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Assay Detail

CHEMBL4399587

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

Binding
Inhibition of protein kinase A (unknown origin) using Kemptide (LRRASLG) as substrate incubated for 15 mins in presence of ATP by spectrophotometric analysis
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

cAMP-dependent protein kinase catalytic subunit alpha (CHEMBL4101)
Type SINGLE PROTEIN
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
Ki 2 7.24 7.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4457150 1 7.52
CHEMBL4453941 1 6.96

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4457150 Ki = 30.0 nM 7.52
CHEMBL4453941 Ki = 110.0 nM 6.96