PT2399

Antagonist of EPAS1

Structure

SERP Rating

In Cells

(1 ratings)

In Model Organisms

(1 ratings)

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Probe PT2399 is in the process of SERP review.

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Information

EPAS1

Antagonist

200 nM up to 2 uM

More...

Probe Availability:

In Vitro Validations

Uniprot ID: Q99814

Target Class: Transcription factor

Target SubClass: Hypoxia-Inducible Factor

Potency: IC50

Potency Value: < 5 nM

Potency Assay: Scintillation Proximity Assay (SPA)

PDB ID for probe-target interaction (3D structure): 5UFP

Structure-activity relationship: yes

Target aliases:

Endothelial PAS domain-containing protein 1, PASD2 ...

DOI Reference: 10.1021/acs.jmedchem.8b01196

Uniprot ID: Q99814

Target Class: Transcription factor

Target SubClass: Hypoxia-Inducible Factor

Potency: Kd

Potency Value: 42 nM

Potency Assay: Isothermal Calorimetry (ITC)

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

Target aliases:

Endothelial PAS domain-containing protein 1, PASD2 ...

DOI Reference: 10.1021/acs.jmedchem.8b01196

In Cell Validations

In Vivo Data

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SERP ratings and comments

SERP Ratings

In Cell Rating

In Model Organisms

SERP Comments:

Off-target activity is suggested based on the anti-proliferative activity in cells lacking HIF-2α. It would be helpful if an off-target (e.g. GPCR/kinase panel) was performed.

(last updated: 24 Sept 2020 )