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Assay Detail

CHEMBL5160522

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

Binding
Displacement of [3H] labeled-N-(4-Fluorophenyl)-3-(4-(4-(2-hydroxypropan-2-yl)-6-(trifluoromethyl)pyridin-3-yl)phenyl)oxetane-3-carboxamide from human IDO1 assessed as dissociation constant by radioligand binding assay
1
Total Activities
1
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

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

Publication

Oxetane Promise Delivered: Discovery of Long-Acting IDO1 Inhibitors Suitable for Q3W Oral or Parenteral Dosing.
Li D, Sloman DL, Achab A, Zhou H, McGowan MA, White C, Gibeau C, Zhang H, Pu Q, Bharathan I, Hopkins B, Liu K, Ferguson H, Fradera X, Lesburg CA, Martinot TA, Qi J, Song ZJ, Yin J, Zhang H, Song L, Wan B, DAddio S, Solban N, Miller JR, Zamlynny B, Bass A, Freeland E, Ykoruk B, Hilliard C, Ferraro J, Zhai J, Knemeyer I, Otte KM, Vincent S, Sciammetta N, Pasternak A, Bennett DJ, Han Y.
J Med Chem (2022) 65 : 6001 -6016
PubMed 35239336 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 1 9.80 9.80

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5192977 1 9.80

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5192977 Kd = 0.158 nM 9.80