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TNNI3 interacting kinase

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Target not currently curated in GtoImmuPdb

Target id: 2247

Nomenclature: TNNI3 interacting kinase

Abbreviated Name: HH498

Family: HH498 subfamily

Contents:

Gene and Protein Information Click here for help
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 835 1p31.1 TNNI3K TNNI3 interacting kinase
Mouse - 834 3 H4 Tnni3k TNNI3 interacting kinase
Rat - 835 2q45 Tnni3k TNNI3 interacting kinase
Previous and Unofficial Names Click here for help
Cark | cardiac ankyrin repeat kinase
Database Links Click here for help
Alphafold Q59H18 (Hs), Q5GIG6 (Mm), Q7TQP6 (Rn)
BRENDA 2.7.11.1
CATH/Gene3D 1.25.40.20
ChEMBL Target CHEMBL5260 (Hs), CHEMBL4879467 (Mm), CHEMBL4802010 (Rn)
Ensembl Gene ENSG00000116783 (Hs), ENSMUSG00000040086 (Mm), ENSRNOG00000028225 (Rn)
Entrez Gene 51086 (Hs), 435766 (Mm), 295531 (Rn)
Human Protein Atlas ENSG00000116783 (Hs)
KEGG Enzyme 2.7.11.1
KEGG Gene hsa:51086 (Hs), mmu:435766 (Mm), rno:295531 (Rn)
OMIM 613932 (Hs)
Pharos Q59H18 (Hs)
RefSeq Nucleotide NM_015978 (Hs), NM_177066 (Mm), NM_181769 (Rn)
RefSeq Protein NP_057062 (Hs), NP_796040 (Mm), NP_861434 (Rn)
UniProtKB Q59H18 (Hs), Q5GIG6 (Mm), Q7TQP6 (Rn)
Wikipedia TNNI3K (Hs)
Selected 3D Structures Click here for help
Image of receptor 3D structure from RCSB PDB
Description:  TNNI3K complexed with 1-(3,5-dichloro-4-((6-(methylamino)pyrimidin-4-yl)oxy)phenyl)-3-(3-(trifluoromethyl)phenyl)urea
PDB Id:  7MGK
Ligand:  GSK329
Resolution:  3.1Å
Species:  Human
References:  4
Enzyme Reaction Click here for help
EC Number: 2.7.11.1

Download all structure-activity data for this target as a CSV file go icon to follow link

Inhibitors
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
sorafenib Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Hs Binding 6.6 pKd 2-3
⤷ pKd 6.6 (Kd 2.8x10-7 M) [2-3]
GSK329 Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 9.3 pKi 4
⤷ pKi 9.3 (Ki 5.4x10-10 M) [4]
GSK329 Small molecule or natural product Ligand has a PDB structure Mm Inhibition 7.9 pKi 4
⤷ pKi 7.9 (Ki 1.3x10-8 M) [4]
GSK329 Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 8.0 pIC50 4
⤷ pIC50 8.0 (IC50 1x10-8 M) [4]
View species-specific inhibitor tables
DiscoveRx KINOMEscan® screen Click here for help
A screen of 72 inhibitors against 456 human kinases. Quantitative data were derived using DiscoveRx KINOMEscan® platform.
http://www.discoverx.com/services/drug-discovery-development-services/kinase-profiling/kinomescan
Reference: 1,5
Key to terms and symbols Click column headers to sort
Target used in screen: TNNI3K
Ligand Sp. Type Action Value Parameter
dasatinib Small molecule or natural product Approved drug Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 8.0 pKd
PD-173955 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 7.3 pKd
alvocidib Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 7.3 pKd
crizotinib Small molecule or natural product Approved drug Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 7.0 pKd
foretinib Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 6.9 pKd
bosutinib Small molecule or natural product Approved drug Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 6.8 pKd
AST-487 Small molecule or natural product Hs Inhibitor Inhibition 6.8 pKd
motesanib Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 6.7 pKd
sorafenib Small molecule or natural product Approved drug Ligand has a PDB structure Hs Inhibitor Inhibition 6.6 pKd
tamatinib Small molecule or natural product Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 6.5 pKd
Displaying the top 10 most potent ligands  View all ligands in screen »
Clinically-Relevant Mutations and Pathophysiology Click here for help
Disease:  Cardiac conduction disease with or without dilated cardiomyopathy; CCDD
OMIM: 616117

References

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1. Davis MI, Hunt JP, Herrgard S, Ciceri P, Wodicka LM, Pallares G, Hocker M, Treiber DK, Zarrinkar PP. (2011) Comprehensive analysis of kinase inhibitor selectivity. Nat Biotechnol, 29 (11): 1046-51. [PMID:22037378]

2. Fabian MA, Biggs 3rd WH, Treiber DK, Atteridge CE, Azimioara MD, Benedetti MG, Carter TA, Ciceri P, Edeen PT, Floyd M et al.. (2005) A small molecule-kinase interaction map for clinical kinase inhibitors. Nat Biotechnol, 23 (3): 329-36. [PMID:15711537]

3. Karaman MW, Herrgard S, Treiber DK, Gallant P, Atteridge CE, Campbell BT, Chan KW, Ciceri P, Davis MI, Edeen PT et al.. (2008) A quantitative analysis of kinase inhibitor selectivity. Nat Biotechnol, 26 (1): 127-32. [PMID:18183025]

4. Patterson JR, Graves AP, Stoy P, Cheung M, Desai TA, Fries H, Gatto Jr GJ, Holt DA, Shewchuk L, Totoritis R et al.. (2021) Identification of Diarylurea Inhibitors of the Cardiac-Specific Kinase TNNI3K by Designing Selectivity Against VEGFR2, p38α, and B-Raf. J Med Chem, 64 (21): 15651-15670. [PMID:34699203]

5. Wodicka LM, Ciceri P, Davis MI, Hunt JP, Floyd M, Salerno S, Hua XH, Ford JM, Armstrong RC, Zarrinkar PP et al.. (2010) Activation state-dependent binding of small molecule kinase inhibitors: structural insights from biochemistry. Chem Biol, 17 (11): 1241-9. [PMID:21095574]

How to cite this page

HH498 subfamily: TNNI3 interacting kinase. Last modified on 17/11/2021. Accessed on 24/01/2025. IUPHAR/BPS Guide to PHARMACOLOGY, https://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2247.