Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL2038009

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

Binding
Inhibition of N-terminal His-tagged human PIM2 expressed in Escherichia coli using AKRRRLSA as substrate after 1 to 2 hrs by luciferasse-luciferin-coupled chemiluminescence assay
ChEMBL ↗
47
Total Activities
47
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-2 (CHEMBL4523) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

The design, synthesis, and biological evaluation of PIM kinase inhibitors.
Tsuhako AL, Brown DS, Koltun ES, Aay N, Arcalas A, Chan V, Du H, Engst S, Franzini M, Galan A, Huang P, Johnston S, Kane B, Kim MH, Laird AD, Lin R, Mock L, Ngan I, Pack M, Stott G, Stout TJ, Yu P, Zaharia C, Zhang W, Zhou P, Nuss JM, Kearney PC, Xu W.
Bioorg Med Chem Lett (2012) 22 : 3732 -3738
PubMed 22542012 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 47 6.21 7.54

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2035630 — — 1 7.54
CHEMBL2035628 — — 1 7.54
CHEMBL2030387 — — 1 7.31
CHEMBL2035629 — — 1 7.17
CHEMBL2030386 — — 1 7.17
CHEMBL2035632 — — 1 7.17
CHEMBL2030388 — — 1 7.14
CHEMBL2035626 — — 1 7.06
CHEMBL2035635 — — 1 6.96
CHEMBL2030376 — — 1 6.92
CHEMBL2035627 — — 1 6.87
CHEMBL2035640 — — 1 6.85
CHEMBL2035638 — — 1 6.85
CHEMBL2035636 — — 1 6.79
CHEMBL2030389 — — 1 6.71
CHEMBL2035633 — — 1 6.71
CHEMBL2035624 — — 1 6.53
CHEMBL2035639 — — 1 6.32
CHEMBL2035634 — — 1 6.30
CHEMBL2035637 — — 1 6.27
CHEMBL2035623 — — 1 6.22
CHEMBL2035642 — — 1 6.21
CHEMBL2035621 — — 1 6.18
CHEMBL2035631 — — 1 6.14
CHEMBL2035603 — — 1 6.11
CHEMBL2035641 — — 1 6.08
CHEMBL2035598 — — 1 6.07
CHEMBL2035620 — — 1 6.07
CHEMBL2035622 — — 1 5.97
CHEMBL2035605 — — 1 5.84

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2035630 — IC50 = 29.0 nM 7.54
CHEMBL2035628 — IC50 = 29.0 nM 7.54
CHEMBL2030387 — IC50 = 49.0 nM 7.31
CHEMBL2035629 — IC50 = 68.0 nM 7.17
CHEMBL2030386 — IC50 = 68.0 nM 7.17
CHEMBL2035632 — IC50 = 68.0 nM 7.17
CHEMBL2030388 — IC50 = 72.0 nM 7.14
CHEMBL2035626 — IC50 = 87.0 nM 7.06
CHEMBL2035635 — IC50 = 110.0 nM 6.96
CHEMBL2030376 — IC50 = 121.0 nM 6.92
CHEMBL2035627 — IC50 = 134.0 nM 6.87
CHEMBL2035640 — IC50 = 140.0 nM 6.85
CHEMBL2035638 — IC50 = 142.0 nM 6.85
CHEMBL2035636 — IC50 = 162.0 nM 6.79
CHEMBL2035633 — IC50 = 197.0 nM 6.71
CHEMBL2030389 — IC50 = 194.0 nM 6.71
CHEMBL2035624 — IC50 = 293.0 nM 6.53
CHEMBL2035639 — IC50 = 480.0 nM 6.32
CHEMBL2035634 — IC50 = 503.0 nM 6.30
CHEMBL2035637 — IC50 = 534.0 nM 6.27
CHEMBL2035623 — IC50 = 598.0 nM 6.22
CHEMBL2035642 — IC50 = 620.0 nM 6.21
CHEMBL2035621 — IC50 = 653.0 nM 6.18
CHEMBL2035631 — IC50 = 730.0 nM 6.14
CHEMBL2035603 — IC50 = 781.0 nM 6.11
CHEMBL2035641 — IC50 = 840.0 nM 6.08
CHEMBL2035598 — IC50 = 858.0 nM 6.07
CHEMBL2035620 — IC50 = 850.0 nM 6.07
CHEMBL2035622 — IC50 = 1068.0 nM 5.97
CHEMBL2035605 — IC50 = 1451.0 nM 5.84
CHEMBL2035625 — IC50 = 1741.0 nM 5.76
CHEMBL2035610 — IC50 = 2330.0 nM 5.63
CHEMBL2035614 — IC50 = 2377.0 nM 5.62
CHEMBL2035617 — IC50 = 3330.0 nM 5.48
CHEMBL2035607 — IC50 = 3429.0 nM 5.46
CHEMBL2035606 — IC50 = 3755.0 nM 5.42
CHEMBL2035604 — IC50 = 3934.0 nM 5.41
CHEMBL2035613 — IC50 = 5000.0 nM 5.30
CHEMBL2035612 — IC50 = 5000.0 nM 5.30
CHEMBL2035611 — IC50 = 5000.0 nM 5.30
CHEMBL2035615 — IC50 = 5000.0 nM 5.30
CHEMBL2035609 — IC50 = 5000.0 nM 5.30
CHEMBL2035608 — IC50 = 5000.0 nM 5.30
CHEMBL2035616 — IC50 = 5000.0 nM 5.30
CHEMBL2035597 — IC50 = 5000.0 nM 5.30
CHEMBL2035619 — IC50 = 5000.0 nM 5.30
CHEMBL2035618 — IC50 > 5000.0 nM -