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Assay Detail

CHEMBL4725185

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

Binding
Transactivation of PXR (unknown origin) assessed as CYP450 induction
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Nuclear receptor subfamily 1 group I member 2 (CHEMBL3401)
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
EC50 7 5.84 6.26

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4746203 1 6.26
CHEMBL4752094 1 6.03
CHEMBL4763467 1 5.97
CHEMBL4756822 1 5.92
CHEMBL4796040 1 5.52
CHEMBL4761987 1 5.32
CHEMBL4757655 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4746203 EC50 = 550.0 nM 6.26
CHEMBL4752094 EC50 = 940.0 nM 6.03
CHEMBL4763467 EC50 = 1060.0 nM 5.97
CHEMBL4756822 EC50 = 1190.0 nM 5.92
CHEMBL4796040 EC50 = 3030.0 nM 5.52
CHEMBL4761987 EC50 = 4820.0 nM 5.32
CHEMBL4757655 EC50 > 50000.0 nM -