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Assay Detail

CHEMBL1042997

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

Binding
Inhibition of indoleamine 2,3-dioxygenase in IFN-gamma-stimulated human HeLa cells assessed as kynurenine formation by spectrophotometry
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HeLa
Confidence 9 — Direct single protein target
Curated By Intermediate

Target

Indoleamine 2,3-dioxygenase 1 (CHEMBL4685)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of potent competitive inhibitors of indoleamine 2,3-dioxygenase with in vivo pharmacodynamic activity and efficacy in a mouse melanoma model.
Yue EW, Douty B, Wayland B, Bower M, Liu X, Leffet L, Wang Q, Bowman KJ, Hansbury MJ, Liu C, Wei M, Li Y, Wynn R, Burn TC, Koblish HK, Fridman JS, Metcalf B, Scherle PA, Combs AP.
J Med Chem (2009) 52 : 7364 -7367
PubMed 19507862 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 19 6.68 7.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL565923 1 7.92
CHEMBL565488 1 7.77
CHEMBL579014 1 7.72
CHEMBL584991 1 7.72
CHEMBL573690 1 7.27
CHEMBL565489 1 6.92
CHEMBL574139 1 6.65
CHEMBL567225 1 6.57
CHEMBL577494 1 6.31
CHEMBL568287 1 6.01
CHEMBL585186 1 6.00
CHEMBL576019 1 5.82
CHEMBL573686 1 5.62
CHEMBL577067 1 5.17
CHEMBL565924 1 -
CHEMBL584992 1 -
CHEMBL567441 1 -
CHEMBL567442 1 -
CHEMBL567317 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL565923 IC50 = 12.0 nM 7.92
CHEMBL565488 IC50 = 17.0 nM 7.77
CHEMBL579014 IC50 = 19.0 nM 7.72
CHEMBL584991 IC50 = 19.0 nM 7.72
CHEMBL573690 IC50 = 54.0 nM 7.27
CHEMBL565489 IC50 = 120.0 nM 6.92
CHEMBL574139 IC50 = 225.0 nM 6.65
CHEMBL567225 IC50 = 270.0 nM 6.57
CHEMBL577494 IC50 = 490.0 nM 6.31
CHEMBL568287 IC50 = 970.0 nM 6.01
CHEMBL585186 IC50 = 1000.0 nM 6.00
CHEMBL576019 IC50 = 1500.0 nM 5.82
CHEMBL573686 IC50 = 2400.0 nM 5.62
CHEMBL577067 IC50 = 6800.0 nM 5.17
CHEMBL565924 IC50 > 2000.0 nM -
CHEMBL584992 IC50 > 2000.0 nM -
CHEMBL567441 IC50 > 2000.0 nM -
CHEMBL567442 IC50 > 2000.0 nM -
CHEMBL567317 IC50 > 2000.0 nM -