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Assay Detail

CHEMBL4725184

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

Binding
Inhibition of IDO1 in IFN-gamma/LPS induced human whole blood assessed as tryptophan/kynurenine level measured after 18 hrs by RapidFire mass spectrometry
12
Total Activities
12
Compounds Tested
1
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 Imidazopyridines as Potent Inhibitors of Indoleamine 2,3-Dioxygenase 1 for Cancer Immunotherapy.
Zhang L,Cherney EC,Zhu X,Lin TA,Gullo-Brown J,Maley D,Johnston-Allegretto K,Kopcho L,Fereshteh M,Huang C,Li X,Traeger SC,Dhar G,Anandam A,Mahankali S,Padmanabhan S,Rajanna P,Murali V,Mariappan T,Borzilleri R,Vite G,Hunt JT,Balog A
ACS Med Chem Lett (2021) 12 : 494 -501
PubMed 33738077 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 12 7.52 8.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4750659 1 8.22
CHEMBL4750211 1 8.05
CHEMBL4746203 1 7.85
CHEMBL4752094 1 7.80
CHEMBL4756822 1 7.68
CHEMBL4779097 1 7.58
CHEMBL4796040 1 7.51
CHEMBL4755937 1 7.50
CHEMBL4743245 1 7.44
CHEMBL4763467 1 7.30
CHEMBL4761987 1 7.02
CHEMBL4757655 1 6.34

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4750659 IC50 = 6.0 nM 8.22
CHEMBL4750211 IC50 = 9.0 nM 8.05
CHEMBL4746203 IC50 = 14.0 nM 7.85
CHEMBL4752094 IC50 = 16.0 nM 7.80
CHEMBL4756822 IC50 = 21.0 nM 7.68
CHEMBL4779097 IC50 = 26.0 nM 7.58
CHEMBL4796040 IC50 = 31.0 nM 7.51
CHEMBL4755937 IC50 = 32.0 nM 7.50
CHEMBL4743245 IC50 = 36.0 nM 7.44
CHEMBL4763467 IC50 = 50.0 nM 7.30
CHEMBL4761987 IC50 = 96.0 nM 7.02
CHEMBL4757655 IC50 = 459.0 nM 6.34