Reaction Details Report a problem with these data
Target
Vascular endothelial growth factor receptor 1
Ligand
BDBM50300690
Substrate
n/a
Meas. Tech.
ChEMBL_655800 (CHEMBL1244844)
Kd
41±n/a nM
Citation
 Zarrinkar, PP; Gunawardane, RN; Cramer, MD; Gardner, MF; Brigham, D; Belli, B; Karaman, MW; Pratz, KW; Pallares, G; Chao, Q; Sprankle, KG; Patel, HK; Levis, M; Armstrong, RC; James, J; Bhagwat, SS AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). Blood 114:2984-92 (2009) [PubMed]  Article 
Target
Name:
Vascular endothelial growth factor receptor 1
Synonyms:
FLT | FLT1 | FRT | Flt-1 | Fms-like tyrosine kinase 1 | Platelet-derived growth factor receptor beta (PDGFRB) | Tyrosine-protein kinase FRT | Tyrosine-protein kinase receptor FLT | VEGFR-1 | VEGFR1 | VGFR1_HUMAN | Vascular endothelial growth factor receptor (VEGFR) | Vascular endothelial growth factor receptor 1 (FLT1) | Vascular endothelial growth factor receptor 1 (VEGFR1) | Vascular endothelial growth factor receptor 1 and 2 (Flt-1 and KDR) | Vascular endothelial growth factor receptor 1 precursor | Vascular permeability factor receptor | fms-related tyrosine kinase 1 | vascular endothelial growth factor/vascular permeability factor receptor
Type:
Receptor Tyrosine Kinase
Mol. Mass.:
150800.23
Organism:
Homo sapiens (Human)
Description:
P17948
Residue:
1338
Sequence:
MVSYWDTGVLLCALLSCLLLTGSSSGSKLKDPELSLKGTQHIMQAGQTLHLQCRGEAAHKWSLPEMVSKESERLSITKSACGRNGKQFCSTLTLNTAQANHTGFYSCKYLAVPTSKKKETESAIYIFISDTGRPFVEMYSEIPEIIHMTEGRELVIPCRVTSPNITVTLKKFPLDTLIPDGKRIIWDSRKGFIISNATYKEIGLLTCEATVNGHLYKTNYLTHRQTNTIIDVQISTPRPVKLLRGHTLVLNCTATTPLNTRVQMTWSYPDEKNKRASVRRRIDQSNSHANIFYSVLTIDKMQNKDKGLYTCRVRSGPSFKSVNTSVHIYDKAFITVKHRKQQVLETVAGKRSYRLSMKVKAFPSPEVVWLKDGLPATEKSARYLTRGYSLIIKDVTEEDAGNYTILLSIKQSNVFKNLTATLIVNVKPQIYEKAVSSFPDPALYPLGSRQILTCTAYGIPQPTIKWFWHPCNHNHSEARCDFCSNNEESFILDADSNMGNRIESITQRMAIIEGKNKMASTLVVADSRISGIYICIASNKVGTVGRNISFYITDVPNGFHVNLEKMPTEGEDLKLSCTVNKFLYRDVTWILLRTVNNRTMHYSISKQKMAITKEHSITLNLTIMNVSLQDSGTYACRARNVYTGEEILQKKEITIRDQEAPYLLRNLSDHTVAISSSTTLDCHANGVPEPQITWFKNNHKIQQEPGIILGPGSSTLFIERVTEEDEGVYHCKATNQKGSVESSAYLTVQGTSDKSNLELITLTCTCVAATLFWLLLTLFIRKMKRSSSEIKTDYLSIIMDPDEVPLDEQCERLPYDASKWEFARERLKLGKSLGRGAFGKVVQASAFGIKKSPTCRTVAVKMLKEGATASEYKALMTELKILTHIGHHLNVVNLLGACTKQGGPLMVIVEYCKYGNLSNYLKSKRDLFFLNKDAALHMEPKKEKMEPGLEQGKKPRLDSVTSSESFASSGFQEDKSLSDVEEEEDSDGFYKEPITMEDLISYSFQVARGMEFLSSRKCIHRDLAARNILLSENNVVKICDFGLARDIYKNPDYVRKGDTRLPLKWMAPESIFDKIYSTKSDVWSYGVLLWEIFSLGGSPYPGVQMDEDFCSRLREGMRMRAPEYSTPEIYQIMLDCWHRDPKERPRFAELVEKLGDLLQANVQQDGKDYIPINAILTGNSGFTYSTPAFSEDFFKESISAPKFNSGSSDDVRYVNAFKFMSLERIKTFEELLPNATSMFDDYQGDSSTLLASPMLKRFTWTDSKPKASLKIDLRVTSKSKESGLSDVSRPSFCHSSCGHVSEGKRRFTYDHAELERKIACCSPPPDYNSVVLYSTPPI
  
Inhibitor
Name:
BDBM50300690
Synonyms:
1-(5-Tert-Butyl-1,2-Oxazol-3-Yl)-3-(4-{7-[2-(Morpholin-4-Yl)ethoxy]imidazo[2,1-B][1,3]benzothiazol-2-Yl}phenyl)urea | AC 010220 | AC 220 | AC-220 | AC010220 | AC220 | ASP-2689 | CHEMBL576982 | N-(5-tert-Butyl-isoxazol-3-yl)-N'-{4-[7-(2-morpholin-4-yl-ethoxy)imidazo[2,1-b][1,3]benzothiazol-2-yl]phenyl}urea | Quizartinib | Quizartinib (AC220) | US10266535, Compound AC220 | US11542261, Compound quizartinib | US9216997, Quizartinib (positive compound)
Type:
Small organic molecule
Emp. Form.:
C29H32N6O4S
Mol. Mass.:
560.667
SMILES:
CC(C)(C)c1cc(NC(=O)Nc2ccc(cc2)-c2cn3c(n2)sc2cc(OCCN4CCOCC4)ccc32)no1
Structure:
Search PDB for entries with ligand similarity: