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Assay Detail

CHEMBL864489

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

Binding
Binding affinity to non phosphorylated PIM1
18
Total Activities
9
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Expert

Target

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

Publication

Structural basis of inhibitor specificity of the human protooncogene proviral insertion site in moloney murine leukemia virus (PIM-1) kinase.
Bullock AN, Debreczeni JE, Fedorov OY, Nelson A, Marsden BD, Knapp S.
J Med Chem (2005) 48 : 7604 -7614
PubMed 16302800 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 9 7.71 8.85
Kb 9 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL388978 STAUROSPORINE 2 8.85
CHEMBL6291 BISINDOLYLMALEIMIDE IX 2 8.10
CHEMBL7463 GF-109203 2 8.00
CHEMBL269264 2 7.92
CHEMBL200528 2 7.60
CHEMBL50 QUERCETIN 3.0 2 7.60
CHEMBL266487 RO-316233 2 7.57
CHEMBL370177 2 7.14
CHEMBL372585 2 6.60

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL388978 STAUROSPORINE Kd = 1.4 nM 8.85
CHEMBL6291 BISINDOLYLMALEIMIDE IX Kd = 8.0 nM 8.10
CHEMBL7463 GF-109203 Kd = 10.0 nM 8.00
CHEMBL269264 Kd = 12.0 nM 7.92
CHEMBL200528 Kd = 25.0 nM 7.60
CHEMBL50 QUERCETIN Kd = 25.0 nM 7.60
CHEMBL266487 RO-316233 Kd = 27.0 nM 7.57
CHEMBL370177 Kd = 72.0 nM 7.14
CHEMBL372585 Kd = 250.0 nM 6.60
CHEMBL7463 GF-109203 Kb = 98.6 10^6/M -
CHEMBL200528 Kb = 39.7 10^6/M -
CHEMBL50 QUERCETIN Kb = 39.3 10^6/M -
CHEMBL372585 Kb = 4.0 10^6/M -
CHEMBL6291 BISINDOLYLMALEIMIDE IX Kb = 127.0 10^6/M -
CHEMBL269264 Kb = 85.2 10^6/M -
CHEMBL266487 RO-316233 Kb = 37.0 10^6/M -
CHEMBL388978 STAUROSPORINE Kb = 705.0 10^6/M -
CHEMBL370177 Kb = 13.8 10^6/M -