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Assay Detail

CHEMBL4675676

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

Binding
Inhibition of human ERG by plate-based planar patch clamp method
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

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 5.16 5.66

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4784088 1 5.66
CHEMBL4751083 1 5.52
CHEMBL4753141 1 5.44
CHEMBL4786316 1 5.35
CHEMBL4762290 1 5.31
CHEMBL4753469 1 5.14
CHEMBL4792651 1 5.00
CHEMBL4752008 1 4.96
CHEMBL4780257 1 4.92
CHEMBL4784783 1 4.85
CHEMBL4744190 1 4.64
CHEMBL3622956 1 -
CHEMBL4793844 1 -
CHEMBL4757235 1 -
CHEMBL4790107 1 -
CHEMBL4753164 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4784088 IC50 = 2200.0 nM 5.66
CHEMBL4751083 IC50 = 3000.0 nM 5.52
CHEMBL4753141 IC50 = 3600.0 nM 5.44
CHEMBL4786316 IC50 = 4500.0 nM 5.35
CHEMBL4762290 IC50 = 4900.0 nM 5.31
CHEMBL4753469 IC50 = 7300.0 nM 5.14
CHEMBL4792651 IC50 = 10000.0 nM 5.00
CHEMBL4752008 IC50 = 11000.0 nM 4.96
CHEMBL4780257 IC50 = 12000.0 nM 4.92
CHEMBL4784783 IC50 = 14000.0 nM 4.85
CHEMBL4744190 IC50 = 23000.0 nM 4.64
CHEMBL3622956 IC50 - -
CHEMBL4793844 IC50 - -
CHEMBL4757235 IC50 > 40000.0 nM -
CHEMBL4790107 IC50 > 40000.0 nM -
CHEMBL4753164 IC50 > 40000.0 nM -