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Assay Detail

CHEMBL3134838

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

Binding
Inhibition of PIM-1 (unknown origin) after 1 hr by HTRF assay
8
Total Activities
8
Compounds Tested
2
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 pim-1 (CHEMBL2147)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

More than just a GPCR ligand: structure-based discovery of thioridazine derivatives as Pim-1 kinase inhibitors
Li W, Wan X, Zeng F, Xie Y, Wang Y, Zhang W, Li L, Huang N
Medchemcomm (2014) 5 : 507 -511
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 7 5.24 5.89
Inhibition 1 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1398474 1 5.89
CHEMBL3133837 1 5.17
CHEMBL479 THIORIDAZINE 4.0 1 5.16
CHEMBL1357558 1 5.15
CHEMBL3133835 1 5.13
CHEMBL3133836 1 5.09
CHEMBL1688550 1 5.06
CHEMBL908 CHLORPROTHIXENE 4.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1398474 IC50 = 1280.0 nM 5.89
CHEMBL3133837 IC50 = 6730.0 nM 5.17
CHEMBL479 THIORIDAZINE IC50 = 6890.0 nM 5.16
CHEMBL1357558 IC50 = 7030.0 nM 5.15
CHEMBL3133835 IC50 = 7390.0 nM 5.13
CHEMBL3133836 IC50 = 8160.0 nM 5.09
CHEMBL1688550 IC50 = 8700.0 nM 5.06
CHEMBL908 CHLORPROTHIXENE Inhibition - % -