by luciferase reporter gene assay | F | 6.8 | pEC50 | 158.49 | nM | EC50 | Bioorg Med Chem Lett (2010) 20: 7191-7199 [PMID:21044842] |
| Histamine H4 receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1255160] [UniProtKB: Q91ZY3] | ||||||||
| ChEMBL | Binding affinity to guinea pig histamine H4 receptor | B | 8.22 | pKi | 6 | nM | Ki | J Med Chem (2015) 58: 7119-7127 [PMID:25993395] |
| Macrophage migration inhibitory factor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2085] [UniProtKB: P14174] | ||||||||
| ChEMBL | Inhibition of MIF tautomerase (unknown origin) using 4-HPP as substrate preincubated for 1 hr followed by substrate addition by Lineweaver-Burk plot anlysis | B | 4.21 | pKi | 62000 | nM | Ki | Bioorg Med Chem Lett (2022) 55: 128445-128445 [PMID:34758374] |
| ChEMBL | Inhibition of MIF tautomerase (unknown origin) using 4-HPP as substrate preincubated for 1 hr followed by substrate addition | B | 4.13 | pIC50 | 73600 | nM | IC50 | Bioorg Med Chem Lett (2022) 55: 128445-128445 [PMID:34758374] |
| Plasmodium falciparum (target type: ORGANISM) [ChEMBL: CHEMBL364] | ||||||||
| ChEMBL | Antiplasmodial activity against Plasmodium falciparum 3D7 infected in RBCs by firefly luciferase reporter gene assay | F | 6.18 | pIC50 | 660 | nM | IC50 | Antimicrob Agents Chemother (2010) 54: 3597-3604 [PMID:20547797] |
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]
