The identification of two novel series of formyl peptide receptor 1 (FPR1) antagonists are reported, represented by methionine benzimidazole 6 and diamide 7. Both series specifically inhibited the binding of labelled fMLF to hrFPR1 and selectively antagonized FPR1 function in human neutrophils, making them useful in vitro validation tools for the target. ..more
Tested Compounds:
Description:
Title: Discovery of small molecule human FPR1 receptor antagonists.
Abstract: The identification of two novel series of formyl peptide receptor 1 (FPR1) antagonists are reported, represented by methionine benzimidazole 6 and diamide 7. Both series specifically inhibited the binding of labelled fMLF to hrFPR1 and selectively antagonized FPR1 function in human neutrophils, making them useful in vitro validation tools for the target.
(PMID: 21486695)
Abstract: The identification of two novel series of formyl peptide receptor 1 (FPR1) antagonists are reported, represented by methionine benzimidazole 6 and diamide 7. Both series specifically inhibited the binding of labelled fMLF to hrFPR1 and selectively antagonized FPR1 function in human neutrophils, making them useful in vitro validation tools for the target.
(PMID: 21486695)
Comment
Putative Target:
ChEMBL Target ID: 22226
Target Type: UNCHECKED
Pref Name: Unchecked
Confidence: Default value - Target unknown or has yet to be assigned
Relationship Type: Default value - Target has yet to be curated
ChEMBL Target ID: 22226
Target Type: UNCHECKED
Pref Name: Unchecked
Confidence: Default value - Target unknown or has yet to be assigned
Relationship Type: Default value - Target has yet to be curated
Categorized Comment
ChEMBL Assay Type: ADMET
ChEMBL Assay Data Source: Scientific Literature
ChEMBL Assay Test Type: In vitro
ChEMBL Assay Tissue: Liver
ChEMBL Assay Cell Type: Hepatocytes
ChEMBL Assay Data Source: Scientific Literature
ChEMBL Assay Test Type: In vitro
ChEMBL Assay Tissue: Liver
ChEMBL Assay Cell Type: Hepatocytes
Result Definitions
| TID | Name | Description | Histogram | Type | Unit | |
|---|---|---|---|---|---|---|
| Outcome | The BioAssay activity outcome | Outcome | ||||
| 1 | CL activity comment | CL activity comment | String | |||
| 2 | CL standard flag | CL standard flag |  | Integer | ||
| 3 | CL qualifier | CL qualifier | String | |||
| 4 | CL published value | CL published value | | Float | uL/min | |
| 5 | CL standard value | CL standard value | | Float | uL/min | |
| 6 | CL data validity | CL data validity | String |
Data Table (Concise)
PageFrom: