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Assay Detail

CHEMBL1919014

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

Binding
Inhibition of human recombinant Pim2 using RSRHSSYPAGT as substrate by radiometric assay in the presence of 5 uM [ATP]
57
Total Activities
57
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

7-(4H-1,2,4-Triazol-3-yl)benzo[c][2,6]naphthyridines: a novel class of Pim kinase inhibitors with potent cell antiproliferative activity.
Pierre F, Stefan E, Nédellec AS, Chevrel MC, Regan CF, Siddiqui-Jain A, Macalino D, Streiner N, Drygin D, Haddach M, O'Brien SE, Anderes K, Ryckman DM.
Bioorg Med Chem Lett (2011) 21 : 6687 -6692
PubMed 21982499 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 57 7.78 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1915636 1 9.00
CHEMBL1915644 1 9.00
CHEMBL1915633 1 9.00
CHEMBL1914471 1 8.70
CHEMBL1915445 1 8.70
CHEMBL1915647 1 8.70
CHEMBL1915646 1 8.70
CHEMBL1915442 1 8.52
CHEMBL1915651 1 8.40
CHEMBL1915650 1 8.40
CHEMBL1915648 1 8.30
CHEMBL1915645 1 8.30
CHEMBL1915443 1 8.22
CHEMBL1915438 1 8.22
CHEMBL1915638 1 8.22
CHEMBL1915448 1 8.15
CHEMBL1915634 1 8.10
CHEMBL1915635 1 8.10
CHEMBL1915428 1 8.10
CHEMBL1915643 1 8.10
CHEMBL1915649 1 8.00
CHEMBL1915433 1 8.00
CHEMBL1915436 1 8.00
CHEMBL1915639 1 8.00
CHEMBL1915640 1 8.00
CHEMBL1915637 1 7.92
CHEMBL1915449 1 7.92
CHEMBL1915641 1 7.92
CHEMBL1915439 1 7.82
CHEMBL1915441 1 7.80

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1915636 IC50 = 1.0 nM 9.00
CHEMBL1915644 IC50 = 1.0 nM 9.00
CHEMBL1915633 IC50 = 1.0 nM 9.00
CHEMBL1914471 IC50 = 2.0 nM 8.70
CHEMBL1915445 IC50 = 2.0 nM 8.70
CHEMBL1915647 IC50 = 2.0 nM 8.70
CHEMBL1915646 IC50 = 2.0 nM 8.70
CHEMBL1915442 IC50 = 3.0 nM 8.52
CHEMBL1915651 IC50 = 4.0 nM 8.40
CHEMBL1915650 IC50 = 4.0 nM 8.40
CHEMBL1915648 IC50 = 5.0 nM 8.30
CHEMBL1915645 IC50 = 5.0 nM 8.30
CHEMBL1915438 IC50 = 6.0 nM 8.22
CHEMBL1915638 IC50 = 6.0 nM 8.22
CHEMBL1915443 IC50 = 6.0 nM 8.22
CHEMBL1915448 IC50 = 7.0 nM 8.15
CHEMBL1915634 IC50 = 8.0 nM 8.10
CHEMBL1915635 IC50 = 8.0 nM 8.10
CHEMBL1915428 IC50 = 8.0 nM 8.10
CHEMBL1915643 IC50 = 8.0 nM 8.10
CHEMBL1915649 IC50 = 10.0 nM 8.00
CHEMBL1915433 IC50 = 10.0 nM 8.00
CHEMBL1915436 IC50 = 10.0 nM 8.00
CHEMBL1915639 IC50 = 10.0 nM 8.00
CHEMBL1915640 IC50 = 10.0 nM 8.00
CHEMBL1915637 IC50 = 12.0 nM 7.92
CHEMBL1915641 IC50 = 12.0 nM 7.92
CHEMBL1915449 IC50 = 12.0 nM 7.92
CHEMBL1915439 IC50 = 15.0 nM 7.82
CHEMBL1915441 IC50 = 16.0 nM 7.80
CHEMBL1915422 IC50 = 18.0 nM 7.75
CHEMBL1915426 IC50 = 18.0 nM 7.75
CHEMBL1915642 IC50 = 20.0 nM 7.70
CHEMBL1915429 IC50 = 20.0 nM 7.70
CHEMBL1915437 IC50 = 21.0 nM 7.68
CHEMBL1915430 IC50 = 26.0 nM 7.58
CHEMBL1915434 IC50 = 26.0 nM 7.58
CHEMBL1915444 IC50 = 31.0 nM 7.51
CHEMBL1915446 IC50 = 44.0 nM 7.36
CHEMBL1915421 IC50 = 54.0 nM 7.27
CHEMBL1915431 IC50 = 55.0 nM 7.26
CHEMBL1915440 IC50 = 59.0 nM 7.23
CHEMBL1915424 IC50 = 74.0 nM 7.13
CHEMBL1915435 IC50 = 92.0 nM 7.04
CHEMBL1649765 IC50 = 94.0 nM 7.03
CHEMBL1915447 IC50 = 113.0 nM 6.95
CHEMBL1915427 IC50 = 117.0 nM 6.93
CHEMBL1915425 IC50 = 158.0 nM 6.80
CHEMBL1915432 IC50 = 174.0 nM 6.76
CHEMBL1230165 SILMITASERTIB IC50 = 186.0 nM 6.73