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Assay Detail

CHEMBL929668

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

Functional
Inhibition of calcium ionophore-stimulated LTB4 production in human PMN cells
39
Total Activities
39
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type PMN
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Substituted 2,2-bisaryl-bicycloheptanes as novel and potent inhibitors of 5-lipoxygenase activating protein.
Macdonald D, Brideau C, Chan CC, Falgueyret JP, Frenette R, Guay J, Hutchinson JH, Perrier H, Prasit P, Riendeau D, Tagari P, Thérien M, Young RN, Girard Y.
Bioorg Med Chem Lett (2008) 18 : 2023 -2027
PubMed 18276139 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 39 7.87 8.77

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL255013 1 8.77
CHEMBL558778 1 8.74
CHEMBL255228 1 8.74
CHEMBL401667 1 8.70
CHEMBL401597 1 8.66
CHEMBL254564 1 8.59
CHEMBL541915 1 8.52
CHEMBL16596 QUIFLAPON 2.0 1 8.51
CHEMBL403980 1 8.41
CHEMBL255227 1 8.39
CHEMBL254547 1 8.38
CHEMBL404275 1 8.30
CHEMBL404266 1 8.30
CHEMBL256765 1 8.23
CHEMBL404016 1 8.21
CHEMBL402024 1 8.15
CHEMBL254747 1 8.15
CHEMBL256975 1 8.10
CHEMBL438166 1 8.06
CHEMBL256976 1 8.05
CHEMBL401699 1 8.02
CHEMBL404015 1 7.99
CHEMBL256766 1 7.80
CHEMBL258432 1 7.72
CHEMBL415093 1 7.62
CHEMBL403199 1 7.38
CHEMBL401668 1 7.36
CHEMBL255011 1 7.33
CHEMBL258213 1 7.22
CHEMBL257621 1 7.10

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL255013 IC50 = 1.7 nM 8.77
CHEMBL558778 IC50 = 1.8 nM 8.74
CHEMBL255228 IC50 = 1.8 nM 8.74
CHEMBL401667 IC50 = 2.0 nM 8.70
CHEMBL401597 IC50 = 2.2 nM 8.66
CHEMBL254564 IC50 = 2.6 nM 8.59
CHEMBL541915 IC50 = 3.0 nM 8.52
CHEMBL16596 QUIFLAPON IC50 = 3.1 nM 8.51
CHEMBL403980 IC50 = 3.9 nM 8.41
CHEMBL255227 IC50 = 4.1 nM 8.39
CHEMBL254547 IC50 = 4.2 nM 8.38
CHEMBL404275 IC50 = 5.0 nM 8.30
CHEMBL404266 IC50 = 5.0 nM 8.30
CHEMBL256765 IC50 = 5.9 nM 8.23
CHEMBL404016 IC50 = 6.1 nM 8.21
CHEMBL402024 IC50 = 7.0 nM 8.15
CHEMBL254747 IC50 = 7.0 nM 8.15
CHEMBL256975 IC50 = 8.0 nM 8.10
CHEMBL438166 IC50 = 8.7 nM 8.06
CHEMBL256976 IC50 = 9.0 nM 8.05
CHEMBL401699 IC50 = 9.5 nM 8.02
CHEMBL404015 IC50 = 10.2 nM 7.99
CHEMBL256766 IC50 = 16.0 nM 7.80
CHEMBL258432 IC50 = 19.0 nM 7.72
CHEMBL415093 IC50 = 24.0 nM 7.62
CHEMBL403199 IC50 = 42.0 nM 7.38
CHEMBL401668 IC50 = 44.0 nM 7.36
CHEMBL255011 IC50 = 47.0 nM 7.33
CHEMBL258213 IC50 = 60.0 nM 7.22
CHEMBL257621 IC50 = 80.0 nM 7.10
CHEMBL255012 IC50 = 152.0 nM 6.82
CHEMBL258215 IC50 = 169.0 nM 6.77
CHEMBL258214 IC50 = 186.0 nM 6.73
CHEMBL430038 IC50 = 217.0 nM 6.66
CHEMBL404267 IC50 = 282.0 nM 6.55
CHEMBL258431 IC50 = 418.0 nM 6.38
CHEMBL255010 IC50 > 2372.0 nM -
CHEMBL257797 IC50 > 1800.0 nM -
CHEMBL404276 IC50 < 1.3 nM -