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Assay Detail

CHEMBL5057987

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

Binding
Inhibition of IDO1 in IFNgamma-stimulated human HeLa cells assessed as reduction in kynurenine formation measured after 48 hrs by spectrophotometry
24
Total Activities
24
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 Autocuration

Target

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

Publication

Discovery of the First Potent IDO1/IDO2 Dual Inhibitors: A Promising Strategy for Cancer Immunotherapy.
He X, He G, Chu Z, Wu H, Wang J, Ge Y, Shen H, Zhang S, Shan J, Peng K, Wei Z, Zou Y, Xu Y, Zhu Q.
J Med Chem (2021) 64 : 17950 -17968
PubMed 34854662 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 24 8.05 8.67

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5091825 1 8.67
CHEMBL5094068 1 8.20
CHEMBL5093631 1 7.87
CHEMBL3545369 EPACADOSTAT 3.0 1 7.45
CHEMBL5092513 1 -
CHEMBL5092138 1 -
CHEMBL5091241 1 -
CHEMBL5084767 1 -
CHEMBL5079469 1 -
CHEMBL5087615 1 -
CHEMBL5091287 1 -
CHEMBL5076683 1 -
CHEMBL5070154 1 -
CHEMBL5078101 1 -
CHEMBL5093816 1 -
CHEMBL5078912 1 -
CHEMBL5085580 1 -
CHEMBL5091590 1 -
CHEMBL5090441 1 -
CHEMBL5084150 1 -
CHEMBL5082481 1 -
CHEMBL5091415 1 -
CHEMBL5091243 1 -
CHEMBL5088729 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5091825 IC50 = 2.16 nM 8.67
CHEMBL5094068 IC50 = 6.3 nM 8.20
CHEMBL5093631 IC50 = 13.61 nM 7.87
CHEMBL3545369 EPACADOSTAT IC50 = 35.76 nM 7.45
CHEMBL5092513 IC50 - -
CHEMBL5092138 IC50 - -
CHEMBL5091241 IC50 - -
CHEMBL5084767 IC50 - -
CHEMBL5079469 IC50 - -
CHEMBL5087615 IC50 - -
CHEMBL5091287 IC50 - -
CHEMBL5076683 IC50 - -
CHEMBL5070154 IC50 - -
CHEMBL5078101 IC50 - -
CHEMBL5093816 IC50 - -
CHEMBL5078912 IC50 - -
CHEMBL5085580 IC50 - -
CHEMBL5091590 IC50 - -
CHEMBL5090441 IC50 - -
CHEMBL5084150 IC50 - -
CHEMBL5082481 IC50 - -
CHEMBL5091415 IC50 - -
CHEMBL5091243 IC50 - -
CHEMBL5088729 IC50 - -