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Target
Serine/threonine-protein kinase PRP4 homolog
Ligand
BDBM213236
Substrate
Serine/threonine-protein kinase PAK 4
Meas. Tech.
MS-Based Biochemical Assay
pH
7.5±n/a
Temperature
298.15±n/a K
IC50
16±n/a nM
Comments
extracted
Citation
 Gao, Q; Mechin, I; Kothari, N; Guo, Z; Deng, G; Haas, K; McManus, J; Hoffmann, D; Wang, A; Wiederschain, D; Rocnik, J; Czechtizky, W; Chen, X; McLean, L; Arlt, H; Harper, D; Liu, F; Majid, T; Patel, V; Lengauer, C; Garcia-Echeverria, C; Zhang, B; Cheng, H; Dorsch, M; Huang, SM Evaluation of cancer dependence and druggability of PRP4 kinase using cellular, biochemical, and structural approaches. J Biol Chem 288:30125-38 (2013) [PubMed]  Article 
Target
Name:
Serine/threonine-protein kinase PRP4 homolog
Synonyms:
KIAA0536 | PRP4 | PRP4 kinase | PRP4 kinase (PRP4) | PRP4 pre-mRNA-processing factor 4 homolog | PRP4B_HUMAN | PRP4H | PRP4K | PRPF4B | Serine/threonine-protein kinase PRP4 homolog
Type:
Enzyme
Mol. Mass.:
117103.41
Organism:
Homo sapiens (Human)
Description:
Q13523
Residue:
1007
Sequence:
MAAAETQSLREQPEMEDANSEKSINEENGEVSEDQSQNKHSRHKKKKHKHRSKHKKHKHSSEEDKDKKHKHKHKHKKHKRKEIIDASDKEGMSPAKRTKLDDLALLEDLEKQRALIKAELDNELMEGKVQSGMGLILQGYESGSEEEGEIHEKARNGNRSSTRSSSTKGKLELVDNKITTKKRSKSRSKERTRHRSDKKKSKGGIEIVKEKTTRSKSKERKKSKSPSKRSKSQDQARKSKSPTLRRRSQEKIGKARSPTDDKVKIEDKSKSKDRKKSPIINESRSRDRGKKSRSPVDLRGKSKDRRSRSKERKSKRSETDKEKKPIKSPSKDASSGKENRSPSRRPGRSPKRRSLSPKPRDKSRRSRSPLLNDRRSKQSKSPSRTLSPGRRAKSRSLERKRREPERRRLSSPRTRPRDDILSRRERSKDASPINRWSPTRRRSRSPIRRRSRSPLRRSRSPRRRSRSPRRRDRGRRSRSRLRRRSRSRGGRRRRSRSKVKEDKFKGSLSEGMKVEQESSSDDNLEDFDVEEEDEEALIEQRRIQRQAIVQKYKYLAEDSNMSVPSEPSSPQSSTRTRSPSPDDILERVAADVKEYERENVDTFEASVKAKHNLMTVEQNNGSSQKKLLAPDMFTESDDMFAAYFDSARLRAAGIGKDFKENPNLRDNWTDAEGYYRVNIGEVLDKRYNVYGYTGQGVFSNVVRARDNARANQEVAVKIIRNNELMQKTGLKELEFLKKLNDADPDDKFHCLRLFRHFYHKQHLCLVFEPLSMNLREVLKKYGKDVGLHIKAVRSYSQQLFLALKLLKRCNILHADIKPDNILVNESKTILKLCDFGSASHVADNDITPYLVSRFYRAPEIIIGKSYDYGIDMWSVGCTLYELYTGKILFPGKTNNHMLKLAMDLKGKMPNKMIRKGVFKDQHFDQNLNFMYIEVDKVTEREKVTVMSTINPTKDLLADLIGCQRLPEDQRKKVHQLKDLLDQILMLDPAKRISINQALQHAFIQEKI
  
Inhibitor
Name:
BDBM213236
Synonyms:
4-ylmethyl)-carbamoyl]-thiophen-2-yl}-benzo[b]thiophene-2-carboxylic acid amine (Compound A)
Type:
Small organic molecule
Emp. Form.:
C20H14ClN3O2S2
Mol. Mass.:
427.927
SMILES:
NC(=O)c1cc2c(cccc2s1)-c1ccc(s1)C(=O)NCc1ccnc(Cl)c1
Structure:
Search PDB for entries with ligand similarity:
Substrate
Name:
Serine/threonine-protein kinase PAK 4
Synonyms:
KIAA1142 | PAK4 | PAK4_HUMAN | p21-Activated kinase 4 (PAK4)
Type:
Protein
Mol. Mass.:
64098.01
Organism:
Homo sapiens (Human)
Description:
O96013
Residue:
591
Sequence:
MFGKRKKRVEISAPSNFEHRVHTGFDQHEQKFTGLPRQWQSLIEESARRPKPLVDPACITSIQPGAPKTIVRGSKGAKDGALTLLLDEFENMSVTRSNSLRRDSPPPPARARQENGMPEEPATTARGGPGKAGSRGRFAGHSEAGGGSGDRRRAGPEKRPKSSREGSGGPQESSRDKRPLSGPDVGTPQPAGLASGAKLAAGRPFNTYPRADTDHPSRGAQGEPHDVAPNGPSAGGLAIPQSSSSSSRPPTRARGAPSPGVLGPHASEPQLAPPACTPAAPAVPGPPGPRSPQREPQRVSHEQFRAALQLVVDPGDPRSYLDNFIKIGEGSTGIVCIATVRSSGKLVAVKKMDLRKQQRRELLFNEVVIMRDYQHENVVEMYNSYLVGDELWVVMEFLEGGALTDIVTHTRMNEEQIAAVCLAVLQALSVLHAQGVIHRDIKSDSILLTHDGRVKLSDFGFCAQVSKEVPRRKSLVGTPYWMAPELISRLPYGPEVDIWSLGIMVIEMVDGEPPYFNEPPLKAMKMIRDNLPPRLKNLHKVSPSLKGFLDRLLVRDPAQRATAAELLKHPFLAKAGPPASIVPLMRQNRTR