Assay Detail

CHEMBL4058752

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Binding

Inhibition of human recombinant IDO-1 using tryptophan as substrate after 22 mins by LC-MS/MS method

ChEMBL ↗

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Target

Indoleamine 2,3-dioxygenase 1 (CHEMBL4685) ↗

Open DB target context

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Indoleamine 2,3-dioxygenase 1 (CHEMBL4685) is the working anchor for this assay review. Loading the live Open DB target snapshot…

Primary target Indoleamine 2,3-dioxygenase 1

CHEMBL4685

Anchored from Assay target.

Protein identity Indoleamine 2,3-dioxygenase 1

Disease frame Disease evidence pending

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Review focus Open DB context pending

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Total Activities

Compounds Tested

Activity Types

Assay Parameters

Assay Information

Assay Type	Binding
Organism	Homo sapiens
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	5.84	6.70

Compounds Tested

Compound	Name	Phase	Activities	Best pChEMBL
CHEMBL4061767	—	—	1	6.70
CHEMBL4086143	PF-06840003	1.0	1	6.39
CHEMBL4090501	—	—	1	4.42

Activity Data

Compound	Name	Type	Rel.	Value	Units	pChEMBL
CHEMBL4061767	—	IC50	=	200.0	nM	6.70
CHEMBL4086143	PF-06840003	IC50	=	410.0	nM	6.39
CHEMBL4090501	—	IC50	=	38000.0	nM	4.42