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Assay Detail

CHEMBL4399600

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

Functional
Inhibition of IL-2 secretion from human PBMC cells stimulated with anti-CD3/CD28 measured after 24 hrs by bead-based FLISA
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

PBMC (CHEMBL613107)
Type CELL-LINE
Organism Homo sapiens

Publication

Discovery of Selective, Orally Bioavailable Pyrazolopyridine Inhibitors of Protein Kinase Cθ (PKCθ) That Ameliorate Symptoms of Experimental Autoimmune Encephalomyelitis.
Collier PN, Twin HC, Knegtel RMA, Boyall D, Brenchley G, Davis CJ, Keily S, Mak C, Miller A, Pierard F, Settimo L, Bolton CM, Chiu P, Curnock A, Doyle E, Tanner AJ, Jimenez JM.
ACS Med Chem Lett (2019) 10 : 1134 -1139
PubMed 31417666 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 19 6.78 8.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4569479 1 8.00
CHEMBL4469412 1 7.70
CHEMBL4528271 1 7.70
CHEMBL4590477 1 7.22
CHEMBL4589844 1 7.05
CHEMBL4532737 1 7.00
CHEMBL4457150 1 6.89
CHEMBL4461370 1 6.77
CHEMBL4454086 1 6.70
CHEMBL4461649 1 6.68
CHEMBL4567363 1 6.60
CHEMBL4522851 1 6.58
CHEMBL4566843 1 6.52
CHEMBL4541215 1 6.48
CHEMBL4584166 1 6.46
CHEMBL4587816 1 6.35
CHEMBL4435004 1 6.26
CHEMBL4444700 1 6.24
CHEMBL4447253 1 5.57

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4569479 IC50 = 10.0 nM 8.00
CHEMBL4469412 IC50 = 20.0 nM 7.70
CHEMBL4528271 IC50 = 20.0 nM 7.70
CHEMBL4590477 IC50 = 60.0 nM 7.22
CHEMBL4589844 IC50 = 90.0 nM 7.05
CHEMBL4532737 IC50 = 100.0 nM 7.00
CHEMBL4457150 IC50 = 130.0 nM 6.89
CHEMBL4461370 IC50 = 170.0 nM 6.77
CHEMBL4454086 IC50 = 200.0 nM 6.70
CHEMBL4461649 IC50 = 210.0 nM 6.68
CHEMBL4567363 IC50 = 250.0 nM 6.60
CHEMBL4522851 IC50 = 260.0 nM 6.58
CHEMBL4566843 IC50 = 300.0 nM 6.52
CHEMBL4541215 IC50 = 330.0 nM 6.48
CHEMBL4584166 IC50 = 350.0 nM 6.46
CHEMBL4587816 IC50 = 450.0 nM 6.35
CHEMBL4435004 IC50 = 550.0 nM 6.26
CHEMBL4444700 IC50 = 580.0 nM 6.24
CHEMBL4447253 IC50 = 2700.0 nM 5.57