Assay Detail

CHEMBL5540262

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

Binding

Inhibition of PKCalpha (unknown origin)

ChEMBL ↗

Free Research Context This assay will appear in recent viewed items on this browser. Open the demo workspace to preview project-only review queues.

Research home Demo workspace

Target

Protein kinase C alpha type (CHEMBL299) ↗

Open DB target context

Use one target anchor to keep assay intent, target linkage, and tested compound review aligned.

Loading context

Protein kinase C alpha type (CHEMBL299) is the working anchor for this assay review. Loading the live Open DB target snapshot…

Primary target Protein kinase C alpha type

CHEMBL299

Anchored from Assay target.

Protein identity Protein kinase C alpha type

Disease frame Disease evidence pending

Open the live target snapshot or evidence card before reviewing assay metadata so target fit and disease framing stay reusable.

Review focus Open DB context pending

Open the live target snapshot before relying on this target frame across surface handoff.

Open target snapshot Open evidence card Search with this context

Total Activities

Compounds Tested

Activity Types

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

Discovery of Darovasertib (NVP-LXS196), a Pan-PKC Inhibitor for the Treatment of Metastatic Uveal Melanoma.

Visser M, Papillon JPN, Luzzio M, LaMarche MJ, Fan J, Michael W, Wang D, Zhang A, Straub C, Mathieu S, Kato M, Palermo M, Chen C, Ramsey T, Joud C, Barrett R, Vattay A, Guo R, Bric A, Chung F, Liang G, Romanowski MJ, Lam J, Thohan S, Atassi F, Wylie A, Cooke VG.
J Med Chem (2024) 67 : 1447 -1459
PubMed 38198520 · DOI

Activity Statistics

Type	Count	Avg pChEMBL	Best pChEMBL
IC50	2	7.90	8.19

Compounds Tested

Compound	Name	Phase	Activities	Best pChEMBL
CHEMBL565612	SOTRASTAURIN	2.0	1	8.19
CHEMBL3982723	DAROVASERTIB	2.0	1	7.60

Activity Data

Compound	Name	Type	Rel.	Value	Units	pChEMBL
CHEMBL565612	SOTRASTAURIN	IC50	=	6.4	nM	8.19
CHEMBL3982723	DAROVASERTIB	IC50	=	25.2	nM	7.60