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TargetInsulin-like growth factor 1 receptor
LigandBDBM50336328
Substrate/Competitorn/a
Meas. Tech.ChEMBL_716595 (CHEMBL1670374)
IC50 8±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 Lett21:1176-80 (2011) [PubMed]  Article
More Info.:Get all data from this article,  Assay Method
 
Insulin-like growth factor 1 receptor
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:
MKSGSGGGSPTSLWGLLFLSAALSLWPTSGEICGPGIDIRNDYQQLKRLENCTVIEGYLH
ILLISKAEDYRSYRFPKLTVITEYLLLFRVAGLESLGDLFPNLTVIRGWKLFYNYALVIF
EMTNLKDIGLYNLRNITRGAIRIEKNADLCYLSTVDWSLILDAVSNNYIVGNKPPKECGD
LCPGTMEEKPMCEKTTINNEYNYRCWTTNRCQKMCPSTCGKRACTENNECCHPECLGSCS
APDNDTACVACRHYYYAGVCVPACPPNTYRFEGWRCVDRDFCANILSAESSDSEGFVIHD
GECMQECPSGFIRNGSQSMYCIPCEGPCPKVCEEEKKTKTIDSVTSAQMLQGCTIFKGNL
LINIRRGNNIASELENFMGLIEVVTGYVKIRHSHALVSLSFLKNLRLILGEEQLEGNYSF
YVLDNQNLQQLWDWDHRNLTIKAGKMYFAFNPKLCVSEIYRMEEVTGTKGRQSKGDINTR
NNGERASCESDVLHFTSTTTSKNRIIITWHRYRPPDYRDLISFTVYYKEAPFKNVTEYDG
QDACGSNSWNMVDVDLPPNKDVEPGILLHGLKPWTQYAVYVKAVTLTMVENDHIRGAKSE
ILYIRTNASVPSIPLDVLSASNSSSQLIVKWNPPSLPNGNLSYYIVRWQRQPQDGYLYRH
NYCSKDKIPIRKYADGTIDIEEVTENPKTEVCGGEKGPCCACPKTEAEKQAEKEEAEYRK
VFENFLHNSIFVPRPERKRRDVMQVANTTMSSRSRNTTAADTYNITDPEELETEYPFFES
RVDNKERTVISNLRPFTLYRIDIHSCNHEAEKLGCSASNFVFARTMPAEGADDIPGPVTW
EPRPENSIFLKWPEPENPNGLILMYEIKYGSQVEDQRECVSRQEYRKYGGAKLNRLNPGN
YTARIQATSLSGNGSWTDPVFFYVQAKTGYENFIHLIIALPVAVLLIVGGLVIMLYVFHR
KRNNSRLGNGVLYASVNPEYFSAADVYVPDEWEVAREKITMSRELGQGSFGMVYEGVAKG
VVKDEPETRVAIKTVNEAASMRERIEFLNEASVMKEFNCHHVVRLLGVVSQGQPTLVIME
LMTRGDLKSYLRSLRPEMENNPVLAPPSLSKMIQMAGEIADGMAYLNANKFVHRDLAARN
CMVAEDFTVKIGDFGMTRDIYETDYYRKGGKGLLPVRWMSPESLKDGVFTTYSDVWSFGV
VLWEIATLAEQPYQGLSNEQVLRFVMEGGLLDKPDNCPDMLFELMRMCWQYNPKMRPSFL
EIISSIKEEMEPGFREVSFYYSEENKLPEPEELDLEPENMESVPLDPSASSSSLPLPDRH
SGHKAENGPGPGVLVLRASFDERQPYAHMNGGRKNERALPLPQSSTC
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  Blast E-value cutoff:
BDBM50336328
n/a
NameBDBM50336328
Synonyms:CHEMBL1667946 | trans-4-(8-amino-1-(8-fluoro-2-phenylquinolin-7-yl)imidazo[1,5-a]pyrazin-3-yl)-N-(pyrimidin-4-yl)cyclohexanecarboxamide
TypeSmall organic molecule
Emp. Form.C32H27FN8O
Mol. Mass.558.6082
SMILESNc1nccn2c(nc(-c3ccc4ccc(nc4c3F)-c3ccccc3)c12)[C@H]1CC[C@@H](CC1)C(=O)Nc1ccncn1 |r,wU:27.31,wD:30.38,(5.26,-16.47,;5.26,-18.01,;3.93,-18.78,;3.93,-20.33,;5.27,-21.1,;6.61,-20.32,;8.08,-20.79,;8.98,-19.53,;8.06,-18.29,;8.83,-16.97,;8.07,-15.64,;8.83,-14.3,;10.38,-14.3,;11.14,-12.98,;12.67,-12.97,;13.45,-14.31,;12.68,-15.63,;11.14,-15.63,;10.38,-16.97,;11.15,-18.3,;14.98,-14.31,;15.75,-15.64,;17.29,-15.64,;18.06,-14.31,;17.28,-12.97,;15.74,-12.98,;6.6,-18.78,;8.56,-22.25,;10.07,-22.55,;10.55,-24.02,;9.52,-25.17,;8.01,-24.85,;7.54,-23.39,;10,-26.63,;9.22,-27.96,;11.54,-26.65,;12.33,-25.32,;13.87,-25.35,;14.65,-24.03,;13.89,-22.68,;12.35,-22.67,;11.57,-23.99,)|
Structure
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