JNJ 7777120 [Ligand Id: 1278] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL129198 (JNJ-7777120) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| H1 receptor/Histamine H1 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL231] [GtoPdb: 262] [UniProtKB: P35367] | ||||||||
| ChEMBL | Displacement of [3H]mepyramine from human 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 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 | 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 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]-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 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]-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 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 | 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 | 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 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 | 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 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 | 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 | 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 | 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 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 | 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 | 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 | 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 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 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 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 | 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 | 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 | 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 | 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 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 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 | 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 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 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]
