Reaction Details |
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Target | Insulin receptor |
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Ligand | BDBM50029668 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_1437632 (CHEMBL3390234) |
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IC50 | 912±n/a nM |
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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 Chem57:8249-67 (2014) [PubMed] Article |
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More Info.: | Get all data from this article, Assay Method |
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Insulin receptor |
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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: | MATGGRRGAAAAPLLVAVAALLLGAAGHLYPGEVCPGMDIRNNLTRLHELENCSVIEGHL
QILLMFKTRPEDFRDLSFPKLIMITDYLLLFRVYGLESLKDLFPNLTVIRGSRLFFNYAL
VIFEMVHLKELGLYNLMNITRGSVRIEKNNELCYLATIDWSRILDSVEDNYIVLNKDDNE
ECGDICPGTAKGKTNCPATVINGQFVERCWTHSHCQKVCPTICKSHGCTAEGLCCHSECL
GNCSQPDDPTKCVACRNFYLDGRCVETCPPPYYHFQDWRCVNFSFCQDLHHKCKNSRRQG
CHQYVIHNNKCIPECPSGYTMNSSNLLCTPCLGPCPKVCHLLEGEKTIDSVTSAQELRGC
TVINGSLIINIRGGNNLAAELEANLGLIEEISGYLKIRRSYALVSLSFFRKLRLIRGETL
EIGNYSFYALDNQNLRQLWDWSKHNLTITQGKLFFHYNPKLCLSEIHKMEEVSGTKGRQE
RNDIALKTNGDQASCENELLKFSYIRTSFDKILLRWEPYWPPDFRDLLGFMLFYKEAPYQ
NVTEFDGQDACGSNSWTVVDIDPPLRSNDPKSQNHPGWLMRGLKPWTQYAIFVKTLVTFS
DERRTYGAKSDIIYVQTDATNPSVPLDPISVSNSSSQIILKWKPPSDPNGNITHYLVFWE
RQAEDSELFELDYCLKGLKLPSRTWSPPFESEDSQKHNQSEYEDSAGECCSCPKTDSQIL
KELEESSFRKTFEDYLHNVVFVPRKTSSGTGAEDPRPSRKRRSLGDVGNVTVAVPTVAAF
PNTSSTSVPTSPEEHRPFEKVVNKESLVISGLRHFTGYRIELQACNQDTPEERCSVAAYV
SARTMPEAKADDIVGPVTHEIFENNVVHLMWQEPKEPNGLIVLYEVSYRRYGDEELHLCV
SRKHFALERGCRLRGLSPGNYSVRIRATSLAGNGSWTEPTYFYVTDYLDVPSNIAKIIIG
PLIFVFLFSVVIGSIYLFLRKRQPDGPLGPLYASSNPEYLSASDVFPCSVYVPDEWEVSR
EKITLLRELGQGSFGMVYEGNARDIIKGEAETRVAVKTVNESASLRERIEFLNEASVMKG
FTCHHVVRLLGVVSKGQPTLVVMELMAHGDLKSYLRSLRPEAENNPGRPPPTLQEMIQMA
AEIADGMAYLNAKKFVHRDLAARNCMVAHDFTVKIGDFGMTRDIYETDYYRKGGKGLLPV
RWMAPESLKDGVFTTSSDMWSFGVVLWEITSLAEQPYQGLSNEQVLKFVMDGGYLDQPDN
CPERVTDLMRMCWQFNPKMRPTFLEIVNLLKDDLHPSFPEVSFFHSEENKAPESEELEME
FEDMENVPLDRSSHCQREEAGGRDGGSSLGFKRSYEEHIPYTHMNGGKKNGRILTLPRSN
PS
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BDBM50029668 |
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n/a |
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Name | BDBM50029668 |
Synonyms: | AZD-9291 | Osimertinib | US10085983, Compound AZD-9291 | US10227342, Example 24 | US11111233, Example AZD9291 | US11896597, Compound AZD9291 | US20230322822, Compound AZD9291 | US9890168, Compound AZD-9291 | WO2022090481, Example osimertinib |
Type | Small organic molecule |
Emp. Form. | C28H33N7O2 |
Mol. Mass. | 499.6073 |
SMILES | COc1cc(N(C)CCN(C)C)c(NC(=O)C=C)cc1Nc1nccc(n1)-c1cn(C)c2ccccc12 |
Structure |
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