Reaction Details Report a problem with these data
Target
Insulin receptor
Ligand
BDBM6416
Substrate
Insulin Kinase Peptide Substrate
Meas. Tech.
Kinase Inhibition Assay
IC50
1690±n/a nM
Citation
 Kuo, GH; Wang, A; Emanuel, S; Deangelis, A; Zhang, R; Connolly, PJ; Murray, WV; Gruninger, RH; Sechler, J; Fuentes-Pesquera, A; Johnson, D; Middleton, SA; Jolliffe, L; Chen, X Synthesis and discovery of pyrazine-pyridine biheteroaryl as a novel series of potent vascular endothelial growth factor receptor-2 inhibitors. J Med Chem 48:1886-900 (2005) [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:
BDBM6416
Synonyms:
3-[(5-{6-[(3-chlorophenyl)amino]pyrazin-2-yl}pyridin-3-yl)amino]propan-1-ol | 3-[[5-[6-[(3-chlorophenyl)amino]pyrazinyl]-3-pyridinyl]amino]-1-propanol | Pyrazine-Pyridine Biheteroaryl 7 | Pyrazine-Pyridine deriv. 15
Type:
Small organic molecule
Emp. Form.:
C18H18ClN5O
Mol. Mass.:
355.821
SMILES:
OCCCNc1cncc(c1)-c1cncc(Nc2cccc(Cl)c2)n1
Structure:
Search PDB for entries with ligand similarity:
Substrate
Name:
Insulin Kinase Peptide Substrate
Synonyms:
n/a
Type:
Peptide
Mol. Mass.:
2621.87
Organism:
n/a
Description:
n/a
Residue:
21
Sequence:
ITINTRDIYETDYYRKAMIDE