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Assay Detail

CHEMBL4628287

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

Binding
Inhibition of IDO1 in IFN-gamma stimulated human HeLa cells assessed as reduction in kynurenine formation using L-tryptophan as substrate incubated for 24 hrs by UV-spectrophotometry
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HeLa
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
EC50 20 7.28 8.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3545369 EPACADOSTAT 3.0 1 8.10
CHEMBL4644903 1 7.96
CHEMBL4639448 1 7.82
CHEMBL4645780 1 7.77
CHEMBL4642406 1 7.70
CHEMBL4637369 1 7.57
CHEMBL4646789 1 7.48
CHEMBL4644666 1 7.39
CHEMBL4639516 1 7.28
CHEMBL4645599 1 7.23
CHEMBL4641167 1 7.14
CHEMBL4648971 1 7.10
CHEMBL4646976 1 7.00
CHEMBL4633995 1 6.84
CHEMBL4643034 1 6.57
CHEMBL4646028 1 6.57
CHEMBL4639397 1 6.25
CHEMBL4635808 1 -
CHEMBL4633901 1 -
CHEMBL4645531 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3545369 EPACADOSTAT EC50 = 8.0 nM 8.10
CHEMBL4644903 EC50 = 11.0 nM 7.96
CHEMBL4639448 EC50 = 15.0 nM 7.82
CHEMBL4645780 EC50 = 17.0 nM 7.77
CHEMBL4642406 EC50 = 20.0 nM 7.70
CHEMBL4637369 EC50 = 27.0 nM 7.57
CHEMBL4646789 EC50 = 33.0 nM 7.48
CHEMBL4644666 EC50 = 41.0 nM 7.39
CHEMBL4639516 EC50 = 53.0 nM 7.28
CHEMBL4645599 EC50 = 59.0 nM 7.23
CHEMBL4641167 EC50 = 73.0 nM 7.14
CHEMBL4648971 EC50 = 79.0 nM 7.10
CHEMBL4646976 EC50 = 101.0 nM 7.00
CHEMBL4633995 EC50 = 143.0 nM 6.84
CHEMBL4643034 EC50 = 268.0 nM 6.57
CHEMBL4646028 EC50 = 268.0 nM 6.57
CHEMBL4639397 EC50 = 556.0 nM 6.25
CHEMBL4635808 EC50 > 800.0 nM -
CHEMBL4633901 EC50 > 800.0 nM -
CHEMBL4645531 EC50 > 800.0 nM -