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Target
Ribosomal protein S6 kinase alpha-2
Ligand
BDBM458758
Substrate
n/a
Meas. Tech.
Kinase Assay
IC50
94±n/a nM
Citation
 Dunn, SE; Jayanthan, A; Nagireddy, JR; Annedi, S; Van Drie, JH; Daynard, TS; Huynh, M Carboxamide derivatives useful as rsk inhibitors US Patent  US10758530 Publication Date 9/1/2020 
Target
Name:
Ribosomal protein S6 kinase alpha-2
Synonyms:
90 kDa ribosomal protein S6 kinase 2 | 90 kDa ribosomal protein S6 kinase 2 (RSK2) | KS6A2_HUMAN | MAP kinase-activated protein kinase 1c | MAPKAPK1C | RPS6KA2 | RPS6KA2(Kin.Dom.1 - N-terminal) | RSK3 | Ribosomal S6 Kinase 3 (RSK-3) | Ribosomal protein S6 kinase alpha 2 | Ribosomal protein S6 kinase alpha 2 (RSK2) | Ribosomal protein S6 kinase alpha-2 | p90-RSK 2 | p90RSK | pp90RSK3
Type:
Serine/threonine-protein kinase
Mol. Mass.:
83259.46
Organism:
Homo sapiens (Human)
Description:
n/a
Residue:
733
Sequence:
MDLSMKKFAVRRFFSVYLRRKSRSKSSSLSRLEEEGVVKEIDISHHVKEGFEKADPSQFELLKVLGQGSYGKVFLVRKVKGSDAGQLYAMKVLKKATLKVRDRVRSKMERDILAEVNHPFIVKLHYAFQTEGKLYLILDFLRGGDLFTRLSKEVMFTEEDVKFYLAELALALDHLHSLGIIYRDLKPENILLDEEGHIKITDFGLSKEAIDHDKRAYSFCGTIEYMAPEVVNRRGHTQSADWWSFGVLMFEMLTGSLPFQGKDRKETMALILKAKLGMPQFLSGEAQSLLRALFKRNPCNRLGAGIDGVEEIKRHPFFVTIDWNTLYRKEIKPPFKPAVGRPEDTFHFDPEFTARTPTDSPGVPPSANAHHLFRGFSFVASSLIQEPSQQDLHKVPVHPIVQQLHGNNIHFTDGYEIKEDIGVGSYSVCKRCVHKATDTEYAVKIIDKSKRDPSEEIEILLRYGQHPNIITLKDVYDDGKFVYLVMELMRGGELLDRILRQRYFSEREASDVLCTITKTMDYLHSQGVVHRDLKPSNILYRDESGSPESIRVCDFGFAKQLRAGNGLLMTPCYTANFVAPEVLKRQGYDAACDIWSLGILLYTMLAGFTPFANGPDDTPEEILARIGSGKYALSGGNWDSISDAAKDVVSKMLHVDPHQRLTAMQVLKHPWVVNREYLSPNQLSRQDVHLVKGAMAATYFALNRTPQAPRLEPVLSSNLAQRRGMKRLTSTRL
  
Inhibitor
Name:
BDBM458758
Synonyms:
(R)-1-benzyl-N-(9-methyl-6-oxo-6,7,8,9-tetrahydropyrido[3′,2′:4,5]pyrrolo[1,2-a]pyrazin-2-yl)-1H-pyrazole-4-carboxamide | US10758530, Compound 15
Type:
Small organic molecule
Emp. Form.:
C22H20N6O2
Mol. Mass.:
400.4332
SMILES:
C[C@@H]1CNC(=O)c2cc3ccc(NC(=O)c4cnn(Cc5ccccc5)c4)nc3n12 |r|
Structure:
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