diamide 7 [Ligand Id: 5830] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL1770298 |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| FPR1 in Human [GtoPdb: 222] [UniProtKB: P21462] | ||||||||
| GtoPdb | - | - | 6.5 | pIC50 | - | - | - | Bioorg Med Chem Lett (2011) 21: 2991-7 [PMID:21486695] |
| FPR1/fMet-Leu-Phe receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1770037] [GtoPdb: 222] [UniProtKB: P33766] | ||||||||
| ChEMBL | Antagonist activity at mouse FPR1 expressed in HEK293 cells assessed as inhibition of fMLFF-stimulated intracellular calcium mobilisation by FLIPR assay | F | 4.6 | pIC50 | 25118.86 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 2991-2997 [PMID:21486695] |
| FPR1/Formyl peptide receptor 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3359] [GtoPdb: 222] [UniProtKB: P21462] | ||||||||
| ChEMBL | Antagonist activity at human FPR1 in expressed in HEK293 cells assessed as inhibition of fMLF-stimulated intracellular calcium mobilisation after 5 mins by FLIPR assay | F | 5.8 | pIC50 | 1584.89 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 2991-2997 [PMID:21486695] |
| ChEMBL | Antagonist activity at FPR1 in human neutrophils assessed as inhibition of fMLF-stimulated degranulation after 15 mins by fluorescence assay | F | 6.4 | pIC50 | 398.11 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 2991-2997 [PMID:21486695] |
| ChEMBL | Antagonist activity at FPR1 in human neutrophils assessed as inhibition of fMLF-stimulated calcium mobilization by FLIPR assay | F | 6.4 | pIC50 | 398.11 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 2991-2997 [PMID:21486695] |
| ChEMBL | Antagonist activity at human FPR1 in human neutrophils assessed as inhibition of fMLF-stimulated intracellular calcium mobilisation by FLIPR assay | F | 6.4 | pIC50 | 398.11 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 6456-6460 [PMID:21955939] |
| ChEMBL | Intrinsic activity at FPR1 in human neutrophils assessed as increase in calcium mobilization by FLIPR assay relative to fMLF | F | 6.5 | pIC50 | 316.23 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 2991-2997 [PMID:21486695] |
| GtoPdb | - | - | 6.5 | pIC50 | - | - | - | Bioorg Med Chem Lett (2011) 21: 2991-7 [PMID:21486695] |
| ChEMBL | Displacement of [3H]fMLF from human FPR1 expressed in CHO cells by scintillation counting | B | 7 | pIC50 | 100 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 2991-2997 [PMID:21486695] |
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]
