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Assay Detail

CHEMBL3999984

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

Binding
Inhibition of human N-terminal His-tagged IDO1 expressed in Escherichia coli using D-Trp as substrate
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

INCB24360 (Epacadostat), a Highly Potent and Selective Indoleamine-2,3-dioxygenase 1 (IDO1) Inhibitor for Immuno-oncology.
Yue EW, Sparks R, Polam P, Modi D, Douty B, Wayland B, Glass B, Takvorian A, Glenn J, Zhu W, Bower M, Liu X, Leffet L, Wang Q, Bowman KJ, Hansbury MJ, Wei M, Li Y, Wynn R, Burn TC, Koblish HK, Fridman JS, Emm T, Scherle PA, Metcalf B, Combs AP.
ACS Med Chem Lett (2017) 8 : 486 -491
PubMed 28523098 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 13 6.88 7.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL565923 1 7.30
CHEMBL3545369 EPACADOSTAT 3.0 1 7.14
CHEMBL584991 1 7.12
CHEMBL3955791 1 7.00
CHEMBL4076756 1 7.00
CHEMBL3979473 1 6.92
CHEMBL4072733 1 6.77
CHEMBL4085426 1 6.75
CHEMBL4091895 1 6.70
CHEMBL4083203 1 6.68
CHEMBL4064144 1 6.64
CHEMBL4099627 1 6.54
CHEMBL4063847 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL565923 IC50 = 50.0 nM 7.30
CHEMBL3545369 EPACADOSTAT IC50 = 73.0 nM 7.14
CHEMBL584991 IC50 = 75.0 nM 7.12
CHEMBL3955791 IC50 = 100.0 nM 7.00
CHEMBL4076756 IC50 = 100.0 nM 7.00
CHEMBL3979473 IC50 = 120.0 nM 6.92
CHEMBL4072733 IC50 = 170.0 nM 6.77
CHEMBL4085426 IC50 = 180.0 nM 6.75
CHEMBL4091895 IC50 = 200.0 nM 6.70
CHEMBL4083203 IC50 = 210.0 nM 6.68
CHEMBL4064144 IC50 = 230.0 nM 6.64
CHEMBL4099627 IC50 = 290.0 nM 6.54
CHEMBL4063847 IC50 > 5000.0 nM -