Reaction Details Report a problem with these data
Target
Insulin-like growth factor 1 receptor
Ligand
BDBM50336325
Substrate
n/a
Meas. Tech.
ChEMBL_716595 (CHEMBL1670374)
IC50
2±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:
BDBM50336325
Synonyms:
CHEMBL1667943 | trans-4-(8-amino-1-(8-fluoro-2-phenylquinolin-7-yl)imidazo[1,5-a]pyrazin-3-yl)-N-(thiazol-2-yl)cyclohexanecarboxamide
Type:
Small organic molecule
Emp. Form.:
C31H26FN7OS
Mol. Mass.:
563.648
SMILES:
Nc1nccn2c(nc(-c3ccc4ccc(nc4c3F)-c3ccccc3)c12)[C@H]1CC[C@@H](CC1)C(=O)Nc1nccs1 |r,wU:27.31,wD:30.38,(5.48,2.11,;5.49,.57,;4.16,-.2,;4.16,-1.75,;5.49,-2.52,;6.83,-1.74,;8.3,-2.21,;9.2,-.95,;8.29,.29,;9.06,1.62,;8.29,2.94,;9.05,4.28,;10.6,4.28,;11.36,5.6,;12.89,5.61,;13.67,4.27,;12.9,2.95,;11.37,2.95,;10.6,1.61,;11.37,.28,;15.2,4.27,;15.97,2.94,;17.51,2.94,;18.28,4.27,;17.5,5.61,;15.96,5.6,;6.82,-.2,;8.79,-3.67,;10.29,-3.97,;10.77,-5.44,;9.74,-6.59,;8.24,-6.27,;7.76,-4.81,;10.22,-8.05,;9.44,-9.37,;11.76,-8.07,;12.52,-9.41,;12.05,-10.87,;13.3,-11.77,;14.54,-10.87,;14.07,-9.4,)|
Structure:
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