thioperamide [Ligand Id: 1267] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL260374 (Thioperamide) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| α2A-adrenoceptor/Alpha-2a adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1867] [GtoPdb: 25] [UniProtKB: P08913] | ||||||||
| ChEMBL | Displacement of [3H]rauwolscine from human adrenergic alpha 2C10 receptor expressed in mouse LTK- cells | B | 6.9 | pKi | 125.89 | nM | Ki | J Med Chem (2008) 51: 5423-5430 [PMID:18683917] |
| α2C-adrenoceptor/Alpha-2c adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1916] [GtoPdb: 27] [UniProtKB: P18825] | ||||||||
| ChEMBL | Displacement of [3H]rauwolscine from human adrenergic alpha 2C4 receptor expressed in mouse LTK- cells | B | 6.46 | pKi | 346.74 | nM | Ki | J Med Chem (2008) 51: 5423-5430 [PMID:18683917] |
| CYP46A1/Cholesterol 24-hydroxylase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4523510] [GtoPdb: 1373] [UniProtKB: Q9Y6A2] | ||||||||
| ChEMBL | Inhibition of CH24H expressing human 293-F cells for 15 minutes using [14C] cholesterol as substrate and measured after 5 hrs by trypan blue staining based thin-layer chromatography | B | 6.37 | pIC50 | 430 | nM | IC50 | J Med Chem (2022) 65: 3343-3358 [PMID:35166541] |
| 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 | B | 5 | pKi | >10000 | nM | Ki | J Med Chem (2008) 51: 5423-5430 [PMID:18683917] |
| ChEMBL | Displacement of [3H]pyrilamine from human H1 receptor expressed in CHO cell membrane after 120 mins by liquid scintillation counting analysis | B | 5 | pKi | >10000 | nM | Ki | Eur J Med Chem (2014) 77: 269-279 [PMID:24650714] |
| H2 receptor/Histamine H2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1941] [GtoPdb: 263] [UniProtKB: P25021] | ||||||||
| ChEMBL | Displacement of [3H]tiotidine from human histamine H2 receptor | B | 5 | pKi | >10000 | nM | Ki | J Med Chem (2008) 51: 5423-5430 [PMID:18683917] |
| H3 receptor/Histamine H3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL264] [GtoPdb: 264] [UniProtKB: Q9Y5N1] | ||||||||
| ChEMBL | Antagonist activity at human histamine H3 receptor expressed in SK-N-MC cells assessed as inhibition of forskolin stimulated cAMP accumulation after 6 hrs | F | 7.2 | pKd | 63.1 | nM | Kd | Eur J Med Chem (2009) 44: 4413-4425 [PMID:19577344] |
| ChEMBL | Mean functional activity against human H3 receptor | B | 7.36 | pKd | 43.65 | nM | Kd | J Med Chem (2005) 48: 2229-2238 [PMID:15771465] |
| ChEMBL | Displacement of [125I]iodoproxyfan from human histamine H3 receptor expressed in CHO-K1 cells | B | 6.22 | pKi | 602.56 | nM | Ki | Bioorg Med Chem Lett (2013) 23: 4886-4891 [PMID:23891186] |
| ChEMBL | Displacement of N-alpha-[methyl-3H]-methylhistamine dihydrochloride from recombinant human histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition constant incubated for 30 mins by liquid scintillation analysis | B | 6.72 | pKi | 191 | nM | Ki | Bioorg Med Chem Lett (2017) 27: 4525-4530 [PMID:28888822] |
| ChEMBL | Displacement of [3H]-Nalpha-Methylhistamine from recombinant human histamine H3 receptor expressed in HEK293 cells after 1 hr by liquid scintillation counting analysis | B | 6.75 | pKi | 177.83 | nM | Ki | Medchemcomm (2019) 10: 234-251 [PMID:30881612] |
| ChEMBL | Displacement of [3H]-Nalpha-methylhistamine from human histamine H3 receptor expressed in CHO cells by liquid scintillation counting | B | 6.8 | pKi | 158.49 | nM | Ki | Medchemcomm (2010) 1: 39-44 |
| ChEMBL | In vitro binding affinity was determined as displacement of [3H]N-R-methylhistamine from C6 cell membranes expressing human histamine H3 receptor | B | 7.14 | pKi | 72.44 | nM | Ki | J Med Chem (2005) 48: 38-55 [PMID:15634000] |
| ChEMBL | Displacement of [3H]NAMH from human full length histamine H3 receptor expressed in rat C6 cells | B | 7.14 | pKi | 72.44 | nM | Ki | J Med Chem (2008) 51: 5423-5430 [PMID:18683917] |
| ChEMBL | In vitro binding affinity was determined as displacement of [3H]N-R-methylhistamine from C6 cell membranes expressing human histamine H3 receptor | B | 7.14 | pKi | 72 | nM | Ki | J Med Chem (2005) 48: 38-55 [PMID:15634000] |
| ChEMBL | Displacement of [3H]N-alpha-methylhistamine from human H3 receptor expressed in HEK-293 cell membrane after 90 mins by liquid scintillation counting analysis | B | 7.15 | pKi | 70.79 | nM | Ki | Eur J Med Chem (2014) 77: 269-279 [PMID:24650714] |
| ChEMBL | Displacement of [3H]NAMH from histamine H3 receptor in human cortex | B | 7.18 | pKi | 66.07 | nM | Ki | J Med Chem (2008) 51: 5423-5430 [PMID:18683917] |
| ChEMBL | Binding affinity to histamine H3 receptor | B | 7.2 | pKi | 63.1 | nM | Ki | Bioorg Med Chem (2009) 17: 7186-7196 [PMID:19773175] |
| ChEMBL | Displacement of [3H]N-alpha-methylhistamine from human histamine H3 receptor expressed in SK-N-MC cells | B | 7.2 | pKi | 63 | nM | Ki | Eur J Med Chem (2009) 44: 4413-4425 [PMID:19577344] |
| ChEMBL | Binding affinity to human Histamine H3 receptor in CHO-K1 cells using [125I]iodoproxyfan as radioligand | B | 7.22 | pKi | 60 | nM | Ki | Bioorg Med Chem Lett (2001) 11: 951-954 [PMID:11294398] |
| ChEMBL | Displacement of [125I]iodoproxyfan from human histamine H3 receptor expressing CHO cells | B | 7.22 | pKi | 60 | nM | Ki | J Med Chem (2003) 46: 1523-1530 [PMID:12672253] |
| ChEMBL | Displacement of [3H]iodoproxyfan from human histamine H3 receptor expressed in CHO-K1 cells | B | 7.22 | pKi | 60 | nM | Ki | Bioorg Med Chem Lett (2009) 19: 6682-6685 [PMID:19846299] |
| ChEMBL | Displacement of [125I]iodoproxyfan from human full-length histamine H3 receptor expressed in HEK293 cells after 60 mins | B | 7.22 | pKi | 60 | nM | Ki | Bioorg Med Chem (2011) 19: 2850-2858 [PMID:21498080] |
| ChEMBL | Binding affinity in Nluc-hH3R assessed in HEK293 cells by NanoBRET binding assay | B | 7.28 | pKi | 52.48 | nM | Ki | J Med Chem (2021) 64: 11695-11708 [PMID:34309390] |
| ChEMBL | Displacement of [3H]N-alpha-methyl-histamine from human histamine H3 receptor expressed in human HEK293-EBNA cells | B | 7.29 | pKi | 51.1 | nM | Ki | J Med Chem (2010) 53: 3585-3593 [PMID:20397706] |
| ChEMBL | Displacement of [3H]Nalpha-methylhistamine form human H3 receptor | B | 7.29 | pKi | 51.1 | nM | Ki | J Med Chem (2006) 49: 5587-5596 [PMID:16942032] |
| ChEMBL | Binding affinity to human histamine H3 receptor | B | 7.3 | pKi | 50.12 | nM | Ki | J Med Chem (2011) 54: 26-53 [PMID:21062081] |
| 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 | 7.3 | pKi | 50.12 | nM | Ki | ACS Med Chem Lett (2023) 14: 1589-1595 [PMID:37974943] |
| 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 | 7.3 | pKi | 50.12 | nM | Ki | ACS Med Chem Lett (2023) 14: 1589-1595 [PMID:37974943] |
| ChEMBL | Displacement of [3H]N-alpha-methylhistamine from human histamine H3 receptor expressed in human SK-N-MC cells by liquid scintillation counting | B | 7.3 | pKi | 50.12 | nM | Ki | Bioorg Med Chem (2009) 17: 3987-3994 [PMID:19414267] |
| ChEMBL | Displacement of clobenpropit-BODIPY-630/650 from recombinant human NLuc-fused H3R expressed in HEK293T cells by Nano-BRET assay | B | 7.3 | pKi | 50.12 | nM | Ki | J Med Chem (2020) 63: 5297-5311 [PMID:32420741] |
| ChEMBL | Displacement of [3H]-N-alpha-methylhistamine from human recombinant H3R expressed in human SK-N-MC cell membranes | B | 7.3 | pKi | 50.12 | nM | Ki | J Med Chem (2020) 63: 5297-5311 [PMID:32420741] |
| ChEMBL | Binding affinity in Nluc-hH3R assessed in HEK293T cells by NanoBRET binding assay | B | 7.3 | pKi | 50.12 | nM | Ki | J Med Chem (2021) 64: 11695-11708 [PMID:34309390] |
| ChEMBL | Inhibition of UR-DEBa242 binding to human recombinant NLuc/GPCR-fused H3R expressed in HEK293T cells measured after 30 mins by furimazine substrate based BRET assay | B | 7.36 | pKi | 43.65 | nM | Ki | J Med Chem (2020) 63: 5297-5311 [PMID:32420741] |
| 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 | 7.38 | pKi | 41.69 | nM | Ki | ACS Med Chem Lett (2023) 14: 1589-1595 [PMID:37974943] |
| ChEMBL | Displacement of [3H]-UR-PI294 from Galphai2/Gbeta1gamma2-coupled human recombinant H3R expressed in baculovirus infected Sf9 insect cell membranes co-expressing RGS4 measured after 60 mins by microbeta scintillation counting method | B | 7.4 | pKi | 39.81 | nM | Ki | J Med Chem (2020) 63: 5297-5311 [PMID:32420741] |
| ChEMBL | Displacement of [3H]N-alpha-methylhistamine from human histamine H3 receptor expressed in SK-N-MC cells | B | 7.5 | pKi | 31.62 | nM | Ki | Eur J Med Chem (2009) 44: 4098-4106 [PMID:19524331] |
| ChEMBL | Displacement of [3H]N-alpha-methylhistamine from human histamine H3 receptor expressed in HEK293 cells after 60 mins by liquid scintillation counting | B | 7.53 | pKi | 29.51 | nM | Ki | J Med Chem (2011) 54: 1693-1703 [PMID:21348462] |
| ChEMBL | Mean binding affinity for human H3 receptor | B | 7.54 | pKi | 28.84 | nM | Ki | J Med Chem (2005) 48: 2229-2238 [PMID:15771465] |
| ChEMBL | Binding affinity to the human histamine H3 receptor | B | 7.6 | pKi | 25 | nM | Ki | J Med Chem (2003) 46: 3957-3960 [PMID:12954048] |
| GtoPdb | - | - | 7.7 | pKi | 19.9 | nM | Ki |
J Pharmacol Exp Ther (2003) 305: 887-96 [PMID:12606603]; Biochem Pharmacol (2004) 68: 933-45 [PMID:15294456]; J Pharmacol Exp Ther (2000) 293: 771-8 [PMID:10869375]; Biochem J (2001) 355: 279-88 [PMID:11284713]; J Pharmacol Exp Ther (2001) 299: 908-14 [PMID:11714875]; Br J Pharmacol (2000) 131: 1247-50 [PMID:11090094]; Eur J Pharmacol (2002) 453: 33-41 [PMID:12393057] |
| ChEMBL | Antagonist potency against human histamine H3 receptor expressed in CHO cells was determined by GTPgamma-S-assay | F | 7.85 | pKi | 14 | nM | Ki | J Med Chem (2004) 47: 2833-2838 [PMID:15139761] |
| ChEMBL | Antagonist potency against human H3 receptor in GTPgamma-S-Assay | F | 7.85 | pKi | 14 | nM | Ki | J Med Chem (2005) 48: 306-311 [PMID:15634025] |
| ChEMBL | Displacement of [125I]-iodoproxyfan from human striatal full length H3 receptor expressed in CHOK1 cells after 60 mins | B | 8.19 | pKi | 6.5 | nM | Ki | Bioorg Med Chem (2018) 26: 2573-2585 [PMID:29681486] |
| ChEMBL | Inhibition of human H3R expressed in methylhistamine-induced human H3-bla U2OS cells incubated for 30 mins by beta-lactamase complementation technology | B | 5.99 | pIC50 | 1030 | nM | IC50 | Eur J Med Chem (2019) 168: 207-220 [PMID:30822710] |
| ChEMBL | Antagonist activity at histamine H3 receptor expressed in HEK293 cells co-transfected with pCRE-Luc gene assessed as inhibition of forskolin/histamine-induced cAMP accumulation after 5 hrs by luciferase reporter gene assay | F | 6.29 | pIC50 | 517.5 | nM | IC50 | Bioorg Med Chem (2011) 19: 7158-7167 [PMID:22019465] |
| ChEMBL | Antagonist activity at human histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of imetit-stimulation ERK1/2 phosphorylation by ELISA analysis | B | 6.53 | pIC50 | 296 | nM | IC50 | Bioorg Med Chem Lett (2017) 27: 4525-4530 [PMID:28888822] |
| ChEMBL | Inverse agonist activity at recombinant human Histamine 3 receptor expressed in CHO-K1 cells assessed as inhibition of RAMH-induced agonist activity preincubated for 20 mins and measured after 60 mins by [35S]-GTPgammaS binding assay | F | 6.85 | pIC50 | 140 | nM | IC50 | J Med Chem (2019) 62: 1203-1217 [PMID:30629436] |
| ChEMBL | Antagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed by forskolin induced cAMP response element activation after 5 hrs by luciferase reporter gene assay | F | 6.92 | pIC50 | 120 | nM | IC50 | Bioorg Med Chem (2013) 21: 5936-5944 [PMID:23978359] |
| ChEMBL | Inverse agonist activity at human H3R expressed in HEK293T-SP-FLAG-hH3R-CRE-CBR cells assessed as reduction in histamine-induced inhibition of forskolin stimulated luciferase activity by luciferase reporter gene assay | F | 7.7 | pIC50 | 19.95 | nM | IC50 | J Med Chem (2020) 63: 5297-5311 [PMID:32420741] |
| ChEMBL | Antagonist activity at human H3 receptor expressed in 293-EBNA cells assessed as inhibition of histamine agonist activity by luciferase reporter gene assay | F | 7.8 | pIC50 | 16 | nM | IC50 | J Med Chem (2006) 49: 5587-5596 [PMID:16942032] |
| ChEMBL | Inhibition of recombinant human histamine H3 receptor stably expressed in HEK293 cells assessed as increase in cAMP accumulation in presence of forskolin incubated for 30 mins by TR-FRET LANCE assay | F | 8.71 | pIC50 | 1.96 | nM | IC50 | J Med Chem (2023) 66: 9658-9683 [PMID:37418295] |
| ChEMBL | Inverse agonist activity at human histamine H3 receptor expressed in CHO cells assessed as inhibition of [35S]-GTPgammaS binding by liquid scintillation counting | F | 7 | pEC50 | 100 | nM | EC50 | Medchemcomm (2010) 1: 39-44 |
| 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 | 7.01 | pEC50 | 97.72 | 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 | 7.01 | pEC50 | 97.72 | nM | EC50 | J Med Chem (2009) 52: 6297-6313 [PMID:19791743] |
| ChEMBL | Inverse 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 | 7.4 | pEC50 | 39.81 | nM | EC50 | J Med Chem (2011) 54: 1693-1703 [PMID:21348462] |
| ChEMBL | Inverse agonist activity at recombinant human histamine H3 receptor expressed in CHO-K1 cells preincubated for 10 mins followed by [35S]GTPgammaS addition and measured after 60 mins by TopCount NXT based scintillation analysis | B | 7.47 | pEC50 | 34 | nM | EC50 | Bioorg Med Chem Lett (2017) 27: 4525-4530 [PMID:28888822] |
| 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 | 8.32 | pKi | 4.8 | nM | Ki | Bioorg Med Chem Lett (2009) 19: 4075-4078 [PMID:19553110] |
| GtoPdb | - | - | 8.8 | pKi | - | - | - | J Neurochem (2004) 90: 1331-8 [PMID:15341517] |
| ChEMBL | Inverse agonist activity at mouse histamine H3 receptor overexpressed in HEK293 cells by [35S]GTPgammaS binding assay | F | 7.96 | pEC50 | 11 | nM | EC50 | Bioorg Med Chem Lett (2009) 19: 4075-4078 [PMID:19553110] |
| H3 receptor/Histamine H3 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4124] [GtoPdb: 264] [UniProtKB: Q9QYN8] | ||||||||
| ChEMBL | Displacement of N-alpha-[methyl-3H]-methylhistamine dihydrochloride from Sprague-Dawley rat brain membrane histamine H3 receptor assessed as inhibition constant incubated for 30 mins by liquid scintillation counting analysis | B | 7.64 | pKi | 23 | nM | Ki | Bioorg Med Chem Lett (2017) 27: 4525-4530 [PMID:28888822] |
| ChEMBL | Displacement of [3H]-Nalpha-Methylhistamine from rat histamine H3 receptor expressed in HEK293T cell membranes after 60 mins by liquid scintillation counting analysis | B | 7.9 | pKi | 12.59 | nM | Ki | Medchemcomm (2019) 10: 234-251 [PMID:30881612] |
| ChEMBL | Displacement of [3H]NAMH from histamine H3 receptor in rat cortex | B | 8.15 | pKi | 7.08 | nM | Ki | J Med Chem (2008) 51: 5423-5430 [PMID:18683917] |
| ChEMBL | Binding affinity to rat Histamine H3 receptor in CHO-K1 cells using [125I]iodoproxyfan as radioligand | B | 8.19 | pKi | 6.5 | nM | Ki | Bioorg Med Chem Lett (2001) 11: 951-954 [PMID:11294398] |
| ChEMBL | In vitro antagonism of the histamine H3-receptor in the rat cerebral cortex. | F | 8.37 | pKi | 4.3 | nM | Ki | J Med Chem (1995) 38: 3342-3350 [PMID:7650687] |
| ChEMBL | Histamine H3 receptor affinity of compound was determined in rat cortical membranes using the H3 selective agonist ligand, [3H]N-alpha-methylhistamine | F | 8.37 | pKi | 4.3 | nM | Ki | Bioorg Med Chem Lett (1997) 7: 3017-3022 |
| ChEMBL | Antagonistic activity was evaluated against histamine H3 receptor using [3H]- N-alpha-methylhistamine as radioligand in experiment 1 | F | 8.37 | pKi | 4.3 | nM | Ki | Bioorg Med Chem Lett (1998) 8: 1133-1138 [PMID:9871722] |
| ChEMBL | In vitro binding affinity against rat histamine H3 receptor | B | 8.4 | pKi | 4 | nM | Ki | J Med Chem (2004) 47: 2678-2687 [PMID:15115409] |
| ChEMBL | In vitro antagonist potency at Histamine H3 receptor measured as K+-evoked [3H]histamine release from synaptosomes of rat cerebral cortex. | F | 8.4 | pKi | 4 | nM | Ki | J Med Chem (1998) 41: 4171-4176 [PMID:9767653] |
| ChEMBL | In vitro inhibitory activity against histamine H3 receptor using [3H]histamine as radioligand from rat cerebral cortex synaptosomes | B | 8.4 | pKi | 4 | nM | Ki | J Med Chem (2004) 47: 3264-3274 [PMID:15163206] |
| ChEMBL | Effect at histamine H3 receptors (in vitro) on synaptosomes of rat cerebral cortex assayed by functional H3-receptor assay. | B | 8.4 | pKi | 4 | nM | Ki | J Med Chem (1999) 42: 593-600 [PMID:10052966] |
| ChEMBL | Rat Histamine H3 receptor antagonism determined by [K+] - evoked depolarization-induced release of [3H]histamine from rat cerebral cortex synaptosomes | F | 8.4 | pKi | 4 | nM | Ki | J Med Chem (1996) 39: 3806-3813 [PMID:8809168] |
| ChEMBL | Histamine H3 receptor antagonist activity in an assay with K+ evoked depolarization-induced release of [3H]-histamine from rat synaptosomes. | F | 8.4 | pKi | 4 | nM | Ki | J Med Chem (2000) 43: 3335-3343 [PMID:10966752] |
| ChEMBL | In vitro antagonistic activity against Histamine H3 receptor on Synaptosomes of rat cerebral cortex. | F | 8.4 | pKi | 4 | nM | Ki | J Med Chem (1996) 39: 1157-1163 [PMID:8676353] |
| ChEMBL | In vitro inhibitory activity against Histamine H3 receptor for K+ evoked depolarization-induced release of [3H]histamine from synaptosomes of rat cerebral cortex | B | 8.4 | pKi | 4 | nM | Ki | Bioorg Med Chem Lett (2000) 10: 2379-2382 [PMID:11055360] |
| ChEMBL | In vitro Histamine H3 receptor antagonist activity in an assay with K+-evoked depolarization-induced release of [3H]histamine from synaptosomes of rat cerebral cortex | F | 8.4 | pKi | 4 | nM | Ki | Bioorg Med Chem Lett (1998) 8: 2011-2016 [PMID:9873477] |
| ChEMBL | Effect on histamine H3 receptors in vitro, on synaptosomes of rat cerebral cortex for the release of [3H]histamine | B | 8.4 | pKi | 4 | nM | Ki | J Med Chem (2000) 43: 3987-3994 [PMID:11052804] |
| ChEMBL | Binding affinity to rat cortical histamine H3 receptor | B | 8.4 | pKi | 3.98 | nM | Ki | J Med Chem (2011) 54: 26-53 [PMID:21062081] |
| ChEMBL | In vitro antagonistic activity tested against Histamine H3 receptor on synaptosomes from rat cerebral cortex | F | 8.4 | pKi | 3.98 | nM | Ki | J Med Chem (1996) 39: 1220-1226 [PMID:8632428] |
| ChEMBL | In vitro antagonistic activity against histamine H3-receptor in an assay with K+-evoked depolarisation-induced release of [3H]histamine of synaptosomes of rat cerebral cortex | F | 8.4 | pKi | 3.98 | nM | Ki | Bioorg Med Chem Lett (1996) 6: 2013-2018 |
| ChEMBL | Displacement of [3H]NAMH from rat full length histamine H3 receptor expressed in rat C6 cells | B | 8.44 | pKi | 3.63 | nM | Ki | J Med Chem (2008) 51: 5423-5430 [PMID:18683917] |
| ChEMBL | In vitro binding affinity was determined as displacement of [3H]N-R-methylhistamine from C6 cell membranes expressing rat histamine H3 receptor | B | 8.44 | pKi | 3.63 | nM | Ki | J Med Chem (2005) 48: 38-55 [PMID:15634000] |
| ChEMBL | In vitro binding affinity was determined as displacement of [3H]N-R-methylhistamine from C6 cell membranes expressing rat histamine H3 receptor | B | 8.44 | pKi | 3.63 | nM | Ki | J Med Chem (2005) 48: 38-55 [PMID:15634000] |
| ChEMBL | Inhibition of rat Histamine H3 receptor using [3H]N-alpha-methyl histamine | B | 8.58 | pKi | 2.65 | nM | Ki | J Med Chem (2003) 46: 1980-1988 [PMID:12723960] |
| ChEMBL | Displacement of [3H]-(R)alpha-MeHA from rat brain H3 receptor | B | 8.68 | pKi | 2.1 | nM | Ki | Bioorg Med Chem (2018) 26: 2573-2585 [PMID:29681486] |
| ChEMBL | Binding affinity against H3 receptor in rat cerebral cortex membranes was evaluated using [3H]N-methyl-histamine as radioligand | B | 8.7 | pKi | 2 | nM | Ki | Bioorg Med Chem Lett (1996) 6: 833-838 |
| ChEMBL | In vitro antagonistic activity against histamine H3 receptor on rat cerebral cortex | F | 8.7 | pKi | 2 | nM | Ki | J Med Chem (1996) 39: 1220-1226 [PMID:8632428] |
| GtoPdb | - | - | 8.8 | pKi | - | - | - |
J Pharmacol Exp Ther (2003) 305: 887-96 [PMID:12606603]; Biochem Pharmacol (2004) 68: 933-45 [PMID:15294456]; J Pharmacol Exp Ther (2000) 293: 771-8 [PMID:10869375]; J Pharmacol Exp Ther (2001) 299: 908-14 [PMID:11714875]; Biochem Biophys Res Commun (2001) 280: 75-80 [PMID:11162480]; Br J Pharmacol (2000) 131: 1247-50 [PMID:11090094]; Eur J Pharmacol (2002) 453: 33-41 [PMID:12393057] |
| ChEMBL | Antagonistic activity was evaluated against histamine H3 receptor using [3H]- N-alpha-methylhistamine as radioligand in experiment 2 | F | 8.81 | pKi | 1.54 | nM | Ki | Bioorg Med Chem Lett (1998) 8: 1133-1138 [PMID:9871722] |
| Histamine H3 receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5076] [UniProtKB: Q9JI35] | ||||||||
| ChEMBL | Antagonist activity at histamine H3 receptor in guinea pig ileum assessed as inhibition of (R)-alpha-methylhistamine-induced response | F | 8.44 | pKd | 3.63 | nM | Kd | J Med Chem (2008) 51: 5423-5430 [PMID:18683917] |
| ChEMBL | Antagonist activity at histamine H3 receptor in Cavia porcellus (guinea pig) ileum assessed as inhibition of electrically-induced contraction | B | 8.66 | pKd | 2.19 | nM | Kd | Med Chem Res (2013) 22: 1287-1304 |
| ChEMBL | Displacement of [3H]Nalpha-methylhistamine from histamine H3 receptors in homogenates of rat cerebral cortex | B | 8.9 | pKd | 1.26 | nM | Kd | J Med Chem (2001) 44: 1666-1674 [PMID:11356102] |
| ChEMBL | Antagonist activity at histamine H3 receptor in guinea pig jejunum assessed as effect on pyrilamine-induced inhibition of electrically evoked contraction treated 20 mins after pyrilamine stimulation | B | 8.98 | pKd | 1.05 | nM | Kd | Medchemcomm (2019) 10: 234-251 [PMID:30881612] |
| ChEMBL | Antagonist activity at histamine H3 receptor in guinea pig jejunum assessed as electrically evoked contractions | F | 9.06 | pKd | 0.87 | nM | Kd | Eur J Med Chem (2009) 44: 1674-1681 [PMID:18990469] |
| ChEMBL | Binding affinity against H3 receptor in guinea pig brain using [3H]N-alpha-methyl histamine as radioligand | B | 8.14 | pKi | 7.3 | nM | Ki | Bioorg Med Chem Lett (2003) 13: 1959-1961 [PMID:12781173] |
| ChEMBL | Inhibition of N-alpha-methylhistamine binding to histamine H3 receptor of guinea pig brain membranes | B | 8.14 | pKi | 7.3 | nM | Ki | Bioorg Med Chem Lett (1998) 8: 2263-2268 [PMID:9873525] |
| ChEMBL | Antagonistic activity for Histamine H3 receptor on electrically evoked guinea-pig ileum contraction | F | 8.4 | pKi | 3.98 | nM | Ki | Bioorg Med Chem Lett (1994) 4: 2907-2912 |
| H4 receptor/Histamine H4 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3759] [GtoPdb: 265] [UniProtKB: Q9H3N8] | ||||||||
| ChEMBL | Displacement of [3H]-histamine from Galphai2/Gbeta1gamma2-coupled human recombinant H4R expressed in baculovirus infected Sf9 insect cell membranes | B | 6.3 | pKi | 501.19 | nM | Ki | J Med Chem (2020) 63: 5297-5311 [PMID:32420741] |
| ChEMBL | Displacement of [3H]-histamine from Galphai2/Gbeta1gamma2-coupled human recombinant H4R expressed in baculovirus infected Sf9 insect cell membranes co-expressing RGS19 | B | 6.3 | pKi | 501.19 | nM | Ki | J Med Chem (2020) 63: 5297-5311 [PMID:32420741] |
| ChEMBL | Displacement of [3H]-histamine from human recombinant H4R stably expressed in human SK-N-MC cell membranes | B | 6.3 | pKi | 501.19 | nM | Ki | J Med Chem (2020) 63: 5297-5311 [PMID:32420741] |
| ChEMBL | Displacement of [3H]-histamine from human recombinant H4R stably expressed in human SK-N-MC cell homogenates | B | 6.3 | pKi | 501.19 | nM | Ki | J Med Chem (2020) 63: 5297-5311 [PMID:32420741] |
| ChEMBL | Displacement of [3H]-UR-PI294 from Galphai2/Gbeta1gamma2-coupled human recombinant H4R expressed in baculovirus infected Sf9 insect cell membranes co-expressing RGS19 measured after 60 mins by microbeta scintillation counting method | B | 6.3 | pKi | 501.19 | nM | Ki | J Med Chem (2020) 63: 5297-5311 [PMID:32420741] |
| ChEMBL | Displacement of UR-DEBa176 from human recombinant H4R expressed in HEK293T-SF-His6-CRE-Luc cells | B | 6.3 | pKi | 501.19 | nM | Ki | J Med Chem (2020) 63: 5297-5311 [PMID:32420741] |
| ChEMBL | Displacement of [3H]-histamine from human recombinant H4R expressed in HEK293T cell homogenates | B | 6.3 | pKi | 501.19 | nM | Ki | J Med Chem (2020) 63: 5297-5311 [PMID:32420741] |
| ChEMBL | Displacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Gai2 and Gb1c2 subunit | B | 6.37 | pKi | 426.58 | nM | Ki | Bioorg Med Chem Lett (2013) 23: 4886-4891 [PMID:23891186] |
| ChEMBL | Displacement of [3H]histamine from human histamine H4 receptor expressed in SK-NM-C cells | B | 6.48 | pKi | 328 | nM | Ki | J Med Chem (2008) 51: 3145-3153 [PMID:18459760] |
| ChEMBL | Displacement of [3H]histamine from human histamine H4 receptor expressed in sf9 cells co-expressing mammalian Galphai2 and Gbeta1gamma2 | B | 6.75 | pKi | 178 | nM | Ki | J Med Chem (2016) 59: 3452-3470 [PMID:27007611] |
| ChEMBL | Inhibition of UR-DEBa242 binding to human recombinant NLuc/GPCR-fused H4R expressed in HEK293T cells measured after 30 mins by furimazine substrate based BRET assay | B | 6.81 | pKi | 154.88 | nM | Ki | J Med Chem (2020) 63: 5297-5311 [PMID:32420741] |
| ChEMBL | Binding affinity to human histamine H4 receptor | B | 6.9 | pKi | 125.89 | nM | Ki | J Med Chem (2011) 54: 26-53 [PMID:21062081] |
| ChEMBL | Displacement of [3H]histamine from human histamine H4 receptor expressed in human SK-N-MC cells by liquid scintillation counting | B | 6.9 | pKi | 125.89 | nM | Ki | Bioorg Med Chem (2009) 17: 3987-3994 [PMID:19414267] |
| ChEMBL | Displacement of [3H]histamine from human histamine H4 receptor expressed in human SK-N-MC cell membrane incubated for 60 mins | B | 6.9 | pKi | 125 | nM | Ki | J Med Chem (2016) 59: 3452-3470 [PMID:27007611] |
| ChEMBL | Displacement of [3H]histamine form human H4 receptor | B | 6.91 | pKi | 124 | nM | Ki | J Med Chem (2006) 49: 5587-5596 [PMID:16942032] |
| ChEMBL | Displacement of [3H]histamine from human H4 receptor expressed in HEK cell membranes | B | 7.1 | pKi | 79 | nM | Ki | Bioorg Med Chem Lett (2012) 22: 461-467 [PMID:22153663] |
| ChEMBL | Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells | B | 7.2 | pKi | 63.1 | nM | Ki | J Med Chem (2010) 53: 2390-2400 [PMID:20192225] |
| ChEMBL | Displacement of clobenpropit-BODIPY-630/650 from recombinant human NLuc-fused H4R expressed in HEK293T cells by Nano-BRET assay | B | 7.2 | pKi | 63.1 | nM | Ki | J Med Chem (2020) 63: 5297-5311 [PMID:32420741] |
| ChEMBL | Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells after 60 mins by liquid scintillation counting | B | 7.2 | pKi | 63.1 | nM | Ki | J Med Chem (2011) 54: 1693-1703 [PMID:21348462] |
| ChEMBL | Displacement of [3H]histamine from human H4 receptor expressed in Sf9 cell membrane co-transfected with Galphai2 and Gbeta1gamma2 after 60 mins by liquid scintillation counting analysis | B | 7.2 | pKi | 63.1 | nM | Ki | Eur J Med Chem (2014) 77: 269-279 [PMID:24650714] |
| ChEMBL | Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells | B | 7.2 | pKi | 63.1 | nM | Ki | J Med Chem (2008) 51: 2457-2467 [PMID:18357976] |
| ChEMBL | Antagonist activity at human H4 receptor expressed in HEK293T cells assessed as inhibition of histamine-induced [35S]GTPgammaS binding | F | 7.2 | pKi | 63 | nM | Ki | Bioorg Med Chem Lett (2012) 22: 461-467 [PMID:22153663] |
| ChEMBL | Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells | B | 7.32 | pKi | 47.86 | nM | Ki | J Med Chem (2008) 51: 5423-5430 [PMID:18683917] |
| ChEMBL | Displacement of [3H]-Nalpha-Methylhistamine from human recombinant histamine H4 receptor expressed in CHO cell membranes after 1 hrs by liquid scintillation counting analysis | B | 7.34 | pKi | 45.71 | nM | Ki | Medchemcomm (2019) 10: 234-251 [PMID:30881612] |
| ChEMBL | Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells | B | 7.37 | pKi | 43 | nM | Ki | Bioorg Med Chem Lett (2009) 19: 6682-6685 [PMID:19846299] |
| ChEMBL | Displacement of [3H]histamine from human full-length histamine H4 receptor expressed in HEK293 cells after 60 mins | B | 7.37 | pKi | 43 | nM | Ki | Bioorg Med Chem (2011) 19: 2850-2858 [PMID:21498080] |
| ChEMBL | Binding affinity to the human histamine H4 receptor | B | 7.57 | pKi | 27 | nM | Ki | J Med Chem (2003) 46: 3957-3960 [PMID:12954048] |
| ChEMBL | Displacement of [3H]histamine human recombinant histamine H4 receptor | B | 7.57 | pKi | 27 | nM | Ki | Bioorg Med Chem Lett (2010) 20: 2516-2519 [PMID:20299215] |
| GtoPdb | - | - | 7.6 | pKi | - | - | - |
J Pharmacol Exp Ther (2003) 305: 887-96 [PMID:12606603]; Biochem Pharmacol (2004) 68: 933-45 [PMID:15294456]; 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] |
| ChEMBL | Binding affinity to histamine H4 receptor | B | 8.4 | pKi | 3.98 | nM | Ki | Bioorg Med Chem (2009) 17: 7186-7196 [PMID:19773175] |
| ChEMBL | Antagonist activity at human H4 receptor expressed in HEK293T cells assessed as inhibition of histamine-induced [35S]GTPgammaS binding | F | 6.01 | pIC50 | 977 | nM | IC50 | Bioorg Med Chem Lett (2012) 22: 461-467 [PMID:22153663] |
| ChEMBL | Antagonist activity at human H4 receptor expressed in 293-EBNA cells assessed as inhibition of histamine agonist activity by luciferase reporter gene assay | F | 6.17 | pIC50 | 680 | nM | IC50 | J Med Chem (2006) 49: 5587-5596 [PMID:16942032] |
| ChEMBL | Antagonist activity at histamine H4 receptor expressed in HEK293 cells co-transfected with pCRE-Luc gene assessed as inhibition of forskolin/histamine-induced cAMP accumulation after 5 hrs by luciferase reporter gene assay | F | 6.18 | pIC50 | 667 | nM | IC50 | Bioorg Med Chem (2011) 19: 7158-7167 [PMID:22019465] |
| ChEMBL | Inverse agonist activity at human H4R expressed in HEK293 cells co-expressing ELucC/ELucN-beta-arrestin2 assessed as inhibition of histamine-induced beta-arrestin recruitment by luciferase reporter gene assay | B | 6.31 | pIC50 | 489.78 | nM | IC50 | J Med Chem (2020) 63: 5297-5311 [PMID:32420741] |
| ChEMBL | Antagonist activity at human H4 receptor expressed in CHO-K1 cells co-expressing G protein alpha16 assessed as inhibition of histamine-induced calcium mobilization incubated for 16 hrs by aequorin-based functional assay | F | 7.72 | pIC50 | 19 | nM | IC50 | J Med Chem (2019) 62: 11416-11422 [PMID:31724859] |
| 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 | 6.38 | pEC50 | 416.87 | nM | EC50 | Bioorg Med Chem Lett (2016) 26: 292-300 [PMID:26718844] |
| 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 | 6.92 | pEC50 | 120.23 | nM | EC50 | J Med Chem (2020) 63: 5297-5311 [PMID:32420741] |
| ChEMBL | Agonist activity at human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19 protein by steady-state GTPase assay | F | 6.96 | pEC50 | 109.65 | nM | EC50 | J Med Chem (2009) 52: 6297-6313 [PMID:19791743] |
| 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 | 6.96 | pEC50 | 109.65 | nM | EC50 | J Med Chem (2009) 52: 2623-2627 [PMID:19317445] |
| 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 | 7.05 | pEC50 | 89.13 | nM | EC50 | Bioorg Med Chem (2009) 17: 7186-7196 [PMID:19773175] |
| ChEMBL | Inverse 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 | 7.1 | pEC50 | 79.43 | nM | EC50 | J Med Chem (2011) 54: 1693-1703 [PMID:21348462] |
| 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 | 7.15 | pEC50 | 70.79 | nM | EC50 | Bioorg Med Chem (2009) 17: 7186-7196 [PMID:19773175] |
| ChEMBL | Inverse agonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of [35S]GTPgammaS binding | F | 7.15 | pEC50 | 70.79 | nM | EC50 | Bioorg Med Chem (2009) 17: 7186-7196 [PMID:19773175] |
| H4 receptor/Histamine H4 receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5657] [GtoPdb: 265] [UniProtKB: Q91ZY2] | ||||||||
| ChEMBL | Displacement of UR-DEBa176 from mouse recombinant H4R expressed in HEK293T-SF-His6-CRE-Luc cells | B | 7.1 | pKi | 79.43 | nM | Ki | J Med Chem (2020) 63: 5297-5311 [PMID:32420741] |
| ChEMBL | Inhibition of UR-DEBa242 binding to mouse recombinant NLuc/GPCR-fused H4R expressed in HEK293T cells measured after 30 mins by furimazine substrate based BRET assay | B | 7.18 | pKi | 66.07 | nM | Ki | J Med Chem (2020) 63: 5297-5311 [PMID:32420741] |
| GtoPdb | - | - | 7.6 | pKi | - | - | - | J Pharmacol Exp Ther (2001) 299: 121-30 [PMID:11561071] |
| 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 | 6.52 | pEC50 | 302 | nM | EC50 | J Med Chem (2020) 63: 5297-5311 [PMID:32420741] |
| ChEMBL | Antagonist activity at mouse H4R expressed in HEK293 cells co-expressing ELucC/ELucN-beta-arrestin2 assessed as inhibition of histamine-induced beta-arrestin recruitment preincubated for 15 mins followed by histamine addition by luciferase reporter gene assay | B | 7.55 | pEC50 | 28.18 | nM | EC50 | J Med Chem (2020) 63: 5297-5311 [PMID:32420741] |
| H4 receptor/Histamine H4 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4468] [GtoPdb: 265] [UniProtKB: Q91ZY1] | ||||||||
| ChEMBL | Binding affinity to rat histamine H4 receptor | B | 7.3 | pKi | 50.12 | nM | Ki | J Med Chem (2011) 54: 26-53 [PMID:21062081] |
| GtoPdb | - | - | 7.6 | pKi | - | - | - | J Pharmacol Exp Ther (2001) 299: 121-30 [PMID:11561071] |
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]
