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Assay Detail

CHEMBL3606410

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

Binding
Inhibition of cSrc T338M/S345C mutant (unknown origin) pre-incubated for 30 mins before substrate and ATP addition by HTRF assay
6
Total Activities
6
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

Proto-oncogene tyrosine-protein kinase Src (CHEMBL267)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Targeting Drug Resistance in EGFR with Covalent Inhibitors: A Structure-Based Design Approach.
Engel J, Richters A, Getlik M, Tomassi S, Keul M, Termathe M, Lategahn J, Becker C, Mayer-Wrangowski S, Grütter C, Uhlenbrock N, Krüll J, Schaumann N, Eppmann S, Kibies P, Hoffgaard F, Heil J, Menninger S, Ortiz-Cuaran S, Heuckmann JM, Tinnefeld V, Zahedi RP, Sos ML, Schultz-Fademrecht C, Thomas RK, Kast SM, Rauh D.
J Med Chem (2015) 58 : 6844 -6863
PubMed 26275028 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 7.18 7.77

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3604937 1 7.77
CHEMBL3604921 1 7.55
CHEMBL1232944 1 7.37
CHEMBL3604910 1 7.32
CHEMBL3604938 1 6.58
CHEMBL3604924 1 6.46

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3604937 IC50 = 17.0 nM 7.77
CHEMBL3604921 IC50 = 28.0 nM 7.55
CHEMBL1232944 IC50 = 43.0 nM 7.37
CHEMBL3604910 IC50 = 48.0 nM 7.32
CHEMBL3604938 IC50 = 260.0 nM 6.58
CHEMBL3604924 IC50 = 349.0 nM 6.46