Ki Summary

Reaction Details

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Target

Heat shock protein HSP 90-beta

Ligand

BDBM20790

Substrate/Competitor

BDBM10852

Meas. Tech.

Her-2 Degradation Assay

7.2±n/a

Temperature

310.15±n/a K

EC50

70±n/a nM

Citation

Kasibhatla, SR; Hong, K; Biamonte, MA; Busch, DJ; Karjian, PL; Sensintaffar, JL; Kamal, A; Lough, RE; Brekken, J; Lundgren, K; Grecko, R; Timony, GA; Ran, Y; Mansfield, R; Fritz, LC; Ulm, E; Burrows, FJ; Boehm, MF Rationally designed high-affinity 2-amino-6-halopurine heat shock protein 90 inhibitors that exhibit potent antitumor activity. J Med Chem50:2767-78 (2007) [PubMed] Article

More Info.:

Get all data from this article, Solution Info, Assay Method

Heat shock protein HSP 90-beta

Name:

Heat shock protein HSP 90-beta

Synonyms:

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

BDBM20790

BDBM10852

Name

BDBM20790

Synonyms:

2-amino-6-halopurine analogue, 18b | 9-[(2-bromo-3,4,5-trimethoxyphenyl)methyl]-6-chloro-9H-purin-2-amine

Type

Small organic molecule

Emp. Form.

C15H15BrClN5O3

Mol. Mass.

428.668

SMILES

COc1cc(Cn2cnc3c(Cl)nc(N)nc23)c(Br)c(OC)c1OC

Structure