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Assay Detail

CHEMBL1219829

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

Binding
Inhibition of PKD2 ( assessed as residual activity at 1 uM ) by TR-FRET assay
4
Total Activities
2
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

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

Target

Serine/threonine-protein kinase D2 (CHEMBL4900)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Identification of orally available naphthyridine protein kinase D inhibitors.
Meredith EL, Ardayfio O, Beattie K, Dobler MR, Enyedy I, Gaul C, Hosagrahara V, Jewell C, Koch K, Lee W, Lehmann H, McKinsey TA, Miranda K, Pagratis N, Pancost M, Patnaik A, Phan D, Plato C, Qian M, Rajaraman V, Rao C, Rozhitskaya O, Ruppen T, Shi J, Siska SJ, Springer C, van Eis M, Vega RB, von Matt A, Yang L, Yoon T, Zhang JH, Zhu N, Monovich LG.
J Med Chem (2010) 53 : 5400 -5421
PubMed 20684591 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Activity 2 - -
IC50 2 8.25 8.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1214998 2 8.70
CHEMBL1214857 2 7.80

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1214998 IC50 = 2.0 nM 8.70
CHEMBL1214857 IC50 = 16.0 nM 7.80
CHEMBL1214857 Activity = 7.0 % -
CHEMBL1214998 Activity = 2.0 % -