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Assay Detail

CHEMBL3816884

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

Binding
Displacement of 5-({[2-({[3-({4-[(5-hydroxy-2-methylphenyl)amino]-2-pyrimidinyl}amino)phenyl]carbonyl}amino)-ethyl]amino}carbonyl)-2-(6-hydroxy-3-oxo-3H-xanthen-9-yl)benzoic acid from full length human TNNI3K expressed in baculovirus system incubated for 60 mins by fluorescence polarization assay
30
Total Activities
30
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 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 30 7.35 7.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3814998 1 7.89
CHEMBL3813957 1 7.89
CHEMBL3814010 1 7.80
CHEMBL3815093 1 7.60
CHEMBL3814442 1 7.60
CHEMBL3814635 1 7.60
CHEMBL3815116 1 7.60
CHEMBL3612666 1 7.50
CHEMBL3612665 1 7.50
CHEMBL3814121 1 7.50
CHEMBL3612661 1 7.40
CHEMBL3813872 1 7.40
CHEMBL3612667 1 7.40
CHEMBL3613195 1 7.30
CHEMBL3813902 1 7.30
CHEMBL3814727 1 7.20
CHEMBL3613177 1 7.20
CHEMBL3813871 1 7.10
CHEMBL3612647 1 7.10
CHEMBL3612664 1 6.89
CHEMBL3814685 1 6.89
CHEMBL3814515 1 6.70
CHEMBL3814179 1 6.70
CHEMBL3814798 1 -
CHEMBL3814871 1 -
CHEMBL3814923 1 -
CHEMBL3814834 1 -
CHEMBL3813948 1 -
CHEMBL3814097 1 -
CHEMBL3613305 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3814998 IC50 = 13.0 nM 7.89
CHEMBL3813957 IC50 = 13.0 nM 7.89
CHEMBL3814010 IC50 = 16.0 nM 7.80
CHEMBL3815093 IC50 = 25.0 nM 7.60
CHEMBL3814442 IC50 = 25.0 nM 7.60
CHEMBL3814635 IC50 = 25.0 nM 7.60
CHEMBL3815116 IC50 = 25.0 nM 7.60
CHEMBL3612666 IC50 = 32.0 nM 7.50
CHEMBL3612665 IC50 = 32.0 nM 7.50
CHEMBL3814121 IC50 = 32.0 nM 7.50
CHEMBL3612661 IC50 = 40.0 nM 7.40
CHEMBL3813872 IC50 = 40.0 nM 7.40
CHEMBL3612667 IC50 = 40.0 nM 7.40
CHEMBL3613195 IC50 = 50.0 nM 7.30
CHEMBL3813902 IC50 = 50.0 nM 7.30
CHEMBL3814727 IC50 = 63.0 nM 7.20
CHEMBL3613177 IC50 = 63.0 nM 7.20
CHEMBL3813871 IC50 = 79.0 nM 7.10
CHEMBL3612647 IC50 = 80.0 nM 7.10
CHEMBL3612664 IC50 = 130.0 nM 6.89
CHEMBL3814685 IC50 = 130.0 nM 6.89
CHEMBL3814515 IC50 = 200.0 nM 6.70
CHEMBL3814179 IC50 = 200.0 nM 6.70
CHEMBL3814798 IC50 < 10.0 nM -
CHEMBL3814871 IC50 < 10.0 nM -
CHEMBL3814923 IC50 < 10.0 nM -
CHEMBL3814834 IC50 < 10.0 nM -
CHEMBL3813948 IC50 < 10.0 nM -
CHEMBL3814097 IC50 < 10.0 nM -
CHEMBL3613305 IC50 < 10.0 nM -