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Assay Detail

CHEMBL1106592

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

Binding
Inhibition of PIM1
42
Total Activities
42
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Identification and structure-activity relationship of 8-hydroxy-quinoline-7-carboxylic acid derivatives as inhibitors of Pim-1 kinase.
Sliman F, Blairvacq M, Durieu E, Meijer L, Rodrigo J, Desmaële D.
Bioorg Med Chem Lett (2010) 20 : 2801 -2805
PubMed 20363627 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 42 5.70 6.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL81714 1 6.70
CHEMBL39958 1 6.40
CHEMBL37139 1 6.30
CHEMBL36586 1 6.30
CHEMBL81284 1 6.30
CHEMBL83419 1 6.22
CHEMBL418613 1 6.16
CHEMBL82029 1 6.00
CHEMBL83746 1 6.00
CHEMBL39092 1 5.77
CHEMBL40170 1 5.70
CHEMBL309885 1 5.70
CHEMBL81182 1 5.68
CHEMBL39301 1 5.68
CHEMBL37431 1 5.60
CHEMBL1098529 1 5.55
CHEMBL82633 1 5.55
CHEMBL142246 1 5.52
CHEMBL310321 1 5.52
CHEMBL36640 1 5.51
CHEMBL59548 1 5.51
CHEMBL40148 1 5.50
CHEMBL80008 1 5.48
CHEMBL431508 1 5.47
CHEMBL39883 1 5.40
CHEMBL1096809 1 5.35
CHEMBL341951 1 5.35
CHEMBL1096159 1 5.30
CHEMBL289303 1 5.30
CHEMBL81686 1 5.29

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL81714 IC50 = 200.0 nM 6.70
CHEMBL39958 IC50 = 400.0 nM 6.40
CHEMBL36586 IC50 = 500.0 nM 6.30
CHEMBL81284 IC50 = 500.0 nM 6.30
CHEMBL37139 IC50 = 500.0 nM 6.30
CHEMBL83419 IC50 = 600.0 nM 6.22
CHEMBL418613 IC50 = 700.0 nM 6.16
CHEMBL82029 IC50 = 1000.0 nM 6.00
CHEMBL83746 IC50 = 1000.0 nM 6.00
CHEMBL39092 IC50 = 1700.0 nM 5.77
CHEMBL40170 IC50 = 2000.0 nM 5.70
CHEMBL309885 IC50 = 2000.0 nM 5.70
CHEMBL81182 IC50 = 2100.0 nM 5.68
CHEMBL39301 IC50 = 2100.0 nM 5.68
CHEMBL37431 IC50 = 2500.0 nM 5.60
CHEMBL1098529 IC50 = 2800.0 nM 5.55
CHEMBL82633 IC50 = 2800.0 nM 5.55
CHEMBL142246 IC50 = 3000.0 nM 5.52
CHEMBL310321 IC50 = 3000.0 nM 5.52
CHEMBL36640 IC50 = 3100.0 nM 5.51
CHEMBL59548 IC50 = 3100.0 nM 5.51
CHEMBL40148 IC50 = 3200.0 nM 5.50
CHEMBL80008 IC50 = 3300.0 nM 5.48
CHEMBL431508 IC50 = 3400.0 nM 5.47
CHEMBL39883 IC50 = 4000.0 nM 5.40
CHEMBL1096809 IC50 = 4500.0 nM 5.35
CHEMBL341951 IC50 = 4500.0 nM 5.35
CHEMBL1096159 IC50 = 5000.0 nM 5.30
CHEMBL289303 IC50 = 5000.0 nM 5.30
CHEMBL81686 IC50 = 5100.0 nM 5.29
CHEMBL37869 IC50 = 5500.0 nM 5.26
CHEMBL1098784 IC50 = 7000.0 nM 5.16
CHEMBL1096158 IC50 > 10000.0 nM -
CHEMBL1096667 IC50 > 10000.0 nM -
CHEMBL142412 IC50 > 10000.0 nM -
CHEMBL188701 IC50 > 10000.0 nM -
CHEMBL1095744 IC50 > 10000.0 nM -
CHEMBL58057 IC50 > 10000.0 nM -
CHEMBL1095743 IC50 > 10000.0 nM -
CHEMBL1095742 IC50 > 10000.0 nM -
CHEMBL39823 IC50 > 10000.0 nM -
CHEMBL1096334 IC50 > 10000.0 nM -