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Assay Detail

CHEMBL4236263

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Binding
Binding affinity to human ERG
2
Total Activities
2
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 potent, highly selective covalent irreversible BTK inhibitors from a fragment hit.
Qiu H, Liu-Bujalski L, Caldwell RD, Follis AV, Gardberg A, Goutopoulos A, Grenningloh R, Head J, Johnson T, Jones R, Mochalkin I, Morandi F, Neagu C, Sherer B.
Bioorg Med Chem Lett (2018) 28 : 2939 -2944
PubMed 30122225 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 2 5.81 5.96

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1873475 IBRUTINIB 4.0 1 5.96
CHEMBL4242598 1 5.66

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1873475 IBRUTINIB Ki = 1100.0 nM 5.96
CHEMBL4242598 Ki = 2200.0 nM 5.66