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Assay Detail

CHEMBL4843234

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

Binding
Inhibition of IDO1 in mouse Panc02 cells assessed as reduction in NFK level incubated for 48 hrs by RFMS analysis
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Mus musculus
Cell Type Panc02
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 7 8.11 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4858888 1 9.00
CHEMBL4855340 1 8.80
CHEMBL4856710 1 8.70
CHEMBL4861332 1 7.85
CHEMBL4853212 1 7.64
CHEMBL4870435 1 7.64
CHEMBL3545369 EPACADOSTAT 3.0 1 7.13

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4858888 IC50 = 1.0 nM 9.00
CHEMBL4855340 IC50 = 1.6 nM 8.80
CHEMBL4856710 IC50 = 2.0 nM 8.70
CHEMBL4861332 IC50 = 14.0 nM 7.85
CHEMBL4853212 IC50 = 23.0 nM 7.64
CHEMBL4870435 IC50 = 23.0 nM 7.64
CHEMBL3545369 EPACADOSTAT IC50 = 74.0 nM 7.13