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Assay Detail

CHEMBL4135736

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

Binding
Inhibition of PIM1 (unknown origin) using TAMRA-ERMRPRKRQGSVRRRV-NH2 as substrate pretreated for 30 mins followed by substrate addition measured after 1 hr by IMAP assay
8
Total Activities
8
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

From PIM1 to PI3Kδ via GSK3β: Target Hopping through the Kinome.
Henley ZA, Bax BD, Inglesby LM, Champigny A, Gaines S, Faulder P, Le J, Thomas DA, Washio Y, Baldwin IR.
ACS Med Chem Lett (2017) 8 : 1093 -1098
PubMed 29057057 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 8 5.78 6.90

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4161596 1 6.90
CHEMBL4172211 1 6.50
CHEMBL260163 1 6.30
CHEMBL4174177 1 5.70
CHEMBL4176717 1 5.60
CHEMBL4165288 1 5.60
CHEMBL4163479 1 4.80
CHEMBL4168859 1 4.80

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4161596 IC50 = 125.89 nM 6.90
CHEMBL4172211 IC50 = 316.23 nM 6.50
CHEMBL260163 IC50 = 501.19 nM 6.30
CHEMBL4174177 IC50 = 1995.26 nM 5.70
CHEMBL4176717 IC50 = 2511.89 nM 5.60
CHEMBL4165288 IC50 = 2511.89 nM 5.60
CHEMBL4163479 IC50 = 15848.93 nM 4.80
CHEMBL4168859 IC50 = 15848.93 nM 4.80