Reaction Details |
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Target | Heat shock protein HSP 90-beta |
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Ligand | BDBM20883 |
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Substrate/Competitor | BDBM15527 |
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Meas. Tech. | Fluorescence Polarization (FP) Assay and Cell Growth Inhibition (SRB) Assay |
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pH | 7.4±n/a |
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Temperature | 295.15±n/a K |
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IC50 | 146±n/a nM |
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EC50 | 315±n/a nM |
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Citation | Brough, PA; Aherne, W; Barril, X; Borgognoni, J; Boxall, K; Cansfield, JE; Cheung, KM; Collins, I; Davies, NG; Drysdale, MJ; Dymock, B; Eccles, SA; Finch, H; Fink, A; Hayes, A; Howes, R; Hubbard, RE; James, K; Jordan, AM; Lockie, A; Martins, V; Massey, A; Matthews, TP; McDonald, E; Northfield, CJ; Pearl, LH; Prodromou, C; Ray, S; Raynaud, FI; Roughley, SD; Sharp, SY; Surgenor, A; Walmsley, DL; Webb, P; Wood, M; Workman, P; Wright, L 4,5-diarylisoxazole Hsp90 chaperone inhibitors: potential therapeutic agents for the treatment of cancer. J Med Chem51:196-218 (2008) [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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BDBM20883 |
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BDBM15527 |
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Name | BDBM20883 |
Synonyms: | 3-(5-chloro-2,4-dihydroxyphenyl)-4-{4-[(diethylamino)methyl]phenyl}-N-ethyl-1H-pyrazole-5-carboxamide | Pyrazole, 19a |
Type | Small organic molecule |
Emp. Form. | C23H27ClN4O3 |
Mol. Mass. | 442.938 |
SMILES | CCNC(=O)c1[nH]nc(c1-c1ccc(CN(CC)CC)cc1)-c1cc(Cl)c(O)cc1O |
Structure |
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