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Target
Insulin-like growth factor 1 receptor
Ligand
BDBM50252297
Substrate
n/a
Meas. Tech.
ChEMBL_487711 (CHEMBL1022736)
IC50
105±n/a nM
Citation
Zimmermann, K; Wittman, MD; Saulnier, MG; Velaparthi, U; Langley, DR; Sang, X; Frennesson, D; Carboni, J; Li, A; Greer, A; Gottardis, M; Attar, RM; Yang, Z; Balimane, P; Discenza, LN; Vyas, D Balancing oral exposure with Cyp3A4 inhibition in benzimidazole-based IGF-IR inhibitors. Bioorg Med Chem Lett 18:4075-80 (2008) [PubMed] Article
More Info.:
Target
Name:
Insulin-like growth factor 1 receptor
Synonyms:
IGF1R_MOUSE | Igf1r
Type:
PROTEIN
Mol. Mass.:
155770.40
Organism:
Mus musculus
Description:
ChEMBL_820934
Residue:
1373
Sequence:
MKSGSGGGSPTSLWGLVFLSAALSLWPTSGEICGPGIDIRNDYQQLKRLENCTVIEGFLHILLISKAEDYRSYRFPKLTVITEYLLLFRVAGLESLGDLFPNLTVIRGWKLFYNYALVIFEMTNLKDIGLYNLRNITRGAIRIEKNADLCYLSTIDWSLILDAVSNNYIVGNKPPKECGDLCPGTLEEKPMCEKTTINNEYNYRCWTTNRCQKMCPSVCGKRACTENNECCHPECLGSCHTPDDNTTCVACRHYYYKGVCVPACPPGTYRFEGWRCVDRDFCANIPNAESSDSDGFVIHDDECMQECPSGFIRNSTQSMYCIPCEGPCPKVCGDEEKKTKTIDSVTSAQMLQGCTILKGNLLINIRRGNNIASELENFMGLIEVVTGYVKIRHSHALVSLSFLKNLRLILGEEQLEGNYSFYVLDNQNLQQLWDWNHRNLTVRSGKMYFAFNPKLCVSEIYRMEEVTGTKGRQSKGDINTRNNGERASCESDVLRFTSTTTWKNRIIITWHRYRPPDYRDLISFTVYYKEAPFKNVTEYDGQDACGSNSWNMVDVDLPPNKEGEPGILLHGLKPWTQYAVYVKAVTLTMVENDHIRGAKSEILYIRTNASVPSIPLDVLSASNSSSQLIVKWNPPTLPNGNLSYYIVRWQRQPQDGYLYRHNYCSKDKIPIRKYADGTIDVEEVTENPKTEVCGGDKGPCCACPKTEAEKQAEKEEAEYRKVFENFLHNSIFVPRPERRRRDVMQVANTTMSSRSRNTTVADTYNITDPEEFETEYPFFESRVDNKERTVISNLRPFTLYRIDIHSCNHEAEKLGCSASNFVFARTMPAEGADDIPGPVTWEPRPENSIFLKWPEPENPNGLILMYEIKYGSQVEDQRECVSRQEYRKYGGAKLNRLNPGNYTARIQATSLSGNGSWTDPVFFYVPAKTTYENFMHLIIALPVAILLIVGGLVIMLYVFHRKRNNSRLGNGVLYASVNPEYFSAADVYVPDEWEVAREKITMNRELGQGSFGMVYEGVAKGVVKDEPETRVAIKTVNEAASMRERIEFLNEASVMKEFNCHHVVRLLGVVSQGQPTLVIMELMTRGDLKSYLRSLRPEVEQNNLVLIPPSLSKMIQMAGEIADGMAYLNANKFVHRDLAARNCMVAEDFTVKIGDFGMTRDIYETDYYRKGGKGLLPVRWMSPESLKDGVFTTHSDVWSFGVVLWEIATLAEQPYQGLSNEQVLRFVMEGGLLDKPDNCPDMLFELMRMCWQYNPKMRPSFLEIIGSIKDEMEPSFQEVSFYYSEENKPPEPEELEMELEMEPENMESVPLDPSASSASLPLPERHSGHKAENGPGPGVLVLRASFDERQPYAHMNGGRANERALPLPQSSTC
Inhibitor
Name:
BDBM50252297
Synonyms:
(S)-3-(6-(4-(4-acetylpiperazin-1-yl)piperidin-1-yl)-4-methyl-1H-benzo[d]imidazol-2-yl)-4-(2-(3-chlorophenyl)-2-hydroxyethylamino)pyridin-2(1H)-one | CHEMBL506169
Type:
Small organic molecule
Emp. Form.:
C32H38ClN7O3
Mol. Mass.:
604.142
SMILES:
CC(=O)N1CCN(CC1)C1CCN(CC1)c1cc(C)c2nc([nH]c2c1)-c1c(NC[C@@H](O)c2cccc(Cl)c2)cc[nH]c1=O |r|