Reaction Details Report a problem with these data
Target
Insulin receptor
Ligand
BDBM50029686
Substrate
n/a
Meas. Tech.
ChEMBL_1437632 (CHEMBL3390234)
IC50
35±n/a nM
Citation
 Finlay, MR; Anderton, M; Ashton, S; Ballard, P; Bethel, PA; Box, MR; Bradbury, RH; Brown, SJ; Butterworth, S; Campbell, A; Chorley, C; Colclough, N; Cross, DA; Currie, GS; Grist, M; Hassall, L; Hill, GB; James, D; James, M; Kemmitt, P; Klinowska, T; Lamont, G; Lamont, SG; Martin, N; McFarland, HL; Mellor, MJ; Orme, JP; Perkins, D; Perkins, P; Richmond, G; Smith, P; Ward, RA; Waring, MJ; Whittaker, D; Wells, S; Wrigley, GL Discovery of a potent and selective EGFR inhibitor (AZD9291) of both sensitizing and T790M resistance mutations that spares the wild type form of the receptor. J Med Chem 57:8249-67 (2014) [PubMed]  Article 
Target
Name:
Insulin receptor
Synonyms:
INSR | INSR protein | INSR_HUMAN | Insulin receptor (IR) | Insulin receptor beta subunit
Type:
Receptor Tyrosine Kinase
Mol. Mass.:
156322.60
Organism:
Homo sapiens (Human)
Description:
P06213
Residue:
1382
Sequence:
MATGGRRGAAAAPLLVAVAALLLGAAGHLYPGEVCPGMDIRNNLTRLHELENCSVIEGHLQILLMFKTRPEDFRDLSFPKLIMITDYLLLFRVYGLESLKDLFPNLTVIRGSRLFFNYALVIFEMVHLKELGLYNLMNITRGSVRIEKNNELCYLATIDWSRILDSVEDNYIVLNKDDNEECGDICPGTAKGKTNCPATVINGQFVERCWTHSHCQKVCPTICKSHGCTAEGLCCHSECLGNCSQPDDPTKCVACRNFYLDGRCVETCPPPYYHFQDWRCVNFSFCQDLHHKCKNSRRQGCHQYVIHNNKCIPECPSGYTMNSSNLLCTPCLGPCPKVCHLLEGEKTIDSVTSAQELRGCTVINGSLIINIRGGNNLAAELEANLGLIEEISGYLKIRRSYALVSLSFFRKLRLIRGETLEIGNYSFYALDNQNLRQLWDWSKHNLTITQGKLFFHYNPKLCLSEIHKMEEVSGTKGRQERNDIALKTNGDQASCENELLKFSYIRTSFDKILLRWEPYWPPDFRDLLGFMLFYKEAPYQNVTEFDGQDACGSNSWTVVDIDPPLRSNDPKSQNHPGWLMRGLKPWTQYAIFVKTLVTFSDERRTYGAKSDIIYVQTDATNPSVPLDPISVSNSSSQIILKWKPPSDPNGNITHYLVFWERQAEDSELFELDYCLKGLKLPSRTWSPPFESEDSQKHNQSEYEDSAGECCSCPKTDSQILKELEESSFRKTFEDYLHNVVFVPRKTSSGTGAEDPRPSRKRRSLGDVGNVTVAVPTVAAFPNTSSTSVPTSPEEHRPFEKVVNKESLVISGLRHFTGYRIELQACNQDTPEERCSVAAYVSARTMPEAKADDIVGPVTHEIFENNVVHLMWQEPKEPNGLIVLYEVSYRRYGDEELHLCVSRKHFALERGCRLRGLSPGNYSVRIRATSLAGNGSWTEPTYFYVTDYLDVPSNIAKIIIGPLIFVFLFSVVIGSIYLFLRKRQPDGPLGPLYASSNPEYLSASDVFPCSVYVPDEWEVSREKITLLRELGQGSFGMVYEGNARDIIKGEAETRVAVKTVNESASLRERIEFLNEASVMKGFTCHHVVRLLGVVSKGQPTLVVMELMAHGDLKSYLRSLRPEAENNPGRPPPTLQEMIQMAAEIADGMAYLNAKKFVHRDLAARNCMVAHDFTVKIGDFGMTRDIYETDYYRKGGKGLLPVRWMAPESLKDGVFTTSSDMWSFGVVLWEITSLAEQPYQGLSNEQVLKFVMDGGYLDQPDNCPERVTDLMRMCWQFNPKMRPTFLEIVNLLKDDLHPSFPEVSFFHSEENKAPESEELEMEFEDMENVPLDRSSHCQREEAGGRDGGSSLGFKRSYEEHIPYTHMNGGKKNGRILTLPRSNPS
  
Inhibitor
Name:
BDBM50029686
Synonyms:
CHEMBL3353405 | US10227342, Example 25
Type:
Small organic molecule
Emp. Form.:
C26H27ClN8O2
Mol. Mass.:
518.998
SMILES:
COc1cc(N2CC(C2)N(C)C)c(NC(=O)C=C)cc1Nc1ncc(Cl)c(n1)-c1cnn2ccccc12
Structure:
Search PDB for entries with ligand similarity: