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 [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 | 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 | 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 | 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 | 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 | 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 | 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 | 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 [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 | 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-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 |
Biochem J (2001) 355: 279-88 [PMID:11284713]; Biochem Pharmacol (2004) 68: 933-45 [PMID:15294456]; J Pharmacol Exp Ther (2003) 305: 887-96 [PMID:12606603]; Br J Pharmacol (2000) 131: 1247-50 [PMID:11090094]; J Pharmacol Exp Ther (2000) 293: 771-8 [PMID:10869375]; J Pharmacol Exp Ther (2001) 299: 908-14 [PMID:11714875]; Eur J Pharmacol (2002) 453: 33-41 [PMID:12393057] |
| 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 | 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 | 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 | 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 | 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] |
| 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 [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 | 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 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 | 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 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 | 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 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 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 | 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 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 | 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 | 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 (2000) 293: 771-8 [PMID:10869375]; J Pharmacol Exp Ther (2003) 305: 887-96 [PMID:12606603]; J Pharmacol Exp Ther (2001) 299: 908-14 [PMID:11714875]; Br J Pharmacol (2000) 131: 1247-50 [PMID:11090094]; Biochem Pharmacol (2004) 68: 933-45 [PMID:15294456]; Eur J Pharmacol (2002) 453: 33-41 [PMID:12393057]; Biochem Biophys Res Commun (2001) 280: 75-80 [PMID:11162480] |
| 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 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]
