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Assay Detail

CHEMBL4680002

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

Binding
Inhibition of IDO1 in IFNgamma-stimulated mouse M109 cells preincubated for 2 hrs followed by IFNgamma stimulation and measured after 18 hrs by
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Mus musculus
Cell Type M109
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Indoleamine 2,3-dioxygenase 1 (CHEMBL1075294)
Type SINGLE PROTEIN
Organism Mus musculus

Publication

Discovery and Preclinical Evaluation of BMS-986242, a Potent, Selective Inhibitor of Indoleamine-2,3-dioxygenase 1.
Cherney EC,Zhang L,Nara S,Zhu X,Gullo-Brown J,Maley D,Lin TA,Hunt JT,Huang C,Yang Z,Darienzo C,Discenza L,Ranasinghe A,Grubb M,Ziemba T,Traeger SC,Li X,Johnston K,Kopcho L,Fereshteh M,Foster K,Stefanski K,Fargnoli J,Swanson J,Brown J,Delpy D,Seitz SP,Borzilleri R,Vite G,Balog A
ACS Med Chem Lett (2021) 12 : 288 -294
PubMed 33603977 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 18 7.24 8.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4786690 1 8.70
CHEMBL4743409 1 8.52
CHEMBL4161733 1 8.30
CHEMBL4755937 1 7.92
CHEMBL4747228 1 7.70
CHEMBL4757725 1 7.32
CHEMBL4793928 1 7.25
CHEMBL4794508 1 7.21
CHEMBL4754556 1 7.17
CHEMBL4740285 1 7.07
CHEMBL4789681 1 7.04
CHEMBL4796405 1 6.67
CHEMBL4757067 1 6.54
CHEMBL4759322 1 6.19
CHEMBL4791270 1 6.11
CHEMBL4758055 1 6.06
CHEMBL4752360 1 -
CHEMBL4791151 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4786690 IC50 = 2.0 nM 8.70
CHEMBL4743409 IC50 = 3.0 nM 8.52
CHEMBL4161733 IC50 = 5.0 nM 8.30
CHEMBL4755937 IC50 = 12.0 nM 7.92
CHEMBL4747228 IC50 = 20.0 nM 7.70
CHEMBL4757725 IC50 = 48.0 nM 7.32
CHEMBL4793928 IC50 = 56.0 nM 7.25
CHEMBL4794508 IC50 = 62.0 nM 7.21
CHEMBL4754556 IC50 = 67.0 nM 7.17
CHEMBL4740285 IC50 = 86.0 nM 7.07
CHEMBL4789681 IC50 = 92.0 nM 7.04
CHEMBL4796405 IC50 = 215.0 nM 6.67
CHEMBL4757067 IC50 = 287.0 nM 6.54
CHEMBL4759322 IC50 = 651.0 nM 6.19
CHEMBL4791270 IC50 = 772.0 nM 6.11
CHEMBL4758055 IC50 = 870.0 nM 6.06
CHEMBL4752360 IC50 > 1000.0 nM -
CHEMBL4791151 IC50 > 1000.0 nM -