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Assay Detail

CHEMBL2020770

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

Binding
Inhibition of human recombinant Pim1 using RSRHSSYPAGT as substrate and 30 uM ATP by radiometric assay
40
Total Activities
40
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

Novel potent dual inhibitors of CK2 and Pim kinases with antiproliferative activity against cancer cells.
Pierre F, Regan CF, Chevrel MC, Siddiqui-Jain A, Macalino D, Streiner N, Drygin D, Haddach M, O'Brien SE, Rice WG, Ryckman DM.
Bioorg Med Chem Lett (2012) 22 : 3327 -3331
PubMed 22460033 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 40 8.01 8.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2017348 1 8.70
CHEMBL2017324 1 8.70
CHEMBL2017323 1 8.52
CHEMBL2017346 1 8.52
CHEMBL2017322 1 8.40
CHEMBL2017347 1 8.40
CHEMBL2017336 1 8.40
CHEMBL2017352 1 8.40
CHEMBL2017328 1 8.40
CHEMBL2017359 1 8.30
CHEMBL2017360 1 8.30
CHEMBL2017343 1 8.30
CHEMBL2017356 1 8.22
CHEMBL2017339 1 8.22
CHEMBL2017326 1 8.15
CHEMBL2017350 1 8.15
CHEMBL2017329 1 8.10
CHEMBL2017332 1 8.10
CHEMBL2017344 1 8.05
CHEMBL2017349 1 8.05
CHEMBL2017342 1 8.05
CHEMBL2017355 1 8.00
CHEMBL2017351 1 7.96
CHEMBL2017331 1 7.92
CHEMBL2017341 1 7.85
CHEMBL2017340 1 7.85
CHEMBL2017330 1 7.85
CHEMBL2017361 1 7.82
CHEMBL2017334 1 7.82
CHEMBL2017353 1 7.80

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2017348 IC50 = 2.0 nM 8.70
CHEMBL2017324 IC50 = 2.0 nM 8.70
CHEMBL2017346 IC50 = 3.0 nM 8.52
CHEMBL2017323 IC50 = 3.0 nM 8.52
CHEMBL2017322 IC50 = 4.0 nM 8.40
CHEMBL2017347 IC50 = 4.0 nM 8.40
CHEMBL2017336 IC50 = 4.0 nM 8.40
CHEMBL2017352 IC50 = 4.0 nM 8.40
CHEMBL2017328 IC50 = 4.0 nM 8.40
CHEMBL2017360 IC50 = 5.0 nM 8.30
CHEMBL2017343 IC50 = 5.0 nM 8.30
CHEMBL2017359 IC50 = 5.0 nM 8.30
CHEMBL2017356 IC50 = 6.0 nM 8.22
CHEMBL2017339 IC50 = 6.0 nM 8.22
CHEMBL2017350 IC50 = 7.0 nM 8.15
CHEMBL2017326 IC50 = 7.0 nM 8.15
CHEMBL2017329 IC50 = 8.0 nM 8.10
CHEMBL2017332 IC50 = 8.0 nM 8.10
CHEMBL2017342 IC50 = 9.0 nM 8.05
CHEMBL2017344 IC50 = 9.0 nM 8.05
CHEMBL2017349 IC50 = 9.0 nM 8.05
CHEMBL2017355 IC50 = 10.0 nM 8.00
CHEMBL2017351 IC50 = 11.0 nM 7.96
CHEMBL2017331 IC50 = 12.0 nM 7.92
CHEMBL2017341 IC50 = 14.0 nM 7.85
CHEMBL2017340 IC50 = 14.0 nM 7.85
CHEMBL2017330 IC50 = 14.0 nM 7.85
CHEMBL2017361 IC50 = 15.0 nM 7.82
CHEMBL2017334 IC50 = 15.0 nM 7.82
CHEMBL2017353 IC50 = 16.0 nM 7.80
CHEMBL2017327 IC50 = 16.0 nM 7.80
CHEMBL2017354 IC50 = 16.0 nM 7.80
CHEMBL2017337 IC50 = 17.0 nM 7.77
CHEMBL2017357 IC50 = 17.0 nM 7.77
CHEMBL2017325 IC50 = 27.0 nM 7.57
CHEMBL2017335 IC50 = 35.0 nM 7.46
CHEMBL2017333 IC50 = 38.0 nM 7.42
CHEMBL2017345 IC50 = 64.0 nM 7.19
CHEMBL2017358 IC50 = 69.0 nM 7.16
CHEMBL2017338 IC50 = 91.0 nM 7.04