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Assay Detail

CHEMBL5033658

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Binding
Inhibition of IDO1 in human HeLa cells
10
Total Activities
10
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 IDO1 inhibitors targeting the protein's apo form through scaffold hopping from holo-IDO1 inhibitor.
Wu Y, Duan Q, Zou Y, Zhu Q, Xu Y.
Bioorg Med Chem Lett (2021) 52 : 128373 -128373
PubMed 34560264 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 10 6.18 8.38

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4777480 1 8.38
CHEMBL5089251 1 6.36
CHEMBL5090258 1 6.36
CHEMBL5085169 1 6.12
CHEMBL5075270 1 6.07
CHEMBL5079654 1 5.87
CHEMBL5084116 1 5.87
CHEMBL5087424 1 5.68
CHEMBL5077922 1 5.58
CHEMBL5088387 1 5.51

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4777480 IC50 = 4.2 nM 8.38
CHEMBL5089251 IC50 = 440.0 nM 6.36
CHEMBL5090258 IC50 = 440.0 nM 6.36
CHEMBL5085169 IC50 = 760.0 nM 6.12
CHEMBL5075270 IC50 = 860.0 nM 6.07
CHEMBL5079654 IC50 = 1340.0 nM 5.87
CHEMBL5084116 IC50 = 1340.0 nM 5.87
CHEMBL5087424 IC50 = 2090.0 nM 5.68
CHEMBL5077922 IC50 = 2610.0 nM 5.58
CHEMBL5088387 IC50 = 3110.0 nM 5.51