Reaction Details |
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Target | Platelet-derived growth factor receptor beta |
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Ligand | BDBM3085 |
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Substrate/Competitor | Poly(E:Y) |
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Meas. Tech. | Kinase Inhibition Assay |
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IC50 | 210±n/a nM |
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Citation | Klutchko, SR; Hamby, JM; Boschelli, DH; Wu, Z; Kraker, AJ; Amar, AM; Hartl, BG; Shen, C; Klohs, WD; Steinkampf, RW; Driscoll, DL; Nelson, JM; Elliott, WL; Roberts, BJ; Stoner, CL; Vincent, PW; Dykes, DJ; Panek, RL; Lu, GH; Major, TC; Dahring, TK; Hallak, H; Bradford, LA; Showalter, HD; Doherty, AM 2-Substituted aminopyrido[2,3-d]pyrimidin-7(8H)-ones. structure-activity relationships against selected tyrosine kinases and in vitro and in vivo anticancer activity. J Med Chem41:3276-92 (1998) [PubMed] Article |
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More Info.: | Get all data from this article, Solution Info, Assay Method |
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Platelet-derived growth factor receptor beta |
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Name: | Platelet-derived growth factor receptor beta |
Synonyms: | Beta-type platelet-derived growth factor receptor | CD140 antigen-like family member B | CD140b antigen | CD_antigen=CD140b | PDGF Receptor Substrate | PDGF-R-beta | PDGFR | PDGFR substrate | PDGFR-1 | PDGFR1 | PDGFRB | PDGFRbeta | PGFRB_HUMAN | Platelet-Derived Growth Factor Receptor, beta | Platelet-derived growth factor receptor 1 | Platelet-derived growth factor receptor beta | Platelet-derived growth factor receptor beta (PDGFR-beta) | Platelet-derived growth factor receptor beta (PDGFRB) | Platelet-derived growth factor receptor beta (PDGFRbeta) | VHL/PDGFRB |
Type: | Enzyme |
Mol. Mass.: | 123922.25 |
Organism: | Homo sapiens (Human) |
Description: | P09619 |
Residue: | 1106 |
Sequence: | MRLPGAMPALALKGELLLLSLLLLLEPQISQGLVVTPPGPELVLNVSSTFVLTCSGSAPV
VWERMSQEPPQEMAKAQDGTFSSVLTLTNLTGLDTGEYFCTHNDSRGLETDERKRLYIFV
PDPTVGFLPNDAEELFIFLTEITEITIPCRVTDPQLVVTLHEKKGDVALPVPYDHQRGFS
GIFEDRSYICKTTIGDREVDSDAYYVYRLQVSSINVSVNAVQTVVRQGENITLMCIVIGN
EVVNFEWTYPRKESGRLVEPVTDFLLDMPYHIRSILHIPSAELEDSGTYTCNVTESVNDH
QDEKAINITVVESGYVRLLGEVGTLQFAELHRSRTLQVVFEAYPPPTVLWFKDNRTLGDS
SAGEIALSTRNVSETRYVSELTLVRVKVAEAGHYTMRAFHEDAEVQLSFQLQINVPVRVL
ELSESHPDSGEQTVRCRGRGMPQPNIIWSACRDLKRCPRELPPTLLGNSSEEESQLETNV
TYWEEEQEFEVVSTLRLQHVDRPLSVRCTLRNAVGQDTQEVIVVPHSLPFKVVVISAILA
LVVLTIISLIILIMLWQKKPRYEIRWKVIESVSSDGHEYIYVDPMQLPYDSTWELPRDQL
VLGRTLGSGAFGQVVEATAHGLSHSQATMKVAVKMLKSTARSSEKQALMSELKIMSHLGP
HLNVVNLLGACTKGGPIYIITEYCRYGDLVDYLHRNKHTFLQHHSDKRRPPSAELYSNAL
PVGLPLPSHVSLTGESDGGYMDMSKDESVDYVPMLDMKGDVKYADIESSNYMAPYDNYVP
SAPERTCRATLINESPVLSYMDLVGFSYQVANGMEFLASKNCVHRDLAARNVLICEGKLV
KICDFGLARDIMRDSNYISKGSTFLPLKWMAPESIFNSLYTTLSDVWSFGILLWEIFTLG
GTPYPELPMNEQFYNAIKRGYRMAQPAHASDEIYEIMQKCWEEKFEIRPPFSQLVLLLER
LLGEGYKKKYQQVDEEFLRSDHPAILRSQARLPGFHGLRSPLDTSSVLYTAVQPNEGDND
YIIPLPDPKPEVADEGPLEGSPSLASSTLNEVNTSSTISCDSPLEPQDEPEPEPQLELQV
EPEPELEQLPDSGCPAPRAEAEDSFL
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BDBM3085 |
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Poly(E:Y) |
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Name: | Poly(E:Y) |
Synonyms: | n/a |
Type: | Random polymer |
Mol. Mass.: | 358.43 |
Organism: | n/a |
Description: | Random copolymer of glutamic acid and tyrosine (4:1). 50 uM ATP containing 0.4 uCi of [gamma-32P]ATP as co-substrate |
Residue: | 3 |
Sequence: | |