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Assay Detail

CHEMBL2330092

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Binding
Inhibition of Abl2 kinase (unknown origin) using Tyr 6 peptide as substrate assessed as residual enzyme activity after every 10 secs measured for 10 mins
11
Total Activities
11
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 ABL2 (CHEMBL4014)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Rapid discovery of a novel series of Abl kinase inhibitors by application of an integrated microfluidic synthesis and screening platform.
Desai B, Dixon K, Farrant E, Feng Q, Gibson KR, van Hoorn WP, Mills J, Morgan T, Parry DM, Ramjee MK, Selway CN, Tarver GJ, Whitlock G, Wright AG.
J Med Chem (2013) 56 : 3033 -3047
PubMed 23441572 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 11 7.82 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2324924 1 9.00
CHEMBL2324926 1 8.22
CHEMBL2324930 1 8.10
CHEMBL2324925 1 8.00
CHEMBL2324927 1 7.92
CHEMBL2324928 1 7.85
CHEMBL2324923 1 7.82
CHEMBL2324931 1 7.75
CHEMBL2324929 1 7.44
CHEMBL2324932 1 7.40
CHEMBL2321908 1 6.53

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2324924 IC50 = 1.0 nM 9.00
CHEMBL2324926 IC50 = 6.0 nM 8.22
CHEMBL2324930 IC50 = 8.0 nM 8.10
CHEMBL2324925 IC50 = 10.0 nM 8.00
CHEMBL2324927 IC50 = 12.0 nM 7.92
CHEMBL2324928 IC50 = 14.0 nM 7.85
CHEMBL2324923 IC50 = 15.0 nM 7.82
CHEMBL2324931 IC50 = 18.0 nM 7.75
CHEMBL2324929 IC50 = 36.0 nM 7.44
CHEMBL2324932 IC50 = 40.0 nM 7.40
CHEMBL2321908 IC50 = 298.0 nM 6.53