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Target
Insulin receptor
Ligand
BDBM50340121
Substrate
n/a
Meas. Tech.
ChEMBL_741309 (CHEMBL1764778)
IC50
3±n/a nM
Citation
 Buchanan, JL; Newcomb, JR; Carney, DP; Chaffee, SC; Chai, L; Cupples, R; Epstein, LF; Gallant, P; Gu, Y; Harmange, JC; Hodge, K; Houk, BE; Huang, X; Jona, J; Joseph, S; Jun, HT; Kumar, R; Li, C; Lu, J; Menges, T; Morrison, MJ; Novak, PM; van der Plas, S; Radinsky, R; Rose, PE; Sawant, S; Sun, JR; Surapaneni, S; Turci, SM; Xu, K; Yanez, E; Zhao, H; Zhu, X Discovery of 2,4-bis-arylamino-1,3-pyrimidines as insulin-like growth factor-1 receptor (IGF-1R) inhibitors. Bioorg Med Chem Lett 21:2394-9 (2011) [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:
BDBM50340121
Synonyms:
CHEMBL1760035 | N4-(quinolin-3-yl)-N2-(3,4,5-trimethoxyphenyl)pyrimidine-2,4-diamine
Type:
Small organic molecule
Emp. Form.:
C22H21N5O3
Mol. Mass.:
403.4338
SMILES:
COc1cc(Nc2nccc(Nc3cnc4ccccc4c3)n2)cc(OC)c1OC
Structure:
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