Target
Insulin receptor
Ligand
BDBM2683
Substrate
peptide 1150
Meas. Tech.
Tyrosine Kinase Inhibition Assay
pH
7.4±n/a
Temperature
296.15±n/a K
IC50
>100000±n/a nM
Citation
 Toullec, DPianetti, PCoste, HBellevergue, PGrand-Perret, TAjakane, MBaudet, VBoissin, PBoursier, ELoriolle, F The bisindolylmaleimide GF 109203X is a potent and selective inhibitor of protein kinase C. J Biol Chem 266:15771-81 (1991) [PubMed] 
Target
Name:
Insulin receptor
Synonyms:
INSR_RAT | IR | Insr | Insulin Receptor Tyrosine Kinase (IRK)
Type:
Enzyme
Mol. Mass.:
156740.87
Organism:
Rattus norvegicus (rat)
Description:
n/a
Residue:
1383
Sequence:
MGSGRGCETTAVPLLMAVAVAGGTAGHLYPGEVCPGMDIRNNLTRLHELENCSVIEGHLQILLMFKTRPEDFRDLSFPKLIMITDYLLLFRVYGLESLKDLFPNLTVIRGSRLFFNYALVIFEMVHLKELGLYNLMNITRGSVRIEKNNELCYLATIDWSRILDYVEDNYIVLNKDDNEECGDVCPGTAKGKTNCPATVINGQFVERCWTHSHCQKVCPTICKSHGCTAEGLCCHKECLGNCSEPDDPTKCVACRNFYLDGQCVETCPPPYYHFQDWRCVNFSFCQDLHYKCRNSRKPGCHQYVIHNNKCIPECPSGYTMNSSNLMCTPCLGPCPKVCQILEGEKTIDSVTSAQELRGCTVINGSLIINIRGGNNLAAELEANLGLIEEISGFLKIRRSYALVSLSFFRKLHLIRGETLEIGNYSFYALDNQNLRQLWDWNKHNLTITQGKLFFHYNPKLCLSEIHKMEEVSGTKGRQERNDIALKTNGDQASCENELLKFSFIRTSFDKILLRWEPYWPPDFRDLLGFMLFYKEAPYQNVTEFDGQDACGSNSWTVVDIDPPQRSNDPKSQTPSHPGWLMRGLKPWTQYAIFVKTLVTFSDERRTYGAKSDIIYVQTDATNPSVPLDPISVSNSSSQIILKWKPPSDPNGNITHYLVYWERQAEDSELFELDYCLKGLKLPSRTWSPPFESDDSQKHNQSEYDDSASECCSCPKTDSQILKELEESSFRKTFEDYLHNVVFVPRKTSSGNGAEDTRPSRKRRSLEEVGNVTATTPTLPDFPNISSTIAPTSHEEHRPFEKVVNKESLVISGLRHFTGYRIELQACNQDSPEERSGVAAYVSARTMPEAKADDIVGPVTHEIFENNVVHLMWQEPKEPNGLIVLYEVSYRRYGDEELHLCVSRKHFALERGCRLRGLSPGNYSVRVRATSLAGNGSWTEPTYFYVTDYLDVPSNIAKIIIGPLIFVFLFSVVIGSIYLFLRKRQPDGPMGPLYASSNPEYLSASDVFPSSVYVPDEWEVPREKITLLRELGQGSFGMVYEGNAKDIIKGEVETRVAVKTVNESASLRERIEFLNEASVMKGFTCHHVVRLLGVVSKGQPTLVVMELMAHGDLKSHLRSLRPDAENNPGRPPPTLQEMIQMTAEIADGMAYLNAKKFVHRDLAARNCMVAHDFTVKIGDFGMTRDIYETDYYRKGGKGLLPVRWMSPESLKDGVFTASSDMWSFGVVLWEITSLAEQPYQGLSNEQVLKFVMDGGYLDPPDNCPERLTDLMRMCWQFNPKMRPTFLEIVNLLKDDLHPSFPEVSFFYSEENKAPESEELEMEFEDMENVPLDRSSHCQREEAGCREGGSSLSIKRTYDEHIPYTHMNGGKKNGRVLTLPRSNPS
  
Inhibitor
Name:
BDBM2683
Synonyms:
2-[1-(3-dimethylaminopropyl)-indol-3-yl]-3-(indol-3-yl)maleimide | 3-{1-[3-(dimethylamino)propyl]-1H-indol-3-yl}-4-(1H-indol-3-yl)-2,5-dihydro-1H-pyrrole-2,5-dione | BIM-1 | CHEMBL7463 | GF 109203X | JMC526193 Compound 2
Type:
Small organic molecule
Emp. Form.:
C25H24N4O2
Mol. Mass.:
412.4837
SMILES:
CN(C)CCCn1cc(C2=C(C(=O)NC2=O)c2c[nH]c3ccccc23)c2ccccc12 |t:9|
Structure:
Search PDB for entries with ligand similarity:
Substrate
Name:
peptide 1150
Synonyms:
n/a
Type:
Peptide
Mol. Mass.:
4295.28
Organism:
n/a
Description:
Amino acids 1142-1153 of the beta subunit of the human insulin receptor. 50 uM [gamma-32P]ATP as co-substrate.
Residue:
37
Sequence:
NHTHRARGASPILETYRGLTHRASPTYRTYRARGLYS