Reaction Details Report a problem with these data
Target
Vascular endothelial growth factor receptor 1
Ligand
BDBM4875
Substrate
polyGluTyr
Meas. Tech.
Kinase Inhibition Assay
IC50
80±n/a nM
Citation
 Bold, G; Altmann, KH; Frei, J; Lang, M; Manley, PW; Traxler, P; Wietfeld, B; Bruggen, J; Buchdunger, E; Cozens, R; Ferrari, S; Furet, P; Hofmann, F; Martiny-Baron, G; Mestan, J; Rosel, J; Sills, M; Stover, D; Acemoglu, F; Boss, E; Emmenegger, R; Lasser, L; Masso, E; Roth, R; Schlachter, C; Vetterli, W New anilinophthalazines as potent and orally well absorbed inhibitors of the VEGF receptor tyrosine kinases useful as antagonists of tumor-driven angiogenesis. J Med Chem 43:2310-23 (2000) [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:
BDBM4875
Synonyms:
1-(3-Hydroxyanilino)-4-(4-pyridylmethyl)phthalazine | 3-{[4-(pyridin-4-ylmethyl)phthalazin-1-yl]amino}phenol | CGP79787 Analog 60
Type:
Small organic molecule
Emp. Form.:
C20H16N4O
Mol. Mass.:
328.3672
SMILES:
Oc1cccc(Nc2nnc(Cc3ccncc3)c3ccccc23)c1
Structure:
Search PDB for entries with ligand similarity:
Substrate
Name:
polyGluTyr
Synonyms:
n/a
Type:
Peptide
Mol. Mass.:
358.43
Organism:
n/a
Description:
polyGluTyr(4:1). 8 uM ATP and 0.2 uCi [gamma-33P]ATP as co-substrate.
Residue:
3
Sequence:
NA