Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL5735292

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

Binding
Indoleamine-2,3-Dioxygenase 1 Inhibitory Activity: Experimental method: IDO-1 can oxidatively cleave the indole ring of tryptophan to form N-formylkynurenine. Referring to the method in the literature (Eddy W. Yue, et al. J. Med. Chem. 2009, 52, 7364-7367), 20 nM IDO-1, 2 mM D-tryptophan, 20 mM ascorbic acid, 3.5M methyl blue and 0.2 mg/mL antioxidant enzyme were sequentially added to 50 mM potassium phosphate buffer at room temperature. Due to the formation of N-formylkynurenine, the reaction rate was recorded by the increasing absorbance of the solution at 321 nm. IC50 values were calculated using Prism GraphPad software.
126
Total Activities
36
Compounds Tested
3
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

Use of aza-tryptanthrin derivatives as inhibitors of IDO1 and/or TDO
(2020)

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 42 6.63 8.26
kon 42 - -
k_off 42 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL584991 3 8.26
CHEMBL365701 6 8.26
CHEMBL5950956 3 8.26
CHEMBL5896110 3 8.26
CHEMBL187652 6 8.26
CHEMBL5977622 3 8.26
CHEMBL5856042 3 8.26
CHEMBL2347793 3 8.26
CHEMBL2347776 3 8.26
CHEMBL5880422 3 8.26
CHEMBL5824667 6 6.26
CHEMBL1098875 3 6.26
CHEMBL5985313 6 6.26
CHEMBL432537 3 6.26
CHEMBL5903836 3 6.26
CHEMBL5967303 3 6.26
CHEMBL5932991 6 6.26
CHEMBL6003894 3 6.26
CHEMBL5743808 3 6.26
CHEMBL5956469 3 6.26
CHEMBL5783618 3 6.26
CHEMBL6029347 3 6.26
CHEMBL6022429 3 6.26
CHEMBL5810711 3 6.26
CHEMBL1098826 6 6.26
CHEMBL5820407 3 6.26
CHEMBL306946 TRYPTANTHRIN 3 5.26
CHEMBL5941164 3 5.26
CHEMBL5962154 3 5.26
CHEMBL5909424 3 5.26

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5950956 IC50 = 5.5 nM 8.26
CHEMBL584991 IC50 = 5.5 nM 8.26
CHEMBL5977622 IC50 = 5.5 nM 8.26
CHEMBL2347793 IC50 = 5.5 nM 8.26
CHEMBL365701 IC50 = 5.5 nM 8.26
CHEMBL187652 IC50 = 5.5 nM 8.26
CHEMBL2347776 IC50 = 5.5 nM 8.26
CHEMBL5856042 IC50 = 5.5 nM 8.26
CHEMBL365701 IC50 = 5.5 nM 8.26
CHEMBL187652 IC50 = 5.5 nM 8.26
CHEMBL5896110 IC50 = 5.5 nM 8.26
CHEMBL5880422 IC50 = 5.5 nM 8.26
CHEMBL5820407 IC50 = 550.0 nM 6.26
CHEMBL1098826 IC50 = 550.0 nM 6.26
CHEMBL5810711 IC50 = 550.0 nM 6.26
CHEMBL5903836 IC50 = 550.0 nM 6.26
CHEMBL6029347 IC50 = 550.0 nM 6.26
CHEMBL5824667 IC50 = 550.0 nM 6.26
CHEMBL432537 IC50 = 550.0 nM 6.26
CHEMBL5932991 IC50 = 550.0 nM 6.26
CHEMBL5985313 IC50 = 550.0 nM 6.26
CHEMBL5967303 IC50 = 550.0 nM 6.26
CHEMBL6022429 IC50 = 550.0 nM 6.26
CHEMBL1098875 IC50 = 550.0 nM 6.26
CHEMBL5985313 IC50 = 550.0 nM 6.26
CHEMBL5783618 IC50 = 550.0 nM 6.26
CHEMBL5824667 IC50 = 550.0 nM 6.26
CHEMBL5743808 IC50 = 550.0 nM 6.26
CHEMBL5932991 IC50 = 550.0 nM 6.26
CHEMBL5956469 IC50 = 550.0 nM 6.26
CHEMBL1098826 IC50 = 550.0 nM 6.26
CHEMBL6003894 IC50 = 550.0 nM 6.26
CHEMBL5952261 IC50 = 5500.0 nM 5.26
CHEMBL6045556 IC50 = 5500.0 nM 5.26
CHEMBL5962154 IC50 = 5500.0 nM 5.26
CHEMBL5909424 IC50 = 5500.0 nM 5.26
CHEMBL5857619 IC50 = 5500.0 nM 5.26
CHEMBL5799295 IC50 = 5500.0 nM 5.26
CHEMBL5869900 IC50 = 5500.0 nM 5.26
CHEMBL5941164 IC50 = 5500.0 nM 5.26
CHEMBL306946 TRYPTANTHRIN IC50 = 5500.0 nM 5.26
CHEMBL5783618 k_off = - s-1 -
CHEMBL5909424 kon = - -
CHEMBL5783618 kon = - -
CHEMBL6022429 kon = - -
CHEMBL6022429 k_off = - s-1 -
CHEMBL5880422 k_off = - s-1 -
CHEMBL5896110 kon = - -
CHEMBL5880422 kon = - -
CHEMBL584991 kon = - -