Reaction Details |
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Target | Insulin receptor |
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Ligand | BDBM50308205 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_613682 (CHEMBL1067602) |
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IC50 | >100000±n/a nM |
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Citation | Egert-Schmidt, AM; Dreher, J; Dunkel, U; Kohfeld, S; Preu, L; Weber, H; Ehlert, JE; Mutschler, B; Totzke, F; Schächtele, C; Kubbutat, MH; Baumann, K; Kunick, C Identification of 2-anilino-9-methoxy-5,7-dihydro-6H-pyrimido[5,4-d][1]benzazepin-6-ones as dual PLK1/VEGF-R2 kinase inhibitor chemotypes by structure-based lead generation. J Med Chem53:2433-42 (2010) [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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BDBM50308205 |
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n/a |
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Name | BDBM50308205 |
Synonyms: | 2-(3-Hydroxyanilino)-5,7-dihydro-6H-pyrido[3,2-b]pyrimido[4,5-d]azepin-6-one | CHEMBL606185 |
Type | Small organic molecule |
Emp. Form. | C17H13N5O2 |
Mol. Mass. | 319.3174 |
SMILES | Oc1cccc(Nc2ncc3CC(=O)Nc4cccnc4-c3n2)c1 |
Structure |
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