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Assay Detail

CHEMBL4843308

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

Functional
In vivo inhibition of IDO1 in tumor of po dosed NSG mouse xenografted with human SKOV3 cells assessed as reduction in KYN level administered twice daily for 5 days measured at 12 hrs post dose
2
Total Activities
1
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Mus musculus
Tissue Neoplasm
Cell Type SK-OV-3
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 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 1 8.24 8.24
IC90 1 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4855340 2 8.24

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4855340 IC50 = 5.8 nM 8.24
CHEMBL4855340 IC90 = 52.0 nM -