Reaction Details  Report a problem with these data
Target
Proto-oncogene tyrosine-protein kinase Src
Ligand
BDBM50544968
Substrate
n/a
Meas. Tech.
ChEMBL_1994130 (CHEMBL4628025)
IC50
>10000±n/a nM
Citation
 Evison, BJ; Palmer, JT; Lambert, G; Treutlein, H; Zeng, J; Nativel, B; Chemello, K; Zhu, Q; Wang, J; Teng, Y; Tang, W; Xu, Y; Rathi, AK; Kumar, S; Suchowerska, AK; Parmar, J; Dixon, I; Kelly, GE; Bonnar, J A small molecule inhibitor of PCSK9 that antagonizes LDL receptor binding via interaction with a cryptic PCSK9 binding groove. Bioorg Med Chem 28:0 (2020) [PubMed]  Article
Target
Name:
Proto-oncogene tyrosine-protein kinase Src
Synonyms:
Calmodulin/Proto-oncogene tyrosine-protein kinase Src | Protein cereblon/Tyrosine-protein kinase SRC | Proto-oncogene c-Src | Proto-oncogene tyrosine-protein kinase Src (c-Src) | SRC | SRC1 | SRC_HUMAN | Tyrosine-protein kinase Src (SRC) | V-src sarcoma (Schmidt-Ruppin A-2) viral oncogene homolog (avian) | c-Src | p60-Src | pp60c-src
Type:
Protein
Mol. Mass.:
59838.60
Organism:
Homo sapiens (Human)
Description:
P12931
Residue:
536
Sequence:
MGSNKSKPKDASQRRRSLEPAENVHGAGGGAFPASQTPSKPASADGHRGPSAAFAPAAAEPKLFGGFNSSDTVTSPQRAGPLAGGVTTFVALYDYESRTETDLSFKKGERLQIVNNTEGDWWLAHSLSTGQTGYIPSNYVAPSDSIQAEEWYFGKITRRESERLLLNAENPRGTFLVRESETTKGAYCLSVSDFDNAKGLNVKHYKIRKLDSGGFYITSRTQFNSLQQLVAYYSKHADGLCHRLTTVCPTSKPQTQGLAKDAWEIPRESLRLEVKLGQGCFGEVWMGTWNGTTRVAIKTLKPGTMSPEAFLQEAQVMKKLRHEKLVQLYAVVSEEPIYIVTEYMSKGSLLDFLKGETGKYLRLPQLVDMAAQIASGMAYVERMNYVHRDLRAANILVGENLVCKVADFGLARLIEDNEYTARQGAKFPIKWTAPEAALYGRFTIKSDVWSFGILLTELTTKGRVPYPGMVNREVLDQVERGYRMPCPPECPESLHDLMCQCWRKEPEERPTFEYLQAFLEDYFTSTEPQYQPGENL
  
Inhibitor
Name:
BDBM50544968
Synonyms:
CHEMBL4642587
Type:
Small organic molecule
Emp. Form.:
C30H29N7O3S
Mol. Mass.:
567.661
SMILES:
Cc1cn(cn1)-c1cc(CCS(N)(=O)=O)cc(NC(=O)c2ccc(C)c(Nc3nccc(n3)-c3ccccc3)c2)c1
Structure:
Search PDB for entries with ligand similarity: