Target
Tyrosine-protein kinase receptor UFO
Ligand
BDBM628983
Substrate
n/a
Meas. Tech.
MERTK, AXL, TYRO3 Kinase Homogeneous Time Resolved Fluorescence (HTRF) Assay
IC50
0.300±n/a nM
Citation
 Tarby, CMNorris, DJLo, JCAhuja, VTSeitz, SPGavai, AVTokarski, JSRajasagi, MWichroski, MBroekema, M URACIL DERIVATIVES AS MER-AXL INHIBITORS US Patent  US20230339891 Publication Date 10/26/2023 
Target
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
  
Inhibitor
Name:
BDBM628983
Synonyms:
N-{4-[(2-{[5-(Dimethylcarbamoyl)-6-(4-methanesulfonylpiperazin-1-yl)pyridin-2-yl]amino}pyridin-4-yl)oxy]-3-fluorophenyl}-3-(4-fluorophenyl)-2,4-dioxo-1-(propan-2-yl)-1,2,3,4-tetrahydropyrimidine-5-carboxamide | US20230339891, Example 97
Type:
Small organic molecule
Emp. Form.:
C38H39F2N9O7S
Mol. Mass.:
803.834
SMILES:
CC(C)n1cc(C(=O)Nc2ccc(Oc3ccnc(Nc4ccc(C(=O)N(C)C)c(n4)N4CCN(CC4)S(C)(=O)=O)c3)c(F)c2)c(=O)n(-c2ccc(F)cc2)c1=O
Structure:
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