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Assay Detail

CHEMBL1219871

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

Binding
Inhibition of PKD1 assessed as inhibition of HDAC5 neuclear export
28
Total Activities
28
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 D1 (CHEMBL3863)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Identification of potent and selective amidobipyridyl inhibitors of protein kinase D.
Meredith EL, Beattie K, Burgis R, Capparelli M, Chapo J, Dipietro L, Gamber G, Enyedy I, Hood DB, Hosagrahara V, Jewell C, Koch KA, Lee W, Lemon DD, McKinsey TA, Miranda K, Pagratis N, Phan D, Plato C, Rao C, Rozhitskaya O, Soldermann N, Springer C, van Eis M, Vega RB, Yan W, Zhu Q, Monovich LG.
J Med Chem (2010) 53 : 5422 -5438
PubMed 20684592 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 27 6.62 7.77
IC50 1 7.50 7.50

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1215151 1 7.77
CHEMBL1215000 1 7.62
CHEMBL1214998 1 7.50
CHEMBL1215078 1 7.18
CHEMBL1214999 1 7.11
CHEMBL1215153 1 7.04
CHEMBL1215363 1 6.94
CHEMBL1215076 1 6.70
CHEMBL1215219 1 6.63
CHEMBL1215360 1 6.47
CHEMBL1215149 1 6.42
CHEMBL1215150 1 6.37
CHEMBL1215002 1 6.36
CHEMBL1215075 1 6.32
CHEMBL1215361 1 6.25
CHEMBL1215074 1 6.17
CHEMBL1215222 1 6.17
CHEMBL1215152 1 6.15
CHEMBL1215286 1 6.12
CHEMBL1215223 1 6.08
CHEMBL1215362 1 -
CHEMBL1215288 1 -
CHEMBL1215287 1 -
CHEMBL1215285 1 -
CHEMBL1215221 1 -
CHEMBL1215220 1 -
CHEMBL1215001 1 -
CHEMBL1215077 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1215151 EC50 = 17.0 nM 7.77
CHEMBL1215000 EC50 = 24.0 nM 7.62
CHEMBL1214998 IC50 = 32.0 nM 7.50
CHEMBL1215078 EC50 = 66.0 nM 7.18
CHEMBL1214999 EC50 = 77.0 nM 7.11
CHEMBL1215153 EC50 = 92.0 nM 7.04
CHEMBL1215363 EC50 = 115.0 nM 6.94
CHEMBL1215076 EC50 = 202.0 nM 6.70
CHEMBL1215219 EC50 = 234.0 nM 6.63
CHEMBL1215360 EC50 = 342.0 nM 6.47
CHEMBL1215149 EC50 = 378.0 nM 6.42
CHEMBL1215150 EC50 = 428.0 nM 6.37
CHEMBL1215002 EC50 = 438.0 nM 6.36
CHEMBL1215075 EC50 = 478.0 nM 6.32
CHEMBL1215361 EC50 = 568.0 nM 6.25
CHEMBL1215074 EC50 = 674.0 nM 6.17
CHEMBL1215222 EC50 = 679.0 nM 6.17
CHEMBL1215152 EC50 = 704.0 nM 6.15
CHEMBL1215286 EC50 = 752.0 nM 6.12
CHEMBL1215223 EC50 = 831.0 nM 6.08
CHEMBL1215362 EC50 > 1000.0 nM -
CHEMBL1215288 EC50 > 1000.0 nM -
CHEMBL1215287 EC50 > 1000.0 nM -
CHEMBL1215285 EC50 > 1000.0 nM -
CHEMBL1215221 EC50 > 1000.0 nM -
CHEMBL1215220 EC50 > 1000.0 nM -
CHEMBL1215001 EC50 > 1000.0 nM -
CHEMBL1215077 EC50 > 1000.0 nM -