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Assay Detail

CHEMBL4044916

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

Binding
Inhibition of human recombinant PIM1 in presence of ATP by ELISA based spectrophotometric analysis
31
Total Activities
31
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 pim-1 (CHEMBL2147)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Structure based drug design of Pim-1 kinase followed by pharmacophore guided synthesis of quinolone-based inhibitors.
Swellmeen L, Shahin R, Al-Hiari Y, Alamiri A, Hasan A, Shaheen O.
Bioorg Med Chem (2017) 25 : 4855 -4875
PubMed 28760531 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 31 8.07 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1952142 1 9.00
CHEMBL1782530 1 9.00
CHEMBL4087294 1 8.70
CHEMBL4105153 1 8.70
CHEMBL4090634 1 8.70
CHEMBL4062679 1 8.70
CHEMBL4087212 1 8.70
CHEMBL4102644 1 8.70
CHEMBL1915449 1 8.70
CHEMBL2035636 1 8.52
CHEMBL2035629 1 8.52
CHEMBL2035628 1 8.40
CHEMBL1952126 1 8.40
CHEMBL4073348 1 8.40
CHEMBL1915438 1 8.30
CHEMBL1952134 1 8.30
CHEMBL1915635 1 8.22
CHEMBL1952144 1 8.22
CHEMBL1915642 1 8.15
CHEMBL4070120 1 8.15
CHEMBL1915443 1 8.15
CHEMBL1952329 SGI-1776 1.0 1 8.15
CHEMBL1915633 1 8.10
CHEMBL1952136 1 8.05
CHEMBL2035632 1 8.05
CHEMBL4077340 1 6.53
CHEMBL4101797 1 5.67
CHEMBL4078430 1 5.48
CHEMBL4083792 1 5.47
CHEMBL4086292 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1952142 IC50 = 1.0 nM 9.00
CHEMBL1782530 IC50 = 1.0 nM 9.00
CHEMBL4087294 IC50 = 2.0 nM 8.70
CHEMBL4105153 IC50 = 2.0 nM 8.70
CHEMBL4090634 IC50 = 2.0 nM 8.70
CHEMBL4062679 IC50 = 2.0 nM 8.70
CHEMBL4087212 IC50 = 2.0 nM 8.70
CHEMBL4102644 IC50 = 2.0 nM 8.70
CHEMBL1915449 IC50 = 2.0 nM 8.70
CHEMBL2035636 IC50 = 3.0 nM 8.52
CHEMBL2035629 IC50 = 3.0 nM 8.52
CHEMBL2035628 IC50 = 4.0 nM 8.40
CHEMBL1952126 IC50 = 4.0 nM 8.40
CHEMBL4073348 IC50 = 4.0 nM 8.40
CHEMBL1915438 IC50 = 5.0 nM 8.30
CHEMBL1952134 IC50 = 5.0 nM 8.30
CHEMBL1915635 IC50 = 6.0 nM 8.22
CHEMBL1952144 IC50 = 6.0 nM 8.22
CHEMBL1915642 IC50 = 7.0 nM 8.15
CHEMBL4070120 IC50 = 7.0 nM 8.15
CHEMBL1915443 IC50 = 7.0 nM 8.15
CHEMBL1952329 SGI-1776 IC50 = 7.0 nM 8.15
CHEMBL1915633 IC50 = 8.0 nM 8.10
CHEMBL1952136 IC50 = 9.0 nM 8.05
CHEMBL2035632 IC50 = 9.0 nM 8.05
CHEMBL4077340 IC50 = 295.0 nM 6.53
CHEMBL4101797 IC50 = 2124.0 nM 5.67
CHEMBL4078430 IC50 = 3335.0 nM 5.48
CHEMBL4083792 IC50 = 3387.0 nM 5.47
CHEMBL4086292 IC50 = 54871000.0 nM -
CHEMBL4102686 IC50 = 56511000.0 nM -