Reaction Details Report a problem with these data
Target
Insulin-like growth factor 1 receptor
Ligand
BDBM15016
Substrate
Peptide Substrate
Meas. Tech.
Homogeneous Time-Resolved Fluorescence (HTRF) Assay
pH
7.4±n/a
Temperature
295.15±n/a K
IC50
2600±1000 nM
Citation
 Bell, IM; Stirdivant, SM; Ahern, J; Culberson, JC; Darke, PL; Dinsmore, CJ; Drakas, RA; Gallicchio, SN; Graham, SL; Heimbrook, DC; Hall, DL; Hua, J; Kett, NR; Kim, AS; Kornienko, M; Kuo, LC; Munshi, SK; Quigley, AG; Reid, JC; Trotter, BW; Waxman, LH; Williams, TM; Zartman, CB Biochemical and structural characterization of a novel class of inhibitors of the type 1 insulin-like growth factor and insulin receptor kinases. Biochemistry 44:9430-40 (2005) [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:
BDBM15016
Synonyms:
Ethyl 5-[(tert-Butylamino)carbonyl]-4-ethyl-2-formyl-1Hpyrrole-3-carboxylate | Pyrrole Analogue 6 | ethyl 5-(tert-butylcarbamoyl)-4-ethyl-2-formyl-1H-pyrrole-3-carboxylate
Type:
Small organic molecule
Emp. Form.:
C15H22N2O4
Mol. Mass.:
294.3462
SMILES:
CCOC(=O)c1c(CC)c([nH]c1C=O)C(=O)NC(C)(C)C
Structure:
Search PDB for entries with ligand similarity:
Substrate
Name:
Peptide Substrate
Synonyms:
n/a
Type:
Peptide
Mol. Mass.:
2600.09
Organism:
n/a
Description:
n/a
Residue:
21
Sequence:
ITINEQEDEPEGDYFEWLENH