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Assay Detail

CHEMBL871537

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

Binding
Inhibition of Src by HTRF kinase assay
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Expert

Target

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

Publication

Discovery of aminoquinazolines as potent, orally bioavailable inhibitors of Lck: synthesis, SAR, and in vivo anti-inflammatory activity.
DiMauro EF, Newcomb J, Nunes JJ, Bemis JE, Boucher C, Buchanan JL, Buckner WH, Cee VJ, Chai L, Deak HL, Epstein LF, Faust T, Gallant P, Geuns-Meyer SD, Gore A, Gu Y, Henkle B, Hodous BL, Hsieh F, Huang X, Kim JL, Lee JH, Martin MW, Masse CE, McGowan DC, Metz D, Mohn D, Morgenstern KA, Oliveira-dos-Santos A, Patel VF, Powers D, Rose PE, Schneider S, Tomlinson SA, Tudor YY, Turci SM, Welcher AA, White RD, Zhao H, Zhu L, Zhu X.
J Med Chem (2006) 49 : 5671 -5686
PubMed 16970394 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 8.24 8.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL215943 1 8.70
CHEMBL386661 1 7.77

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL215943 IC50 = 2.0 nM 8.70
CHEMBL386661 IC50 = 17.0 nM 7.77