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BioAssay: AID 630824

Inhibition of CYP3A4

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
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 Tested Compounds
 Tested Compounds
All(2)
 
 
Unspecified(2)
 
 
 Tested Substances
 Tested Substances
All(2)
 
 
Unspecified(2)
 
 
 Related BioAssays
 Related BioAssays
AID: 630824
Data Source: ChEMBL (788272)
BioAssay Type: Confirmatory, Concentration-Response Relationship Observed
Depositor Category: Literature, Extracted
BioAssay Version:
Deposit Date: 2012-09-09
Modify Date: 2014-05-24

Data Table ( Complete ):           All
Tested Compounds:
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)
Comment
Putative Target:

ChEMBL Target ID: 17045
Target Type: SINGLE PROTEIN
Pref Name: Cytochrome P450 3A4
Synonyms: 1;8-cineole 2-exo-monooxygenase;Albendazole monooxygenase;Albendazole sulfoxidase;CYPIIIA3;CYPIIIA4;Cytochrome P450 3A3;Cytochrome P450 3A4;Cytochrome P450 HLp;Cytochrome P450 NF-25;Cytochrome P450-PCN1;Nifedipine oxidase;Quinine 3-monooxygenase;Taurochenodeoxycholate 6-alpha-hydroxylase;
Gene Name: CYP3A3;CYP3A4;
Protein Accession: P08684;
Protein GI: 116241312;
Organism: Homo sapiens
Tax ID: 9606
Target Classification: enzyme cytochrome p450 cyp_3 cyp_3a cyp_3a4
Confidence: Homologous single protein target assigned
Relationship Type: Homologous protein target assigned
Categorized Comment
Assay Type: ADME

Assay Data Source: Scientific Literature

BAO: Assay Format: biochemical format

Result Definitions
TIDNameDescriptionHistogramTypeUnit
OutcomeThe BioAssay activity outcomeOutcome
1IC50*IC50 PubChem standard valueFloatμM
2IC50 activity commentIC50 activity commentString
3IC50 standard flagIC50 standard flagInteger
4IC50 qualifierIC50 qualifierString
5IC50 published valueIC50 published valueFloat
6IC50 standard valueIC50 standard valueFloatnM

* Activity Concentration.

Data Table (Concise)
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