Onalespib

Inhibitor of HSP90AA1, HSP90AB1

Structure

SERP Rating

In Cells

(1 ratings)

In Model Organisms

(1 ratings)

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Probe Onalespib is in the process of SERP review.

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Information

HSP90AA1
HSP90AB1

Inhibitor

30 nM
Reviewer recommended concentration: 10 - 100 nM

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Probe Availability:

In Vitro Validations

Uniprot ID: P07900

Target Class: Other post-translational modification

Target SubClass: Chaperone

Potency: Kd

Potency Value: 0.71 nM

Potency Assay: ITC

PDB ID for probe-target interaction (3D structure): 2XJX

Structure-activity relationship: yes

Target aliases:

Heat shock protein HSP 90-alpha, HSPCA, HSPC1, HSP ...

DOI Reference: 10.1021/jm100060b

In Cell Validations

In Vivo Data

Off-Target Selectivity Assesments

Probe Selectivity in Vitro:

hERG inhibition 7% @ 3 uM, 42 % @ 30 uM, Clean profile against the major cytochrome P450 isoforms (≤40% inhibition at 10 μM for 1A2, 2D6, 3A4, 2C9, 2C19)

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SERP ratings and comments

SERP Ratings

In Cell Rating

In Model Organisms

SERP Comments:

Onalespib appears to be a selective HSP90 inhibitor with good pharmacological properties that permit in vivo dosing.

(last updated: 3 Jan 2022 )