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Assay Detail

CHEMBL4479780

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

Binding
Inhibition of full-length recombinant human His-tagged SRC expressed in baculovirus expression system by Adapta assay
4
Total Activities
4
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

Proto-oncogene tyrosine-protein kinase Src (CHEMBL267)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Optimization of microtubule affinity regulating kinase (MARK) inhibitors with improved physical properties.
Sloman DL, Noucti N, Altman MD, Chen D, Mislak AC, Szewczak A, Hayashi M, Warren L, Dellovade T, Wu Z, Marcus J, Walker D, Su HP, Edavettal SC, Munshi S, Hutton M, Nuthall H, Stanton MG.
Bioorg Med Chem Lett (2016) 26 : 4362 -4366
PubMed 27491711 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 7.11 8.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4568087 1 8.52
CHEMBL4569508 1 7.43
CHEMBL4550702 1 7.38
CHEMBL4552628 1 5.09

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4568087 IC50 = 3.0 nM 8.52
CHEMBL4569508 IC50 = 37.0 nM 7.43
CHEMBL4550702 IC50 = 42.0 nM 7.38
CHEMBL4552628 IC50 = 8100.0 nM 5.09