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Assay Detail

CHEMBL1839617

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

Binding
Inhibition of BRK pretreated for 30 mins by microplate reader
67
Total Activities
67
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

Protein-tyrosine kinase 6 (CHEMBL4601)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of novel imidazo[1,2-a]pyrazin-8-amines as Brk/PTK6 inhibitors.
Zeng H, Belanger DB, Curran PJ, Shipps GW, Miao H, Bracken JB, Arshad Siddiqui M, Malkowski M, Wang Y.
Bioorg Med Chem Lett (2011) 21 : 5870 -5875
PubMed 21855335 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 67 7.48 8.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1836842 1 8.70
CHEMBL1836806 1 8.52
CHEMBL1836844 1 8.52
CHEMBL1836854 1 8.52
CHEMBL1836863 1 8.52
CHEMBL1836846 1 8.30
CHEMBL1836755 1 8.22
CHEMBL1836865 1 8.22
CHEMBL1836840 1 8.15
CHEMBL1836867 1 8.15
CHEMBL1836802 1 8.15
CHEMBL1836810 1 8.10
CHEMBL1836805 1 8.10
CHEMBL5416410 DASATINIB 4.0 1 8.05
CHEMBL1836862 1 8.05
CHEMBL1836754 1 8.00
CHEMBL1836864 1 8.00
CHEMBL1836853 1 8.00
CHEMBL1836847 1 8.00
CHEMBL1836843 1 8.00
CHEMBL1836815 1 8.00
CHEMBL1836799 1 8.00
CHEMBL1836760 1 8.00
CHEMBL1836796 1 7.96
CHEMBL1836841 1 7.96
CHEMBL1836761 1 7.92
CHEMBL1739550 1 7.89
CHEMBL1836845 1 7.89
CHEMBL1836800 1 7.82
CHEMBL1836837 1 7.80

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1836842 IC50 = 2.0 nM 8.70
CHEMBL1836806 IC50 = 3.0 nM 8.52
CHEMBL1836863 IC50 = 3.0 nM 8.52
CHEMBL1836844 IC50 = 3.0 nM 8.52
CHEMBL1836854 IC50 = 3.0 nM 8.52
CHEMBL1836846 IC50 = 5.0 nM 8.30
CHEMBL1836755 IC50 = 6.0 nM 8.22
CHEMBL1836865 IC50 = 6.0 nM 8.22
CHEMBL1836802 IC50 = 7.0 nM 8.15
CHEMBL1836840 IC50 = 7.0 nM 8.15
CHEMBL1836867 IC50 = 7.0 nM 8.15
CHEMBL1836810 IC50 = 8.0 nM 8.10
CHEMBL1836805 IC50 = 8.0 nM 8.10
CHEMBL1836862 IC50 = 9.0 nM 8.05
CHEMBL5416410 DASATINIB IC50 = 9.0 nM 8.05
CHEMBL1836754 IC50 = 10.0 nM 8.00
CHEMBL1836760 IC50 = 10.0 nM 8.00
CHEMBL1836799 IC50 = 10.0 nM 8.00
CHEMBL1836815 IC50 = 10.0 nM 8.00
CHEMBL1836843 IC50 = 10.0 nM 8.00
CHEMBL1836847 IC50 = 10.0 nM 8.00
CHEMBL1836853 IC50 = 10.0 nM 8.00
CHEMBL1836864 IC50 = 10.0 nM 8.00
CHEMBL1836796 IC50 = 11.0 nM 7.96
CHEMBL1836841 IC50 = 11.0 nM 7.96
CHEMBL1836761 IC50 = 12.0 nM 7.92
CHEMBL1836845 IC50 = 13.0 nM 7.89
CHEMBL1739550 IC50 = 13.0 nM 7.89
CHEMBL1836800 IC50 = 15.0 nM 7.82
CHEMBL1836837 IC50 = 16.0 nM 7.80
CHEMBL1836807 IC50 = 16.0 nM 7.80
CHEMBL1836838 IC50 = 18.0 nM 7.75
CHEMBL1836839 IC50 = 19.0 nM 7.72
CHEMBL1836803 IC50 = 23.0 nM 7.64
CHEMBL1836861 IC50 = 30.0 nM 7.52
CHEMBL1836801 IC50 = 32.0 nM 7.50
CHEMBL1836814 IC50 = 34.0 nM 7.47
CHEMBL1836804 IC50 = 38.0 nM 7.42
CHEMBL1836748 IC50 = 51.0 nM 7.29
CHEMBL1836813 IC50 = 60.0 nM 7.22
CHEMBL1836850 IC50 = 63.0 nM 7.20
CHEMBL1836849 IC50 = 64.0 nM 7.19
CHEMBL1836808 IC50 = 68.0 nM 7.17
CHEMBL1836855 IC50 = 70.0 nM 7.16
CHEMBL1836812 IC50 = 72.0 nM 7.14
CHEMBL1836797 IC50 = 75.0 nM 7.12
CHEMBL1836809 IC50 = 93.0 nM 7.03
CHEMBL1836757 IC50 = 97.0 nM 7.01
CHEMBL1836758 IC50 = 104.0 nM 6.98
CHEMBL1836848 IC50 = 124.0 nM 6.91