Reaction Details Report a problem with these data
Target
Transcription factor ETV6/Tyrosine-protein kinase receptor UFO
Ligand
BDBM144315
Substrate
n/a
Meas. Tech.
ChEMBL_1921288 (CHEMBL4424133)
IC50
8.5±n/a nM
Citation
 Wang, Y; Xing, L; Ji, Y; Ye, J; Dai, Y; Gu, W; Ai, J; Song, Z Discovery of a potent tyrosine kinase AXL inhibitor bearing the 3-((2,3,4,5-tetrahydro-1H-benzo[d]azepin-7-yl)amino)pyrazine core. Bioorg Med Chem Lett 29:836-838 (2019) [PubMed]  Article 
Target
Name:
Transcription factor ETV6/Tyrosine-protein kinase receptor UFO
Synonyms:
TEL/AXL
Type:
n/a
Mol. Mass.:
n/a
Description:
ASSAY_ID of ChEMBL is 1921288
Components:
This complex has 2 components.
Component 1
Name:
Tyrosine-protein kinase receptor UFO
Synonyms:
AXL | AXL oncogene | TEL/AXL | Tyrosine-protein kinase receptor UFO (AXL) | UFO | UFO_HUMAN
Type:
Enzyme
Mol. Mass.:
98316.97
Organism:
Homo sapiens (Human)
Description:
P30530
Residue:
894
Sequence:
MAWRCPRMGRVPLAWCLALCGWACMAPRGTQAEESPFVGNPGNITGARGLTGTLRCQLQVQGEPPEVHWLRDGQILELADSTQTQVPLGEDEQDDWIVVSQLRITSLQLSDTGQYQCLVFLGHQTFVSQPGYVGLEGLPYFLEEPEDRTVAANTPFNLSCQAQGPPEPVDLLWLQDAVPLATAPGHGPQRSLHVPGLNKTSSFSCEAHNAKGVTTSRTATITVLPQQPRNLHLVSRQPTELEVAWTPGLSGIYPLTHCTLQAVLSDDGMGIQAGEPDPPEEPLTSQASVPPHQLRLGSLHPHTPYHIRVACTSSQGPSSWTHWLPVETPEGVPLGPPENISATRNGSQAFVHWQEPRAPLQGTLLGYRLAYQGQDTPEVLMDIGLRQEVTLELQGDGSVSNLTVCVAAYTAAGDGPWSLPVPLEAWRPGQAQPVHQLVKEPSTPAFSWPWWYVLLGAVVAAACVLILALFLVHRRKKETRYGEVFEPTVERGELVVRYRVRKSYSRRTTEATLNSLGISEELKEKLRDVMVDRHKVALGKTLGEGEFGAVMEGQLNQDDSILKVAVKTMKIAICTRSELEDFLSEAVCMKEFDHPNVMRLIGVCFQGSERESFPAPVVILPFMKHGDLHSFLLYSRLGDQPVYLPTQMLVKFMADIASGMEYLSTKRFIHRDLAARNCMLNENMSVCVADFGLSKKIYNGDYYRQGRIAKMPVKWIAIESLADRVYTSKSDVWSFGVTMWEIATRGQTPYPGVENSEIYDYLRQGNRLKQPADCLDGLYALMSRCWELNPQDRPSFTELREDLENTLKALPPAQEPDEILYVNMDEGGGYPEPPGAAGGADPPTQPDPKDSCSCLTAAEVHPAGRYVLCPSTTPSPAQPADRGSPAAPGQEDGA
  
Component 2
Name:
Transcription factor ETV6
Synonyms:
ETS translocation variant 6 | ETS-related protein Tel1 | ETV6 | ETV6_HUMAN | TEL | TEL1
Type:
PROTEIN
Mol. Mass.:
53009.91
Organism:
Homo sapiens (Human)
Description:
ChEMBL_107623
Residue:
452
Sequence:
MSETPAQCSIKQERISYTPPESPVPSYASSTPLHVPVPRALRMEEDSIRLPAHLRLQPIYWSRDDVAQWLKWAENEFSLRPIDSNTFEMNGKALLLLTKEDFRYRSPHSGDVLYELLQHILKQRKPRILFSPFFHPGNSIHTQPEVILHQNHEEDNCVQRTPRPSVDNVHHNPPTIELLHRSRSPITTNHRPSPDPEQRPLRSPLDNMIRRLSPAERAQGPRPHQENNHQESYPLSVSPMENNHCPASSESHPKPSSPRQESTRVIQLMPSPIMHPLILNPRHSVDFKQSRLSEDGLHREGKPINLSHREDLAYMNHIMVSVSPPEEHAMPIGRIADCRLLWDYVYQLLSDSRYENFIRWEDKESKIFRIVDPNGLARLWGNHKNRTNMTYEKMSRALRHYYKLNIIRKEPGQRLLFRFMKTPDEIMSGRTDRLEHLESQELDEQIYQEDEC
  
Inhibitor
Name:
BDBM144315
Synonyms:
Gilteritinib | US11512074, Example T-9 | US8969336, 547 | US8969336, 577
Type:
Small organic molecule
Emp. Form.:
C29H44N8O3
Mol. Mass.:
552.7115
SMILES:
CCc1nc(C(N)=O)c(Nc2ccc(N3CCC(CC3)N3CCN(C)CC3)c(OC)c2)nc1NC1CCOCC1
Structure:
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