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ChEMBL ligand: CHEMBL2158814 (AZD-3778) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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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]