Reaction Details |
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Target | Insulin receptor |
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Ligand | BDBM15011 |
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Substrate/Competitor | Peptide Substrate |
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Meas. Tech. | Homogeneous Time-Resolved Fluorescence (HTRF) Assay |
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pH | 7.4±n/a |
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Temperature | 295.15±n/a K |
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IC50 | 12000±5400 nM |
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Citation | Bell, IM; Stirdivant, SM; Ahern, J; Culberson, JC; Darke, PL; Dinsmore, CJ; Drakas, RA; Gallicchio, SN; Graham, SL; Heimbrook, DC; Hall, DL; Hua, J; Kett, NR; Kim, AS; Kornienko, M; Kuo, LC; Munshi, SK; Quigley, AG; Reid, JC; Trotter, BW; Waxman, LH; Williams, TM; Zartman, CB Biochemical and structural characterization of a novel class of inhibitors of the type 1 insulin-like growth factor and insulin receptor kinases. Biochemistry44:9430-40 (2005) [PubMed] Article |
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More Info.: | Get all data from this article, Inhibition_Run data, Solution Info, 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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BDBM15011 |
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Peptide Substrate |
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Name: | Peptide Substrate |
Synonyms: | n/a |
Type: | Peptide |
Mol. Mass.: | 2600.09 |
Organism: | n/a |
Description: | n/a |
Residue: | 21 |
Sequence: | biotin-EQEDEPEGDYFEWLE-NH2
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