AZD3778 [Ligand Id: 7679] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL2158814 (AZD-3778)
  • CCR3/C-C chemokine receptor type 3 in Human [ChEMBL: CHEMBL3473] [GtoPdb: 60] [UniProtKB: P51677]
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  • H1 receptor/Histamine H1 receptor in Human [ChEMBL: CHEMBL231] [GtoPdb: 262] [UniProtKB: P35367]
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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 31:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, Cibrián-Uhalte E, Davies M, Dedman N, Karlsson A, Magariños MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]