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Assay Detail

CHEMBL619241

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

Binding
Tested for inhibition of 5-Lipoxygenase (ARBL) in calcium-stimulated rat basophilic leukemia cells(RBL-1)
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Cell Type RBL-1
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

Polyunsaturated fatty acid 5-lipoxygenase (CHEMBL312)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Synthesis of reversed hydroxamic acids of indomethacin: dual inhibitors of cyclooxygenase and 5-lipoxygenase
Kramer JB, Boschelli DH, Connor DT, Kostlan CR, Flynn DL, Dyer RD, Bornemeier DA, Kennedy JA, Wright CD, Kuipers PJ
Bioorg Med Chem Lett (1992) 2 : 1655 -1660
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 8 6.00 6.47

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL42593 1 6.47
CHEMBL295243 1 6.40
CHEMBL295008 1 6.24
CHEMBL296543 1 6.08
CHEMBL410500 1 5.85
CHEMBL46871 1 5.85
CHEMBL295829 OXAMETACIN 2.0 1 5.12
CHEMBL6 INDOMETHACIN 4.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL42593 IC50 = 340.0 nM 6.47
CHEMBL295243 IC50 = 400.0 nM 6.40
CHEMBL295008 IC50 = 570.0 nM 6.24
CHEMBL296543 IC50 = 830.0 nM 6.08
CHEMBL410500 IC50 = 1400.0 nM 5.85
CHEMBL46871 IC50 = 1400.0 nM 5.85
CHEMBL295829 OXAMETACIN IC50 = 7500.0 nM 5.12
CHEMBL6 INDOMETHACIN IC50 > 100000.0 nM -