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Assay Detail

CHEMBL1827700

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ADMET
Inhibition of human ERG
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Transcriptional regulator ERG (CHEMBL1293191)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Identification of a series of 4-[3-(quinolin-2-yl)-1,2,4-oxadiazol-5-yl]piperazinyl ureas as potent smoothened antagonist hedgehog pathway inhibitors.
Ontoria JM, Bufi LL, Torrisi C, Bresciani A, Giomini C, Rowley M, Serafini S, Bin H, Hao W, Steinkühler C, Jones P.
Bioorg Med Chem Lett (2011) 21 : 5274 -5282
PubMed 21803580 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 4.71 4.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1823591 1 4.92
CHEMBL1823616 1 4.50
CHEMBL1823865 1 -
CHEMBL1822468 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1823591 IC50 = 12000.0 nM 4.92
CHEMBL1823616 IC50 = 32000.0 nM 4.50
CHEMBL1823865 IC50 > 30000.0 nM -
CHEMBL1822468 IC50 > 30000.0 nM -