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Assay Detail

CHEMBL1919425

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

Binding
Inhibition of PIM3 using RSRHSSYPAGT as substrate by radiometric assay in the presence of 155 uM [ATP]
10
Total Activities
10
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-3 (CHEMBL5407)
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 10 6.74 7.46

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1915641 1 7.46
CHEMBL1915442 1 7.24
CHEMBL1915438 1 7.07
CHEMBL1915448 1 6.92
CHEMBL1915638 1 6.81
CHEMBL1915640 1 6.63
CHEMBL1915433 1 6.46
CHEMBL1915644 1 6.43
CHEMBL1915639 1 6.34
CHEMBL1915445 1 6.06

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1915641 IC50 = 35.0 nM 7.46
CHEMBL1915442 IC50 = 57.0 nM 7.24
CHEMBL1915438 IC50 = 86.0 nM 7.07
CHEMBL1915448 IC50 = 120.0 nM 6.92
CHEMBL1915638 IC50 = 154.0 nM 6.81
CHEMBL1915640 IC50 = 235.0 nM 6.63
CHEMBL1915433 IC50 = 343.0 nM 6.46
CHEMBL1915644 IC50 = 367.0 nM 6.43
CHEMBL1915639 IC50 = 459.0 nM 6.34
CHEMBL1915445 IC50 = 875.0 nM 6.06