Reaction Details |
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Target | Heat shock protein HSP 90-beta |
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Ligand | BDBM20773 |
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Substrate/Competitor | BDBM10852 |
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Meas. Tech. | Her-2 Degradation Assay |
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pH | 7.2±n/a |
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Temperature | 310.15±n/a K |
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EC50 | 300±n/a nM |
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Comments | EC50=700 nM in MTS cell-growth inhibition assay. |
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Citation | Zhang, L; Fan, J; Vu, K; Hong, K; Le Brazidec, JY; Shi, J; Biamonte, M; Busch, DJ; Lough, RE; Grecko, R; Ran, Y; Sensintaffar, JL; Kamal, A; Lundgren, K; Burrows, FJ; Mansfield, R; Timony, GA; Ulm, EH; Kasibhatla, SR; Boehm, MF 7'-substituted benzothiazolothio- and pyridinothiazolothio-purines as potent heat shock protein 90 inhibitors. J Med Chem49:5352-62 (2006) [PubMed] Article |
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More Info.: | Get all data from this article, Solution Info, Assay Method |
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Heat shock protein HSP 90-beta |
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Name: | Heat shock protein HSP 90-beta |
Synonyms: | HS90B_HUMAN | HSP 84 | HSP 90 | HSP90AB1 | HSP90B | HSPC2 | HSPCB | Heat Shock Protein 90 (Hsp90) | Heat shock protein HSP 90 (Hsp90) |
Type: | Molecular Chaperone |
Mol. Mass.: | 83229.45 |
Organism: | Homo sapiens (Human) |
Description: | P08238 |
Residue: | 724 |
Sequence: | MPEEVHHGEEEVETFAFQAEIAQLMSLIINTFYSNKEIFLRELISNASDALDKIRYESLT
DPSKLDSGKELKIDIIPNPQERTLTLVDTGIGMTKADLINNLGTIAKSGTKAFMEALQAG
ADISMIGQFGVGFYSAYLVAEKVVVITKHNDDEQYAWESSAGGSFTVRADHGEPIGRGTK
VILHLKEDQTEYLEERRVKEVVKKHSQFIGYPITLYLEKEREKEISDDEAEEEKGEKEEE
DKDDEEKPKIEDVGSDEEDDSGKDKKKKTKKIKEKYIDQEELNKTKPIWTRNPDDITQEE
YGEFYKSLTNDWEDHLAVKHFSVEGQLEFRALLFIPRRAPFDLFENKKKKNNIKLYVRRV
FIMDSCDELIPEYLNFIRGVVDSEDLPLNISREMLQQSKILKVIRKNIVKKCLELFSELA
EDKENYKKFYEAFSKNLKLGIHEDSTNRRRLSELLRYHTSQSGDEMTSLSEYVSRMKETQ
KSIYYITGESKEQVANSAFVERVRKRGFEVVYMTEPIDEYCVQQLKEFDGKSLVSVTKEG
LELPEDEEEKKKMEESKAKFENLCKLMKEILDKKVEKVTISNRLVSSPCCIVTSTYGWTA
NMERIMKAQALRDNSTMGYMMAKKHLEINPDHPIVETLRQKAEADKNDKAVKDLVVLLFE
TALLSSGFSLEDPQTHSNRIYRMIKLGLGIDEDEVAAEEPNAAVPDEIPPLEGDEDASRM
EEVD
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BDBM20773 |
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BDBM10852 |
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Name | BDBM20773 |
Synonyms: | 2-{6-amino-8-[(7-chloro-1,3-benzothiazol-2-yl)sulfanyl]-9H-purin-9-yl}ethan-1-ol | Benzothiazole analogue, 31 |
Type | Small organic molecule |
Emp. Form. | C14H11ClN6OS2 |
Mol. Mass. | 378.86 |
SMILES | Nc1ncnc2n(CCO)c(Sc3nc4cccc(Cl)c4s3)nc12 |
Structure |
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