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Assay Detail

CHEMBL760771

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

Binding
In vitro inhibition of Prostaglandin G/H synthase pathway in rat basophilic leukemia (RBL-1) cells
ChEMBL ↗
66
Total Activities
66
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Cell Type RBL-1
Confidence 4 — Cell-line / Tissue
Curated By Autocuration

Target

Cyclooxygenase (CHEMBL2095157) ↗
Type PROTEIN FAMILY
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 66 5.75 8.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1908355 TENIDAP 2.0 1 8.00
CHEMBL61422 — — 1 7.70
CHEMBL292324 — — 1 7.16
CHEMBL64370 — — 1 7.00
CHEMBL293617 — — 1 6.70
CHEMBL62772 — — 1 6.70
CHEMBL62101 — — 1 6.70
CHEMBL64858 — — 1 6.70
CHEMBL276850 PHENOXAZINE — 1 6.46
CHEMBL62693 — — 1 6.40
CHEMBL62616 — — 1 6.32
CHEMBL61952 — — 1 6.30
CHEMBL302879 — — 1 6.30
CHEMBL64337 — — 1 6.30
CHEMBL64763 — — 1 6.16
CHEMBL62572 — — 1 6.16
CHEMBL302838 — — 1 6.16
CHEMBL60136 — — 1 6.16
CHEMBL418665 — — 1 6.16
CHEMBL64396 — — 1 6.10
CHEMBL63546 — — 1 6.10
CHEMBL64435 — — 1 6.10
CHEMBL60994 — — 1 6.10
CHEMBL828 PHENOTHIAZINE 2.0 1 6.03
CHEMBL304690 — — 1 6.00
CHEMBL62916 — — 1 5.92
CHEMBL64490 — — 1 5.82
CHEMBL304205 ACRIDAN — 1 5.72
CHEMBL436352 — — 1 5.70
CHEMBL64738 — — 1 5.66

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1908355 TENIDAP IC50 = 10.0 nM 8.00
CHEMBL61422 — IC50 = 20.0 nM 7.70
CHEMBL292324 — IC50 = 70.0 nM 7.16
CHEMBL64370 — IC50 = 100.0 nM 7.00
CHEMBL293617 — IC50 = 200.0 nM 6.70
CHEMBL62772 — IC50 = 200.0 nM 6.70
CHEMBL62101 — IC50 = 200.0 nM 6.70
CHEMBL64858 — IC50 = 200.0 nM 6.70
CHEMBL276850 PHENOXAZINE IC50 = 350.0 nM 6.46
CHEMBL62693 — IC50 = 400.0 nM 6.40
CHEMBL62616 — IC50 = 480.0 nM 6.32
CHEMBL61952 — IC50 = 500.0 nM 6.30
CHEMBL302879 — IC50 = 500.0 nM 6.30
CHEMBL64337 — IC50 = 500.0 nM 6.30
CHEMBL418665 — IC50 = 700.0 nM 6.16
CHEMBL64763 — IC50 = 700.0 nM 6.16
CHEMBL302838 — IC50 = 700.0 nM 6.16
CHEMBL60136 — IC50 = 700.0 nM 6.16
CHEMBL62572 — IC50 = 700.0 nM 6.16
CHEMBL64396 — IC50 = 800.0 nM 6.10
CHEMBL63546 — IC50 = 800.0 nM 6.10
CHEMBL64435 — IC50 = 800.0 nM 6.10
CHEMBL60994 — IC50 = 800.0 nM 6.10
CHEMBL828 PHENOTHIAZINE IC50 = 940.0 nM 6.03
CHEMBL304690 — IC50 = 1000.0 nM 6.00
CHEMBL62916 — IC50 = 1200.0 nM 5.92
CHEMBL64490 — IC50 = 1500.0 nM 5.82
CHEMBL304205 ACRIDAN IC50 = 1900.0 nM 5.72
CHEMBL436352 — IC50 = 2000.0 nM 5.70
CHEMBL64738 — IC50 = 2200.0 nM 5.66
CHEMBL62617 — IC50 = 2400.0 nM 5.62
CHEMBL64403 — IC50 = 2400.0 nM 5.62
CHEMBL60790 — IC50 = 2600.0 nM 5.58
CHEMBL304698 — IC50 = 2800.0 nM 5.55
CHEMBL64399 — IC50 = 2900.0 nM 5.54
CHEMBL304647 — IC50 = 3300.0 nM 5.48
CHEMBL60993 — IC50 = 3400.0 nM 5.47
CHEMBL60499 — IC50 = 3500.0 nM 5.46
CHEMBL61065 — IC50 = 3600.0 nM 5.44
CHEMBL64064 — IC50 = 3900.0 nM 5.41
CHEMBL59756 — IC50 = 5000.0 nM 5.30
CHEMBL64458 — IC50 = 5000.0 nM 5.30
CHEMBL64422 — IC50 = 5100.0 nM 5.29
CHEMBL418514 — IC50 = 5400.0 nM 5.27
CHEMBL292884 — IC50 = 5700.0 nM 5.24
CHEMBL64076 — IC50 = 5700.0 nM 5.24
CHEMBL60165 — IC50 = 6200.0 nM 5.21
CHEMBL444828 — IC50 = 6400.0 nM 5.19
CHEMBL417557 — IC50 = 6900.0 nM 5.16
CHEMBL59748 — IC50 = 7200.0 nM 5.14