Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL902547

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

Binding
Inhibition of Lck
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Intermediate

Target

Tyrosine-protein kinase Lck (CHEMBL258)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of 4-amino-5,6-biaryl-furo[2,3-d]pyrimidines as inhibitors of Lck: development of an expedient and divergent synthetic route and preliminary SAR.
DiMauro EF, Newcomb J, Nunes JJ, Bemis JE, Boucher C, Buchanan JL, Buckner WH, Cheng A, Faust T, Hsieh F, Huang X, Lee JH, Marshall TL, Martin MW, McGowan DC, Schneider S, Turci SM, White RD, Zhu X.
Bioorg Med Chem Lett (2007) 17 : 2305 -2309
PubMed 17280833 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 19 7.64 8.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL247667 1 8.30
CHEMBL247479 1 8.22
CHEMBL247677 1 8.22
CHEMBL399212 1 8.10
CHEMBL247468 1 8.05
CHEMBL247480 1 7.96
CHEMBL247880 1 7.96
CHEMBL247878 1 7.96
CHEMBL248286 1 7.85
CHEMBL247469 1 7.85
CHEMBL394490 1 7.66
CHEMBL248081 1 7.66
CHEMBL248080 1 7.57
CHEMBL247866 1 7.44
CHEMBL248079 1 7.38
CHEMBL247272 1 7.09
CHEMBL399008 1 7.08
CHEMBL247070 1 6.91
CHEMBL247068 1 5.92

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL247667 IC50 = 5.0 nM 8.30
CHEMBL247479 IC50 = 6.0 nM 8.22
CHEMBL247677 IC50 = 6.0 nM 8.22
CHEMBL399212 IC50 = 8.0 nM 8.10
CHEMBL247468 IC50 = 9.0 nM 8.05
CHEMBL247480 IC50 = 11.0 nM 7.96
CHEMBL247880 IC50 = 11.0 nM 7.96
CHEMBL247878 IC50 = 11.0 nM 7.96
CHEMBL248286 IC50 = 14.0 nM 7.85
CHEMBL247469 IC50 = 14.0 nM 7.85
CHEMBL394490 IC50 = 22.0 nM 7.66
CHEMBL248081 IC50 = 22.0 nM 7.66
CHEMBL248080 IC50 = 27.0 nM 7.57
CHEMBL247866 IC50 = 36.0 nM 7.44
CHEMBL248079 IC50 = 42.0 nM 7.38
CHEMBL247272 IC50 = 81.0 nM 7.09
CHEMBL399008 IC50 = 83.0 nM 7.08
CHEMBL247070 IC50 = 122.0 nM 6.91
CHEMBL247068 IC50 = 1210.0 nM 5.92