histamine [Ligand Id: 1204] 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 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 | - | - | - |
J Pharmacol Exp Ther (2001) 299: 121-30 [PMID:11561071]; Mol Pharmacol (2001) 59: 420-6 [PMID:11179434]; Br J Pharmacol (2006) 147: 744-54 [PMID:16432504]; Mol Pharmacol (2001) 59: 434-41 [PMID:11179436]; J Pharmacol Exp Ther (2005) 314: 1310-21 [PMID:15947036]; J Pharmacol Exp Ther (2001) 296: 1058-66 [PMID:11181941]; 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 | 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] |
| 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] |
| GtoPdb | - | - | 7.4 | pKi | - | - | - | J Pharmacol Exp Ther (2001) 299: 121-30 [PMID:11561071] |
| 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] |
| 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] |
| GtoPdb | - | - | 7.2 | pKi | - | - | - | J Pharmacol Exp Ther (2001) 299: 121-30 [PMID:11561071] |
| 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] |
| 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 33:
Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
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]
