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Assay Detail

CHEMBL4399583

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Binding
Inhibition of human ERG
5
Total Activities
5
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 Selective, Orally Bioavailable Pyrazolopyridine Inhibitors of Protein Kinase Cθ (PKCθ) That Ameliorate Symptoms of Experimental Autoimmune Encephalomyelitis.
Collier PN, Twin HC, Knegtel RMA, Boyall D, Brenchley G, Davis CJ, Keily S, Mak C, Miller A, Pierard F, Settimo L, Bolton CM, Chiu P, Curnock A, Doyle E, Tanner AJ, Jimenez JM.
ACS Med Chem Lett (2019) 10 : 1134 -1139
PubMed 31417666 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 5.84 6.16

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4590477 1 6.16
CHEMBL4589844 1 5.52
CHEMBL4457150 1 -
CHEMBL4587816 1 -
CHEMBL4461649 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4590477 IC50 = 700.0 nM 6.16
CHEMBL4589844 IC50 = 3000.0 nM 5.52
CHEMBL4457150 IC50 > 10000.0 nM -
CHEMBL4587816 IC50 > 10000.0 nM -
CHEMBL4461649 IC50 > 10000.0 nM -