Target
Insulin receptor
Ligand
BDBM27895
Substrate
polyGlu4Tyr
Meas. Tech.
Axl Enzyme Inhibition Assay
Temperature
298.15±n/a K
IC50
19800±n/a nM
Comments
extracted
Citation
 Huang, HHutta, DARinker, JMHu, HParsons, WHSchubert, CDesjarlais, RLCrysler, CSChaikin, MADonatelli, RRChen, YCheng, DZhou, ZYurkow, EManthey, CLPlayer, MR Pyrido[2,3-d]pyrimidin-5-ones: A Novel Class of Antiinflammatory Macrophage Colony-Stimulating Factor-1 Receptor Inhibitors (dagger). J Med Chem 52:1081-99 (2009) [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:
BDBM27895
Synonyms:
8-(2,3-dihydro-1H-inden-5-yl)-N-methoxy-2-({4-[2-(4-methylpiperazin-1-yl)ethyl]phenyl}amino)-5-oxo-5H,8H-pyrido[2,3-d]pyrimidine-6-carboxamide | Pyrido[2,3-d]pyrimidin-5-one, 18a
Type:
Small organic molecule
Emp. Form.:
C31H35N7O3
Mol. Mass.:
553.6547
SMILES:
CONC(=O)c1cn(-c2ccc3CCCc3c2)c2nc(Nc3ccc(CCN4CCN(C)CC4)cc3)ncc2c1=O
Structure:
Search PDB for entries with ligand similarity:
Substrate
Name:
polyGlu4Tyr
Synonyms:
n/a
Type:
Random copolymer
Mol. Mass.:
358.43
Organism:
n/a
Description:
n/a
Residue:
3
Sequence:
NA