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Assay Detail

CHEMBL3824532

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

Binding
Inhibition of human YES using poly[Glu,Tyr]4:1 as substrate in presence of [gamma-33P] ATP
8
Total Activities
8
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 Yes (CHEMBL2073)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Rapid Discovery and Structure-Activity Relationships of Pyrazolopyrimidines That Potently Suppress Breast Cancer Cell Growth via SRC Kinase Inhibition with Exceptional Selectivity over ABL Kinase.
Fraser C, Dawson JC, Dowling R, Houston DR, Weiss JT, Munro AF, Muir M, Harrington L, Webster SP, Frame MC, Brunton VG, Patton EE, Carragher NO, Unciti-Broceta A.
J Med Chem (2016) 59 : 4697 -4710
PubMed 27115835 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 8 6.90 7.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3823861 1 7.92
CHEMBL306380 1 7.44
CHEMBL3823212 1 7.15
CHEMBL3823849 1 6.46
CHEMBL3799221 1 6.25
CHEMBL3822591 1 6.16
CHEMBL3824089 1 -
CHEMBL5416410 DASATINIB 4.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3823861 IC50 = 12.0 nM 7.92
CHEMBL306380 IC50 = 36.0 nM 7.44
CHEMBL3823212 IC50 = 71.0 nM 7.15
CHEMBL3823849 IC50 = 344.0 nM 6.46
CHEMBL3799221 IC50 = 566.0 nM 6.25
CHEMBL3822591 IC50 = 696.0 nM 6.16
CHEMBL3824089 IC50 < 0.5 nM -
CHEMBL5416410 DASATINIB IC50 < 0.5 nM -