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Target
Insulin-like growth factor 1 receptor
Ligand
BDBM50336321
Substrate
n/a
Meas. Tech.
ChEMBL_716595 (CHEMBL1670374)
IC50
5±n/a nM
Citation
 Jin, M; Kleinberg, A; Cooke, A; Gokhale, PC; Foreman, K; Dong, H; Siu, KW; Bittner, MA; Mulvihill, KM; Yao, Y; Landfair, D; O'Connor, M; Mak, G; Pachter, JA; Wild, R; Rosenfeld-Franklin, M; Ji, Q; Mulvihill, 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:
BDBM50336321
Synonyms:
CHEMBL1667939 | trans-4-(8-amino-1-(8-fluoro-2-phenylquinolin-7-yl)imidazo[1,5-a]pyrazin-3-yl)-N-methylcyclohexanecarboxamide
Type:
Small organic molecule
Emp. Form.:
C29H27FN6O
Mol. Mass.:
494.5627
SMILES:
CNC(=O)[C@H]1CC[C@@H](CC1)c1nc(-c2ccc3ccc(nc3c2F)-c2ccccc2)c2c(N)nccn12 |r,wU:7.10,wD:4.3,(12.87,-39.64,;12.08,-40.96,;10.54,-40.95,;9.76,-42.27,;10.06,-39.48,;11.09,-38.33,;10.61,-36.86,;9.11,-36.56,;8.08,-37.71,;8.56,-39.16,;8.62,-35.1,;9.52,-33.85,;8.61,-32.61,;9.38,-31.28,;8.61,-29.95,;9.37,-28.62,;10.92,-28.62,;11.68,-27.29,;13.21,-27.29,;13.99,-28.62,;13.22,-29.95,;11.69,-29.95,;10.92,-31.28,;11.69,-32.62,;15.52,-28.62,;16.29,-29.96,;17.83,-29.96,;18.6,-28.62,;17.82,-27.29,;16.28,-27.29,;7.14,-33.09,;5.81,-32.33,;5.8,-30.79,;4.48,-33.1,;4.48,-34.64,;5.81,-35.41,;7.15,-34.63,)|
Structure:
Search PDB for entries with ligand similarity: