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Assay Detail

CHEMBL4036032

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

Binding
Inhibition of recombinant human His-tagged IDO1 expressed in Escherichia coli BL21(DE3) cells assessed as inhibition of kynurenine production using L-tryptophan as substrate after 1 hr by fluorescence assay relative to control
7
Total Activities
7
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

Identification and preliminary structure-activity relationships of 1-Indanone derivatives as novel indoleamine-2,3-dioxygenase 1 (IDO1) inhibitors.
Gao D, Li Y.
Bioorg Med Chem (2017) 25 : 3780 -3791
PubMed 28526475 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 7 4.95 5.56

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4079351 1 5.56
CHEMBL4062551 1 5.28
CHEMBL4072215 1 5.01
CHEMBL4101667 1 4.98
CHEMBL4063611 1 4.97
CHEMBL4074982 1 4.83
CHEMBL571209 INDOXIMOD 2.0 1 4.02

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4079351 IC50 = 2780.0 nM 5.56
CHEMBL4062551 IC50 = 5255.0 nM 5.28
CHEMBL4072215 IC50 = 9784.0 nM 5.01
CHEMBL4101667 IC50 = 10390.0 nM 4.98
CHEMBL4063611 IC50 = 10700.0 nM 4.97
CHEMBL4074982 IC50 = 14970.0 nM 4.83
CHEMBL571209 INDOXIMOD IC50 = 95600.0 nM 4.02