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Assay Detail

CHEMBL618066

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

Binding
Inhibition 5-lipoxygenase mediated LTB4 formation in rat basophilic leukemia (RBL-1) cells
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Cell Type RBL-1
Confidence 9 — Direct single protein target
Curated By Expert

Target

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

Publication

1,3,4-Oxadiazole, 1,3,4-thiadiazole, and 1,2,4-triazole analogs of the fenamates: in vitro inhibition of cyclooxygenase and 5-lipoxygenase activities.
Boschelli DH, Connor DT, Bornemeier DA, Dyer RD, Kennedy JA, Kuipers PJ, Okonkwo GC, Schrier DJ, Wright CD.
J Med Chem (1993) 36 : 1802 -1810
PubMed 8515419 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 14 5.86 6.54

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL53532 1 6.54
CHEMBL300637 1 6.17
CHEMBL301136 1 6.16
CHEMBL297733 1 6.16
CHEMBL54156 1 6.13
CHEMBL298672 1 6.11
CHEMBL299794 1 6.06
CHEMBL53610 1 6.05
CHEMBL50833 1 6.00
CHEMBL417022 1 5.85
CHEMBL53805 1 5.77
CHEMBL301990 1 5.52
CHEMBL298776 1 4.92
CHEMBL509 MECLOFENAMIC ACID 4.0 1 4.62

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL53532 IC50 = 290.0 nM 6.54
CHEMBL300637 IC50 = 680.0 nM 6.17
CHEMBL301136 IC50 = 690.0 nM 6.16
CHEMBL297733 IC50 = 690.0 nM 6.16
CHEMBL54156 IC50 = 740.0 nM 6.13
CHEMBL298672 IC50 = 770.0 nM 6.11
CHEMBL299794 IC50 = 870.0 nM 6.06
CHEMBL53610 IC50 = 890.0 nM 6.05
CHEMBL50833 IC50 = 1000.0 nM 6.00
CHEMBL417022 IC50 = 1400.0 nM 5.85
CHEMBL53805 IC50 = 1700.0 nM 5.77
CHEMBL301990 IC50 = 3000.0 nM 5.52
CHEMBL298776 IC50 = 12000.0 nM 4.92
CHEMBL509 MECLOFENAMIC ACID IC50 = 24000.0 nM 4.62