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