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Assay Detail

CHEMBL4383515

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Binding
Inhibition of recombinant full length C-terminal His-tagged human TDO expressed in Escherichia coli using L-Trp as substrate after 30 mins
11
Total Activities
11
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

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

Publication

Tryptophan 2,3-dioxygenase inhibitory activities of tryptanthrin derivatives.
Zhang S, Qi F, Fang X, Yang D, Hu H, Huang Q, Kuang C, Yang Q.
Eur J Med Chem (2018) 160 : 133 -145
PubMed 30321802 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 11 5.41 7.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL432537 1 7.00
CHEMBL1098875 1 6.03
CHEMBL72165 1 6.03
CHEMBL3087009 1 5.83
CHEMBL312537 1 5.49
CHEMBL306946 TRYPTANTHRIN 1 5.41
CHEMBL3086870 1 5.01
CHEMBL1812545 1 4.73
CHEMBL3087010 1 4.35
CHEMBL3545369 EPACADOSTAT 3.0 1 4.19
CHEMBL1276265 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL432537 IC50 = 101.0 nM 7.00
CHEMBL1098875 IC50 = 937.0 nM 6.03
CHEMBL72165 IC50 = 937.0 nM 6.03
CHEMBL3087009 IC50 = 1490.0 nM 5.83
CHEMBL312537 IC50 = 3230.0 nM 5.49
CHEMBL306946 TRYPTANTHRIN IC50 = 3940.0 nM 5.41
CHEMBL3086870 IC50 = 9810.0 nM 5.01
CHEMBL1812545 IC50 = 18700.0 nM 4.73
CHEMBL3087010 IC50 = 44800.0 nM 4.35
CHEMBL3545369 EPACADOSTAT IC50 = 64500.0 nM 4.19
CHEMBL1276265 IC50 = 224200.0 nM -