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Assay Detail

CHEMBL902548

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Functional
Inhibition of T cell activation in human mixed lymphocyte reaction
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type T-cell
Confidence 1 — Organism
Curated By Autocuration

Target

T-cell (CHEMBL614309)
Type CELL-LINE

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 6.09 6.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL248081 1 6.92
CHEMBL248080 1 6.86
CHEMBL247880 1 6.64
CHEMBL247468 1 6.64
CHEMBL247677 1 6.47
CHEMBL248286 1 6.44
CHEMBL247878 1 6.36
CHEMBL247479 1 6.33
CHEMBL247866 1 6.27
CHEMBL247480 1 6.17
CHEMBL399212 1 6.08
CHEMBL247667 1 5.78
CHEMBL247272 1 5.77
CHEMBL247068 1 5.67
CHEMBL399008 1 5.62
CHEMBL247469 1 5.61
CHEMBL248079 1 5.51
CHEMBL394490 1 5.49
CHEMBL247070 1 5.05

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL248081 IC50 = 121.0 nM 6.92
CHEMBL248080 IC50 = 138.0 nM 6.86
CHEMBL247880 IC50 = 227.0 nM 6.64
CHEMBL247468 IC50 = 227.0 nM 6.64
CHEMBL247677 IC50 = 337.0 nM 6.47
CHEMBL248286 IC50 = 360.0 nM 6.44
CHEMBL247878 IC50 = 437.0 nM 6.36
CHEMBL247479 IC50 = 464.0 nM 6.33
CHEMBL247866 IC50 = 533.0 nM 6.27
CHEMBL247480 IC50 = 670.0 nM 6.17
CHEMBL399212 IC50 = 825.0 nM 6.08
CHEMBL247667 IC50 = 1672.0 nM 5.78
CHEMBL247272 IC50 = 1710.0 nM 5.77
CHEMBL247068 IC50 = 2130.0 nM 5.67
CHEMBL399008 IC50 = 2376.0 nM 5.62
CHEMBL247469 IC50 = 2452.0 nM 5.61
CHEMBL248079 IC50 = 3084.0 nM 5.51
CHEMBL394490 IC50 = 3223.0 nM 5.49
CHEMBL247070 IC50 = 8950.0 nM 5.05