Reaction Details Report a problem with these data
Target
Insulin-like growth factor 1 receptor
Ligand
BDBM27836
Substrate
Biotinylated substrate peptide
Meas. Tech.
IGF-1R Inhibition Assay
pH
7.5±n/a
Temperature
295.15±n/a K
IC50
4±n/a nM
Citation
 Chamberlain, SD; Wilson, JW; Deanda, F; Patnaik, S; Redman, AM; Yang, B; Shewchuk, L; Sabbatini, P; Leesnitzer, MA; Groy, A; Atkins, C; Gerding, R; Hassell, AM; Lei, H; Mook, RA; Moorthy, G; Rowand, JL; Stevens, KL; Kumar, R; Shotwell, JB Discovery of 4,6-bis-anilino-1H-pyrrolo[2,3-d]pyrimidines: potent inhibitors of the IGF-1R receptor tyrosine kinase. Bioorg Med Chem Lett 19:469-73 (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:
BDBM27836
Synonyms:
2-fluoro-6-{[2-({3-fluoro-2-methoxy-4-[4-(propan-2-yl)piperazin-1-yl]phenyl}amino)-7H-pyrrolo[2,3-d]pyrimidin-4-yl]amino}benzamide | 4,6-bis-anilino-1H-pyrrolo[2,3-d]pyrimidine, 20
Type:
Small organic molecule
Emp. Form.:
C27H30F2N8O2
Mol. Mass.:
536.5763
SMILES:
COc1c(Nc2nc(Nc3cccc(F)c3C(N)=O)c3cc[nH]c3n2)ccc(N2CCN(CC2)C(C)C)c1F
Structure:
Search PDB for entries with ligand similarity:
Substrate
Name:
Biotinylated substrate peptide
Synonyms:
n/a
Type:
Peptide
Mol. Mass.:
3542.16
Organism:
n/a
Description:
n/a
Residue:
29
Sequence:
ITINAMINHEYLAEEEEYMMMMAKKKKNH