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Assay Detail

CHEMBL4383517

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

Binding
Mixed type uncompetitive inhibition of recombinant full length C-terminal His-tagged human TDO expressed in Escherichia coli using L-Trp as substrate after 30 mins by Dixon plot analysis
4
Total Activities
4
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
Ki 4 5.63 6.08

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL312537 1 6.08
CHEMBL3086870 1 6.06
CHEMBL3087009 1 6.00
CHEMBL1276265 1 4.37

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL312537 Ki = 834.0 nM 6.08
CHEMBL3086870 Ki = 876.0 nM 6.06
CHEMBL3087009 Ki = 1000.0 nM 6.00
CHEMBL1276265 Ki = 42700.0 nM 4.37