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Assay Detail

CHEMBL3889158

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Binding
In Vitro Inhibition Activity Assay: The compounds of formula I were tested for their activity on different PKC isoforms according to a published method (D. Geiges et al. Biochem. Pharmacol. 1997; 53:865-875) The assay is performed in a 96-well polypropylene microtiterplate (Costar 3794) that has been previously siliconized with Sigmacote (Sigma SL-2). The reaction mixture (50 μL) contains 10 μL of the relevant PKC isozyme together with 25 μL of the PKC inhibitor compound and 15 μL of a mix solution that contains 200 μg/mL protamine sulfate, 10 mM Mg(NO3)2, 10 μM ATP (Boehringer 519987) and 3750 Bq of 33P-ATP (Hartmann Analytic SFC301, 110 TBq/mmol) in 20 mM Tris-buffer pH 7.4+0.1% BSA. Incubation was performed for 15 minutes at 32° C. in a microtiterplate shaking incubator (Biolabo Scientific Instruments). Reaction was stopped by adding 10 μl of 0.5 M Na2EDTA, pH 7.4. 50 μl of mixture are pipetted onto a pre-wetted phosphocellulose paper (Whatmann 3698-915) under gentle pressure.
ChEMBL ↗
123
Total Activities
116
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

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

Publication

Protein kinase C inhibitors and methods of their use
(2016)

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 123 9.12 9.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3984070 — — 1 9.89
CHEMBL3963605 — — 1 9.89
CHEMBL3895998 — — 1 9.89
CHEMBL3920517 — — 1 9.89
CHEMBL3893533 — — 1 9.89
CHEMBL3966595 — — 2 9.89
CHEMBL3982497 — — 1 9.89
CHEMBL3966643 — — 2 9.89
CHEMBL3969856 — — 1 9.89
CHEMBL3958917 — — 1 9.89
CHEMBL3983009 — — 1 9.89
CHEMBL3970090 — — 1 9.89
CHEMBL3943147 — — 1 9.89
CHEMBL3980746 — — 2 9.89
CHEMBL3951893 — — 1 9.89
CHEMBL3984009 — — 1 9.89
CHEMBL3958761 — — 1 9.89
CHEMBL3932204 — — 2 9.89
CHEMBL3892099 — — 1 9.89
CHEMBL3957715 — — 1 9.89
CHEMBL3945647 — — 1 9.85
CHEMBL3943813 — — 1 9.82
CHEMBL3987185 — — 1 9.80
CHEMBL3970893 — — 1 9.77
CHEMBL3976541 — — 1 9.72
CHEMBL3942619 — — 1 9.72
CHEMBL3957149 — — 1 9.70
CHEMBL3901073 — — 1 9.66
CHEMBL4115475 — — 1 9.62
CHEMBL3915489 — — 1 9.60

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3958917 — IC50 = 0.13 nM 9.89
CHEMBL3963605 — IC50 = 0.13 nM 9.89
CHEMBL3932204 — IC50 = 0.13 nM 9.89
CHEMBL3958761 — IC50 = 0.13 nM 9.89
CHEMBL3984009 — IC50 = 0.13 nM 9.89
CHEMBL3951893 — IC50 = 0.13 nM 9.89
CHEMBL3980746 — IC50 = 0.13 nM 9.89
CHEMBL3943147 — IC50 = 0.13 nM 9.89
CHEMBL3970090 — IC50 = 0.13 nM 9.89
CHEMBL3983009 — IC50 = 0.13 nM 9.89
CHEMBL3957715 — IC50 = 0.13 nM 9.89
CHEMBL3969856 — IC50 = 0.13 nM 9.89
CHEMBL3966643 — IC50 = 0.13 nM 9.89
CHEMBL3982497 — IC50 = 0.13 nM 9.89
CHEMBL3966595 — IC50 = 0.13 nM 9.89
CHEMBL3893533 — IC50 = 0.13 nM 9.89
CHEMBL3980746 — IC50 = 0.13 nM 9.89
CHEMBL3966643 — IC50 = 0.13 nM 9.89
CHEMBL3966595 — IC50 = 0.13 nM 9.89
CHEMBL3920517 — IC50 = 0.13 nM 9.89
CHEMBL3895998 — IC50 = 0.13 nM 9.89
CHEMBL3984070 — IC50 = 0.13 nM 9.89
CHEMBL3892099 — IC50 = 0.13 nM 9.89
CHEMBL3945647 — IC50 = 0.14 nM 9.85
CHEMBL3943813 — IC50 = 0.15 nM 9.82
CHEMBL3987185 — IC50 = 0.16 nM 9.80
CHEMBL3970893 — IC50 = 0.17 nM 9.77
CHEMBL3942619 — IC50 = 0.19 nM 9.72
CHEMBL3976541 — IC50 = 0.19 nM 9.72
CHEMBL3957149 — IC50 = 0.2 nM 9.70
CHEMBL3932204 — IC50 = 0.2 nM 9.70
CHEMBL3901073 — IC50 = 0.22 nM 9.66
CHEMBL4115475 — IC50 = 0.24 nM 9.62
CHEMBL3915489 — IC50 = 0.25 nM 9.60
CHEMBL3912038 — IC50 = 0.25 nM 9.60
CHEMBL3960459 — IC50 = 0.25 nM 9.60
CHEMBL4109540 — IC50 = 0.26 nM 9.59
CHEMBL3967547 — IC50 = 0.27 nM 9.57
CHEMBL3975977 — IC50 = 0.29 nM 9.54
CHEMBL3893839 — IC50 = 0.3 nM 9.52
CHEMBL3946659 — IC50 = 0.3 nM 9.52
CHEMBL3893246 — IC50 = 0.32 nM 9.49
CHEMBL3950697 — IC50 = 0.33 nM 9.48
CHEMBL3904204 — IC50 = 0.33 nM 9.48
CHEMBL3907088 — IC50 = 0.35 nM 9.46
CHEMBL3965722 — IC50 = 0.36 nM 9.44
CHEMBL3937993 — IC50 = 0.4 nM 9.40
CHEMBL3908251 — IC50 = 0.4 nM 9.40
CHEMBL3942560 — IC50 = 0.4 nM 9.40
CHEMBL3909349 — IC50 = 0.43 nM 9.37