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Assay Detail

CHEMBL4383516

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

Binding
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
7
Total Activities
7
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 7 5.81 6.67

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL432537 1 6.67
CHEMBL1098875 1 6.47
CHEMBL72165 1 6.45
CHEMBL306946 TRYPTANTHRIN 1 6.24
CHEMBL1812545 1 5.13
CHEMBL3087010 1 5.08
CHEMBL3545369 EPACADOSTAT 3.0 1 4.66

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL432537 Ki = 215.0 nM 6.67
CHEMBL1098875 Ki = 336.0 nM 6.47
CHEMBL72165 Ki = 356.0 nM 6.45
CHEMBL306946 TRYPTANTHRIN Ki = 581.0 nM 6.24
CHEMBL1812545 Ki = 7470.0 nM 5.13
CHEMBL3087010 Ki = 8410.0 nM 5.08
CHEMBL3545369 EPACADOSTAT Ki = 21700.0 nM 4.66