ChEMBL ligand: CHEMBL185951 (JNJ-10191584)
H3 receptor/Histamine H3 receptor in Human [ChEMBL: CHEMBL264] [GtoPdb: 264] [UniProtKB: Q9Y5N1] There should be some charts here, you may need to enable JavaScript!
H4 receptor/Histamine H4 receptor in Human [ChEMBL: CHEMBL3759] [GtoPdb: 265] [UniProtKB: Q9H3N8] 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
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 histamine H3 receptor	B	4.85	pKi	14053	nM	Ki	J Med Chem (2005) 48: 8289-8298 [PMID:16366610]
ChEMBL	Binding affinity towards human histamine H3 receptor was determined by [3H]Na-methylhistamine binding to SK-N-MC cell membranes	B	5.4	pKi	3981.07	nM	Ki	Bioorg Med Chem Lett (2004) 14: 5251-5256 [PMID:15454206]
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	5.5	pEC50	3162.28	nM	EC50	Bioorg Med Chem Lett (2004) 14: 5251-5256 [PMID:15454206]
H4 receptor/Histamine H4 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3759] [GtoPdb: 265] [UniProtKB: Q9H3N8]
ChEMBL	Antagonistic activity at human histamine H4 receptor in SK-N-MC cells by inhibition of forskolin-stimulated cAMP-mediated reporter gene activity	F	7.7	pKd	19.95	nM	Kd	J Med Chem (2005) 48: 8289-8298 [PMID:16366610]
GtoPdb	-	-	7.1	pKi	-	-	-	Bioorg Med Chem Lett (2004) 14: 5251-6 [PMID:15454206]
ChEMBL	Binding affinity towards human histamine H4 receptor was determined by [3H]Na-methylhistamine binding to SK-N-MC cell membranes	B	7.1	pKi	79.43	nM	Ki	Bioorg Med Chem Lett (2004) 14: 5251-5256 [PMID:15454206]
ChEMBL	Displacement of [3H]histamine from human recombinant histamine H4 receptor expressed in CHO cells coexpressing Ga15 by radioligand filtration binding assay	B	7.32	pKi	47.7	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	7.32	pKi	47.7	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	7.4	pKi	39.6	nM	Ki	Bioorg Med Chem Lett (2012) 22: 1156-1159 [PMID:22189138]
ChEMBL	Antagonist activity at human histamine H4 receptor by functional assay	F	7.4	pKi	39.6	nM	Ki	Bioorg Med Chem Lett (2011) 21: 6591-6595 [PMID:21955944]
ChEMBL	Binding affinity to histamine H4 receptor (unknown origin) assessed as inhibition constant	B	7.57	pKi	27	nM	Ki	Eur J Med Chem (2023) 249: 115151-115151 [PMID:36731273]
ChEMBL	Displacement of [3H]histamine from human H4 receptor expressed in HEK cell membranes	B	7.59	pKi	26	nM	Ki	Bioorg Med Chem Lett (2012) 22: 461-467 [PMID:22153663]
ChEMBL	Displacement of [3H]histamine from human histamine H4 receptor	B	7.59	pKi	26	nM	Ki	Bioorg Med Chem Lett (2011) 21: 3113-3116 [PMID:21458260]
ChEMBL	Displacement of [3H]histamine from recombinant human histamine H4 receptor in SK-N-MC cells	B	7.59	pKi	26	nM	Ki	J Med Chem (2005) 48: 8289-8298 [PMID:16366610]
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	7.7	pKi	20	nM	Ki	J Med Chem (2014) 57: 2429-2439 [PMID:24495018]
ChEMBL	Inhibition of human eosinophil chemotaxis mediated by histamine H4 receptor	F	6.28	pIC50	530	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	6.86	pIC50	138	nM	IC50	J Med Chem (2005) 48: 8289-8298 [PMID:16366610]

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]