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Assay Detail

CHEMBL972499

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Functional
Reduction of chemotaxis in human neutrophils assessed as inhibition of fMLP-OMe-induced cell migration pretreated 10 mins before fMLP-OMe challenge
22
Total Activities
22
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type Neutrophil
Confidence 1 — Organism
Curated By Autocuration

Target

Neutrophil (CHEMBL613710)
Type CELL-LINE

Publication

1-Methyl and 1-(2-hydroxyalkyl)-5-(3-alkyl/cycloalkyl/phenyl/naphthylureido)-1H-pyrazole-4-carboxylic acid ethyl esters as potent human neutrophil chemotaxis inhibitors.
Bruno O, Brullo C, Bondavalli F, Schenone S, Spisani S, Falzarano MS, Varani K, Barocelli E, Ballabeni V, Giorgio C, Tognolini M.
Bioorg Med Chem (2009) 17 : 3379 -3387
PubMed 19362486 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 22 7.93 10.33

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL160 CYCLOSPORINE 4.0 1 10.33
CHEMBL466493 1 9.72
CHEMBL507797 1 9.37
CHEMBL467717 1 8.96
CHEMBL450095 1 8.49
CHEMBL466056 1 8.11
CHEMBL468744 1 8.01
CHEMBL466698 1 7.92
CHEMBL468084 1 7.82
CHEMBL466113 1 7.75
CHEMBL512960 1 7.70
CHEMBL512980 1 7.11
CHEMBL467873 1 7.05
CHEMBL467249 1 7.00
CHEMBL505321 1 6.92
CHEMBL513307 1 6.82
CHEMBL466492 1 5.70
CHEMBL468085 1 -
CHEMBL512997 1 -
CHEMBL468536 1 -
CHEMBL468745 1 -
CHEMBL468746 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL160 CYCLOSPORINE IC50 = 0.047 nM 10.33
CHEMBL466493 IC50 = 0.19 nM 9.72
CHEMBL507797 IC50 = 0.43 nM 9.37
CHEMBL467717 IC50 = 1.1 nM 8.96
CHEMBL450095 IC50 = 3.2 nM 8.49
CHEMBL466056 IC50 = 7.8 nM 8.11
CHEMBL468744 IC50 = 9.8 nM 8.01
CHEMBL466698 IC50 = 12.0 nM 7.92
CHEMBL468084 IC50 = 15.0 nM 7.82
CHEMBL466113 IC50 = 18.0 nM 7.75
CHEMBL512960 IC50 = 20.0 nM 7.70
CHEMBL512980 IC50 = 77.0 nM 7.11
CHEMBL467873 IC50 = 90.0 nM 7.05
CHEMBL467249 IC50 = 100.0 nM 7.00
CHEMBL505321 IC50 = 120.0 nM 6.92
CHEMBL513307 IC50 = 150.0 nM 6.82
CHEMBL466492 IC50 = 2000.0 nM 5.70
CHEMBL468085 IC50 > 10.0 nM -
CHEMBL512997 IC50 > 10.0 nM -
CHEMBL468536 IC50 > 10.0 nM -
CHEMBL468745 IC50 > 10.0 nM -
CHEMBL468746 IC50 > 10.0 nM -