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Assay Detail

CHEMBL972500

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 IL8-induced cell migration pretreated 10 mins before IL8 challenge
25
Total Activities
25
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 25 8.71 10.26

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL513307 1 10.26
CHEMBL467717 1 10.05
CHEMBL468536 1 9.70
CHEMBL466493 1 9.44
CHEMBL512960 1 9.00
CHEMBL466113 1 8.89
CHEMBL450095 1 8.72
CHEMBL466698 1 8.02
CHEMBL226836 1 8.00
CHEMBL226887 1 7.85
CHEMBL226939 1 7.35
CHEMBL450013 1 7.26
CHEMBL467249 1 -
CHEMBL512997 1 -
CHEMBL468084 1 -
CHEMBL468744 1 -
CHEMBL467873 1 -
CHEMBL468085 1 -
CHEMBL507797 1 -
CHEMBL505321 1 -
CHEMBL468746 1 -
CHEMBL512980 1 -
CHEMBL466492 1 -
CHEMBL466056 1 -
CHEMBL468745 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL513307 IC50 = 0.0546 nM 10.26
CHEMBL467717 IC50 = 0.09 nM 10.05
CHEMBL468536 IC50 = 0.2 nM 9.70
CHEMBL466493 IC50 = 0.36 nM 9.44
CHEMBL512960 IC50 = 1.0 nM 9.00
CHEMBL466113 IC50 = 1.3 nM 8.89
CHEMBL450095 IC50 = 1.9 nM 8.72
CHEMBL466698 IC50 = 9.6 nM 8.02
CHEMBL226836 IC50 = 10.0 nM 8.00
CHEMBL226887 IC50 = 14.0 nM 7.85
CHEMBL226939 IC50 = 45.0 nM 7.35
CHEMBL450013 IC50 = 55.0 nM 7.26
CHEMBL467249 IC50 = 0.00055 nM -
CHEMBL512997 IC50 = 0.0007 nM -
CHEMBL468084 IC50 = 0.00054 nM -
CHEMBL468744 IC50 = 0.00097 nM -
CHEMBL467873 IC50 = 0.00082 nM -
CHEMBL468085 IC50 = 0.00099 nM -
CHEMBL507797 IC50 = 0.0032 nM -
CHEMBL505321 IC50 = 0.0016 nM -
CHEMBL468746 IC50 = 0.0074 nM -
CHEMBL512980 IC50 = 0.0018 nM -
CHEMBL466492 IC50 = 8e-05 nM -
CHEMBL466056 IC50 = 0.0076 nM -
CHEMBL468745 IC50 = 0.0042 nM -