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Assay Detail

CHEMBL4684571

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

Binding
Inhibition of human IDO1 expressed in HEK293T cells assessed as reduction in N-formylkynurenine production incubated for 12 hrs by microplate reader analysis
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK293T
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Design, synthesis, and biological evaluation of 1,2,5-oxadiazole-3-carboximidamide derivatives as novel indoleamine-2,3-dioxygenase 1 inhibitors.
Song X,Sun P,Wang J,Guo W,Wang Y,Meng LH,Liu H
Eur J Med Chem (2020) 189 : 112059 -112059
PubMed 31981851 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 15 7.13 8.02

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3545369 EPACADOSTAT 3.0 1 8.02
CHEMBL4783332 1 7.70
CHEMBL4746161 1 7.37
CHEMBL4740235 1 7.37
CHEMBL4749003 1 7.30
CHEMBL4761345 1 7.24
CHEMBL4745884 1 7.16
CHEMBL4779669 1 6.90
CHEMBL4778450 1 6.86
CHEMBL4740111 1 6.81
CHEMBL4750297 1 6.75
CHEMBL4750230 1 6.73
CHEMBL4792825 1 6.48
CHEMBL4777641 1 -
CHEMBL4746720 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3545369 EPACADOSTAT IC50 = 9.63 nM 8.02
CHEMBL4783332 IC50 = 19.88 nM 7.70
CHEMBL4746161 IC50 = 42.58 nM 7.37
CHEMBL4740235 IC50 = 42.99 nM 7.37
CHEMBL4749003 IC50 = 49.83 nM 7.30
CHEMBL4761345 IC50 = 57.76 nM 7.24
CHEMBL4745884 IC50 = 68.59 nM 7.16
CHEMBL4779669 IC50 = 125.44 nM 6.90
CHEMBL4778450 IC50 = 137.95 nM 6.86
CHEMBL4740111 IC50 = 153.75 nM 6.81
CHEMBL4750297 IC50 = 177.35 nM 6.75
CHEMBL4750230 IC50 = 186.2 nM 6.73
CHEMBL4792825 IC50 = 333.65 nM 6.48
CHEMBL4777641 IC50 > 1000.0 nM -
CHEMBL4746720 IC50 > 1000.0 nM -