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Assay Detail

CHEMBL819920

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

Binding
Inhibition of tyrosine kinase activity in ER 22 membrane fraction by competition with the RRSrc peptide using [32P]-gamma ATP as radioligand
21
Total Activities
21
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Synthesis and structure-activity studies of a series of [(hydroxybenzyl)amino]salicylates as inhibitors of EGF receptor-associated tyrosine kinase activity.
Chen H, Boiziau J, Parker F, Maroun R, Tocque B, Roques BP, Garbay-Jaureguiberry C.
J Med Chem (1993) 36 : 4094 -4098
PubMed 8258833 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 21 5.49 7.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL319620 LAVENDUSTIN C 1 7.52
CHEMBL133283 1 6.70
CHEMBL131653 1 6.22
CHEMBL334334 1 5.80
CHEMBL129907 1 5.62
CHEMBL316764 1 5.30
CHEMBL129930 1 5.30
CHEMBL131092 1 5.00
CHEMBL131407 1 4.60
CHEMBL132907 1 4.35
CHEMBL133758 1 4.00
CHEMBL130893 1 -
CHEMBL340449 1 -
CHEMBL130116 1 -
CHEMBL130694 1 -
CHEMBL334739 1 -
CHEMBL130117 1 -
CHEMBL130523 1 -
CHEMBL129989 1 -
CHEMBL335074 1 -
CHEMBL133563 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL319620 LAVENDUSTIN C IC50 = 30.0 nM 7.52
CHEMBL133283 IC50 = 200.0 nM 6.70
CHEMBL131653 IC50 = 600.0 nM 6.22
CHEMBL334334 IC50 = 1600.0 nM 5.80
CHEMBL129907 IC50 = 2400.0 nM 5.62
CHEMBL316764 IC50 = 5000.0 nM 5.30
CHEMBL129930 IC50 = 5000.0 nM 5.30
CHEMBL131092 IC50 = 10000.0 nM 5.00
CHEMBL131407 IC50 = 25000.0 nM 4.60
CHEMBL132907 IC50 = 45000.0 nM 4.35
CHEMBL133758 IC50 = 100000.0 nM 4.00
CHEMBL130893 IC50 > 10000.0 nM -
CHEMBL340449 IC50 > 10000.0 nM -
CHEMBL130116 IC50 > 10000.0 nM -
CHEMBL130694 IC50 > 100000.0 nM -
CHEMBL334739 IC50 > 100000.0 nM -
CHEMBL130117 IC50 > 10000.0 nM -
CHEMBL130523 IC50 > 100000.0 nM -
CHEMBL129989 IC50 > 100000.0 nM -
CHEMBL335074 IC50 > 100000.0 nM -
CHEMBL133563 IC50 > 100000.0 nM -