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Assay Detail

CHEMBL1817446

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

Binding
Inhibition of mouse TDO expressed in mouse P815B cells assessed as inhibition of tryptophan catabolism by measuring kynurenine production after 8 hrs by HPLC analysis
76
Total Activities
76
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Mus musculus
Cell Type P815B
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Tryptophan 2,3-dioxygenase (CHEMBL1075307)
Type SINGLE PROTEIN
Organism Mus musculus

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
IC50 76 5.03 6.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1812539 1 6.00
CHEMBL355606 1 6.00
CHEMBL441669 1 6.00
CHEMBL1812545 1 5.70
CHEMBL1812546 1 5.70
CHEMBL435072 1 5.52
CHEMBL1812531 1 5.52
CHEMBL1812540 1 5.52
CHEMBL1812543 1 5.52
CHEMBL1812547 1 5.52
CHEMBL168956 1 5.30
CHEMBL1812554 1 5.22
CHEMBL1812506 1 5.00
CHEMBL1812544 1 5.00
CHEMBL1812538 1 5.00
CHEMBL1812535 1 5.00
CHEMBL1812541 1 4.89
CHEMBL1812498 1 4.75
CHEMBL445966 1 4.75
CHEMBL1812512 1 4.70
CHEMBL166509 1 4.70
CHEMBL1812520 1 4.70
CHEMBL171548 1 4.70
CHEMBL1812513 1 4.40
CHEMBL1812515 1 4.40
CHEMBL1812533 1 4.40
CHEMBL176991 1 4.36
CHEMBL1812526 1 4.30
CHEMBL1812548 1 4.10
CHEMBL1812553 1 4.10

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1812539 IC50 = 1000.0 nM 6.00
CHEMBL441669 IC50 = 1000.0 nM 6.00
CHEMBL355606 IC50 = 1000.0 nM 6.00
CHEMBL1812545 IC50 = 2000.0 nM 5.70
CHEMBL1812546 IC50 = 2000.0 nM 5.70
CHEMBL435072 IC50 = 3000.0 nM 5.52
CHEMBL1812531 IC50 = 3000.0 nM 5.52
CHEMBL1812540 IC50 = 3000.0 nM 5.52
CHEMBL1812543 IC50 = 3000.0 nM 5.52
CHEMBL1812547 IC50 = 3000.0 nM 5.52
CHEMBL168956 IC50 = 5000.0 nM 5.30
CHEMBL1812554 IC50 = 6000.0 nM 5.22
CHEMBL1812538 IC50 = 10000.0 nM 5.00
CHEMBL1812506 IC50 = 10000.0 nM 5.00
CHEMBL1812544 IC50 = 10000.0 nM 5.00
CHEMBL1812535 IC50 = 10000.0 nM 5.00
CHEMBL1812541 IC50 = 13000.0 nM 4.89
CHEMBL1812498 IC50 = 18000.0 nM 4.75
CHEMBL445966 IC50 = 18000.0 nM 4.75
CHEMBL1812512 IC50 = 20000.0 nM 4.70
CHEMBL166509 IC50 = 20000.0 nM 4.70
CHEMBL1812520 IC50 = 20000.0 nM 4.70
CHEMBL171548 IC50 = 20000.0 nM 4.70
CHEMBL1812533 IC50 = 40000.0 nM 4.40
CHEMBL1812513 IC50 = 40000.0 nM 4.40
CHEMBL1812515 IC50 = 40000.0 nM 4.40
CHEMBL176991 IC50 = 44000.0 nM 4.36
CHEMBL1812526 IC50 = 50000.0 nM 4.30
CHEMBL1812548 IC50 = 80000.0 nM 4.10
CHEMBL1812553 IC50 = 80000.0 nM 4.10
CHEMBL1812497 IC50 > 200000.0 nM -
CHEMBL1812496 IC50 > 200000.0 nM -
CHEMBL1812495 IC50 > 200000.0 nM -
CHEMBL1812511 IC50 > 200000.0 nM -
CHEMBL1812550 IC50 > 80000.0 nM -
CHEMBL1812549 IC50 > 80000.0 nM -
CHEMBL1812552 IC50 > 80000.0 nM -
CHEMBL1812653 IC50 > 200000.0 nM -
CHEMBL46724 IC50 > 80000.0 nM -
CHEMBL1812654 IC50 > 80000.0 nM -
CHEMBL1812551 IC50 > 80000.0 nM -
CHEMBL1812542 IC50 > 80000.0 nM -
CHEMBL1812656 IC50 > 80000.0 nM -
CHEMBL1812530 IC50 > 200000.0 nM -
CHEMBL1812536 IC50 > 200000.0 nM -
CHEMBL1812655 IC50 > 80000.0 nM -
CHEMBL1812658 IC50 > 80000.0 nM -
CHEMBL1812657 IC50 > 80000.0 nM -
CHEMBL1812659 IC50 > 80000.0 nM -
CHEMBL1812537 IC50 > 200000.0 nM -