A series of pyrazole inhibitors of the human FPR1 receptor have been identified from high throughput screening. The compounds demonstrate potent inhibition in human neutrophils and attractive physicochemical and in vitro DMPK profiles to be of further interest. ..more
BioActive Compounds: 2
Description:
Title: Discovery of pyrazoles as novel FPR1 antagonists.
Abstract: A series of pyrazole inhibitors of the human FPR1 receptor have been identified from high throughput screening. The compounds demonstrate potent inhibition in human neutrophils and attractive physicochemical and in vitro DMPK profiles to be of further interest.
(PMID: 21955939)
Abstract: A series of pyrazole inhibitors of the human FPR1 receptor have been identified from high throughput screening. The compounds demonstrate potent inhibition in human neutrophils and attractive physicochemical and in vitro DMPK profiles to be of further interest.
(PMID: 21955939)
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
| TID | Name | Description | Histogram | Type | Unit | |
|---|---|---|---|---|---|---|
| Outcome | The BioAssay activity outcome | Outcome | ||||
| 1 | Kd* | Kd PubChem standard value |  | Float | μM | |
| 2 | Kd activity comment | Kd activity comment | String | |||
| 3 | Kd standard flag | Kd standard flag | | Integer | ||
| 4 | Kd qualifier | Kd qualifier | String | |||
| 5 | Kd published value | Kd published value | | Float | nM | |
| 6 | Kd standard value | Kd standard value | | Float | nM |
* Activity Concentration.
Data Table (Concise)
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