methionine benzimidazole 6 [Ligand Id: 5829] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL1770297 |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| 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 | 5.5 | pIC50 | 3162.28 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 2991-2997 [PMID:21486695] |
| ChEMBL | Intrinsic activity at FPR1 in human neutrophils assessed as increase in calcium mobilization by FLIPR assay relative to fMLF | F | 6.3 | pIC50 | 501.19 | 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 | 6.3 | pIC50 | 501.19 | 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 | 6.3 | pIC50 | 501.19 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 6456-6460 [PMID:21955939] |
| GtoPdb | - | - | 6.3 | pIC50 | - | - | - | Bioorg Med Chem Lett (2011) 21: 2991-7 [PMID:21486695] |
| ChEMBL | Antagonist activity at FPR1 in human neutrophils assessed as inhibition of fMLF-stimulated degranulation after 15 mins by fluorescence assay | F | 6.8 | pIC50 | 158.49 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 2991-2997 [PMID:21486695] |
| ChEMBL | Displacement of [3H]fMLF from human FPR1 expressed in CHO cells by scintillation counting | B | 7.5 | pIC50 | 31.62 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 2991-2997 [PMID:21486695] |
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]
