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Assay Detail

CHEMBL5316849

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

Binding
Inhibition of PKD1 (unknown origin)
16
Total Activities
16
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

Serine/threonine-protein kinase D1 (CHEMBL3863)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Small Molecule Inhibitors of Protein Kinase D: Early Development, Current Approaches, and Future Directions.
Wang QJ, Wipf P.
J Med Chem (2023) 66 : 122 -139
PubMed 36538005 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 16 7.05 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5440043 1 9.00
CHEMBL5419827 1 9.00
CHEMBL5428541 1 9.00
CHEMBL281948 K-252A 1 8.15
CHEMBL5413306 1 7.80
CHEMBL302449 GO-6976 1 7.70
CHEMBL388978 STAUROSPORINE 1 7.40
CHEMBL5398617 1 7.28
CHEMBL238125 1 6.97
CHEMBL264406 1 6.81
CHEMBL471474 HYPOTHEMYCIN 1 6.30
CHEMBL5434569 1 5.99
CHEMBL5432054 1 5.63
CHEMBL5399250 1 5.62
CHEMBL1504776 1 5.50
CHEMBL261491 1 4.70

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5440043 IC50 = 1.0 nM 9.00
CHEMBL5419827 IC50 = 1.0 nM 9.00
CHEMBL5428541 IC50 = 1.0 nM 9.00
CHEMBL281948 K-252A IC50 = 7.0 nM 8.15
CHEMBL5413306 IC50 = 16.0 nM 7.80
CHEMBL302449 GO-6976 IC50 = 20.0 nM 7.70
CHEMBL388978 STAUROSPORINE IC50 = 40.0 nM 7.40
CHEMBL5398617 IC50 = 53.0 nM 7.28
CHEMBL238125 IC50 = 106.0 nM 6.97
CHEMBL264406 IC50 = 155.0 nM 6.81
CHEMBL471474 HYPOTHEMYCIN IC50 = 500.0 nM 6.30
CHEMBL5434569 IC50 = 1030.0 nM 5.99
CHEMBL5432054 IC50 = 2340.0 nM 5.63
CHEMBL5399250 IC50 = 2390.0 nM 5.62
CHEMBL1504776 IC50 = 3200.0 nM 5.50
CHEMBL261491 IC50 = 20000.0 nM 4.70