Target
Insulin-like growth factor 1 receptor
Ligand
BDBM50336331
Substrate
n/a
Meas. Tech.
ChEMBL_716595 (CHEMBL1670374)
IC50
14±n/a nM
Citation
 Jin, MKleinberg, ACooke, AGokhale, PCForeman, KDong, HSiu, KWBittner, MAMulvihill, KMYao, YLandfair, DO'Connor, MMak, GPachter, JAWild, RRosenfeld-Franklin, MJi, QMulvihill, MJ Potent and selective cyclohexyl-derived imidazopyrazine insulin-like growth factor 1 receptor inhibitors with in vivo efficacy. Bioorg Med Chem Lett 21:1176-80 (2011) [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:
BDBM50336331
Synonyms:
CHEMBL1667950 | trans-4-(8-amino-1-(8-fluoro-2-phenylquinolin-7-yl)imidazo[1,5-a]pyrazin-3-yl)-N-(1-methyl-1H-benzo[d]imidazol-2-yl)cyclohexanecarboxamide
Type:
Small organic molecule
Emp. Form.:
C36H31FN8O
Mol. Mass.:
610.6827
SMILES:
Cn1c(NC(=O)[C@H]2CC[C@@H](CC2)c2nc(-c3ccc4ccc(nc4c3F)-c3ccccc3)c3c(N)nccn23)nc2ccccc12 |r,wU:9.12,wD:6.5,(31.09,-42.68,;30.06,-41.52,;28.53,-41.68,;27.74,-43,;26.2,-42.98,;25.41,-44.31,;25.72,-41.52,;26.75,-40.37,;26.27,-38.9,;24.76,-38.6,;23.73,-39.74,;24.21,-41.2,;24.27,-37.14,;25.17,-35.88,;24.26,-34.64,;25.03,-33.31,;24.26,-31.98,;25.03,-30.65,;26.58,-30.65,;27.34,-29.32,;28.87,-29.32,;29.64,-30.65,;28.87,-31.98,;27.34,-31.98,;26.57,-33.32,;27.34,-34.65,;31.18,-30.65,;31.95,-31.99,;33.49,-31.99,;34.26,-30.65,;33.48,-29.31,;31.94,-29.32,;22.79,-35.12,;21.46,-34.36,;21.45,-32.82,;20.13,-35.13,;20.13,-36.68,;21.46,-37.45,;22.8,-36.67,;27.92,-40.25,;29.08,-39.24,;29.09,-37.71,;30.42,-36.95,;31.75,-37.73,;31.73,-39.27,;30.4,-40.02,)|
Structure:
Search PDB for entries with ligand similarity: