Reaction Details |
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Target | ATP-dependent molecular chaperone HSP82 |
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Ligand | BDBM50409989 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_304597 (CHEMBL828486) |
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IC50 | 1550±n/a nM |
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Citation | Cheung, KM; Matthews, TP; James, K; Rowlands, MG; Boxall, KJ; Sharp, SY; Maloney, A; Roe, SM; Prodromou, C; Pearl, LH; Aherne, GW; McDonald, E; Workman, P The identification, synthesis, protein crystal structure and in vitro biochemical evaluation of a new 3,4-diarylpyrazole class of Hsp90 inhibitors. Bioorg Med Chem Lett15:3338-43 (2005) [PubMed] Article |
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More Info.: | Get all data from this article, Assay Method |
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ATP-dependent molecular chaperone HSP82 |
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Name: | ATP-dependent molecular chaperone HSP82 |
Synonyms: | 82 kDa heat shock protein | ATP-dependent molecular chaperone HSP82 | HSP82 | HSP82_YEAST | HSP90 | Heat Shock Protein 90 (Hsp90) | Heat shock protein Hsp90 heat-inducible isoform |
Type: | Molecular Chaperone |
Mol. Mass.: | 81369.08 |
Organism: | Saccharomyces cerevisiae |
Description: | Histidine-tagged yeast HSP90 was transformed into E. coli and purified (>90%) by metal affinity, gel filtration, and ion-exchange chromatography. |
Residue: | 709 |
Sequence: | MASETFEFQAEITQLMSLIINTVYSNKEIFLRELISNASDALDKIRYKSLSDPKQLETEP
DLFIRITPKPEQKVLEIRDSGIGMTKAELINNLGTIAKSGTKAFMEALSAGADVSMIGQF
GVGFYSLFLVADRVQVISKSNDDEQYIWESNAGGSFTVTLDEVNERIGRGTILRLFLKDD
QLEYLEEKRIKEVIKRHSEFVAYPIQLVVTKEVEKEVPIPEEEKKDEEKKDEEKKDEDDK
KPKLEEVDEEEEKKPKTKKVKEEVQEIEELNKTKPLWTRNPSDITQEEYNAFYKSISNDW
EDPLYVKHFSVEGQLEFRAILFIPKRAPFDLFESKKKKNNIKLYVRRVFITDEAEDLIPE
WLSFVKGVVDSEDLPLNLSREMLQQNKIMKVIRKNIVKKLIEAFNEIAEDSEQFEKFYSA
FSKNIKLGVHEDTQNRAALAKLLRYNSTKSVDELTSLTDYVTRMPEHQKNIYYITGESLK
AVEKSPFLDALKAKNFEVLFLTDPIDEYAFTQLKEFEGKTLVDITKDFELEETDEEKAER
EKEIKEYEPLTKALKEILGDQVEKVVVSYKLLDAPAAIRTGQFGWSANMERIMKAQALRD
SSMSSYMSSKKTFEISPKSPIIKELKKRVDEGGAQDKTVKDLTKLLYETALLTSGFSLDE
PTSFASRINRLISLGLNIDEDEETETAPEASTAAPVEEVPADTEMEEVD
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BDBM50409989 |
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n/a |
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Name | BDBM50409989 |
Synonyms: | CHEMBL361941 |
Type | Small organic molecule |
Emp. Form. | C21H14ClFN2O2 |
Mol. Mass. | 380.799 |
SMILES | Oc1cc(O)c(cc1Cl)-c1n[nH]cc1-c1ccc(cc1)-c1ccc(F)cc1 |
Structure |
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