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Assay Detail

CHEMBL2320524

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

Binding
Binding affinity to phosphorylated wild type ABL1 (unknown origin) after 1 hr
1
Total Activities
1
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

Tyrosine-protein kinase ABL1 (CHEMBL1862)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Identification of GZD824 as an orally bioavailable inhibitor that targets phosphorylated and nonphosphorylated breakpoint cluster region-Abelson (Bcr-Abl) kinase and overcomes clinically acquired mutation-induced resistance against imatinib.
Ren X, Pan X, Zhang Z, Wang D, Lu X, Li Y, Wen D, Long H, Luo J, Feng Y, Zhuang X, Zhang F, Liu J, Leng F, Lang X, Bai Y, She M, Tu Z, Pan J, Ding K, Ding K.
J Med Chem (2013) 56 : 879 -894
PubMed 23301703 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 1 9.47 9.47

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2316582 OLVEREMBATINIB 3.0 1 9.47

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2316582 OLVEREMBATINIB Kd = 0.34 nM 9.47