JNJ 7777120 [Ligand Id: 1278] activity data from GtoPdb and ChEMBL
Click here for a description of the charts and data table
Please tell us if you are using this feature and what you think!
| ChEMBL ligand: CHEMBL129198 (JNJ-7777120) |
|---|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
| 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 H1R expressed in Sf9 cells co-expressing RGS4 after 90 mins by liquid scintillation counting | B | 4.33 | pKi | 46773.51 | nM | Ki | Bioorg Med Chem Lett (2011) 21: 6274-6280 [PMID:21944853] |
| ChEMBL | Binding affinity to human histamine H1 receptor | B | 6.01 | pKi | 977.24 | nM | Ki | J Med Chem (2008) 51: 7094-7098 [PMID:18983139] |
| Histamine H1 receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3943] [UniProtKB: P31389] | ||||||||
| ChEMBL | Antagonist activity at H1R in guinea pig ileum assessed as inhibition of histamine-induced muscle contraction after 15 mins | F | 5.8 | pKd | 1584.89 | nM | Kd | Bioorg Med Chem Lett (2011) 21: 6274-6280 [PMID:21944853] |
| ChEMBL | Antagonist activity at histamine H1 receptor in guinea-pig ileum assessed as inhibition of histamine-induced contractions after 15 mins | B | 6.11 | pKd | 776.25 | nM | Kd | Bioorg Med Chem (2019) 27: 1254-1262 [PMID:30792106] |
| H2 receptor/Histamine H2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1941] [GtoPdb: 263] [UniProtKB: P25021] | ||||||||
| ChEMBL | Binding affinity to human histamine H2 receptor | B | 5.07 | pKi | >8511.38 | nM | Ki | J Med Chem (2008) 51: 7094-7098 [PMID:18983139] |
| H3 receptor/Histamine H3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL264] [GtoPdb: 264] [UniProtKB: Q9Y5N1] | ||||||||
| ChEMBL | Binding affinity to human histamine H3 receptor | B | 4.7 | pKi | >20000 | nM | Ki | Bioorg Med Chem Lett (2012) 22: 1156-1159 [PMID:22189138] |
| ChEMBL | Binding affinity to human histamine H3 receptor | B | 4.82 | pKi | 15300 | nM | Ki | Bioorg Med Chem Lett (2012) 22: 1156-1159 [PMID:22189138] |
| ChEMBL | Binding affinity to histamine H3 receptor | B | 5.29 | pKi | 5125 | nM | Ki | J Med Chem (2005) 48: 8289-8298 [PMID:16366610] |
| ChEMBL | Displacement of [3H]histamine from human H3 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting | B | 5.3 | pKi | 5011.87 | nM | Ki | J Med Chem (2011) 54: 8136-8147 [PMID:22003888] |
| ChEMBL | Binding affinity to human histamine H3 receptor | B | 5.65 | pKi | 2238.72 | nM | Ki | J Med Chem (2008) 51: 7094-7098 [PMID:18983139] |
| ChEMBL | Binding affinity to human histamine H3 receptor | B | 5.65 | pKi | 2238.72 | nM | Ki | J Med Chem (2008) 51: 6571-6580 [PMID:18811133] |
| ChEMBL | Binding affinity towards human histamine H3 receptor was determined by [3H]Na-methylhistamine binding to SK-N-MC cell membranes | B | 5.7 | pKi | 1995.26 | nM | Ki | Bioorg Med Chem Lett (2004) 14: 5251-5256 [PMID:15454206] |
| ChEMBL | Displacement of [3H]-N-alpha-methylhistamine from recombinant human histamine H3 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting method | B | 4 | pIC50 | >100000 | nM | IC50 | J Med Chem (2018) 61: 2949-2961 [PMID:29579390] |
| ChEMBL | Effective concentration required against human histamine H3 receptor was determined by the inhibition of the cAMP stimulated beta-galactosidase transcription in SK-N-MC cells | B | 6 | pEC50 | 1000 | nM | EC50 | Bioorg Med Chem Lett (2004) 14: 5251-5256 [PMID:15454206] |
| H3 receptor/Histamine H3 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4124] [GtoPdb: 264] [UniProtKB: Q9QYN8] | ||||||||
| ChEMBL | Binding affinity to rat histamine H3 receptor | B | 5.84 | pKi | 1445.44 | nM | Ki | J Med Chem (2008) 51: 7094-7098 [PMID:18983139] |
| ChEMBL | Binding affinity to rat histamine H3 receptor | B | 5.88 | pKi | 1318.26 | nM | Ki | J Med Chem (2008) 51: 6571-6580 [PMID:18811133] |
| H4 receptor/Histamine H4 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3759] [GtoPdb: 265] [UniProtKB: Q9H3N8] | ||||||||
| ChEMBL | pA2 value against histamine h4 receptor | B | 8 | pKd | 10 | nM | Kd | Bioorg Med Chem Lett (2004) 14: 5251-5256 [PMID:15454206] |
| ChEMBL | Antagonistic activity at human histamine H4 receptor in SK-N-MC cells by inhibition of forskolin-stimulated cAMP-mediated reporter gene activity | F | 8.1 | pKd | 7.94 | nM | Kd | J Med Chem (2005) 48: 8289-8298 [PMID:16366610] |
| ChEMBL | Decrease in the forskolin stimulatedcAMP levels was determined using SK-N-MC cells stably transfected with the human H4 receptor | F | 8.14 | pKd | 7.24 | nM | Kd | J Med Chem (2003) 46: 3957-3960 [PMID:12954048] |
| ChEMBL | Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells by competitive kinetic analysis | B | 8.4 | pKd | 3.98 | nM | Kd | Bioorg Med Chem Lett (2013) 23: 2663-2670 [PMID:23558237] |
| ChEMBL | Displacement of [3H]histamine from human histamine H4 receptor L175'5.39V mutant transfected in HEK293T cells after 1.5 hrs by liquid scintillation counting analysis | B | 6.4 | pKi | 398.11 | nM | Ki | Medchemcomm (2013) 4: 193-204 |
| ChEMBL | Displacement of [3H]histamine from human recombinant histamine H4 receptor expressed in CHO cells coexpressing Ga15 by radioligand filtration binding assay | B | 6.93 | pKi | 118 | nM | Ki | Bioorg Med Chem Lett (2012) 22: 1156-1159 [PMID:22189138] |
| ChEMBL | Displacement of [3H]histamine from human histamine H4 receptor expressed in sf9 cells co-expressing mammalian Galphai2 and Gbeta1gamma2 | B | 7.16 | pKi | 69 | nM | Ki | J Med Chem (2016) 59: 3452-3470 [PMID:27007611] |
| ChEMBL | Displacement of [3H]-histamine from human recombinant H4R expressed in HEK293T cell homogenates | B | 7.2 | pKi | 63.1 | 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 | 7.2 | pKi | 63.1 | 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 | 7.2 | pKi | 63.1 | 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 | 7.2 | pKi | 63.1 | 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 | 7.2 | pKi | 63.1 | 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 | B | 7.2 | pKi | 63.1 | 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 | 7.2 | pKi | 63.1 | nM | Ki | J Med Chem (2020) 63: 5297-5311 [PMID:32420741] |
| ChEMBL | Binding affinity to histamine H4 receptor | B | 7.3 | pKi | 50.12 | nM | Ki | Bioorg Med Chem (2009) 17: 7186-7196 [PMID:19773175] |
| ChEMBL | Antagonist activity at human histamine H4 receptor expressed in HEK293 cells assessed as rev inhibition of forskolin-stimulated cAMP accumulation by CRE-betalactamase reporter gene assay | F | 7.34 | pKi | 46 | nM | Ki | Bioorg Med Chem Lett (2012) 22: 1156-1159 [PMID:22189138] |
| ChEMBL | Binding affinity to histamine 4 receptor (unknown origin) | B | 7.45 | pKi | 35.48 | nM | Ki | Bioorg Med Chem Lett (2016) 26: 292-300 [PMID:26718844] |
| ChEMBL | Displacement of [3H]histamine from human histamine H4 receptor E182'5.46Q mutant transfected in HEK293T cells after 1.5 hrs by liquid scintillation counting analysis | B | 7.5 | pKi | 31.62 | nM | Ki | Medchemcomm (2013) 4: 193-204 |
| ChEMBL | Displacement of [3H]histamine from wild type human histamine H4 receptor transfected in HEK293T cells after 1.5 hrs by liquid scintillation counting analysis | B | 7.7 | pKi | 19.95 | nM | Ki | Medchemcomm (2013) 4: 193-204 |
| ChEMBL | Binding affinity towards human histamine H4 receptor was determined by [3H]Na-methylhistamine binding to SK-N-MC cell membranes | B | 7.7 | pKi | 19.95 | nM | Ki | Bioorg Med Chem Lett (2004) 14: 5251-5256 [PMID:15454206] |
| ChEMBL | Displacement of [3H]histamine from human H4R expressed in Sf9 cells co-expressing RGS19, Galphai2 and Gbeta1gamma2 after 60 mins by liquid scintillation counting | B | 7.73 | pKi | 18.62 | nM | Ki | Bioorg Med Chem Lett (2011) 21: 6274-6280 [PMID:21944853] |
| ChEMBL | Displacement of [3H]histamine from human histamine H4 receptor expressed in SK-NM-C cells | B | 7.77 | pKi | 17 | nM | Ki | J Med Chem (2008) 51: 3145-3153 [PMID:18459760] |
| ChEMBL | Antagonist activity at Homo sapiens (human) histamine H4 receptor | B | 7.77 | pKi | 17 | nM | Ki | Med Chem Res (2004) 13: 619-630 |
| 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 transfected in SK-N-MC cells | B | 7.8 | pKi | 15.85 | nM | Ki | J Med Chem (2006) 49: 4512-4516 [PMID:16854056] |
| ChEMBL | Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells | B | 7.8 | pKi | 15.85 | nM | Ki | J Med Chem (2008) 51: 2457-2467 [PMID:18357976] |
| ChEMBL | Displacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 | B | 7.85 | pKi | 14 | nM | Ki | Bioorg Med Chem (2009) 17: 7186-7196 [PMID:19773175] |
| ChEMBL | Displacement of [3H]histamine from human histamine H4 receptor expressed in human SK-N-MC cell membrane incubated for 60 mins | B | 7.89 | pKi | 13 | nM | Ki | J Med Chem (2016) 59: 3452-3470 [PMID:27007611] |
| ChEMBL | Displacement of clobenpropit-BODIPY-630/650 from recombinant human NLuc-fused H4R expressed in HEK293T cells by Nano-BRET assay | B | 7.9 | pKi | 12.59 | 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 by liquid scintillation counting | B | 7.92 | pKi | 12.02 | nM | Ki | J Med Chem (2008) 51: 7094-7098 [PMID:18983139] |
| ChEMBL | Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells | B | 7.92 | pKi | 12.02 | nM | Ki | J Med Chem (2008) 51: 6547-6557 [PMID:18817367] |
| ChEMBL | Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells | B | 7.92 | pKi | 12.02 | nM | Ki | J Med Chem (2008) 51: 6571-6580 [PMID:18811133] |
| ChEMBL | Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells | B | 7.92 | pKi | 12 | nM | Ki | J Med Chem (2008) 51: 6547-6557 [PMID:18817367] |
| ChEMBL | Displacement of [3H]-histamine from full length human H4R expressed in HEK293 cells | B | 8.1 | pKi | 8 | nM | Ki | Bioorg Med Chem Lett (2011) 21: 6596-6602 [PMID:21920751] |
| ChEMBL | Displacement of [3H]histamine from human recombinant histamine H4 receptor expressed in CHO cells coexpressing Ga15 by radioligand filtration binding assay | B | 8.1 | pKi | 8 | nM | Ki | Bioorg Med Chem Lett (2012) 22: 1156-1159 [PMID:22189138] |
| ChEMBL | Displacement of [3H]histamine from human histamine H4 receptor expressed in CHO cells after 90 mins by scintillation counting technique | B | 8.1 | pKi | 8 | nM | Ki | Bioorg Med Chem Lett (2011) 21: 6591-6595 [PMID:21955944] |
| ChEMBL | Antagonist activity at human histamine H4 receptor by functional assay | F | 8.17 | pKi | 6.8 | nM | Ki | Bioorg Med Chem Lett (2011) 21: 6591-6595 [PMID:21955944] |
| ChEMBL | Antagonist activity at human histamine H4 receptor expressed in HEK293 cells assessed as rev inhibition of forskolin-stimulated cAMP accumulation by CRE-betalactamase reporter gene assay | F | 8.17 | pKi | 6.8 | nM | Ki | Bioorg Med Chem Lett (2012) 22: 1156-1159 [PMID:22189138] |
| ChEMBL | Antagonist activity at full length human H4R expressed in HEK293 cells assessed as reversal of forskolin-induced cAMP production by CRE-beta-lactamase reporter gene assay | F | 8.17 | pKi | 6.8 | nM | Ki | Bioorg Med Chem Lett (2011) 21: 6596-6602 [PMID:21920751] |
| ChEMBL | Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells | B | 8.2 | pKi | 6.31 | nM | Ki | Eur J Med Chem (2012) 54: 660-668 [PMID:22749391] |
| ChEMBL | Displacement of [3H]histamine displacement from human recombinant histamine H4 receptor expressed in SK-NM-C cells after 45 mins | B | 8.2 | pKi | 6.31 | nM | Ki | J Med Chem (2013) 56: 4264-4276 [PMID:23668417] |
| ChEMBL | Binding affinity to human histamine H4 receptor | B | 8.22 | pKi | 6 | nM | Ki | Bioorg Med Chem Lett (2012) 22: 461-467 [PMID:22153663] |
| GtoPdb | - | - | 8.3 | pKi | 5.01 | nM | Ki |
J Pharmacol Exp Ther (2005) 314: 1310-21 [PMID:15947036]; J Pharmacol Exp Ther (2004) 309: 404-413 [PMID:14722321]; J Med Chem (2006) 49: 4512-6 [PMID:16854056] |
| ChEMBL | Displacement of [3H]histamine from human recombinant histamine H4 receptor | B | 8.3 | pKi | 5 | nM | Ki | Bioorg Med Chem Lett (2015) 25: 956-959 [PMID:25595684] |
| ChEMBL | Displacement of [3H]histamine from human recombinant histamine H4 receptor | B | 8.3 | pKi | 5 | nM | Ki | Bioorg Med Chem Lett (2014) 24: 5489-5492 [PMID:25455490] |
| ChEMBL | Displacement of [3H]histamine from human recombinant histamine H4 receptor expressed in SK-N-MC cells after 45 mins by competition binding analysis | B | 8.3 | pKi | 5 | nM | Ki | J Med Chem (2014) 57: 2429-2439 [PMID:24495018] |
| ChEMBL | Displacement of [3H]histamine from human histamine 4 receptor expressed in HEK293T cell membranes incubated for 1 hr by radioligand binding assay | B | 8.31 | pKi | 4.9 | nM | Ki | Bioorg Med Chem Lett (2016) 26: 292-300 [PMID:26718844] |
| ChEMBL | Binding affinity to human histamine H4 receptor | B | 8.35 | pKi | 4.5 | nM | Ki | J Med Chem (2015) 58: 7119-7127 [PMID:25993395] |
| ChEMBL | Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells | B | 8.38 | pKi | 4.17 | nM | Ki | J Med Chem (2008) 51: 7855-7865 [PMID:19053770] |
| 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 | 8.38 | pKi | 4.17 | nM | Ki | J Med Chem (2020) 63: 5297-5311 [PMID:32420741] |
| ChEMBL | Binding affinity to histamine H4 receptor (unknown origin) assessed as inhibition constant | B | 8.39 | pKi | 4.1 | nM | Ki | Eur J Med Chem (2023) 249: 115151-115151 [PMID:36731273] |
| ChEMBL | Displacement of [3H]- histamine from the recombinant human histamine H4 receptor | B | 8.4 | pKi | 4 | nM | Ki | J Med Chem (2003) 46: 3957-3960 [PMID:12954048] |
| ChEMBL | Displacement of [3H]histamine from human H4 receptor expressed in HEK cell membranes | B | 8.4 | pKi | 4 | nM | Ki | Bioorg Med Chem Lett (2012) 22: 461-467 [PMID:22153663] |
| ChEMBL | Antagonist activity at Homo sapiens (human) histamine H4 receptor | B | 8.4 | pKi | 4 | nM | Ki | Med Chem Res (2004) 13: 619-630 |
| ChEMBL | Displacement of [3H]histamine from human histamine H4 receptor | B | 8.4 | pKi | 4 | nM | Ki | Bioorg Med Chem Lett (2011) 21: 3113-3116 [PMID:21458260] |
| ChEMBL | Binding affinity to human histamine H4 receptor | B | 8.4 | pKi | 4 | nM | Ki | Bioorg Med Chem Lett (2012) 22: 1156-1159 [PMID:22189138] |
| ChEMBL | Displacement of [3H]histamine from recombinant human histamine H4 receptor in SK-N-MC cells | B | 8.4 | pKi | 4 | nM | Ki | J Med Chem (2005) 48: 8289-8298 [PMID:16366610] |
| ChEMBL | Displacement of [3H]-histamine from human H4R expressed in HEK293T cells | B | 8.48 | pKi | 3.31 | nM | Ki | Bioorg Med Chem Lett (2011) 21: 6596-6602 [PMID:21920751] |
| ChEMBL | Antagonist activity at H4R in human eosinophils assessed as inhibition of histamine-induced CD11b upregulation | F | 6.65 | pIC50 | 221.4 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 6596-6602 [PMID:21920751] |
| ChEMBL | Antagonist actiivty at human H4R expressed in human U2OS cells assessed as inhibition of [35S]GTPgammaS binding after 30 mins by scintillation proximity assay | F | 6.7 | pIC50 | 199.53 | nM | IC50 | J Med Chem (2014) 57: 6887-6896 [PMID:24697360] |
| ChEMBL | Antagonist activity at H4R in human eosinophils assessed as inhibition of histamine-induced shape change by GAFS assay | F | 6.7 | pIC50 | 199 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 6596-6602 [PMID:21920751] |
| ChEMBL | Inhibition of histamine H4 receptor-mediated chemotaxis in human eosinophils | B | 7.07 | pIC50 | 86 | nM | IC50 | Eur J Med Chem (2012) 54: 660-668 [PMID:22749391] |
| ChEMBL | Inhibition of human eosinophil chemotaxis mediated by histamine H4 receptor | F | 7.07 | pIC50 | 86 | nM | IC50 | J Med Chem (2005) 48: 8289-8298 [PMID:16366610] |
| ChEMBL | Inhibition of mouse bone-marrow mast cell chemotaxis mediated by histamine H4 receptor | F | 7.4 | pIC50 | 40 | nM | IC50 | J Med Chem (2005) 48: 8289-8298 [PMID:16366610] |
| ChEMBL | Antagonist activity at H4R in human eosinophils assessed as inhibition of imetit-induced shape change by GAFS assay | F | 7.52 | pIC50 | 30 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 6596-6602 [PMID:21920751] |
| ChEMBL | Displacement of [3H]-histamine from recombinant human histamine H4 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting method | B | 7.54 | pIC50 | 29 | nM | IC50 | J Med Chem (2018) 61: 2949-2961 [PMID:29579390] |
| ChEMBL | Antagonist activity at recombinant human H4 receptor expressed in CHOK1 cells co-expressing Galpha16/aequorin assessed as inhibition of histamine-induced intracellular calcium flux preincubated for 30 mins followed by histamine addition and measured for 30 secs in presence of coelenterazine by luminescence assay | F | 7.89 | pIC50 | 13 | nM | IC50 | Bioorg Med Chem (2019) 27: 1254-1262 [PMID:30792106] |
| ChEMBL | Antagonist activity at H4R in human eosinophils assessed as inhibition of histamine-induced actin polymerisation | F | 8.28 | pIC50 | 5.3 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 6596-6602 [PMID:21920751] |
| ChEMBL | Agonist activity at human H4R expressed in human U2OS cells assessed as recruitment of beta-arrestin after 2 hrs by PathHunter beta-galactosidase enzyme fragment complementation assay | B | 7.6 | pEC50 | 25.12 | nM | EC50 | J Med Chem (2014) 57: 6887-6896 [PMID:24697360] |
| 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 | 7.8 | pEC50 | 15.85 | nM | EC50 | Bioorg Med Chem (2009) 17: 7186-7196 [PMID:19773175] |
| ChEMBL | Agonist activity at histamine H4 receptor (unknown origin) assessed as increase in beta-arrestin recruitment | B | 7.9 | pEC50 | 12.59 | nM | EC50 | J Med Chem (2018) 61: 9841-9878 [PMID:29939744] |
| 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 | 6.9 | pKi | 125.89 | 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 | 7.93 | pKi | 11.75 | nM | Ki | J Med Chem (2020) 63: 5297-5311 [PMID:32420741] |
| ChEMBL | Displacement of [3H]-histamine from mouse H4R expressed in HEK293T cells | B | 8.41 | pKi | 3.89 | nM | Ki | Bioorg Med Chem Lett (2011) 21: 6596-6602 [PMID:21920751] |
| ChEMBL | Inhibition of histamine H4 receptor-mediated chemotaxis in mouse bone marrow cells | B | 7.4 | pIC50 | 40 | nM | IC50 | Eur J Med Chem (2012) 54: 660-668 [PMID:22749391] |
| ChEMBL | Agonist activity at mouse H4R by [35S]-GTPgammaS-binding assay | F | 6.1 | pEC50 | 794.33 | nM | EC50 | J Med Chem (2019) 62: 8338-8356 [PMID:31469288] |
| ChEMBL | Antagonist activity at mouse histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assay | F | 8.62 | pEC50 | 2.4 | nM | EC50 | J Med Chem (2008) 51: 6547-6557 [PMID:18817367] |
| 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 | 8.22 | pKi | 6 | nM | Ki | Bioorg Med Chem Lett (2012) 22: 461-467 [PMID:22153663] |
| ChEMBL | Displacement of [3H]histamine from rat histamine H4 receptor expressed in HEK293 cells by liquid scintillation counting | B | 8.33 | pKi | 4.68 | nM | Ki | J Med Chem (2008) 51: 7094-7098 [PMID:18983139] |
| ChEMBL | Displacement of [3H]-histamine from rat H4R expressed in HEK293T cells | B | 8.37 | pKi | 4.27 | nM | Ki | Bioorg Med Chem Lett (2011) 21: 6596-6602 [PMID:21920751] |
| ChEMBL | Displacement of [3H]histamine from rat histamine H4 receptor expressed in HEK293 cells | B | 8.57 | pKi | 2.69 | nM | Ki | J Med Chem (2008) 51: 6547-6557 [PMID:18817367] |
| ChEMBL | Displacement of [3H]histamine from rat histamine H4 receptor expressed in HEK293 cells | B | 8.57 | pKi | 2.69 | nM | Ki | J Med Chem (2008) 51: 6571-6580 [PMID:18811133] |
| ChEMBL | Binding affinity of compound towards rat histamine H4 receptor | B | 8.62 | pKi | 2.4 | nM | Ki | J Med Chem (2003) 46: 3957-3960 [PMID:12954048] |
| ChEMBL | Agonist activity at rat H4R by [35S]-GTPgammaS-binding assay | F | 6.13 | pEC50 | 741.31 | nM | EC50 | J Med Chem (2019) 62: 8338-8356 [PMID:31469288] |
| ChEMBL | Agonist activity at rat histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein by GTPgammaS assay | F | 7.37 | pEC50 | 42.66 | nM | EC50 | J Med Chem (2008) 51: 6571-6580 [PMID:18811133] |
| ChEMBL | Antagonist activity at rat histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assay | F | 8.59 | pEC50 | 2.57 | nM | EC50 | J Med Chem (2008) 51: 6547-6557 [PMID:18817367] |
| Histamine H4 receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1255160] [UniProtKB: Q91ZY3] | ||||||||
| ChEMBL | Displacement of [3H]-histamine from guinea pig H4R expressed in HEK293T cells | B | 5.97 | pKi | 1071.52 | nM | Ki | Bioorg Med Chem Lett (2011) 21: 6596-6602 [PMID:21920751] |
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]
