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Assay Detail

CHEMBL1663311

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

Functional
Immunosuppressive activity in peripheral blood lymphocytes isolated from two individuals assessed as proliferation using [methyl-3H]thymidine by mixed lymphocyte reaction assay
33
Total Activities
33
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

Target

Lymphocyte (CHEMBL612599)
Type CELL-LINE

Publication

Discovery of 7-N-piperazinylthiazolo[5,4-d]pyrimidine analogues as a novel class of immunosuppressive agents with in vivo biological activity.
Jang MY, Lin Y, De Jonghe S, Gao LJ, Vanderhoydonck B, Froeyen M, Rozenski J, Herman J, Louat T, Van Belle K, Waer M, Herdewijn P.
J Med Chem (2011) 54 : 655 -668
PubMed 21171614 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 33 6.43 7.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1652683 1 7.92
CHEMBL1652684 1 7.92
CHEMBL1652682 1 7.40
CHEMBL1652676 1 7.40
CHEMBL1652677 1 7.30
CHEMBL160 CYCLOSPORINE 4.0 1 7.27
CHEMBL1652680 1 7.16
CHEMBL1652679 1 7.05
CHEMBL1652678 1 6.64
CHEMBL1652675 1 6.57
CHEMBL1652658 1 6.52
CHEMBL1652674 1 6.46
CHEMBL1652681 1 6.42
CHEMBL1652655 1 6.31
CHEMBL1652666 1 6.16
CHEMBL1652673 1 6.16
CHEMBL1652657 1 6.16
CHEMBL1652667 1 6.16
CHEMBL1652665 1 6.10
CHEMBL1652672 1 6.04
CHEMBL1652671 1 6.02
CHEMBL1652664 1 5.52
CHEMBL1652670 1 5.45
CHEMBL1652654 1 5.37
CHEMBL1652669 1 5.36
CHEMBL1652668 1 5.36
CHEMBL1652660 1 5.31
CHEMBL1643476 1 -
CHEMBL1652663 1 -
CHEMBL1652662 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1652683 IC50 = 12.0 nM 7.92
CHEMBL1652684 IC50 = 12.0 nM 7.92
CHEMBL1652682 IC50 = 40.0 nM 7.40
CHEMBL1652676 IC50 = 40.0 nM 7.40
CHEMBL1652677 IC50 = 50.0 nM 7.30
CHEMBL160 CYCLOSPORINE IC50 = 54.0 nM 7.27
CHEMBL1652680 IC50 = 70.0 nM 7.16
CHEMBL1652679 IC50 = 90.0 nM 7.05
CHEMBL1652678 IC50 = 230.0 nM 6.64
CHEMBL1652675 IC50 = 270.0 nM 6.57
CHEMBL1652658 IC50 = 300.0 nM 6.52
CHEMBL1652674 IC50 = 350.0 nM 6.46
CHEMBL1652681 IC50 = 380.0 nM 6.42
CHEMBL1652655 IC50 = 490.0 nM 6.31
CHEMBL1652657 IC50 = 700.0 nM 6.16
CHEMBL1652673 IC50 = 690.0 nM 6.16
CHEMBL1652667 IC50 = 700.0 nM 6.16
CHEMBL1652666 IC50 = 700.0 nM 6.16
CHEMBL1652665 IC50 = 800.0 nM 6.10
CHEMBL1652672 IC50 = 920.0 nM 6.04
CHEMBL1652671 IC50 = 960.0 nM 6.02
CHEMBL1652664 IC50 = 3000.0 nM 5.52
CHEMBL1652670 IC50 = 3540.0 nM 5.45
CHEMBL1652654 IC50 = 4300.0 nM 5.37
CHEMBL1652669 IC50 = 4400.0 nM 5.36
CHEMBL1652668 IC50 = 4380.0 nM 5.36
CHEMBL1652660 IC50 = 4900.0 nM 5.31
CHEMBL1643476 IC50 > 10000.0 nM -
CHEMBL1652663 IC50 > 10000.0 nM -
CHEMBL1652662 IC50 > 10000.0 nM -
CHEMBL1652661 IC50 > 10000.0 nM -
CHEMBL1652659 IC50 > 10000.0 nM -
CHEMBL1652656 IC50 > 10000.0 nM -