Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL3816952

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

Binding
Inhibition of human myc-tagged TNNI3K autophosphorylation overexpressed in HEKMSR2 cells incubated for 30 mins by time resolved fluorescence assay
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEKMSR2
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Serine/threonine-protein kinase TNNI3K (CHEMBL5260)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

GSK114: A selective inhibitor for elucidating the biological role of TNNI3K.
Lawhorn BG, Philp J, Graves AP, Shewchuk L, Holt DA, Gatto GJ, Kallander LS.
Bioorg Med Chem Lett (2016) 26 : 3355 -3358
PubMed 27246618 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 13 7.22 8.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3814834 1 8.00
CHEMBL3813948 1 7.89
CHEMBL3814871 1 7.60
CHEMBL3814923 1 7.60
CHEMBL3613195 1 7.30
CHEMBL3814010 1 7.30
CHEMBL3814998 1 7.30
CHEMBL3814097 1 7.20
CHEMBL3813957 1 7.10
CHEMBL3815093 1 7.00
CHEMBL3814635 1 6.80
CHEMBL3814442 1 6.50
CHEMBL3815116 1 6.30

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3814834 IC50 = 10.0 nM 8.00
CHEMBL3813948 IC50 = 13.0 nM 7.89
CHEMBL3814871 IC50 = 25.0 nM 7.60
CHEMBL3814923 IC50 = 25.0 nM 7.60
CHEMBL3613195 IC50 = 50.0 nM 7.30
CHEMBL3814010 IC50 = 50.0 nM 7.30
CHEMBL3814998 IC50 = 50.0 nM 7.30
CHEMBL3814097 IC50 = 63.0 nM 7.20
CHEMBL3813957 IC50 = 79.0 nM 7.10
CHEMBL3815093 IC50 = 100.0 nM 7.00
CHEMBL3814635 IC50 = 160.0 nM 6.80
CHEMBL3814442 IC50 = 320.0 nM 6.50
CHEMBL3815116 IC50 = 500.0 nM 6.30