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Assay Detail

CHEMBL997396

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Binding
Inhibition of human recombinant PKCalpha
8
Total Activities
8
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

Protein kinase C alpha type (CHEMBL299)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Phenylethanoid glycosides from Digitalis purpurea and Penstemon linarioides with PKCalpha-inhibitory activity.
Zhou BN, Bahler BD, Hofmann GA, Mattern MR, Johnson RK, Kingston DG.
J Nat Prod (1998) 61 : 1410 -1412
PubMed 9834166 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 8 5.21 6.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL481635 CALCEOLARIOSIDE A 1 6.22
CHEMBL504363 FORSYTHIASIDE 1 5.72
CHEMBL518414 CALCEOLARIOSIDE B 1 5.34
CHEMBL444478 ACETOSIDE 2.0 1 5.03
CHEMBL452413 PLANTAINOSIDE D 1 4.83
CHEMBL450121 LEUCOSCEPTOSIDE A 1 4.72
CHEMBL499145 POLIUMOSIDE 1 4.61
CHEMBL506920 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL481635 CALCEOLARIOSIDE A IC50 = 600.0 nM 6.22
CHEMBL504363 FORSYTHIASIDE IC50 = 1900.0 nM 5.72
CHEMBL518414 CALCEOLARIOSIDE B IC50 = 4600.0 nM 5.34
CHEMBL444478 ACETOSIDE IC50 = 9300.0 nM 5.03
CHEMBL452413 PLANTAINOSIDE D IC50 = 14800.0 nM 4.83
CHEMBL450121 LEUCOSCEPTOSIDE A IC50 = 19000.0 nM 4.72
CHEMBL499145 POLIUMOSIDE IC50 = 24400.0 nM 4.61
CHEMBL506920 IC50 = 125000.0 nM -