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Assay Detail

CHEMBL2019768

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

Binding
Inhibition of human recombinant Sky using poly-GT as substrate and [33P]ATP after 40 mins by beta counting
42
Total Activities
42
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 receptor TYRO3 (CHEMBL5314)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Pyrazine-based Syk kinase inhibitors.
Forns P, Esteve C, Taboada L, Alonso JA, Orellana A, Maldonado M, Carreño C, Ramis I, López M, Miralpeix M, Vidal B.
Bioorg Med Chem Lett (2012) 22 : 2784 -2788
PubMed 22425453 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 42 6.86 7.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2018145 1 7.70
CHEMBL2018146 1 7.70
CHEMBL2018015 1 7.55
CHEMBL2018025 1 7.52
CHEMBL2018023 1 7.52
CHEMBL2018014 1 7.47
CHEMBL2018027 1 7.40
CHEMBL2018022 1 7.40
CHEMBL2018028 1 7.40
CHEMBL2018032 1 7.40
CHEMBL2018013 1 7.38
CHEMBL2018026 1 7.30
CHEMBL2018024 1 7.30
CHEMBL2018020 1 7.30
CHEMBL2018029 1 7.22
CHEMBL2018031 1 7.22
CHEMBL2018147 1 7.22
CHEMBL2018010 1 7.22
CHEMBL2018143 1 7.22
CHEMBL2018016 1 7.17
CHEMBL2018030 1 7.10
CHEMBL2018012 1 7.07
CHEMBL2018018 1 7.00
CHEMBL2018011 1 7.00
CHEMBL2018019 1 6.96
CHEMBL2018002 1 6.92
CHEMBL2018144 1 6.75
CHEMBL2018021 1 6.47
CHEMBL2018009 1 6.47
CHEMBL2018005 1 6.42

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2018145 IC50 = 20.0 nM 7.70
CHEMBL2018146 IC50 = 20.0 nM 7.70
CHEMBL2018015 IC50 = 28.0 nM 7.55
CHEMBL2018025 IC50 = 30.0 nM 7.52
CHEMBL2018023 IC50 = 30.0 nM 7.52
CHEMBL2018014 IC50 = 34.0 nM 7.47
CHEMBL2018032 IC50 = 40.0 nM 7.40
CHEMBL2018028 IC50 = 40.0 nM 7.40
CHEMBL2018027 IC50 = 40.0 nM 7.40
CHEMBL2018022 IC50 = 40.0 nM 7.40
CHEMBL2018013 IC50 = 42.0 nM 7.38
CHEMBL2018024 IC50 = 50.0 nM 7.30
CHEMBL2018020 IC50 = 50.0 nM 7.30
CHEMBL2018026 IC50 = 50.0 nM 7.30
CHEMBL2018143 IC50 = 60.0 nM 7.22
CHEMBL2018029 IC50 = 60.0 nM 7.22
CHEMBL2018010 IC50 = 60.0 nM 7.22
CHEMBL2018147 IC50 = 60.0 nM 7.22
CHEMBL2018031 IC50 = 60.0 nM 7.22
CHEMBL2018016 IC50 = 67.0 nM 7.17
CHEMBL2018030 IC50 = 80.0 nM 7.10
CHEMBL2018012 IC50 = 85.0 nM 7.07
CHEMBL2018011 IC50 = 100.0 nM 7.00
CHEMBL2018018 IC50 = 100.0 nM 7.00
CHEMBL2018019 IC50 = 110.0 nM 6.96
CHEMBL2018002 IC50 = 120.0 nM 6.92
CHEMBL2018144 IC50 = 180.0 nM 6.75
CHEMBL2018021 IC50 = 340.0 nM 6.47
CHEMBL2018009 IC50 = 340.0 nM 6.47
CHEMBL2018005 IC50 = 380.0 nM 6.42
CHEMBL2018001 IC50 = 380.0 nM 6.42
CHEMBL2018017 IC50 = 400.0 nM 6.40
CHEMBL2018006 IC50 = 490.0 nM 6.31
CHEMBL2018008 IC50 = 640.0 nM 6.19
CHEMBL2018004 IC50 = 650.0 nM 6.19
CHEMBL2017998 IC50 = 670.0 nM 6.17
CHEMBL2017999 IC50 = 1400.0 nM 5.85
CHEMBL2018000 IC50 = 1900.0 nM 5.72
CHEMBL2017997 IC50 = 2400.0 nM 5.62
CHEMBL2018003 IC50 = 2600.0 nM 5.58
CHEMBL2018148 IC50 = 10000.0 nM 5.00
CHEMBL2018007 IC50 > 50000.0 nM -