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Target not currently curated in GtoImmuPdb
Target id: 1507
Nomenclature: CDC42 binding protein kinase alpha
Abbreviated Name: MRCKα
Family: GEK subfamily
Gene and Protein Information ![]() |
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Species | TM | AA | Chromosomal Location | Gene Symbol | Gene Name | Reference |
Human | - | 1732 | 1q42.13 | CDC42BPA | CDC42 binding protein kinase alpha | |
Mouse | - | 1719 | 1 H4 | Cdc42bpa | CDC42 binding protein kinase alpha | |
Rat | - | 1732 | 13q26 | Cdc42bpa | CDC42 binding protein kinase alpha |
Previous and Unofficial Names ![]() |
MRCKA | MRCK alpha | serine/threonine-protein kinase MRCK alpha | MRCK | PK428 | CDC42 binding protein kinase alpha (DMPK-like) |
Database Links ![]() |
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Alphafold | Q5VT25 (Hs), Q3UU96 (Mm), O54874 (Rn) |
BRENDA | 2.7.11.1 |
CATH/Gene3D | 2.30.29.30, 3.90.810.10 |
ChEMBL Target | CHEMBL4516 (Hs) |
Ensembl Gene | ENSG00000143776 (Hs), ENSMUSG00000026490 (Mm), ENSRNOG00000002841 (Rn) |
Entrez Gene | 8476 (Hs), 226751 (Mm), 114116 (Rn) |
Human Protein Atlas | ENSG00000143776 (Hs) |
KEGG Enzyme | 2.7.11.1 |
KEGG Gene | hsa:8476 (Hs), mmu:226751 (Mm), rno:114116 (Rn) |
OMIM | 603412 (Hs) |
Pharos | Q5VT25 (Hs) |
RefSeq Nucleotide | NM_003607 (Hs), NM_001033285 (Mm), NM_053657 (Rn) |
RefSeq Protein | NP_003598 (Hs), NP_001028457 (Mm), NP_446109 (Rn) |
UniProtKB | Q5VT25 (Hs), Q3UU96 (Mm), O54874 (Rn) |
Wikipedia | CDC42BPA (Hs) |
Selected 3D Structures ![]() |
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Enzyme Reaction ![]() |
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Download all structure-activity data for this target as a CSV file
Inhibitors | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
Key to terms and symbols | View all chemical structures | Click column headers to sort | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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DiscoveRx KINOMEscan® screen ![]() |
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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: 3,6 |
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Target used in screen: MRCKA | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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Displaying the top 10 most potent ligands View all ligands in screen » |
EMD Millipore KinaseProfilerTM screen/Reaction Biology Kinase HotspotSM screen ![]() |
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A screen profiling 158 kinase inhibitors (Calbiochem Protein Kinase Inhibitor Library I and II, catalogue numbers 539744 and 539745) for their inhibitory activity at 1µM and 10µM against 234 human recombinant kinases using the EMD Millipore KinaseProfilerTM service. A screen profiling the inhibitory activity of 178 commercially available kinase inhibitors at 0.5µM against a panel of 300 recombinant protein kinases using the Reaction Biology Corporation Kinase HotspotSM platform. http://www.millipore.com/techpublications/tech1/pf3036 http://www.reactionbiology.com/webapps/main/pages/kinase.aspx Reference: 1,4 |
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Target used in screen: MRCKα/MRCKa(CDC42BPA) | ||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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Displaying the top 10 most potent ligands View all ligands in screen » |
1. Anastassiadis T, Deacon SW, Devarajan K, Ma H, Peterson JR. (2011) Comprehensive assay of kinase catalytic activity reveals features of kinase inhibitor selectivity. Nat Biotechnol, 29 (11): 1039-45. [PMID:22037377]
2. Chen YT, Vojkovsky T, Fang X, Pocas JR, Grant W, Handy AMW, Schroter T, LoGrasso P, Bannister TD, Feng Y. (2011) Asymmetric synthesis of potent chroman-based Rho kinase (ROCK-II) inhibitors. Medchemcomm, 2: 73-75.
3. 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]
4. Gao Y, Davies SP, Augustin M, Woodward A, Patel UA, Kovelman R, Harvey KJ. (2013) A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. Biochem J, 451 (2): 313-28. [PMID:23398362]
5. Pireddu R, Forinash KD, Sun NN, Martin MP, Sung SS, Alexander B, Zhu JY, Guida WC, Schönbrunn E, Sebti SM et al.. (2012) Pyridylthiazole-based ureas as inhibitors of Rho associated protein kinases (ROCK1 and 2). Medchemcomm, 3 (6): 699-709. [PMID:23275831]
6. 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]
GEK subfamily: CDC42 binding protein kinase alpha. Last modified on 29/01/2016. Accessed on 16/03/2025. IUPHAR/BPS Guide to PHARMACOLOGY, https://www.guidetoimmunopharmacology.org/GRAC/ObjectDisplayForward?objectId=1507.