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Assay Detail

CHEMBL3616263

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

Binding
Inhibition of human myc-tagged TNNI3K autophosphorylation overexpressed in HEKMSRII cells preincubated for 30 mins followed by pervanadate solution addition measured after 20 mins by DELFIA
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEKMSRII
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 Purines and 7-Deazapurines as Potent and Selective Type I Inhibitors of Troponin I-Interacting Kinase (TNNI3K).
Lawhorn BG, Philp J, Zhao Y, Louer C, Hammond M, Cheung M, Fries H, Graves AP, Shewchuk L, Wang L, Cottom JE, Qi H, Zhao H, Totoritis R, Zhang G, Schwartz B, Li H, Sweitzer S, Holt DA, Gatto GJ, Kallander LS.
J Med Chem (2015) 58 : 7431 -7448
PubMed 26355916 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 10 7.82 9.15

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3613198 1 9.15
CHEMBL3613197 1 8.80
CHEMBL3613305 1 8.20
CHEMBL3613199 1 8.10
CHEMBL3613309 1 8.00
CHEMBL3613307 1 7.80
CHEMBL3613306 1 7.40
CHEMBL3613195 1 7.30
CHEMBL3613196 1 7.00
CHEMBL3613308 1 6.40

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3613198 IC50 = 0.7 nM 9.15
CHEMBL3613197 IC50 = 1.6 nM 8.80
CHEMBL3613305 IC50 = 6.3 nM 8.20
CHEMBL3613199 IC50 = 7.9 nM 8.10
CHEMBL3613309 IC50 = 10.0 nM 8.00
CHEMBL3613307 IC50 = 16.0 nM 7.80
CHEMBL3613306 IC50 = 40.0 nM 7.40
CHEMBL3613195 IC50 = 50.0 nM 7.30
CHEMBL3613196 IC50 = 100.0 nM 7.00
CHEMBL3613308 IC50 = 398.0 nM 6.40