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Assay Detail

CHEMBL619928

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

Binding
In vitro inhibition of 5-lipoxygenase pathway in rat basophilic leukemia (RBL-1) cells
68
Total Activities
68
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 Expert

Target

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

Publication

1,2-Dihydro-1-oxopyrrolo[3,2,1-kl]phenothiazine-2-carboxamides and congeners, dual cyclooxygenase/5-lipoxygenase inhibitors with antiinflammatory activity.
Mylari BL, Carty TJ, Moore PF, Zembrowski WJ.
J Med Chem (1990) 33 : 2019 -2024
PubMed 2113951 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 68 5.65 7.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL64404 1 7.70
CHEMBL62772 1 7.00
CHEMBL64337 1 6.52
CHEMBL64763 1 6.52
CHEMBL302879 1 6.52
CHEMBL276850 PHENOXAZINE 1 6.50
CHEMBL64051 1 6.40
CHEMBL60994 1 6.40
CHEMBL63546 1 6.30
CHEMBL64422 1 6.30
CHEMBL61952 1 6.22
CHEMBL64490 1 6.22
CHEMBL64858 1 6.16
CHEMBL304698 1 6.16
CHEMBL64064 1 6.16
CHEMBL60136 1 6.10
CHEMBL292884 1 6.10
CHEMBL62572 1 6.05
CHEMBL64370 1 6.05
CHEMBL62693 1 6.00
CHEMBL64396 1 5.96
CHEMBL62617 1 5.92
CHEMBL444828 1 5.92
CHEMBL293617 1 5.89
CHEMBL62616 1 5.89
CHEMBL60499 1 5.85
CHEMBL292324 1 5.85
CHEMBL828 PHENOTHIAZINE 2.0 1 5.85
CHEMBL61422 1 5.82
CHEMBL304205 ACRIDAN 1 5.80

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL64404 IC50 = 20.0 nM 7.70
CHEMBL62772 IC50 = 100.0 nM 7.00
CHEMBL64337 IC50 = 300.0 nM 6.52
CHEMBL64763 IC50 = 300.0 nM 6.52
CHEMBL302879 IC50 = 300.0 nM 6.52
CHEMBL276850 PHENOXAZINE IC50 = 320.0 nM 6.50
CHEMBL64051 IC50 = 400.0 nM 6.40
CHEMBL60994 IC50 = 400.0 nM 6.40
CHEMBL63546 IC50 = 500.0 nM 6.30
CHEMBL64422 IC50 = 500.0 nM 6.30
CHEMBL61952 IC50 = 600.0 nM 6.22
CHEMBL64490 IC50 = 600.0 nM 6.22
CHEMBL304698 IC50 = 700.0 nM 6.16
CHEMBL64064 IC50 = 700.0 nM 6.16
CHEMBL64858 IC50 = 700.0 nM 6.16
CHEMBL60136 IC50 = 800.0 nM 6.10
CHEMBL292884 IC50 = 800.0 nM 6.10
CHEMBL62572 IC50 = 900.0 nM 6.05
CHEMBL64370 IC50 = 900.0 nM 6.05
CHEMBL62693 IC50 = 1000.0 nM 6.00
CHEMBL64396 IC50 = 1100.0 nM 5.96
CHEMBL62617 IC50 = 1200.0 nM 5.92
CHEMBL444828 IC50 = 1200.0 nM 5.92
CHEMBL293617 IC50 = 1300.0 nM 5.89
CHEMBL62616 IC50 = 1300.0 nM 5.89
CHEMBL60499 IC50 = 1400.0 nM 5.85
CHEMBL828 PHENOTHIAZINE IC50 = 1400.0 nM 5.85
CHEMBL292324 IC50 = 1400.0 nM 5.85
CHEMBL61422 IC50 = 1500.0 nM 5.82
CHEMBL304205 ACRIDAN IC50 = 1600.0 nM 5.80
CHEMBL60790 IC50 = 1600.0 nM 5.80
CHEMBL62101 IC50 = 1600.0 nM 5.80
CHEMBL304647 IC50 = 1900.0 nM 5.72
CHEMBL418665 IC50 = 1900.0 nM 5.72
CHEMBL64738 IC50 = 1900.0 nM 5.72
CHEMBL64435 IC50 = 2100.0 nM 5.68
CHEMBL61065 IC50 = 2300.0 nM 5.64
CHEMBL64403 IC50 = 2500.0 nM 5.60
CHEMBL62916 IC50 = 2600.0 nM 5.58
CHEMBL417557 IC50 = 2700.0 nM 5.57
CHEMBL59748 IC50 = 2800.0 nM 5.55
CHEMBL64399 IC50 = 2800.0 nM 5.55
CHEMBL304663 IC50 = 3000.0 nM 5.52
CHEMBL64458 IC50 = 3000.0 nM 5.52
CHEMBL302414 IC50 = 4000.0 nM 5.40
CHEMBL304690 IC50 = 4400.0 nM 5.36
CHEMBL302394 IC50 = 5900.0 nM 5.23
CHEMBL293910 IC50 = 7200.0 nM 5.14
CHEMBL1908355 TENIDAP IC50 = 9000.0 nM 5.05
CHEMBL293858 IC50 = 9000.0 nM 5.05