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Assay Detail

CHEMBL4841801

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

Binding
Inhibition of human myc-TNNI3K expressed in HEK-MSR2 cells assessed as reduction in TNNI3K autophosphorylation preincubated for 30 mins followed by pervanadate addition and measured after 20 mins by DELFIA
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Identification of Diarylurea Inhibitors of the Cardiac-Specific Kinase TNNI3K by Designing Selectivity Against VEGFR2, p38α, and B-Raf.
Patterson JR, Graves AP, Stoy P, Cheung M, Desai TA, Fries H, Gatto GJ, Holt DA, Shewchuk L, Totoritis R, Wang L, Kallander LS.
J Med Chem (2021) 64 : 15651 -15670
PubMed 34699203 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 11 7.39 8.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4868757 1 8.10
CHEMBL4094739 1 8.10
CHEMBL4849349 1 7.80
CHEMBL4863580 1 7.70
CHEMBL4871527 1 7.40
CHEMBL4854957 1 7.30
CHEMBL3613195 1 7.30
CHEMBL4869303 1 7.00
CHEMBL4867552 1 7.00
CHEMBL3815093 1 7.00
CHEMBL1336 SORAFENIB 4.0 1 6.60

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4868757 IC50 = 7.9 nM 8.10
CHEMBL4094739 IC50 = 8.0 nM 8.10
CHEMBL4849349 IC50 = 16.0 nM 7.80
CHEMBL4863580 IC50 = 20.0 nM 7.70
CHEMBL4871527 IC50 = 40.0 nM 7.40
CHEMBL4854957 IC50 = 50.0 nM 7.30
CHEMBL3613195 IC50 = 50.0 nM 7.30
CHEMBL4869303 IC50 = 100.0 nM 7.00
CHEMBL4867552 IC50 = 100.0 nM 7.00
CHEMBL3815093 IC50 = 100.0 nM 7.00
CHEMBL1336 SORAFENIB IC50 = 250.0 nM 6.60