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Assay Detail

CHEMBL1049488

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

Functional
Immunosuppressive activity in C57BL/6 mouse lymphocytes cocultured with mitomycin C-stimulated BALB/c mouse splenocyte assessed as [3H]thymidine incorporation after 72 hrs by mixed lymphocyte reaction
29
Total Activities
29
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Mus musculus
Cell Type Lymphocyte
Confidence 1 — Organism
Curated By Autocuration

Target

Lymphocyte (CHEMBL612599)
Type CELL-LINE

Publication

Ring-fused pyrazole derivatives as potent inhibitors of lymphocyte-specific kinase (Lck): Structure, synthesis, and SAR.
Takayama T, Umemiya H, Amada H, Yabuuchi T, Koami T, Shiozawa F, Oka Y, Takaoka A, Yamaguchi A, Endo M, Sato M.
Bioorg Med Chem Lett (2010) 20 : 112 -116
PubMed 19945867 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 29 7.89 9.13

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL591325 1 9.13
CHEMBL591326 1 9.07
CHEMBL596079 1 8.96
CHEMBL601096 1 8.92
CHEMBL595401 1 8.89
CHEMBL591324 1 8.89
CHEMBL600873 1 8.82
CHEMBL596078 1 8.36
CHEMBL591322 1 8.19
CHEMBL603859 1 8.17
CHEMBL595624 1 8.09
CHEMBL591091 1 8.08
CHEMBL592262 1 7.92
CHEMBL592260 1 7.92
CHEMBL591793 1 7.82
CHEMBL591559 1 7.80
CHEMBL582959 1 7.68
CHEMBL595625 1 7.64
CHEMBL607366 1 7.60
CHEMBL595398 1 7.42
CHEMBL592267 1 7.30
CHEMBL606459 1 7.28
CHEMBL592261 1 7.24
CHEMBL592507 1 7.21
CHEMBL603737 1 7.06
CHEMBL604694 1 6.75
CHEMBL592026 1 6.52
CHEMBL592505 1 6.21
CHEMBL605724 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL591325 IC50 = 0.74 nM 9.13
CHEMBL591326 IC50 = 0.85 nM 9.07
CHEMBL596079 IC50 = 1.1 nM 8.96
CHEMBL601096 IC50 = 1.2 nM 8.92
CHEMBL595401 IC50 = 1.3 nM 8.89
CHEMBL591324 IC50 = 1.3 nM 8.89
CHEMBL600873 IC50 = 1.5 nM 8.82
CHEMBL596078 IC50 = 4.4 nM 8.36
CHEMBL591322 IC50 = 6.4 nM 8.19
CHEMBL603859 IC50 = 6.7 nM 8.17
CHEMBL595624 IC50 = 8.2 nM 8.09
CHEMBL591091 IC50 = 8.4 nM 8.08
CHEMBL592262 IC50 = 12.0 nM 7.92
CHEMBL592260 IC50 = 12.0 nM 7.92
CHEMBL591793 IC50 = 15.0 nM 7.82
CHEMBL591559 IC50 = 16.0 nM 7.80
CHEMBL582959 IC50 = 21.0 nM 7.68
CHEMBL595625 IC50 = 23.0 nM 7.64
CHEMBL607366 IC50 = 25.0 nM 7.60
CHEMBL595398 IC50 = 38.0 nM 7.42
CHEMBL592267 IC50 = 50.0 nM 7.30
CHEMBL606459 IC50 = 52.0 nM 7.28
CHEMBL592261 IC50 = 58.0 nM 7.24
CHEMBL592507 IC50 = 61.0 nM 7.21
CHEMBL603737 IC50 = 88.0 nM 7.06
CHEMBL604694 IC50 = 180.0 nM 6.75
CHEMBL592026 IC50 = 300.0 nM 6.52
CHEMBL592505 IC50 = 620.0 nM 6.21
CHEMBL605724 IC50 > 1000.0 nM -