Reaction Details
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Heat shock protein HSP 90-beta
Ligand
BDBM20743
Substrate
BDBM10852
Meas. Tech.
Her-2 Degradation Assay
pH
7.2±n/a
Temperature
310.15±n/a K
EC50
5000±n/a nM
Citation
Biamonte, MA; Shi, J; Hong, K; Hurst, DC; Zhang, L; Fan, J; Busch, DJ; Karjian, PL; Maldonado, AA; Sensintaffar, JL; Yang, YC; Kamal, A; Lough, RE; Lundgren, K; Burrows, FJ; Timony, GA; Boehm, MF; Kasibhatla, SR Orally active purine-based inhibitors of the heat shock protein 90. J Med Chem 49:817-28 (2006) [PubMed] Article More Info.:
Target
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:
MPEEVHHGEEEVETFAFQAEIAQLMSLIINTFYSNKEIFLRELISNASDALDKIRYESLTDPSKLDSGKELKIDIIPNPQERTLTLVDTGIGMTKADLINNLGTIAKSGTKAFMEALQAGADISMIGQFGVGFYSAYLVAEKVVVITKHNDDEQYAWESSAGGSFTVRADHGEPIGRGTKVILHLKEDQTEYLEERRVKEVVKKHSQFIGYPITLYLEKEREKEISDDEAEEEKGEKEEEDKDDEEKPKIEDVGSDEEDDSGKDKKKKTKKIKEKYIDQEELNKTKPIWTRNPDDITQEEYGEFYKSLTNDWEDHLAVKHFSVEGQLEFRALLFIPRRAPFDLFENKKKKNNIKLYVRRVFIMDSCDELIPEYLNFIRGVVDSEDLPLNISREMLQQSKILKVIRKNIVKKCLELFSELAEDKENYKKFYEAFSKNLKLGIHEDSTNRRRLSELLRYHTSQSGDEMTSLSEYVSRMKETQKSIYYITGESKEQVANSAFVERVRKRGFEVVYMTEPIDEYCVQQLKEFDGKSLVSVTKEGLELPEDEEEKKKMEESKAKFENLCKLMKEILDKKVEKVTISNRLVSSPCCIVTSTYGWTANMERIMKAQALRDNSTMGYMMAKKHLEINPDHPIVETLRQKAEADKNDKAVKDLVVLLFETALLSSGFSLEDPQTHSNRIYRMIKLGLGIDEDEVAAEEPNAAVPDEIPPLEGDEDASRMEEVD
Inhibitor
Name:
BDBM20743
Synonyms:
8-benzyladenine analogue, 12d | 9-butyl-8-[(2-iodo-5-methoxyphenyl)methyl]-9H-purin-6-amine
Type:
Small organic molecule
Emp. Form.:
C17H20IN5O
Mol. Mass.:
437.2781
SMILES:
CCCCn1c(Cc2cc(OC)ccc2I)nc2c(N)ncnc12
Structure:
Substrate