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Assay Detail

CHEMBL1817449

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

Binding
Competitive inhibition of human recombinant TDO expressed in Escherichia coli BL21 using L-tryptophan as substrate by measuring conversion of N-formylkynurenine into kynurenine after 30 mins by Michaelis-Menten steady state 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 (TDO) inhibitors. 3-(2-(pyridyl)ethenyl)indoles as potential anticancer immunomodulators.
Dolusić E, Larrieu P, Moineaux L, Stroobant V, Pilotte L, Colau D, Pochet L, Van den Eynde B, Masereel B, Wouters J, Frédérick R.
J Med Chem (2011) 54 : 5320 -5334
PubMed 21726069 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 4 5.27 6.06

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL355606 1 6.06
CHEMBL1812545 1 5.25
CHEMBL1812547 1 4.49
CHEMBL54976 TRYPTOPHAN 4.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL355606 Ki = 880.0 nM 6.06
CHEMBL1812545 Ki = 5600.0 nM 5.25
CHEMBL1812547 Ki = 32400.0 nM 4.49
CHEMBL54976 TRYPTOPHAN Ki = 11500000.0 nM -