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Assay Detail

CHEMBL701322

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

Functional
The drug dependent inhibition of LTB4 biosynthesis in human whole blood (HWB) activated with the ionophore A-23187
31
Total Activities
29
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Tissue Blood
Confidence 1 — Organism
Curated By Expert

Target

Homo sapiens (CHEMBL372)
Type ORGANISM
Organism Homo sapiens

Publication

Substituted indoles as potent and orally active 5-lipoxygenase activating protein (FLAP) inhibitors.
Frenette R, Hutchinson JH, Léger S, Thérien M, Brideau C, Chan CC, Charleson S, Ethier D, Guay J, Jones TR, McAuliffe M, Piechuta H, Riendeau D, Tagari P, Girard Y.
Bioorg Med Chem Lett (1999) 9 : 2391 -2396
PubMed 10476875 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 31 6.32 6.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL82760 1 6.89
CHEMBL38958 1 6.89
CHEMBL38545 1 6.58
CHEMBL80696 1 6.57
CHEMBL289751 1 6.57
CHEMBL2114162 1 6.55
CHEMBL78938 3 6.44
CHEMBL79383 1 6.40
CHEMBL39617 1 6.39
CHEMBL3350287 1 6.33
CHEMBL16596 QUIFLAPON 2.0 1 6.30
CHEMBL311968 1 6.17
CHEMBL78013 1 6.06
CHEMBL433133 1 6.01
CHEMBL78854 1 5.60
CHEMBL78201 1 5.54
CHEMBL310384 1 -
CHEMBL40073 1 -
CHEMBL81904 1 -
CHEMBL78789 1 -
CHEMBL80287 1 -
CHEMBL39473 1 -
CHEMBL80726 1 -
CHEMBL79881 1 -
CHEMBL80802 1 -
CHEMBL80158 1 -
CHEMBL80512 1 -
CHEMBL310276 1 -
CHEMBL310055 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL82760 IC50 = 130.0 nM 6.89
CHEMBL38958 IC50 = 130.0 nM 6.89
CHEMBL38545 IC50 = 260.0 nM 6.58
CHEMBL80696 IC50 = 270.0 nM 6.57
CHEMBL289751 IC50 = 270.0 nM 6.57
CHEMBL2114162 IC50 = 280.0 nM 6.55
CHEMBL78938 IC50 = 362.0 nM 6.44
CHEMBL79383 IC50 = 400.0 nM 6.40
CHEMBL39617 IC50 = 410.0 nM 6.39
CHEMBL3350287 IC50 = 470.0 nM 6.33
CHEMBL16596 QUIFLAPON IC50 = 500.0 nM 6.30
CHEMBL311968 IC50 = 670.0 nM 6.17
CHEMBL78938 IC50 = 803.0 nM 6.09
CHEMBL78013 IC50 = 880.0 nM 6.06
CHEMBL433133 IC50 = 980.0 nM 6.01
CHEMBL78854 IC50 = 2500.0 nM 5.60
CHEMBL78201 IC50 = 2890.0 nM 5.54
CHEMBL80726 IC50 > 3000.0 nM -
CHEMBL40073 IC50 > 3000.0 nM -
CHEMBL81904 IC50 > 3000.0 nM -
CHEMBL78789 IC50 > 3000.0 nM -
CHEMBL80287 IC50 > 3000.0 nM -
CHEMBL78938 IC50 > 3000.0 nM -
CHEMBL39473 IC50 > 3000.0 nM -
CHEMBL79881 IC50 > 3000.0 nM -
CHEMBL310384 IC50 > 3000.0 nM -
CHEMBL80802 IC50 > 3000.0 nM -
CHEMBL80158 IC50 > 3000.0 nM -
CHEMBL80512 IC50 > 3000.0 nM -
CHEMBL310276 IC50 > 3000.0 nM -
CHEMBL310055 IC50 > 3000.0 nM -