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Assay Detail

CHEMBL2156129

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Functional
Immunosuppressive activity in human lymphocytes assessed as alloantigen-induced T cell proliferation by mixed lymphocyte reaction assay
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type Lymphocyte
Confidence 1 — Organism
Curated By Autocuration

Publication

Structure-activity relationship and pharmacokinetic studies of sotrastaurin (AEB071), a promising novel medicine for prevention of graft rejection and treatment of psoriasis.
Wagner J, von Matt P, Faller B, Cooke NG, Albert R, Sedrani R, Wiegand H, Jean C, Beerli C, Weckbecker G, Evenou JP, Zenke G, Cottens S.
J Med Chem (2011) 54 : 6028 -6039
PubMed 21797275 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 7 7.43 7.82

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2151411 1 7.82
CHEMBL568580 1 7.60
CHEMBL565612 SOTRASTAURIN 2.0 1 7.43
CHEMBL2153748 1 7.43
CHEMBL1996510 1 7.29
CHEMBL2151415 1 7.00
CHEMBL2153747 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2151411 IC50 = 15.0 nM 7.82
CHEMBL568580 IC50 = 25.0 nM 7.60
CHEMBL565612 SOTRASTAURIN IC50 = 37.0 nM 7.43
CHEMBL2153748 IC50 = 37.0 nM 7.43
CHEMBL1996510 IC50 = 51.0 nM 7.29
CHEMBL2151415 IC50 = 99.0 nM 7.00
CHEMBL2153747 IC50 - -