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Assay Detail

CHEMBL1053102

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Functional
Antiproliferative activity against JAK3 expressing human resting Jurkat cells
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Jurkat (CHEMBL397)
Type CELL-LINE
Organism Homo sapiens

Publication

Synthetic staurosporines via a ring closing metathesis strategy as potent JAK3 inhibitors and modulators of allergic responses.
Wilson LJ, Malaviya R, Yang C, Argentieri R, Wang B, Chen X, Murray WV, Cavender D.
Bioorg Med Chem Lett (2009) 19 : 3333 -3338
PubMed 19427203 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 15 5.63 6.51

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL388978 STAUROSPORINE 1 6.51
CHEMBL558241 1 6.21
CHEMBL557559 1 5.80
CHEMBL562934 1 5.25
CHEMBL558115 1 5.00
CHEMBL559787 1 5.00
CHEMBL557846 1 -
CHEMBL563588 1 -
CHEMBL565066 1 -
CHEMBL557101 1 -
CHEMBL564940 1 -
CHEMBL550791 1 -
CHEMBL16958 STAUROSPORINONE 1 -
CHEMBL563795 1 -
CHEMBL557709 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL388978 STAUROSPORINE IC50 = 311.0 nM 6.51
CHEMBL558241 IC50 = 616.0 nM 6.21
CHEMBL557559 IC50 = 1600.0 nM 5.80
CHEMBL562934 IC50 = 5670.0 nM 5.25
CHEMBL558115 IC50 = 10000.0 nM 5.00
CHEMBL559787 IC50 = 10000.0 nM 5.00
CHEMBL557846 IC50 > 10000.0 nM -
CHEMBL563588 IC50 > 10000.0 nM -
CHEMBL565066 IC50 > 10000.0 nM -
CHEMBL557101 IC50 > 10000.0 nM -
CHEMBL564940 IC50 > 10000.0 nM -
CHEMBL550791 IC50 > 10000.0 nM -
CHEMBL16958 STAUROSPORINONE IC50 - -
CHEMBL563795 IC50 - -
CHEMBL557709 IC50 > 10000.0 nM -