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Assay Detail

CHEMBL4843307

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

Binding
Inhibition of IDO1 in human whole blood stimulated with IFNgamma/LPS using L-tryptophan/kynurenine as substrate incubated for 15 mins followed by IFNgamma/LPS stimulation and incubated for 24 hrs by LC-MS analysis
8
Total Activities
4
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Tissue Blood
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 IACS-9779 and IACS-70465 as Potent Inhibitors Targeting Indoleamine 2,3-Dioxygenase 1 (IDO1) Apoenzyme.
Hamilton MM, Mseeh F, McAfoos TJ, Leonard PG, Reyna NJ, Harris AL, Xu A, Han M, Soth MJ, Czako B, Theroff JP, Mandal PK, Burke JP, Virgin-Downey B, Petrocchi A, Pfaffinger D, Rogers NE, Parker CA, Yu SS, Jiang Y, Krapp S, Lammens A, Trevitt G, Tremblay MR, Mikule K, Wilcoxen K, Cross JB, Jones P, Marszalek JR, Lewis RT.
J Med Chem (2021) 64 : 11302 -11329
PubMed 34292726 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 7.43 7.85
IC90 4 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4856710 2 7.85
CHEMBL4855340 2 7.58
CHEMBL4858888 2 7.34
CHEMBL4861332 2 6.94

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4856710 IC50 = 14.0 nM 7.85
CHEMBL4855340 IC50 = 26.0 nM 7.58
CHEMBL4858888 IC50 = 46.0 nM 7.34
CHEMBL4861332 IC50 = 116.0 nM 6.94
CHEMBL4861332 IC90 = 1047.0 nM -
CHEMBL4858888 IC90 = 411.0 nM -
CHEMBL4856710 IC90 = 124.0 nM -
CHEMBL4855340 IC90 = 260.0 nM -