Reaction Details |
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Target | Insulin receptor |
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Ligand | BDBM50307987 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_608407 (CHEMBL1064436) |
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IC50 | >10000±n/a nM |
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Citation | Brasca, MG; Albanese, C; Alzani, R; Amici, R; Avanzi, N; Ballinari, D; Bischoff, J; Borghi, D; Casale, E; Croci, V; Fiorentini, F; Isacchi, A; Mercurio, C; Nesi, M; Orsini, P; Pastori, W; Pesenti, E; Pevarello, P; Roussel, P; Varasi, M; Volpi, D; Vulpetti, A; Ciomei, M Optimization of 6,6-dimethyl pyrrolo[3,4-c]pyrazoles: Identification of PHA-793887, a potent CDK inhibitor suitable for intravenous dosing. Bioorg Med Chem18:1844-53 (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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BDBM50307987 |
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n/a |
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Name | BDBM50307987 |
Synonyms: | CHEMBL604712 | N-[5-(2,2-Dimethylpropanoyl)-6,6-dimethyl-1,4,5,6-tetrahydropyrrolo[3,4-c]pyrazol-3-yl]-3,5-difluorobenzamide |
Type | Small organic molecule |
Emp. Form. | C19H22F2N4O2 |
Mol. Mass. | 376.4004 |
SMILES | CC(C)(C)C(=O)N1Cc2c(NC(=O)c3cc(F)cc(F)c3)[nH]nc2C1(C)C |
Structure |
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