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PT2399 | Antagonist of EPAS1
RATINGS:
Cellular Use: (1 reviews)

In Model Organisms: (1 reviews)
Probe Summary
Selectivity
Potency
In Vivo
Control Compounds
Chemical Information
References
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Probe Summary

Targets Biochemical/Biophysical Potency Cellular Potency
EPAS1
  • IC50:< 5 nM
  • Kd:42 nM
  • EC50:6 nM
  • EC50:14 nM
Antagonist
200 nM up to 2 uM

Selectivity

Potency
Cellular
In Vitro

EPAS1

Mode of Action: Antagonist

Structure-Activity-Relationship data available? No

DOI Reference: 10.1021/acs.jmedchem.8b01196

In Vivo Validations

Mouse, Rat
Dose: 10 mg/Kg PO, 3 mg/Kg IV
Route of delivery: Intravenous, Oral
Plasma half life: 7.3 (m) 2.9 (r) h
Systemic clearance: 34.3 (m) 57.6 (r) mL min–1 kg–1

DOI Reference: 10.1021/acs.jmedchem.8b01196

Orthogonal Probes def

PT2385

Chemical Information

Molecular Formula C17H10F5NO4S
SMILEs N#Cc1cc(F)cc(Oc2ccc(S(=O)(=O)C(F)F)c3c2CC(F)(F)[C@H]3O)c1
InChI InChI=1S/C17H10F5NO4S/c18-9-3-8(7-23)4-10(5-9)27-12-1-2-13(28(25,26)16(19)20)14-11(12)6-17(21,22)15(14)24/h1-5,15-16,24H,6H2/t15-/m0/s1
Molecular weight 419.03 Da
AlogP 3.7107800000000015
HBond acceptors 5
HBond donors 1
Atoms 38

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Expert Reviews

by SERP
(on 24 Sept 2020 )
Cellular Use Rating
In Model Organisms
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.
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