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Target
Ribosomal protein S6 kinase alpha-5
Ligand
BDBM50326208
Substrate
n/a
Meas. Tech.
ChEMBL_659364 (CHEMBL1247991)
IC50
>25000±n/a nM
Citation
Cee, VJ; Schenkel, LB; Hodous, BL; Deak, HL; Nguyen, HN; Olivieri, PR; Romero, K; Bak, A; Be, X; Bellon, S; Bush, TL; Cheng, AC; Chung, G; Coats, S; Eden, PM; Hanestad, K; Gallant, PL; Gu, Y; Huang, X; Kendall, RL; Lin, MH; Morrison, MJ; Patel, VF; Radinsky, R; Rose, PE; Ross, S; Sun, JR; Tang, J; Zhao, H; Payton, M; Geuns-Meyer, SD Discovery of a potent, selective, and orally bioavailable pyridinyl-pyrimidine phthalazine aurora kinase inhibitor. J Med Chem 53:6368-77 (2010) [PubMed] Article
More Info.:
Target
Name:
Ribosomal protein S6 kinase alpha-5
Synonyms:
90 kDa ribosomal protein S6 kinase 5 | KS6A5_HUMAN | MSK1 | Mitogen- and Stress-Activated Protein Kinase 1 (MSK1) | Nuclear mitogen- and stress-activated protein kinase 1 | Nuclear mitogen- and stress-activated protein kinase 1 (MSK1) | RPS6KA5 | RPS6KA5(Kin.Dom.2 - C-terminal) | RSK-like protein kinase | RSKL | Ribosomal protein S6 kinase | Ribosomal protein S6 kinase alpha 5 | Ribosomal protein S6 kinase alpha-5
Type:
Serine/threonine-protein kinase
Mol. Mass.:
89874.44
Organism:
Homo sapiens (Human)
Description:
n/a
Residue:
802
Sequence:
MEEEGGSSGGAAGTSADGGDGGEQLLTVKHELRTANLTGHAEKVGIENFELLKVLGTGAYGKVFLVRKISGHDTGKLYAMKVLKKATIVQKAKTTEHTRTERQVLEHIRQSPFLVTLHYAFQTETKLHLILDYINGGELFTHLSQRERFTEHEVQIYVGEIVLALEHLHKLGIIYRDIKLENILLDSNGHVVLTDFGLSKEFVADETERAYSFCGTIEYMAPDIVRGGDSGHDKAVDWWSLGVLMYELLTGASPFTVDGEKNSQAEISRRILKSEPPYPQEMSALAKDLIQRLLMKDPKKRLGCGPRDADEIKEHLFFQKINWDDLAAKKVPAPFKPVIRDELDVSNFAEEFTEMDPTYSPAALPQSSEKLFQGYSFVAPSILFKRNAAVIDPLQFHMGVERPGVTNVARSAMMKDSPFYQHYDLDLKDKPLGEGSFSICRKCVHKKSNQAFAVKIISKRMEANTQKEITALKLCEGHPNIVKLHEVFHDQLHTFLVMELLNGGELFERIKKKKHFSETEASYIMRKLVSAVSHMHDVGVVHRDLKPENLLFTDENDNLEIKIIDFGFARLKPPDNQPLKTPCFTLHYAAPELLNQNGYDESCDLWSLGVILYTMLSGQVPFQSHDRSLTCTSAVEIMKKIKKGDFSFEGEAWKNVSQEAKDLIQGLLTVDPNKRLKMSGLRYNEWLQDGSQLSSNPLMTPDILGSSGAAVHTCVKATFHAFNKYKREGFCLQNVDKAPLAKRRKMKKTSTSTETRSSSSESSHSSSSHSHGKTTPTKTLQPSNPADSNNPETLFQFSDSVA
Inhibitor
Name:
BDBM50326208
Synonyms:
4-(4-Fluorophenyl)-N-(4-(3-(2-(methylamino)pyrimidin-4-yl)-pyridin-2-yloxy)phenyl)phthalazin-1-amine | CHEMBL1243326
Type:
Small organic molecule
Emp. Form.:
C30H22FN7O
Mol. Mass.:
515.5404
SMILES:
CNc1nccc(n1)-c1cccnc1Oc1ccc(Nc2nnc(-c3ccc(F)cc3)c3ccccc23)cc1