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Assay Detail

CHEMBL4058756

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Binding
Inhibition of IDO-1 in IFN-gamma-stimulated human HeLa cells assessed as decrease in kynurenine production after 16 to 24 hrs by PDMAB method
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HeLa
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Indoleamine 2,3-dioxygenase 1 (CHEMBL4685)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of a Novel and Selective Indoleamine 2,3-Dioxygenase (IDO-1) Inhibitor 3-(5-Fluoro-1H-indol-3-yl)pyrrolidine-2,5-dione (EOS200271/PF-06840003) and Its Characterization as a Potential Clinical Candidate.
Crosignani S, Bingham P, Bottemanne P, Cannelle H, Cauwenberghs S, Cordonnier M, Dalvie D, Deroose F, Feng JL, Gomes B, Greasley S, Kaiser SE, Kraus M, Négrerie M, Maegley K, Miller N, Murray BW, Schneider M, Soloweij J, Stewart AE, Tumang J, Torti VR, Van Den Eynde B, Wythes M.
J Med Chem (2017) 60 : 9617 -9629
PubMed 29111717 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 5.55 6.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4061767 1 6.00
CHEMBL4086143 PF-06840003 1.0 1 5.75
CHEMBL4090501 1 4.89

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4061767 IC50 = 1000.0 nM 6.00
CHEMBL4086143 PF-06840003 IC50 = 1800.0 nM 5.75
CHEMBL4090501 IC50 = 13000.0 nM 4.89