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Assay Detail

CHEMBL4373003

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

Binding
Inhibition of PIM2 (unknown origin) assessed as reduction in BAD phosphorylation at Ser-112 residue by TR-FRET assay
22
Total Activities
19
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

Discovery of N-substituted 7-azaindoles as Pan-PIM kinases inhibitors - Lead optimization - Part III.
Barberis C, Pribish J, Tserlin E, Gross A, Czekaj M, Barragué M, Erdman P, Maniar S, Jiang J, Fire L, Patel V, Hebert A, Levit M, Wang A, Sun F, Huang SA.
Bioorg Med Chem Lett (2019) 29 : 491 -495
PubMed 30553737 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 22 8.05 8.57

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4448325 1 8.57
CHEMBL4457529 1 8.40
CHEMBL4540910 1 8.29
CHEMBL4470576 1 8.24
CHEMBL4466764 2 8.22
CHEMBL4583118 2 8.21
CHEMBL4588948 1 8.21
CHEMBL4446498 1 8.17
CHEMBL4518492 2 8.13
CHEMBL4564586 1 8.05
CHEMBL4593810 1 8.03
CHEMBL4587382 1 8.00
CHEMBL4528544 1 7.99
CHEMBL4541837 1 7.98
CHEMBL4466080 1 7.96
CHEMBL4457389 1 7.80
CHEMBL4563802 1 7.76
CHEMBL4533366 1 7.68
CHEMBL4445116 1 7.53

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4448325 IC50 = 2.7 nM 8.57
CHEMBL4457529 IC50 = 4.0 nM 8.40
CHEMBL4540910 IC50 = 5.1 nM 8.29
CHEMBL4470576 IC50 = 5.7 nM 8.24
CHEMBL4466764 IC50 = 6.0 nM 8.22
CHEMBL4588948 IC50 = 6.1 nM 8.21
CHEMBL4583118 IC50 = 6.1 nM 8.21
CHEMBL4446498 IC50 = 6.7 nM 8.17
CHEMBL4518492 IC50 = 7.4 nM 8.13
CHEMBL4583118 IC50 = 7.6 nM 8.12
CHEMBL4466764 IC50 = 8.8 nM 8.06
CHEMBL4564586 IC50 = 9.0 nM 8.05
CHEMBL4593810 IC50 = 9.3 nM 8.03
CHEMBL4587382 IC50 = 9.9 nM 8.00
CHEMBL4528544 IC50 = 10.2 nM 7.99
CHEMBL4541837 IC50 = 10.4 nM 7.98
CHEMBL4466080 IC50 = 11.0 nM 7.96
CHEMBL4457389 IC50 = 15.7 nM 7.80
CHEMBL4563802 IC50 = 17.5 nM 7.76
CHEMBL4518492 IC50 = 21.0 nM 7.68
CHEMBL4533366 IC50 = 21.0 nM 7.68
CHEMBL4445116 IC50 = 29.4 nM 7.53