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
BioActive Compounds: 4
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
Compounds with activity <= 50uM or explicitly reported as active by ChEMBL are flagged as active in this PubChem assay presentation.
Putative Target:
ChEMBL Target ID: 13010
Target Type: SINGLE PROTEIN
Pref Name: Formyl peptide receptor 1
Description: fMet-Leu-Phe receptor
Organism: Homo sapiens
Tax ID: 9606
Confidence: Homologous single protein target assigned
Relationship Type: Homologous protein target assigned
ChEMBL target type: Target is a single protein chain
Putative Target:
ChEMBL Target ID: 13010
Target Type: SINGLE PROTEIN
Pref Name: Formyl peptide receptor 1
Description: fMet-Leu-Phe receptor
Organism: Homo sapiens
Tax ID: 9606
Confidence: Homologous single protein target assigned
Relationship Type: Homologous protein target assigned
ChEMBL target type: Target is a single protein chain
Categorized Comment
ChEMBL Assay Type: Functional
ChEMBL Assay Data Source: Scientific Literature
ChEMBL Assay Data Source: Scientific Literature
Result Definitions
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| TID | Name | Description | Histogram | Type | Unit | |
|---|---|---|---|---|---|---|
| Outcome | The BioAssay activity outcome | Outcome | ||||
| 1 | IC50* | IC50 PubChem standard value |  | Float | μM | |
| 2 | IC50 activity comment | IC50 activity comment | String | |||
| 3 | IC50 standard flag | IC50 standard flag | | Integer | ||
| 4 | IC50 qualifier | IC50 qualifier | String | |||
| 5 | IC50 published value | IC50 published value | | Float | nM | |
| 6 | IC50 standard value | IC50 standard value | | Float | nM | |
| 7 | Ki activity comment | Ki activity comment | String | |||
| 8 | Ki standard flag | Ki standard flag | | Integer | ||
| 9 | Ki qualifier | Ki qualifier | String | |||
| 10 | Ki published value | Ki published value | | Float | nM | |
| 11 | Ki standard value | Ki standard value | | Float | nM |
* Activity Concentration.
Data Table (Concise)
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