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Assay Detail

CHEMBL4137134

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

Binding
Displacement of [3H]PDBu from full length recombinant human PKCalpha expressed in baculovirus expression system after 5 mins by scintillation counting
41
Total Activities
41
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

α-Arylidene Diacylglycerol-Lactones (DAG-Lactones) as Selective Ras Guanine-Releasing Protein 3 (RasGRP3) Ligands.
Ann J, Czikora A, Saini AS, Zhou X, Mitchell GA, Lewin NE, Peach ML, Blumberg PM, Lee J.
J Med Chem (2018) 61 : 6261 -6276
PubMed 29860841 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 41 6.99 7.87

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4160361 1 7.87
CHEMBL4167900 1 7.81
CHEMBL4172461 1 7.60
CHEMBL4160540 1 7.59
CHEMBL4167589 1 7.59
CHEMBL4175934 1 7.56
CHEMBL4175761 1 7.54
CHEMBL4174723 1 7.54
CHEMBL4175128 1 7.52
CHEMBL4174397 1 7.52
CHEMBL519741 1 7.50
CHEMBL4161221 1 7.50
CHEMBL4175333 1 7.43
CHEMBL488667 1 7.41
CHEMBL4160647 1 7.37
CHEMBL4164402 1 7.20
CHEMBL4162516 1 7.18
CHEMBL4163130 1 7.14
CHEMBL4161062 1 7.10
CHEMBL461374 1 7.08
CHEMBL461754 1 7.07
CHEMBL4163809 1 6.95
CHEMBL4165117 1 6.94
CHEMBL4169454 1 6.90
CHEMBL508870 1 6.89
CHEMBL4167264 1 6.87
CHEMBL4168968 1 6.84
CHEMBL4167457 1 6.74
CHEMBL472521 1 6.73
CHEMBL452307 1 6.60

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4160361 Ki = 13.6 nM 7.87
CHEMBL4167900 Ki = 15.6 nM 7.81
CHEMBL4172461 Ki = 25.2 nM 7.60
CHEMBL4160540 Ki = 25.65 nM 7.59
CHEMBL4167589 Ki = 25.4 nM 7.59
CHEMBL4175934 Ki = 27.6 nM 7.56
CHEMBL4175761 Ki = 29.0 nM 7.54
CHEMBL4174723 Ki = 28.77 nM 7.54
CHEMBL4175128 Ki = 30.4 nM 7.52
CHEMBL4174397 Ki = 30.1 nM 7.52
CHEMBL4161221 Ki = 31.3 nM 7.50
CHEMBL519741 Ki = 31.7 nM 7.50
CHEMBL4175333 Ki = 37.0 nM 7.43
CHEMBL488667 Ki = 39.0 nM 7.41
CHEMBL4160647 Ki = 42.3 nM 7.37
CHEMBL4164402 Ki = 62.5 nM 7.20
CHEMBL4162516 Ki = 65.9 nM 7.18
CHEMBL4163130 Ki = 72.0 nM 7.14
CHEMBL4161062 Ki = 79.1 nM 7.10
CHEMBL461374 Ki = 82.2 nM 7.08
CHEMBL461754 Ki = 84.7 nM 7.07
CHEMBL4163809 Ki = 112.0 nM 6.95
CHEMBL4165117 Ki = 114.0 nM 6.94
CHEMBL4169454 Ki = 127.0 nM 6.90
CHEMBL508870 Ki = 128.0 nM 6.89
CHEMBL4167264 Ki = 135.0 nM 6.87
CHEMBL4168968 Ki = 146.0 nM 6.84
CHEMBL4167457 Ki = 183.8 nM 6.74
CHEMBL472521 Ki = 186.0 nM 6.73
CHEMBL452307 Ki = 252.0 nM 6.60
CHEMBL4171253 Ki = 249.0 nM 6.60
CHEMBL4170226 Ki = 375.0 nM 6.43
CHEMBL4175742 Ki = 383.0 nM 6.42
CHEMBL4160009 Ki = 439.0 nM 6.36
CHEMBL488674 Ki = 446.0 nM 6.35
CHEMBL470094 Ki = 1188.0 nM 5.92
CHEMBL487483 Ki = 1480.0 nM 5.83
CHEMBL4170651 Ki = 2308.0 nM 5.64
CHEMBL4173300 Ki = 3640.0 nM 5.44
CHEMBL4168982 Ki > 30000.0 nM -
CHEMBL4164472 Ki > 30000.0 nM -