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Assay Detail

CHEMBL3374860

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

Binding
Inhibition of Pim1 (unknown origin) using luciferase-luciferin based ATP detection reagent by Kinase-Glo assay
27
Total Activities
27
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

Synthesis and Biological Evaluation of Pyrazolo[1,5-a]pyrimidine Compounds as Potent and Selective Pim-1 Inhibitors.
Xu Y, Brenning BG, Kultgen SG, Foulks JM, Clifford A, Lai S, Chan A, Merx S, McCullar MV, Kanner SB, Ho KK.
ACS Med Chem Lett (2015) 6 : 63 -67
PubMed 25589932 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 27 6.99 8.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3355542 1 8.30
CHEMBL1952329 SGI-1776 1.0 1 8.12
CHEMBL3355552 1 7.77
CHEMBL3355987 1 7.64
CHEMBL3355557 1 7.62
CHEMBL3355550 1 7.60
CHEMBL3355544 1 7.57
CHEMBL3355541 1 7.35
CHEMBL3355551 1 7.27
CHEMBL3355553 1 7.18
CHEMBL3355988 1 7.17
CHEMBL3355558 1 7.03
CHEMBL3355555 1 6.96
CHEMBL3355543 1 6.88
CHEMBL3355554 1 6.83
CHEMBL3355549 1 6.83
CHEMBL3355990 1 6.79
CHEMBL3355991 1 6.78
CHEMBL3355989 1 6.73
CHEMBL3355545 1 6.71
CHEMBL3355546 1 6.69
CHEMBL3355559 1 6.62
CHEMBL3355547 1 6.42
CHEMBL3355560 1 6.42
CHEMBL3355548 1 6.20
CHEMBL3355540 1 4.28
CHEMBL3355556 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3355542 IC50 = 5.0 nM 8.30
CHEMBL1952329 SGI-1776 IC50 = 7.6 nM 8.12
CHEMBL3355552 IC50 = 17.0 nM 7.77
CHEMBL3355987 IC50 = 23.0 nM 7.64
CHEMBL3355557 IC50 = 24.0 nM 7.62
CHEMBL3355550 IC50 = 25.0 nM 7.60
CHEMBL3355544 IC50 = 27.0 nM 7.57
CHEMBL3355541 IC50 = 45.0 nM 7.35
CHEMBL3355551 IC50 = 54.0 nM 7.27
CHEMBL3355553 IC50 = 66.0 nM 7.18
CHEMBL3355988 IC50 = 68.0 nM 7.17
CHEMBL3355558 IC50 = 94.0 nM 7.03
CHEMBL3355555 IC50 = 111.0 nM 6.96
CHEMBL3355543 IC50 = 132.0 nM 6.88
CHEMBL3355554 IC50 = 149.0 nM 6.83
CHEMBL3355549 IC50 = 148.0 nM 6.83
CHEMBL3355990 IC50 = 164.0 nM 6.79
CHEMBL3355991 IC50 = 168.0 nM 6.78
CHEMBL3355989 IC50 = 186.0 nM 6.73
CHEMBL3355545 IC50 = 197.0 nM 6.71
CHEMBL3355546 IC50 = 204.0 nM 6.69
CHEMBL3355559 IC50 = 237.0 nM 6.62
CHEMBL3355547 IC50 = 378.0 nM 6.42
CHEMBL3355560 IC50 = 378.0 nM 6.42
CHEMBL3355548 IC50 = 633.0 nM 6.20
CHEMBL3355540 IC50 = 52000.0 nM 4.28
CHEMBL3355556 IC50 - -