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Assay Detail

CHEMBL903376

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

Binding
Inhibition of Pim1 kinase
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Serine/threonine-protein kinase pim-1 (CHEMBL2147)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Identification and structure-activity relationships of substituted pyridones as inhibitors of Pim-1 kinase.
Cheney IW, Yan S, Appleby T, Walker H, Vo T, Yao N, Hamatake R, Hong Z, Wu JZ.
Bioorg Med Chem Lett (2007) 17 : 1679 -1683
PubMed 17251021 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 18 5.87 7.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL391586 1 7.30
CHEMBL246457 1 6.47
CHEMBL246458 1 6.43
CHEMBL393238 1 6.37
CHEMBL246656 1 6.04
CHEMBL246661 1 5.99
CHEMBL246663 1 5.94
CHEMBL246657 1 5.91
CHEMBL397641 1 5.75
CHEMBL246655 1 5.36
CHEMBL247682 1 5.32
CHEMBL247684 1 4.70
CHEMBL427876 1 4.70
CHEMBL248091 1 -
CHEMBL395464 1 -
CHEMBL247681 1 -
CHEMBL391154 1 -
CHEMBL247077 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL391586 IC50 = 50.0 nM 7.30
CHEMBL246457 IC50 = 340.0 nM 6.47
CHEMBL246458 IC50 = 370.0 nM 6.43
CHEMBL393238 IC50 = 430.0 nM 6.37
CHEMBL246656 IC50 = 920.0 nM 6.04
CHEMBL246661 IC50 = 1030.0 nM 5.99
CHEMBL246663 IC50 = 1140.0 nM 5.94
CHEMBL246657 IC50 = 1230.0 nM 5.91
CHEMBL397641 IC50 = 1770.0 nM 5.75
CHEMBL246655 IC50 = 4410.0 nM 5.36
CHEMBL247682 IC50 = 4790.0 nM 5.32
CHEMBL247684 IC50 = 20000.0 nM 4.70
CHEMBL427876 IC50 = 20000.0 nM 4.70
CHEMBL248091 IC50 > 20000.0 nM -
CHEMBL395464 IC50 > 20000.0 nM -
CHEMBL247681 IC50 > 20000.0 nM -
CHEMBL391154 IC50 > 20000.0 nM -
CHEMBL247077 IC50 > 20000.0 nM -