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Assay Detail

CHEMBL4675674

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

Binding
Inhibition of recombinant full length SYK (unknown origin) by biochemical Omnia assay
ChEMBL ↗
16
Total Activities
16
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 SYK (CHEMBL2599) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Optimization of a series of potent, selective and orally bioavailable SYK inhibitors.
Grimster NP,Gingipalli L,Barlaam B,Su Q,Zheng X,Watson D,Wang H,Simpson I,Pike A,Balazs A,Boiko S,Ikeda TP,Impastato AC,Jones NH,Kawatkar S,Kemmitt P,Lamont S,Patel J,Read J,Sarkar U,Sha L,Tomlinson RC,Wang H,Wilson DM,Zehnder TE,Wang L,Wang P,Goldberg FW,Shao W,Fawell S,Dry H,Dowling JE,Edmondson SD
Bioorg Med Chem Lett (2020) 30 : 127433 -127433
PubMed 32717371 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 16 9.78 10.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3622956 — — 1 10.52
CHEMBL4744190 — — 1 10.52
CHEMBL4780257 — — 1 10.22
CHEMBL4753469 — — 1 10.05
CHEMBL4753141 — — 1 9.96
CHEMBL4784088 — — 1 9.89
CHEMBL4752008 — — 1 9.85
CHEMBL4753164 — — 1 9.72
CHEMBL4792651 — — 1 9.70
CHEMBL4786316 — — 1 9.68
CHEMBL4762290 — — 1 9.66
CHEMBL4784783 — — 1 9.62
CHEMBL4790107 — — 1 9.59
CHEMBL4751083 — — 1 9.51
CHEMBL4793844 — — 1 9.03
CHEMBL4757235 — — 1 9.02

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3622956 — IC50 = 0.03 nM 10.52
CHEMBL4744190 — IC50 = 0.03 nM 10.52
CHEMBL4780257 — IC50 = 0.06 nM 10.22
CHEMBL4753469 — IC50 = 0.09 nM 10.05
CHEMBL4753141 — IC50 = 0.11 nM 9.96
CHEMBL4784088 — IC50 = 0.13 nM 9.89
CHEMBL4752008 — IC50 = 0.14 nM 9.85
CHEMBL4753164 — IC50 = 0.19 nM 9.72
CHEMBL4792651 — IC50 = 0.2 nM 9.70
CHEMBL4786316 — IC50 = 0.21 nM 9.68
CHEMBL4762290 — IC50 = 0.22 nM 9.66
CHEMBL4784783 — IC50 = 0.24 nM 9.62
CHEMBL4790107 — IC50 = 0.26 nM 9.59
CHEMBL4751083 — IC50 = 0.31 nM 9.51
CHEMBL4793844 — IC50 = 0.94 nM 9.03
CHEMBL4757235 — IC50 = 0.95 nM 9.02