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Assay Detail

CHEMBL4620355

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Binding
Inhibition of IDO1 in human HeLa cells
14
Total Activities
14
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

Synthesis of novel tryptanthrin derivatives as dual inhibitors of indoleamine 2,3-dioxygenase 1 and tryptophan 2,3-dioxygenase.
Li Y, Zhang S, Wang R, Cui M, Liu W, Yang Q, Kuang C.
Bioorg Med Chem Lett (2020) 30 : 127159 -127159
PubMed 32247733 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 14 6.44 7.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4648181 1 7.70
CHEMBL3545369 EPACADOSTAT 3.0 1 7.70
CHEMBL4645973 1 7.22
CHEMBL4644380 1 7.10
CHEMBL4645897 1 6.82
CHEMBL4643029 1 6.80
CHEMBL4635512 1 6.64
CHEMBL4643729 1 6.43
CHEMBL4646483 1 6.16
CHEMBL4644195 1 6.12
CHEMBL4633682 1 5.74
CHEMBL4646657 1 5.51
CHEMBL4647345 1 5.42
CHEMBL1969772 1 4.79

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4648181 IC50 = 20.0 nM 7.70
CHEMBL3545369 EPACADOSTAT IC50 = 20.0 nM 7.70
CHEMBL4645973 IC50 = 60.0 nM 7.22
CHEMBL4644380 IC50 = 80.0 nM 7.10
CHEMBL4645897 IC50 = 150.0 nM 6.82
CHEMBL4643029 IC50 = 160.0 nM 6.80
CHEMBL4635512 IC50 = 230.0 nM 6.64
CHEMBL4643729 IC50 = 370.0 nM 6.43
CHEMBL4646483 IC50 = 700.0 nM 6.16
CHEMBL4644195 IC50 = 750.0 nM 6.12
CHEMBL4633682 IC50 = 1840.0 nM 5.74
CHEMBL4646657 IC50 = 3100.0 nM 5.51
CHEMBL4647345 IC50 = 3760.0 nM 5.42
CHEMBL1969772 IC50 = 16300.0 nM 4.79