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AZD9833 | AZD9833 : Degrader of ESR1
RATINGS:
Cellular Use: (0 reviews)

In Model Organisms: (0 reviews)
Probe Summary
Selectivity
Potency
In Vivo
Control Compounds
Chemical Information
References
Vendors
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Probe Summary

Targets Biochemical/Biophysical Potency Cellular Potency
ESR1
  • IC50:2.5 nM
  • pIC50, Dmax:9.8; 99 %
Degrader, Antagonist
10 nM

Selectivity

Potency
Cellular
In Vitro

ESR1

Mode of Action: Degrader, Antagonist

Structure-Activity-Relationship data available? No

DOI Reference: 10.1021/acs.jmedchem.0c01163

In Vivo Validations

Mouse, Rat
Dose: 2/5 IV/PO mg/Kg (M), 0.5/1 IV/PO mg/Kg (R)
Route of delivery: Intravenous, Oral
Plasma half life: 5.1 (M), 3.0 (R) h
Systemic clearance: 59 (M), 73 (R) mL/min/kg

DOI Reference: 10.1021/acs.jmedchem.0c01163

Chemical Information

Molecular Formula C24H28F4N6
SMILEs C[C@@H]1Cc2c(ccc3[nH]ncc23)[C@@H](c2ccc(NC3CN(CCCF)C3)cn2)N1CC(F)(F)F
InChI InChI=1S/C24H28F4N6/c1-15-9-19-18(4-6-21-20(19)11-30-32-21)23(34(15)14-24(26,27)28)22-5-3-16(10-29-22)31-17-12-33(13-17)8-2-7-25/h3-6,10-11,15,17,23,31H,2,7-9,12-14H2,1H3,(H,30,32)/t15-,23+/m1/s1
Molecular weight 476.23 Da
AlogP 0.0
HBond acceptors 6
HBond donors 2
Atoms 62

References

Publications

Cross References

canSARChEMBLBindingDB

Vendors

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Expert Reviews

No SERP comments found for AZD9833

Probe AZD9833 is in the process of SERP review.

Please continue to check back for new reviews and commentary.