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Assay Detail

CHEMBL978650

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

Binding
Inhibition of chicken cSrc single mutant expressed in Escherichia coli
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Gallus gallus
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Proto-oncogene tyrosine-protein kinase Src (CHEMBL3655)
Type SINGLE PROTEIN
Organism Gallus gallus

Publication

Structural insights into how irreversible inhibitors can overcome drug resistance in EGFR.
Michalczyk A, Klüter S, Rode HB, Simard JR, Grütter C, Rabiller M, Rauh D.
Bioorg Med Chem (2008) 16 : 3482 -3488
PubMed 18316192 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 6.07 6.63

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL94061 1 6.63
CHEMBL285063 1 6.47
CHEMBL553 ERLOTINIB 4.0 1 6.00
CHEMBL188762 1 5.19

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL94061 IC50 = 236.0 nM 6.63
CHEMBL285063 IC50 = 340.0 nM 6.47
CHEMBL553 ERLOTINIB IC50 = 990.0 nM 6.00
CHEMBL188762 IC50 = 6400.0 nM 5.19