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Assay Detail

CHEMBL4367272

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Binding
Inhibition of human ERG
18
Total Activities
18
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

Publication

Discovery of Clinical Candidate (1R,4r)-4-((R)-2-((S)-6-Fluoro-5H-imidazo[5,1-a]isoindol-5-yl)-1-hydroxyethyl)cyclohexan-1-ol (Navoximod), a Potent and Selective Inhibitor of Indoleamine 2,3-Dioxygenase 1.
Kumar S, Waldo JP, Jaipuri FA, Marcinowicz A, Van Allen C, Adams J, Kesharwani T, Zhang X, Metz R, Oh AJ, Harris SF, Mautino MR.
J Med Chem (2019) 62 : 6705 -6733
PubMed 31264862 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 18 4.52 4.88

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4570289 1 4.88
CHEMBL4550278 1 4.80
CHEMBL3753837 1 4.64
CHEMBL4450473 1 4.52
CHEMBL4517185 1 4.47
CHEMBL4543526 1 4.19
CHEMBL3989951 NAVOXIMOD 2.0 1 4.15
CHEMBL4576829 1 -
CHEMBL4461858 1 -
CHEMBL4562289 1 -
CHEMBL4540038 1 -
CHEMBL4535605 1 -
CHEMBL4530496 1 -
CHEMBL4467206 1 -
CHEMBL4476312 1 -
CHEMBL4446572 1 -
CHEMBL4435301 1 -
CHEMBL4443852 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4570289 EC50 = 13200.0 nM 4.88
CHEMBL4550278 EC50 = 16000.0 nM 4.80
CHEMBL3753837 EC50 = 23000.0 nM 4.64
CHEMBL4450473 EC50 = 30000.0 nM 4.52
CHEMBL4517185 EC50 = 34000.0 nM 4.47
CHEMBL4543526 EC50 = 65000.0 nM 4.19
CHEMBL3989951 NAVOXIMOD EC50 = 71000.0 nM 4.15
CHEMBL4576829 EC50 > 100000.0 nM -
CHEMBL4461858 EC50 - -
CHEMBL4562289 EC50 - -
CHEMBL4540038 EC50 - -
CHEMBL4535605 EC50 - -
CHEMBL4530496 EC50 > 100000.0 nM -
CHEMBL4467206 EC50 - -
CHEMBL4476312 EC50 - -
CHEMBL4446572 EC50 - -
CHEMBL4435301 EC50 - -
CHEMBL4443852 EC50 - -