Reaction Details Report a problem with these data
Target
Insulin-like growth factor 1 receptor
Ligand
BDBM28094
Substrate
Biotinylated substrate peptide
Meas. Tech.
In Vitro Kinase Inhibition Assay
pH
7.5±n/a
Temperature
295.15±n/a K
IC50
13700±4980 nM
Citation
 Miller, LM; Mayer, SC; Berger, DM; Boschelli, DH; Boschelli, F; Di, L; Du, X; Dutia, M; Floyd, MB; Johnson, M; Kenny, CH; Krishnamurthy, G; Moy, F; Petusky, S; Tkach, D; Torres, N; Wu, B; Xu, W Lead identification to generate 3-cyanoquinoline inhibitors of insulin-like growth factor receptor (IGF-1R) for potential use in cancer treatment. Bioorg Med Chem Lett 19:62-6 (2009) [PubMed]  Article 
Target
Name:
Insulin-like growth factor 1 receptor
Synonyms:
CD_antigen=CD221 | IGF-I receptor | IGF1R | IGF1R_HUMAN | Insulin-like growth factor 1 receptor (IGF1R) | Insulin-like growth factor 1 receptor (IGFIR) | Insulin-like growth factor 1 receptor alpha chain | Insulin-like growth factor 1 receptor beta chain | Insulin-like growth factor I receptor | Insulin-like growth factor receptor (IGFR)
Type:
Protein
Mol. Mass.:
154776.79
Organism:
Homo sapiens (Human)
Description:
P08069
Residue:
1367
Sequence:
MKSGSGGGSPTSLWGLLFLSAALSLWPTSGEICGPGIDIRNDYQQLKRLENCTVIEGYLHILLISKAEDYRSYRFPKLTVITEYLLLFRVAGLESLGDLFPNLTVIRGWKLFYNYALVIFEMTNLKDIGLYNLRNITRGAIRIEKNADLCYLSTVDWSLILDAVSNNYIVGNKPPKECGDLCPGTMEEKPMCEKTTINNEYNYRCWTTNRCQKMCPSTCGKRACTENNECCHPECLGSCSAPDNDTACVACRHYYYAGVCVPACPPNTYRFEGWRCVDRDFCANILSAESSDSEGFVIHDGECMQECPSGFIRNGSQSMYCIPCEGPCPKVCEEEKKTKTIDSVTSAQMLQGCTIFKGNLLINIRRGNNIASELENFMGLIEVVTGYVKIRHSHALVSLSFLKNLRLILGEEQLEGNYSFYVLDNQNLQQLWDWDHRNLTIKAGKMYFAFNPKLCVSEIYRMEEVTGTKGRQSKGDINTRNNGERASCESDVLHFTSTTTSKNRIIITWHRYRPPDYRDLISFTVYYKEAPFKNVTEYDGQDACGSNSWNMVDVDLPPNKDVEPGILLHGLKPWTQYAVYVKAVTLTMVENDHIRGAKSEILYIRTNASVPSIPLDVLSASNSSSQLIVKWNPPSLPNGNLSYYIVRWQRQPQDGYLYRHNYCSKDKIPIRKYADGTIDIEEVTENPKTEVCGGEKGPCCACPKTEAEKQAEKEEAEYRKVFENFLHNSIFVPRPERKRRDVMQVANTTMSSRSRNTTAADTYNITDPEELETEYPFFESRVDNKERTVISNLRPFTLYRIDIHSCNHEAEKLGCSASNFVFARTMPAEGADDIPGPVTWEPRPENSIFLKWPEPENPNGLILMYEIKYGSQVEDQRECVSRQEYRKYGGAKLNRLNPGNYTARIQATSLSGNGSWTDPVFFYVQAKTGYENFIHLIIALPVAVLLIVGGLVIMLYVFHRKRNNSRLGNGVLYASVNPEYFSAADVYVPDEWEVAREKITMSRELGQGSFGMVYEGVAKGVVKDEPETRVAIKTVNEAASMRERIEFLNEASVMKEFNCHHVVRLLGVVSQGQPTLVIMELMTRGDLKSYLRSLRPEMENNPVLAPPSLSKMIQMAGEIADGMAYLNANKFVHRDLAARNCMVAEDFTVKIGDFGMTRDIYETDYYRKGGKGLLPVRWMSPESLKDGVFTTYSDVWSFGVVLWEIATLAEQPYQGLSNEQVLRFVMEGGLLDKPDNCPDMLFELMRMCWQYNPKMRPSFLEIISSIKEEMEPGFREVSFYYSEENKLPEPEELDLEPENMESVPLDPSASSSSLPLPDRHSGHKAENGPGPGVLVLRASFDERQPYAHMNGGRKNERALPLPQSSTC
  
Inhibitor
Name:
BDBM28094
Synonyms:
3-cyanoquinoline, 19 | 4-({3-chloro-4-[(1-ethyl-4,5-dimethyl-1H-imidazol-2-yl)sulfanyl]phenyl}amino)-6-methoxy-7-[(3-phenylpropyl)amino]quinoline-3-carbonitrile
Type:
Small organic molecule
Emp. Form.:
C33H33ClN6OS
Mol. Mass.:
597.173
SMILES:
CCn1c(C)c(C)nc1Sc1ccc(Nc2c(cnc3cc(NCCCc4ccccc4)c(OC)cc23)C#N)cc1Cl
Structure:
Search PDB for entries with ligand similarity:
Substrate
Name:
Biotinylated substrate peptide
Synonyms:
n/a
Type:
Peptide
Mol. Mass.:
2453.64
Organism:
n/a
Description:
n/a
Residue:
19
Sequence:
ITINNHTRDIYETDYYRKH