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Assay Detail

CHEMBL5617583

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

Binding
Inhibition of human TDO transfected in HEK293T cells using L-tryptophan as substrate incubated for 24 hrs by absorbance based microplate analysis
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK293T
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Tryptophan 2,3-dioxygenase (CHEMBL2140)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery, synthesis and biological evaluation of novel isoquinoline derivatives as potent indoleamine 2, 3-dioxygenase 1 and tryptophan 2, 3-dioxygenase dual inhibitors.
Lin Z, Ning X, Lai R, Hai L, Nie R, Guo L, Li G, Yang Z, Wu Y.
Eur J Med Chem (2024) 279 : 116852 -116852
PubMed 39276584 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 10 4.94 5.91

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1812545 1 5.91
CHEMBL5618748 1 5.14
CHEMBL5620309 1 4.83
CHEMBL5619421 1 4.83
CHEMBL5618425 1 4.65
CHEMBL5618823 1 4.62
CHEMBL5618165 1 4.59
CHEMBL5618428 1 -
CHEMBL5619903 1 -
CHEMBL5619886 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1812545 IC50 = 1240.0 nM 5.91
CHEMBL5618748 IC50 = 7230.0 nM 5.14
CHEMBL5620309 IC50 = 14610.0 nM 4.83
CHEMBL5619421 IC50 = 14770.0 nM 4.83
CHEMBL5618425 IC50 = 22330.0 nM 4.65
CHEMBL5618823 IC50 = 23950.0 nM 4.62
CHEMBL5618165 IC50 = 25850.0 nM 4.59
CHEMBL5618428 IC50 > 30000.0 nM -
CHEMBL5619903 IC50 > 30000.0 nM -
CHEMBL5619886 IC50 > 30000.0 nM -