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Assay Detail

CHEMBL4725179

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

Binding
Inhibition of IDO1 in recombinant IFN-gamma induced human HeLa cells incubated for 18 hrs by fluorescence microplate reader assay
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HeLa
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 20 8.09 8.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4750659 1 8.70
CHEMBL4750211 1 8.70
CHEMBL4756822 1 8.70
CHEMBL4161733 1 8.70
CHEMBL4763467 1 8.52
CHEMBL4750132 1 8.52
CHEMBL4780978 1 8.52
CHEMBL4746203 1 8.52
CHEMBL4796040 1 8.52
CHEMBL4755937 1 8.52
CHEMBL4779097 1 8.40
CHEMBL4752094 1 8.22
CHEMBL4743245 1 8.15
CHEMBL4748491 1 7.96
CHEMBL4757655 1 7.89
CHEMBL4761987 1 7.89
CHEMBL4750005 1 7.70
CHEMBL4799065 1 6.78
CHEMBL4779779 1 6.62
CHEMBL4760452 1 6.30

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4750659 IC50 = 2.0 nM 8.70
CHEMBL4750211 IC50 = 2.0 nM 8.70
CHEMBL4756822 IC50 = 2.0 nM 8.70
CHEMBL4161733 IC50 = 2.0 nM 8.70
CHEMBL4763467 IC50 = 3.0 nM 8.52
CHEMBL4750132 IC50 = 3.0 nM 8.52
CHEMBL4780978 IC50 = 3.0 nM 8.52
CHEMBL4746203 IC50 = 3.0 nM 8.52
CHEMBL4796040 IC50 = 3.0 nM 8.52
CHEMBL4755937 IC50 = 3.0 nM 8.52
CHEMBL4779097 IC50 = 4.0 nM 8.40
CHEMBL4752094 IC50 = 6.0 nM 8.22
CHEMBL4743245 IC50 = 7.0 nM 8.15
CHEMBL4748491 IC50 = 11.0 nM 7.96
CHEMBL4757655 IC50 = 13.0 nM 7.89
CHEMBL4761987 IC50 = 13.0 nM 7.89
CHEMBL4750005 IC50 = 20.0 nM 7.70
CHEMBL4799065 IC50 = 165.0 nM 6.78
CHEMBL4779779 IC50 = 239.0 nM 6.62
CHEMBL4760452 IC50 = 495.0 nM 6.30