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Assay Detail

CHEMBL4408555

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

Binding
Inhibition of recombinant N-terminal His-tagged human IDO1 expressed in Escherichia coli assessed as reduction in N-formylkynurenine formation using L-tryptophan as substrate
14
Total Activities
14
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

Discovery of phosphonamidate IDO1 inhibitors for the treatment of non-small cell lung cancer.
Du Q, Feng X, Wang Y, Xu X, Zhang Y, Qu X, Li Z, Bian J.
Eur J Med Chem (2019) 182 : 111629 -111629
PubMed 31445231 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 14 6.97 7.14

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3545369 EPACADOSTAT 3.0 1 7.14
CHEMBL4472697 1 7.11
CHEMBL4454093 1 7.00
CHEMBL4455008 1 7.00
CHEMBL4552082 1 6.99
CHEMBL4514196 1 6.98
CHEMBL4581189 1 6.96
CHEMBL4567170 1 6.94
CHEMBL4552649 1 6.94
CHEMBL4436582 1 6.92
CHEMBL4514159 1 6.92
CHEMBL4444787 1 6.92
CHEMBL4455785 1 6.92
CHEMBL4460529 1 6.89

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3545369 EPACADOSTAT IC50 = 72.0 nM 7.14
CHEMBL4472697 IC50 = 78.0 nM 7.11
CHEMBL4454093 IC50 = 99.0 nM 7.00
CHEMBL4455008 IC50 = 101.0 nM 7.00
CHEMBL4552082 IC50 = 102.0 nM 6.99
CHEMBL4514196 IC50 = 104.0 nM 6.98
CHEMBL4581189 IC50 = 109.0 nM 6.96
CHEMBL4567170 IC50 = 115.0 nM 6.94
CHEMBL4552649 IC50 = 114.0 nM 6.94
CHEMBL4436582 IC50 = 121.0 nM 6.92
CHEMBL4514159 IC50 = 120.0 nM 6.92
CHEMBL4444787 IC50 = 120.0 nM 6.92
CHEMBL4455785 IC50 = 121.0 nM 6.92
CHEMBL4460529 IC50 = 130.0 nM 6.89