ChEMBL ligand: CHEMBL2158814 (AZD-3778)
CCR3/C-C chemokine receptor type 3 in Human [ChEMBL: CHEMBL3473] [GtoPdb: 60] [UniProtKB: P51677] There should be some charts here, you may need to enable JavaScript!
Kv11.1/HERG in Human [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809] There should be some charts here, you may need to enable JavaScript!
H1 receptor/Histamine H1 receptor in Human [ChEMBL: CHEMBL231] [GtoPdb: 262] [UniProtKB: P35367] 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
CCR3/C-C chemokine receptor type 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3473] [GtoPdb: 60] [UniProtKB: P51677]
ChEMBL	Antagonist activity at CCR3 receptor in human polymorphonuclear leukocytes assessed as inhibition of eotaxin-induced CD11b expression after 15 mins by flow cytometric analysis	F	7	pKd	100	nM	Kd	Bioorg Med Chem Lett (2012) 22: 6688-6693 [PMID:23031591]
ChEMBL	Binding affinity to human CCR3 expressed in CHOK1 cells by radioligand displacement assay	B	8.2	pKi	6.31	nM	Ki	Bioorg Med Chem Lett (2012) 22: 6694-6699 [PMID:23021991]
ChEMBL	Binding affinity to human CCR3 receptor expressed in CHOK1 cells by radioligand displacement assay	B	8.2	pKi	6.31	nM	Ki	Bioorg Med Chem Lett (2012) 22: 6688-6693 [PMID:23031591]
GtoPdb	Assay using sodium salt of the compound	-	8.2	pKi	6.3	nM	Ki	Bioorg Med Chem Lett (2012) 22: 6688-93 [PMID:23031591]
ChEMBL	Antagonist activity at CCR3 assessed as inhibition of eotaxin binding	B	8.09	pIC50	8.1	nM	IC50	J Med Chem (2012) 55: 9363-9392 [PMID:22931505]
Kv11.1/HERG in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809]
ChEMBL	Displacement of 3,7-Bis[2-(4-nitro[3,5-3H]phenyl)ethyl]-3,7-diazabicyclo[3.3.1]nonane from human ERG expressed in HEK cells after 3 hrs by TopCount analysis	B	4.6	pIC50	25118.86	nM	IC50	Bioorg Med Chem Lett (2012) 22: 6694-6699 [PMID:23021991]
ChEMBL	Inhibition of human ERG expressed in HEK293 cells by electrophysiological ion flux assay	B	4.8	pIC50	>15848.93	nM	IC50	Bioorg Med Chem Lett (2012) 22: 6688-6693 [PMID:23031591]
GtoPdb	-	-	4.8	pIC50	15800	nM	IC50	Bioorg Med Chem Lett (2012) 22: 6688-93 [PMID:23031591]
H1 receptor/Histamine H1 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL231] [GtoPdb: 262] [UniProtKB: P35367]
GtoPdb	Assayed using the sodium salt of the compound	-	7.5	pKi	31.6	nM	Ki	Bioorg Med Chem Lett (2012) 22: 6688-93 [PMID:23031591]
ChEMBL	Binding affinity to histamine H1 receptor	B	7.5	pKi	31.62	nM	Ki	Bioorg Med Chem Lett (2012) 22: 6694-6699 [PMID:23021991]
ChEMBL	Displacement of [3H]pyrilamine from human H1 receptor expressed in CHOK1 cells	B	7.5	pKi	31.62	nM	Ki	Bioorg Med Chem Lett (2012) 22: 6688-6693 [PMID:23031591]
ChEMBL	Binding affinity to histamine H1 receptor	B	7.4	pIC50	40	nM	IC50	J Med Chem (2012) 55: 9363-9392 [PMID:22931505]

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]