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Assay Detail

CHEMBL4058753

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Binding
Inhibition of mouse IDO-1 using tryptophan as substrate after 22 mins by LC-MS/MS method
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Indoleamine 2,3-dioxygenase 1 (CHEMBL1075294)
Type SINGLE PROTEIN
Organism Mus musculus

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 2 5.48 5.82

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4086143 PF-06840003 1.0 1 5.82
CHEMBL4061767 1 5.14

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4086143 PF-06840003 IC50 = 1500.0 nM 5.82
CHEMBL4061767 IC50 = 7300.0 nM 5.14