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Assay Detail

CHEMBL4628286

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

Binding
Inhibition of IDO1 (unknown origin) assessed as reduction in kynurenine formation using L-tryptophan as substrate incubated for 60 mins by fluorescence based assay
20
Total Activities
20
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 novel hydroxyamidine derivatives as indoleamine 2,3-dioxygenase 1 inhibitors with in vivo anti-tumor efficacy.
Liu C, Nan Y, Xia Z, Gu K, Chen C, Dong X, Ju D, Zhao W.
Bioorg Med Chem Lett (2020) 30 : 127038 -127038
PubMed 32088128 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 20 6.86 7.18

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3545369 EPACADOSTAT 3.0 1 7.18
CHEMBL4641167 1 7.16
CHEMBL4644903 1 7.15
CHEMBL4637369 1 7.06
CHEMBL4644666 1 7.02
CHEMBL4642406 1 7.01
CHEMBL4645599 1 7.00
CHEMBL4645780 1 6.98
CHEMBL4639397 1 6.97
CHEMBL4639448 1 6.90
CHEMBL4645531 1 6.90
CHEMBL4633901 1 6.87
CHEMBL4643034 1 6.85
CHEMBL4633995 1 6.72
CHEMBL4639516 1 6.68
CHEMBL4648971 1 6.67
CHEMBL4646789 1 6.66
CHEMBL4646976 1 6.66
CHEMBL4646028 1 6.51
CHEMBL4635808 1 6.21

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3545369 EPACADOSTAT IC50 = 66.0 nM 7.18
CHEMBL4641167 IC50 = 69.0 nM 7.16
CHEMBL4644903 IC50 = 71.0 nM 7.15
CHEMBL4637369 IC50 = 87.0 nM 7.06
CHEMBL4644666 IC50 = 95.0 nM 7.02
CHEMBL4642406 IC50 = 97.0 nM 7.01
CHEMBL4645599 IC50 = 99.0 nM 7.00
CHEMBL4645780 IC50 = 105.0 nM 6.98
CHEMBL4639397 IC50 = 108.0 nM 6.97
CHEMBL4639448 IC50 = 126.0 nM 6.90
CHEMBL4645531 IC50 = 126.0 nM 6.90
CHEMBL4633901 IC50 = 135.0 nM 6.87
CHEMBL4643034 IC50 = 140.0 nM 6.85
CHEMBL4633995 IC50 = 191.0 nM 6.72
CHEMBL4639516 IC50 = 208.0 nM 6.68
CHEMBL4648971 IC50 = 212.0 nM 6.67
CHEMBL4646789 IC50 = 218.0 nM 6.66
CHEMBL4646976 IC50 = 218.0 nM 6.66
CHEMBL4646028 IC50 = 312.0 nM 6.51
CHEMBL4635808 IC50 = 609.0 nM 6.21