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Target
Ribosomal protein S6 kinase alpha-2
Ligand
BDBM25017
Substrate
n/a
Meas. Tech.
ChEMBL_2131821 (CHEMBL4841336)
IC50
18±n/a nM
Citation
 Yuan, Y; Xu, J; Jiang, L; Yu, K; Ge, Y; Li, M; He, H; Niu, Q; Shi, X; Fan, L; Chen, Z; Zhao, Z; Li, S; Xu, Y; Wang, Z; Li, H Discovery, Optimization, and Structure-Activity Relationship Study of Novel and Potent RSK4 Inhibitors as Promising Agents for the Treatment of Esophageal Squamous Cell Carcinoma. J Med Chem 64:13572-13587 (2021) [PubMed]  Article 
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:
BDBM25017
Synonyms:
2-[(3,5-difluoro-4-hydroxyphenyl)amino]-5,7-dimethyl-8-(3-methylbutyl)-5,6,7,8-tetrahydropteridin-6-one | BI-D1870 | US11851436, Compound BI-D1870
Type:
Small organic molecule
Emp. Form.:
C19H23F2N5O2
Mol. Mass.:
391.415
SMILES:
CC(C)CCN1C(C)C(=O)N(C)c2cnc(Nc3cc(F)c(O)c(F)c3)nc12
Structure:
Search PDB for entries with ligand similarity: